Patent ID: 6723715
Filing Date: 2004-04-20
Classification: A61P,C07J

Abstract:
14,15-cyclopranoandrostanes of the 19-norandrostane series of the formula (I) wherein R1 is a hydrogen atom, a hydroxy group, C1-10-alkyl, a C1-10-alkyloxy, a C1-15 acyloxy, a C4-15-aryloxy, a C7-15-aralkyloxy or a C7-15-alkylaryloxy group;R2 represents a hydrogen atom, a hydroxy group, a C1-10 alkyl group, a C1-10 acyl group, a C1-10 acyloxy group, a C6-15 aryl group, a C7-15 aralkyl group, a C7-15 alkylaryl group, a â€”(CH2)nCH2Y group with n=0, 1 or 2 and Y representing a halogen atom or a pseudohalogen; a (CH2)mCH&boxH;CH(CH2)pR6 group with m=0,1, 2 or 3 and p=0, 1 or 2 and R6 representing a hydrogen atom, a C1-10-alkyl group, a C6-15 aryl group, a C7-15 aralkyl group, a C7-15 alkylaryl group, a hydroxyl group, a C1-10 alkyloxy group, a C1-10 acyloxy group; a â€”(CH2)oCâ‰¡CR7 group with o=0, 1 or 2 and R7 representing a hydrogen atom, a halogen atom, a C1-10 alkyl group, a C6-15 aryl group, a C7-15 aralkyl group, a C7-15 alkylaryl group or a C1-10 acyl group; or R1 and R2 together represent a keto group, a methylene group, a difluoromethylene group or, with inclusion of C-17, a spirooxirane or a 2,2-dimethyl-1,3-dioxolane; R3 represents a hydrogen atom or an &agr;-C1-10 alkyl group or &bgr;-C1-10 alkyl group; R4 represents a halogen atom, a pseudohalogen, a hydroxy group or a perfluoroalkyl group; R5 represents a C1-4 alkyl group, wherein an &agr;-cyclopropane or a &bgr;-cyclopropane group is between C-14 and C-15; and wherein optionally a 9,10-double bond is present and optionally an 11,12-double bond is present, with the proviso that, if both the 9,10-double bond and the 11,12-double bond are present or if only the 11,12-double bond is present, then R4 can be a hydrogen atom in addition to said halogen atom, said pseudohalogen, said hydroxy group or said perfluoroalkyl group; and with the further proviso that, if R5 is a methyl group, then R4 can be a hydrogen atom in addition to said halogen atom, said pseudohalogen, said hydroxy group or said perfluoroalkyl group; or pharmaceutically tolerated salts thereof.