Patents Represented by Attorney, Agent or Law Firm David L. Rose
  • 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
  • Gamma-ketoacid dipeptides as inhibitors of caspase-3
    Patent number: 6225288
    Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: May 1, 2001
    Assignee: Merk Frosst Canada & Co.
    Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
  • Sulfonamides as cell adhesion inhibitors
    Patent number: 6221888
    Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;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 29, 1999
    Date of Patent: April 24, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Malcolm Maccoss, Sander G. Mills, Richard A. Mumford
  • Nodulisporic acid derivatives
    Patent number: 6221894
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: April 24, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Peter T. Meinke, Thomas L. Shih, Michael H. Fisher
  • Diaryl-2-(5H)-furanones as Cox-2 inhibitors
    Patent number: 6222048
    Abstract: The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula (I). The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: April 24, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cameron Black, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
  • 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
  • Prostaglandin receptor ligands
    Patent number: 6211197
    Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q  II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.
    Type: Grant
    Filed: October 4, 1999
    Date of Patent: April 3, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
  • Aminocyclohexane derivatives as 5-HT receptor agonists
    Patent number: 6211219
    Abstract: A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; 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-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
    Type: Grant
    Filed: January 4, 1999
    Date of Patent: April 3, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
  • Diphenyl-1,2,3-thiadiazol-3-oxides, compositions and methods of use
    Patent number: 6211210
    Abstract: The invention encompasses compounds of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: April 3, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cheuk Kun Lau, Chun-Sing Li, Cameron Black, Michel Therien, Jacques Yves Gauthier
  • 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
  • Substituted imidazoles having cytokine inhibitory activity
    Patent number: 6207687
    Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which may be useful for the treatment of cytokine mediated diseases such as arthritis.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: March 27, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
  • PDE IV inhibiting compounds, compositions and methods of treatment
    Patent number: 6204275
    Abstract: The invention encompasses compounds of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: March 20, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Richard Friesen, Yvbes Ducharme, Daniel Dube, Yves Girard, Richard Frenette, Chun Li, Marc Blouin, Nathalie Chauret, Laird Trimble
  • Leukotriene C4 synthase
    Patent number: 6204034
    Abstract: Leukotriene C4 synthase polypeptide identified by photoaffinity labelling, and purification of leukotriene C4 synthase to homogeneity is described.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: March 20, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventor: Donald W. Nicholson
  • Process for making diaryl pyridines useful as COX-2 inhibitors
    Patent number: 6204387
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: March 23, 2000
    Date of Patent: March 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Linda Gerena, Michel Journet, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives as GABA alpha 5 ligands
    Patent number: 6200975
    Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: March 13, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
  • Substituted 1H-pyridinyl-2-ones as GABAA-&agr; 2/3 ligands
    Patent number: 6200982
    Abstract: Substituted 1H-Pyridinyl-2-ones are useful as GABAA-Alpha 2/3 ligands.
    Type: Grant
    Filed: February 11, 2000
    Date of Patent: March 13, 2001
    Assignee: Merck & Dohme Limited
    Inventors: Ian James Collins, Stephen Robert Fletcher, Timothy Harrison, Paul David Leeson, Christopher Richard Moyes, Alan John Nadin, Michael Rowley, Timothy Jason Sparey, Martin Richard Teall
  • Heterosubstituted pyridine derivatives as PDE4 inhibitors
    Patent number: 6200993
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4). or a pharmaceutically acceptable salt or hydrate thereof. The invention also encompasses pharmaceutical compositions and methods for treatment.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: March 13, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Bernard Cote, Richard Friesen, Richard Frenette, Mario Girard, Yves Girard, Cedrickx Godbout, Daniel Guay, Pierre Hamel, Marc Blouin, Yves Ducharme, Sylvie Prescott
  • Arylthiazolidinedione derivitives
    Patent number: 6200998
    Abstract: Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: March 13, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Soumya P. Sahoo, Wei Han, Richard L. Tolman, Jeffrey Bergman, Conrad Santini, Ranjit Desai, Victoria K. Lombardo, Julia K. Boueres, Dominick F. Gratale
  • Enhancement of return to independent living status with a growth hormone secretagogue
    Patent number: 6194402
    Abstract: A growth hormone secretagogue is useful for enhancing the return of patients to independent living status following acute deconditioning such as that which may result from immobilization, surgery, or major injury such as hip fracture.
    Type: Grant
    Filed: August 31, 1999
    Date of Patent: February 27, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark Bach, Vivian Fuh, Jennifer Ng, Alice Taylor