Patents Assigned to Merck Sharp
  • 2-PYRIDYLOXY-4-ETHER OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20160016935
    Abstract: The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether 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: March 3, 2014
    Publication date: January 21, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: SCOTT D. KUDUK, JASON W. SKUDLAREK
  • P2X3 receptor antagonists for treatment of pain
    Patent number: 9238647
    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: January 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
  • Pegylated interleukin-10
    Patent number: 9238079
    Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Seoju Lee, David C. Wylie, Susan Cannon-Carlson
  • Process and intermediates for preparing macrolactams
    Patent number: 9238604
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Feng Xu, Guy Humphrey, Tao Pei, Zhiguo Jake Song, Tao Wang, Laura Artino
  • Formulations for c-Met kinase inhibitors
    Patent number: 9238571
    Abstract: The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Robert Ward
  • COMPOSITIONS AND METHODS FOR TREATING CANCER
    Publication number: 20160008361
    Abstract: The instant invention relates to methods for the treatment of WEE1 kinase associated cancer by administering a WEE1 inhibitor, wherein the WEE1 inhibitor is WEE1-1 or a pharmaceutically acceptable salt thereof, or WEE1-2 or a pharmaceutically acceptable salt thereof. In another embodiment, the invention relates to a method for treating a WEE1 kinase associated cancer patient, comprising administering a WEE1 inhibitor, wherein the cancer cells of said patient to be treated are characterized by low expression levels of PKMYT1.
    Type: Application
    Filed: November 22, 2013
    Publication date: January 14, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Stuart Denham Shumway
  • COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
    Publication number: 20160009689
    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: Application
    Filed: February 27, 2014
    Publication date: January 14, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Wei Li, Andrew Stamford, Marc Poirer, Paul Tempest
  • Compounds that are ERK inhibitors
    Patent number: 9233979
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: January 12, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin J. Wilson, David J. Witter, Phieng Siliphaivanh, Kathryn Lipford, David Sloman, Danielle Falcone, Brendan O'Boyle, Umar Faruk Mansoor, Jongwon Lim, Joey L. Methot, Christopher Boyce, Lei Chen, Matthew H. Daniels, Salem Fevrier, Xianhai Huang, Ravi Kurukulasuriya, Ling Tong, Wei Zhou, Joseph Kozlowski, Milana M. Maletic, Bidhan A. Shinkre, Jayanth Thiruvellore Thatai, Raman Kumar Bakshi, Ganesh Babu Karunakaran
  • Leucine-rich repeat kinase enzyme activity
    Patent number: 9233977
    Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: January 12, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John A. McCauley, Hemaka A. Rajapakse, Thomas J. Greshock, John Sanders, Boyoung Kim, Vanessa L. Rada, Jonathan T. Kern, Heather H. Stevenson, Mark T. Bilodeau
  • INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
    Publication number: 20160002259
    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, kidney disease, edema, and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: February 12, 2014
    Publication date: January 7, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda Keh DeJesus, Fa-Xiang Ding, Shuzhi Dong, Jessica L. Frie, Xin Gu, Jinlong Jiang, Aurash Shahripour, Barbara Pio, Haifeng Tang, Shawn Walsh
  • GASTRO-RETENTIVE FORMULATIONS
    Publication number: 20160000721
    Abstract: The present invention relates to pharmaceutical compositions of the poorly soluble drugs, and pharmaceutically acceptable salts thereof, in a controlled-release gastric retained oral dosage form. Such compositions are formulated so as to deliver the majority of the incorporated drug into the stomach and upper gastrointestinal tract, with restricted drug delivery in the lower gastrointestinal tract. The dosage forms have multiple layers including an active layer with a first swellable polymer with raltegravir incorporated therein and a non-active layer with a second swellable polymer having a similar molecular weight or a higher molecular weight as the swellable polymer in the active layer.
    Type: Application
    Filed: December 18, 2013
    Publication date: January 7, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, Ashlesh Sheth, Ronald L. Smith
  • Gamma secretase inhibitors
    Patent number: 9226927
    Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: January 5, 2016
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Wen-Lian Wu, Duane A. Burnett
  • Pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors
    Patent number: 9227971
    Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: January 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Arshad Siddiqui, Yang Nan, Mehul F. Patel, Panduranga Adulla P. Reddy, Umar Faruk Mansoor, Zhaoyang Meng, Lalanthi Dilrukshi Vitharana, Lianyun Zhao, Amit K. Mandal, Duan Liu, Shuyi Tang, Andrew McRiner, David B. Belanger, Patrick J. Curran, Chaoyang Dai, Angie R. Angeles, Liping Yang, Matthew Hersh Daniels
  • Pyridine CGRP receptor antagonists
    Patent number: 9227973
    Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which 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: May 3, 2013
    Date of Patent: January 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • Aliphatic spirolactam CGRP receptor antagonists
    Patent number: 9227972
    Abstract: The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which 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: May 3, 2013
    Date of Patent: January 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair, Helen Mitchell
  • IL-8 level as a determinant of responsivity of a cancer to treatment
    Patent number: 9229008
    Abstract: The present application includes methods for using IL-8 as a biomarker for, e.g., tumor size, for example, during course of treatment with an anti-cancer agent such as an ERK inhibitor.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: January 5, 2016
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Ahmed A. Samatar, Brian Long, Priya Dayananth, Diane Levitan, Marsha Smith
  • Compounds that are ERK inhibitors
    Patent number: 9226922
    Abstract: Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: January 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin J. Wilson, David J. Witter, Matthew H. Daniels, Angie R. Angeles, Phieng Siliphaivanh, David Sloman, Brendan O'Boyle, Danielle Falcone, Catherine White, Ron Ferguson, Wei Zhou, Kathryn Lipford, Umar Faruk Mansoor, Salem Fevrier, Xianhai Huang, Ravi Kurukulasuriya, Judson E. Richard, Shuyi Tang, Christopher Boyce, Joseph Kozlowski, Raman Kumar Bakshi, Ganesh Babu Karunakaran
  • O-GLYCOSYLATED CARBOXY TERMINAL PORTION (CTP) PEPTIDE-BASED INSULIN AND INSULIN ANALOGUES
    Publication number: 20150374795
    Abstract: Compositions and formulations comprising insulin or insulin analogues comprising a carboxy terminal portion (CTP) peptide comprising amino acids 112-188 to 142 of the beta subunit of human chorionic gonadotropin (hCG?) or a partial variant thereof that includes at least one O-glycosylation site of the CTP peptide, wherein the CTP peptide of the CTP peptide-based insulin or insulin analogue is O-glycosylated are described. In particular embodiments, the O-glycosylated insulin analogues are produced in vivo and in further embodiments, the O-glycosylated CTP-based insulin analogues comprise predominantly mannotriose and mannotetrose O-glycans or predominantly mannose O-glycans.
    Type: Application
    Filed: November 22, 2013
    Publication date: December 31, 2015
    Applicants: MERCK SHARP & DOHME CORP., INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Richard D. DiMarchi, Pengyun Li, Michael Meehl
  • Cyclic amine substituted oxazolidinone CETP inhibitor
    Patent number: 9221834
    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. In the compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: December 29, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhijian Lu, Yi-Heng Chen, Cameron Smith, Hong Li, Christopher F. Thompson, Julianne Hunt, Florida Kallashi, Ramzi Sweis, Peter Sinclair, Samantha E. Adamson, Guizhen Dong, Debra L. Ondeyka, Xiaoxia Qian, Wanying Sun, Petr Vachal, Kake Zhao
  • C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
    Patent number: 9221839
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of ring A, ring B, ring C, R2, R3, R4, m, n, p, and -L1- is as defined herein. The novel compounds of the invention may be 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 Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: December 29, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Eric J. Gilbert, Andrew W. Stamford