304875-19-2Relevant articles and documents
Thio-oxindole derivatives
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Page column 58, (2010/11/30)
This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1and R2are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl;1-propynyl; or3-propynyl; or R1and R2are joined to form an alkyl, alkenyl or heterocyclic ring; or R1and R2together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3is H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, alkynyl, substituted alkynyl, or CORA; RAis H, C1to C3alkyl, substituted C1to C3alkyl, C1to C3alkoxy, substituted C1to C3alkoxy, C1to C3aminoalkyl, or substituted C1to C3aminoalkyl; R4is H, halogen, CN, NH2, NO2, C1to C6alkyl, or substituted C1to C6alkyl, C1to C6alkoxy, substituted C1to C6alkoxy, C1to C6aminoalkyl, or substituted C1to C6aminoalkyl; R5is optionally substituted and selected from a benzene ring, a five or six membered heterocyclic ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2or NR6; or an indol-4-yl, indol-7-yl or benzo-2-thiophene moiety; Q1is S, NR7, CR8R9; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
