Patents Assigned to Merck Sharp
  • Stable formulations of antibodies to human programmed death receptor PD-1 and related treatments
    Patent number: 9220776
    Abstract: The present invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. The present invention further provides methods for treating various cancers and chronic infections with stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: December 29, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Manoj K. Sharma, Chakravarthy Nachu Narasimhan, Kevin James Gergich, Soonmo Peter Kang
  • Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
    Patent number: 9221809
    Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: December 29, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. McElroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Craig R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
  • Factor IXa Inhibitors
    Publication number: 20150368269
    Abstract: The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, 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.
    Type: Application
    Filed: December 16, 2013
    Publication date: December 24, 2015
    Applicants: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Cameron James Smith, Edward Sherer, Louis-Charles Campeau, James Balkovec, William John Greenlee, Derun Li, Liangqin Guo, Tin-Yau Chan, Yi-Heng Chen, Yili Chen, Samuel Chackalamannil, John Qiang Tan, Tomokazu Hirabayashi, Mika Sekioka
  • 2,6,7 SUBSTITUTED PURINES AS HDM2 INHIBITORS
    Publication number: 20150368247
    Abstract: The present invention provides 2,6,7 substituted purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: February 4, 2014
    Publication date: December 24, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Liping Yang
  • MDL-1 LIGAND
    Publication number: 20150368344
    Abstract: The invention provides methods for modulation interactions between MDL-1 and its binding partner, Gal9. Also provided are methods to screen for modulators of MDL-1/Gal9 interaction.
    Type: Application
    Filed: June 19, 2015
    Publication date: December 24, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Barbara Joyce-Shaikh, Douglas C. Wilson, Daniel J. Cua, Drake M. LaFace, Maribel Beaumont, Holly Cherwinski, Mark Hsieh, Sabrina Benchaar, Joseph H. Phillips
  • TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C
    Publication number: 20150368246
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase 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: February 3, 2014
    Publication date: December 24, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Zhong Lai, Ravi Nargund, Karen Marcantonio, Dong Xiao, Linda L. Brockunier, Nicolas Zorn, Qun Dang, Xuanjia Peng, Peng Li
  • 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
    Patent number: 9216173
    Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B 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) kinase.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: December 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
  • TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C
    Publication number: 20150361101
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase 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: February 3, 2014
    Publication date: December 17, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Linda L. Brockunier, Ravi Nargund, Karen Marcantonio, Nicolas Zorn, Dong Xiao, Xuanjia Peng, Peng Li, Tao Guo
  • HETEROBICYCLO-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
    Publication number: 20150361098
    Abstract: Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Application
    Filed: December 20, 2013
    Publication date: December 17, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Xianhai Huang, Timothy J. Henderson, Jae-Hun Kim, Christopher Boyce, Pauline Ting, Junying Zheng, Edward Metzger, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Qiaolin Deng
  • THIAZOLE-SUBSTITUTED AMINOPYRIDINES AS SPLEEN TYROSINE KINASE INHIBITORS
    Publication number: 20150353535
    Abstract: The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript t 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: Application
    Filed: December 19, 2013
    Publication date: December 10, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Andrew M. Haidle, Yuan Liu, Alan B. Northrup, Brendan O'Boyle, Ryan D. Otte, Michael H. Reutershan, Dilrukshi Vitharana, Hyun Chong Woo
  • 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS
    Publication number: 20150353553
    Abstract: The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: January 29, 2014
    Publication date: December 10, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Carolyn Michele Cammarano, Matthew P. Christopher, Christopher Dinsmore, Ronald J. Doll, Francesc Xavier Fradera Llinas, Chaomin Li, Michelle Machacek, Michelle Martinez, Latha G. Nair, Weidong Pan, Michael Hale Reutershan, Manami Shizuka, Dietrich P. Steinhuebel, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Yaolin Wang, Liping Yang, Stephane L. Bogen, Matthew E. Voss, Jagannath Panda, Anthappan Tony Kurissery
  • BTK INHIBITORS
    Publication number: 20150353565
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Application
    Filed: January 17, 2014
    Publication date: December 10, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: RONALD M. KIM, JIAN LIU, HAO WU, SHILAN LIU, CHUNDAO YANG, SHULING ZHENG
  • SUBSTITUTED ISOQUINOLINES AS CRTH2 RECEPTOR MODULATORS
    Publication number: 20150353498
    Abstract: The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: September 26, 2013
    Publication date: December 10, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xianhai Huang, Anandan Palani, Ashwin U. Rao, Hongjun Zhang, Wei Zhou
  • BTK INHIBITORS
    Publication number: 20150353570
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Application
    Filed: January 22, 2014
    Publication date: December 10, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: RONALD M. KIM, JIAN LIU, XIAOLEI GAO, SOBHANA BABU BOGA, DEODIALSINGH GUIADEEN, JOSEPH A. KOZLOWSKI, WENSHENG WU, RAJAN ANAND, YOUNONG YU, OLEG B. SELYUTIN, YING-DUO GAO, HAO WU, SHILAN LIU, CHUNDAO YANG, HONGJIAN WANG
  • Anilinopiperazine derivatives and methods of use thereof
    Patent number: 9206142
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory S. Poker, Timothy J. Guzi
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9206198
    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 conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
  • N-linked lactam M1 receptor positive allosteric mogulators
    Patent number: 9206200
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9206199
    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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
  • C2,C6 OXACYCLIC-FUSED THIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20150344500
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, 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: December 16, 2013
    Publication date: December 3, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Wen-Lian Wu, Duane A. Burnett
  • MEDICATION INJECTOR WITH NEAR-EMPTY ALERT
    Publication number: 20150343157
    Abstract: A medication injector that has an alert indicator that alerts the user when the medication injector is approaching near the end of its medication supply is disclosed. The alert indicator gives the user an opportunity to make preparations to obtain additional medication for the injector if there is an insufficient amount of medication in the injector to enable the user to dispense the required dosage amount with the next injection. Initially, the alert indicator is not visible to the user, but becomes visible to the user when the injector is near empty.
    Type: Application
    Filed: December 5, 2013
    Publication date: December 3, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Peter A. Basile, Jeffrey C. Givan, Steven Carl Persak