Patent ID: 6365582
Filing Date: 2002-04-02
Classification: A61P,C07J

Abstract:
An S-substituted 11&bgr;-benzaldoxime-estra-4,9-dien-carbonic acid thioester compound of the formula I: or a pharmaceutically acceptable salt thereof; whereinR1 is an alkyl radical having 1 to 10 carbon atoms, an aryl radical having 6 to 10 carbon atoms or an alkylaryl or arylalkyl radical each having 7 to 10 carbon atoms; R2 is a hydrogen atom or an alkyl radical having 1 to 3 carbon atoms; R3 is a hydroxyl group, an O-alkyl group having 1 to 10 carbon atoms, an O-aryl group having 6 to 10 carbon atoms, an O-aralkyl group or an O-alkylaryl group, each having 7 to 10 carbon atoms, â€”OCOR5, â€”OCONHR5 or â€”OCOOR5; R4 is a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aralkyl or alkylaryl group each having 7 to 10 carbon atoms, â€”Câ‰¡CCH2OH, â€”(CH2)nCH2Y, â€”OR5, â€”OCOR6, â€”(CH2)mâ€”CH&boxH;CH(CH2)pâ€”R6â€² or â€”(CH2)oCâ‰¡CR7; wherein n=0, 1 or 2; m=0, 1, 2 or 3; p=0, 1 or 2; and o=0, 1 or 2; wherein Y is a fluorine atom, a chlorine atom, a bromine atom, an iodine atom, a cyano group, an amino group, an azido group, a thiocyano group, â€”OR6, â€”SR6, â€”(CO)OR6 or â€”(CO)SR6; wherein R6 is a hydrogen atom, an alkyl radical having 1 to 10 carbon atoms, an aryl radical having 6 to 10 carbon atoms, an alkylaryl or arylalkyl radical each having 7 to 10 carbon atoms or â€”COR5; wherein R6â€² is a hydrogen atom, an alkyl radical having 1 to 10 carbon atoms, an aryl radical having 6 to 10 carbon atoms, an alkylaryl or arylalkyl radical each having 7 to 10 carbon atoms, â€”OR5, â€”OC OR5 or â€”COR5; wherein R7 is a hydrogen atom, a fluorine atom, a chlorine atom, a bromine atom, an iodine atom, an alkyl radical having 1 to 10 carbon atoms, an aryl radical having 6 to 10 carbon atoms, an alkylaryl or arylalkyl radical each having 7 to 10 carbon atoms, â€”OR5, â€”CH2OR5 or â€”OCOR5; and wherein R5 is a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms or an aralkyl or alkylaryl group each having 7 to 10 carbon atoms; or, alternatively, wherein R3 and R4 taken together form an optionally substituted five-member or six-member ring having at least one carbon atom and from 0 to 4 hetero atoms, and each of said hetero atoms is selected from the group consisting of oxygen, sulfur, selenium, tellurium, nitrogen, phosphorus, silicon and germanium.