Patents Assigned to Merck Sharp
  • TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20160229850
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: September 17, 2014
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS
    Publication number: 20160228419
    Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: September 26, 2014
    Publication date: August 11, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Tao Yu, Yonglian Zhang, Sherman Tim Waddell, Andrew Stamford, John S. Wai, Paul J. Coleman, John M. Sanders, Ronald Ferguson
  • Bridged bicyclic piperidine derivatives and methods of use thereof
    Patent number: 9409918
    Abstract: The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: August 9, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Andrew Stamford, William J. Greenlee, Santhosh Francis Neelamkavil
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9409924
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: August 9, 2016
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Tong-Shuang Li, Ernest McEachern, David Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold Selnick
  • Piperidinone carboxamide spirohydantoin CGRP receptor antagonists
    Patent number: 9409916
    Abstract: The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and 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: March 14, 2012
    Date of Patent: August 9, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Justin Belardi
  • 5?-substituted nucleoside analogs and methods of use thereof for the treatment of viral diseases
    Patent number: 9408863
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: August 9, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • FORMULATIONS FOR CGRP RECEPTOR ANTAGONISTS
    Publication number: 20160220552
    Abstract: The instant invention relates to liquid pharmaceutical compositions containing CGRP receptor antagonists. The CGRP receptor antagonist liquid pharmaceutical compositions of the instant invention are alcohol-free, low volume liquid pharmaceutical compositions that can be taken without water for the treatment of migraine headache.
    Type: Application
    Filed: September 11, 2014
    Publication date: August 4, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Majid Mahjour, Leonardo R. Allain, Sutthilug Sotthivirat, Russell G. Maus, Rebecca Nofsinger, Lisa Lupton, Wei Xu, Francis Flanagan
  • C5-SPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20160222032
    Abstract: In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. 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, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: September 8, 2014
    Publication date: August 4, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Wen-Lian Wu, Jared N. Cumming
  • TRICYCLIC GYRASE INHIBITORS
    Publication number: 20160222015
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Application
    Filed: September 10, 2014
    Publication date: August 4, 2016
    Applicants: Merck Sharp & Dohme Corp., Lawrence Livermore National Security, LLC
    Inventors: John Finn, Leslie William Tari, Zhiyong Chen, Junhu Zhang, Douglas Phillipson, Suk Joong Lee, Michael Trzoss, Daniel Bensen, Xiaoming Li, Min Teng, Voon Ong, Allen John Borchardt, Thanh To Lam, Felice C. Lightstone, Sergio E. Wong, Toan B. Nguyen
  • Mineralocorticoid receptor antagonists
    Patent number: 9403807
    Abstract: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: August 2, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alejandro Crespo, Ping Lan, Rudrajit Mal, Anthony Ogawa, Hong Shen, Peter J. Sinclair, Zhongxiang Sun, Ellen K. Vande Bunte, Zhicai Wu, Kun Liu, Robert J. DeVita, Dong-Ming Shen, Min Shu, John Qiang Tan, Changhe Qi, Yuguang Wang, Richard Beresis
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 9403790
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: August 2, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber, Ping Chen
  • Fc CONTAINING POLYPEPTIDES HAVING INCREASED BINDING TO FcGammaRIIB
    Publication number: 20160215061
    Abstract: The present invention is directed to methods and compositions for the production of Fc-containing polypeptides which are useful as human or animal therapeutic agents, and which comprise increased anti-inflammatory properties and improved FcyRIIb binding.
    Type: Application
    Filed: October 3, 2014
    Publication date: July 28, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Hussam H. Shaheen, Andy Stadheim, Natarajan Sethuraman
  • 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS
    Publication number: 20160214997
    Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
    Type: Application
    Filed: August 25, 2014
    Publication date: July 28, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ali Amjad, Gioconda V. Gallo, Timothy J. Henderson, Rongze Kuang, Yeon-Hee Lim, Michael Man-Chu Lo, Edward Metzger, Manuel de Lera Ruiz, Andrew Stamford, Paul Tempest, Brent Whitehead, Heping Wu
  • 2-PYRIDYLOXY-4-ESTER OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20160214960
    Abstract: The present invention is directed to 2-pyridyloxy-4-ester compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ester compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: December 16, 2013
    Publication date: July 28, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: SCOTT D. KUDUK, JASON W. SKUDLAREK
  • Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
    Patent number: 9399651
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: July 26, 2016
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, Wesley B. Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan R. Kett, Amy Zartman
  • PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
    Publication number: 20160207926
    Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflamation, asthma, COPD and cancer.
    Type: Application
    Filed: November 15, 2013
    Publication date: July 21, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Michael D. Altman, Yongqi Deng, Solomon Kattar, Jason D. Katz, Joey L. Methot, Hua Zhou, Meredeth McGowan, Matthew P. Christopher, Yudith Garcia, Neville John Anthony, Francesc Xavier Fradera Llinas, Liping Yang, Changwei Mu, Xiaona Wang, Feng Shi, Baijun Ye, Sixing Zhang, Xiaoli Zhao, Rong Zhang, Kin Chiu Fong, Xiansheng Leng
  • Inhibitors of the Renal Outer Medullary Potassium Channel
    Publication number: 20160207922
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: July 28, 2014
    Publication date: July 21, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Ronald Dale Ferguson, II, Zack Zhiqiang Guo, Harry Chobanian, Jessica Frie, Yan Guo, Zhicai Wu, Yang Yu, Ming Wang
  • Inhibiting the transient receptor potential A1 ion channel
    Patent number: 9394308
    Abstract: This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain and respiratory conditions.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: July 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingyi Li, Lily Cheng, Christopher M. Liu, Iwona E. Wrona, Blaise S. Lippa, Chester A. Metcalf, III, Andrew J. Jackson, Lauren M. Chapman
  • Pyrazole carboxamides as Janus kinase inhibitors
    Patent number: 9394282
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: July 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
  • PREPARATION AND USE OF 3-PYRIDYL SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS
    Publication number: 20160200713
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is halo; —CN; alkyl; cycloalkyl; alkoxy; phenyl, which is optionally substituted one or twice independently by alkyl, halo, or —CN; or a thiophene ring, which is optionally substituted once or twice independently by alkyl. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Application
    Filed: August 18, 2014
    Publication date: July 14, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: James Francis Dropinski, Milana Maletic, Jae-hun Kim, Deyou Sha