Patents Represented by Attorney, Agent or Law Firm J. Eric Thies
  • Eosinophil eotaxin receptor
    Patent number: 6271347
    Abstract: The eosinophil eotaxin receptor has been isolated, cloned and sequenced. This receptor is a human &bgr;-chemokine receptor and has been designated “CC CKR3”. The eosinophil eotaxin receptor may be used to screen and identify compounds that bind to the eosinophil eotaxin receptor. Such compounds would be useful in the treatment and prevention of atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and particularly bronchial asthma.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: August 7, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Bruce L. Daugherty, Julie A. Demartino, Salvatore J. Siciliano, Martin S. Springer
  • Human neurokinin-3 receptor
    Patent number: 6258943
    Abstract: A recombinant human neurokinin-3 receptor (hereinafter identified as human NK3R) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK3R complementary DNA; expression systems, including a CHO (chinese hamster ovarian cell line) stable expression system; and an assay using the CHO expression system. Human NK3R can be used in an assay to identify and evaluate entities that bind to the neurokinin-3 receptor.
    Type: Grant
    Filed: July 12, 1993
    Date of Patent: July 10, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Tung Ming Fong, Ruey-Ruey C. Huang, Catherine D. Strader
  • Stabilization of the reagent dimethyl titanocene
    Patent number: 6255550
    Abstract: The present invention is directed to organic solutions of the reagent dimethyl titanocene which further comprise a sterically hindered ester and optionally titanocene dichloride. Stability of the reagent dimethyl titanocene is enhanced by the presence of the sterically hindered ester.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: July 3, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Mark Huffman
  • Process for the synthesis of 3,5-bis(trifluoromethyl)-bromobenzene
    Patent number: 6255545
    Abstract: The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)bromobenzene (CAS 328-70-1). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: July 3, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, Fuh-Rong Tsay
  • Method for treating attention deficit disorder
    Patent number: 6242446
    Abstract: Tachykinin receptor antagonists that are useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity in a patient, are desclosed.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: June 5, 2001
    Assignee: Merck & Co., Inc.
    Inventors: David L. Glatt, Mark S. Kramer, Nadia Rupniak
  • F-18 radiolabeled neurokinin-1 receptor antagonists
    Patent number: 6241964
    Abstract: The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
    Type: Grant
    Filed: September 28, 1999
    Date of Patent: June 5, 2001
    Assignee: Merck & Co., Inc.
    Inventors: H. Donald Burns, Terence G. Hamill, Raymond E. Gibson
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 6235735
    Abstract: Substituted heterocycles of the general structural formula: 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: March 16, 2000
    Date of Patent: May 22, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J Hale, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Tamara Ladduwahetty, Timothy Harrison, Brian John Williams
  • Method for treating or preventing psychosomatic and psychoimmunologic disorders
    Patent number: 6232311
    Abstract: A tachykinin receptor antagonist is useful for treating or preventing a psychosomatic disorder in a patient.
    Type: Grant
    Filed: August 10, 1999
    Date of Patent: May 15, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Nadia Rupniak, Mark S. Kramer
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6229010
    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)phenyl-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)phenyl-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 9, 1999
    Date of Patent: May 8, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Louis Crocker, James McCauley
  • Spiro-azacyclic derivatives and their use as therapeutic agents
    Patent number: 6225320
    Abstract: Substituted spiro-azacyclic derivatives of structural formula I are tachykinin receptor antagonists of use, for example, in the treatment of pain, inflammation, migraine, emesis and posttherpetic neuralgia Wherein A is a pyridyl, X is —CH2—, Y is —CH2— or —CH═ and q is 2.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 1, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher John Swain, Christopher George Thomson
  • Substituted 3-(benzylamino)piperidine derivatives and their use as therapeutic agents
    Patent number: 6214846
    Abstract: The present invention relates to compounds of formula (I), wherein R1 represents a fluoroC1-2alkoxy group; and R2 represents a hydrogen or halogen atom or a C1-4alkyl, C1-4alkoxy, fluoroC1-4alkyl or fluoroC1-4alkoxy group; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain or inflammation, migraine, emesis, postherpetic neuralgia, depression or anxiety.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: April 10, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Jason Matthew Elliott
  • Naphtho-fused lactams promote release of growth hormone
    Patent number: 6211174
    Abstract: The present invention is directed to certain naphtho-fused lactams of the general structural formula: wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6, A, L, X, n, p and w 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.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: April 3, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. Devita, Matthew J. Wyvratt
  • Tachykinin antagonist and an opioid analgesic effective at treating pain or nociception
    Patent number: 6180624
    Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a morpholine or thiomorpholine tachykinin antagonist and an opioid analgesic.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: January 30, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Raymond George Hill
  • Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one
    Patent number: 6177564
    Abstract: The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula: This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
    Type: Grant
    Filed: September 9, 1999
    Date of Patent: January 23, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Todd D. Nelson, Mahadevan Bhupathy
  • Spiro-azacyclic derivatives and their use as therapeutic agents
    Patent number: 6172077
    Abstract: The present invention is directed to substituted spiro-azacyclic derivatives of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R9, R10, X, Y, p and q 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: October 22, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Jason Matthew Elliott, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Pyrrolidine and piperidine modulators of chemokine receptor activity
    Patent number: 6166037
    Abstract: The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Budhu, Edward Holson, Jeffrey J. Hale, Christopher Lynch, Malcolm Maccoss, Scott C. Berk, Sander G. Mills, Christopher A. Willoughby
  • Use of an NK-1 receptor antagonist and an SSRI for treating obesity
    Patent number: 6162805
    Abstract: The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: December 19, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Franz Fridolin Hefti
  • Use of NK-1 receptor antagonists for treating movement disorders
    Patent number: 6156749
    Abstract: The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 antagonist for the manufacture of a medicament for oral administration for the treatment or prevention of movement disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Nadia Melanie Rupniak
  • Cyclic amine modulators of chemokine receptor activity
    Patent number: 6140349
    Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: February 1, 1999
    Date of Patent: October 31, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Malcolm Maccoss, Paul E. Finke, Sander G. Mills, Bryan Oates, Shankaran Kothandaraman, Dooseop Kim, Liping Wang
  • Use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine to treat motion sickness
    Patent number: 6140324
    Abstract: The present invention relates to the use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine for the treatment or prevention of motion sickness. There is also provided pharmaceutical compositions and products comprising a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: October 31, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Frederick David Tattersall