Abstract: Described are new 16-substituted and 7,16-disubstituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.

Abstract: Compounds of the formula ##STR1## are inhibitors of 5.alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: Selected 17.beta.-Polyaroyl-4-aza-5.alpha.-androst-1-en-3-ones as steroidal reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethylR.sup.2 is polycyclic aromatic radical which can be substituted with one or more of: --OH, protected --OH, --OC.sub.1 --C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, or nitro, wherein the doted line represents a double bond which can be present, and pharmaceutically acceptable salts or esters thereof, and a pharmaceutical formulation. The above compounds are active as steroidal reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

Abstract: Specific 17.beta.-thiobenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as antiandrogenic agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is phenyl substituted with one or more of: --SH, --SC.sub.1 --C.sub.4 alkyl, --SO--C.sub.1 --C.sub.4 alkyl, --SO.sub.2 --C.sub.1 --C.sub.4 alkyl, --SO.sub.2 N--(C.sub.1 -C.sub.4 alkyl).sub.2, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m SH, --S(CH.sub.2).sub.n OCOCH.sub.3, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above sulfur-containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

Abstract: Novel 17.beta.-hydroxybenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as tetosterone reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethy andR.sup.2 is phenyl substituted with one or more of: --OH, --OFC.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m H, --(CH.sub.2).sub.n COOH, including protected --OH, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above oxygen containing radicals is present, wherein the dotted line represents a double bond which can be present, pharmaceutically acceptable salts and esters thereof, and a pharmaceutical formulation thereof. The above compounds are active as testosterone reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

Abstract: New 17.beta.-aminobenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as benign prostatic hypertrophy agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is phenyl substituted with --N(R.sup.3).sub.2, which can be protected, where R.sub.3 is independently H or C.sub.1 -C.sub.4 alkyl, wherein the phenyl ring can also be further substituted by C.sub.1 -C.sub.4 alkyl, wherein the dotted line can represent a double bond, and pharmaceutically acceptable salts thereof, and a pharmaceutical formulation thereof. The above compounds are active as benign prostatic hypertrophy therapy agents and are useful topically for the treatment of acne, seborrhea, female hirsutism, and particularly effective systemically in the treatment of benign prostatic hypertrophy.

Abstract: Disclosed are Schiff's base derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.