Diazabicyclooctane derivatives and therapeutic uses thereof

US6531468B2 · kind B2 · utility

Assignee

• PFIZER INC. · US

Inventors

• Anton Fliri · Stonington, US
• Randall J. Gallaschun · Lebanon, US

Key dates

• Filing date: Aug 1, 2001
• Grant date: Mar 11, 2003
• Expiry date: Aug 1, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides diazabicyclooctane derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein the group represents R1 and R2 are selected independently from H, (C1-C6)alkyl, (C1-C6)fluoroalkyl, halogen (e.g., F. Cl, Br, I), cyano, nitro, O—(C1-C6)alkyl, O—(C1-C6)fluoroalkyl, —NHC(O)R4 and —OR4, where R4 and R5 are selected independently from H, (C1-C6)alkyl, and a 5- to 7-membered aryl or heteroaryl ring, or R1 and R2 together with the atoms to which they are attached, form a carbocyclic 5- or 6-membered ring or a heterocyclic 5- or 6-membered ring; andR3 is selected from the group consisting of H, (C1-C6)alkyl, (CH2)m-aryl or (CH2)m-heteroaryl, wherein m is an integer from 1 to 4, each aryl or heteroaryl group optionally substituted with Cl, Br, CN, CF3, O—(C1-C6)alkyl, (C1-C6)alkyl, sulfonyl(C1-C6)alkyl, —CO(C1-C6)alkyl, —CONH2, —CONH(C1-C6)alkyl, —CON((C1-C6)alkyl)2, or CH(OH)(C1-C6)alkyl.The invention also relates to pharmaceutical compositions of a compound of formula (I), and methods of use thereof in the treatment of diseases, conditions or disorders of the central nervous system. Fu…