IP Library Granted Patent US 8,748,401
Granted Patent B2
US 8,748,401 · App. 13/917,124 · Granted Jun 10, 2014

Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Inventors: James D. Rodgers (Landenberg, PA); Adam Shilling (Wilmington, DE); Argyrios G. Arvanitis (Kennett Square, PA); Stacey Shepard (Wilmington, DE); Laurine G. Galya (Wilmington, DE); Mei Li (Wilmington, DE); Frank M. Nedza (Wilmington, DE)
Assignee: Incyte Corporation
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Quick Facts
Patent No.
US 8,748,401
App. No.
13/917,124
Granted
Jun 10, 2014
Kind
B2
Abstract

The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.

Claims (31)

1. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

one C—H group is replaced with:

or,

two C—H groups are each independently replaced with C—OH and one C—H group is replaced with:

and pharmaceutically acceptable salts thereof.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein one C—H group is replaced with

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein one saturated C—H group is replaced with

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein two C—H groups are each independently replaced with C—OH and one C—H group is replaced with:

5. A compound of claim 1 , which is:

6-(3-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid

or a pharmaceutically acceptable salt of any of the aforementioned.

6. A compound of claim 1 , selected from:

6-(1-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

6-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyano-1-cyclopentylethoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

6-(2-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

6-(2-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-cyano-2-cyclopentylethoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid; and

6-(3-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

or a pharmaceutically acceptable salt of any of the aforementioned.

7. A compound which is:

6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid

or a pharmaceutically acceptable salt of any of the aforementioned.

8. A compound selected from:

6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-6-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid; and

6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;

or a pharmaceutically acceptable salt of any of the aforementioned.

9. The compound of claim 1 , or pharmaceutically acceptable salt thereof, which is substantially isolated.

10. A composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

11. The composition of claim 10 , which is suitable for oral administration.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE OMMISSION OF SECOND RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 035292 FRAME: 0004. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jul 2, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 036054/0696 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION AND INCYTE CORPORATION
Reel/Frame 035924/0004 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2013
From: RODGERS, JAMES D.; SHILLING, ADAM; ARVANITIS, ARGYRIOS G.; SHEPARD, STACEY; GALYA, LAURINE G.; LI, MEI; NEDZA, FRANK M.
To: INCYTE CORPORATION
Reel/Frame 031201/0978 →
Continuity (4)
Continuation 12901001 · Oct 8, 2010
Provisional Application 61250387 · Oct 9, 2009
Provisional Application 61316218 · Mar 22, 2010
Related Publication 20130345157A1 · Dec 26, 2013