Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Application
Filed:
December 12, 2016
Publication date:
December 20, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Yongxin Han, Abdelghani Achab, Purakkattle Biju, Yongqi Deng, Xavier Fradera, Liangqin Guo, Shuwen He, Joseph Kozlowski, Ravi Kurukulasuriya, Kun Liu, Meredeth Ann McGowan, Qinglin Pu, Nunzio Sciammetta, Hongjun Zhang, Hua Zhou
Abstract: Compounds of Formula I: 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 HV 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:
December 12, 2016
Publication date:
December 20, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Wenlang Fu, Zhiqiang Guo, Ning Qi, Izzat T. Raheem, Petr Vachal, Ming Wang, John D. Schreier
Abstract: Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Na 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 pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.
Type:
Application
Filed:
December 15, 2016
Publication date:
December 20, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Thomas J. Greshock, James Mulhearn, Liangqin Guo, Ting Zhang, Deping Wang, Ronald M. Kim, Mark E. Layton, Michael J. Kelly, III, Rajan Anand, Philippe Nantermet, Tianying Jian, Anthony J. Roecker, Walter Won, Gang Zhou
Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
Type:
Grant
Filed:
July 29, 2015
Date of Patent:
December 18, 2018
Assignee:
Merck Sharp & Dohme B.V.
Inventors:
Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
Abstract: A drug delivery device comprising a main body extending between distal and proximal ends comprising a hollow cylinder comprising an outer and an inner surface, wherein the inner surface comprises threads; a screw within the main body, comprising a hollow cylinder comprising an inner and an outer surface, wherein said outer surface comprises threads, wherein threads of outer surface of the screw are engaged with threads of inner surface of the main body; a plunger extending between distal and proximal ends, wherein the distal end of the plunger engages the proximal end of the screw; and a drug container extending between distal and proximal ends, and comprising a change in cross section from proximal to distal end, wherein the container is within the screw, and wherein the proximal end of the drug container is fixed to the screw and distal end of the container is fixed to the main body.
Abstract: The present invention relates to carboxamide 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:
March 7, 2016
Date of Patent:
December 18, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jongwon Lim, Michael D. Altman, Matthew L. Childers, Craig R. Gibeau, Ginny Dai Ho, Honchung Tsui
Abstract: A process is described for purifying insulin and insulin analogs that comprises use of two or more orthogonal chromatographic purification steps in tandem following enzymatic digestion of the propeptide-insulin precursor to remove specific product impurities, improve process consistency, and increase process redundancy in the purification of the insulin or insulin analog, e.g., insulin lispro.
Type:
Grant
Filed:
July 16, 2015
Date of Patent:
December 18, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Douglas S. Watson, Allison D. Ortigosa, Michael A. Rauscher, Kathryn M. Story
Abstract: The present invention is directed to amidoethyl azole 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:
December 18, 2015
Date of Patent:
December 18, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Nigel Liverton, Yunfu Luo
Abstract: Use of a GPR119 agonist in the prevention or treatment of hypoglycemia is disclosed, addition, pharmaceutical compositions and combinations of a GPR1 19 agonist with insulin, insulin analog, insulin secretagogue or or other drug(s) that reduces plasma glucose levels to below 70 mg/dL described herein.
Type:
Application
Filed:
December 13, 2016
Publication date:
December 13, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
David E. Kelley, Ping Liu, Harold B. Wood, Scott D. Edmondson, Hideo Makimura, Xiaoyan Li, Timothy Joseph Kowalski
Abstract: The present invention is directed to pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Application
Filed:
June 6, 2018
Publication date:
December 13, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ashok ARASAPPAN, Jason M. COX, John S. DEBENHAM, Zhuyan GUO, Jiafang HE, Zahid HUSSAIN, Zhong LAI, Derun LI, Dongfang MENG, Subharekha RAGHAVAN, Sriram TYAGARAJAN
Abstract: In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are 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:
Application
Filed:
November 29, 2016
Publication date:
December 13, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Michael T. Rudd, David Jonathan Bennett, Jenny Wai, Zhaoyang Meng
Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
December 4, 2015
Date of Patent:
December 11, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Thomas H. Graham, Mark W. Embrey, Abbas Walji, Sherman T. Waddell
Abstract: The invention is directed to immobilized ketoreductases and methods of making and using them. Enzymes are protein molecules which serve to accelerate the chemical reactions of living cells (often by several orders of magnitude). Without enzymes, most biochemical reactions would be too slow to even carry out life processes. Enzymes display great specificity and are not permanently modified by their participation in reactions. Since they are not changed during the reactions, enzymes can be cost effectively used as catalysts for a desired chemical transformation.
Type:
Grant
Filed:
March 12, 2014
Date of Patent:
December 11, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Matthew D. Truppo, Hongmei Li, Johannah R. Moncecchi, Hallena Strotman
Abstract: The present invention is directed to pyrrolidine 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:
December 14, 2015
Date of Patent:
December 11, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Nigel Liverton, Yunfu Luo, Jason W. Skudlarek
Abstract: The present invention is directed to methods and compositions for the production of Fc-containing polypeptides having improved properties and comprising mutations at positions 243 and 264 of the Fc region.
Abstract: A system and method for presenting product-specific content on a client device, such as a smart cellphone, tablet, or laptop computer, based on a scanned DataMatrix barcode. A DataMatrix barcode is read by an optical scanner attached to the client device and an application recognizes and parses the data encoded in the DataMatrix barcode to obtain a unique alphanumeric identifier. The unique identifier is transmitted to a digital content server via a data communications network and used by the digital content server to retrieve product-specific content created and maintained on the digital content server by a content management system. The product-specific content, if found on the server, is transmitted to the client device and presented on an output device in accordance with a predefined presentation template.
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:
August 21, 2017
Date of Patent:
December 4, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dong-Ming Shen, Rongze Kuang, Puneet Kumar, Joseph L. Duffy, Cheng Zhu, Amjad Ali, Meng Yang, John S. Debenham
Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
Type:
Grant
Filed:
March 2, 2018
Date of Patent:
December 4, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Katherine Young, David B. Olsen, Sheo B. Singh, Jing Su, Robert R. Wilkening, James M. Apgar, Dongfang Meng, Dann Parker, Mihir Mandal, Lihu Yang, Ronald E. Painter, Qun Dang, Takao Suzuki
Abstract: The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
Type:
Application
Filed:
December 12, 2016
Publication date:
November 29, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Haifeng Tang, Weiguo Liu, Fa-Xiang Ding, Wanying Sun, Yi Zang, Weidong Pan, Anthony Ogawa, Linda Brockunier, Xianhai Huang, Hongwu Wang, Rudrajit Mal, Tesfaye Biftu, Min Park, Yan Guo, Jinlong Jiang, Helen Y. Chen, Christopher W. Plummer