US 5,371,078 AGranted

Angiostatic steroids and methods and compositions for controlling ocular hypertension

AssigneeAlcon Laboratories, Inc.

InventorsAbbot F. Clark, Raymond E. Conrow

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Abstract

Angiostatic steroids for use in controlling ocular hypertension are disclosed. Pharmaceutical compositions of the angiostatic steroids and methods for their use in treating ocular hypertension, including controlling the ocular hypertension associated with primary open angle glaucoma, are disclosed. In addition, the combination of the compounds with glucocorticoids for the prevention of elevated IOP during the treatment of inflammation is disclosed.

Claims10

Dependent claims

A method for controlling ocular hypertension which comprises administering a pharmaceutically effective amount of a compound selected from the group consisting of:

21 -methyl-5.beta.-pregnan-3.alpha.,11.beta.,17.alpha.,21-tetrol-20-one 21-methyl ether;
3.beta.-azido-5.beta.-pregnan-11.beta.,17.alpha.,21-triol-20-one-21-acetat e;
3.beta.-acetamido-5.beta.-pregnan-11.beta.,17.alpha.,21-triol-20-one-21-ac etate;
20-(4-fluorophenyl)thio-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
20-azido-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
20-(carbethoxymethyl)thio-21 -nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
20-acetamido-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol-3-acetate;
16.alpha.-(2-hydroxyethyl)-17.beta.-methyl-5.beta.-androstan-3.alpha.,17.a lpha.-diol;
20-cyano-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
17.alpha.-methyl-5.beta.-androstan-3.alpha.,17.beta.-diol;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.-ol;
21-nor-5.beta.pregn-17(20)-en-3.alpha.-ol-3-acetate;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.-ol-16-acetic acid-3-acetate;
21-nor-5.beta.-pregnan-3.alpha.,17.alpha.20-triol;
21-nor-5.beta.-pregnan-3.alpha.,17.alpha.,20-triol-3-acetate;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.,16-diol-3-acetate-16-(O-methyl)mal onate;
21-nor-5.alpha.-pregnan-3.alpha.,17.alpha.,20-triol-3phosphate;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.,16-diol;
21-nor-5.beta.-pregnan-3.alpha.,17.beta.,20-triol;
21-nor-5.alpha.-pregnan-3.alpha.,17.beta.,20-triol;
4-androsten-3-one-17.beta.-carboxylic acid;
17.alpha.-ethynl-5(10)-estren-17.beta.-ol-3-on 1,3,5(10)-estratrien-3,17.beta.-diol;
and 4.9(11)-pregnadien-17.alpha.,21-diol-3,20-dione-21-acetate.

20 more elements

A composition for controlling ocular hypertension comprising a pharmaceutically effective amount of a compound selected from the group consisting of:

21 -methyl-5.beta.-pregnan-3.alpha., 11.beta., 17.alpha.,21-tetrol-20-one 21-methyl ether;
3.beta.-azido-5.beta.-pregnan-11.beta.,17.alpha.,21-triol-20-one-21-acetat e;
3.beta.-acetamido-5.beta.-pregnan-11.beta.,17.alpha.,21-triol-20-one-21-ac etate;
20-(4-fluorophenyl)thio-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
20-azido-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
20-(carbethoxymethyl)thio-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
20-acetamido-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol-3-acetate;
16.alpha.-(2-hydroxyethyl)-17.beta.-methyl-5.beta.-androstan-3.alpha.,17.a lpha.-diol;
20-cyano-21-nor-5.beta.-pregnan-3.alpha.,17.alpha.-diol;
17.alpha.-methyl-5.beta.-androstan-3.alpha.,17.beta.-diol;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.-ol;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.-ol-3-acetate;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.-ol-16-acetic acid-3-acetate;
21-nor-5.beta.-pregnan-3.alpha.,17.alpha.,20-triol;
21-nor-5.beta.-pregnan-3.alpha.,17.alpha.,20-triol-3-acetate;
21-nor-5.beta.-pregn-17(20)-en-3.alpha.,16-diol-3-acetate-16-(O-methyl)mal onate;
21-nor-5.alpha.-pregnan-3.alpha.,17.alpha.,20-triol-3-phosphate;
21-nor-5.beta.-pregn-17(20l)-3.alpha.,16-diol;
21-nor-5.beta.-pregnan-3.alpha.,17.beta.,20-triol;
21-nor-5.alpha.-pregnan-3.alpha.,17.beta.20-triol;
4-androsten-3-one-17.beta.-carboxylic acid;
17.alpha.-ethynyl-5(10)-estren-17.beta.-ol-3-one;
17.alpha.-ethynyl-1,3,5(10)estratrien-3,17.beta.-diol;
and 4,9(11)-pregnadien-17.alpha.21-diol-3,20dione-21-acetate.

21 more elements

Dependencies are inferred from the claim text.

Facts

Application: 07/941,485Filed 8 Sep 1992 · continuation in part
Priority: 31 Oct 1988
Granted: 6 Dec 1994
Term ends: Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 31/569
Substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone: substituted in position 17…
A61K 31/56
Medicinal preparations containing organic active ingredients: compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives…
A61K 31/565
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids: not substituted in position 17 beta by a…
A61K 31/57
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids: substituted in position 17 beta by a chain…

Family

Serial264,918Parent of this continuation · filed 31 Oct 1988
Serial419,226Parent of this continuation-in-part · filed 10 Oct 1989
Serial559,123Parent of this continuation-in-part · filed 27 Jul 1990
US 4,876,250 AParent of this continuation
US 5,371,078 AThis patent

From the US filing history. Foreign family members aren’t listed.

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Abstract

Facts

Application

07/941,485Filed 8 Sep 1992 · continuation in part

Priority

31 Oct 1988

Granted

6 Dec 1994

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 31/569
Substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone: substituted in position 17…
A61K 31/56
Medicinal preparations containing organic active ingredients: compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives…
A61K 31/565
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids: not substituted in position 17 beta by a…
A61K 31/57
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids: substituted in position 17 beta by a chain…

Family

Serial264,918Parent of this continuation · filed 31 Oct 1988

Serial419,226Parent of this continuation-in-part · filed 10 Oct 1989

Serial559,123Parent of this continuation-in-part · filed 27 Jul 1990

US 4,876,250 AParent of this continuation

US 5,371,078 AThis patent

From the US filing history. Foreign family members aren’t listed.