Patents Assigned to Merck Sharp
  • Biocatalytic transamination process
    Patent number: 9738915
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: employing dynamic kinetic resolution (DKR). The DKR process involves an enzymatic enantioselective amination reaction catalyzed by transaminases. The process can be used to manufacture key intermediates in the preparation of poly (ADP-ribose) polymerase (PARP) inhibitors which may be useful for the treatment of cancer.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: August 22, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Gerard Bulger, Birgit Kosjek, Nelo Rivera
  • HCV NS3 protease inhibitors
    Patent number: 9738661
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: August 22, 2017
    Assignees: MERCK SHARP & DOHME CORP., MSD ITALIA S.R.L.
    Inventors: Nigel J. Liverton, Vincenzo Summa, Steven Harper, John A. McCauley, Joseph J. Romano, Michael T. Rudd
  • INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170233412
    Abstract: The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: September 23, 2015
    Publication date: August 17, 2017
    Applicants: MERCK SHARP & DOHME CORP., MSD R&D (CHINA) CO., LTD.
    Inventors: JIAQIANG CAI, ALEJANDRO CRESPO, XIAOXING DU, BYRON GABRIEL DUBOIS, DEODIALSINGH GUIADEEN, SHANKARAN KOTHANDARAMAN, PING LIU, RONGQIANG LIU, WEIGUO QUAN, CHRISTOPHER SINZ, LIPING WANG
  • PROCESSES FOR THE PREPARATION OF A BACE INHIBITOR
    Publication number: 20170233382
    Abstract: This invention provides processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2. In addition, the invention provides certain synthetic intermediates which are useful, among other things, for the preparation of the Compound of Formula (I).
    Type: Application
    Filed: August 10, 2015
    Publication date: August 17, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Steven P. Miller, Carmela Molinaro, David Thaisrivongs, Feng Xu, Richard Desmond, Hongming Li, Qinghao Chen, Andrew W. Stamford, Zhiguo Jake Song, Lushi Tan
  • Solid Pharmaceutical Compositions Containing An Integrase Inhibitor
    Publication number: 20170231993
    Abstract: Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.
    Type: Application
    Filed: April 10, 2017
    Publication date: August 17, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Majid Mahjour, Feng Li, Decheng Ma, Sutthilug Sotthivirat
  • CELL LINE 3M
    Publication number: 20170233477
    Abstract: The present invention provides, inter alia, an isolated cell line, 3M as well as methods for making such a cell line and methods of using such a cell line, e.g., to produce a protein such as an immunoglobulin.
    Type: Application
    Filed: April 12, 2017
    Publication date: August 17, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ankit A. Merchant, Yung-Shyeng Tsao
  • SALT FORMS OF CEFTOLOZANE
    Publication number: 20170233408
    Abstract: This disclosure relates to salt forms of ceftolozane, processes for making these salt forms, and compositions comprising the same. Also disclosed are stabilized compositions of ceftolozane. Provided herein are salt forms of ceftolozane, processes for making these salt forms and compositions comprising the same. The salt forms provided herein include ceftolozane bromide, ceftolozane edisylate, ceftolozane mesylate, ceftolozane chloride, ceftolozane sulfate, ceftolozane maleate, ceftolozane phosphate, and ceftolozane ketoglutarate.
    Type: Application
    Filed: August 17, 2015
    Publication date: August 17, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jian-Qiao Gu, Valdas Jurkauskas, Carlos Lopez, Kristos Adrian Moshos, Pradip M. Pathare, Sudhakar Garad, You Seok Hwang
  • NOVEL CRYSTALLINE FORMS OF A BACE INHIBITOR, COMPOSITIONS, AND THEIR USE
    Publication number: 20170233383
    Abstract: The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A? pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A? pathologies, including Alzheimer's disease, are disclosed herein.
    Type: Application
    Filed: September 25, 2015
    Publication date: August 17, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott Trzaska, Zachary E. Dance, Yong Liu, Richard John Varsolona, Gregory York
  • Biomarkers for TSLP treatment
    Patent number: 9732151
    Abstract: The present invention relates to biomarker responsive to treatment with an anti-Thymic Stromal Lymphopoietin (TSLP) antibody.
    Type: Grant
    Filed: October 31, 2012
    Date of Patent: August 15, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Maribel Beaumont, Jeanine D. Mattson, Jennifer R. Louten, Terrill K. McClanahan, Rene de Waal Malefyt
  • Purine inhibitors of human phosphatidylinositol 3-kinase delta
    Patent number: 9730940
    Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: August 15, 2017
    Assignee: Merck Sharp & Dohme
    Inventors: Abdelghani Abe Achab, Michael D. Altman, Yongqi Deng, Timothy Guzi, Solomon Kattar, Jason D. Katz, Joey L. Methot, Hua Zhou, Meredeth McGowan, Matthew P. Christopher, Yudith Garcia, Neville John Anthony, Francesc Xavier Fradera Llinas, Kin Chiu Fong, Xiansheng Leng, Changwei Mu, Sixing Zhang, Rong Zhang
  • 2?-alkynyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
    Patent number: 9732111
    Abstract: The present invention relates to 2?-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2?-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: August 15, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Yuhua Huang, Lingyan Wang, Stephane L. Bogen, Angela D. Kerekes, Vinay M. Girijavallabhan, Gabor Butora, Quang Truong, Ian Davies, Ann E. Weber
  • Diazepane orexin receptor antagonists
    Patent number: 9732077
    Abstract: The present invention is directed to diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the diazepane 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: December 16, 2014
    Date of Patent: August 15, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Thomas S. Reger, Anthony J. Roecker
  • C2-carbocyclic iminothiazine dioxides as BACE inhibitors, compositions, and their use
    Patent number: 9732088
    Abstract: In its many embodiments, the present invention provides certain C2-carbocyclic iminothiazine dioxide compounds, including compounds Formula (I); or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, n, ring C, RC and p 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: May 28, 2015
    Date of Patent: August 15, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Jared N. Cumming, Shuwen He, Brandon M. Taoka, Quang T. Truong, Wen-Lian Wu
  • Tricyclic gyrase inhibitors
    Patent number: 9732083
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: August 15, 2017
    Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: Daniel Bensen, Zhiyong Chen, John Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Douglas W. Phillipson, Leslie William Tari, Michael Trzoss, Junhu Zhang, Felice C. Lightstone, Toan B. Nguyen, Sergio E. Wong, Paul Aristoff, Michael Jung
  • INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170226120
    Abstract: The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: September 23, 2015
    Publication date: August 10, 2017
    Applicants: MERCK SHARP & DOHME CORP., MSD R&D (CHINA) CO., LTD.
    Inventors: JIAQIANG CAI, ALEJANDRO CRESPO, XIAOXING DU, BYRON GABRIEL DUBOIS, PING LIU, RONGQIANG LIU, WEIGUO QUAN, CHRISTOPHER SINZ, LIPING WANG
  • NOVEL CRYSTALLINE FORMS OF A BACE INHIBITOR, COMPOSITIONS, AND THEIR USE
    Publication number: 20170226098
    Abstract: The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A? pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A? pathologies, including Alzheimer's disease, are disclosed herein.
    Type: Application
    Filed: August 10, 2015
    Publication date: August 10, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Irina Kazakevich, Scott Trzaska, Tao Feng
  • INTERMEDIATES IN THE SYNTHESIS OF CEPHALOSPORIN COMPOUNDS
    Publication number: 20170226126
    Abstract: Described herein are crystalline forms of a compound of formula (III?), including toluene solvates off A TD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane. Provided herein is a crystalline form of a compound of formula (III?): wherein X is CI, Br, or I; and R1 and R2 are each independently an oxygen protecting group; processes for making the crystalline form, and use of said form in the synthesis of antibacterial cephalosporins such as ceftolozane.
    Type: Application
    Filed: August 14, 2015
    Publication date: August 10, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
  • INHIBITORY RNA FOR ENHANCED PROTEIN PRODUCTION IN RECOMBINANT MAMMALIAN CELLS
    Publication number: 20170226550
    Abstract: The invention provides methods and compositions for improving production of exogenous polypeptides in large scale culture of mammalian host cells. The methods and compositions utilize RNA interference to inhibit expression of one or more specific host cell proteins. The present invention is based on the identification of specific mammalian genes and sequences therein that are useful as RNAi targets to enhance the production of exogenous proteins in mammalian cell culture.
    Type: Application
    Filed: August 4, 2015
    Publication date: August 10, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jianxin Ye, Krista Alvin, Siyan Zhang
  • ANTI-COAGULATION FACTOR XI ANTIBODIES
    Publication number: 20170226225
    Abstract: Antibodies that bind the apple 2 domain of human coagulation Factor XI and inhibit activation of FXI by coagulation factor XIIa are described.
    Type: Application
    Filed: January 19, 2017
    Publication date: August 10, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zhu Chen, Kenneth P. Ellsworth, James A. Milligan, Elizabeth Oldham, Dietmar Seiffert, Vaishnavi Ganti, Mohammad Tabrizifard
  • Process for preparing tetracyclic heterocycle compounds
    Patent number: 9725464
    Abstract: The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: August 8, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian Mangion, Cheng-yi Chen, Ingyu Jeon, Yonggang Chen, Hongmei Li, Hoa N. Nguyen, Peter E. Maligres, Artis Klapars, Ilia Zavialov, Nobuyoshi Yasuda