Patents Assigned to Merck Sharp
  • Patent number: 8580938
    Abstract: The invention relates to binding compounds that specifically bind to human TSLP, as well as uses thereof, e.g., in the treatment of inflammatory disorders.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Rene de Waal Malefyt
  • Patent number: 8580782
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, 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 diseases associated with the CDKs using such compounds or compositions.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc A. Labroli, Kartik M. Keertikar
  • Publication number: 20130296278
    Abstract: A compound having the structure (I) useful for treating hypertension, pulmonary arterial hypertension, congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Application
    Filed: January 12, 2012
    Publication date: November 7, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Shrenik K. Shah, James Dellureficio
  • Patent number: 8575166
    Abstract: This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason L. Davis, Michael John Mayer, Hubert B. Josien
  • Patent number: 8575152
    Abstract: This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or —(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, —(1-4C)alkyl or —OR16; —R4 is —H, —(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; —(1-6C)alkyl, —(2-6C)alkenyl or —(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; —(1-6C)alkyl, —(2-6C)alkenyl, —(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, —(1-4C)alkyl, —(1-4C)alkoxy, —(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or —(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or —(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or —(1-4C)alkyl; —R13 is —H, —(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, —(
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ralf Plate, Christiaan Gerardus Johannes Maria Jans
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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