Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether 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.
Abstract: The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.
Type:
Application
Filed:
May 24, 2016
Publication date:
May 17, 2018
Applicants:
Merck Sharp & Dohme Corp., MSD R & D (China) Co. LTD.
Inventors:
Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yilli Chen, Yimin Qian, Shimin Xu, Chunmel Hu, William D. Shipe, Jianmin Fu, Zhigang Guo, HAITANG LI, Yingjian Bo
Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
Type:
Grant
Filed:
September 25, 2015
Date of Patent:
May 15, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael D. Altman, Brian M. Andresen, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. MacLean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Luis Torres
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:
Grant
Filed:
September 23, 2015
Date of Patent:
May 15, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jiaqiang Cai, Alejandro Crespo, Xiaoxing Du, Byron Gabriel Dubois, Deodialsingh Guiadeen, Shankaran Kothandaraman, Ping Liu, Rongqiang Liu, Weiguo Quan, Christopher Sinz, Liping Wang
Abstract: The invention is directed to pharmaceutically acceptable salts of suvorexant, which is an antagonist of orexin receptors. The pharmaceutically acceptable salts of suvorexant are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is further directed to pharmaceutical compositions comprising pharmaceutically acceptable salts of suvorexant.
Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
Abstract: Provided are methods of modulating cytokine activity, e.g., for the purpose of treating immune and inflammatory disorders, including tumors and cancer. Also provided are methods of administering agonists or antagonists of IL-33 and IL-33 receptor.
Type:
Grant
Filed:
February 3, 2014
Date of Patent:
May 15, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jochen Schmitz, Martin Oft, Robert A. Kastelein, J. Fernando Bazan
Abstract: Provided are methods of modulating cytokine activity, e.g., for the purpose of treating immune and inflammatory disorders, including tumors and cancer. Also provided are methods of administering agonists or antagonists of IL-33 and IL-33 receptor.
Type:
Application
Filed:
December 20, 2017
Publication date:
May 10, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Jochen Schmitz, Martin Oft, Robert A. Kastelein, J. Fernando Bazan
Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.
Type:
Application
Filed:
December 19, 2017
Publication date:
May 10, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyoshi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch
Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R7, R8 and R9 are as herein described. The present invention also provides pharmaceutical compositions comprising these compounds and methods for their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
Type:
Application
Filed:
April 4, 2016
Publication date:
May 10, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Tony SIU, Michael D. ALTMAN, Brian M. ANDRESEN, Jian LIU, Joseph KOZLOWSKI, Sobhana Babu BOGA, Younong YU, Rajan ANAND, Jiaqiang CAI, Dahai WANG, Shilan LIU
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:
Grant
Filed:
October 27, 2016
Date of Patent:
May 8, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts 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 of Formula (I) in the treatment of Btk mediated disorders.
Type:
Application
Filed:
December 17, 2015
Publication date:
May 3, 2018
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
JIAN LIU, JOSEPH A. KOZLOWSKI, SOBHANA BABU BOGA, XIAOLEI GAO, DEODIAL GUY GUIADEEN, JIAQIANG CAI, SHILAN LIU, DAHAI WANG, HAO WU, CHUNDAO YANG
Abstract: Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
Type:
Grant
Filed:
March 19, 2014
Date of Patent:
May 1, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher Dinsmore, Peter Fuller, David Guerin, Christopher F. Thompson, Qinglin Pu, Mark E. Scott, Jason David Katz, Ravi Kurukulasuriya, Joshua T. Close, Danielle Falcone, Jason Brubaker, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng
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:
Grant
Filed:
March 19, 2014
Date of Patent:
May 1, 2018
Assignee:
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
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Type:
Grant
Filed:
December 1, 2014
Date of Patent:
May 1, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Thomas Bara, Harry R. Chobanian, Yan Guo, Hubert Josien, Michael Miller, Barbara Pio, Christopher W. Plummer, Cangming Yang, Dong Xiao
Abstract: In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2A, R2B, R2, R3, RN, ring A, RA, m, ring B, RB, and n 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.
Abstract: This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administration of an RGD mimetic integrin receptor antagonist, either as a single agent or in combination with other agents.
Type:
Application
Filed:
March 24, 2016
Publication date:
April 26, 2018
Applicant:
Merck Sharp & Dohme Corp
Inventors:
Jason M. COX, Lijun MA, Xiaoyan ZHOU, Robin E. HAIMBACH, Paul J. COLEMAN, Haihong ZHOU, David E. KELLEY, Selwyn Aubrey STOCH, Le T. DUONG, Maarten HOEK
Abstract: Insulin conjugates comprising an insulin analog molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
Type:
Application
Filed:
April 4, 2016
Publication date:
April 26, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Danqing Feng, Erin N. Guidry, Pei Huo, Niels C. Kaarsholm, Songnian Lin, Ravi P. Nargund, Lin Yan
Abstract: The present invention is directed to process for making Compounds of Formula (II): (II), and salts thereof, wherein B, X, R2, R3, R4 R7, R8 and R9 are defined herein.
Abstract: Antibodies which block binding of hPD-1 to hPD-L1 or hPD-L2 and their variable region sequences are disclosed. A method of increasing the activity (or reducing downmodulation) of an immune cell through the PD-1 pathway is also disclosed.
Type:
Application
Filed:
November 13, 2017
Publication date:
April 26, 2018
Applicant:
Merck Sharp & Dohme B.V.
Inventors:
Gregory John Carven, Hans van Eenennaam, Gradus Johannes Dulos