Abstract: 2,3-Dihydro-1-(8-methyl-1,2,4-triazolo [4,3-b]pyridazin-6-yl)-4(1H)-pyridinone has been prepared in substantially pure form and has been found to be useful for alleviating bronchial spasms in mammals. Synthesis of this material through phenylselenyl intermediates is described.
Abstract: The present invention is directed to a group of compounds which are haloethyl substituted steroidal enzyme inhibitors. These compounds are useful as aromatase, 19-hydroxylase, and aldosterone biosynthesis inhibitors and they are prepared from the corresponding epoxide.
Type:
Grant
Filed:
September 6, 1991
Date of Patent:
October 12, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Norton P. Peet, Joseph P. Burkhart, J. O'Neal Johnston
Abstract: The present invention pertains to a new class of compounds which can be characterized as 1,4-disubstituted piperidinyl compounds useful as antiarrhythmics, analgesics, and serotonin 5HT.sub.2 antagonists.
Type:
Grant
Filed:
December 16, 1991
Date of Patent:
November 24, 1992
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Albert A. Carr, Richard C. Dage, John E. Koerner, Tung Li, Francis P. Miller
Abstract: The present invention relates to allenyl amines, more specifically, .beta.-ethenylidene(substituted) ethanamines, possessing antihypertensive activity, and having the general formula ##STR1## wherein n is the integer 0, 1 or 2; each X independently is a substituent selected from the group consisting of loweralkyl, halo, --O--(loweralkyl), --S--(loweralkyl), --SO--(loweralkyl), --SO.sub.2 --(loweralkyl), CO.sub.2 R and CH.sub.2 OR, wherein R is loweralkyl and each loweralkyl group is from 1 to about 6 carbon atoms, or the pharmaceutically-acceptable addition salts thereof. These compounds are prepared by a novel reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.
Type:
Grant
Filed:
April 21, 1989
Date of Patent:
May 12, 1992
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Thomas M. Bargar, Charlotte L. Barney, Donald P. Matthews, Robert J. Broersma
Abstract: Novel cyclic vinylogous N-hydroxy-N-methylureas are useful in the treatment of leukotriene mediated conditions such as asthma and rheumatoid arthritis.
Abstract: This invention relates to novel derivatives of tetralin, to the processes for their preparation, to their use as amino-peptidase inhibitors and to their end-use application as immunomodulators and as analgesic agents.
Abstract: This invention relates to a process for preparing an olifinated tricyclic lactam which comprises reacting an amine with alkylnitrite to form a diazoamide compound which is further reacted with strong acid and phosphine, and finally with a strong base and formaldehyde.
Abstract: The present invention is directed to a new class of compounds useful as antiarrhythmics, analgesics and serotonin 5HT.sub.2 antagonists, which compounds have the following formula: ##STR1## wherein; Y is represented by H, CO(CH.sub.2).sub.n CH.sub.3 in which n is an integer from 0-3, or SO.sub.2 (CH.sub.2).sub.n CH.sub.3 in which n is an integer from 0--3; X is represented CO, CHOH, or C.dbd.N--O--A, wherein A is represented by hydrogen or a C.sub.1-4 alkyl; R is either selected from the group consisting of halogens, lower alkyl groups, lower alkoxy groups, and hydrogen or R is a divalent substituent and is represented by a 3,4-methylenedioxy or a 3,4-ethylenedioxy substituent; m is an integer from 1-5; and the pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
August 26, 1988
Date of Patent:
March 3, 1992
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Albert A. Carr, John E. Koerner, Richard C. Dage, Tung Li, Francis P. Miller
Abstract: This invention relates to novel 3-aryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.
Type:
Grant
Filed:
June 15, 1990
Date of Patent:
November 26, 1991
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Charlotte L. Barney, Donald P. Matthews
Abstract: This invention relates to novel derivatives of tetralin, to the processes for their preparation, to their use as aminopeptidase inhibitors and to their end-use application as immunomodulators and as analgesic agents.
Abstract: This invention relates to novel aryl- or heteroaryl-1-alkyl-pyrrole-2-carboxylic acid compounds useful in treating interleukin-1 mediated conditions.
Abstract: This invention relates to the method of using aryl- or heteroaryl-1-alkyl-pyrrole-2-carboxylic acid compounds to treat interleukin-1 mediated conditions.
Abstract: Novel cyclic vinylogous N-hydroxy-N-methylureas are useful in the treatment of leukotriene mediated conditions such as asthma and rheumatoid arthritis.
Abstract: This invention relates to novel (aryl or heteroaromatic methyl)-2,2'-1H-biimidazoles; to a process for their production comprising of reacting an appropriate alpha-brominated or alpha-chlorinated, substituted or nonsubstituted, methylated monoaromatic ring compound with 2,2'-bi-1H-imidazole in a solvent such as ethanol in the presence of a base such as sodium hydroxide under reflux conditions; and to pharmaceutical compositions and methods of treating hypertension with such compounds.
Type:
Grant
Filed:
March 2, 1990
Date of Patent:
May 21, 1991
Assignee:
Merrell Dow Pharmaceuticals
Inventors:
Donald P. Matthews, Jeffrey P. Whitten, James B. McCarthy
Abstract: This invention relates to novel quinolyloxazole-2-ones which are useful as protein kinase C inhibitors, effective in the treatment of hypertension and asthma. This invention also includes a novel procedure for producing an intermediate ketone compound involving the reaction of a bromo-quinoline compound with butyl lithium and further reacting the lithiated compound with N-methyl-N-methoxyalkanamide.
Type:
Grant
Filed:
February 23, 1990
Date of Patent:
March 12, 1991
Assignee:
Merrell Dow Pharmaceuticals
Inventors:
Winton D. Jones, Richard C. Dage, George P. Claxton, Hsien C. Cheng, Phillip J. Robinson
Abstract: This invention relates to novel quinolyloxazole-2-ones which are useful as protein kinase C inhibitors, effective in the treatment of hypertension and asthma. This invention also includes a novel procedure for producing an intermediate ketone compound involving the reaction of a bromo-quinoline compound with butyl lithium and further reacting the lithiated compound with N-methyl-N-methoxyalkanamide.
Type:
Grant
Filed:
February 23, 1990
Date of Patent:
February 5, 1991
Assignee:
Merrell Dow Pharmaceuticals
Inventors:
Winton D. Jones, George P. Claxton, Richard C. Dage, Hsien C. Cheng, Phillip J. Robinson
Abstract: This invention relates to novel 3-heteroaryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.
Type:
Grant
Filed:
July 25, 1989
Date of Patent:
January 1, 1991
Assignee:
Merrell Dow Pharmaceutical
Inventors:
James R. McCarthy, Donald P. Matthews, Charlotte L. Barney
Abstract: This invention relates to derivatives of fused bicyclic or tricyclic lactams, to the intermediates and processes useful for their preparation and to their pharmacological effect in inhibiting the angiotensin converting enzyme and to their end-use application in the treatment of hypertension.