Patents Represented by Attorney William J. Stein
  • Patent number: 5374632
    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.
    Type: Grant
    Filed: August 17, 1992
    Date of Patent: December 20, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Robert J. Cregge
  • Patent number: 5252565
    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
  • Patent number: 5166211
    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
  • Patent number: 5134154
    Abstract: The present invention is directed to a new class of phenoxy-heterocyclic compounds and to their use as anti-depressants and as anxiolytics.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: July 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Jules Freedman, Mark W. Dudley
  • Patent number: 5112852
    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
  • Patent number: 5109010
    Abstract: Novel cyclic vinylogous N-hydroxy-N-methylureas are useful in the treatment of leukotriene mediated conditions such as asthma and rheumatoid arthritis.
    Type: Grant
    Filed: April 5, 1991
    Date of Patent: April 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight
  • Patent number: 5106861
    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.
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: April 21, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Hugues d'Orchymont, Celine Tarnus
  • Patent number: 5095110
    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.
    Type: Grant
    Filed: February 9, 1990
    Date of Patent: March 10, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight
  • Patent number: 5093341
    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
  • Patent number: 5068465
    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
  • Patent number: 5041673
    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.
    Type: Grant
    Filed: January 4, 1990
    Date of Patent: August 20, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Hugues d'Orchymont, Celine Tarnus
  • Patent number: 5041554
    Abstract: This invention relates to novel aryl- or heteroaryl-1-alkyl-pyrrole-2-carboxylic acid compounds useful in treating interleukin-1 mediated conditions.
    Type: Grant
    Filed: February 23, 1990
    Date of Patent: August 20, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Roger A. Parker, George Ku
  • Patent number: 5039695
    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.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: August 13, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Roger A. Parker, George Ku
  • Patent number: 5026861
    Abstract: Novel cyclic vinylogous N-hydroxy-N-methylureas are useful in the treatment of leukotriene mediated conditions such as asthma and rheumatoid arthritis.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: June 25, 1991
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Gary A. Flynn, Douglas W. Beight
  • Patent number: 5017591
    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
  • Patent number: 4999431
    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
  • Patent number: 4990519
    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
  • Patent number: 4981868
    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
  • Patent number: 4973585
    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.
    Type: Grant
    Filed: May 10, 1989
    Date of Patent: November 27, 1990
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Gary A. Flynn, Douglas W. Beight
  • Patent number: 4970228
    Abstract: This invention relates to novel aminoalkyl substituted heterocyclic sulfur compounds which are useful as antihypertensive agents.
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: November 13, 1990
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Thomas M. Bargar, Robert J. Broersma, Lawrence C. Creemer