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:
August 28, 1986
Date of Patent:
August 2, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
Abstract: Potent, irreversible dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors or 2-cyano-2-phenethylamine, and methods of using these inhibitors or 2-cyano-2-phenethylamine to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Type:
Grant
Filed:
September 9, 1985
Date of Patent:
July 26, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Pamela A. Chambers, James S. Frazee, Carl Kaiser, Lawrence I. Kruse
Abstract: This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylallyl group. The compounds have histamine H.sub.2 -antagonist activity.
Type:
Grant
Filed:
October 31, 1985
Date of Patent:
July 19, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Tetraphosphine-coordinated gold (I) compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method of treating tumor cells sensitive to such a compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
Abstract: A novel process for preparing 6-amino-3-hydrazinopyridazine derivatives comprising reacting a 3-amino-6-chloropyridazine derivative with ethyl carbazate under aqueous conditions.
Type:
Grant
Filed:
May 13, 1986
Date of Patent:
July 12, 1988
Assignee:
ISF Societa per Azioni
Inventors:
Mario Pinza, Riccardo Monguzzi, Riccardo Colombo
Abstract: Heterocyclic phosphine compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method for treating tumor cells sensitive to such a compound which comprises adminstering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
Abstract: This invention relates to tricyclic pyridazinone compounds, pharmaceutical compositions containing the compounds, and a method of stimulating cardiac activity in a mammal by administering an effective amount of the compound. A compound of the invention is 7-carboxamido-4,4a-dihydro-4a-methyl-[5H]-indeno[1,2-c]-pyridazin-3[2H]-on e.
Type:
Grant
Filed:
September 22, 1987
Date of Patent:
July 5, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Certain vasopressin-like compounds whose structures have a .beta.,.beta.-diethyl-.beta.-mercaptopropionic acid at position 1 have unexpectedly potent V.sub.2 -antagonist activity. A species of the group is [1-.beta.,.beta.-diethyl-.beta.-mercaptopropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-arginine-9-desglycine]vasopressin.
Type:
Grant
Filed:
March 19, 1987
Date of Patent:
June 7, 1988
Assignee:
Smithkline Beckman Corporation
Inventors:
William F. Huffman, Michael L. Moore, Nelson C. Yim
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.
Abstract: Compositions and methods useful for enhancing the transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise the active agent together with an effective amount of certain amides of heterocyclic amines as defined herein as penetration enhancers and topically administering to human or animal skin or other membranes the resulting compositions.
Abstract: Compounds having the formula: ##STR1## which are ester prodrugs of potent dopamine-.beta.-hydroxylase inhibitors and thus are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmeceutical compositions including these compounds, and methods of using these compounds to inhibit dopamine-.beta.-hydroxylase activity in mammals.
Type:
Grant
Filed:
April 8, 1986
Date of Patent:
May 10, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
James S. Frazee, Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
Abstract: Peptides whose structures resemble those of vasopressin antagonists but have both a carboxamido amino acid unit and a basic amino acid unit in the side chain have good antagonist activity. A species of the invention is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-8-glutamine-9-desglycine]-vasopressi n.
Type:
Grant
Filed:
October 23, 1985
Date of Patent:
May 3, 1988
Assignee:
Smithkline Beckman Corporation
Inventors:
William M. Bryan, William F. Huffman, Michael L. Moore
Abstract: This invention relates to intermediates of Mannich-alkynyl aminothiadiazole oxides having histamine H.sub.2 -antagonist activity. A particular final product of this invention is 3-amino-4-[7-piperidinohept-5-ynylamino]-1,2,5-thiadiazole-1-oxide.
Type:
Grant
Filed:
December 8, 1986
Date of Patent:
March 22, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl- C.sub.4 to C.sub.10 alkyl or ##STR3## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and R.sub.
Abstract: 1-substituted-2-mercapto(or aminomethyl)benzimidazole compounds of the formula ##STR1## inhibit dopamine-.beta.-hydroxylase activity. Intermediates are also disclosed.
Abstract: New 3,4-diamino-1,2,5-thiadiazole oxide derivatives which are histamine H.sub.1 -antagonists. A specific compound of this invention is 3-[3-[N-(4-fluorobenzyl)-N-pyrid-2-yl-amino]propylamino]-4-[pyrimidin-4-yl -methylamino]-1,2,5-thiadiazole-1-oxide.
Type:
Grant
Filed:
February 4, 1986
Date of Patent:
March 1, 1988
Assignee:
Smith Kline & French Laboratories Limited