Search Patents
  • Silylated piperidine derivatives
    Patent number: 8420622
    Abstract: Compounds of formula I: I wherein at least one of R4 and R5 comprises Si(R6)3 as a substituent selectively attenuate production of A?(1-42) and hence find use in treatment of Alzheimer's disease and related conditions.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 16, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Benito Munoz, Jed Hubbs, Christopher L. Hamblett, Hua Zhou, Michelle Martinez
  • 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
  • Mitotic Kinesin Inhibitors
    Publication number: 20090005418
    Abstract: The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: August 15, 2005
    Publication date: January 1, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6077853
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Steven D. Young
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5972966
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherpeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: October 26, 1999
    Assignee: Merck & Co., Inc.
    Inventor: S. Jane deSolms
  • Fibrinogen receptor antagonist prodrugs
    Patent number: 5990107
    Abstract: Fibrinogen receptor antagonist alcohol prodrugs having the structure, for example, of ##STR1## more particularly, ##STR2##
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: November 23, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Melissa S. Egbertson, George D. Hartman, William C. Lumma, John S. Wai, Steven D. Young
  • Piperidinylmethyloxazolidinone derivative
    Patent number: 6413989
    Abstract: The invention relates to the compound 5-[4-(4-fluorobenzyl) piperidin-1-ylmethyl]-3-(4-hydroxy-phenyl)oxazolidin-2-one of the formula I and to physiologically acceptable salts thereof. The compound acts as a neuroleptic.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: July 2, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Helmut Prucher, Gerd Bartoszyk, Christoph Seyfried, Rudolf Gottschlich, Joachim Leibrock
  • 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
  • Method for treating inflammatory diseases by administering a thrombin inhibitor
    Patent number: 6362190
    Abstract: The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with an oral composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis and sarcoidosis.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: March 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jules Shafer, Denise M. Visco
  • 4-Benzylthiophene (or furan)-2-sulfonamides as antiglaucoma agents
    Patent number: 4914111
    Abstract: Thiophene (or furan)-2-sulfonamides with a 4-benzyl substituent are effective in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration.
    Type: Grant
    Filed: March 23, 1987
    Date of Patent: April 3, 1990
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Wasyl Halczenko
  • .beta.-adrenergic blocking imidazolylphenoxy propanolamines
    Patent number: 4642311
    Abstract: Substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: May 7, 1984
    Date of Patent: February 10, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • 4-aryl-4-piperidine (or pyrrolidine or hexahydroazepine) carbinols and heterocyclic analogs thereof
    Patent number: 5086063
    Abstract: Known and novel 4-aryl-4-piperidinecarbinols and heterocyclic analogs are useful as analgesics. Also provided are novel pyrrolidinecarbinols and hexahydroazepine carbinols which are useful as analgesics, antidepressants and, in some cases, as anorectic agents.
    Type: Grant
    Filed: August 28, 1989
    Date of Patent: February 4, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Engelbert Ciganek, Leonard Cook
  • Indolepiperidine derivatives
    Patent number: 5670511
    Abstract: Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: September 23, 1997
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Joachim Marz, Hartmut Greiner, Christoph Seyfried, Gerd Bartoszyk
  • IMIDAZOLE DERIVATIVES
    Publication number: 20100249132
    Abstract: Compounds of the formula (I), in which R1, D, E, L, Q, X and q have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.
    Type: Application
    Filed: September 9, 2008
    Publication date: September 30, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Melanie Schultz, Kai Schiemann, Gerard Botton, Andree Blaukat, Ingo Kober
  • NOVEL CASE OF RENIN INHIBITORS
    Publication number: 20100120859
    Abstract: The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: May 23, 2008
    Publication date: May 13, 2010
    Applicant: MERCK FROSST CANADA LTD.
    Inventors: Tom Yao-Hsiang Wu, Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Erich L. Grimm, Sebastien Laliberte, Austin Chen
  • Triaryl substituted imidazoles as glucagon antagonists
    Patent number: 5880139
    Abstract: 2,4-Diaryl-5-pyridylimidazoles are glucagon antagonists. The compounds block the action of glucagon at its receptor. Thus, the compounds can be used in the prophylaxis or treatment of disease states in mammals mediated by elevated levels of glucagon. Examples of such disease states include diabetes, obesity, hypertension, and cachexia and the like.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Linda L. Chang
  • Conformationally restricted HIV-1 protease inhibitors
    Patent number: 5512560
    Abstract: HIV protease inhibitors containing hydroxypyrrolidine or hydroxypiperidine with one or more basic amines are disclosed.
    Type: Grant
    Filed: March 29, 1994
    Date of Patent: April 30, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Byeong M. Kim, Joseph P. Vacca
  • L-654,040, antibacterial agent
    Patent number: 4963569
    Abstract: L-654,040 of the structure: ##STR1## is a novel antibacterial and isolated from the novel organism Streptoverticillium synroense, strain MA6011, deposited at the ATCC.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Sara A. Currie, Thomas W. Miller, Eugene L. Dulaney, James P. Springer, Mary E. Valiant, Sagrario Mochales del Val, Sheldon B. Zimmerman
  • Prolylcarboxypeptidase inhibitors
    Patent number: 9006268
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: June 6, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John S. Debenham, Jinlong Jiang, Christina B. Madsen-Duggan, Dong-Ming Shen
  • PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS
    Publication number: 20120071460
    Abstract: The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description.
    Type: Application
    Filed: June 7, 2010
    Publication date: March 22, 2012
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, Charles Baker-Glenn, Wesley Blackaby, Chris Knight