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

Patent metadata

Field	Value
Publication number	US-11472809-B2
Application number	US-202017014533-A
Country	US
Kind code	B2
Filing date	Sep 8, 2020
Priority date	Feb 24, 2016
Publication date	Oct 18, 2022
Grant date	Oct 18, 2022

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 structureor a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.

First claim

What is claimed is:

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.

Assignees

• Pfizer

Inventors

• Brown Matthew Frank
• DERMENCI Alpay
• Fensome Andrew
• Gerstenberger Brian Stephen
• Hayward Matthew Merrill
• Owen Dafydd Rhys
• Wright Stephen Wayne
• Xing Li Huang
• Yang Xiaojing

Classifications

• A61P13/12

  of the kidneys · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P17/06

  Antipsoriatics · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title