Claims
- 1. A compound of formula (I),
- 2. A compound of claim 1 wherein
R3 and R4 are independently
(a) hydrogen, (b) alkyl, haloalkyl, (hydroxy)alkyl, cycloalkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl, (aryl)alkyl or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b; or (c) R3 and R4 together with the nitrogen atom to which they are attached combine to form a heterocyclo ring optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b.
- 3. A compound of claim 2 wherein
R6 is
(a) alkyl, alkenyl, alkynyl, heteroaryl or aryl any of which may be optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d; or (b) —OR7a.
- 4. A compound of claim 3 wherein R7a is alkyl optionally substituted with Z1c.
- 5. A compound of claim 4 wherein
Z1b, Z2b and Z3b are optional substituents independently selected from —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —N(Y1)—U2—NY2Y3, —N(Y4)—U2—Y1, or —N(Y4)—U2—H; Z1c is
(a) —OH, —OY1 or (b) aryl optionally substituted with —OH or —OY1; Z1d, Z2d and Z3d are optional substituents independently selected from
(a) cyano, halo, —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —S(O)tY1, —N(Y1)—U2—NY2Y3, —N(Y4)—U2—Y, or —N(Y4)—U2—H; (b) alkyl or alkoxy optionally substituted with one or more cyano, halo, —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —S(O)tY1, —N(Y1)—U2—NY2Y3, —N(Y4)—U2—Y1, or —N(Y4)—U2—H.
- 6. A compound of of claim 5 wherein
R3 is hydrogen; R4 is alkyl, haloalkyl, (hydroxy)alkyl, cycloalkyl, (cycloalkyl)alkyl, heterocyclo, (heterocyclo)alkyl, (aryl)alkyl or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b; R6 is
(a) alkynyl optionally substituted with Z1d where Z1d is aryl which may be further optionally independently substituted with one or more cyano, halo, —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —S(O)tY1, —N(Y1)—U2—NY2Y3, —N(Y4)—U2—Y1, or —N(Y4)—U2—H; (b) aryl optionally independently substituted as valence allows with one or more Z1d, Z2d an Z3d; (c) —OR7a; or (d) heterocyclo optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d; Z1b, Z2b and Z3b are optional substituents independently selected from —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —N(Y4)—U2—Y, or —N(Y4)—U2—H where
U1 is a bond, U2 is —U3—C(O)—U4— or —U3—C(O)O—U4— and U3 and U4 are independently a bond or alkylene; Z1c is
(a) —OY1 where Y1 is aryl, or (b) aryl optionally substituted with —OH or —OY1 where Y1 is alkyl; Z1d, Z2d and Z3d are optional substituents independently selected from
(a) cyano, halo, —OH, —OY1, —C(O)tH, —C(O)tY1, —S(O)tY1, or (b) alkyl or alkoxy optionally substituted with one or more cyano, halo, —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —S(O)tY1, —N(Y4)—U2—Y1, or —N(Y4)—U2—H where
U1 is a bond, or —C(O)—, U2 is —U3—C(O)—U4—, —U3—C(O)O—U4—, or —U3—SO2—U4—, and U3 and U4 are indepedently a bond or alkylene.
- 7. A compound of claim 6 wherein
R1 is alkyl; R2 is hydrogen; and R5 is hydrogen or alkyl.
- 8. A compound of claim one having the formula IIa
- 9. A compound of claim 8 wherein
R3 and R4 are independently
(a) hydrogen, (b) alkyl, haloalkyl, (hydroxy)alkyl, cycloalkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl, (aryl)alkyl or (heteroaryl)alkyl and of which may be optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b; or (c) R3 and R4 together with the nitrogen atom to which they are attached combine to form a heterocyclo ring optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b.
- 10. A compound of claim 9 wherein
Z1b, Z2b and Z3b are optional substituents independently selected from —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —N(Y1)—U2—NY2Y3, —N(Y4)—U2—Y1, or —N(Y4)—U2—H.
- 11. A compound of claim 10 wherein
R1 is alkyl; R2 is hydrogen; and R5 is hydrogen or alkyl.
- 12. A compound of claim 1 having formula IIb
- 13. A compound of claim 12 wherein
R3 and R4 are independently
(a) hydrogen, (b) alkyl, haloalkyl, (hydroxy)alkyl, cycloalkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl, (aryl)alkyl or (heteroaryl)alkyl and of which may be optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b; or (c) R3 and R4 together with the nitrogen atom to which they are attached combine to form a heterocyclo ring optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b.
- 14. A compound of claim 13 wherein
Z1b, Z2b and Z3b are optional substituents independently selected from —OH, —OY1, —U1—NY2Y3, —C(O)tH, —C(O)tY1, —N(Y1)—U2—NY2Y3, —N(Y4)—U2—Y1, or —N(Y4)—U2—H.
- 15. A compound of claim 14 wherein
R1 is alkyl; R2 is hydrogen; and R5 is hydrogen or alkyl.
- 16. A pharmaceutical composition comprising (a) at least one compound according to claim 1, or a pharmaceutically acceptable salt, hydrate or prodrug thereof, and (b) a pharmaceutically-acceptable carrier or diluent.
- 17. A method of treating an inflammatory or immune disease or disorder comprising administering to a mammal in need thereof a therapeutically-effective amount of at least one compound according to claim 1.
- 18. The method of claim 17 in which the inflammatory or immune disease is selected from rheumatoid arthritis, asthma, inflammatory bowel disease, chronic obstructive pulmonary disease, and psoriasis.
- 19. A method of treating cancer comprising administering to a mammal in need thereof a therapeutically-effective amount of at least one compound according to claim 15.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] The present application claims the priority benefit of U.S. Provisional Application No. 60/449,770, filed Feb. 25, 2003, which is expressly incorporated fully herein by reference.
Provisional Applications (1)
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Number |
Date |
Country |
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60449770 |
Feb 2003 |
US |
Patent Application
20040204432
