Search Patents
  • Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment
    Patent number: 8455520
    Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5925651
    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 1, 1997
    Date of Patent: July 20, 1999
    Assignee: Merck & Co., Inc.
    Inventor: John H. Hutchinson
  • N-cyclopentyl modulators of chemokine receptor activity
    Patent number: 6472410
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, 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-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: October 29, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kevin T. Chapman, Malcolm Maccoss, Sander G. Mills, Jennifer L. Loebach, Bryan Oates
  • Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors
    Patent number: 5939418
    Abstract: Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: ##STR1## where X is O, S or NR.sup.15.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: August 17, 1999
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
  • Antipsychotic 1-cycloalkylpiperidines
    Patent number: 5266572
    Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
    Type: Grant
    Filed: June 18, 1992
    Date of Patent: November 30, 1993
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Gary A. Cain, Paul J. Gilligan, Sang W. Tam
  • BENZAMIDES
    Publication number: 20130023522
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: July 17, 2012
    Publication date: January 24, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
  • 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
    Patent number: 4996203
    Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.
    Type: Grant
    Filed: June 8, 1989
    Date of Patent: February 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
  • 2,5-disubstituted piperidine orexin receptor antagonists
    Patent number: 8669272
    Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, John D. Schreier, David B. Whitman
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5491164
    Abstract: The present invention comprises dipeptide analogs that inhibit the farnesylation of Ras. These farnesyl-protein transferase inhibitors are characterized by the inclusion of a cyclic amine in the backbone of the dipeptide. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: February 13, 1996
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel J. Graham
  • Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof
    Patent number: 10913733
    Abstract: The present invention is directed to thiazolyl piperidine compounds of the general structural formula I: which are inhibitors of O-GlcNAcase. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which O-GlcNAcase is involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which O-GlcNAcase is involved.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: February 9, 2021
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Harold G. Selnick, Yuanxi Zhou
  • Acylated piperidine derivatives as melanocortin-4 receptor agonists
    Patent number: 6818658
    Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: February 3, 2003
    Date of Patent: November 16, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Feroze Ujjainwalla, Lin Chu, Mark T. Goulet, Bonnie Louridas, Matthew J. Wyvratt, Daniel Warner
  • 1,3-oxazolidin-2-one derivatives useful as CETP inhibitors
    Patent number: 7915271
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: March 29, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
  • 1,3-OXAZOLIDIN -2-ONE DERIVATIVES USEFUL AS CETP INHIBITORS
    Publication number: 20110178059
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 21, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad ALI, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
  • Acylated piperidine derivatives as melanocortin-4 receptor agonists
    Patent number: 7700778
    Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: April 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
  • 1-aryloxy-3-(substituted aminoalkylamino)-2-propanols
    Patent number: 4593039
    Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as antihypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.
    Type: Grant
    Filed: April 2, 1984
    Date of Patent: June 3, 1986
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Sandor L. Varga, Gerald S. Ponticello
  • Novel NIP Thiazole Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydroge-Nase-1
    Publication number: 20110060007
    Abstract: The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: April 8, 2009
    Publication date: March 10, 2011
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftling
    Inventors: Caroline Leriche, Denis Carniato, Didier Roche, Christine Charon, Liliane Doare
  • CGRP receptor antagonists
    Patent number: 7491713
    Abstract: Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, pharmaceutical compositions comprising these compounds, use of these compounds and compositions to prevent or treat diseases involving CGRP.
    Type: Grant
    Filed: January 25, 2005
    Date of Patent: February 17, 2009
    Assignee: Merck + Co., Inc.
    Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams
  • 5-oxygenated HMG-CoA reductase inhibitors
    Patent number: 4963538
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Thiazolypiperidine derivatives as MTP inhibitors
    Patent number: 7674803
    Abstract: The present invention relates to thiazolylpiperidine derivatives of the general formula (I): in which: A represents a radical chosen from the radicals a1 and a2 below: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3 below: and R1, R2, R2?, R3, R4, R5, Y and Z are as defined in the description. Application of the compounds of the formula (I) to the treatment of hypertriglyceridaemia, hypercholesterolaemia and dyslipidaemia.
    Type: Grant
    Filed: June 2, 2004
    Date of Patent: March 9, 2010
    Assignee: Merck Patent GmbH
    Inventors: Philippe Guèdat, Francois Collonges, Hervé Dumas, Jean-Yves Ortholand, Jacques Decerprit, Jaxques Barbanton, Robert J. Foster, Peter Kane, Bernd Went
  • N-cyclopentyl modulators of chemokine receptor activity
    Patent number: 6593346
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, 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-5 and/or CCR-3.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: July 15, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates