Patents Assigned to Merck Sharp
  • Publication number: 20170210732
    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: July 23, 2015
    Publication date: July 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D. Edmondson, Zhuyan Guo, Sung-Sau So, Anthony K. Ogawa, Rongze Kuang, Heping Wu, Amjad Ali, Ying-Duo Gao, Yu Jiang, Chunsing Li, Tingting Yu
  • Publication number: 20170209545
    Abstract: A method for crystallizing insulin or insulin analogs under alkaline conditions in the presence of zinc, purifying the crystals by filtering through a filter, and drying the crystals captured on the filter to produce crystalline insulin or insulin analog compositions is described. Method has been exemplified with insulin lispro.
    Type: Application
    Filed: August 21, 2015
    Publication date: July 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Douglas S. Watson, Allison C. Ortigosa, Mark C. Sleevi, Kathryn M. Story
  • Patent number: 9714243
    Abstract: The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R1, R2, R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: July 25, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark W. Embrey, Thomas H. Graham, Abbas Walji, Sherman T. Waddell, Tao Yu, Yonglian Zhang, Wensheng Liu, Paul J. Coleman, John Wai, Thomas Steele, Christina Di Marco
  • Publication number: 20170202209
    Abstract: A mixing apparatus (1) for mixing slaughter offal with a preservative agent, the apparatus comprising an offal collection tank (3) with a bottom (4) provided with a discharge opening (5) connectable to a closable discharge, an agitator (8) extending into the offal collection tank, and a pump unit (9) operatively connectable to the discharge, wherein the apparatus further comprises a preservative reservoir (7) mounted on top of the collection tank (3). A collection and preservation system is provided, wherein the addition of preservation agent can be strictly controlled, can easily and quickly be installed and connected when it is to be used. After use, the system is easily removed and cleaned.
    Type: Application
    Filed: February 25, 2016
    Publication date: July 20, 2017
    Applicant: Merck Sharp & Dohme B.V.
    Inventors: Adolph Bartholomeus Gijtenbeek, Harry van Tuijn, Marinus Johannes Gerardus Maria Ploegmakers
  • Patent number: 9707234
    Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R11 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Wensheng Liu, Tao Yu, Yonglian Zhang, Sherman T. Waddell, John S. Wai, Paul J. Coleman, John M. Sanders, Mark W. Embrey, Abbas M. Walji, Ronald Dale Ferguson, II, Christine Ng Di Marco, Thomas G. Steele, Lihong Hu, Xuanjia Peng
  • Patent number: 9708270
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mariappan Chelliah, Hong Dong Chu, Jason M. Cox, John S. Debenham, Keith Eagen, Ping Lan, Clare London, Michael A. Plotkin, Unmesh Shah, Christopher Joseph Sinz, Zhongxiang Sun, Henry M. Vaccaro, Srikanth Venkatraman
  • Patent number: 9709568
    Abstract: The present disclosure provides isolated antibodies that specifically bind to human PD-L1, as well as antigen binding fragments of such antibodies, and kits comprising the anti-PD-L1 antibodies or binding fragments and a set of reagents for detecting a complex of the antibody, or antigen binding fragment thereof, bound to human PD-L1. The antibodies and antigen binding fragments of this disclosure are useful for immunohistochemical detection of human PD-L1 expression in tissue samples. Nucleic acid molecules encoding the antibodies and antigen binding fragments of this disclosure, as well as expression vectors and host cells for expression thereof, are also provided.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert H. Pierce, Patricia Bourne, Linda Liang, Michael Bigler
  • Patent number: 9708273
    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: Grant
    Filed: August 17, 2015
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng DiMarco, Thomas J. Greshock
  • Patent number: 9708308
    Abstract: The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substitut
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: July 18, 2017
    Assignees: Merck Sharp Dohme Corp., Mochida Pharmacuetical Co., Ltd.
    Inventors: Cameron James Smith, John Qiang Tan, Ting Zhang, James Balkovec, William John Greenlee, Liangqin Guo, Yi-Heng Chen, Yili Chen, Jiayi Xu, Samuel Chackalamannil, Tomokazu Hirabayashi, Hiroshi Nagasue, Kouki Ogawa
  • Patent number: 9708336
    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: Grant
    Filed: January 16, 2015
    Date of Patent: July 18, 2017
    Assignee: 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
  • Patent number: 9708347
    Abstract: Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim
  • Patent number: 9707276
    Abstract: Compositions and formulations comprising insulin or insulin analogs comprising a carboxy terminal portion (CTP) peptide comprising amino acids 112-118 to 145 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 analog is O-glycosylated are described. In particular embodiments, the O-glycosylated insulin analogs are produced in vivo and in further embodiments, the O-glycosylated CTP-based insulin analogs comprise predominantly mannotriose and mannotetrose O-glycans or predominantly mannose O-glycans.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Meehl, Richard D. DiMarchi, Pengyun Li
  • Publication number: 20170197991
    Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Application
    Filed: February 2, 2017
    Publication date: July 13, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Xianhai Huang, Timothy J. Henderson, Jae-Hun Kim, Christopher Boyce, Pauline Ting, Junying Zheng, Edward Metzger, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Qiaolin Deng
  • Publication number: 20170197953
    Abstract: The present invention provides a compound of Formula I (The chemical formula should be inserted here.) 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: May 22, 2015
    Publication date: July 13, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D. Edmondson, Zhuyan Guo, Eric Mertz, Anthony K. Ogawa, Sung-Sau So, Wanying Sun, Linda L. Brockunier, Amjad Ali, Rongze Kuang, Heping Wu
  • Publication number: 20170198042
    Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
    Type: Application
    Filed: March 22, 2017
    Publication date: July 13, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi
  • Patent number: 9701693
    Abstract: The invention provides compounds 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: July 11, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
  • Patent number: 9701751
    Abstract: Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: July 11, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiao Min Schebye, Grigori P. Ermakov, Douglas J. Hodges, Leonard G. Presta
  • Patent number: 9701669
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is —[C(Ra)(Rb)]x—[C(Rb)(Rb)]y—C(O)NH2, or —N(H)—[(CH2)]z—C(O)—NH2, W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Grant
    Filed: August 18, 2014
    Date of Patent: July 11, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhiqiang Yang, Fengqi Zhang, Guizhen Dong, Sandra Lee Knowles, Milana Maletic
  • Publication number: 20170189441
    Abstract: Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)a-(G)b; wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P)c-(L)d-(G)e; wherein P is a peptide and each occurrence of P is independently selected from Table 2; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.
    Type: Application
    Filed: November 3, 2014
    Publication date: July 6, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Thomas J. Tucker, David M. Tellers, Boyoung Kim, Rob Burke, Kathleen B. Calati, Matthew G. Stanton, Rubina G. Parmar, Jeffery G. Aaronson, Weimin Wang
  • Patent number: 9695163
    Abstract: The present invention is directed to thiazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thiazole 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: July 4, 2017
    Assignee: MERCK SHARP & DOHME CORP
    Inventors: Nigel Liverton, Douglas C. Beshore, Scott D. Kuduk, Yunfu Luo, Na Meng, Tingting Yu