Nitrogen-Containing heterocyclyl ketones and methods of use
First Claim
Patent Images
1. A compound of the following Formula I, II, III or IV enantiomers, diastereomers and salts thereof whereina and b are independently absent or a bond;
- n is an integer from 0 to 6 as allowed by valence;
v is an integer from 0 to 2;
when a is a bond X is CR4* or N, and when a is absent X is CR4R5 or NR6;
when b is a bond Y and Z are independently CR4 or N, and when b is absent one of Y and Z is CR4R5 and the other is NR6;
W, Y* and Z* are independently CR4* or N;
V, U and U* are independently CR4* or N provided that only one of U and U* is N;
L is absent, C1-6alkylene, C3-10cycloalkylene, C3-10heterocycloalkylene C2-8alkenylene or C2-8alkynylene any of which may be optionally independently substituted with one or more halo, —
OR7 or —
NR8R9 and further wherein any two substituent groups bound to the same tetravalent carbon atom may optionally combine to form a spiro-fused cycloalkyl or heterocyclyl ring;
M is absent, —
O—
, —
S(O)v—
, —
NR6—
, —
C(═
O)NR6—
, —
NR6(C═
O)—
, —
SO2NR6—
, —
NR6SO2—
, provided that L and M are not both simultaneously absent;
or -L-M-R2 may combine to formwherein A is CH or N; and
B, C, D and E are independently CH2, O, NR6 or S(O)v, provided that only one of A, B, C, D and E can be a heteroatom;
R1 is(1) halo, —
CN, —
NR6—
(C═
O)R7, —
NR6—
(C═
O)OR7, —
NR6—
(C═
O)NR8R9, —
(C═
O)NR8R9, —
(C═
O)OR7, —
(C═
O)R7, —
S(O)vR7, —
SO2NR8R9, —
NR8R9 or —
OR7 (2) cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl any of which may be optionally independently substituted with one or more R10 as allowed by valance;
R2 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl or cycloalkylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valence;
R2a is aryl, heteroaryl, cycloalkyl or heterocyclyl any of which may be optionally independently substituted with one or more R10 as allowed by valence;
R3 is an optional substituent independently selected at each occurrence from halo, cyano, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, —
(C═
O)0-1OR7, —
(C═
O)0-1NR8R9, —
S(O)vR7, —
SO2NR8R9, —
C═
OR7, —
NR8C═
OR7, —
NR6—
C═
O—
NR8R9 and —
NR8SO2R7;
R4*, R4 and R5 at each occurrence are independently H or one of the optional substituents listed in the definition of R3 provided that R4 and R5 cannot be simultaneously selected from —
OR7, —
NR8R9;
—
S(O)vR7, —
SO2NR8R9, —
NR8C═
OR7, —
NR6—
C═
O—
NR8R9 and —
NR8SO2R7;
R6 at each occurrence is independently(1) H, or(2) alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance;
R7 at each occurrence is independently(1) H, or(2) alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance;
R8 and R9 at each occurrence are independently(1) H, or(2) alkyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heteroalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance;
or R8 and R9 together with the nitrogen atom to which they are attached may combine to form a heterocyclyl ring; and
R10 is one or more optional substituent independently selected at each occurrence as allowed by valance from halo, oxo, cyano, alkyl, haloalkyl, cycloalkyl, heterocyclyl, heteroaryl, aryl, heterocyclylalkyl, heteroarylalkyl, arylalkyl, —
(CR4R5)0-3OR7, —
(CR4R5)0-3NR8R9, —
(CR4R5)0-3N(R6)C═
OR7, —
(CR4R5)0-3N(R6)(C═
O)OR7, —
(CR4R5)0-3C═
ONR8R9, —
(CR4R5)0-30(C═
O)NR8R9, —
(CR4R5)0-3C═
OR7, —
(CR4R5)0-3(C═
O)OR7, —
(CR4R5)0-3N(R6)C═
ONR8R9, —
(CR4R5)0-3S(O)vR7, —
(CR4R5)0-3SO2NR8R9 or —
(CR4R5)0-3NR6SO2R7.
1 Assignment
0 Petitions
Accused Products
Abstract
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
76 Citations
46 Claims
-
1. A compound of the following Formula I, II, III or IV
enantiomers, diastereomers and salts thereof wherein a and b are independently absent or a bond; -
n is an integer from 0 to 6 as allowed by valence; v is an integer from 0 to 2; when a is a bond X is CR4* or N, and when a is absent X is CR4R5 or NR6; when b is a bond Y and Z are independently CR4 or N, and when b is absent one of Y and Z is CR4R5 and the other is NR6; W, Y* and Z* are independently CR4* or N; V, U and U* are independently CR4* or N provided that only one of U and U* is N; L is absent, C1-6alkylene, C3-10cycloalkylene, C3-10heterocycloalkylene C2-8alkenylene or C2-8alkynylene any of which may be optionally independently substituted with one or more halo, —
OR7 or —
NR8R9 and further wherein any two substituent groups bound to the same tetravalent carbon atom may optionally combine to form a spiro-fused cycloalkyl or heterocyclyl ring;M is absent, —
O—
, —
S(O)v—
, —
NR6—
, —
C(═
O)NR6—
, —
NR6(C═
O)—
, —
SO2NR6—
, —
NR6SO2—
, provided that L and M are not both simultaneously absent;or -L-M-R2 may combine to form wherein A is CH or N; and
B, C, D and E are independently CH2, O, NR6 or S(O)v, provided that only one of A, B, C, D and E can be a heteroatom;R1 is (1) halo, —
CN, —
NR6—
(C═
O)R7, —
NR6—
(C═
O)OR7, —
NR6—
(C═
O)NR8R9, —
(C═
O)NR8R9, —
(C═
O)OR7, —
(C═
O)R7, —
S(O)vR7, —
SO2NR8R9, —
NR8R9 or —
OR7(2) cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; R2 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl or cycloalkylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valence; R2a is aryl, heteroaryl, cycloalkyl or heterocyclyl any of which may be optionally independently substituted with one or more R10 as allowed by valence; R3 is an optional substituent independently selected at each occurrence from halo, cyano, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, —
(C═
O)0-1OR7, —
(C═
O)0-1NR8R9, —
S(O)vR7, —
SO2NR8R9, —
C═
OR7, —
NR8C═
OR7, —
NR6—
C═
O—
NR8R9 and —
NR8SO2R7;R4*, R4 and R5 at each occurrence are independently H or one of the optional substituents listed in the definition of R3 provided that R4 and R5 cannot be simultaneously selected from —
OR7, —
NR8R9;
—
S(O)vR7, —
SO2NR8R9, —
NR8C═
OR7, —
NR6—
C═
O—
NR8R9 and —
NR8SO2R7;R6 at each occurrence is independently (1) H, or (2) alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; R7 at each occurrence is independently (1) H, or (2) alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; R8 and R9 at each occurrence are independently (1) H, or (2) alkyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heteroalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; or R8 and R9 together with the nitrogen atom to which they are attached may combine to form a heterocyclyl ring; and R10 is one or more optional substituent independently selected at each occurrence as allowed by valance from halo, oxo, cyano, alkyl, haloalkyl, cycloalkyl, heterocyclyl, heteroaryl, aryl, heterocyclylalkyl, heteroarylalkyl, arylalkyl, —
(CR4R5)0-3OR7, —
(CR4R5)0-3NR8R9, —
(CR4R5)0-3N(R6)C═
OR7, —
(CR4R5)0-3N(R6)(C═
O)OR7, —
(CR4R5)0-3C═
ONR8R9, —
(CR4R5)0-30(C═
O)NR8R9, —
(CR4R5)0-3C═
OR7, —
(CR4R5)0-3(C═
O)OR7, —
(CR4R5)0-3N(R6)C═
ONR8R9, —
(CR4R5)0-3S(O)vR7, —
(CR4R5)0-3SO2NR8R9 or —
(CR4R5)0-3NR6SO2R7.- 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, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46)
(2) aryl, heteroaryl, heterocyclyl, alkenyl or alkynyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
-
-
3. A compound of claim 2 wherein R1 is aryl, heteroaryl or heterocyclyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
-
4. A compound of claim 1 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
5. A compound of claim 2 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
6. A compound of claim 3 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
7. A compound of claim 6 wherein
R1 is phenyl, naphthyl, naphthyridinyl, thienyl, benzothienyl, furan, benzofuranyl, pyridyl, pyrazinyl, pyrimidinyl, imidazolyl, triazolyl, quinoxalinyl, benzodioxolyl, benzodioxinyl dihydrobenzodioxinyl, indolinyl, indolyl, benzoimidazolyl, benzoisoxazol, benzoisothiozazol, benzoxazole, benzothiazol, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, morpholinyl, pyrrolidinyl, pyrazolyl, indazolyl, piperazinyl, piperadinyl, azetidinyl, pyranyl, pyridazinyl, dihydropyranyl, tetrahydropyranyl, quinolinyl, quinazolinyl, cinnolinyl, phthalazinyl, dihydroquinolinyl or isoquinolinyl any of which may be optionally independently substituted as allowed by valance with one or more R10; - and
R2 is quinolinyl, isoquinolinyl, naphthyl, pyrrolopyridinyl, naphthyridinyl quinazolinyl, indazolyl, quinoxalinyl, pyridyl, pyrimidinyl, pyridonyl, pyrimidonyl, cinnolinyl, azaindolyl, azabenzothienyl, azaindazolyl, 7H-pyrrolo[2,3-d]pyrimidine, 1H-pyrazolo[3,4-d]pyrimidine or phenyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
- and
-
8. A compound of claim 7 wherein R2 is quinolinyl.
-
9. A compound of claim 1 having the structure of Formula IA
enantiomers, diastereomers and salts thereof. -
10. A compound of claim 9 wherein R1 is
(1) — - NR8R9, —
NR6CONR8R9, —
NR6COOR7, —
CN, or —
CONR8R9;
or(2) aryl, heteroaryl, heterocyclyl, alkenyl or alkynyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
- NR8R9, —
-
11. A compound of claim 10 wherein R1 is aryl, heteroaryl or heterocyclyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
-
12. A compound of claim 9 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
13. A compound of claim 11 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
14. A compound of claim 13 wherein
R1 is phenyl, naphthyl, naphthyridinyl, thienyl, benzothienyl, furan, benzofuranyl, pyridyl, pyrazinyl, pyrimidinyl, imidazolyl, triazolyl, quinoxalinyl, benzodioxolyl, benzodioxinyl dihydrobenzodioxinyl, indolinyl, indolyl, benzoimidazolyl, benzoisoxazol, benzoisothiozazol, benzoxazole, benzothiazol, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, morpholinyl, pyrrolidinyl, pyrazolyl, indazolyl, piperazinyl, piperadinyl, azetidinyl, pyranyl, pyridazinyl, dihydropyranyl, tetrahydropyranyl, quinolinyl, quinazolinyl, cinnolinyl, phthalazinyl, dihydroquinolinyl or isoquinolinyl any of which may be optionally independently substituted as allowed by valance with one or more R10; - and
R2 is quinolinyl, isoquinolinyl, naphthyl, pyrrolopyridinyl, naphthyridinyl quinazolinyl, indazolyl, quinoxalinyl, pyridyl, pyrimidinyl, pyridonyl, pyrimidonyl, cinnolinyl, azaindolyl, azabenzothienyl, azaindazolyl, 7H-pyrrolo[2,3-d]pyrimidine, 1H-pyrazolo[3,4-d]pyrimidine or phenyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
- and
-
15. A compound of claim 14 wherein R2 is quinolinyl.
-
16. A compound of claim 1 having the structure of Formula IB
enantiomers, diastereomers and salts thereof. -
17. A compound of claim 16 wherein R1 is
(1) — - NR8R9, —
NR6CONR8R9, —
NR6COOR7, —
CN, or —
CONR8R9;
or(2) aryl, heteroaryl, heterocyclyl, alkenyl or alkynyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
- NR8R9, —
-
18. A compound of claim 17 wherein R1 is aryl, heteroaryl or heterocyclyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
-
19. A compound of claim 16 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
20. A compound of claim 18 wherein
M is absent, — - O—
or —
NR6—
; andR2 is aryl or heteroaryl either of which may be optionally independently substituted as allowed by valance with one or more R10.
- O—
-
21. A compound of claim 20 wherein
R1 is phenyl, naphthyl, naphthyridinyl, thienyl, benzothienyl, furan, benzofuranyl, pyridyl, pyrazinyl, pyrimidinyl, imidazolyl, triazolyl, quinoxalinyl, benzodioxolyl, benzodioxinyl dihydrobenzodioxinyl, indolinyl, indolyl, benzoimidazolyl, benzoisoxazol, benzoisothiozazol, benzoxazole, benzothiazol, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, morpholinyl, pyrrolidinyl, pyrazolyl, indazolyl, piperazinyl, piperadinyl, azetidinyl, pyranyl, pyridazinyl, dihydropyranyl, tetrahydropyranyl, quinolinyl, quinazolinyl, cinnolinyl, phthalazinyl, dihydroquinolinyl or isoquinolinyl any of which may be optionally independently substituted as allowed by valance with one or more R10; - and
R2 is quinolinyl, isoquinolinyl, naphthyl, pyrrolopyridinyl, naphthyridinyl quinazolinyl, indazolyl, quinoxalinyl, pyridyl, pyrimidinyl, pyridonyl, pyrimidonyl, cinnolinyl, azaindolyl, azabenzothienyl, azaindazolyl, 7H-pyrrolo[2,3-d]pyrimidine, 1H-pyrazolo[3,4-d]pyrimidine or phenyl any of which may be optionally independently substituted as allowed by valance with one or more R10.
- and
-
22. A compound of claim 21 wherein R2 is quinolinyl.
-
23. A compound of claim 9 selected from
and salts thereof. -
24. A compound of claim 16 selected from
and salts thereof. -
25. A compound of claim 1 having the structure of Formula IC
enantiomers, diastereomers and salts thereof. -
26. A compound of claim 25 having the structure
and salts thereof. -
27. A compound of claim 1 having the structure of Formula IIA
enantiomers, diastereomers and salts thereof. -
28. A compound of claim 27 having the structure
and salts thereof. -
29. A compound of claim 1 having the structure of Formula ID
enantiomers, diastereomers and salts thereof. -
30. A compound of claim 29 selected from
and salts thereof -
33. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically-acceptable carrier.
-
34. A method of treating cancer in a subject, said method comprising administering an effective amount of a compound of claim 1.
-
35. The method of claim 34 comprising a combination with a compound selected from antibiotic-type agents, alkylating agents, antimetabolite agents, hormonal agents, immunological agents, interferon-type agents and miscellaneous agents.
-
36. A method of treating angiogenesis in a subject, said method comprising administering an effective amount of a compound of claim 1.
-
37. A method of treating proliferation-related disorders in a mammal, said method comprising administering an effective amount of a compound of claim 1.
-
38. A method of reducing blood flow in a tumor in a subject, said method comprising administering an effective amount of a compound of claim 1.
-
39. A method of reducing tumor size in a subject, said method comprising administering an effective amount of a compound of claim 1.
-
40. A method of treating diabetic retinopathy in a subject, said method comprising administering an effective amount of a compound of claim 1.
-
41. A method of treating inflammation in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a compound of claim 1.
-
42. A method of inhibiting T cell activation in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a compound of claim 1.
-
43. A method of treating arthritis, rheumatoid arthritis, psoriatic arthritis, or osteoarthritis in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a compound of claim 1.
-
44. A method of treating organ transplant, acute transplant or heterograft or homograft rejection, or transplantation tolerance induction in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a compound of claim 1.
-
45. A method of treating ischemic or reperfusion injury, myocardial infarction, or stroke in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a compound of claim 1.
-
46. A method of treating multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn'"'"'s disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto'"'"'s thyroiditis, Sjogren'"'"'s syndrome, autoimmune hyperthyroidism, Addison'"'"'s disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia greata, chronic actinic dermatitis, eczema, Behcet'"'"'s disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary'"'"'s syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis in a mammal, or diagnostic imaging in a mammal, the method comprising administering to the mammal a therapeutically-effective amount of a compound according to claim 1.
-
31. A compound of Formula V
enantiomers, diastereomers and salts thereof wherein n is an integer from 0 to 3; -
v is an integer from 0 to 2; L is absent, C1-6alkylene, C3-10cycloalkylene, C3-10heterocycloalkylene C2-8alkenylene or C2-8alkynylene any of which may be optionally independently substituted with one or more halo, —
OR7 or —
NR8R9 and further wherein any two substituent groups bound to the same tetravalent carbon atom may optionally combine to form a spiro-fused cycloalkyl or heterocyclyl ring;M is absent, —
O—
, —
S(O)v—
, —
NR6—
, —
C(═
O)NR6—
, —
NR6(C═
O)—
, —
SO2NR6—
, —
NR6SO2—
, provided that L and M are not both simultaneously absent;R1 is (1) halo, —
CN, —
NR6—
(C═
O)R7, —
NR6—
(C═
O)OR7, —
NR6—
(C═
O)NR8R9, —
(C═
O)NR8R9, —
(C═
O)OR7, —
(C═
O)R7, —
S(O)vR7—
SO2NR8R9, —
NR8R9 or —
OR7(2) cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; R2 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl or cycloalkylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valence; R3 is an optional substituent independently selected at each occurrence from halo, cyano, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, —
(C═
O)0-1OR7, —
(C═
O)0-1NR8R9, —
S(O)vR7, —
SO2NR8R9, —
C═
OR7, —
NR8C═
OR7, —
NR6—
C═
O—
NR8R9 and —
NR8SO2R7;R4*, R4 and R5 at each occurrence are independently H or one of the optional substituents listed in the definition of R3 provided that R4 and R5 cannot be simultaneously selected from —
OR7, —
NR8R9;
—
S(O)vR7, —
SO2NR8R9, —
NR8C═
OR7, —
NR6—
C═
O—
NR8R9 and —
NR8SO2R7;R6 at each occurrence is independently (1) H, or (2) alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; R7 at each occurrence is independently (1) H, or (2) alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl any of which may be optionally independently substituted with one or more R10 as allowed by valance; R8 and R9 at each occurrence are independently H, alkyl, cycloalkyl, heteroalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heteralkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl or R8 and R9 together with the nitrogen atom to which they are attached may combine to form a heterocyclyl ring; and R10 is one or more optional substituent independently selected at each occurrence as allowed by valance from halo, oxo, cyano, alkyl, haloalkyl, cycloalkyl, heterocyclyl, heteroaryl, aryl, heterocyclylalkyl, heteroarylalkyl, arylalkyl, —
(CR4R5)0-3OR7, —
(CR4R5)0-3NR8R9, —
(CR4R5)0-3N(R6)C═
OR7, —
(CR4R5)0-3N(R6)(C═
O)OR7, —
(CR4R5)0-3C═
ONR8R9, —
(CR4R5)0-3O(C═
O)NR8R9, —
(CR4R5)0-3C═
OR7, —
(CR4R5)0-3(C═
O)OR7, —
(CR4R5)0-3N(R6)C═
ONR8R9, —
(CR4R5)0-3S(O)vR7, —
(CR4R5)0-3SO2NR8R9 or —
(CR4R5)0-3NR6SO2R7. - View Dependent Claims (32)
-
Specification
-
- Resources
Litigation Campaign Assessment
Thank you for your request. You will receive a custom alert email when the Litigation Campaign Assessment is available.
×
-
Current AssigneeAmgen Inc.
-
Original AssigneeAmgen Inc.
-
InventorsNorman, Mark H., D'Angelo, Noel, Booker, Shon, Albrecht, Brian K., Kim, Tae-Seong, Bellon, Steven, Harmange, Jean-Christophe, Xi, Ning, Liu, Longbin, Siegmund, Aaron C., Yang, Kevin, Cheng, Alan C., D'Amico, Derin, Stec, Markian
-
Granted Patent
-
Time in Patent OfficeDays
-
Field of Search
-
US Class Current514/252.04
-
CPC Class CodesA61P 1/04 for ulcers, gastritis or re...A61P 11/02 Nasal agents, e.g. deconges...A61P 11/06 AntiasthmaticsA61P 13/12 of the kidneysA61P 17/00 Drugs for dermatological di...A61P 17/04 AntipruriticsA61P 17/06 AntipsoriaticsA61P 19/02 for joint disorders, e.g. a...A61P 25/00 Drugs for disorders of the ...A61P 29/00 Non-central analgesic, anti...A61P 3/10 for hyperglycaemia, e.g. an...A61P 35/00 Antineoplastic agentsA61P 37/06 Immunosuppressants, e.g. dr...A61P 37/08 Antiallergic agents antiast...A61P 43/00 Drugs for specific purposes...A61P 5/14 of the thyroid hormones, e....A61P 9/00 Drugs for disorders of the ...A61P 9/10 for treating ischaemic or a...C07D 237/16 Two oxygen atomsC07D 401/06 linked by a carbon chain co...View All
