Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) 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:
January 11, 2018
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
JIAN LIU, JOSEPH A. KOZLOWSKI, XIAOLEI GAO, DEODIAL GUY GUIADEEN, SHILAN LIU, DAHAI WANG
Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
September 26, 2014
Date of Patent:
January 9, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tao Yu, Yonglian Zhang, Sherman Tim Waddell, Andrew Stamford, John S. Wai, Paul J. Coleman, John M. Sanders, Ronald Ferguson, Thomas H. Graham, Hong Li
Abstract: The present invention relates to dengue virus vaccine compositions comprising a first and a second dengue vaccine, wherein the first dengue vaccine is a live, attenuated dengue vaccine and the second dengue vaccine is a recombinant dengue subunit vaccine or an inactivated dengue vaccine; wherein the live attenuated dengue vaccine comprises at least one live, attenuated dengue virus or at least one live attenuated chimeric flavivirus. The dengue virus vaccine compositions of the invention may further comprise one or more adjuvants. In preferred embodiments of the invention, the first and the second dengue vaccine are tetravalent. The invention also relates to methods of using the dengue virus vaccine compositions of the invention to treat or prevent dengue infection, or to prevent, ameliorate, or delay the onset or progression of the clinical manifestations thereof.
Type:
Grant
Filed:
June 17, 2014
Date of Patent:
January 9, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Andrew Bett, Beth-Ann Griswold Coller, Govindarajan Dhanasekaran, Ramesh V. Chintala
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:
Grant
Filed:
March 23, 2015
Date of Patent:
January 9, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
Abstract: The instant invention relates to mesogenic media comprising one or more compounds of formula D wherein the parameters are as specified in the text, preferably to mesogenic media showing a blue phase, preferably stabilised by a polymer, and their use in electro-optical light modulation elements and their respective use in displays, as well as to such devices.
Abstract: The present invention relates to a method for producing a marking in a coating on a substrate or on the surface of a molding, where the marking represents a negative marking within a luminescent surrounding field and is generated using a laser beam, to a marking produced with the aid of the method, and to the use thereof, in particular for the labeling of products.
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:
Grant
Filed:
October 26, 2015
Date of Patent:
January 9, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Fa-Xiang Ding, Shuzhi Dong, Jinlong Jiang, Takao Suzuki, Joseph P. Vacca, Shouning Xu
Abstract: Compounds of the formula I in which X, Y, Q1, M, Q2 and B have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
Type:
Grant
Filed:
April 9, 2014
Date of Patent:
January 9, 2018
Assignee:
Merck Patent Gmbh
Inventors:
Guenter Hoelzemann, Dieter Dorsch, Ansgar Wegener, Oliver Poeschke, Michael Busch
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:
Grant
Filed:
March 23, 2015
Date of Patent:
January 9, 2018
Assignee:
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
Abstract: The invention provides novel substituted indazole compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
Type:
Grant
Filed:
July 30, 2015
Date of Patent:
January 9, 2018
Assignees:
Merck Patent GmbH, Cancer Research Technology Limited
Abstract: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:
Type:
Grant
Filed:
July 16, 2015
Date of Patent:
January 9, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
John Y. L. Chung, Feng Peng, Yonggang Chen, Amude Mahmoud Kassim, Cheng-yi Chen, Mathew Maust, Mark McLaughlin, Michael J. Zacuto, Qinghao Chen, Lushi Tan, Zhiguo Jake Song, Yang Cao, Feng Xu
Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds comprising a self-alignment additive for vertical alignment and additionally at least one compound of formula I as described more closely within this disclosure (polymerizable HALS), especially for vertically aligned display applications.
Abstract: The invention relates to a light modulation element comprising a cholesteric liquid crystalline medium sandwiched between two substrates (1), provided with a common electrode structure (2) and a driving electrode structure (3) individually, wherein the substrate with driving and/or common electrode structure is additionally provided with an alignment electrode structure (4) which is separated from the driving and or common electrode structure on the same substrate by a dielectric layer (5), characterized in that it comprises at least one alignment layer (6) directly adjacent to the liquid crystalline medium. The invention is further related to a method of production of said light modulation element and to the use of said light modulation element in various types of optical and electro-optical devices, such as electro-optical displays, liquid crystal displays (LCDs), non-linear optic (NLO) devices, and optical information storage devices.
Type:
Application
Filed:
December 30, 2015
Publication date:
January 4, 2018
Applicant:
Merck Patent GmbH
Inventors:
Kuan-Yu CHEN, Ming-Chou WU, Bernd FIEBRANZ, Harald SEIBERT
Abstract: The present invention relates to the preparation and use of recombinant variants of group 5 allergens of the Poaceae (true grasses), which are characterised by reduced IgE reactivity compared with known wild-type allergens and at the same time substantially retained reactivity with T-lymphocytes.
Type:
Application
Filed:
September 11, 2017
Publication date:
January 4, 2018
Applicant:
Merck Patent GmbH
Inventors:
Martin WALD, Andreas NANDY, Helmut FIEBIG, Bernhard WEBER, Helga KAHLERT, Gerald REESE, Oliver CROMWELL
Abstract: An electronic component (10) comprising a plurality of switching elements (1) which comprise, in this sequence, a first electrode (16), a molecular layer (18) bonded to a substrate, and a second electrode (20), where the molecular layer essentially consists of molecules (M) which contain a connecting group (V) and an end group (E) having a polar or ionic function, is suitable as memristive device for digital information storage.
Type:
Application
Filed:
December 8, 2015
Publication date:
January 4, 2018
Applicant:
MERCK PATENT GMBH
Inventors:
Peer KIRSCH, Qiong TONG, Andreas RUHL, Marc TORNOW, Achyut BORA
Abstract: The invention includes a granular composition comprising the active ingredient (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3- carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (5)-N-(3-(6-isopro-poxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-di-hydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide Form 1 HCl, about 10-30% (5)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base.
Type:
Application
Filed:
December 14, 2015
Publication date:
January 4, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Deepak Bahl, Yung-Chi Lee, Alfred Lee, William Anthony Marinaro, Jr., Dan Zhang, Tao Feng
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:
January 15, 2016
Publication date:
January 4, 2018
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Eric Mertz, Weiguo Liu, Scott D. Edmondson, Amjad Ali, Ying-Duo Gao, Santhosh F. Neelamkavil, Sung-Sau So, Remond Moningka, Wanying Sun, Alan Hruza, Linda L. Brockunier
Abstract: The present invention relates to liquid-crystalline media comprising one or more compounds of formula T and one or more compounds selected from the group of compounds of formulae I, II and III, in which the parameters have the meaning indicated in Claim 1, and to components comprising these media for high-frequency technology, in particular phase shifters and microwave array antennas.
Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.
Type:
Application
Filed:
August 24, 2017
Publication date:
January 4, 2018
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Vinay M. Girijavallabhan, David B. Olsen, Zhibo Zhang, Jianmin Fu, Bing-Yu Tang