Patents Assigned to Merck Sharp & Dohme
  • Patent number: 9469608
    Abstract: Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8and R9, each time in which they occur, are independently H, C1-6alkyl, —CH2F, —CHF2, CF3or —CH2OH; W is a) —CHR1R2, where R1is —C(CH3)3, and R2is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3and R4, or tri-substituted with R3, R4and R5; R3is —CF3, —COOH, —COOR7, —C(O)R6, —CH(OH)R6,
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: October 18, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Tesfaye Biftu, Barbara Pio, Zhicai Wu
  • Publication number: 20160297862
    Abstract: A method for crystallizing insulin or insulin analogs under alkaline conditions and purifying the insulin or insulin analog crystals by filtering through a filter and drying the insulin or insulin analog crystals captured on the filter to produce crystalline insulin or insulin analog crystal compositions is described. In particular aspects, the method may be used to crystalize insulin glargine.
    Type: Application
    Filed: December 1, 2014
    Publication date: October 13, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, William Perry, Mark C. Sleevi, Luis Sierra
  • Patent number: 9464108
    Abstract: The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: October 11, 2016
    Assignee: Merck Sharp & Dohme B.V.
    Inventor: Martin Ostendorf
  • Publication number: 20160289207
    Abstract: The present invention is directed to substituted 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: November 10, 2014
    Publication date: October 6, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Duane DeMong, Michael Miller, Hong Liu, Xing Dai, Thomas Greshock, Andrew Stamford, Ravi Nargund
  • Patent number: 9457039
    Abstract: 2?-disubstituted substituted nucleoside derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (1), wherein A is N3 or NH2 and X, Y, R1, R2, R3, R4, R5 and R18 are as defined herein. Compositions comprising at least one 2?-disubstituted nucleoside derivative, and methods of using the 2?-disubstituted nucleoside derivatives for treating or preventing HCV infection in a patient are disclosed.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: October 4, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Weidong Pan, Qun Dang, Ian Davies
  • Patent number: 9458181
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: October 4, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Publication number: 20160280704
    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: Application
    Filed: March 19, 2014
    Publication date: September 29, 2016
    Applicant: 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
  • Patent number: 9453038
    Abstract: Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: September 27, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Rui Zhang, Brian Campbell, Sunita V. Dewnani, Jiayi Xu, Libo Xu, Emma R. Parmee, Roman Kats-Kagan
  • Patent number: 9453034
    Abstract: In its many embodiments, the present invention provides certain C2-azaspirosubstituted iminothiazine dioxide compounds. 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: March 11, 2014
    Date of Patent: September 27, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Jared N. Cumming, Jack D. Scott, Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford
  • Publication number: 20160272633
    Abstract: Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 22, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Peter Fuller, David Guerin, Christopher F. Thompson, Qinglin Pu, Mark E. Scott, Jason David Katz, Ravi Kuruklasuriya, Joshua T. Close, Danielle Falcone, Jason Brubaker, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng
  • Publication number: 20160272634
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 22, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Christopher F. Thompson, Danielle Falcone, Wei Deng, Luis Torres, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng, Mark E. Scott
  • Publication number: 20160272632
    Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 22, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Matthew Lloyd Childers, Peter Fuller, David Guerin, Jason David Katz, Qinglin Pu, Mark E. Scott, Christopher F. Thompson, Michelle Martinez, Danielle Falcone, Luis Torres, Yongqi Deng, Ravi Kurukulasuriya, Hongbo Zeng, Yunfeng Bai, Norman Kong, Yumei Liu, Zhixiang Zheng
  • Patent number: 9446130
    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: January 17, 2014
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Jian Liu, Hao Wu, Shilan Liu, Chundao Yang, Shuling Zheng
  • Patent number: 9447085
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiadiazine compounds, or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers. The novel compounds of the invention are 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: December 9, 2013
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Jack D. Scott, Tesfaye Biftu
  • Patent number: 9447403
    Abstract: The present invention relates to peptides of the enolase protein from Staphylococcus aureus as well as nucleic acid and nucleic acid sequence homologs encoding the peptides. The present invention also relates to a composition, particularly a S. aureus vaccine, comprising one or more of the enolase peptides described herein or a fragment, derivative or variant thereof capable of generating an immune response that induces a protective antibody response or opsonophagocytic activity of human neutrophils for S. aureus. The present invention also encompasses methods of treating and/or reducing the likelihood of a Staphylococcus infection by administering a composition of the invention.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tessie B. McNeely, Leslie Cope, Sharon Smith, Amita Joshi, Irene Pak, Arthur Fridman
  • Patent number: 9440952
    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: September 13, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Hong Liu, Xing Dai, Joel M. Harris, Bernard Neustadt, Andrew Stamford, Marc Poirier, John A. McCauley, Thomas Greshock, Heather Stevenson, John Sanders, Jonathan Kern
  • Publication number: 20160257670
    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: Application
    Filed: October 27, 2014
    Publication date: September 8, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Haifeng Tang, Jessica Frie, Ronald Dale Ferguson, Zhiqiang Guo, Zhi-Cai Shi, Brian Cato, Qinghong Fu
  • Publication number: 20160257668
    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: October 6, 2014
    Publication date: September 8, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ning SHAO, Scott D. EDMONDSON, Santhosh NEELAMKAVIL, Zhuyan GUO, Eric MERTZ, Yi ZANG, Jiafang HE
  • Patent number: 9433621
    Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: September 6, 2016
    Assignees: Merck Sharp & Dohme Corp., Southern Research Institute
    Inventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Francisco Velazquez, Vinay M. Girijavallabhan, Yuhua Huang, Hollis S. Kezar, III, Joseph A. Maddry, Robert C. Reynolds, Abhijit Roychowdhury, Anita T. Fowler, John A. Secrist, III, Joseph A. Kozlowski, Bandarpalle B. Shankar, Ling Tong, Seong Heon Kim, Malcolm MacCoss, Srikanth Venkatraman, Vishal Verma
  • Publication number: 20160251375
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. 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: Application
    Filed: October 14, 2014
    Publication date: September 1, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Feng XU, Richard DESMOND, Guy R. HUMPHREY, Hongming LI, Ji QI, Rebecca T. RUCK, Zhiguo Jake SONG, Tao WANG, Yong-Li ZHONG, Jeonghan PARK, Laura Marie ARTINO, Richard John VARSOLONA