Patents Represented by Attorney, Agent or Law Firm David L. Rose
  • Naphthyl compounds promote release of growth hormone
    Patent number: 6121325
    Abstract: The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: September 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Meng Hsin Chen, Gregori J. Morriello, Ravi Nargund, Arthur A. Patchett, Lihu Yang
  • Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
    Patent number: 6117855
    Abstract: The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of CNS-penetrant NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: September 12, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Emma Joanne Carlson, Nadia Melanie Rupniak
  • Somatostatin agonists
    Patent number: 6117880
    Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are also orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostastin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. Further objects will become apparent from reading the following description.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: September 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Liangquin Guo, Ralph T. Mosley, Alexander Pasternak, Arthur A. Patchett, Lihu Yang
  • Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
    Patent number: 6114315
    Abstract: The present invention provides methods for the treatment or prevention of major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
    Type: Grant
    Filed: June 11, 1998
    Date of Patent: September 5, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Antiemetic use of triazolo-pyridazine derivatives
    Patent number: 6110915
    Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, as shown in Formula I, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of emesis.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: August 29, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jose Luis Castro Pineiro, Frederick David Tattersall
  • Histone deacetylase as target for antiprotozoal agents
    Patent number: 6110697
    Abstract: Histone deacetylase inhibition provides a target for identifying potential antiprotozoal compounds. Histone deacetylase inhibitors are useful as therapeutic agents against protozoal infections.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: August 29, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Paula M. Dulski, Robert W. Myers, Anne M. Gumett, Sandra J. Rattray, Dennis M. Schmatz
  • Neuroprotective use of triazolo-pyridazine derivatives
    Patent number: 6107296
    Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives as shown in Formula I, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit therof, and are accordingly of benefit in the treatment and/or prevention of neurodegeneration arising from cerebral ischemia.
    Type: Grant
    Filed: December 7, 1998
    Date of Patent: August 22, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventor: Jose Luis Castro Pineiro
  • Diazabicyclooctane derivatives having selective 5-HT.sub.1Dalpha agonist activity
    Patent number: 6107321
    Abstract: A class of 3-substituted 3,7-diazabicyclo[3.3.0]octane derivatives, further substituted at the 7-position by an optionally substituted alkenyl, alkynyl, arylcarbonyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: August 22, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Andrew Madin
  • Use of NK-1 receptors antagonists for treating schizophrenic disorders
    Patent number: 6100256
    Abstract: The present invention provides a method for the treatment or prevention of schizophrenic disorders using an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
    Type: Grant
    Filed: June 11, 1998
    Date of Patent: August 8, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen May Seward, Christopher John Swain, Brian John Williams
  • Use of NK-1 receptor antagonists for treating amnestic disorders
    Patent number: 6096729
    Abstract: The present invention provides methods for the treatment or prevention of amnestic disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: August 1, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6096742
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Grant
    Filed: December 15, 1998
    Date of Patent: August 1, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Louis Crocker, James McCauley
  • 3-benzylaminopiperidines as tachykinin receptor antagonists
    Patent number: 6096766
    Abstract: The present invention relates to certain 3-benzylaminopiperidines which are tachykinin receptor antagonists and are useful in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: June 9, 1998
    Date of Patent: August 1, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Jason Matthew Elliott, Christopher John Swain
  • Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative agents
    Patent number: 6090785
    Abstract: Novel N-carboxyalkylpeptidyl compounds represented by the formula ##STR1## which are found to be useful inhibitors of matrix metalloendoproteinases which degrade major components of articular cartilage and basement membranes causing degenerative diseases such as arthritis, periodontal disease, corneal ulceration and the like, and certain cancers, are described.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Craig K. Esser, William K. Hagmann, Ihor E. Kopka
  • Substituted pyrrole derivatives as cell adhesion inhibitors
    Patent number: 6090841
    Abstract: Substituted pyrrole derivatives of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Linda Chang, Malcolm MacCoss, William K. Hagmann
  • Antidiabetic agents
    Patent number: 6090839
    Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
  • Use of NK-1 receptor antagonists for treating mania
    Patent number: 6090819
    Abstract: A method for the treatment or prevention of mania or hypomania is disclosed comprising administering 3-[2-cyclopropoxy-5-(trifluoromethoxy)phenyl]-6-phenyl-1-oxa-7-aza-spiro[4 .5]decane.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: July 18, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventor: Nadia Melanie Rupniak
  • Benzisoxazole-derived antidiabetic compounds
    Patent number: 6090836
    Abstract: The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Joel P. Berger, Gregory D. Berger, Kenneth J. Fitch, Donald W. Graham, Anthony B. Jones, Derek von Langen, Mark D. Leibowitz, David E. Moller, Arthur A. Patchett, Conrad Santini, Soumya P. Sahoo, Richard L. Tolman, Richard B. Toupence, Thomas F. Walsh
  • Use of NK-1 receptor antagonists for treating stress disorders
    Patent number: 6087348
    Abstract: The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: July 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Method of enhancing cognition with 2-(4-methoxyphenyl)-pyrazolo[4,3-c]quinolin-3-one
    Patent number: 6087372
    Abstract: The present invention provides the use of 2-(4-methoxyphenyl)-pyrazolo[4,3-c]quiniolin-3-one or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for enhancing cognition, particularly in Alzheimer's Disease, a method of enhancing cognition and pharmaceutically acceptable salts such as the hemi camphor sulfonate.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: July 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Gerard Raphael Dawson, Angus Murray MacLeod, Guy Ralph Seabrook
  • Spiro-ketal derivatives and their use as therapeutic agents
    Patent number: 6080740
    Abstract: The present invention is directed to spiro-ketal derivatives of the formula (I): ##STR1## (wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are defined herein) which are tachykinin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jonathan David Moseley, Christopher John Swain