Patents Assigned to Merck Sharp
  • C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170246300
    Abstract: In its many embodiments, the present invention provides certain C5-C6 fused tricyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R2, R3, RA, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: September 28, 2015
    Publication date: August 31, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Jared N. Cumming, Jack D. Scott
  • DIAZINE-FUSED AMIDINES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170247377
    Abstract: In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: September 14, 2015
    Publication date: August 31, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shuwen He, Jared N. Cumming, Andrew W. Stamford
  • INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20170247388
    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: Application
    Filed: September 25, 2015
    Publication date: August 31, 2017
    Applicant: 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
  • Process for Making Nucleoside Phosphoramidate Compounds
    Publication number: 20170246198
    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).
    Type: Application
    Filed: October 20, 2015
    Publication date: August 31, 2017
    Applicants: IDENIX Pharmaceuticals LLC, Merck Sharp & Dohme Corp.
    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
  • METHOD FOR SCREENING DRUG-SACCHARIDE CONJUGATES
    Publication number: 20170248580
    Abstract: Methods for identifying drug-saccharide conjugates that bind the mannose receptor, C type 1, (MRC1) and may be taken up by cells expressing MRC1, and the use of such drug-saccharide conjugates for treatment of particular diseases are described. In particular, the methods for identifying insulin-saccharide conjugates that bind the MRC1 receptor and may be taken up by cells expressing the MRC1 and use of such conjugates for treatment of diabetes are described.
    Type: Application
    Filed: May 15, 2017
    Publication date: August 31, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yingjun Mu, Ruojing Yang, Xinghai Li, Margaret Wu, Qing Dallas-yang, Yuli Chen, Ge Dai, Songnian Lin, David E. Kelley, Mark Erion
  • SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170247336
    Abstract: The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: October 8, 2015
    Publication date: August 31, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: FEZ UJJAINWALLA, JOHN QIANG TAN, QUN DANG, CHRISTOPHER J. SINZ, ALEJANDRO CRESPO, MING WANG, YILI CHEN, JIAQIANG CAI, FAN WU, XIAOXING DU
  • 4-heteroaryl substituted benzoic acid compounds as RORgammaT inhibitors and uses thereof
    Patent number: 9745265
    Abstract: The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: August 29, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth J. Barr, Corey E. Bienstock, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Dongshan Zhang, Neville J. Anthony, Blair T. Lapointe, Yuan Tian
  • Indoline compounds as aldosterone synthase inhibitors
    Patent number: 9745282
    Abstract: This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: August 29, 2017
    Assignees: Merck Sharp & Dohme Corp, ElexoPharm GmbH
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lina Yin, Rolf Hartmann, Qingzhong Hu, Ralf Heim, Christina Zimmer
  • 2-pyridyloxy-4-ether orexin receptor antagonists
    Patent number: 9745284
    Abstract: The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether 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 pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: August 29, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
    Patent number: 9745295
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: August 29, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Neville J. Anthony, Brian M. Andresen, Alan B. Northrup, Kaleen K. Childers, Anthony Donofrio, Thomas A. Miller, Yuan Liu, Michelle R. Machacek, Hyun Chong Woo, Kerrie B. Spencer, John Michael Ellis, Michael D. Altman, Eric T. Romeo, Daniel Guay, Jonathan Grimm, Marie-Eve Lebrun, Joel S. Robichaud, Liping Wang, Byron DuBois, Qiaolin Deng
  • Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use
    Patent number: 9745324
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: August 29, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Jared N. Cumming, Jack D. Scott, Hong Liu, Anandan Palani
  • Compounds that are ERK inhibitors
    Patent number: 9745307
    Abstract: Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: August 29, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson
  • ETHYL N-BOC PIPERIDINYL PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
    Publication number: 20170240567
    Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: October 21, 2015
    Publication date: August 24, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Scott, David Guerin, Danielle Molinari, Sam Kattar, Peter Fuller, Christopher Dinsmore, Normon Kong, Yunfeng Bai, Jianmin FU, Yumei Liu, Zhixiang Zheng
  • Preparation and Use of Cyclic Sulfonamide Derivatives as PAR-1 Receptor Antagonists
    Publication number: 20170240539
    Abstract: The present invention relates to cyclic sulfonamide derivatives of Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 9, 2015
    Publication date: August 24, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Andrew W. Stamford, Zhi-Qiang Yang, Milana Maletic, Senlin Cai, Xiaobang Duan, Jianhua Cao
  • INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170240555
    Abstract: The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: September 23, 2015
    Publication date: August 24, 2017
    Applicants: MERCK SHARP & DOHME CORP., MSD R&D (CHINA) CO., LTD.
    Inventors: JIAQIANG CAI, VINCENT COLANDREA, ALEJANDRO CRESPO, JOHN DEBENHAM, XIAOXING DU, DEODIALSINGH GUIADEEN, PING LIU, RONGQIANG LIU, CHRISTINA B. MADSEN-DUGGAN, JOSHUA G. MCCOY, WEIGUO QUAN, CHRISTOPHER SINZ, LIPING WANG
  • FACTOR XIa INHIBITORS
    Publication number: 20170240523
    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, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: July 23, 2015
    Publication date: August 24, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D Edmondson, Zhuyan Guo, Alan Hruza, Sung-Sau So, Wanying Sun, Amjad All, Rongze Kuang, Ying-Duo Gao, Anthony K Ogawa
  • Factor XIa Inhibitors
    Publication number: 20170240524
    Abstract: The present invention provides a compound of Formula (I) (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: Application
    Filed: July 23, 2015
    Publication date: August 24, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Scott D. Edmondson, Alan Hruza, Jiafang He, Sung-Sau So, Amjad Ali, Ying-Duo Gao
  • SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170240513
    Abstract: The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: October 8, 2015
    Publication date: August 24, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: FEZ UJJAINWALLA, JOHN QIANG TAN, QUN DANG, CHRISTOPHER J. SINZ, MING WANG, YILI CHEN, JIAQIANG CAI
  • SUBSTITUTED PYRIDINE INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170240511
    Abstract: The present invention concerns compounds of formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: October 8, 2015
    Publication date: August 24, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: FEZ UJJAINWALLA, JOHN QIANG TAN, QUN DANG, CHRISTOPHER J. SINZ, MING WANG, JIAQIANG CAI, XIAOXING DU, YILI CHEN
  • HIV protease inhibitors
    Patent number: 9737545
    Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, 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. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: August 22, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Helen Juteau, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Christian Nadeau, Daniel Simard, Satyanarayana Tummanapalli, Vouy Linh Truong, Karine M. Villeneuve, Peter D. Williams