Patents Assigned to Merck Sharp and Dohme
  • Triazole derivatives for treatment of Alzheimer's disease
    Patent number: 8575150
    Abstract: According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A?42 and hence are useful in treatment of Alzheimer's disease and related conditions.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Joey Methot, Hua Zhou, Adam J. Schell, Benito Munoz, Alexey A. Rivkin, Sean P. Ahearn, Stephanie Chichetti, Rachel N. MacCoss, Sam Kattar, Matthew Christopher, Chaomin Li, Andrew Rosenau, William Colby Brown
  • Active metabolite of a thrombin receptor antagonist
    Patent number: 8575351
    Abstract: Disclosed herein is an active metabolite (“M20”) of a molecule that is useful as a thrombin receptor antagonist: Also disclosed are formulations of this compound, synthetic routes to this compound, and methods of treating a variety of cardiovascular conditions, including acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering the active metabolilte.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kimberly Nguyen Voronin, Natalia A. Penner
  • COMBINATION THERAPY FOR TREATING CANCER COMPRISING AN IGF-1R INHIBITOR AND AN AKT INHIBITOR
    Publication number: 20130287763
    Abstract: The present invention relates to a method of treating cancer by administering an IGF-1R specific antibody in combination with an anti-cancer agent exemplified by an Akt pathway inhibitor. The first and second amounts together comprise a therapeutically effective amount.
    Type: Application
    Filed: July 25, 2011
    Publication date: October 31, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Sriram Sathyanarayanan, Christopher Winter, Andrew Bloecher, Erin Valentine
  • Bicyclic dihydroimidazolone CGRP receptor antagonists
    Patent number: 8569291
    Abstract: Compounds of formula (I): wherein variables B, G1, G2, G3, G4, Ea, Eb, Ec, A1, A2, A3, A4, R6 and RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Craig A. Stump
  • Biaryl-spiroaminooxzaoline analogues as alpha 2C adrenergic receptor modulators
    Patent number: 8569312
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
    Patent number: 8569310
    Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula (a) have the general structure: (a) wherein each variable is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ulrich Iserloh, Andrew W. Stamford, Jared N Cumming
  • Method for reducing the appearance of false positive bands in SDS-page analysis of proteolytic digestion of a sample
    Patent number: 8569007
    Abstract: The present invention includes a method for reducing the appearance of false positive bands in SDS-PAGE analysis of proteolytic digestion, of a sample that comprises an immunoglobulin polypeptide, at pH 8.8.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kimberly Margaret Louise May, Susan V. Cannon-Carlson, Brittany Charlotte Larkin, Collette Marie Cutler
  • P2Xreceptor antagonists for treatment of pain
    Patent number: 8569512
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Brendan M. Crowley, Zhengwu J. Deng, Daniel V. Paone, Craig M. Potteiger
  • Prolylcarboxypeptidase inhibitors
    Patent number: 8569299
    Abstract: Compounds of structural formulas I-1 and I-2 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 3, 2011
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Thomas H. Graham, Wensheng Liu, Iyassu K. Sebhat, Dong-Ming Shen, Zhi-Cai Shi
  • Intrauterine system
    Patent number: 8568374
    Abstract: An intrauterine system is disclosed for use in the treatment of dysfunctional uterine bleeding; menorraghia; dysmenorrhoea; endometriosis; uterine fibroids; climacteric complaints; osteoporosis; and urogenital atrophy. The system is formed by a frame defining an interior space for receipt of a deposit of a therapeutically effective dose of a biologically active compound. The frame has an open structure allowing access to a substantial part of an outer surface of the deposit, and the deposit has a rate controlling structure that controls a rate of release of the compound within the uterus. One or more retention elements are provided on the frame for retaining the frame within the uterus of a female mammal.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Wouter De Graaff, Harm Veenstra, Titia Martine Truce Mulders
  • Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
    Patent number: 8569521
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Anne Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao
  • FUSED TRICYCLIC INHIBITORS OF MAMMALIAN TARGET OF RAPAMYCIN
    Publication number: 20130281474
    Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Application
    Filed: September 26, 2011
    Publication date: October 24, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Zhaoyang Meng, Panduranga Abdulla Reddy, M. Arshad Siddiqui
  • POLYCYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20130280214
    Abstract: The present invention relates to Polycyclic Heterocycle Derivatives, such as compound 1: (1) compositions comprising the Polycyclic Heterocycle Derivatives, and methods of using the Polycyclic Heterocycle Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: September 28, 2011
    Publication date: October 24, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph P. Vacca, Craig A. Coburn, David B. Olsen, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Cyclic benzimidazole derivatives useful as anti-diabetic agents
    Patent number: 8563746
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: October 22, 2013
    Assignees: Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.
    Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
  • Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
    Patent number: 8563543
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: October 22, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Lingyan Wang, Wei Li
  • 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
    Patent number: 8557848
    Abstract: The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Srikanth Venkatraman, F. George Njoroge, Stuart B. Rosenblum, Charles A. Lesburg, Jose S. Duca, Neng-Yang Shih, Francisco Velazquez, Gopinadhan N. Anilkumar, Qingbei Zeng, Joseph A. Kozlowski
  • Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
    Patent number: 8557826
    Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew W. Stamford, Jared N Cumming
  • Aryl methyl benzoquinazolinine M1 receptor positive allosteric modulators
    Patent number: 8557832
    Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
  • Heterocyclic fused phenanthrolinone M1 receptor positive allosteric modulators
    Patent number: 8557992
    Abstract: The present invention is directed to heterocyclic fused phenanthrolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: June 10, 2011
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Macrocyclic heterocyclic aspartyl protease inhibitors
    Patent number: 8557798
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt