IP Library › Granted Patent US 11,472,809
Granted Patent B2
US 11,472,809 · App. 17/014,533 · Granted Oct 18, 2022

Pyrazolo[1,5-a]pyrazin-4-yl derivatives

Inventors: Matthew Frank Brown (Stonington, CT); Alpay Dermenci (East Lyme, CT); Andrew Fensome (Harvard, MA); Brian Stephen Gerstenberger (Brookline, MA); Matthew Merrill Hayward (Old Lyme, CT); Dafydd Rhys Owen (Concord, MA); Stephen Wayne Wright (Old Lyme, CT); Li Huang Xing (Lexington, MA); Xiaojing Yang (Waterford, CT)
Assignee: Pfizer Inc.
C07D487/04A61K31/4985
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Quick Facts
Patent No.
US 11,472,809
App. No.
17/014,533
Granted
Oct 18, 2022
Kind
B2
Abstract

There is a method for treating a psoriasis. A compound is administered in a therapeutically effective amount to a subject suffering therefrom. The compound has the structure or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.

Claims (10)

1. A method of treating a psoriasis comprising administering to a subject suffering therefrom a therapeutically effective amount of a compound having the structure (Ic):

or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein:

R″ is H, —COR 6 , —CONR 7 R 8 , C 1 -C 6 alkyl-, or hydroxy(C 1 -C 6 alkyl)-;

R 2 is selected from the group consisting of H, C 1 -C 6 alkyl, C1-C 6 alkoxy-, hydroxy(C 1 -C 6 alkyl)-, phenyl(C 1 -C 6 alkyl-), formyl, heteroaryl, heterocyclic, —COR 6 , —OCOR 6 , —COOR 6 , —NR 7 COR 6 , —CONR 7 R 8 , and —(CH 2 ) n —W, where W is cyano, hydroxy, C 3 -C 8 cycloalkyl, —SO 2 NR 7 R 8 , and —SO 2 —R 9 , where R 9 is C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C 1 -C 6 alkyl;

R 3 is H, C 1 -C 6 alkyl, amino, cyano, or C 1 -C 6 alkoxy-;

R 5 is H, amino, C 1 -C 6 alkyl, or hydroxy(C 1 -C 6 alkyl)-;

R 6 , R 7 and R 8 are each independently H, C 1 -C 6 alkyl, C 1 -C 4 alkoxy(C 1 -C 6 alkyl)-, or C 3 -C 8 cycloalkyl, said C 1 -C 6 alkyl is optionally substituted by halo, CN or hydroxy; or, R 7 and R 8 together with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C 1 -C 6 alkyl; and, n is 0, 1, 2 or 3.

2. The method of claim 1 , wherein R″ is C 1 -C 6 alkyl.

3. The method of claim 1 , wherein R″ is C 1 -C 6 alkyl and R 5 is H.

4. The method of claim 1 , wherein the compound is (1r,3r)-3-(cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile, or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2021
From: BROWN, MATTHEW FRANK; DERMENCI, ALPAY; FENSOME, ANDREW; GERSTENBERGER, BRIAN STEPHEN; HAYWARD, MATTHEW MERRILL; OWEN, DAFYDD RHYS; WRIGHT, STEPHEN WAYNE; XING, LI HUANG; YANG, XIAOJING
To: PFIZER INC.
Reel/Frame 058393/0427 →
Continuity (4)
Continuation 16181596 · Nov 6, 2018
Division 15437618 · Feb 21, 2017
Provisional Application 62299130 · Feb 24, 2016
Related Publication 20200399281A1 · Dec 24, 2020