Therapeutic compounds
OwnerM. Uckun Fatihinventor
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Abstract
The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.
Claims27
A method of treating graft versus host disease in a mammal comprising:
- administering to a mammal a graft versus host disease treating effective amount of;
- (a) methotrexate;
- and
- (b) a compound of formula I:
- 7
- wherein
- X is selected from the group consisting of HN, R11N, S, O, CH2, and R11CH;
- R11 is (C1-C4)alkyl or (C1-C4)alkanoyl;
- R1-R5 are each independently selected from the group consisting of hydrogen, hydroxy and halo;
- R6, R7, and R8 are each independently selected from the group consisting of hydrogen, hydroxy, mercapto, amino, nitro, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylthio and halo;
- and
- R9 and R10 are each independently hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, halo or (C1-C4)alkanoyl;
- or R9 and R10 together are methylenedioxy;
- or a pharmaceutically acceptable salt thereof.
A method comprising;
- administering to a mammal a graft versus host disease treating effective amount of;
- (a) methotrexate;
- and
- (b) a compound of formula II:
- 8
- or a pharmaceutically acceptable salt thereof.
A method for prophylactically treating a mammal to prevent graft versus host disease comprising:
- administering to a mammal a graft versus host disease prophylactically effective amount of a compound of formula I:
- 9
- wherein
- X is selected from the group consisting of HN, R11N, S, O, CH2, and R11CH;
- R11 is (C1-C4)alkyl or (C1-C4)alkanoyl;
- R1-R5 are each independently selected from the group consisting of hydrogen, hydroxy and halo;
- R6, R7, and R8 are each independently selected from the group consisting of hydrogen, hydroxy, mercapto, amino, nitro, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylthio and halo;
- and
- R9 and R10 are each independently hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, halo or (C1-C4)alkanoyl;
- or R9 and R10 together are methylenedioxy;
- or a
- pharmaceutically acceptable salt thereof.
A composition comprising:
- (a) a therapeutically effective amount of methotrexate;
- and
- (b) a therapeutically effective amount of a compound of formula I:
- 10
- wherein
- X is selected from the group consisting of HN, R11N, S, O, CH2, and R11CH;
- R11 is (C1-C4)alkyl or (C1-C4)alkanoyl;
- R1-R5 are each independently selected from the group consisting of hydrogen, hydroxy and halo;
- R6, R7, and R8 are each independently selected from the group consisting of hydrogen, hydroxy, mercapto, amino, nitro, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylthio and halo;
- and
- R9 and R10 are each independently hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, halo or (C1-C4)alkanoyl;
- or R9 and R10 together are methylenedioxy;
- or a pharmaceutically acceptable salt thereof.
A composition comprising;
- (a) a therapeutically effective amount of methotrexate;
- and
- (b) a therapeutically effective amount of a compound of formula II:
- 11
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising:
- (a) a therapeutically effective amount of methotrexate;
- (b) a therapeutically effective amount of a compound of formula I:
- 12
- wherein
- X is selected from the group consisting of HN, R11N, S, O, CH2, and R11CH;
- R11 is (C1-C4)alkyl or (C1-C4)alkanoyl;
- R1-R5 are each independently selected from the group consisting of hydrogen, hydroxy and halo;
- R6, R7, and R8 are each independently selected from the group consisting of hydrogen, hydroxy, mercapto, amino, nitro, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylthio and halo;
- and
- R9 and R10 are each independently hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, halo or (C1-C4)alkanoyl;
- or R9 and R10 together are methylenedioxy;
- or a pharmaceutically acceptable salt thereof;
- and
- (c) a pharmaceutically acceptable carrier.
A pharmaceutical composition comprising;
- (a) a therapeutically effective amount of methotrexate;
- and
- (b) a therapeutically effective amount of a compound of formula II:
- 13
- or a pharmaceutically acceptable salt thereof;
- and
- (c) a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.