Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.
Type:
Grant
Filed:
October 1, 2015
Date of Patent:
May 21, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Markus Klein, Oliver Schadt, Philipp Haselmayer, Michael Busch
Abstract: The present invention relates to liquid-crystalline media (LC media) having negative or positive dielectric anisotropy, comprising a low-molecular-weight component and a polymerizable component. The polymerizable component comprises self-aligning, polymerizable mesogens (polymerizable self-alignment additives) which effect homeotropic (vertical) alignment of the LC media at a surface or the cell walls of a liquid-crystal display (LC display). The invention therefore also encompasses LC displays having homeotropic alignment of the LC medium without alignment layers. The invention discloses novel structures for polymerizable self-alignment additives which have a certain position of the functional groups.
Type:
Grant
Filed:
June 25, 2015
Date of Patent:
May 21, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Graziano Archetti, Izumi Saito, Rocco Fortte, Oliver Heppert, Andreas Taugerbeck, Elena Neumann
Abstract: The invention relates to methods of treating cancer in a subject, comprising administering to the subject a therapeutically effective amount of an inhibitor of the interaction between the PD-1 receptor and its ligand PD-L1.
Type:
Application
Filed:
May 22, 2017
Publication date:
May 16, 2019
Applicants:
MERCK PATENT GMBH, PFIZER INC.
Inventors:
Dimitry NUYTEN, Alexei MOROZOV, Adrian WOOLFSON, Aron THALL, Kevin CHIN, Satjit BRAR
Abstract: The present invention relates to organic dielectric layers comprising a polycycloolefinic polymer with a pendent chromophoric group having an absorption maximum in the wavelength range from 230 to 290 nm, and to organic electronic devices comprising them.
Type:
Application
Filed:
May 15, 2017
Publication date:
May 16, 2019
Applicants:
PROMERUS, LLC, MERCK PATENT GMBH
Inventors:
IRINA AFONINA, TOMAS BACKLUND, LARRY F RHODES, HUGH A BURGOON
Abstract: A method can treat a patient suffering from at least one of fibrosis and a fibrotic disorder. The method includes administering a therapeutically effective amount of an anti-?v integrin antibody DI17E6, or a biologically active variant or modification thereof, to the patient.
Abstract: The present invention relates to certain SGLT-2 inhibitors, such as ertugliflozin or a co-crystal or a pharmaceutically acceptable salt thereof, for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD).
Type:
Application
Filed:
January 10, 2019
Publication date:
May 16, 2019
Applicants:
Merck Sharp & Dohme Corp., Pfizer Inc.
Inventors:
Ramachandra G. Naik, Elizabeth S. Ommen, James Michael Rusnak, Steven G. Terra
Abstract: The present invention provides compositions comprising insulin receptor partial agonists in association with GLP-1 analogues (e.g., liraglutide) as well as methods for using the compositions for example, to treat or prevent diabetes or to decrease body weight.
Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
Type:
Application
Filed:
January 10, 2019
Publication date:
May 16, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Application
Filed:
November 12, 2018
Publication date:
May 16, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Yongxin Han, Abdelghani Achab, Yongqi Deng, Xavier Fradera, Craig Gibeau, Brett A. Hopkins, Derun Li, Kun Liu, Meredeth A. McGowan, Nunzio Sciammetta, David Sloman, Catherine White, Hongjun Zhang, Hua Zhou
Abstract: The present invention is directed to pyrimidine carboxamide 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 hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
March 21, 2016
Date of Patent:
May 14, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dong-Ming Shen, Jonathan E. Wilson, Meng Yang, Dann Parker, Zack Zhiqiang Guo, Alejandro Crespo, Deping Wang, Troy McCracken
Abstract: The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Grant
Filed:
November 20, 2017
Date of Patent:
May 14, 2019
Assignee:
Merck Patent GmbH
Inventors:
Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao
Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
Type:
Grant
Filed:
March 12, 2014
Date of Patent:
May 14, 2019
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
Abstract: The present invention relates to compounds according to Formula (I) and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment o RORgammaT-mediated diseases or conditions.
Type:
Grant
Filed:
October 27, 2016
Date of Patent:
May 14, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Blair T. Lapointe, Peter H. Fuller, Hakan Gunaydin, Kun Liu, Mark E. Scott, B. Wesley Trotter, Hongjun Zhang
Abstract: The present invention is directed to pyrimidinone amide compounds which may be useful as therapeutic agents for the treatment of central nervous system and/or peripheral 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, Alzheimer's, cognitive impairment, anxiety, depression, migraines, or Huntington's disease, Parkinson's disease, Parkinson's disease dementia (PDD), and other diseases associated with striatal hypofunction or basal ganglia dysfunction.
Abstract: The present invention relates to certain SGLT-2 inhibitors, such as ertugliflozin or a co-crystal or a pharmaceutically acceptable salt thereof, for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD). The present invention also relates to methods for preventing neuronal damage following the incidence of ischemic stroke and close-head traumatic brain injury in animals comprising the step of administering to an animal, in need of such treatment, a therapeutically effective amount of ertugliflozin or a co-crystal or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 5, 2015
Date of Patent:
May 14, 2019
Assignees:
Merck Sharp & Dohme Corp., Pfizer Inc.
Inventors:
Ramachandra G. Naik, Elizabeth S. Ommen, James Michael Rusnak, Steven G. Terra
Abstract: The present invention relates to laser-markable and laser-weldable polymeric materials which are distinguished by the fact that they comprise, as laser absorber, at least one copper-doped zinc sulfide.
Type:
Grant
Filed:
November 18, 2015
Date of Patent:
May 14, 2019
Assignee:
Merck Patent GmbH
Inventors:
Reinhold Rueger, Ulrich Quittmann, Silvia Rosenberger
Abstract: The present invention relates to bisimidazolium salts, to novel mono- and biscarbenes derived therefrom, and to metal complexes which contain corresponding mono- and biscarbenes as ligands, to a process for the preparation of the bisimidazolium salts according to the invention, the mono- and biscarbenes according to the invention and to the metal complexes according to the invention, and to the use of the bisimidazolium salts according to the invention, the mono- and biscarbenes according to the invention and to the use of the metal complexes according to the invention.
Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) 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 hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
June 27, 2016
Date of Patent:
May 14, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Shawn J. Stachel, Michael P. Dwyer, Christopher J. Sinz, Jonathan E. Wilson, Daniel V. Paone, Yili Chen, Shimin Xu
Abstract: Compounds of the formula I in which X, Y, R1 and R2 have the meanings indicated in claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.
Abstract: The present invention relates to the use of an amino sugar as plasticizer in formulations comprising a polymer as carrier for active ingredients, in particular for compositions which are intensively mixed by treatment in a melt extrusion and then formulated by suitable post-treatment.