Document Type and Number:
Japanese Patent JPH07506363
Kind Code:
A
Abstract:
PCT No. PCT/US93/03778 Sec. 371 Date Oct. 28, 1994 Sec. 102(e) Date Oct. 28, 1994 PCT Filed Apr. 22, 1993 PCT Pub. No. WO93/22333 PCT Pub. Date Nov. 11, 1993Invented are 17 alpha and 17 beta -substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following (I) wherein Z is alpha or beta in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R is a) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: -OC6-C12aryl, -OC1-C4alkyl, halogen, carboxy and -S(O)nR7, where n is 0-2 and R7 is hydrogen or C1-4alkyl; b) C3-C8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of: -OC6-C12aryl, -(CH2)mOH, -OC1-C4alkyl, C6-C12aryl, C1-C4alkyl, trifluoromethyl, halogen, -(CH2)pCOOH, -S(O)nR7 and protected -OH, where m is 0-4, p is 0-3, n is 0-2 and R7 is hydrogen or C1-4alkyl; or c) C4-C12aryl, optionally containing one or more heteroatoms, provided that when C is 4 the aromatic ring contains at least one heteroatom, and optionally substituted with one or more substituents selected from the group consisting of: -OC6-C12aryl, -(CH2)mOH, C6-C12aryl, C1-C4alkyl, -OC1-C4alkyl, trifluoromethyl, halogen, -(CH2)pCOOH, -S(O)nR7 and protected -OH, where m is 0-4, p is 0-3, n is 0-2 and R7 is hydrogen or C1-4alkyl. Also invented are pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5 alpha -reductase. Also invented are intermediates and processes used in preparing these compounds.
Application Number:
JP51936793A
Publication Date:
July 13, 1995
Filing Date:
April 22, 1993
Export Citation:
International Classes:
A61K8/49; A61K31/56; A61K31/57; A61K8/00; A61Q5/00; A61Q9/04; C07J1/00; C07J3/00; C07J5/00; C07J7/00; C07J9/00; C07J17/00; C07J31/00; C07J33/00; C07J41/00; C07J43/00; C07C69/00; C07J63/00; (IPC1-7): C07J5/00; A61K7/06; A61K31/57