Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Type:
Grant
Filed:
September 15, 1989
Date of Patent:
March 27, 1990
Assignee:
SmithKline Beckman Corporation
Inventors:
Lawrence I. Kruse, Stephen T. Ross, Eliot H. Ohlstein
Abstract: The present invention relates to the use of certain indolone derivatives in particular, 4-(2-di-n-propyl-aminoethyl)-2-(3H)-indolone in a method of treatment of Parkinsons disease.
Type:
Grant
Filed:
March 13, 1989
Date of Patent:
March 27, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the 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:
December 1, 1987
Date of Patent:
March 20, 1990
Assignee:
SmithKline Beckman Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinylmethyl]-thyronine.
Type:
Grant
Filed:
March 16, 1988
Date of Patent:
March 20, 1990
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
Abstract: New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by a Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
Type:
Grant
Filed:
May 9, 1988
Date of Patent:
March 13, 1990
Assignee:
SmithKline Beckman Corporation
Inventors:
James F. Callahan, William F. Huffman, Kenneth A. Newlander, Nelson C. F. Yim
Abstract: Phosphodiesterase (type III) inhibitors having the formula: ##STR1## which are useful in stimulating cardiac activity and in treating congestive heart failure and bronchoconstriction, pharmaceutical compositions including these inhibitors, and methods of using these compounds to produce phosphodiesterase (type III) inhibition in mammals.
Type:
Grant
Filed:
October 14, 1986
Date of Patent:
March 6, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to pyridazinone derivatives which have inotropic, vasodilator and bronchodilator activity. The compounds of the invention are described by formula (I): ##STR1## wherein: R.sup.1 is hydrogen or methyl;R.sup.2 is hydrogen or methyl; and represent double or single bonds; and the benzene ring is para- or meta-substituted; and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
July 1, 1986
Date of Patent:
February 27, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: A vaccine for protecting canine animals from disease caused by infection with canine corona virus (CCV) which comprises an effective amount of the cell-associated CCV peplomer protein. A polyvalent vaccine comprising an effective amount of cell-associated CCV peplomer protein and an effective amount of an antigenic component which is protective against one or more additional pathogenic organisms or viruses are also disclosed.
Abstract: 2-pyridyl and 4-pyridyl phosphine gold compounds of the formula: ##STR1## and 2-pyridyl phosphine gold compounds of the formula: ##STR2## and pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound.
Abstract: The invention provides a class of alkanoic acids substituted with a benzenesulphonamidopyridyl group. The compounds have activity as thromboxane A.sub.2 -antagonists.
Type:
Grant
Filed:
April 7, 1988
Date of Patent:
February 20, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylalkyl group. The compounds have histamine H.sub.2 -antagonist activity.
Type:
Grant
Filed:
April 19, 1988
Date of Patent:
January 16, 1990
Assignee:
Smith Kline & French Laboratories Limited
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:
July 28, 1987
Date of Patent:
December 19, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: This invention relates to purinone derivatives which have bronchodilator, vasodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)-6-purinone.
Type:
Grant
Filed:
January 27, 1988
Date of Patent:
December 5, 1989
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mannals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Type:
Grant
Filed:
December 29, 1987
Date of Patent:
November 21, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Lawrence I. Kruse, Stephen T. Ross, Eliot H. Ohlstein
Abstract: Carboxamide derivatives of glcopeptide antibiotics and their salts are useful for treating or preventing infection in an animal by gram-positive bacteria and also increase feed-utilization efficiency, promote growth in domestic animals and increase propionate production in lactating ruminants.
Abstract: Invented are phosphonic 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 21, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: Disclosed are novel substituted 3-aralkylimidazolines of the structure. ##STR1## processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy in particular as dopamine-.beta.-hydroxylase inhibitors.
Type:
Grant
Filed:
December 31, 1987
Date of Patent:
October 24, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Lawrence I. Kruse, Thomas B. Leonard, Stephen T. Ross
Abstract: Vasopressin-like peptide whose structures have been modified by an alpha-methyl amino acid at the 4 or 7 position are set forth. These compounds have potent vasopressin antagonist activities.