IP Library › Patent Application 16583938
Patent Application
App. No. 16/583,938

METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE

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Patent No.
US None
App. No.
16/583,938
Abstract

The present invention provides active metablites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Claims (29)

1 - 6 . (canceled)

7 . A method of treating an autoimmune skin disease in a patient, comprising administering to said patient a therapeutically effective amount of a compound selected from:

3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(3-hydroxycyclopentyl)-propanenitrile;

3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(2-hydroxycyclopentyl-)propanenitrile; and

3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(3-oxocyclopentyl)-propanenitrile,

or a pharmaceutically acceptable salt thereof,

and a pharmaceutically acceptable carrier.

8 - 10 . (canceled)

11 . The method of claim 7 , wherein said autoimmune skin disease is bullous skin disorder.

12 . The method of claim 11 , wherein said bullous skin disorder is pemphigus vulgaris (PV) or bullous pemphigoid (BP).

13 . (canceled)

14 . The method of claim 7 , wherein said autoimmune skin disease is atopic dermatitis, psoriasis, skin sensitization, skin irritation, skin rash, contact dermatitis or allergic contact sensitization.

15 - 53 . (canceled)

54 . The method of claim 11 , wherein the bullous skin disorder is pemphigus vulgaris (PV).

55 . The method of claim 11 , wherein the bullous skin disorder is bullous pemphigoid (BP).

56 . The method of claim 14 , wherein the autoimmune skin disease is atopic dermatitis.

57 . The method of claim 14 , wherein the autoimmune skin disease is psoriasis.

58 . The method of claim 7 , wherein about 5 to about 1000 mg of the compound, or pharmaceutically acceptable salt thereof, is administered to the patient.

59 . The method of claim 7 , further comprising administering to the patient at least one additional therapeutic agent.

60 . The method of claim 59 , wherein the therapeutic agent is administered to a patient simultaneously or sequentially.

61 . The method of claim 59 , wherein said therapeutic agent is an immunosuppressant.

62 . The method of claim 59 , wherein said therapeutic agent is a steroid.

63 . The method of claim 59 , wherein said therapeutic agent is a corticosteroid.

64 . The method of claim 63 , wherein said corticosteroid is dexamethasone or prednisone.

65 . The method of claim 7 , wherein the compound is 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(3-hydroxycyclopentyl)propanenitrile.

66 . The method of claim 7 , wherein the compound is 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(2-hydroxycyclopentyl)propanenitrile.

67 . The method of claim 7 , wherein the compound is 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(3-oxycyclopentyl)propanenitrile.

68 . The method of claim 7 , wherein the pharmaceutical composition is suitable for oral administration.

69 . The method of claim 7 , wherein the pharmaceutical composition is in tablet form.