Abstract: Invented is a Method of Treating Prostatic Adenocarcinoma by employing a steroid 5-.alpha.-reductase inhibiting compound or a combination of steroid 5-.alpha.-reductase inhibiting compounds.
Abstract: Polystyrene polymers bearing a quaternary ammonium group are disclosed. They are useful in the treatment of hypercholesterolaemia and the prevention of atherosclerosis. A compound of the invention is 6-(N,N-dimethyl-N-octylammonio)hexanoylated polystyrene chloride.
Type:
Grant
Filed:
May 21, 1990
Date of Patent:
December 28, 1993
Assignee:
SmithKline & French Laboratories Limited
Inventors:
Albert A. Jaxa-Chamiec, Deirdre M. B. Hickey, Virendra P. Shah
Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.
Type:
Grant
Filed:
February 4, 1992
Date of Patent:
August 17, 1993
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: Polystyrene polymers having a quaternised ammonium group and their use in a method of treatment of hypercholesterolaemia. A particular compound of the invention is (N,N-dimethyl-N-dodecyl-ammoniomethylstyrene-ethyl methacrylate-divinylbenzene co-polymer, chloride salt.
Type:
Grant
Filed:
June 12, 1990
Date of Patent:
July 27, 1993
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Albert A. Jaxa-Chamiec, Deirdre M. B. Hickey
Abstract: Substituted gem-diphosphonate compounds having use as cholesterol lowering agents are disclosed. A compound of the invention is tetraethyl-2-[3-t-butyl-4-hydroxynaphthyl]ethenylidene-1,1-diphosphonate.
Abstract: Invented are 3-acetic acid-steroidal compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase including using these compounds to reduce prostate size and to treat prostatic adenocarcinoma. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
June 11, 1990
Date of Patent:
August 11, 1992
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: Polymers bearing a quaternary ammonium group are disclosed as being useful in lowering serum cholesterol levels in man. A compound of the invention is N,N-dimethyl-N-(2-(N,N-dimethylcarbamoyl)ethyl)-ammoniomethyl-substitut ed polystyrene, chloride salt.
Type:
Grant
Filed:
June 12, 1990
Date of Patent:
May 12, 1992
Assignee:
Smith Kline & French Laboratories
Inventors:
Albert A. Jaxa-Chamiec, Deirdre M. B. Hickey
Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.
Type:
Grant
Filed:
October 10, 1989
Date of Patent:
May 5, 1992
Assignee:
Smithkline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: Polymers bearing a quaternary ammonium group are disclosed as being useful in lowering serum cholesterol levels in man. A compound of the invention is N-(2-N,N-dimethylamino)ethyl)-N,N-dimethylammoniomethyl-substituted polystyrene, chloride salt.
Type:
Grant
Filed:
June 12, 1990
Date of Patent:
May 5, 1992
Assignee:
Smith Kline & Franch Laboratories Limited
Inventors:
Albert A. Jaxa-Chamiec, Deirdre M. B. Hickey
Abstract: Pyridiniomethacrylate polymers are described which are of use in the treatment of elevated serum cholesterol levels. A compound of the invention is cross-linked 3-(N-methyl-3-pyridinio)propyl methacrylate chloride.
Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 11-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase.
Type:
Grant
Filed:
November 1, 1989
Date of Patent:
August 20, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Brian W. Metcalf, Mark A. Levy
Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.
Type:
Grant
Filed:
August 24, 1989
Date of Patent:
July 16, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Brian W. Metcalf, Dennis A. Holt, Mark A. Levy
Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.
Type:
Grant
Filed:
December 23, 1988
Date of Patent:
June 25, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: New 14.alpha.-carboxyalkyl sterols are regulators of HMG-CoA reductase and inhibitors of mammalian 14.alpha.-methyl demethylase and are useful in lowering serum cholesterol levels and treating fungal infections.
Type:
Grant
Filed:
August 24, 1989
Date of Patent:
June 11, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Jerry L. Adams, Timothy F. Gallagher, Ruth J. Mayer, Brian W. Metcalf
Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
March 23, 1990
Date of Patent:
May 21, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Conrad J. Kowalski, Mark A. Levy, Brian W. Metcalf, Ann M. Tickner
Abstract: This invention relates to an improved process for the preparation of substituted indolinone derivatives using reductive cyclization conditions.
Type:
Grant
Filed:
June 15, 1988
Date of Patent:
March 5, 1991
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Invented are 3-nitro- substituted steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
August 23, 1989
Date of Patent:
November 13, 1990
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: Invented are sulfonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
December 23, 1988
Date of Patent:
November 13, 1990
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
July 14, 1989
Date of Patent:
September 4, 1990
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf