Patents Assigned to Merck Sharp
  • METALLO-BETA-LACTAMASE INHIBITORS
    Publication number: 20160333021
    Abstract: The present invention relates to compounds of formula (I) that are metallo-?-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with ?-lactam antibiotics for overcoming resistance.
    Type: Application
    Filed: January 16, 2015
    Publication date: November 17, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mihir Mandal, Haifeng Tang, Li Xiao, Jing Su, Guoqing Li, Shu-Wei Yang, Weidong Pan, Haiqun Tang, Reynalda DeJesus, Jacqueline Hicks, Matthew Lombardo, Hong Chu, William Hagmann, Alex Pasternak, Xin Gu, Jinlong Jiang, Shuzhi Dong, Fa-Xiang Ding, Clare London, Dipshikha Biswas, Katherine Young, David N. Hunter, Zhiqiang Zhao, Dexi Yang
  • Process for preparing fluoroleucine alkyl esters
    Patent number: 9493400
    Abstract: This invention relates to a resolution process for the preparation of fluoroleucine alkyl esters.
    Type: Grant
    Filed: March 25, 2013
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nelo Rivera, Yadagiri R. Pendri, Sreenivas Mende, Bramhananda N. Reddy
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9493474
    Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
  • Acyclic cyanoethylpyrazoles as janus kinase inhibitors
    Patent number: 9493441
    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: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
  • Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
    Patent number: 9493461
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Zhong Lai, Ravi Nargund, Karen Marcantonio, Dong Xiao, Linda L. Brockunier, Nicolas Zorn, Qun Dang, Xuanjia Peng, Peng Li
  • Compounds inhibiting leucine-rich repeat kinase enzyme activity
    Patent number: 9493440
    Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. 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 LRRK-2 kinase is involved.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Wei Li, Andrew Stamford, Marc Poirer, Paul Tempest
  • Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
    Patent number: 9493479
    Abstract: The present invention relates to 4-Pyridone Compounds of Formula (I); and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, and R3 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridone Compound, and methods of using the 4-Pyridone Compounds for treating or preventing HIV infection in a subject or the clinical manifestations thereof.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, John S. Wai, Andrew Stamford, Wensheng Liu
  • THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
    Publication number: 20160326156
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Application
    Filed: December 18, 2014
    Publication date: November 10, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas A. Miller, Alessia Petrocchi, Eric T. Romeo, Dilrukshi Vitharana, Solomon D. Kattar, Alan B. Northrup, Michael D. Altman, Neville J. Anthony
  • BTK INHIBITORS
    Publication number: 20160326164
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Application
    Filed: December 16, 2014
    Publication date: November 10, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JIAN LIU, RONALD M. KIM, JOSEPH KOZLOWSKI, DEODIALSINGH GUIADEEN, ARTO D. KRIKORIAN, YOUNONG YU
  • C-6 Spirocarbocyclic Iminothiadiazine Dioxides as BACE Inhibitors, Compositions, and Their Use
    Publication number: 20160326155
    Abstract: In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R4, ring A, RA, m, L1, and RL 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: December 14, 2014
    Publication date: November 10, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Jared N. Cumming, Timothy Blizzard, Michael Ellis
  • 3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof
    Patent number: 9487490
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: November 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth J. Barr, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Dongshan Zhang, Brian M. Andresen, Neville J. Anthony, Blair T. Lapointe, Nunzio Sciammetta
  • Pyrrolidine derived beta 3 adrenergic receptor agonists
    Patent number: 9486448
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: November 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth Jay Barr, Mark E. Scott, Christopher F. Thompson, Neville Anthony, Carolyn Michele Cammarano, Raman Kumar Bakshi, Subhendu Kumar Mohanty, Chandra Sekhar Korapala, Prashant R. Latthe, Vyjayanthi N. Kambam, Sujit Kumar Sarkar, Jayanth Thiruvellore Thatai
  • Mineralocorticoid receptor antagonists
    Patent number: 9487506
    Abstract: Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: November 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ping Lan, Kun Liu, Anthony Ogawa, Hong Shen, Christine Yang, Yuguang Wang, Richard Beresis, Changhe Qi
  • Process for making CGRP receptor antagonists
    Patent number: 9487523
    Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine, utilizing a highly effective spiroacid synthesis.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin M. Belyk, Edward Cleator, Shen-Chun Kuo, Peter Emmanuel Maligres, Bangping Xiang, Nobuyoshi Yasuda, Jianguo Yin
  • C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
    Patent number: 9489013
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted thiadiazine compounds, including compounds Formula (I): (structure represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R4, ring A, RA, m, -L1-, RL, and ring C 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: Grant
    Filed: December 16, 2013
    Date of Patent: November 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Andrew W. Stamford, Ulrich Iserloh
  • Imidazolyl analogs as syk inhibitors
    Patent number: 9487504
    Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: November 8, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Jongwon Lim, Michael H. Reutershan, John Michael Ellis, Kaleen Konrad Childers, Anthony Donofrio, Michael D. Altman, Andrew M. Haidle, Anna Zabierek, Matthew Christopher, Jonathan Grimm, Jason Burch, Maria Emilia Di Francesco, Alessia Petrocchi, Christian Beaulieu, Vouy Linh Truong, Alan B. Northrup, Marc Blouin
  • DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20160318923
    Abstract: The present invention is directed to diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the diazepane 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, 2014
    Publication date: November 3, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: SCOTT D. KUDUK, THOMAS S. REGER, ANTHONY J. ROECKER
  • Liposomal Formulations for Allosteric AKT Inhibitors
    Publication number: 20160317444
    Abstract: Disclosed herein is a lipid nanoparticle (LNP) composition comprising (a) an Akt inhibitor; (b) DSPC; (c) cholesterol; and (d) PEG-DMG. Also disclosed herein is a method for preparing the lipid composition using a scalable tangential flow micro-mixing technology.
    Type: Application
    Filed: December 12, 2014
    Publication date: November 3, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael Hughes Smith, Marian Gindy
  • FUSED BICYCLIC ISOXAZOLINES AS INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN
    Publication number: 20160318950
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is (CH2) or O, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:
    Type: Application
    Filed: December 12, 2014
    Publication date: November 3, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick SHAO, Feng YE, Petr VACHAL
  • MEDIA MILLING PROCESS FOR THE MANUFACTURE OF ACTIVE PHARMACEUTICAL INGREDIENTS IN PROPELLANTS
    Publication number: 20160317391
    Abstract: The invention disclosed herein is a novel media milling process performed in an atmosphere of propellants(s) utilizing a resonant acoustic mixing (RAM) device. The process is utilized to reduce the particle size of API (optionally including excipients) to a respirable size range while ensuring the retention of the crystallinity of the milled API.
    Type: Application
    Filed: December 12, 2014
    Publication date: November 3, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: BALAJI BHARATWAJ, SAI PRASANTH CHAMARTHY, CHINEDU G. OREKIE, YOEN-JU SON