17 a .beta.-hydroxy-7 .alpha.-methyl-d-homo-19-norandrost-4,16-diene-3-one and the 17-esters thereof: methods of preparation and uses

A pharmaceutical composition useful by oral administration for producing an androgenic response in a male mammal which comprises an effective androgenic response producing amount of a compound of the formula ##STR19## wherein R.sup.1 is hydrogen or an acyl of the formula

• --(C.dbd.O)--R.sup.2
• wherein R.sup.2 is an organic substituent selected from the group consisting of a 1 to 24 carbon atom alkyl, a 2 to 24 carbon atom alkenyl, a 2 to 24 carbon atom alkynyl, a 3 to 8 carbon atom cycloalkyl, a 4 to 32 carbon atom cycloalkylalkylene, a 1 to 24 carbon atom haloalkyl, phenyl or 1 or 2 naphthyl aryl containing up to 4 one to six carbon atom alkyl substituents, a halophenyl and a halonaphthyl each containing up to 4 one to six carbon atom alkyl substituents, and an aralkyl made up of a 1 to 6 carbon atom alkyl substituted with a phenyl or a naphthyl each containing from 0 to 4 one to six carbon atom alkyls, in admixture with a pharmaceutically acceptable oral excipient.

A pharmaceutical composition useful by oral administration for control of fertility in a male mammal while maintaining the male libido which comprises an effective fertility controlling amount of LHRH antagonist and an effective androgenic response producing amount of a compound of the formula ##STR20## wherein R.sup.1 is hydrogen or an acyl of the formula

• --(C.dbd.O)--R.sup.2
• wherein R.sup.2 is an organic substituent selected from the group consisting of a 1 to 24 carbon atom alkyl, a 2 to 24 carbon atom alkenyl, a 2 to 24 carbon atom alkynyl, a 3 to 8 carbon atom cycloalkyl, a 4 to 32 carbon atom cycloalkylalkylene, a 1 to 24 carbon atom haloalkyl, phenyl or 1 or 2 naphthyl aryl containing up to 4 one to six carbon atom alkyl substituents, a halophenyl and a halonaphthyl each containing up to 4 one to six carbon atom alkyl substituents, and an aralkyl made up of a 1 to 6 carbon atom alkyl substituted with a phenyl or a naphthyl each containing from 0 to 4 one to six carbon atom alkyls, in admixture with a pharmaceutically acceptable oral excipient.

A method for decreasing fertility in a male mammal comprising administering to the mammal an effective spermatogenesis decreasing amount of a compound of the formula ##STR21## wherein R.sup.1 is hydrogen or an acyl of the formula

• --(C.dbd.O)--R.sup.2
• wherein R.sup.2 is an organic substituent selected from the group consisting of a 1 to 24 carbon atom alkyl, a 2 to 24 carbon atom alkenyl, a 2 to 24 carbon atom alkynyl, a 3 to 8 carbon atom cycloalkyl, a 4 to 32 carbon atom cycloalkylalkylene, a 1 to 24 carbon atom haloalkyl, phenyl or 1 or 2 naphthyl aryl containing up to 4 one to six carbon atom alkyl substituents, a halophenyl and a halonaphthyl each containing up to 4 one to six carbon atom alkyl substituents, and an aralkyl made up of a 1 to 6 carbon atom alkyl substituted with a phenyl or a naphthyl each containing from 0 to 4 one to six carbon atom alkyls.

A method for increasing fertility in a male mammal comprising administering to the mammal an effective spermatogenesis increasing amount of a compound of the formula ##STR22## wherein R.sup.1 is hydrogen or an acyl of the formula

• --(C.dbd.O)--R.sup.2
• wherein R.sup.2 is an organic substituent selected from the group consisting of a 1 to 24 carbon atom alkyl, a 2 to 24 carbon atom alkenyl, a 2 to 24 carbon atom alkynyl, a 3 to 8 carbon atom cycloalkyl, a 4 to 32 carbon atom cycloalkylalkylene, a 1 to 24 carbon atom haloalkyl, phenyl or 1 or 2 naphthyl aryl containing up to 4 one to six carbon atom alkyl substituents, a halophenyl and a halonaphthyl each containing up to 4 one to six carbon atom alkyl substituents, and an aralkyl made up of a 1 to 6 carbon atom alkyl substituted with a phenyl or a naphthyl each containing from 0 to 4 one to six carbon atom alkyls.

A method for achieving an androgenic response in a male mammal comprising orally administering to the mammal an effective oral androgenic response producing amount of a compound of the formula ##STR23## wherein R.sup.1 is hydrogen or an acyl of the formula

• --(C.dbd.O)--R.sup.2
• wherein R.sup.2 is an organic substituent selected from the group consisting of a 1 to 24 carbon atom alkyl, a 2 to 24 carbon atom alkenyl, a 2 to 24 carbon atom alkynyl, a 3 to 8 carbon atom cycloalkyl, a 4 to 32 carbon atom cycloalkylalkylene, a 1 to 24 carbon atom haloalkyl, phenyl or 1 or 2 naphthyl aryl containing up to 4 one to six carbon atom alkyl substituents, a halophenyl and a halonaphthyl each containing up to 4 one to six carbon atom alkyl substituents, and an aralkyl made up of a 1 to 6 carbon atom alkyl substituted with a phenyl or a naphthyl each containing from 0 to 4 one to six carbon atom alkyls.