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).

  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 5922706
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: July 13, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
  • Substituted 2-acylamino-pyridines as inhibitors of nitric oxide synthase
    Patent number: 5908842
    Abstract: Substituted 2-acylaminopyridine compounds and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: June 1, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ravindra Guthikonda, William Hagmann, Malcolm Maccoss, Shrenik Shah, Philippe Durette
  • Phenyl spiroethercycloalkyl tachykinin receptor antagonists
    Patent number: 5877191
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: March 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Yuan-Ching Chiang, Conrad Dorn, Paul Finke, Jeffrey Hale, Malcolm Maccoss, Sander Mills, Albert Robichaud
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 5872116
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: February 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Trypthophan ureas as neurokinnin antagonists
    Patent number: 5869489
    Abstract: Disclosed are Substituted azacycles of formula I ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: February 9, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Shrenik K. Shah, Hongbo Qi, Malcolm Maccoss
  • Spiro-substituted azacycles as tachykinin receptor antagonists
    Patent number: 5869496
    Abstract: Disclosed are spiro-substituted azacycles of formula (I), are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, emesis and asthma. In particular compounds of formula (I) are shown to be neurokinin antagonists.
    Type: Grant
    Filed: July 11, 1995
    Date of Patent: February 9, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Hongbo Qi, Shrenik K. Shah
  • Substituted ketone derivatives as inhibitors of interleukin-1.beta. converting enzyme
    Patent number: 5866545
    Abstract: This invention relates to substituted ketone derivatives of formula (I) useful in the treatment of inflammation in lung, central nervous system, kidney, joints, endocardium, pericardium, eyes, ears, skin, gastrointestinal tract and urogenital system. More particularly, this invention relates to substituted ketone drivatives that are useful inhibitors of interleukin-1.beta. converting enzyme (ICE). Interleukin-1.beta. converting enzyme (ICE) has been identified as the enzyme responsible for converting precursor interleukin-1.beta. (IL-1.beta.) to biologically active IL-1.beta..
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: February 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: William K. Hagmann, Justin J. Zhao, Malcolm MacCoss, Adnan M. Mjalli
  • Morpholine compounds are prodrugs useful as tachykinin receptor antagonists
    Patent number: 5780467
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, and emesis.
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: July 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills
  • Cycloalkyl tachykinin receptor antagonists
    Patent number: 5750549
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: May 12, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Ping Chen, Philippe L. Durette, Paul Finke, Jeffrey Hale, Edward Holson, Ihor Kopka, Malcolm MacCoss, Laura Meurer, Sander G. Mills, Albert Robichaud
  • Substituted azetidiones as anti-inflammatory and antidegenerative agents
    Patent number: 5747485
    Abstract: Substituted azetidinones are herein disclosed for use in the treatment of various elastase-mediated diseases.
    Type: Grant
    Filed: June 5, 1997
    Date of Patent: May 5, 1998
    Assignee: Merck & Co., Inc.
    Inventors: James Doherty, Conrad Dorn, Philippe Durette, Paul Finke, Malcolm Maccoss, Sander Mills, Shrenik Shah, Soumya Sahoo, William Hagmann, Jeffrey Hale, Thomas Lanza
  • Aralkylamino substituted azacyclic therapeutic agents
    Patent number: 5728716
    Abstract: Aralkylamino substituted azacyclic compounds of formula (I) and their salts and prodrugs. The variables are defined herein. The compounds are useful as tachykinin antagonists and are of particular use in the treatment of pain, inflammation, migraine, and emesis.
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: March 17, 1998
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Malcolm MacCoss, Christopher John Swain
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 5719147
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Treatment of migraine with morpholine tachykinin receptor antagonists
    Patent number: 5716942
    Abstract: Substituted heterocycles of the general 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: February 10, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Malcolm MacCoss, Jeffrey J. Hale, Sander G. Mills
  • Morpholine compounds are prodrugs useful as tachykinin receptor antagonists
    Patent number: 5691336
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, and emesis.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: November 25, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills
  • Prodrugs of herpes TK inhibitors
    Patent number: 5663175
    Abstract: Certain prodrugs such as ##STR1## are useful in the inhibition of herpes virus thymidine kinase, the prevention or treatment of recurrent infection by herpes virus, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating recurrent infection by herpes virus are also described.
    Type: Grant
    Filed: December 9, 1994
    Date of Patent: September 2, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Richard L. Tolman, John D. Karkas, Derek Von Langen, Malcolm MacCoss
  • Process for preparing morpholine tachykinin receptor antagonists
    Patent number: 5637699
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: June 10, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Paul E. Finke, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark S. Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian J. Williams
  • Cyclic amidine analogs as inhibitors of nitric oxide synthase
    Patent number: 5629322
    Abstract: Disclosed herein are compounds of Formula I ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 13, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Ravindra N. Guthikonda, Stephan K. Grant, Malcolm Maccoss, Shrenik K. Shah, Kothandaraman Shankaran, Charles G. Caldwell, Philippe L. Durette
  • N-acylpiperidine tachykinin antagonists
    Patent number: 5610165
    Abstract: N-Acylpiperidines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: March 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Malcolm MacCoss, Sander G. Mills
  • Substituted aryl piperazines as neurokinin antagonists
    Patent number: 5607936
    Abstract: Disclosed are substituted aryl piperazines of Formula I ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula I are shown to be neurokinin antagonists.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: March 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Yuan-Ching P. Chiang, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Daniel J. Miller, Sander G. Mills, Albert J. Robichaud, Shrenik K. Shah
  • Substituted azetidinones as anti-inflammatory and antidegenerative agents
    Patent number: 5591737
    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. ##STR1## wherein R.sub.4 is (a) ##STR2## or (b) ##STR3## where R.sub.x is carboxy C.sub.1-6 alkyl, benzyloxycarbonylC.sub.1-3 alkyl, or t-butoxycarbonylC.sub.1-3 alkyl,whereinQ is a covalent bond or ##STR4## wherein R.sub.5 and R.sub.6 are each individually C.sub.1-3 alkyl or hydrogen,Y is ##STR5## or a covalent bond.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: January 7, 1997
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Conrad P. Dorn, Philippe L. Durette, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Soumya P. Sahoo, Jeffrey J. Hale, Thomas J. Lanza, William K. Hagmann