Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N?; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
Type:
Grant
Filed:
December 1, 2015
Date of Patent:
October 2, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Dann L. Parker, Jr., Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Wanying Sun, Feroze Ujjainwalla, Chunhui Huang
Abstract: The present invention relates to coloured laser-markable and laser-weldable polymeric materials which are distinguished by the fact that they comprise, as absorber, at least one doped tin oxide or indium oxide having a large specific surface area.
Abstract: The invention is directed to novel anhydrous crystalline butenedioate salt form 1 of Compound I, which is a modulator of muscarinic M1 receptors. The novel crystalline forms of compound I are useful in the treatment or prevention of Alzheimer's disease and other disorders and diseases in which muscarinic M1 receptors are involved. The invention is further directed to pharmaceutical compositions comprising the novel crystalline forms of Compound I.
Type:
Application
Filed:
September 26, 2016
Publication date:
September 27, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
C. Scott Shultz, Courtney Maguire, Yanke Xu
Abstract: The invention relates to bismuth perfluoroalkylphosphinates as Lewis acid catalysts, the compounds, and processes for the preparation thereof. ArxBi[OP(O)(Rf)2]3-x??(Ia), Ar3Bi[OP(O)(Rf)2]2??(Ib).
Type:
Application
Filed:
September 7, 2016
Publication date:
September 27, 2018
Applicant:
MERCK PATENT GMBH
Inventors:
Berthold Theo HOGE, Sven Joerg-Ruediger August SOLYNTJES, Nikolai (Mykola) IGNATIEV
Abstract: The invention relates to perfluoroalkyl group-containing bismuth compounds as Lewis acid catalysts, to specific compounds, and to the method for the production thereof.
Type:
Application
Filed:
September 16, 2016
Publication date:
September 27, 2018
Applicant:
MERCK PATENT GMBH
Inventors:
Berthold Theo HOGE, Sven Joerg-Ruediger August SOLYNTJES, Anne Julia BADER, Nikolai IGNATIEV
Abstract: The invention relates to a liquid-crystalline medium comprising at least one compound of the formula I, in which R1 and R2 have the meanings indicated in Claim 1, and to the use thereof in electro-optical liquid-crystal displays.
Abstract: The present invention relates to Phosphate 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 Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
March 25, 2016
Date of Patent:
September 25, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
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:
Grant
Filed:
April 11, 2016
Date of Patent:
September 25, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Eric Mertz, Scott D. Edmondson, Sung-Sau So, Wanying Sun, Weiguo Liu, Santhosh F. Neelamkavil, Ying-Duo Gao, Alan Hruza, Yi Zang, Amjad Ali, Rudrajit Mal, Jiafang He, Rongze Kuang, Heping Wu, Anthony K. Ogawa, Andrew F. Nolting
Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Grant
Filed:
April 18, 2017
Date of Patent:
September 25, 2018
Assignee:
Merck Patent GmbH
Inventors:
Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth C. Deselm, Hui Qiu, Yufang Xiao, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
Abstract: The invention provides novel heterocyclic carboxamide compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Grant
Filed:
August 3, 2016
Date of Patent:
September 25, 2018
Assignee:
Merck Patent GmbH
Inventors:
Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Ruoxi Lan, Lizbeth Celeste De Selm, Constantin Neagu, Justin Potnick, Srinivasa R. Karra, Theresa L Johnson
Abstract: The present invention relates to pyrazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle stimulating hormone receptor (FSHR).
Type:
Grant
Filed:
June 24, 2014
Date of Patent:
September 25, 2018
Assignee:
Merck Patent GmbH
Inventors:
Henry Yu, Marianne Donnelly, Ngan Nguyen, Xuliang Jiang
Abstract: The present invention relates to liquid-crystalline media comprising a) one or more compounds of the formula ST-1, as defined herein, and b) one or more compounds of the formula ST-2, as defined herein, and c) one or more compounds of the formula RV, as defined herein, and d) one or more compounds selected from formula IA and IB, as defined herein, and to liquid-crystal displays containing these media, especially to displays addressed by an active matrix and in particular to displays of the in-plane switching (IPS) or fringe-field switching (FFS) type.
Abstract: The invention relates to arylamino compounds and to the use thereof in electronic devices, for example organic electroluminescent devices. The invention furthermore relates to electronic devices comprising one or more of the said compounds, for example as hole-transport materials in a corresponding functional layer of the device. The invention furthermore relates to a process for the preparation of the said compounds, and to a formulation comprising one or more of the said compounds.
Type:
Application
Filed:
May 23, 2018
Publication date:
September 20, 2018
Applicant:
Merck Patent GmbH
Inventors:
Philipp Stoessel, Frank Voges, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Christian Wirges
Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
Type:
Application
Filed:
January 31, 2018
Publication date:
September 20, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ayesha Sitlani, Carl P. Sparrow, Shilpa Pandit, Jon H. Condra, Holly A. Hammond
Abstract: Liquid-crystalline media containing a) one or more compounds of formula IA, and b) one or more compounds of formula II and c) one or more compounds of formulae III-1 to III-4, their use in electro-optical displays, particularly in active-matrix displays based on the VA, ECB, FFS or IPS effect.
Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
Abstract: Disclosed are pigment powders containing only coated BiOCl flakes, which flakes area) BiOCl flakes having a coating containing yellow iron oxide Fe2O3*xH2O, optionally a colorant, optionally an adjuvant, and optionally SiO2, b) BiOCl flakes having a coating containing SiO2, optionally a colorant, and optionally an adjuvant, c) BiOCl flakes having a coating containing a colorant, SiO2, optionally yellow iron oxide Fe2O3*xH2O, and optionally an adjuvant, or d) BiOCl flakes having a coating containing Fe3O4 and optionally SiO2, to a process for the preparation of the pigment powders, and to the use thereof especially in cosmetic formulations.
Type:
Application
Filed:
March 19, 2018
Publication date:
September 20, 2018
Applicant:
Merck Patent GmbH
Inventors:
Padma KAVIRATNA, Mark TELLEFSEN, Qingmin CHENG, Matthew EDDENS, Qinyun PENG
Abstract: A liquid-crystalline medium which comprises at least one compound of the formula I, and one or more compounds of the formula ST and to the use thereof for an active-matrix display, in particular based on the VA, PSA, PA-VA, SS-VA, SA-VA, PS-VA, PALC, IPS, PS-IPS, UB-FFS, U-IPS, FFS or PS-FFS effect.
Abstract: The invention relates to arylamino compounds and to the use thereof in electronic devices, for example organic electroluminescent devices. The invention furthermore relates to electronic devices comprising one or more of the said compounds, for example as hole-transport materials in a corresponding functional layer of the device. The invention furthermore relates to a process for the preparation of the said compounds, and to a formulation comprising one or more of the said compounds.
Type:
Application
Filed:
May 23, 2018
Publication date:
September 20, 2018
Applicant:
Merck Patent GmbH
Inventors:
Philipp Stoessel, Frank Voges, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Christian Wirges
Abstract: The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries arthritis, pain, allodynia or hyperalgesia.