IP Library › Granted Patent US 10,364,246
Granted Patent B2
US 10,364,246 · App. 16/243,874 · Granted Jul 30, 2019

Small molecule inhibitors of the JAK family of kinases

Inventors: Tatiana Koudriakova (Poway, CA); Kevin D. Kreutter (Arlington, MA); Kristi Leonard (Lansdale, PA); Michele C. Rizzolio (San Diego, CA); Russell C. Smith (San Diego, CA); Mark S. Tichenor (San Diego, CA); Aihua Wang (Jamison, PA)
Assignee: Janssen Pharmaceutica NV
C07D471/14
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Quick Facts
Patent No.
US 10,364,246
App. No.
16/243,874
Granted
Jul 30, 2019
Kind
B2
Abstract

2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.

Claims (26)

1. A compound selected from the group consisting of

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(2-hydroxy-2-methylpropyl)acetamide;

2-((1r,4r)-4-(2-(1H-Imidazol-4-yl)imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile;

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-((1-hydroxycyclopropyl)methyl)acetamide; and

pharmaceutically acceptable salts, and combinations thereof.

2. A compound as claimed in claim 1 , wherein said compound is selected from the group consisting of

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(2-hydroxy-2-methylpropyl)acetamide;

2-((1r,4r)-4-(2-(1H-Imidazol-4-yl)imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile; and

pharmaceutically acceptable salts, and combinations thereof.

3. A compound as claimed in claim 1 , wherein said compound is selected from the group consisting of

2-((1r,4r)-4-(2-(1H-Imidazol-4-yl)imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile;

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-((1-hydroxycyclopropyl)methyl)acetamide; and

pharmaceutically acceptable salts, and combinations thereof.

4. A compound as claimed in claim 1 , wherein said compound is selected from the group consisting of

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(2-hydroxy-2-methylpropyl)acetamide;

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-((1-hydroxycyclopropyl)methyl)acetamide;

pharmaceutically acceptable salts, and combinations thereof.

5. A compound selected from the group consisting of

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(2-hydroxy-2-methylpropyl)acetamide;

2-((1r,4r)-4-(2-(1H-Imidazol-4-yl)imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile;

2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-((1-hydroxycyclopropyl)methyl)acetamide; and

pharmaceutically acceptable co-crystals thereof.

6. A pharmaceutical composition comprising a therapeutically effective amount of a compound as claimed in claim 1 .

7. A pharmaceutical composition as claimed in claim 6 , wherein said compound is 2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(2-hydroxy-2-methylpropyl)acetamide.

8. A pharmaceutical composition as claimed in claim 6 , wherein said compound is 2-((1r,4r)-4-(2-(1H-Imidazol-4-yl)imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile.

9. A pharmaceutical composition as claimed in claim 6 , wherein said compound is 2-(1-((1r,4r)-4-(Cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-((1-hydroxycyclopropyl)methyl)acetamide.

Continuity (5)
Continuation 15843642 · Dec 15, 2017
Provisional Application 62596607 · Dec 8, 2017
Provisional Application 62592680 · Nov 30, 2017
Provisional Application 62435609 · Dec 16, 2016
Related Publication 20190185474A1 · Jun 20, 2019
Cited By (2)
US 12,202,831 US 12,390,451