Patents Assigned to Merck Sharp
  • Publication number: 20180258171
    Abstract: The present disclosure provides antibodies and antigen binding fragments thereof including, but not limited to, monoclonal antibodies that specifically bind to human programmed death ligand 2 (PD-L2). The invention further provides nucleic acids encoding the antibodies and antigen binding fragments of the invention and host cells transformed therewith. The antibodies and antigen binding proteins of the invention are useful in methods for the immunohistochemical detection of human PD-L2 expression in tissue samples.
    Type: Application
    Filed: September 20, 2016
    Publication date: September 13, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jennifer H. Yearley, Linda Liang, Michael Eric Bigler, Christopher John Gibson
  • Patent number: 10072025
    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: Grant
    Filed: October 21, 2015
    Date of Patent: September 11, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Scott, David Guerin, Danielle Molinari, Sam Kattar, Peter Fuller, Christopher Dinsmore, Norman Kong, Yunfeng Bai, Jianmin Fu, Yumei Liu, Zhixiang Zheng
  • Patent number: 10072072
    Abstract: The present invention relates to monoclonal antibodies which have high anti-RSV neutralizing titers. The invention further provides for isolated nucleic acids encoding the antibodies of the invention and host cells transformed therewith. The invention yet further provides for diagnostic, prophylactic and therapeutic methods employing the antibodies and nucleic acids of the invention, particularly as a passive immunotherapy agent in infants and the elderly.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: September 11, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • Publication number: 20180250232
    Abstract: A process for preparing spray dried solid dispersions of (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H4ndazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base and hypromellose acetate succinate for pharmaceutical preparations including pharmaceutical capsule preparations.
    Type: Application
    Filed: August 29, 2016
    Publication date: September 6, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yung-Chi Lee, Dan Zhang
  • Patent number: 10065967
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).
    Type: Grant
    Filed: July 21, 2017
    Date of Patent: September 4, 2018
    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
  • Patent number: 10065947
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: September 4, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • Patent number: 10065945
    Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: September 4, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Timothy A. Blizzard, Brian T. Campbell, Helen Y. Chen, John S. Debenham, Sunita V. Dewnani, Byron Dubois, Candido Gude, Zack Zhiqiang Guo, Bart Harper, Zhiyong Hu, Songnian Lin, Ping Liu, Ming Wang, Feroze Ujjainwalla, Jiayi Xu, Libo Xu, Rui Zhang
  • Publication number: 20180244744
    Abstract: A process for solubilization and refolding of precursor insulin or insulin analogs from inclusion body isolates for use in the production of insulin or insulin analog is described.
    Type: Application
    Filed: August 29, 2016
    Publication date: August 30, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, Rebecca A. Chmielowski, Mark C. Sleevi
  • Publication number: 20180244712
    Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
    Type: Application
    Filed: February 1, 2018
    Publication date: August 30, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Rui Liang, Jongwon Lim, Hong Liu, Min Lu, Alan B. Northrup, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Quang T. Truong, Shawn P. Walsh, Kake Zhao
  • Publication number: 20180244656
    Abstract: The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
    Type: Application
    Filed: June 24, 2016
    Publication date: August 30, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu
  • Patent number: 10059680
    Abstract: Thiadiazolyl-oximinoacetic acid derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds. Compound (1) (TATD) is commercially available (CAS No. 76028-96-1). It has now been discovered that the thiadiazolyl-oximinoacetic acid derivative compound (1) (TATD) can be prepared from dimethyl malonate (SM 1, CAS No. 108-59-8) according to methods described herein. The methods provide products having desirable purity.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas
  • Patent number: 10059705
    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.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Christopher F. Thompson, Danielle Falcone, Wei Deng, Luis Torres, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng, Mark E. Scott
  • Patent number: 10059667
    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: February 3, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Duane DeMong, Yan Guo, Zhiyong Hu, Michael Miller, Barbara Pio, Christopher W. Plummer, Dong Xiao, Cangming Yang
  • Patent number: 10058544
    Abstract: The invention includes a granular composition comprising the active ingredient (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (S)—N-(3-(6-isopro-poxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-di-hydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide Form 1 HCl, about 10-30% (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Deepak Bahl, Yung-Chi Lee, Alfred Lee, William Anthony Marinaro, Jr., Dan Zhang, Tao Feng
  • Publication number: 20180237422
    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: Application
    Filed: March 11, 2016
    Publication date: August 23, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Christopher J. Sinz, Alejandro Crespo, Johnathan E. Wilson, Troy McCraken, Shimin XU, Haitang Li
  • Publication number: 20180237524
    Abstract: Crystals of pembrolizumab and structurally similar anti-PD-1 monoclonal antibodies are provided, as well as methods of producing such crystals, and uses of compositions comprising such antibody crystals, e.g. in treatment of cancers. The present invention satisfies these needs and more by providing pembrolizumab crystals and a method producing pembrolizumab crystals. One embodiment of the method of the invention produces crystals suitable for X-ray diffraction, and the inventors herein used such crystals to solve the three-dimensional structure of pembrolizumab to 2.3 A resolution.
    Type: Application
    Filed: February 22, 2016
    Publication date: August 23, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Paul Reichert, Winifred W. Prosise, Giovanna Scapin, Xiaoyu Yang, Ramesh Kashi, Corey Strickland
  • Publication number: 20180237856
    Abstract: The present invention provides genetic markers on human chromosome 1 that are associated with a beneficial response to CRTH2 receptor antagonists. These CRTH2 receptor antagonist response markers are useful, inter alia, to identify patients who are most likely to benefit from treatment with CRTH2 receptor antagonist compositions and drug products, in methods of treating patients having a disease susceptible to treatment with a CRTH2 receptor antagonist, and in methods for selecting the most appropriate therapy for such patients.
    Type: Application
    Filed: July 21, 2016
    Publication date: August 23, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Gregory J. Opiteck, Peggy H. Wong, Joshua McElwee, Devan V. Mehrotra, Steven Greenberg, Zifang Guo
  • Publication number: 20180237469
    Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
    Type: Application
    Filed: February 1, 2018
    Publication date: August 23, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Rui Liang, Jongwon Lim, Hong Liu, Min Lu, Alan B. Northrup, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Quang T. Truong, Shawn P. Walsh, Kake Zhao
  • Patent number: 10053466
    Abstract: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of: ?and reductive amination of:
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: August 21, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Feng Peng, Yonggang Chen, Amude Mahmoud Kassim, Cheng-yi Chen, Mathew Maust, Mark McLaughlin, Michael J. Zacuto, Qinghao Chen, Lushi Tan, Zhiguo Jake Song, Yang Cao, Feng Xu
  • Patent number: 10053515
    Abstract: Antibodies that bind the apple 2 domain of human coagulation Factor XI and inhibit activation of FXI by coagulation factor XIIa are described.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: August 21, 2018
    Assignees: Merck Sharp & Dohme Corp., Adimab LLC
    Inventors: Zhu Chen, Kenneth P. Ellsworth, James A. Milligan, Elizabeth Oldham, Dietmar Seiffert, Vaishnavi Ganti, Mohammad Tabrizifard, Bianka Prinz