2,1-benzisothiazoline 2,2-dioxides

US6339098B1 · kind B1 · utility

Assignees

• Amerimas Home Products, Inc. · US
• Ligand Pharmaceuticals Incorporated · US

Inventors

• Mark A. Collins · Norristown, US
• Valerie A. Mackner · Conshohocken, US
• Jay E. Wrobel · Lawrenceville, US
• James P. Edwards · San Diego, US
• Todd K. Jones · Solana Beach, US
• Christopher M. Tegley · Thousand Oaks, US
• Lin Zhi · San Diego, US

Key dates

• Filing date: Apr 19, 2000
• Grant date: Jan 15, 2002
• Expiry date: Apr 19, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, heteroarylalkyl, and alkynyl. R1 and R2 may be taken together to form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)PCH2—, O(CH2)qO—, —CH2CH2OCH2CH2—, —CH2CH2NR7CH2CH2—. R1 and R2 may be taken together to form a double bond, the double bond having two methyl groups bonded to the terminal end, having a cycloalkyl group bonded to the terminal end, having an oxygen bonded to the terminal end, or having a cycloether bonded to the terminal end; or a double bond. R3 is hydrogen, hydroxyl, NH2, alkyl, substituted alkyl, alkenyl, alkynyl, substituted or, CORA. R4 is hydrogen, halogen, —CN, —NH2, alkyl, substituted alkyl, alkoxy, alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is a trisubstituted phenyl ring having the structure, or is a five or six membered heteroaryl ring, containing 1, 2, or 3 heteroatoms sel…