Abstract: A system and a method are disclosed for searching and ranking molecules based on specificity. To this end, a processor receives a request to search for molecules that correspond to biological features, and generates a mapping of molecules to the biological features by searching publications for a reference to a biological feature in connection with a molecule, and responsively adding to the mapping any found references. The processor determines a respective specificity score for each respective molecule of the plurality of molecules by determining which of the plurality of biological features are mapped to each respective molecule, and for each such respective biological feature, in response to determining that there is not more than one concrete instance that is mapped to the respective molecule, incrementing the respective specificity score by a unit. The processor generates a ranking based on the respective specificity scores and outputs the ranking.
Abstract: The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
Type:
Grant
Filed:
October 6, 2017
Date of Patent:
April 13, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Umar Faruk Mansoor, Christian Fischer, Phieng Siliphaivanh, Luis Torres, Hakan Gunaydin, David L. Sloman
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 15, 2017
Date of Patent:
April 6, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael Miller, Harry R. Chobanian, Shuwen He, Jinsong Hao, Barbara Pio, Yan Guo, Dong Xiao
Abstract: Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
Type:
Grant
Filed:
November 13, 2017
Date of Patent:
April 6, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Thomas J. Greshock, James Mulhearn, Anthony J. Roecker, Tianying Jian, Gang Zhou, Liangqin Guo, Walter Won, Ting Zhang, Rajan Anand, John E. Stelmach, Deping Wang, Ronald M. Kim, Mark E. Layton, Christopher S. Burgey, Philippe G. Nantermet
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:
August 6, 2015
Date of Patent:
April 6, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Helen Chen, Steven L. Colletti, Duane DeMong, Yan Guo, Michael Miller, Anilkumar Nair, Christopher W. Plummer, Dong Xiao, De-Yi Yang
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 Formula (I).
Type:
Application
Filed:
November 12, 2018
Publication date:
April 1, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Steven L. Colletti, Duane DeMong, Kevin D. Dykstra, Zhiyong Hu, Michael Miller
Abstract: This invention relates to novel implant drug delivery systems for long-acting delivery of antiviral drugs. These compositions are useful for the treatment or prevention of human immunodeficiency virus (HIV) infection.
Type:
Application
Filed:
April 5, 2018
Publication date:
April 1, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Stephanie Elizabeth Barrett, Marian E. Gindy, Li Li, Ryan S. Teller, Seth P. Forster
Abstract: The present invention relates to methods for the recombinant expression of chlamydia major outer membrane protein (MOMP) comprising transforming a population of E. coli host cells with an expression vector comprising a nucleic acid molecule that encodes chlamydia MOMP and encodes a leader sequence for targeting the MOMP to the outer membrane of the cell, wherein the nucleic acid molecule is operatively linked to a promoter. The method of the invention allows expression of MOMP in the outer membrane of the cell, which leads to protein folding that is more like native MOMP relative to a MOMP protein that is expressed intracellularly. Also provided by the invention are uses of the recombinant MOMP in pharmaceutical compositions and methods for the treatment and/or prophylaxis of chlamydia infection and/or the effects thereof.
Type:
Application
Filed:
June 8, 2020
Publication date:
April 1, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Lan Zhang, Zhiyun Wen, Craig T. Przysiecki, Puneet Khandelwal, Ping Qiu
Abstract: In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
Type:
Grant
Filed:
October 9, 2017
Date of Patent:
March 30, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu
Abstract: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R9, and A are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. 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 LRRK-2 kinase is involved.
Type:
Grant
Filed:
August 28, 2015
Date of Patent:
March 23, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Xing Dai, Kallol Basu, Duane DeMong, Sarah W. Li, Michael Miller, Jack D. Scott, Andrew W. Stamford
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 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. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula (I) and derivatives thereof.
Abstract: 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:
Application
Filed:
October 30, 2017
Publication date:
March 18, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
BRENDAN M. CROWLEY, IAN M. BELL, ANDREW JOHN HARVEY, BRIAN T. CAMPBELL, THOMAS J. GRESHOCK, VANESSA L. RADA
Abstract: The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
Type:
Grant
Filed:
November 13, 2017
Date of Patent:
March 16, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dong-Ming Shen, Thomas H. Graham, Jinlong Jiang, Fa-Xiang Ding, Clare Tudge
Abstract: A process for producing recombinant trypsin from prokaryote host cells in high yield and high specific activity is described. In particular, a process for producing recombinant trypsin from E. coli is described.
Abstract: The present invention is directed to azabicyclo[4.1.0]heptane compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. 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 M4 muscarinic acetylcholine 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 M4 muscarinic acetylcholine receptors are involved.
Type:
Grant
Filed:
June 4, 2018
Date of Patent:
March 16, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dane James Clausen, James I. Fells, Joseph A. Kozlowski, Ping Liu, Robert D. Mazzola, Jr.
Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
Type:
Grant
Filed:
April 29, 2019
Date of Patent:
March 16, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Mihir B. Mandal, David B. Olsen, Jing Su, Lihu Yang, Katherine Young, Takao Suzuki, Lanying You
Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of cancer.
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 (I).
Type:
Application
Filed:
April 29, 2019
Publication date:
March 11, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Brendan M. Crowley, Brian T. Campbell, Harry R. Chobanian, James I. Fells, Deodial G. Guiadeen, Thomas J. Greshock, Kenneth J. Leavitt, Vanessa L. Rada, Ian M. Bell