5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS

US 20090203690A1
Filed: 12/04/2008
Published: 08/13/2009
Est. Priority Date: 06/08/2007
Status: Active Grant

First Claim

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1. A compound of formula (I)

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Abstract

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,

wherein A, R₁, R₂, R₃and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

186 Citations

163 Claims

1. A compound of formula (I)
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163)
- - 2. The compound according to claim 1, whereinA is (ii), (iii), (iv), (vii), (x), (xiv), (xv), (xvi), (xvii), (xviii), (xix), (xx), (xxi), (xxii), or (xxiii).
  - 3. The compound according to claim 2, wherein A is (ii)
  - 4. The compound according to claim 3, whereinR₁is hydrogen, heterocycle, R_aR_bN—
    - , or R_cR_dN—
      
      C(O)—
      
      ;
      
      R₂is hydrogen, alkoxycarbonyl or R_eR_fN-alkyl-C(O)—
      
      ;
      
      R₄is alkyl, alkoxyalkyl, aryl, cycloalkyl, heterocycle, heterocyclealkyl, R_jR_kN—
      
      or R_jR_kN-alkyl-;
      
      R₅is alkyl, aryl or heteroaryl;
      
      R_aand R_bare each independently hydrogen, arylalkyl, cycloalkylalkyl, R₄—
      
      C(O)—
      
      or R₅—
      
      S(O)₂—
      
      ;
      
      R_jand R_kare each independently hydrogen, alkyl, aryl cycloalkyl or heterocycle;
      
      R_iiis alkyl, alkoxyalkyl, alkoxycarbonylalkyl, aryl, arylalkyl, aryloxyalkyl, arylcarbonyl, arylthioalkyl, carboxy, carboxyalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylcarbonyl, halogen, heteroaryl, heteroarylalkyl, heterocyclealkyl, heterocyclecarbonyl, hydroxyalkyl, trialkylsilylalkyl, Z_aZ_bNalkyl-, or Z_cZ_dNC(O)—
      
      ;
      
      Z_aand Z_bare each independently hydrogen or alkyl;
      
      Z_cand Z_dare each independently hydrogen, alkyl, alkoxyalkyl, aryl, arylalkyl, cycloalkylalkyl or heterocyclealkyl;
      
      m is 0; and
      
      b is 0, 1 or 2.
  - 5. The compound according to claim 3, whereinR₁is hydrogen or R_aR_bN—
    - ;
      
      R₂is hydrogen;
      
      R₄is alkyl, alkoxyalkyl or aryl;
      
      R₅is alkyl or aryl;
      
      R_aand R_bare each independently hydrogen, arylalkyl, R₄—
      
      C(O)—
      
      or R₅—
      
      S(O)₂—
      
      ;
      
      R_iiis alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl or halogen;
      
      b is 1 or 2; and
      
      m is 0.
  - 6. The compound according to claim 3, whereinR₁is hydrogen, aryl, heteroaryl or R_aR_bN—
    - , wherein the heteroaryl is triazole substituted with arylalkyl;
      
      R₄is alkoxyalkyl, alkyl, aryl, or R_jR_kN—
      
      ;
      
      R₅is alkyl, aryl, or heteroaryl;
      
      R_aand R_bare each independently hydrogen, arylalkyl, R₄—
      
      C(O)—
      
      , or R₅—
      
      S(O)₂—
      
      ;
      
      R_jand R_kare alkyl;
      
      R_iiis alkyl, alkoxyalkyl, aryl, arylalkyl, aryl(hydroxy)alkyl, aryloxyalkyl, arylcarbonyl, arylthioalkyl, carboxy, cycloalkyl, cycloalkylalkyl, cycloalkylcarbonyl, halogen, heteroaryl, heteroarylalkyl, heterocyclealkyl, heterocyclecarbonyl, hydroxyalkyl, Z_aZ_bNalkyl or Z_cZ_dNC(O)—
      
      ;
      
      Z_aand Z_bare each independently hydrogen or H₂Nalkyl-C(O)—
      
      ;
      
      Z_cand Z_dare each independently hydrogen, alkoxyalkyl, alkyl, arylalkyl, cycloalkyl, cycloalkylalkyl, or heterocyclealkyl;
      
      b is 1 or 2; and
      
      m is 0.
  - 7. The compound according to claim 3, whereinR₁is hydrogen, alkoxycarbonyl, alkyl, aryl, heteroaryl, heterocycle, R_aR_bN—
    - , or R_cR_dN—
      
      C(O)—
      
      ;
      
      R₂is hydrogen, heterocyclecarbonyl, or arylcarbonyl;
      
      R₄is alkyl, alkoxyalkyl, aryl, heterocyclealkyl, R_jR_kN—
      
      or R_jR_kN-alkyl-;
      
      R₅is alkyl, or aryl;
      
      R_aand R_bare each independently hydrogen, alkyl, arylalkyl, cycloalkylalkyl, heterocyclealkyl, R₄—
      
      C(O)—
      
      or R₅—
      
      S(O)₂—
      
      ;
      
      R_c, and R_dare each independently alkyl;
      
      R_jand R_kare each independently hydrogen, alkyl, aryl, arylalkyl, or cycloalkyl;
      
      R_iiis alkyl, aryl, arylalkyl, arylcarbonyl, cycloalkyl, cycloalkylalkyl, halogen, heteroaryl, heterocyclealkyl, heterocyclecarbonyl, or Z_cZ_dNC(O)—
      
      ;
      
      Z_cand Z_dare each independently hydrogen, alkyl, alkoxyalkyl, aryl;
      
      m is 0; and
      
      b is 1 or 2.
  - 8. The compound according to claim 2, wherein A is (iii)
  - 9. The compound according to claim 2, wherein A is (iii)
  - 10. The compound according to claim 2, wherein A is (iv)
  - 11. The compound according to claim 2, wherein A is (vii)
  - 12. The compound according to claim 2, wherein A is (vii)
  - 13. The compound according to claim 2, wherein A is (vii)
  - 14. The compound according to claim 2, wherein A is (x)
  - 15. The compound according to claim 2, wherein A is (xiv)
  - 16. The compound according to claim 2, wherein A is (xv)
  - 17. The compound according to claim 2, wherein A is (xvi)
  - 18. The compound according to claim 2, wherein A is (xvii)
  - 19. The compound according to claim 2, wherein A is (xviii)
  - 20. The compound according to claim 2, wherein A is (xix)
  - 21. The compound according to claim 2, wherein A is (xx)
  - 22. The compound according to claim 2, wherein A is (xxi)
  - 23. The compound according to claim 2, wherein A is (xxii)
  - 24. The compound according to claim 2, wherein A is (xxiii)
  - 25. The compound of claim 1, that is5-(1-benzyl-1H-1,2,3-triazol-5-yl)-1H-indazole compound with 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazole;
    - 5-(1H-1,2,3-triazol-5-yl)-1H-indazole;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazole;
      
      5-[1-(2-methylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3-methylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(4-methylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3-methoxybenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2-fluorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3-fluorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(4-fluorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2-chlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3-chlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(4-chlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2-bromobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2-nitrobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3-nitrobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      2-{[4-(1H-indazol-5-yl)-1H-1,2,3-triazol-1-yl]methyl}benzonitrile;
      
      3-{[4-(1H-indazol-5-yl)-1H-1,2,3-triazol-1-yl]methyl}benzonitrile;
      
      4-{[4-(1H-indazol-5-yl)-1H-1,2,3-triazol-1-yl]methyl}benzonitrile;
      
      5-{1-[2-(trifluoromethyl)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-{1-[3-(trifluoromethyl)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-{1-[4-(trifluoromethyl)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-{1-[3-(trifluoromethoxy)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-{1-[4-(trifluoromethoxy)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-[1-(4-tert-butylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      methyl 3-{[4-(1H-indazol-5-yl)-1H-1,2,3-triazol-1-yl]methyl}benzoate;
      
      methyl 4-{[4-(1H-indazol-5-yl)-1H-1,2,3-triazol-1-yl]methyl}benzoate;
      
      5-[1-(2,4-dimethylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3,5-dimethylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2,3-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2,4-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(2,5-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-(3,5-dichlorobenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-{1-[2,4-bis(trifluoromethyl)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      N-cyclohexyl-6-(1H-indazol-5-yl)imidazo[2,1-b][1,3]thiazol-5-amine;
      
      N-cyclohexyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-amine;
      
      N-cyclohexyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrazin-3-amine;
      
      5-[1-benzyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-1H-indazole;
      
      N-{3-[4-(4-fluorophenyl)-5-(1H-indazol-5-yl)-1H-imidazol-1-yl]propyl}-N,N-dimethylamine;
      
      N-cyclohexyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;
      
      5-[4-(4-fluorophenyl)-1-(1-phenylethyl)-1H-imidazol-5-yl]-1H-indazole;
      
      2-(1H-indazol-5-yl)-N-isopropylimidazo[1,2-a]pyrimidin-3-amine;
      
      4-(1H-indazol-5-yl)-N-phenyl-1,3-thiazol-2-amine;
      
      5-(2-methyl-1,3-thiazol-4-yl)-1H-indazole;
      
      N-ethyl-4-(1H-indazol-5-yl)-1,3-thiazol-2-amine;
      
      N-benzyl-4-(1H-indazol-5-yl)-1,3-thiazol-2-amine;
      
      4-(1H-indazol-5-yl)-1,3-thiazol-2-amine;
      
      4-(1H-indazol-5-yl)-N-(2-phenylethyl)-1,3-thiazol-2-amine;
      
      N-benzyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;
      
      N-butyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;
      
      N-(4-chlorophenyl)-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;
      
      2-(1H-indazol-5-yl)-N-(4-methoxyphenyl)imidazo[1,2-a]pyrimidin-3-amine;
      
      2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidine;
      
      methyl N-[2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-yl]glycinate;
      
      N-benzyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-amine;
      
      N-(4-chlorophenyl)-2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-amine;
      
      2-(1H-indazol-5-yl)-N-(4-methoxyphenyl)imidazo[1,2-a]pyridin-3-amine;
      
      tert-butyl 4-[4-(4-fluorophenyl)-5-(1H-indazol-5-yl)-1H-imidazol-1-yl]piperidine-1-carboxylate;
      
      3,5-bis(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazole;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-phenyl-1H-indazole;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1-[(1-methylpiperidin-4-yl)carbonyl]-1H-indazol-3-amine;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-methoxyacetamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²,N²-dimethylglycinamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]butanamide;
      
      5-[4-(4-fluorophenyl)-1-piperidin-4-yl-1H-imidazol-5-yl]-1H-indazole;
      
      5-{4-(4-fluorophenyl)-1-[2-(1-methylpyrrolidin-2-yl)ethyl]-1H-imidazol-5-yl}-1H-indazole;
      
      5-{4-(4-fluorophenyl)-1-[3-(4-methylpiperazin-1-yl)propyl]-1H-imidazol-5-yl}-1H-indazole;
      
      ethyl 5-(1H-indazol-5-yl)isoxazole-3-carboxylate;
      
      5-(1H-indazol-5-yl)-N-methylisoxazole-3-carboxamide;
      
      5-(3-benzylisoxazol-5-yl)-1H-indazole;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzamide;
      
      5-(3-propylisoxazol-5-yl)-1H-indazole;
      
      N-benzyl-4-(1H-indazol-5-yl)-5-phenyl-1,3-thiazol-2-amine;
      
      4-(1H-indazol-5-yl)-N,5-diphenyl-1,3-thiazol-2-amine;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazole;
      
      5-(1-benzyl-4-cyclopropyl-1H-1,2,3-triazol-5-yl)-1H-indazole;
      
      2-(1H-indazol-5-yl)-3-phenylimidazo[1,2-a]pyrimidine;
      
      5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[3-(piperidin-1-ylcarbonyl)isoxazol-5-yl]-1H-indazole;
      
      5-(1H-indazol-5-yl)-N-phenylisoxazole-3-carboxamide;
      
      N-cyclohexyl-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-[3-(piperidin-1-ylmethyl)isoxazol-5-yl]-1H-indazole;
      
      [5-(1H-indazol-5-yl)isoxazol-3-yl]methanol;
      
      5-(1H-indazol-5-yl)-N-(2-methoxyethyl)isoxazole-3-carboxamide;
      
      5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazole;
      
      5-(4-benzyl-1H-1,2,3-triazol-1-yl)-1H-indazole;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      5-(1-benzyl-4-cyclopropyl-1H-1,2,3-triazol-5-yl)-1H-indazol-3-amine;
      
      5-(3-isobutylisoxazol-5-yl)-1H-indazol-3-amine;
      
      5-(3-benzylisoxazol-5-yl)-1H-indazol-3-amine;
      
      N-{2-[4-(4-fluorophenyl)-5-(1H-indazol-5-yl)-1H-imidazol-1-yl]ethyl}-N,N-dimethylamine;
      
      5-[4-(4-fluorophenyl)-1-(3-morpholin-4-ylpropyl)-1H-imidazol-5-yl]-1H-indazole;
      
      5-[4-(4-fluorophenyl)-1-(3-pyrrolidin-1-ylpropyl)-1H-imidazol-5-yl]-1H-indazole;
      
      5-{4-(4-fluorophenyl)-1-[2-(4-methylpiperidin-1-yl)ethyl]-1H-imidazol-5-yl}-1H-indazole;
      
      5-[1-(1-benzylpiperidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-1H-indazole;
      
      5-[4-(4-fluorophenyl)-1-(2-morpholin-4-ylethyl)-1H-imidazol-5-yl]-1H-indazole;
      
      5-[1-(1-benzylpyrrolidin-3-yl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-1H-indazole;
      
      2-{4-[4-(4-fluorophenyl)-5-(1H-indazol-5-yl)-1H-imidazol-1-yl]piperidin-1-yl}-2-oxoethanol;
      
      5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      2-[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]propan-2-ol;
      
      5-[4-(methoxymethyl)-1H-1,2,3-triazol-1-yl]-1H-indazole;
      
      1-[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]-1-phenylethanol;
      
      5-(4-propyl-1H-1,2,3-triazol-1-yl)-1H-indazole;
      
      1-[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]propan-2-ol;
      
      3-[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]propan-1-ol;
      
      1-{[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]methyl}-1H-1,2,3-benzotriazole;
      
      5-{4-[(phenylthio)methyl]-1H-1,2,3-triazol-1-yl}-1H-indazole;
      
      5-(4-cyclopropyl-1H-1,2,3-triazol-1-yl)-1H-indazole;
      
      5-[4-(2-phenylethyl)-1H-1,2,3-triazol-1-yl]-1H-indazole;
      
      5-[4-(cyclohexylmethyl)-1H-1,2,3-triazol-1-yl]-1H-indazole;
      
      5-(4-cyclopentyl-1H-1,2,3-triazol-1-yl)-1H-indazole;
      
      1-[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]cyclohexanol;
      
      5-[4-(phenoxymethyl)-1H-1,2,3-triazol-1-yl]-1H-indazole;
      
      5-{4-[(1,1-dioxidothiomorpholin-4-yl)methyl]-1H-1,2,3-triazol-1-yl}-1H-indazole;
      
      5-[4-(3-phenylpropyl)-1H-1,2,3-triazol-1-yl]-1H-indazole;
      
      [1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl](phenyl)methanone;
      
      N,N-diethyl-N-{[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]methyl}amine;
      
      ethyl N-[2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-yl]-beta-alaninate;
      
      5-(1-benzyl-5-methyl-1H-1,2,3-triazol-4-yl)-1H-indazole;
      
      5-(1-benzyl-5-methyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      N³-[2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-yl]-β
      
      -alaninamide;
      
      5-(1-benzyl-5-iodo-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      N-{3-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]phenyl}-N′
      
      -(3-methylphenyl)urea;
      
      5-(1H-indazol-5-yl)-N-(2-isopropoxyethyl)isoxazole-3-carboxamide;
      
      5-[3-(morpholin-4-ylcarbonyl)isoxazol-5-yl]-1H-indazole;
      
      5-(1H-indazol-5-yl)-N-(3-morpholin-4-ylpropyl)isoxazole-3-carboxamide;
      
      N-[2-(1H-imidazol-4-yl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      (3R)-1-{[5-(1H-indazol-5-yl)isoxazol-3-yl]carbonyl}piperidin-3-ol;
      
      1-{[5-(1H-indazol-5-yl)isoxazol-3-yl]carbonyl}piperidine-3-carboxamide;
      
      2-[2-(4-{[5-(1H-indazol-5-yl)isoxazol-3-yl]carbonyl}piperazin-1-yl)ethoxy]ethanol;
      
      5-{3-[(4-methyl-1,4-diazepan-1-yl)carbonyl]isoxazol-5-yl}-1H-indazole;
      
      N-(3-hydroxypropyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1R)-2-hydroxy-1-phenylethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[3-(1H-imidazol-1-yl)propyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[3-(2-oxopyrrolidin-1-yl)propyl]isoxazole-3-carboxamide;
      
      N-{2-[4-(aminosulfonyl)phenyl]ethyl}-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      [1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl](3-chlorophenyl)methanone;
      
      [1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl](cyclopropyl)methanone;
      
      5-[5-cyclopropyl-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      N¹-{[1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl]methyl}glycinamide;
      
      (4-fluorophenyl)[4-(1H-indazol-5-yl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-5-yl]methanone;
      
      (4-chlorophenyl)[4-(1H-indazol-5-yl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-5-yl]methanone;
      
      (3-chlorophenyl)[4-(1H-indazol-5-yl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-5-yl]methanone;
      
      (2-chlorophenyl)[4-(1H-indazol-5-yl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-5-yl]methanone;
      
      cyclopentyl[4-(1H-indazol-5-yl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-5-yl]methanone;
      
      1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxylic acid;
      
      5-{5-(4-fluorophenyl)-1-[4-(trifluoromethyl)benzyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      [4-(1H-indazol-5-yl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-5-yl](tetrahydro-2H-pyran-4-yl)methanone;
      
      5-[1-benzyl-5-(2-methylphenyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-{1-benzyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      1-{[1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl]carbonyl}piperidin-4-ol;
      
      1-acetyl-5-[5-(4-fluorophenyl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      1-benzyl-4-(1H-indazol-5-yl)-N,N-dimethyl-1H-1,2,3-triazole-5-carboxamide;
      
      N,1-dibenzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      N-(2-hydroxy-2-phenylethyl)-5-(1H-indazol-5-yl)-N-methylisoxazole-3-carboxamide;
      
      N-[(1S)-2-hydroxy-1-phenylethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-benzyl-N-(2-hydroxyethyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-[1-benzyl-5-(2-methylphenyl)-1H-1,2,3-triazol-4-yl]-3-methyl-1H-indazole;
      
      5-[1-benzyl-5-(2-methylphenyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      2-{2-[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]ethyl}-1H-isoindole-1,3(2H)-dione;
      
      5-{4-[(2,4-dichlorophenoxy)methyl]-1H-1,2,3-triazol-1-yl}-1H-indazole;
      
      5-{4-[(2,6-dichlorophenoxy)methyl]-1H-1,2,3-triazol-1-yl}-1H-indazole;
      
      5-[5-(4-fluorophenyl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      1-{[1-(1H-indazol-5-yl)-1H-1,2,3-triazol-4-yl]methyl}-1H-indazole;
      
      5-[1-benzyl-5-(piperidin-1-ylcarbonyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[5-(2-methylphenyl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[5-(2-methylphenyl)-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(morpholin-4-ylcarbonyl)-1H-1,2,3-triazol-4-yl]-1H-indazole;
      
      5-[1-benzyl-5-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      N-[(1S)-1-benzyl-2-hydroxyethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-{3-[(3-phenylmorpholin-4-yl)carbonyl]isoxazol-5-yl}-1H-indazole;
      
      N-benzyl-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      ((1S)-2-{[5-(1H-indazol-5-yl)isoxazol-3-yl]carbonyl}-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl)methanol;
      
      N-[(1R)-3-hydroxy-1-phenylpropyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1S)-3-hydroxy-1-phenylpropyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-2,3-dihydro-1H-inden-1-yl-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-2,3-dihydro-1H-inden-2-yl-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(1-phenylpropyl)isoxazole-3-carboxamide;
      
      5-{1-benzyl-5-[3-(dimethylamino)phenyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-amine;
      
      5-{1-benzyl-5-[4-(dimethylamino)phenyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-amine;
      
      N-{3-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]phenyl}acetamide;
      
      N-{4-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]phenyl}acetamide;
      
      5-{1-benzyl-5-[3-(1H-pyrazol-1-yl)phenyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(1-methyl-1H-pyrazol-4-yl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      3-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]-N-phenylbenzamide;
      
      3-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]-N-benzylbenzamide;
      
      5-[1-benzyl-5-(1-methyl-1H-indol-5-yl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(3-methoxyphenyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(3-morpholin-4-ylphenyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      5-[3-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)isoxazol-5-yl]-1H-indazole;
      
      5-{3-[(4-methyl-2-phenylpiperazin-1-yl)carbonyl]isoxazol-5-yl}-1H-indazole;
      
      1-{[1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl]carbonyl}piperidin-4-amine;
      
      N-[5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzamide;
      
      N-[5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzenesulfonamide;
      
      N-[5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -(4-methoxyphenyl)urea;
      
      N-[5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]butanamide;
      
      N-[5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-methylpropanamide;
      
      N-[5-(1-benzyl-5-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]cyclopropanecarboxamide;
      
      N-[1-benzoyl-5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-3-fluorobenzamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzamide;
      
      N-benzyl-5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      N-[(1R)-1-benzyl-2-hydroxyethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1-benzyl-1H-pyrazol-4-yl)-1H-indazole;
      
      N-[(1R)-3-hydroxy-1-phenylpropyl]-5-(3-methyl-1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      3-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]phenol;
      
      3-[4-(3-amino-1H-indazol-5-yl)-1-benzyl-1H-1,2,3-triazol-5-yl]benzamide;
      
      5-{1-benzyl-5-[4-(methylsulfonyl)phenyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-amine;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-chlorobenzamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-4-chlorobenzamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]ethanesulfonamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzenesulfonamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-chlorobenzenesulfonamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-3-chlorobenzenesulfonamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-4-chlorobenzenesulfonamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2,5-dimethylfuran-3-sulfonamide;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-N-(2-chlorobenzyl)-1H-indazol-3-amine;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-N-(3-chlorobenzyl)-1H-indazol-3-amine;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-3-chlorobenzamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-furamide;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-N-ethyl-1H-indazol-3-amine;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-N-(4-chlorobenzyl)-1H-indazol-3-amine;
      
      5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-N-(3-furylmethyl)-1H-indazol-3-amine;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -[5-methyl-2-(trifluoromethyl)-3-furyl]urea;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-3-furamide;
      
      5-(1H-indazol-5-yl)-N-[(1S)-1-phenylpropyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1R)-1-phenylpropyl]isoxazole-3-carboxamide;
      
      5-(1-benzyl-1H-pyrazol-4-yl)-1H-indazol-3-amine;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-(2-isopropoxyethyl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-(tetrahydrofuran-3-ylmethyl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-cyclopentyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-(cyclopentylmethyl)-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-ethyl-4-(1H-indazol-5-yl)-N-methyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-isopropyl-N-methyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-(2-methoxyethyl)-N-methyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-phenyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-(4-chlorophenyl)-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-4-(1H-indazol-5-yl)-N-(2-morpholin-4-ylethyl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-[2-(dimethylamino)ethyl]-4-(1H-indazol-5-yl)-N-methyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-(2-hydroxyethyl)-4-(1H-indazol-5-yl)-N-propyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-[3-(dimethylamino)propyl]-4-(1H-indazol-5-yl)-N-methyl-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-[2-(diethylamino)ethyl]-4-(1H-indazol-5-yl)-N-methyl-1H-1,2,3-triazole-5-carboxamide;
      
      N,1-dibenzyl-N-ethyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      N,1-dibenzyl-N-(2-hydroxyethyl)-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      (3R)-1-{[1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl]carbonyl}piperidin-3-ol;
      
      1-{[1-benzyl-4-(1H-indazol-5-yl)-1H-1,2,3-triazol-5-yl]carbonyl}piperidine-4-carboxamide;
      
      5-{1-benzyl-5-[(2,6-dimethylmorpholin-4-yl)carbonyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-{5-[(4-acetylpiperazin-1-yl)carbonyl]-1-benzyl-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      5-{1-benzyl-5-[(4-phenylpiperazin-1-yl)carbonyl]-1H-1,2,3-triazol-4-yl}-1H-indazole;
      
      1-benzyl-N-[(1R)-1-(hydroxymethyl)-2-methylpropyl]-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-[(1S)-1-(hydroxymethyl)-2-methylpropyl]-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      1-benzyl-N-[3-(1H-imidazol-1-yl)propyl]-4-(1H-indazol-5-yl)-1H-1,2,3-triazole-5-carboxamide;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -ethylurea;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -phenylurea;
      
      N-benzyl-N¹-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]urea;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -(2-chlorophenyl)urea;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -(3-chlorophenyl)urea;
      
      N-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -(4-chlorophenyl)urea;
      
      N-[5-(1-benzyl-5-iodo-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]benzamide;
      
      3-[4-(3-amino-1H-indazol-5-yl)-1H-pyrazol-1-yl]propanenitrile;
      
      2-[4-(3-amino-1H-indazol-5-yl)-1H-pyrazol-1-yl]acetamide;
      
      methyl 3-[4-(3-amino-1H-indazol-5-yl)-1H-pyrazol-1-yl]propanoate;
      
      3-[4-(3-amino-1H-indazol-5-yl)-1H-pyrazol-1-yl]propanamide;
      
      [4-(3-amino-1H-indazol-5-yl)-1H-pyrazol-1-yl]acetonitrile;
      
      4-(3-amino-1H-indazol-5-yl)-N,N-dimethyl-1H-imidazole-1-sulfonamide;
      
      5-pyrazin-2-yl-1H-indazol-3-amine;
      
      5-thien-2-yl-1H-indazol-3-amine;
      
      5-(2-aminopyrimidin-4-yl)-1H-indazol-3-amine;
      
      5-(2-methoxypyridin-3-yl)-1H-indazol-3-amine;
      
      5-imidazo[1,2-a]pyridin-3-yl-1H-indazol-3-amine;
      
      N²,N²-dimethyl-N¹-[5-(1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]glycinamide;
      
      5-(1H-pyrazol-5-yl)-1H-indazol-3-amine;
      
      5-(4-methyl-1H-imidazol-5-yl)-1H-indazol-3-amine;
      
      5-(1H-imidazol-4-yl)-1H-indazol-3-amine;
      
      N²,N²-dimethyl-N¹-{5-[1-(3-methylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-yl}glycinamide;
      
      5-(1-benzyl-1H-imidazol-4-yl)-1H-indazol-3-amine;
      
      N¹-{5-[1-(4-tert-butylbenzyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-yl}-N²,N²-dimethylglycinamide;
      
      N²,N²-dimethyl-N¹-{5-[1-(2-piperidin-1-ylethyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-yl}glycinamide;
      
      N²,N²-dimethyl-N¹-{5-[1-(2-morpholin-4-ylethyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-yl}glycinamide;
      
      N¹-(5-{1-[2-(3,5-dimethylisoxazol-4-yl)ethyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-yl)-N²,N²-dimethylglycinamide;
      
      N¹-(5-{1-[2-(3,5-dimethyl-1H-pyrazol-4-yl)ethyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-yl)-N²,N²-dimethylglycinamide;
      
      2-(4-{3-[(N,N-dimethylglycyl)amino]-1H-indazol-5-yl}-1H-1,2,3-triazol-1-yl)-2-methylpropanoic acid;
      
      ethyl (4-{3-[(N,N-dimethylglycyl)amino]-1H-indazol-5-yl}-1H-1,2,3-triazol-1-yl)acetate;
      
      N²,N²-dimethyl-N¹-(5-{1-[(trimethylsilyl)methyl]-1H-1,2,3-triazol-4-yl}-1H-indazol-3-yl)glycinamide;
      
      N¹-[5-(3-furyl)-1H-indazol-3-yl]-N²,N²-dimethylglycinamide;
      
      N²,N²-dimethyl-N¹-[5-(1H-pyrazol-5-yl)-1H-indazol-3-yl]glycinamide;
      
      N²,N²-dimethyl-N¹-(5-pyrimidin-5-yl-1H-indazol-3-yl)glycinamide;
      
      N¹-[5-(2,1,3-benzoxadiazol-5-yl)-1H-indazol-3-yl]-N²,N²-dimethylglycinamide;
      
      N²,N²-dimethyl-N¹-[5-(1H-pyrazol-4-yl)-1H-indazol-3-yl]glycinamide;
      
      N²,N²-dimethyl-N¹-[5-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-3-yl]glycinamide;
      
      N¹-[5-(3,5-dimethyl-1H-pyrazol-4-yl)-1H-indazol-3-yl]-N²,N²-dimethylglycinamide;
      
      N¹-{5-[2-(dimethylamino)pyrimidin-5-yl]-1H-indazol-3-yl}-N²,N²-dimethylglycinamide;
      
      N²,N²-dimethyl-N¹-[5-(2-morpholin-4-ylpyrimidin-5-yl)-1H-indazol-3-yl]glycinamide;
      
      N²,N²-dimethyl-N¹-{5-[1-(2-morpholin-4-ylethyl)-1H-pyrazol-4-yl]-1H-indazol-3-yl}glycinamide;
      
      N¹-[5-(1-benzyl-5-cyclopropyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²,N²-dimethylglycinamide;
      
      N¹-[5-(1-benzyl-1H-pyrazol-4-yl)-1H-indazol-3-yl]-N²,N²-dimethylglycinamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-methylglycinamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-pyrrolidin-1-ylacetamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-cyclopentylglycinamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-cyclopropylglycinamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-tetrahydro-2H-pyran-4-ylglycinamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-(3-hydroxypyrrolidin-1-yl)acetamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-(3-hydroxypiperidin-1-yl)acetamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N³,N³-dimethyl-beta-alaninamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-morpholin-4-ylacetamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-(4-methylpiperazin-1-yl)acetamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-(3-oxopiperazin-1-yl)acetamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-isopropylglycinamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-cyclohexylglycinamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]acetamide;
      
      N¹-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N²-cyclobutylglycinamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -propylurea;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]ethanesulfonamide;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(cyclopropylmethyl)-1H-indazol-3-amine;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-N′
      
      -ethylurea;
      
      1-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]pyrrolidin-2-one;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-4-(dimethylamino)butanamide;
      
      N-3,4-dihydro-1H-isochromen-4-yl-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-(cyclohexylmethyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-(3-chlorobenzyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(2-methoxybenzyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[4-(trifluoromethyl)benzyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(pyridin-2-ylmethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(pyridin-4-ylmethyl)isoxazole-3-carboxamide;
      
      N-(2-chlorobenzyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-(4-chlorobenzyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(1-phenyl-2-piperidin-1-ylethyl)isoxazole-3-carboxamide;
      
      N-[2-(1H-imidazol-1-yl)-1-phenylethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(2-morpholin-4-yl-1-phenylethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[2-(4-methylpiperazin-1-yl)-1-phenylethyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(1-phenyl-2-pyrrolidin-1-ylethyl)isoxazole-3-carboxamide;
      
      tert-butyl 2-({[5-(1H-indazol-5-yl)isoxazol-3-yl]carbonyl}amino)-2-phenylethylcarbamate;
      
      5-(1H-indazol-5-yl)-N-(1-naphthylmethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(2-phenylethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(2-pyridin-2-ylethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(2-pyridin-3-ylethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-(2-pyridin-4-ylethyl)isoxazole-3-carboxamide;
      
      N-[2-(2-chlorophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[2-(3-chlorophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[2-(4-chlorophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-benzyl-N-ethyl-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-methyl-N-(1-naphthylmethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-methyl-N-(2-phenylethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-methyl-N-(2-pyridin-2-ylethyl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1R)-1-phenylethyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1S)-1-(1-naphthyl)ethyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1R)-1-(1-naphthyl)ethyl]isoxazole-3-carboxamide;
      
      N-[3-(dimethylamino)-1-phenylpropyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-(3,4-dihydro-2H-1,5-benzodioxepin-6-ylmethyl)-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1-methyl-1H-indol-4-yl)methyl]isoxazole-3-carboxamide;
      
      5-{3-[(3-phenylpyrrolidin-1-yl)carbonyl]isoxazol-5-yl}-1H-indazole;
      
      5-{3-[(2-phenylpyrrolidin-1-yl)carbonyl]isoxazol-5-yl}-1H-indazole;
      
      5-{3-[(2-phenylpiperidin-1-yl)carbonyl]isoxazol-5-yl}-1H-indazole;
      
      5-(1H-indazol-5-yl)-N-[(1S)-1-phenylethyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1R)-1-(4-methylphenyl)ethyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1S)-1-(4-methylphenyl)ethyl]isoxazole-3-carboxamide;
      
      N-[(1R,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1R,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1R)-1-(4-bromophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1S)-1-(4-bromophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1R)-1-(4-chlorophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[(1S)-1-(4-chlorophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1S)-1-(2-naphthyl)ethyl]isoxazole-3-carboxamide;
      
      N-[1-(4-ethoxyphenyl)-2-hydroxyethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[2-hydroxy-1-(4-isopropylphenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[1-(3,4-dimethylphenyl)-2-hydroxyethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[2-hydroxy-1-(2-methoxyphenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[2-hydroxy-1-(4-methylphenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1R)-1-(2-methoxyphenyl)ethyl]isoxazole-3-carboxamide;
      
      N-[(1S)-1-(3,4-difluorophenyl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]isoxazole-3-carboxamide;
      
      5-(1H-indazol-5-yl)-N-{(1R)-1-[3-(trifluoromethyl)phenyl]ethyl} isoxazole-3-carboxamide;
      
      N-[1-(2,3-dihydro-1,4-benzodioxin-6-yl)ethyl]-5-(1H-indazol-5-yl)isoxazole-3-carboxamide;
      
      N-[1-(3,5-dichlorophenyl)-2-hydroxyethyl]-5-(H-indazol-5-yl)isoxazole-3-carboxamide;
      
      tert-butyl 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-[({[6-(trifluoromethyl)pyridin-2-yl]amino}carbonyl)amino]-1H-indazole-1-carboxylate;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1-[(1-methylpiperidin-2-yl)carbonyl]-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1-[(dimethylamino)acetyl]-1H-indazol-3-amine;
      
      tert-butyl 3-amino-5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazole-1-carboxylate;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-piperidin-1-ylacetamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-2-morpholin-4-ylacetamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-1-methylpiperidine-2-carboxamide;
      
      2-(1H-indazol-5-yl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]-1,3-thiazole-5-carboxamide;
      
      N-[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]-3-fluorobenzamide;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N,N-dimethyl-1H-indazole-3-carboxamide;
      
      methyl 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazole-3-carboxylate;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(1-methyl-1H-imidazol-2-yl)-1H-indazole;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-morpholin-4-yl-1H-indazole;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(4-methylpiperazin-1-yl)-1H-indazole;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-thien-2-yl-1H-indazole;
      
      5-(1-benzyl-5-cyclohexyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(cyclohexylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(1,3-thiazol-2-yl)-1H-indazole;
      
      5-(1,5-dibenzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      5-(1-benzyl-5-thien-2-yl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(2-morpholin-4-ylethyl)-1H-indazol-3-amine;
      
      5-[1-benzyl-5-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-3-methyl-1H-indazole;
      
      5-[1-benzyl-5-(cyclopentylmethyl)-1H-1,2,3-triazol-4-yl]-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-butyl-1H-indazol-3-amine;
      
      N-benzyl-5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(4-chlorobenzyl)-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(4-methoxybenzyl)-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(3-fluorobenzyl)-1H-indazol-3-amine;
      
      4-({[5-(1-benzyl-1H-1,2,3-triazol-4-yl)-1H-indazol-3-yl]amino}methyl)benzonitrile;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(2,4-difluorobenzyl)-1H-indazol-3-amine;
      
      5-(1-benzyl-1H-1,2,3-triazol-4-yl)-N-(cyclohexylmethyl)-1H-indazol-3-amine;
      
      or5-(1-phenyl-1H-1,2,3-triazol-4-yl)-1H-indazole.
  - 26. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) according to claim 1, in combination with a pharmaceutically suitable carrier.
  - 27. A method of inhibiting Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2 comprising administering a therapeutically effective amount of a compound of Formula (I) according to claim 1.
  - 28. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 4, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 29. The method according to claim 28, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 30. The method accord to claim 29, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 31. The method according to claim 30, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 32. The method according to claim 29, wherein the dementia is vascular dementia.
  - 33. The method according to claim 29, wherein the cerebrovascular accident is age related macular degeneration.
  - 34. The method according to claim 28, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 35. The method according to claim 34, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 36. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 9, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 37. The method according to claim 36, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 38. The method accord to claim 37, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 39. The method according to claim 38, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 40. The method according to claim 37, wherein the dementia is vascular dementia.
  - 41. The method according to claim 37, wherein the cerebrovascular accident is age related macular degeneration.
  - 42. The method according to claim 36, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 43. The method according to claim 42, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 44. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 10, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 45. The method according to claim 44, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 46. The method accord to claim 45, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 47. The method according to claim 46, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 48. The method according to claim 45, wherein the dementia is vascular dementia.
  - 49. The method according to claim 45, wherein the cerebrovascular accident is age related macular degeneration.
  - 50. The method according to claim 44, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 51. The method according to claim 50, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 52. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 12, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 53. The method according to claim 52, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 54. The method accord to claim 53, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 55. The method according to claim 54, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 56. The method according to claim 53, wherein the dementia is vascular dementia.
  - 57. The method according to claim 53, wherein the cerebrovascular accident is age related macular degeneration.
  - 58. The method according to claim 52, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 59. The method according to claim 58, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 60. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 15, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 61. The method according to claim 60, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 62. The method accord to claim 61, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 63. The method according to claim 62, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 64. The method according to claim 61, wherein the dementia is vascular dementia.
  - 65. The method according to claim 61, wherein the cerebrovascular accident is age related macular degeneration.
  - 66. The method according to claim 60, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 67. The method according to claim 66, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 68. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 16, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 69. The method according to claim 68, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 70. The method accord to claim 69, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 71. The method according to claim 70, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 72. The method according to claim 69, wherein the dementia is vascular dementia.
  - 73. The method according to claim 69, wherein the cerebrovascular accident is age related macular degeneration.
  - 74. The method according to claim 68, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 75. The method according to claim 74, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 76. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 17, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 77. The method according to claim 76, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 78. The method accord to claim 77, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 79. The method according to claim 78, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 80. The method according to claim 77, wherein the dementia is vascular dementia.
  - 81. The method according to claim 77, wherein the cerebrovascular accident is age related macular degeneration.
  - 82. The method according to claim 76, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 83. The method according to claim 82, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 84. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 18, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 85. The method according to claim 84, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 86. The method accord to claim 85, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 87. The method according to claim 86, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 88. The method according to claim 85, wherein the dementia is vascular dementia.
  - 89. The method according to claim 85, wherein the cerebrovascular accident is age related macular degeneration.
  - 90. The method according to claim 84, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 91. The method according to claim 90, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 92. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 19, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 93. The method according to claim 92, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 94. The method accord to claim 93, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 95. The method according to claim 94, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 96. The method according to claim 93, wherein the dementia is vascular dementia.
  - 97. The method according to claim 93, wherein the cerebrovascular accident is age related macular degeneration.
  - 98. The method according to claim 92, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 99. The method according to claim 98, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 100. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 20, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 101. The method according to claim 100, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 102. The method accord to claim 101, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 103. The method according to claim 102, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 104. The method according to claim 101, wherein the dementia is vascular dementia.
  - 105. The method according to claim 101, wherein the cerebrovascular accident is age related macular degeneration.
  - 106. The method according to claim 100, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 107. The method according to claim 106, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 108. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 21, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 109. The method according to claim 108, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 110. The method accord to claim 109, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 111. The method according to claim 110, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 112. The method according to claim 109, wherein the dementia is vascular dementia.
  - 113. The method according to claim 109, wherein the cerebrovascular accident is age related macular degeneration.
  - 114. The method according to claim 108, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 115. The method according to claim 114, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 116. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 22, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 117. The method according to claim 116, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 118. The method accord to claim 117, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 119. The method according to claim 118, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 120. The method according to claim 117, wherein the dementia is vascular dementia.
  - 121. The method according to claim 117, wherein the cerebrovascular accident is age related macular degeneration.
  - 122. The method according to claim 116, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 123. The method according to claim 122, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 124. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 23, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 125. The method according to claim 124, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 126. The method accord to claim 125, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 127. The method according to claim 126, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 128. The method according to claim 125, wherein the dementia is vascular dementia.
  - 129. The method according to claim 125, wherein the cerebrovascular accident is age related macular degeneration.
  - 130. The method according to claim 124, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 131. The method according to claim 130, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 132. A method of inhibiting GSK-3 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 24, wherein the inhibition of GSK-3 kinase is useful for the treatment or prevention of diseases or disorders regulated by GSK-3 kinase in a human in need thereof.
  - 133. The method according to claim 132, wherein the inhibition of GSK-3 kinase is useful for stimulation of neuroregeneration and the treatment and prevention of neurodegenerative diseases, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, multiple sclerosis, cognitive and attention deficits associated with Alzheimer'"'"'s disease, acute and chronic neurodegenerative diseases, dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, retinopathies and glaucoma.
  - 134. The method accord to claim 133, wherein the acute and chronic neurodegenerative diseases are Parkinson'"'"'s disease and tauopathies.
  - 135. The method according to claim 134, wherein the tauopathies are frontotemporoparietal dementia, corticobasal degeneration, Pick'"'"'s disease, and progressive supranuclear palsy.
  - 136. The method according to claim 133, wherein the dementia is vascular dementia.
  - 137. The method according to claim 133, wherein the cerebrovascular accident is age related macular degeneration.
  - 138. The method according to claim 132, wherein the inhibition of GSK-3 kinase is useful for the treatment non-insulin dependent diabetes and obesity, manic depressive illness, schizophrenia, alopecia, cancer, osteoarthritis, rheumatoid arthritis, and osteoporosis.
  - 139. The method according to claim 138, wherein the cancer is breast cancer, non-small cell lung carcinoma, thyroid cancer, T or B-cell leukemia, and virus-induced tumors.
  - 140. A method of inhibiting JAK kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 1 wherein the inhibition of JAK kinase is useful for the treatment or prevention of diseases or disorders regulated by JAK kinases in a human in need thereof.
  - 141. The method according to claim 140, wherein the inhibition of JAK kinase is useful for the treatment of autoimmune diseases, myeloproliferative syndromes and cardiovascular diseases associated with abnormal activity of JAK kinases comprises administering to a mammalian organism in need thereof an effective amount of a compound according to claim 5.
  - 142. The method according to claim 141, wherein the myeloproliferative syndromes are leukemias, lymphomas or cancer.
  - 143. The method according to claim 142, wherein the cancer is hematologic cancer.
  - 144. The method according to claim 141, wherein the autoimmune diseases are rheumatoid arthritis and psoriasis.
  - 145. The method according to claim 140, wherein the inhibition of JAK kinase is useful for the treatment of autoimmune diseases, myeloproliferative syndromes and cardiovascular diseases associated with abnormal activity of JAK kinases comprises administering to a mammalian organism in need thereof an effective amount of a compound according to claim 9.
  - 146. The method according to claim 145, wherein the myeloproliferative syndromes are leukemias, lymphomas or cancer.
  - 147. The method according to claim 146, wherein the cancer is hematologic cancer.
  - 148. The method according to claim 145, wherein the autoimmune diseases are rheumatoid arthritis and psoriasis.
  - 149. The method according to claim 140, wherein the inhibition of JAK kinase is useful for the treatment of autoimmune diseases, myeloproliferative syndromes and cardiovascular diseases associated with abnormal activity of JAK kinases comprises administering to a mammalian organism in need thereof an effective amount of a compound according to claim 13.
  - 150. The method according to claim 149, wherein the myeloproliferative syndromes are leukemias, lymphomas or cancer.
  - 151. The method according to claim 150, wherein the cancer is hematologic cancer.
  - 152. The method according to claim 149, wherein the autoimmune diseases are rheumatoid arthritis and psoriasis.
  - 153. A method of inhibiting ROCK kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 3, wherein the inhibition of ROCK kinase is useful for the treatment of neurodegeneration, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, pulmonary inflammation associated with asthma, asthma, for accelerated regeneration and enhanced functional recovery after spinal-cord injury, for multiple sclerosis, pain, hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, induction of new axonal growth, axonal rewiring across lesions within the CNS, amyotrophic lateral sclerosis, Huntington'"'"'s disease, Parkinson'"'"'s disease, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn'"'"'s disease, psoriasis, ulcerative colitis, Lupus, cancer and tumor metastasis, anti-viral and anti-bacterial applications, insulin resistance, diabetes, cystic fibrosis, angina pectoris, and arteriosclerosis.
  - 154. A method of inhibiting ROCK kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 6, wherein the inhibition of ROCK kinase is useful for the treatment of neurodegeneration, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, pulmonary inflammation associated with asthma, asthma, for accelerated regeneration and enhanced functional recovery after spinal-cord injury, for multiple sclerosis, pain, hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, induction of new axonal growth, axonal rewiring across lesions within the CNS, amyotrophic lateral sclerosis, Huntington'"'"'s disease, Parkinson'"'"'s disease, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn'"'"'s disease, psoriasis, ulcerative colitis, Lupus, cancer and tumor metastasis, anti-viral and anti-bacterial applications, insulin resistance, diabetes, cystic fibrosis, angina pectoris, and arteriosclerosis.
  - 155. A method of inhibiting ROCK kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 8, wherein the inhibition of ROCK kinase is useful for the treatment of neurodegeneration, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, pulmonary inflammation associated with asthma, asthma, for accelerated regeneration and enhanced functional recovery after spinal-cord injury, for multiple sclerosis, pain, hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, induction of new axonal growth, axonal rewiring across lesions within the CNS, amyotrophic lateral sclerosis, Huntington'"'"'s disease, Parkinson'"'"'s disease, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn'"'"'s disease, psoriasis, ulcerative colitis, Lupus, cancer and tumor metastasis, anti-viral and anti-bacterial applications, insulin resistance, diabetes, cystic fibrosis, angina pectoris, and arteriosclerosis.
  - 156. A method of inhibiting ROCK kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 11, wherein the inhibition of ROCK kinase is useful for the treatment of neurodegeneration, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, pulmonary inflammation associated with asthma, asthma, for accelerated regeneration and enhanced functional recovery after spinal-cord injury, for multiple sclerosis, pain, hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, induction of new axonal growth, axonal rewiring across lesions within the CNS, amyotrophic lateral sclerosis, Huntington'"'"'s disease, Parkinson'"'"'s disease, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn'"'"'s disease, psoriasis, ulcerative colitis, Lupus, cancer and tumor metastasis, anti-viral and anti-bacterial applications, insulin resistance, diabetes, cystic fibrosis, angina pectoris, and arteriosclerosis.
  - 157. A method of inhibiting ROCK kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 14, wherein the inhibition of ROCK kinase is useful for the treatment of neurodegeneration, inflammatory and demyelinating diseases, Alzheimer'"'"'s disease, stroke, pulmonary inflammation associated with asthma, asthma, for accelerated regeneration and enhanced functional recovery after spinal-cord injury, for multiple sclerosis, pain, hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, induction of new axonal growth, axonal rewiring across lesions within the CNS, amyotrophic lateral sclerosis, Huntington'"'"'s disease, Parkinson'"'"'s disease, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn'"'"'s disease, psoriasis, ulcerative colitis, Lupus, cancer and tumor metastasis, anti-viral and anti-bacterial applications, insulin resistance, diabetes, cystic fibrosis, angina pectoris, and arteriosclerosis.
  - 158. A method of inhibiting Cdc7 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 3, wherein the inhibition of Cdc7 kinase is useful for the treatment of cancers and proliferative disorders.
  - 159. The method according to claim 158, wherein the cancers are bladder cancer;
    - breast cancer;
      
      colon cancer;
      
      kidney cancer;
      
      liver cancer;
      
      lung cancer;
      
      esophagus cancer;
      
      gallbladder cancer;
      
      ovarian cancer;
      
      pancreatic cancer;
      
      stomach cancer;
      
      cervical cancer;
      
      thyroid cancer;
      
      prostate cancer;
      
      skin cancer, wherein said skin cancer is squamous cell carcinoma;
      
      hematopoietic tumors of lymphoid lineage, wherein said tumors are leukemia, acute lymphocytic leukemia, acute lymphoblastic leukemia, B-cell lymphoma, T-cell lymphoma, Hodgkin'"'"'s lymphoma, non-Hodgkin'"'"'s lymphoma, hairy cell lymphoma, and Burkitt'"'"'s lymphoma;
      
      hematopoietic tumors of myeloid lineage, wherein said tumors are acute and chronic myelogenous leukemias, myelodysplastic syndrome and promyelocytic leukemia;
      
      tumors of mesenchymal origin, wherein the tumors are fibrosarcoma and rhabdomyosarcoma;
      
      tumors of the central and peripheral nervous system, wherein said tumors are astrocytoma, neuroblastoma, glioma and schwannomas; and
      
      other tumors, wherein said tumors are melanoma, seminoma, teratocarcinoma, osteosarcoma, xeroderma pegmentosum, keratoxanthoma, thyroid follicular cancer and Kaposi'"'"'s sarcoma.
  - 160. The method according to claim 158, wherein the proliferative disorders are benign prostate hyperplasia, familial adenomatosis, polyposis, neuro-fibromatosis, psoriasis, vascular smooth cell proliferation associated with atherosclerosis, pulmonary fibrosis, arthritis, glomerulonephritis, and post-surgical stenosis and restenosis.
  - 161. A method of inhibiting Cdc7 kinase comprising administering a therapeutically effective amount of a compound of Formula (I), according to claim 7, wherein the inhibition of Cdc7 kinase is useful for the treatment of cancers and proliferative disorders.
  - 162. The method according to claim 161, wherein the cancers are bladder cancer;
    - breast cancer;
      
      colon cancer;
      
      kidney cancer;
      
      liver cancer;
      
      lung cancer;
      
      esophagus cancer;
      
      gallbladder cancer;
      
      ovarian cancer;
      
      pancreatic cancer;
      
      stomach cancer;
      
      cervical cancer;
      
      thyroid cancer;
      
      prostate cancer;
      
      skin cancer, wherein said skin cancer is squamous cell carcinoma;
      
      hematopoietic tumors of lymphoid lineage, wherein said tumors are leukemia, acute lymphocytic leukemia, acute lymphoblastic leukemia, B-cell lymphoma, T-cell lymphoma, Hodgkin'"'"'s lymphoma, non-Hodgkin'"'"'s lymphoma, hairy cell lymphoma, and Burkitt'"'"'s lymphoma;
      
      hematopoietic tumors of myeloid lineage, wherein said tumors are acute and chronic myelogenous leukemias, myelodysplastic syndrome and promyelocytic leukemia;
      
      tumors of mesenchymal origin, wherein the tumors are fibrosarcoma and rhabdomyosarcoma;
      
      tumors of the central and peripheral nervous system, wherein said tumors are astrocytoma, neuroblastoma, glioma and schwannomas; and
      
      other tumors, wherein said tumors are melanoma, seminoma, teratocarcinoma, osteosarcoma, xeroderma pegmentosum, keratoxanthoma, thyroid follicular cancer and Kaposi'"'"'s sarcoma.
  - 163. The method according to claim 161, wherein the proliferative disorders are benign prostate hyperplasia, familial adenomatosis, polyposis, neuro-fibromatosis, psoriasis, vascular smooth cell proliferation associated with atherosclerosis, pulmonary fibrosis, arthritis, glomerulonephritis, and post-surgical stenosis and restenosis.

Specification

Resources

Litigation Campaign Assessment

Granted Patent

US 8,648,069 B2
Time in Patent Office

Days
Field of Search
US Class Current

514/234.500
CPC Class Codes

A61P 25/28   for treating neurodegenerat...

A61P 35/00   Antineoplastic agents

C07D 401/14   containing three or more he...

C07D 403/04   directly linked by a ring-m...

C07D 403/14   containing three or more he...

C07D 405/04   directly linked by a ring-m...

C07D 405/14   containing three or more he...

C07D 409/14   containing three or more he...

C07D 413/04   directly linked by a ring-m...

C07D 413/14   containing three or more he...

C07D 417/04   directly linked by a ring-m...

C07D 417/14   containing three or more he...

C07D 471/04   Ortho-condensed systems

C07D 487/04   Ortho-condensed systems

C07D 513/04   Ortho-condensed systems

5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS

First Claim

2 Assignments

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Abstract

186 Citations

163 Claims

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5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS

First Claim

2 Assignments

Subscription Required

Subscription Required

0 Petitions

Subscription Required

Accused Products

Subscription Required

Abstract

186 Citations

163 Claims

Specification

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Solutions

Use Cases

Quick Links