Patents Assigned to Merck Sharp
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 9649294
    Abstract: Glucagon receptor antagonist compounds are disclosed which are of long duration of action. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: October 30, 2014
    Date of Patent: May 16, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Libo Xu, Emma R. Parmee, Xibin Liao
  • Solid pharmaceutical compositions containing an integrase inhibitor
    Patent number: 9649311
    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: Grant
    Filed: October 21, 2010
    Date of Patent: May 16, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Majid Mahjour, Feng Li, Decheng Ma, Sutthilug Sotthivirat
  • REACTIONS OF THIADIAZOLYL-OXIMINOACETIC ACID DERIVATIVE COMPOUNDS
    Publication number: 20170129906
    Abstract: This disclosure relates to an improved synthesis of cephalosporin antibiotic compounds such as ceftolozane, and compositions and methods of use thereof. Thiadiazolyl-oximinoacetic acid compounds such as TATD can be reacted to yield the activated thiadiazolyl-oximinoacetic acid methanesulfonate ester compounds useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Application
    Filed: June 19, 2015
    Publication date: May 11, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jukauskas, Manuel Scanu, Michele Benotti
  • 2-pyridyloxy-3-nitrile-4-substituted orexin receptor antagonists
    Patent number: 9643955
    Abstract: The present invention is directed to 2-pyridyloxy-3-nitrile-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-nitrile-4-substituted 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, 2013
    Date of Patent: May 9, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
    Patent number: 9643982
    Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8, A, X and n are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: April 18, 2014
    Date of Patent: May 9, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Paul J. Coleman, Timothy J. Hartingh, Izzat T. Raheem, John Schreier, John Sisko, John Wai, Thomas H. Graham, Lihong Hu, Xuanjia Peng
  • PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILLARY
    Publication number: 20170119912
    Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
    Type: Application
    Filed: June 9, 2015
    Publication date: May 4, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abbas W. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
  • ANTIBODY NEUTRALIZING HUMAN RESPIRATORY SYNCYTIAL VIRUS
    Publication number: 20170121394
    Abstract: The present invention relates to monoclonal antibodies which have high anti-RSV neutralizing titers. The invention further provides for isolated nucleic acids encoding the antibodies of the invention and host cells transformed therewith. The invention yet further provides for diagnostic, prophylactic and therapeutic methods employing the antibodies and nucleic acids of the invention, particularly as a passive immunotherapy agent in infants and the elderly.
    Type: Application
    Filed: October 27, 2016
    Publication date: May 4, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use
    Patent number: 9636337
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: May 2, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Substituted pyrrolopyrimidines as HDM2 inhibitors
    Patent number: 9637493
    Abstract: The present invention provides substituted pyrrolopyrimidines of Formula I as described herein or a pharmaceutically acceptable salt or solvate thereof: The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: May 2, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Francesc Xavier Fradera Llinas, Amit Ashokro Kudale, Michelle Machacek, Michael Hale Reutershan, Christopher Francis Thompson, B. Wesley Trotter, Liping Yang, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll, Matthew E. Voss
  • Btk inhibitors
    Patent number: 9637486
    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: December 16, 2014
    Date of Patent: May 2, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Jian Liu, Ronald M. Kim, Joseph Kozlowski, Arto D. Krikorian, Rajan Anand
  • C2-CARBOCYCLIC IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170114065
    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: Application
    Filed: May 28, 2015
    Publication date: April 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Jared N. Cumming, Shuwen He, Brandon M. Taoka, Quang T. Truong, Wen-Lian Wu
  • PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
    Publication number: 20170114078
    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: Application
    Filed: June 9, 2015
    Publication date: April 27, 2017
    Applicant: Merck Sharp Dohme Corp.
    Inventors: Meredeth Ann McGowan, Kin Chiu Fong, Neville John Anthony, Hua Zhou, Jason D. Katz, Lihu Yang, Chaomin Li, Yuan Tian, Changwei Mu, Baijun Ye, Feng Shi, Xiaoli Zhao, Jianmin Fu, Yabin Li
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170114071
    Abstract: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein 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 TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 27, 2017
    Applicants: Merck Sharp & Dohme Corp., MSD R & D (China) Co., LTD.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi- Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Kerim Babaoglu, Dongfang Meng, Jane Wu, Ping Liu, Harold B. Wood, Jianming Bao, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170114056
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are 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 TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi- Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Keith P. Moore, Ping Liu, Harold B. Wood, Chun Sing Li, Qinghua Mao, Douglas C. Beshore
  • INSULIN RECEPTOR PARTIAL AGONISTS
    Publication number: 20170107268
    Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
    Type: Application
    Filed: November 19, 2015
    Publication date: April 20, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Songnian Lin, Lin Yan, Pei Huo, Dmitri Pissarnitski, Danqing Feng, Ravi Nargund, Yuping Zhu, Ahmet Kekec, Christina B. Madsen-Duggan, Zhi-Cai Shi, Zhicai Wu, Yingjun Mu
  • SURFACE DISPLAY OF WHOLE ANTIBODIES IN EUKARYOTES
    Publication number: 20170107509
    Abstract: Methods for display of recombinant whole immunoglobulins or immunoglobulin libraries on the surface of eukaryote host cells, including yeast and filamentous fungi, are described. The methods are useful for screening libraries of recombinant immunoglobulins in eukaryote host cells to identify immunoglobulins that are specific for an antigen of interest.
    Type: Application
    Filed: January 27, 2016
    Publication date: April 20, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
  • IMIDAZO-PYRAZINE DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20170107236
    Abstract: A compound of Formula II or a pharmaceutically acceptable salt thereof, are capable of monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula II, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula II or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 29, 2015
    Publication date: April 20, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brian T. Campbell, Guizhen Dong, Joie Garfunkle, Alexander Kim, Olga Ornoski, Dann L. Parker, JR., Subharekha Raghavan, Libo Xu, Zhiquang Yang
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170107204
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are 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 TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 20, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • Amino-pyrimidine-containing spleen tyrosine kinase (Syk) inhibitors
    Patent number: 9624210
    Abstract: The invention provides certain amino-pyrimidine-containing compounds. 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: December 9, 2013
    Date of Patent: April 18, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventor: Michelle R. Machacek
  • Nucleoside kinase bypass compositions and methods
    Patent number: 9624249
    Abstract: The present invention relates to disulfide masked prodrug compounds of Formula (I), nucleoside kinase bypass compositions thereof and methods that are amenable to bioactivation by a reducing agent such as glutathione: Such disulfide based compounds, compositions, and methods can be useful, for example, in providing prodrugs for use as therapeutics.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: April 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Gabor Butora