INHIBITORS OF 5-ALPHA-TESTOSTERONE REDUCTASE

• Main Authors: HAFFNER, CURT, DALE, MALONEY, PATRICK, REED, ANDREWS, ROBERT, CARL, FRYE, STEPHEN, VERNON, CRIBBS, CYNTHIA, MARKERT
• Format: Patent
• Language: English; French; German
• Published: 22.04.1998
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC USE OF COSMETICS OR SIMILAR TOILETPREPARATIONS; STEROIDS

PCT No. PCT/US92/11109 Sec. 371 Date Aug. 15, 1994 Sec. 102(e) Date Aug. 15, 1994 PCT Filed Dec. 18, 1992 PCT Pub. No. WO/9313124 PCT Pub. Date Jul. 8, 1993The present invention relates to certain substituted 17 beta -substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) (I) (IG) wherein R1 and R2 are i) independently hydrogen or lower alkyl and the bond between the carbons bearing R1 and R2 is a single or a double bond, or ii) taken together are a -CH2- group to form a cyclopropane ring, and the bond between the carbons bearing R1 and R2 is a single bond; R3c is hydrogen; R4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, -(CH2)mCO2R16, -(CH2)mAra, -(CH2)n'CONR17R18, -(CH2)n'NR17R18 or -(CH2)n'OR16, wherein R16 is hydrogen, lower alkyl or lower alkenyl; R17 and R18 are independently hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ara is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5; R19 and R20 are independently hydrogen or lower alkyl, or taken together R19 and R20 form a carbonyl group (=O); R5c is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR21R22, wherein R21 and R22 are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations.