Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
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Abstract
The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I:
wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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Citations
39 Claims
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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)
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2. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein W is N.
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3. The compound of claim 2, or a pharmaceutically acceptable salt thereof, wherein L is C(R6)2, C(═
- O), C(═
O)O, C(═
O)N(R7), S(═
O)2, S(═
O)2N(R7) or C(═
NR7a)N(R7).
- O), C(═
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4. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R6 is H, R7 is H or methyl, and R7a is CN.
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5. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein W is CH.
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6. The compound of claim 5, or a pharmaceutically acceptable salt thereof, wherein L is O.
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7. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein Y is cyano.
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8. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are each H.
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9. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein n is 0.
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10. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein m is 1.
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11. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein A is H, methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, 1,2-dimethylpropyl, 1-(tert-butyl)methyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, a tetrahydropyran ring, a pyrrolidine ring, a piperidine ring, a pyridine ring, a pyrimidine ring, a thiazole ring, or a pyrazine ring;
- each of which is optionally substituted with p independently selected R8 substituents;
provided when L is O, S, C(═
O), C(═
O)O, S(═
O), or S(═
O)2, then A is not H.
- each of which is optionally substituted with p independently selected R8 substituents;
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12. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each R8 is independently selected from halo, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —
- ORa, —
SRa, —
S(═
O)Rb, —
S(═
O)2Rb, —
S(═
O)2NReRf, —
C(═
O)Rb, —
C(═
O)ORa, —
C(═
O)NReRf, —
OC(═
O)Rb, —
OC(═
O)NReRf, —
NReRf, —
NRcC(═
O)Rd, —
NRcC(═
O)ORd, —
NRcS(═
O)2Rd, and —
NRcS(═
O)2NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups.
- ORa, —
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13. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each R8 is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl, —
- ORa, —
C(═
O)ORa, and —
NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups; and
wherein each Ra, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl.
- ORa, —
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14. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each Rg is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl, —
- ORa1, —
S(═
O)2Rb1, —
S(═
O)2NRe1Rf1, —
C(═
O)Rb1, —
C(═
O)ORa1, and —
NRe1Rf1;
wherein said C1-6 alkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl and are each optionally substituted by 1, 2, 3, or 4 independently selected Rh groups.
- ORa1, —
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15. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each Rg is independently selected from C2-7 heterocycloalkyl, —
- ORa and —
NRe1Rf1;
wherein said C2-7 heterocycloalkyl is optionally substituted by 1 or 2 Rh groups independently selected from fluoro, OH, C1-3 alkyl, C1-3 alkoxy, and hydroxy-C1-4 alkyl; and
wherein each Ra1, Re1 and Rf1 are independently selected from H, C3-7 cycloalkyl, and C1-6 alkyl.
- ORa and —
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16. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each Rh is independently selected from fluoro, OH, C1-3 alkyl, C1-3 alkoxy, and hydroxy-C1-4 alkyl.
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17. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is N; Z is N; R1, R2, and R3 are each H; Y is cyano; W is N and L is C(R6)2, C(═
O), C(═
O)N(R7), S(═
O)2, or S(═
O)2N(R7);
orW is CH and L is O; A is C1-6 alkyl, C3-10 cycloalkyl, C2-10 heterocycloalkyl, C6-10 aryl, or C1-10 heteroaryl; wherein said C1-6 alkyl, C3-10 cycloalkyl, C2-10 heterocycloalkyl, C6-10 aryl, and C1-10 heteroaryl are each optionally substituted with p independently selected R8 substituents;
wherein p is 1, 2, 3, 4, or 5;each R8 is independently selected from halo, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —
ORa, —
SRa, —
S(═
O)Rb, —
S(═
O)2Rb, —
S(═
O)2NReRf, —
C(═
O)Rb, —
C(═
O)ORa, —
C(═
O)NReRf, —
OC(═
O)Rb, —
OC(═
O)NReRf, —
NReRf, —
NRcC(═
O)Rd, —
NRcC(═
O)ORd, —
NRcS(═
O)2Rd, and —
NRcS(═
O)2NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups;each Rg is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl, —
S(═
O)2Rb1, —
S(═
O)2NRe1Rf1, —
C(═
O)Rb1, —
C(═
O)ORa1, and —
NRe1Rf1;
wherein said C1-6 alkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl are each optionally substituted by 1, 2, 3, or 4 independently selected Rh groups;each Ra, Rc, Rd, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; each Rb is independently selected from C1-6 alkyl and C1-6 haloalkyl; each Ra1, Rc1, Rd1, Re1, and Rf1 is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; each Rb1 is independently selected from C1-6 alkyl and C1-6 haloalkyl; n is 0; and m is 1.
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18. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is N; Z is N; R1, R2, and R3 are each H; Y is cyano; W is N and L is C(R6)2, C(═
O), C(═
O)N(R7), S(═
O)2, or S(═
O)2N(R7);
orW is CH and L is O; A is C1-6 alkyl, C3-10 cycloalkyl, C2-10 heterocycloalkyl, C6-10 aryl, or C1-10 heteroaryl; wherein said C1-6 alkyl, C3-10 cycloalkyl, C2-10 heterocycloalkyl, C6-10 aryl, and C1-10 heteroaryl are each optionally substituted with p independently selected R8 substituents;
wherein p is 1, 2, 3, 4, or 5;each R8 is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, —
ORa and —
NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups;each Rg is independently selected from C2-7 heterocycloalkyl and —
NRe1Rf1;
wherein said C2-7 heterocycloalkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rh groups;each Rh is independently selected from C1-4 alkyl; each Ra, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; each Ra1, Re1, and Rf1 is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; n is 0; and m is 1.
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19. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is N; Z is N; R1, R2, and R3 are each H; Y is cyano; W is N and L is C(R6)2, C(═
O), C(═
O)N(R7), S(═
O)2, or S(═
O)2N(R7);R6 is H; R7 is H or methyl; A is methyl, ethyl, cyclopropyl, phenyl, a pyrrolidine ring, a piperidine ring, a pyridine ring, a pyrimidine ring, a thiazole ring, or a pyrazine ring;
each of which is optionally substituted with p independently selected R8 substituents;
wherein p is 1, 2, or 3;each R8 is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, —
ORa and —
NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups;each Rg is independently selected from C2-7 heterocycloalkyl and —
NRe1Rf1;
wherein said C2-7 heterocycloalkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rh groups;each Rh is independently C1-4 alkyl; each Ra, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; each Ra1, Re1, and Rf1 is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; n is 0; and m is 1.
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20. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is N; Z is N; R1, R2, and R3 are each H; Y is cyano; W is CH and L is O; R6 is H; R7 is H or methyl; A is phenyl, which is optionally substituted with p independently selected R8 substituents;
wherein p is 1, 2, or 3;each R8 is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, —
ORa and —
NReRf;
wherein said C1-6 alkyl is optionally substituted by p independently selected Rg groups;each Rg is independently selected from C2-7 heterocycloalkyl and —
NRe1Rf1;
wherein said C2-7 heterocycloalkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rh groups;each Rh is independently C1-4 alkyl; each Ra, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; each Ra1, Re1, and Rf1 is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl; n is 0; and m is 1.
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21. The compound accordingly to claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is N; Z is N; R1, R2, and R3 are each H; Y is cyano; W is N and L is C(R6)2, C(═
O), C(═
O)O, C(═
O)N(R7), S(═
O)2, S(═
O)2N(R7) or C(═
NR7a)N(R7);
orW is CH and L is O; R6 is H; R7 is H or methyl; R7a is CN; A is H, methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, 1,2-dimethylpropyl, 1-(tert-butyl)methyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, a tetrahydropyran ring, a pyrrolidine ring, a piperidine ring, a pyridine ring, a pyrimidine ring, a thiazole ring, or a pyrazine ring;
wherein said methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, 1,2-dimethylpropyl, 1-(tert-butyl)methyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, a tetrahydropyran ring, pyrrolidine ring, piperidine ring, pyridine ring, pyrimidine ring, thiazole ring, and pyrazine ring are each optionally substituted with p independently selected R8 substituents;
provided when L is O, S, C(═
O), C(═
O)O, S(═
O), or S(═
O)2, then A is not H;each R8 is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl, —
ORa, —
C(═
O)ORa, and —
NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups; and
wherein each Ra, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl;each Rg is independently selected from C2-7 heterocycloalkyl, —
ORa and —
NRe1Rf1;
wherein said C2-7 heterocycloalkyl is optionally substituted by 1 or 2 Rh groups independently selected from fluoro, OH, C1-3 alkyl, C1-3 alkoxy, and hydroxy-C1-4 alkyl; and
wherein each Ra1, Re1 and Rf1 are independently selected from H, C3-7 cycloalkyl, and C1-6 alkyl;p is 1, 2, or 3; m is 1; and n is 0.
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22. The compound accordingly to claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is N; Z is N; R1, R2, and R3 are each H; Y is cyano; W is N and L is C(R6)2, C(═
O), C(═
O)O, C(═
O)N(R7), S(═
O)2, or S(═
O)2N(R7);
orW is CH and L is O; R6 is H; R7 is H or methyl; A is methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, 1,2-dimethylpropyl, 1-(tert-butyl)methyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, a tetrahydropyran ring, a pyrrolidine ring, a piperidine ring, a pyridine ring, a pyrimidine ring, a thiazole ring, or a pyrazine ring;
each of which is optionally substituted with p independently selected R8 substituents;each R8 is independently selected from halo, cyano, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, C2-7 heterocycloalkyl, —
ORa, —
C(═
O)ORa, and —
NReRf;
wherein said C1-6 alkyl is optionally substituted by 1, 2, 3, or 4 independently selected Rg groups; and
wherein each Ra, Re, and Rf is independently selected from H, C1-6 alkyl, and C1-6 haloalkyl;each Rg is independently selected from C2-7 heterocycloalkyl, —
ORa1, —
NRe1Rf1;
wherein said C2-7 heterocycloalkyl is optionally substituted by 1 or 2 Rh groups independently selected from fluoro, OH, C1-3 alkyl, C1-3 alkoxy, and hydroxy-C1-4 alkyl; and
wherein each Ra1, Re1 and Rf1 are independently selected from H, C3-7 cycloalkyl, and C1-6 alkyl;p is 1, 2, or 3; m is 1; and n is 0.
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23. The compound according to claim 1, wherein said compound has Formula IV:
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24. The compound according to claim 1, wherein said compound has Formula V:
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25. The compound according to claim 1, selected from:
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3-[(4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)methyl]-5-fluorobenzonitrile; 3-[(4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)methyl]-6-(dimethylamino)-2-fluorobenzonitrile; 4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[4-fluoro-2-(trifluoromethyl)phenyl]piperazine-1-carboxamide; {3-(4-{[(2S)-2-methylpyrrolidin-1-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-(4-{[(2S)-2-ethylpyrrolidin-1-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; [1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile; {3-[4-(3,5-difluorobenzoyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[(2-chloro-5-fluoropyridin-3-yl)carbonyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[(5-fluoropyridin-3-yl)carbonyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[2-(difluoromethyl)-3-fluoroisonicotinoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 3-[(4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)carbonyl]-5-fluorobenzonitrile; [1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[4-(trifluoromethyl)-1,3-thiazol-2-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile; [1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[6-(trifluoromethyl)pyrazin-2-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile; {3-[4-(3,4-difluorobenzoyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-[4-(2-chloro-3,6-difluorobenzyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[3-fluoro-5-(trifluoromethyl)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[2-fluoro-4-(trifluoromethyl)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-[4-(pyrrolidin-1-ylcarbonyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)cyclobutyl}acetonitrile; {3-(4-{[6-(difluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[2-fluoro-3-(trifluoromethyl)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[(5-fluoropyridin-3-yl)methyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[(2-isopropylpyrimidin-4-yl)carbonyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-[4-(piperidin-1-ylcarbonyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[4-fluoro-3-(trifluoromethoxy)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-(4-{[3-fluoro-5-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[4-chlorobenzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-{4-[2-fluoro-4-(trifluoromethyl)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N,N-dimethylpiperazine-1-carboxamide; {3-(4-{3-[(dimethylamino)methyl]-5-fluorobenzoyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-(4-{3-[(dimethylamino)methyl]-5-fluorobenzyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-[4-(ethylsulfonyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-[4-(cyclopropylsulfonyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N,N-dimethylpiperazine-1-sulfonamide; 4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-ethyl-N-methylpiperazine-1-carboxamide; {3-{4-[3-[(dimethylamino)methyl]-5-(trifluoromethyl)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-[4-(3-fluoro-5-{[(2S)-2-methylpyrrolidin-1-yl]methyl}phenoxy)piperidin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {3-(4-{3-[(dimethylamino)methyl]-5-fluorophenoxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; [1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile-dl; and or a pharmaceutically acceptable salt of any of the aforementioned.
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26. The compound of claim 1, selected from:
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3-[(4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)carbonyl]-5-[(dimethylamino)methyl]benzonitrile; 3-[(4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)methyl]-5-[(dimethylamino)methyl]benzonitrile; 3-[(4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)methyl]-5-[(dimethylamino)methyl]benzonitrile; {trans-3-{4-[3-[(dimethylamino)methyl]-5-(trifluoromethyl)benzyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-{4-[3-[(dimethylamino)methyl]-5-(trifluoromethyl)benzyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[(ethylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 6-[(4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)carbonyl]-2-(trifluoromethyl)pyrimidine-4-carboxylic acid; {trans-3-(4-{[6-(azetidin-1-ylmethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[(methylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(hydroxymethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[(dimethylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(pyrrolidin-1-ylmethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(aminomethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[(isopropylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[(cyclobutylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[(tert-butylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(1-hydroxy-1-methylethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(1-hydroxy-1-methylethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(methoxymethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(1-aminocyclobutyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(1-aminocyclobutyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[1-(dimethylamino)cyclobutyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-[1-(dimethylamino)cyclobutyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(dimethylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(hydroxymethyl)-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(methylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(1-methoxy-1-methylethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-[1-(methylamino)cyclobutyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 2-[(4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)carbonyl]-6-(trifluoromethyl)isonicotinonitrile; {trans-3-(4-{[6-(1-hydroxycyclobutyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(4,5-dihydro-1H-imidazol-2-yl)-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{3-(difluoromethyl)-5-[(dimethylamino)methyl]benzoyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(1-hydroxy-1-methylethyl)-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(methoxymethyl)-6-(trifluoromethyl)pyridin-2-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-isopropyl-N-methylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-methyl-N-propylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-ethylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[3-(dimethylamino)propyl]-N-methylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclopropyl-N-methylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-methyl-N-(2,2,2-trifluoroethyl)piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-isopropylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-(trans-4-hydroxycyclohexyl)piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(3R)-tetrahydrofuran-3-yl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-(2-hydroxycyclopentyl)piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S,2R)-2-hydroxycyclopentyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclopentylpiperazine-1-carboxamide; {trans-3-(4-{[(3S)-3-hydroxypyrrolidin-1-yl]carbonyl}piperazin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-(cyclopropylmethyl)piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1R)-1,2-dimethylpropyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-1,2-dimethylpropyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-1-cyclopropylethyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1R)-1-cyclopropylethyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclopropylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclobutylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-(2,2-dimethylpropyl)piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-isobutylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1R)-1-methylpropyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-1-methylpropyl]piperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclobutylpiperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1R)-1-methylpropyl]piperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-1-methylpropyl]piperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclopropylpiperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-isopropylpiperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-cyclopentylpiperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1R)-1,2-dimethylpropyl]piperazine-1-carboxamide; 4-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-1,2-dimethylpropyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-methylpiperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1R)-2,2,2-trifluoro-1-methylethyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-2,2,2-trifluoro-1-methylethyl]piperazine-1-carboxamide; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[(1S)-1-(trifluoromethyl)propyl]piperazine-1-carboxamide; [trans-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[(2R)-2-(trifluoromethyl)pyrrolidin-1-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile; [trans-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[(2S)-2-(trifluoromethyl)pyrrolidin-1-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile; N′
-cyano-4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N,N-dimethylpiperazine-1-carboximidamide;{trans-3-[4-(methylsulfonyl)piperazin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; isopropyl 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazine-1-carboxylate; {cis-3-(4-{[4-(methoxymethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(methoxymethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(hydroxymethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[4-(hydroxymethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(1-hydroxy-1-methylethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(tert-butylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[4-[(tert-butylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(dimethylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(ethylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(methylamino)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 2-[(1-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperidin-4-yl)oxy]-6-(trifluoromethyl)isonicotinonitrile; 2-[(1-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperidin-4-yl)oxy]-6-(trifluoromethyl)isonicotinonitrile; {cis-3-{4-[3-[(dimethylamino)methyl]-5-(trifluoromethyl)benzoyl]piperazin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 3-[(4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperazin-1-yl)carbonyl]-5-[(dimethylamino)methyl]benzonitrile; {cis-3-(4-{[6-(pyrrolidin-1-ylmethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(morpholin-4-ylmethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(azetidin-1-ylmethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 3-[(1-{cis-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}piperidin-4-yl)oxy]-5-[(dimethylamino)methyl]benzonitrile; {cis-3-{4-[3-[(dimethylamino)methyl]-5-(trifluoromethyl)phenoxy]piperidin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-{4-[3-[(diethylamino)methyl]-5-(trifluoromethyl)phenoxy]piperidin-1-yl}-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{3-(difluoromethyl)-5-[(dimethylamino)methyl]phenoxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-[4-({6-chloro-4-[(dimethylamino)methyl]pyridin-2-yl}oxy)piperidin-1-yl]-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-[(dimethylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-[(ethylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-[(3-hydroxyazetidin-1-yl)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-methyl-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(hydroxymethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(aminomethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; 4-{trans-3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}-N-[2,2,2-trifluoro-1-(trifluoromethyl)ethyl]piperazine-1-carboxamide; {trans-3-(4-{[4-{[(2-hydroxy-1,1-dimethylethyl)amino]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-{[(2-hydroxyethyl)amino]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-{[(3-hydroxypropyl)amino]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(azetidin-1-ylmethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(3-hydroxyazetidin-1-yl)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(pyrrolidin-1-ylmethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-(morpholin-4-ylmethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-[(3,3-difluoropyrrolidin-1-yl)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-{[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[4-{[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[6-(2-hydroxyethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {trans-3-(4-{[6-(2-hydroxyethyl)-2-(trifluoromethyl)pyrimidin-4-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; {cis-3-(4-{[4-[(2-oxo-1,3-oxazolidin-3-yl)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; and {trans-3-(4-{[4-[(2-oxo-1,3-oxazolidin-3-yl)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile; or a pharmaceutically acceptable salt of any of the aforementioned.
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27. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein the cyclobutyl ring in Formula I is the cis form.
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28. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein the cyclobutyl ring in Formula I is the trans form.
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29. A composition comprising a compound according to claim 1, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.
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30. The compound of claim 1, which is [trans-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-(4-{[2-(trifluoromethyl)pyrimidin-4-yl]carbonyl}piperazin-1-yl)cyclobutyl]acetonitrile, or a pharmaceutically acceptable salt thereof.
-
31. The compound of claim 1, which is {trans-3-(4-{[4-[(3-hydroxyazetidin-1-yl)methyl]-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile, or a pharmaceutically acceptable salt thereof.
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32. The compound of claim 1, which is {trans-3-(4-{[4-{[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile.
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33. The compound of claim 1, which is {trans-3-(4-{[4-{[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl}-6-(trifluoromethyl)pyridin-2-yl]oxy}piperidin-1-yl)-1-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile.
-
34. A composition comprising a compound according to claim 30, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.
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35. A composition comprising a compound according to claim 31, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.
-
36. A composition comprising a compound according to claim 32 and at least one pharmaceutically acceptable carrier.
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37. A composition comprising a compound according to claim 33 and at least one pharmaceutically acceptable carrier.
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38. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein:
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X is CH or N; Y is H, cyano, halo, C1-3 alkyl, or C1-3 haloalkyl; Z is N; W is CH or N; when W is CH, then L is O, S, C(R6)2, C(═
O), C(═
O)N(R7), C(═
O)O, C(═
O)C(R6)2, S(═
O), S(═
O)2, S(═
O)N(R7), or S(═
O)2N(R7);
orwhen W is N, then L is C(R6)2, C(═
O), C(═
O)O, C(═
O)N(R7), C(═
O)C(R6)2, S(═
O), S(═
O)2, S(═
O)N(R7), or S(═
O)2N(R7);R1, R2 and R3 are each independently H, hydroxy, halo, C1-3 alkyl, or C1-3 haloalkyl; each R5 is independently hydroxy, C1-4 alkoxy, fluorine, C1-4 alkyl, hydroxy-C1-4-alkyl, C1-4 alkoxy-C1-4-alkyl, or C1-4 fluoroalkyl; each R6 is, independently, H or C1-4 alkyl;
ortwo R6 groups, together with the carbon atom to which they are attached, form a 3-, 4-, 5-, or 6-membered cycloalkyl ring; R7 is H or C1-4 alkyl; A is C1-6 alkyl, C3-10 cycloalkyl, C2-10 heterocycloalkyl, C6-10 aryl, or C1-10 heteroaryl; wherein said C1-6 alkyl, C3-10 cycloalkyl, C2-10 heterocycloalkyl, C6-10 aryl, and C1-10 heteroaryl are each optionally substituted with p independently selected R8 substituents;
wherein p is 1, 2, 3, 4, or 5;each R8 is independently selected from halo, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-4-alkyl, C2-10 heterocycloalkyl, C2-10 heterocycloalkyl-C1-4-alkyl, C6-10 aryl, C6-10 aryl-C1-4-alkyl, C1-10 heteroaryl, C1-10 heteroaryl-C1-4-alkyl, —
ORa, —
SRa, —
S(═
O)Rb, —
S(═
O)2Rb, —
S(═
O)2NReRf, —
C(═
O)Rb, —
C(═
O)ORa, —
C(═
O)NReRf, —
OC(═
O)Rb, —
OC(═
O)NReRf, —
NReRf, —
NRcC(═
O)Rd, —
NRcC(═
O)ORd, —
NRcS(═
O)2Rd, and —
NRcS(═
O)2NReRf;
wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-4-alkyl, C2-10 heterocycloalkyl, C2-10 heterocycloalkyl-C1-4-alkyl, C6-10 aryl, C6-10 aryl-C1-4-alkyl, C1-10 heteroaryl, and C1-10 heteroaryl-C1-4-alkyl are each optionally substituted by 1, 2, 3, or 4 independently selected Rg groups;each Ra, Rc, Rd, Re, and Rf is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-4-alkyl, C2-10 heterocycloalkyl, C2-10 heterocycloalkyl-C1-4-alkyl, C6-10 aryl, C6-10 aryl-C1-4-alkyl, C1-10 heteroaryl, and C1-10 heteroaryl-C1-4-alkyl;
wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-4-alkyl, C2-10 heterocycloalkyl, C2-10 heterocycloalkyl-C1-4-alkyl, C6-10 aryl, C6-10 aryl-C1-4-alkyl, C1-10 heteroaryl, and C1-10 heteroaryl-C1-4-alkyl are each optionally substituted by 1, 2, 3, or 4 independently selected Rg groups;each Rb is independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-4-alkyl, C2-10 heterocycloalkyl, C2-10 heterocycloalkyl-C1-4-alkyl, C6-10 aryl, C6-10 aryl-C1-4-alkyl, C1-10 heteroaryl, and C1-10 heteroaryl-C1-4-alkyl;
wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-4-alkyl, C2-10 heterocycloalkyl, C2-10 heterocycloalkyl-C1-4-alkyl, C6-10 aryl, C6-10 aryl-C1-4-alkyl, C1-10 heteroaryl, and C1-10 heteroaryl-C1-4-alkyl are each optionally substituted by 1, 2, 3, or 4 independently selected Rg groups;each Rg is independently selected from halo, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3-alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1-3-alkyl, phenyl, phenyl-C1-3-alkyl, C1-7 heteroaryl, C1-7 heteroaryl-C1-3-alkyl, —
ORa1, —
SRa1, —
S(═
O)Rb1, —
S(═
O)2Rb1, —
S(═
O)2NRe1Rf1, —
C(═
O)Rb1, —
C(═
O)ORa1, —
C(═
O)NRe1Rf1, —
OC(═
O)Rb1, —
OC(═
O)NRe1Rf1, —
NRe1Rf1, —
NRc1C(═
O)Rd1, —
NRc1C(═
O)ORd1, —
NRc1S(═
O)2Rd1,and —
NRc1S(═
O)2NRe1Rf1;
wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3-alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1-3-alkyl, phenyl, phenyl-C1-3-alkyl, C1-7 heteroaryl, and C1-7 heteroaryl-C1-3-alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected Rh groups;each Ra1, Rc1, Rd1, Re1, and Rf1 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3-alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1-3-alkyl, phenyl, phenyl-C1-3-alkyl, C1-7 heteroaryl, and C1-7 heteroaryl-C1-3-alkyl;
wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3-alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1-3-alkyl, phenyl, phenyl-C1-3-alkyl, C1-7 heteroaryl, and C1-7 heteroaryl-C1-3-alkyl are each optionally substituted by 1, 2, 3, or 4 independently selected Rh groups;each Rb1 is independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3-alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1-3-alkyl, phenyl, phenyl-C1-3-alkyl, C1-7 heteroaryl, and C1-7 heteroaryl-C1-3-alkyl;
wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3-alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1-3-alkyl, phenyl, phenyl-C1-3-alkyl, C1-7 heteroaryl, and C1-7 heteroaryl-C1-3-alkyl are each optionally substituted by 1, 2, 3, or 4 independently selected Rh groups;each Rh is independently selected from cyano, halo, hydroxy, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, amino, C1-4 alkylamino, di-C1-4-alkylamino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di(C1-6 alkyl)carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di(C1-6 alkyl)aminosulfonyl, aminosulfonylamino, C1-6 alkylaminosulfonylamino, di(C1-6 alkyl)aminosulfonylamino, aminocarbonylamino, C1-6 alkylaminocarbonylamino, and di(C1-6 alkyl)aminocarbonylamino; m is 0, 1, or 2; and n is 0, 1, 2, 3, or 4.
-
-
39. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein X is N.
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2. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein W is N.
Specification
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Current AssigneeIncyte Holdings Corporation And Incyte Corporation
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Original AssigneeIncyte Corporation
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InventorsRodgers, James D., Shepard, Stacey, Zhu, Wenyu, Shao, Lixin, Glenn, Joseph
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Primary Examiner(s)Moore, Susanna
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Application NumberUS13/300,094Publication NumberTime in Patent Office1,152 DaysField of Search544/280, 514/265.1US Class Current514/265.1CPC Class CodesA01N 43/90 having two or more relevant...A61K 31/519 ortho- or peri-condensed wi...A61P 1/00 Drugs for disorders of the ...A61P 1/04 for ulcers, gastritis or re...A61P 1/16 for liver or gallbladder di...A61P 13/12 of the kidneysA61P 17/00 Drugs for dermatological di...A61P 17/02 for treating wounds, ulcers...A61P 17/06 AntipsoriaticsA61P 17/08 AntiseborrheicsA61P 19/00 Drugs for skeletal disordersA61P 19/02 for joint disorders, e.g. a...A61P 19/04 for non-specific disorders ...A61P 19/08 for bone diseases, e.g. rac...A61P 19/10 for osteoporosisA61P 21/04 for myasthenia gravisA61P 25/00 Drugs for disorders of the ...A61P 27/04 Artificial tears; Irrigatio...A61P 29/00 Non-central analgesic, anti...A61P 3/04 Anorexiants; Antiobesity ag...A61P 3/10 : for hyperglycaemia, e.g. an...A61P 35/00 : Antineoplastic agentsA61P 35/02 : specific for leukemiaA61P 35/04 : specific for metastasisA61P 37/00 : Drugs for immunological or ...A61P 37/02 : ImmunomodulatorsA61P 37/06 : Immunosuppressants, e.g. dr...A61P 43/00 : Drugs for specific purposes...A61P 5/12 : for decreasing, blocking or...A61P 5/14 : of the thyroid hormones, e....A61P 7/00 : Drugs for disorders of the ...A61P 9/10 : for treating ischaemic or a...C07D 471/04 : Ortho-condensed systemsC07D 487/04 : Ortho-condensed systemsC07D 491/107 : with only one oxygen atom a...