Patents Assigned to Merck Sharp
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9839629
    Abstract: Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as 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. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuzhi Dong, Alexander Pasternak, Xin Gu, Qinghong Fu, Jinlong Jiang, Fa-Xiang Ding, Haifeng Tang, Reynalda K. DeJesus, Takao Suzuki
  • Allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 9840481
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Thomas J. Greshock, Deodial G. Guiadeen, Andrew John Harvey, Belinda C. Huff, Kenneth J. Leavitt, Vanessa L. Rada, John M. Sanders, William D. Shipe, Linda M. Suen, Ian M. Bell
  • NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20170349585
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: June 7, 2017
    Publication date: December 7, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
  • BTK INHIBITORS
    Publication number: 20170349593
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts 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 of Formula (I) in the treatment of Btk mediated disorders.
    Type: Application
    Filed: December 17, 2015
    Publication date: December 7, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JIAN LIU, JOSEPH A. KOZLOWSKI, SOBHANA BABU BOGA, DEODIAL GUY GUIADEEN, WENSHENG YU, JIAQIANG CAI, SHILAN LIU
  • HIV protease inhibitors
    Patent number: 9834526
    Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: December 5, 2017
    Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
  • Use of pegylated IL-10 to treat cancer
    Patent number: 9833514
    Abstract: Provided are methods of treatment for tumors. In particular, methods are provided for use of a chemically modified IL-10 to treat tumors.
    Type: Grant
    Filed: May 16, 2016
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Martin Oft, Catherine Sheppard, John Brian Mumm, Lingling Wu
  • Piperidinone carboxamide azaindane CGRP receptor antagonists
    Patent number: 9833448
    Abstract: The present invention is directed to piperidinone carboxamide azaindane 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: October 14, 2016
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • BTK inhibitors
    Patent number: 9834554
    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: Grant
    Filed: December 16, 2014
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jian Liu, Ronald M. Kim, Joseph Kozlowski, Deodialsingh Guiadeen, Arto D. Krikorian, Younong Yu
  • Antidiabetic substituted heteroaryl compounds
    Patent number: 9834563
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William K. Hagmann, Bing Li, Jason W. Szewczyk, Bowei Wang, Dann Parker, Timothy Blizzard, Hubert Josien, Purakkattle Biju, Harry Chobanian, Candido Gude, Ravi P. Nargund, Barbara Pio, Qun Dang, Linus S. Lin, Bin Hu, Mingxiang Cui, Zhengxia Chen, Meibi Dai, Zaihong Zhang, Ying Lv, Lili Tian
  • Sitagliptin tannate complex
    Patent number: 9833463
    Abstract: The present invention provides for a sitagliptin tannate complex or a pharmaceutical compositions or a pharmaceutically acceptable intermediates comprising said complex. This invention also relates to a processes to prepare the sitagliptin tannate complex as well as to methods of using the sitagliptin tannate complex to treat diabetes, obesity and high blood pressure.
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wycliffe Omwancha, Rubi Burlage
  • PROCESS FOR REFOLDING RECOMBINANT CHYMOTRYPSIN
    Publication number: 20170342397
    Abstract: A process for refolding recombinant chymotrypsin produced from prokaryote host cells is described. In particular, the present invention provides a process for refolding recombinant chymotrypsin produced from E. coli is described.
    Type: Application
    Filed: November 13, 2015
    Publication date: November 30, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mark C. Sleevi, Jack Lile, Bryn Grimison
  • PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170342052
    Abstract: The present invention is directed to pyrrolidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 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 compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: December 14, 2015
    Publication date: November 30, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Yunfu Luo, Jason W. Skudlarek
  • CRYSTAL FORMS OF A CCR5 ANTAGONIST
    Publication number: 20170342053
    Abstract: The present disclosure relates to forms of a CCR5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3S)-4-((1R)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone.
    Type: Application
    Filed: November 11, 2015
    Publication date: November 30, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.
    Inventors: Alfred Y. LEE, William De WILDT
  • TERTIARY ALCOHOL IMIDAZOPYRAZINE BTK INHIBITORS
    Publication number: 20170342076
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I 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 of Formula I in the treatment of Btk mediated disorders.
    Type: Application
    Filed: December 17, 2015
    Publication date: November 30, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JIAN LIU, JOSEPH A. KOZLOWSKI, BRIAN M. ANDRESEN, SOBHANA BABU BOGA, XIAOLEI GAO, DEODIAL GUY GUIADEEN, JIAQIANG CAI, SHILAN LIU, DAHAI WANG, HAO WU, CHUNDAO YANG
  • BTK INHIBITORS
    Publication number: 20170340631
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers 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 of Formula (I) in the treatment of Btk mediated disorders.
    Type: Application
    Filed: December 17, 2015
    Publication date: November 30, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JIAN LIU, JOSEPH A. KOZLOWSKI, ABDUL-BASIT ALHASSAN, RAJAN ANAND, SOBHANA BABU BOGA, DEODIAL GUY GUIADEEN, WENSHENG YU, YOUNONG YU, SHILAN LIU, HAO WU, CHUNDAO YANG
  • STABLE ACIDIC INSULIN FORMULATIONS
    Publication number: 20170340738
    Abstract: While the present invention is described herein with reference to illustrated embodiments, it should be understood that the invention is not limited hereto. Those having ordinary skill in the art and access to the teachings herein will recognize additional modifications and embodiments within the scope thereof. Therefore, the present invention is limited only by the claims attached herein.
    Type: Application
    Filed: May 15, 2017
    Publication date: November 30, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Maya S. Salnikova, Christina R. Vessely, Jeffrey T. Blue
  • Oxazole orexin receptor antagonists
    Patent number: 9828368
    Abstract: The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole 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: Grant
    Filed: August 4, 2014
    Date of Patent: November 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel Liverton, Douglas C. Beshore, Scott D. Kuduk, Yunfu Luo, Na Meng, Tingting Yu
  • Fused tetracyclic heterocyclic compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 9828365
    Abstract: The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A?, R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: November 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph Kozlowski, Craig Coburn, Wensheng Yu, Ling Tong, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang, Tao Ji
  • Treating cancer with a combination of a PD-1 antagonist and dinaciclib
    Patent number: 9827309
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and the CDK inhibitor dincaciclib, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express PD-L1.
    Type: Grant
    Filed: August 15, 2014
    Date of Patent: November 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter Richard Strack, Robert Booher, Venkataraman Sriram, Joseph H. Phillips
  • Anti-ILT5 antibodies and ILT5-binding antibody fragments
    Patent number: 9828425
    Abstract: Disclosed herein are antibodies and ILT5-binding fragments thereof that specifically bind to ILT5, e.g., human ILT5 (hILT5), and pharmaceutical compositions comprising such ILT5-binding antibodies and ILT5-binding fragments thereof.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: November 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Irina Apostolou, Paul Ponath, Joe Ponte, Michael Rosenzweig