Patents Assigned to Merck Sharp & Dohme
  • Publication number: 20160243128
    Abstract: The present invention relates to Polycyclic Heterocycle Derivatives, such as compound 1: (1) compositions comprising the Polycyclic Heterocycle Derivatives, and methods of using the Polycyclic Heterocycle Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: May 9, 2016
    Publication date: August 25, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joseph P. Vacca, Craig A. Coburn, David B. Olsen, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Patent number: 9422255
    Abstract: In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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: March 11, 2014
    Date of Patent: August 23, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tanweer A. Khan, Jack D. Scott, Jared N. Cumming
  • Patent number: 9422277
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 5-membered ring, and each of the remaining variables shown in the formula 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 Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: August 23, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh
  • Patent number: 9422266
    Abstract: Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula 1a.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: August 23, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael W. Miller, Andrew W. Stamford, Kallol Basu, Scott Edmondson, Zhiqiang Guo, William B. Geiss
  • Patent number: 9422355
    Abstract: Purified genes encoding cytokines from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: August 23, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: J. Fernando Bazan, Rene de Waal Malefyt, Yong-Jun Liu, Vassili Soumelis
  • Publication number: 20160235727
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of us ing the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: September 29, 2014
    Publication date: August 18, 2016
    Applicant: 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
  • Patent number: 9416111
    Abstract: The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t 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) kinase.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew M. Haidle, Michael D. Altman, Solomon D. Kattar, Matthew Christopher, John Michael Ellis, Christian Fischer, Alan B. Northrup, Kaleen Konrad Childers
  • Patent number: 9416154
    Abstract: The present invention relates to 5?-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2 and R3 are as defined herein and B is a 7-deaza-9-purinyl moiety. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Derivative, and methods of using the 5?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Vinay Girijavallabhan, Stephane L. Bogen, Qun Dang, David B. Olsen
  • Patent number: 9416389
    Abstract: Disclosed are methods for reducing detectable mannosylation of N-linked and O-linked oligosaccharides in lower eukaryote host cells. In particular, recombinant lower eukaryote host cells are provided in which expression of the GDP-mannose transporter encoded by the Vanadate Resistant Glycosylation 4 (VRG4) gene has been disrupted. In general, the VRG4 gene is essential for cell viability; however, the present invention provides host cells that are viable when expression of the VRG4 gene therein has been disrupted. The host cells are capable of producing proteins or glycoproteins that have reduced or no detectable ?-linked mannose, ?-linked mannose or phosphomannose containing N- and/or O-glycans.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Stephen R. Hamilton
  • Patent number: 9416108
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, Andrew W. Stamford
  • Patent number: 9416126
    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: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Wei Li, Joel Harris, Andrew Stamford, Marc Poirier, Paul Tempest
  • Patent number: 9416129
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula 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 Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh, Lingyan Wang, John P. Caldwell
  • Publication number: 20160228532
    Abstract: This present invention relates to compositions and methods for stabilizing a dried vaccine formulations. In particular, the invention provides a method for producing a vaccine composition comprising the steps of providing an aqueous composition comprising a buffer, the vaccine components and between 17.5% w/w and 60% w/w of a non-polymeric sugar, freezing the composition, and applying microwave radiation under a pressure lower than atmospheric pressure in order to sublimate the composition and obtain a dried vaccine formulation. The invention also provides a product obtainable by this method.
    Type: Application
    Filed: October 13, 2014
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Jessica Sinacola, Morrisa Jones
  • 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
  • Publication number: 20160229804
    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
  • Publication number: 20160229813
    Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: August 17, 2015
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
  • Publication number: 20160229839
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: September 23, 2014
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Scott D. Edmondson, Ning Shao, Santhosh Neelamkavil, Corey Poker, Zahid Hussain, Zhuyan Guo, Nancy Jo Kevin, Yi Zang, Jiafang He
  • 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
  • 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
  • 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