Heteroaryl Substituted Pyrrolo[2,3-B] Pyridines And Pyrrolo[2,3-B] Pyrimidines As Janus Kinase Inhibitors
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines 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.
1 - 88 . (canceled)
89 . A method of treating a skin disorder in a patient, comprising administering to the skin of said patient a compound, which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof; wherein said administering is topical administration.
90 . The method of claim 89 , wherein the compound is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.
91 . The method of claim 90 , wherein said topical administration is transdermal administration.
92 . The method of claim 90 , wherein said topical administration is transdermal administration epidermal administration.
93 . The method of claim 90 , wherein said compound or salt is administered in the form of a pharmaceutical composition comprising said compound or salt and a pharmaceutically acceptable carrier.
94 . The method of claim 93 , wherein said pharmaceutical composition is a cream.
95 . The method of claim 93 , wherein said pharmaceutical composition is an ointment.
96 . The method of claim 93 , wherein said pharmaceutical composition is a lotion.
97 . The method of claim 93 , wherein said pharmaceutical composition is a gel.
98 . The method of claim 90 , wherein a therapeutically effective amount of said compound or salt is administered to the skin of said patient.
99 . The method of claim 98 , wherein the skin disorder is psoriasis.
100 . The method of claim 98 , wherein the skin disorder is psoriasis vulgaris.
101 . The method of claim 98 , wherein skin disorder is atopic dermatitis, skin rash, skin irritation, or skin sensitization.
102 . The method of claim 90 , wherein the individual is need of inhibition of JAK1 and/or JAK2.
103 . A pharmaceutical composition, comprising a compound, which is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, wherein said pharmaceutical composition is suitable for topical administration.
104 . The pharmaceutical composition of claim 103 , wherein the compound is a pharmaceutical salt of (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile.
105 . The pharmaceutical composition of claim 103 , wherein said composition is a cream.
106 . The pharmaceutical composition of claim 103 , wherein said composition is an ointment.
107 . The pharmaceutical composition of claim 103 , wherein said composition is a lotion.
108 . The pharmaceutical composition of claim 103 , wherein said composition is a gel.
109 . The pharmaceutical composition of claim 103 , wherein said composition is suitable for epidermal administration.
110 . A method of treating a JAK-associated disease in a patient, comprising administering to the skin of said patient a compound, which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof; wherein said administering is topical administration.
111 . The method of claim 110 , wherein the compound is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.
112 . The method of claim 111 , wherein said topical administration is transdermal.
113 . The method of claim 111 , wherein said topical administration is epidermal.
114 . The method of claim 111 , wherein said compound or salt is administered in the form of pharmaceutical composition comprising said compound or salt and a pharmaceutically acceptable carrier.
115 . The method of claim 114 , wherein said pharmaceutical composition is a cream.
116 . The method of claim 114 , wherein said pharmaceutical composition is an ointment.
117 . The method of claim 114 , wherein said pharmaceutical composition is a lotion.
118 . The method of claim 114 , wherein said pharmaceutical composition is a gel.
119 . The method of claim 111 , wherein the JAK-associated skin disease in a patient is associated with inhibiting JAK1 and/or JAK2 in a patient in need thereof.
120 . A method of inhibiting JAK1 and/or JAK2 associated with a skin disease in a patient in need thereof, comprising administering to the skin of said patient a compound, which is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof; wherein said administering is topical administration.