Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Type:
Application
Filed:
December 4, 2017
Publication date:
April 5, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
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:
April 3, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael D. Altman, 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, Graham F. Smith
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:
September 30, 2014
Date of Patent:
April 3, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tesfaye Biftu, Purakkattle Biju, Steven L. Colletti, Mingxiang Cui, William K. Hagmann, Bin Hu, Hubert Josien, Nam Fung Kar, Anilkumar Nair, Ravi Nargund, Donald M. Sperbeck, Cheng Zhu
Abstract: The present invention relates to anti-CD27 antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
Inventors:
Amy M. Beebe, Jason Ka Jen Cheung, Veronica Juan, Laurence Fayadat-Dilman, Svetlana Sadekova, Jerelyn Wong, Hans van Eenennaam, Andrea van Elsas, Lars Guelen, Thierry Olivier Fischmann, Winifred W. Prosise
Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild 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:
Application
Filed:
September 25, 2017
Publication date:
March 29, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Iyassu K. Sebhat, Ashok Arasappan, Scott B. Hoyt, Robert R. Wilkening, Duane DeMong
Abstract: The present invention is directed to stable pharmaceutical formulations. More specifically, the present invention is directed to stable pharmaceutical formulations of testosterone undecanoate.
Abstract: Pharmaceutical compositions are provided in unit dosage forms comprising ceftolozane and tazobactam in separate unit dosage form containers, ceftolozane prepared in the absence of tazobactam, tazobactam prepared in the absence of ceftolozane, and/or compositions where ceftolozane and tazobactam are first combined within a unit dosage form container.
Type:
Grant
Filed:
March 16, 2016
Date of Patent:
March 27, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Joseph Terracciano, Nicole Miller Damour, Chun Jiang, Giovanni Fogliato, Giuseppe Alessandro Donadelli, Dario Resemini
Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
Type:
Grant
Filed:
December 10, 2015
Date of Patent:
March 27, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Seoju Lee, David C. Wylie, Susan V. Cannon-Carlson
Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation
Type:
Grant
Filed:
October 9, 2017
Date of Patent:
March 27, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Andrew John Harvey, Ian M. Bell
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:
July 9, 2015
Date of Patent:
March 27, 2018
Assignee:
Merck Sharp Dohme Corp.
Inventors:
Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinglong Jiang, Shuzhi Dong, Xin Gu
Abstract: A method for the treatment of cancer by administering a therapeutically effective amount of a cyclin-dependent kinase (CDK) inhibitor with a therapeutically effective amount of a B cell chronic lymphocytic leukemia/lymphoma 2 inhibitor (“B Cell CLL/Lymphoma 2”, or “BCL-2”). Administration of the CDK inhibitor and BCL-2 inhibitor can be simultaneous, successive or separate.
Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
Type:
Application
Filed:
November 29, 2017
Publication date:
March 22, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Sydney O. Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
Abstract: The present disclosure provides processes for describing and quantifying the expression of human programmed death ligand-1 (PD-L1) in tumor tissue sections as detected by immunohistochemical assay using an antibody that specifically binds to PD-L1. The results generated using these processes have a variety of experimental, diagnostic and prognostic applications.
Type:
Application
Filed:
September 22, 2017
Publication date:
March 22, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Marisa Dolled-Filhart, Kenneth Emancipator, Frank Lynch, Robert H. Pierce, Dianna Wu
Abstract: The present invention is directed to methyloxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 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 compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
Type:
Grant
Filed:
November 30, 2015
Date of Patent:
March 20, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Nigel Liverton, Yunfu Luo
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:
October 4, 2017
Publication date:
March 15, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Abbas M. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (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:
March 13, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Ping Liu, Dann Parker, Chun Sing Li, Qinghua Mao
Abstract: The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.
Inventors:
Cameron James Smith, John Qiang Tan, Ting Zhang, James Balkovec, William John Greenlee, Liangqin Guo, Yi-Heng Chen, Yili Chen, Samuel Chackalamannil, Tomokazu Hirabayashi, Mika Sekioka
Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
Type:
Application
Filed:
November 9, 2017
Publication date:
March 8, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
John Y.L. CHUNG, Kevin CAMPOS, Edward CLEATOR, Robert F. DUNN, Andrew GIBSON, R. Scott HOERRNER, Stephen KEEN, Dave LIEBERMAN, Zhuqing LIU, Joseph LYNCH, Kevin M. MALONEY, Feng XU, Nobuyoshi YASUDA, Naoki YOSHIKAWA, Yong-Li ZHONG
Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
Type:
Application
Filed:
September 25, 2017
Publication date:
March 8, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Petr Vachal, Izzat Raheem, Zhiqiang Guo, Timothy John Hartingh
Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
Type:
Application
Filed:
November 20, 2017
Publication date:
March 8, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi