Patents by Inventor Malcolm Maccoss

Malcolm Maccoss has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Treatment of emesis with morpholine tachykinin receptor antagonists
    Patent number: 5512570
    Abstract: Substituted heterocycles of the structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, emesis and nausea.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: April 30, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Malcolm MacCoss, Jeffrey J. Hale, Sander G. Mills
  • Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
    Patent number: 5434248
    Abstract: Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia.
    Type: Grant
    Filed: June 2, 1993
    Date of Patent: July 18, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Kevin T. Chapman, Herb G. Bull, Malcolm MacCoss, Nancy A. Thornberry, Jeffrey R. Weidner, Adnan M. Mjalli
  • Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
    Patent number: 5430128
    Abstract: Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia.
    Type: Grant
    Filed: November 21, 1994
    Date of Patent: July 4, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Kevin T. Chapman, Malcolm MacCoss, Adnan Mjalli
  • Assay for evaluating inhibition of polymorphonuclear leukocyte elastase by N-substituted azetidinones
    Patent number: 5420010
    Abstract: N-substituted azetidinones are a class of inhibitors of human leukocytes elastase which are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the assay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured. The assays are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.
    Type: Grant
    Filed: July 30, 1993
    Date of Patent: May 30, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, William K. Hagmann, William A. Hanlon, John L. Humes, Wilson B. Knight, Malcolm MacCoss, Richard A. Mumford, Shrenik K. Shah
  • Substituted triazolinones, triazolinethiones, and triazolinimines as angiotensin II antagonists
    Patent number: 5411980
    Abstract: There are disclosed new substituted triazolinone, triazolinethione, and triazolinimine compounds which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1## wherein G is R.sup.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: May 2, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Linda L. Chang, Malcolm MacCoss, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Kelly Flanagan
  • Process of making chiral 2-aryl-1,4-butanediamine derivatives as useful neurokinin-A antagonists
    Patent number: 5391819
    Abstract: Disclosed herein is a process of making chiral 2-aryl-1,4-butanediamine derivatives useful as neurokinin-A antagonists of Formula 7 ##STR1##
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills
  • Substituted imidazo-fused 5-membered ring heterocycles as angiotensin II antagonists
    Patent number: 5389660
    Abstract: There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: February 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss, Nathan B. Mantlo, Arthur A. Patchett, Prasun K. Chakravarty, Thomas F. Walsh
  • Alicyclic compounds as tachykinin receptor antagonists
    Patent number: 5387595
    Abstract: Substituted alicyclic compounds of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma.
    Type: Grant
    Filed: August 26, 1992
    Date of Patent: February 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Paul E. Finke, Malcolm MacCoss, Daniel J. Miller, Dennis J. Underwood
  • Substituted azetidinones as anti-inflammatory and antidegenerative agents
    Patent number: 5348953
    Abstract: New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
    Type: Grant
    Filed: December 17, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Paul E. Finke, William K. Hagmann, Amy L. Kissinger, Malcolm MacCoss, Shrenik K. Shah
  • N,N-diacylpiperazine tachykinin antagonists
    Patent number: 5344830
    Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: September 6, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
  • Substituted triazoles as angiotensin II antagonists
    Patent number: 5336778
    Abstract: Novel substituted triazoles of the formula (I), which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Christine L. Cantone, Linda L. Chang, Malcolm Maccoss, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
  • Substituted pyrimidines, pyrimidinones and pyridopyrimidines
    Patent number: 5324729
    Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
  • N,N-diacylpiperazines
    Patent number: 5292726
    Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: May 19, 1992
    Date of Patent: March 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Sander G. Mills, Mu T. Wu
  • Monospecific antibodies useful in evaluating inhibition of polymorphonuclear leukocyte elastase by N-substituted azetidinones
    Patent number: 5274080
    Abstract: Inhibitors of human leukocytes elastase are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the radioimmunoassay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured utilizing polyclonal antibodies capable of binding to one or more haptens of formula II ##STR1## wherein M is allyl or n-propyl,Z.sub.1 is(a) 5-benzofuranyl or(b) substituted phenyl wherein the substituent is methyl or ethyloxy.The assays utilizing these antibodies are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.
    Type: Grant
    Filed: August 26, 1991
    Date of Patent: December 28, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Malcolm MacCoss, Richard A. Mumford
  • Substituted imidazopyridazines as angiotensin II antagonists
    Patent number: 5260285
    Abstract: Novel substituted imidazopyridazines of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
  • Substituted pyrazolopyrimidines as angiotensin II antagonists
    Patent number: 5250521
    Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
  • Substituted azetidinones as anti-inflammatory and antidegenerative agents
    Patent number: 5229381
    Abstract: New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: July 20, 1993
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Conrad P. Dorn, Paul E. Finke, William K. Hagmann, Malcolm MacCoss, Shrenik K. Shah
  • Angiotensin II antagonists incorporating a substituted imidazo [1,2-b][1,2,4]triazole
    Patent number: 5187179
    Abstract: There are disclosed substituted imidazo[1,2-b][1,2,4]triazole derivatives of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 22, 1991
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Steven M. Hutchins, Malcolm MacCoss
  • Substituted pyrimidines, pyrimidinones and pyridopyrimidines
    Patent number: 5166206
    Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: November 24, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
  • Substituted imidazo-fused 5-membered ring heterocycles and their use as angiotensin II antagonsists
    Patent number: 5164407
    Abstract: There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: April 25, 1990
    Date of Patent: November 17, 1992
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss, Nathan B. Mantlo, Arthur A. Patchett, Prasun K. Chakravarty, Thomas F. Walsh