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 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 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 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 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: 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 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 compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Type:
Application
Filed:
November 1, 2017
Publication date:
May 2, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
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:
Grant
Filed:
December 4, 2017
Date of Patent:
April 30, 2019
Assignee:
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 instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
Type:
Application
Filed:
March 24, 2017
Publication date:
April 25, 2019
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Abdelghani Abe Achab, Matthew P. Christopher, Francesc Xavier Fradera Llinas, Jason D. Katz, Joey L. Methot, Hua Zhou, Shimin Xu, Jianmin Fu, Ning Fu, Yabin Li, Xichao Wang
Abstract: Intelligent refrigerator system for storing pharmaceutical product containers, such as vials, ampules, syringes, bottles, medication tubes, blister packs and cartons, at the point of dispensing. Embodiments of the invention use product identification technology, such as radio-frequency identification (RFID) tags and readers, to uniquely identify containers as they are added to or removed from the cold storage compartment of the refrigerator, and automatically retrieve from a local or remote database a variety of details associated with the containers and their contents, such as manufacturing data, expiration dates, time out of refrigeration, inventory levels, safety information, usage statistics, known contraindications and warnings, etc. If the details indicate that there is a problem with a particular pharmaceutical (e.g.
Abstract: An application shim receives transactions that will update a portion of data stored in an existing data store. A reduced representation of the pre-update portion of data is generated and compared to an existing reduced representation of the same portion of data to verify that the data has not been tampered with. An updated reduced representation is generated based on the post-update portion of data. The updated reduced representation is added to a distributed ledger such as a block chain. Further verification of non-tampering may be provided by comparing the reduced representation stored by the system and the one appended to the blockchain. If a discrepancy is identified, appropriate corrective action may be taken, such as blocking further transactions, notifying responsible entities, and/or restoring the data from a backup.
Abstract: A supercritical extractor system may include extractor chambers coupled to a supercritical fluid pump and configured to receive a matrix for an extraction process and a supercritical fluid from the supercritical fluid pump, and evaporator chambers coupled to the extractor chambers and configured to output an extractant from the matrix. Each evaporator chamber may include a body defining a cavity, a cone within the cavity, and arms coupled between an inner surface of the body and the cone. The supercritical extractor system may include a condenser coupled between the evaporator chambers and the supercritical fluid reservoir, and a controller coupled to the supercritical fluid pump, the extractor chambers, and the evaporator chambers and configured to monitor a characteristic during the extraction process.
Type:
Application
Filed:
April 18, 2017
Publication date:
April 11, 2019
Applicants:
Merck Sharp & Dohme Corp., The Board of Regents, The University of Texas System
Inventors:
Tong-Ming Fu, Aimin Tang, Dai Wang, Zhiqiang An, Ningyan Zhang, Sha Ha
Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
Inventors:
Bryon L. Simmons, Kevin R. Campos, Artis Klapars, Alistair J. Stewart, Benjamin A. Mayes, Peter E. Maligres, Alan Hyde, Steven Mark Silverman, Yong-Li Zhong, Adel M. Moussa, Kenneth Baker, Kara Van Valkenburg
Abstract: The present invention provides a chewable dosage form having a matrix comprising: a combination of active pharmaceutical ingredients which is metformin hydrochloride and sitagliptin or a pharmaceutically acceptable salt thereof, fully or partially pregelatinized starch, a texture-modifying gum, a lubricant, an emulsifier, a flavoring agent, and a sweetener. The present invention also provides a method of treating diabetes, e.g., non-insulin dependent (Type 2) diabetes mellitus, comprising administering a therapeutically effective amount of the chewable dosage form to a mammalian patient in need thereof.
Abstract: The present invention provides a chewable dosage form having a matrix comprising: a combination of active pharmaceutical ingredients which is metformin hydrochloride and sitagliptin or a pharmaceutically acceptable salt thereof; a fully or partially pregelatinized starch, a polyethylene glycol polymer; a lubricant; an emulsifier; a flavoring agent; and a sweetener. The present invention also provides a method of treating diabetes, e.g., non-insulin dependent (Type 2) diabetes mellitus, comprising administering a therapeutically effective amount of the chewable dosage form to a mammalian patient in need thereof.
Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
May 23, 2016
Date of Patent:
April 2, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Joie Garfunkle, Olga Ornoski, Dann L. Parker, Jr., Subharekha Raghavan, Libo Xu
Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R7, R8 and R9 are as herein described. The present invention also provides pharmaceutical compositions comprising these compounds and methods for 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:
Grant
Filed:
April 4, 2016
Date of Patent:
April 2, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tony Siu, Michael D. Altman, Brian M. Andresen, Jian Liu, Joseph Kozlowski, Sobhana Babu Boga, Younong Yu, Rajan Anand, Jiaqiang Cai, Dahai Wang, Shilan Liu
Abstract: Disclosed are compounds of Formula A-1, or a salt thereof: Formula A-1, where J, K, Q and R1 are as defined herein, which compounds have properties for inhibiting sodium ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-1 or their salts, and methods of treating pain (e.g. chronic pain), or cough or itch disorders using the same.
Type:
Application
Filed:
March 17, 2017
Publication date:
March 28, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Anthony J. Roecker, Mark E. Layton, Thomas J. Greshock, Joseph E. Pero, Michael J. Kelly, III, Ting Zhang