Patents Assigned to Merck Sharp
  • Hydroxy-substituted orexin receptor antagonists
    Patent number: 9725434
    Abstract: The present invention is directed to hydroxy 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 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: April 21, 2014
    Date of Patent: August 8, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Nigel L. Liverton, Jason W. Skudlarek
  • C5-spiro iminothiazine dioxides as BACE inhibitors, compositions, and their use
    Patent number: 9725468
    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: Grant
    Filed: September 8, 2014
    Date of Patent: August 8, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Wen-Lian Wu, Jared N. Cumming
  • Methods for treating intrapulmonary infections
    Patent number: 9724353
    Abstract: This disclosure relates to the treatment of intrapulmonary bacterial infections, including treatment of nosocomial pneumonia lung infections with pharmaceutical compositions containing the cephalosporin ceftolozane.
    Type: Grant
    Filed: October 13, 2014
    Date of Patent: August 8, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Gurudatt A. Chandorkar, Jennifer A. Huntington, Tara Parsons, Obiamiwe C. Umeh
  • Cycloalkyl nitrile pyrazolo pyridones as Janus kinase inhibitors
    Patent number: 9725445
    Abstract: Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: August 8, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Lloyd Childers, Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Qinglin Pu, Mark E. Scott, Christopher F. Thompson, Hongjun Zhang, Danielle Falcone, Luis Torres, Jason Brubaker, Hongbo Zeng, Jiaqiang Cai, Xiaoxing Du, Chonggang Wang, Yunfeng Bai, Norman Kong, Yumei Liu, Zhixiang Zheng
  • CCR9 ANTAGONIST COMPOUNDS
    Publication number: 20170216295
    Abstract: Provided herein are compounds that inhibit CCR9 receptor function. Also provided herein are methods of treating inflammatory disease in a subject, comprising administering to the subject a compound of the invention. Accordingly, in one aspect, provided herein is a compound of Formula (1) or a pharmaceutically acceptable salt thereof. In another aspect, provided herein is a pharmaceutical composition, comprising a compound of Formula (1), and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: July 27, 2015
    Publication date: August 3, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Bhuamik Pandya, Blaise Lippa, Xin Zhang, Jon Christian Baber, Jan Antionette C. Romero, Jing Zhang
  • INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20170217981
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibutors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: September 25, 2015
    Publication date: August 3, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: MICHAEL D. ALTMAN, JASON D. BRUBAKER, MATTHEW L. CHILDERS, ANTHONY DONOFRIO, THIERRY FISCHMANN, CRAIG R. GIBEAU, SOLOMON D. KATTAR, CHARLES A. LESBURG, JONGWON LIM, JOHN K.F. MACLEAN, UMAR F. MANSOOR, ALAN B. NORTHRUP, JOHN M. SANDERS, GRAHAM F. SMITH
  • FUSED TETRACYCLIC HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20170217940
    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: Application
    Filed: December 15, 2014
    Publication date: August 3, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph Kozlowski, Craig Coburn, Wensheng Yu, Ling Tong, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang, Tao Ji
  • [7,6]-FUSED BICYCLIC ANTIDIABETIC COMPOUNDS
    Publication number: 20170217942
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, 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: Application
    Filed: August 5, 2015
    Publication date: August 3, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Duane DeMong, Christopher W. Plummer, Minghai Fang, Bin Hu
  • HIV PROTEASE INHIBITORS
    Publication number: 20170217986
    Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV 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: Application
    Filed: March 2, 2015
    Publication date: August 3, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Thomas J. Greshock, M. Katharine Holloway, Peter D. Williams, Christian Beaulieu, Sheldon Crane, Stephanie Lessard, Daniel Mckay, Carmela Molinaro, Oscar Miguel Moradei, Vijayasaradhi Sivalenka, Vouy Linh Truong, Satyanarayana Tummanapalli
  • BTK Inhibitors
    Patent number: 9718828
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: August 1, 2017
    Assignees: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Hans C. A. Raaijmakers, Allard Kaptein, Arthur A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C. H. M. Wijkmans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 9718819
    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: Grant
    Filed: February 1, 2016
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yunfu Luo, Zhiyu Lei
  • Spirocyclic CETP inhibitors
    Patent number: 9717714
    Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. The chemical compounds that are disclosed cholesterol ester transfer protein (CETP) and are expected to have utility in raising HDL-C, lowering LDL-C, and in the treatment and prevention of atherosclerosis.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Debra Ondeyka, Xiaoxia Qian, Petr Vachal, Sriram Tyagarajan, Cameron J. Smith, Hong Li, Jianming Bao
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9718808
    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: Grant
    Filed: January 5, 2015
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dipshikha Biswas, Fa-Xiang Ding, Shuzhi Dong, Xin Gu, Jinlong Jiang, Alexander Pasternak, Takao Suzuki, Joseph Vacca, Shouning Xu
  • Compounds inhibiting leucine-rich repeat kinase enzyme activity
    Patent number: 9718818
    Abstract: The present invention is directed to azaindazole 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: August 18, 2014
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duane DeMong, Thomas J. Greshock, Ronald K. Chang, Xing Dai, Hong Liu, John A. McCauley, Wei Li, Kallol Basu, Jack D. Scott, Michael Miller
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9718782
    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: Grant
    Filed: September 17, 2014
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9718854
    Abstract: The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: August 1, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Kun Liu, Harold G. Selnick, Zhongyong Wei, Changwei Mu, Yaode Wang, Xiaona Wang
  • MONOCYCLIC ISOXAZOLINES AS INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN
    Publication number: 20170210715
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein D1, D2 and D3 are each N, CH, or substituted CH, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: July 24, 2015
    Publication date: July 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Feng Ye, Petr Vachal, Jayanth Thiruveliore Thatal
  • INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20170209446
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: September 25, 2015
    Publication date: July 27, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: MICHAEL D. ALTMAN, BRIAN M. ANDRESEN, JASON D. BRUBAKER, ANTHONY DONOFRIO, THIERRY FISCHMANN, CRAIG R. GIBEAU, CHARLES A. LESBURG, JONGWON LIM, JOHN K.F. MACLEAN, UMAR F. MANSOOR, ALAN B. NORTHRUP, JOHN M. SANDERS, GRAHAM F. SMITH, LUIS TORRES
  • [5,6]-FUSED BICYCLIC ANTIDIABETIC COMPOUNDS
    Publication number: 20170210727
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, 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: Application
    Filed: August 3, 2015
    Publication date: July 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Chen, Duane DeMong, Paul E. Finke, Christopher W. Plummer
  • Autoinjector pen
    Patent number: D793547
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Greg Burkett, Shu Kuen Chang, Angie Kim, Jin Ko, Scott Mackie, Philip G. Green, Sharad Gupta, Angela M. Amend Kwasnik, Christin L. O'Neill, Robert Stianchi, Witold Swiatek