Uncompetitive inhibition of steroid and 5.alpha.-reductose
AssigneeSmithKline Beecham Corporation
InventorMichael Henry
Life of this patent
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Abstract
Invented are compositions of competitive and uncompetitive inhibitors of steroid 5-.alpha.-reductase, pharmaceutical compositions containing the compositions of inhibitors and methods of using these compositions to inhibit steroid 5-.alpha.-reductase. Also invented in the method of co-administating a 5-.alpha.-reductase inhibitor and further active ingredients.
Claims12
A composition comprising an uncompetitive inhibitor of steroid 5-.alpha.-reductase and a compound selected from the group consisting of:
- N-t-butyl-5-.alpha.-androst-1ene-4-aza-17.beta.-carboxamide-3-one;
- 17.beta.-N,N-diisopropylcarboxamide-3-nitro-5-.alpha.-androst-3ene;
- 17.beta.-N-t-butylcarboxamide-3-nitro-5-.alpha.-androst-3-ene;
- and
- 17.beta.-N,N-diisopropylcarboxamide-3-nitro-5-.alpha.-androst-2-ene.
A composition comprising a competitive inhibitor of steroid 5-.alpha.-reductase and a compound selected from the group consisting of:
- N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid or a salt thereof;
- N,N-diisopropyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)-estra-1,3,5(10)-triene-3-carboxylic acid or a salt thereof;
- 17.beta.-t-butylcarboxamide)-estra-1,3,5(10)-triene-3-carboxylic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)-estra-1,3,5(10)-triene-3-sulfonic acid or a salt thereof;
- 17.beta.-(N-t-butylcarboxamide)-estra-1,3,5(10)-triene-3-sulfonic acid or a salt thereof;
- 17.beta.(N,N-diisopropylcarboxamide)-estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 17.beta.-(N-t-butylcarboxmide)-estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 20-.alpha.-(hydroxymethyl)-A-nor-5-.alpha.-pregn-1-ene-2-carboxylic acid or a salt thereof;
- 17.beta.-(N-t-butylcarboxamide)-estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 17.beta.-N-t-butylcarboxamide-androst-3,5-diene-3-phosphinic acid or a salt thereof;
- 17.beta.-N,N-diisopropylcarboxamide-androst-3,5-diene-3-phosphinic acid or a salt thereof;
- 17.beta.-N-t-butylcarboxamide-androst-3,5-diene-3-phosphonic acid or a salt thereof;
- and
- 17.beta.-N,N-diisopropylcarboxamide-androst-3,5-diene-3-phosphonic acid or a salt thereof.
The method of inhibiting steroid 5-.alpha.-reductase activity in mammals in need thereof which comprises administering to the subject consecutively, in separate pharmaceutical compositions, an uncompetitive inhibitor of steroid 5-.alpha.-reductase and a compound selected from the group consisting of:
- N-t-butyl-5-.alpha.-androst-1-ene-4-aza-17.beta.-carboxamide-3-one;
- 17.beta.-N,N-diisopropylcarboxamide-3-nitro-5-.alpha.-androst-3ene;
- 17.beta.-N-t-butylcarboxamide-3-nitro-5-.alpha.-androst-3-ene;
- and
- 17.beta.-N,N-diisopropylcarboxamide-3-nitro-5-.alpha.-androst-2-ene.
The method of inhibiting steroid 5-.alpha.-reductase activity in mammals in need thereof which comprises administering to the subject consecutively, in separate pharmaceutical compositions, a competitive inhibitor of steroid 5-.alpha.-reductase and a compound selected from the group consisting of:
- N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid or a salt thereof;
- N,N-diisopropyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)-estra-1,3,5(10)-triene-3-carboxylic acid or a salt thereof;
- 1.beta. -(N-t-butylcarboxamide)-estra-1,3,5(10)-triene-3-carboxylic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)-estra-1,3,5(10)-triene-3-sulfonic acid or a salt thereof;
- 17.beta.-(N-t-butylcarboxamide)-estra-1,3,5(10)-triene-3-sulfonic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)-estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 17.beta.-(N-t-butylcarboxmide)-estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 17.beta.-(N,N-diisopropylcarboxamide)estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 20-.alpha.-(hydroxymethyl)-A-nor-5-.alpha.-pregn-1-ene-2-carboxylic acid or a salt thereof;
- 17.beta.-(N-t-butylcarboxamide)-estra-1,3,5(10)-triene-3-phosphonic acid or a salt thereof;
- 17.beta.-N-t-butylcarboxamide-androst-3,5-diene-3-phosphinic acid or a salt thereof;
- 17.beta.-N,N-diisopropylcarboxamide-androst-3,5-diene-3-phosphinic acid or a salt thereof;
- 17.beta.-N-t-butylcarboxamide-androst-3,5-diene-3-phosphonic acid or a salt thereof;
- and
- 17.beta.-N,N-diisopropylcarboxamide-androst-3,5-diene-3-phosphonic acid or a salt thereof.
Dependencies are inferred from the claim text.