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

US10822341B2 · kind B2 · utility

Assignee

• PFIZER INC. · US

Inventors

• Matthew Frank Brown · Stonington, US
• Alpay Dermenci · East Lyme, US
• Andrew Fensome · Wayne, US
• Brian Stephen Gerstenberger · Brookline, US
• Matthew Merrill Hayward · Old Lyme, US
• Dafydd Rhys Owen · Concord, US
• Stephen Wayne Wright · Old Lyme, US
• Li Xing · Lexington, US
• Xiaojing Yang · Waterford, US

Key dates

• Filing date: Nov 6, 2018
• Grant date: Nov 3, 2020
• Expiry date: Nov 6, 2038

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A′ and A″ are independently O, C═O, C—R′ or N—R″, where R′ and R″ may independently be H, amino, —NR7COR6, COR6, —CONR7R8, C1-C6 alkyl, or hydroxy(C1-C6 alkyl), and R″ may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A′ and A″ is O or C═O; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), formyl, heteroaryl, heterocyclic, —COR6, —OCOR6, —COOR6, —NR7COR6, —CONR7R8, and —(CH2)n—W, where W is cyano, hydroxy, C3-C8 cycloalkyl, —SO2NR7R8, and —SO2—R9, where R9 is C1-C6 alkyl, C3-C8 cycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C1-C6 alkyl; X is C—R3 or N, where R3 may be H or C1-C6 alkyl; R4 and R5 are independently H, amino, C1-C6 alkyl, or h…