Patents Assigned to Merck Sharp
  • Publication number: 20200031838
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Application
    Filed: October 1, 2019
    Publication date: January 30, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John Y.L. CHUNG, Kevin CAMPOS, Edward CLEATOR, Robert F. DUNN, Andrew GIBSON, R. Scott HOERRNER, Stephen KEEN, Dave LIEBERMAN, Zhuqing LIU, Joseph LYNCH, Kevin M. MALONEY, Feng XU, Nobuyoshi YASUDA, Naoki YOSHIKAWA, Yong-Li ZHONG
  • Patent number: 10544155
    Abstract: The present invention relates to spirocyclic quinolizine derivatives and pharmaceutically acceptable salts or prodrug thereof, compositions comprising at least one spirocyclic quinolizine derivative, and methods of using the spirocyclic quinolizine derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: January 28, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yonglian Zhang, Sherman T. Waddell, Tao Yu, John A. McCauley, Andrew Stamford
  • Patent number: 10543317
    Abstract: The present invention relates to a drug delivery device comprising a drug container having at least one bellow. The at least one bellow has a first surface and an opposing second surface. The first surface is comprised of a first Belleville spring and the opposing second surface is comprised of a second Belleville spring, wherein the second Belleville spring has a higher spring rate than the first Belleville spring.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: January 28, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter A. Basile, Steven Carl Persak, Mikhail Gotliboym
  • Patent number: 10544130
    Abstract: The present invention relates to metallo-?-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-?-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: Grant
    Filed: January 10, 2019
    Date of Patent: January 28, 2020
    Assignee: 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: 10546243
    Abstract: This disclosure relates to a method for estimating a particle size distribution (PSD) and a morphology for a set of particles. A computer system receives a plurality of chord length distributions (CLDs) of different types for a set of particles. The computer system then estimates a morphology for the set of particles based on the plurality of received CLDs. The computer system also identifies a plurality of descriptors of the plurality of CLDs for the set of particles based on the plurality of received CLDs. The computer system then estimates metrics for the PSD for the set of particles based on the plurality of identified CLD descriptors. Based on the estimated PSD metrics for the set of particles, the computer system generates an estimate of the PSD for the set of particles. Finally, the computer system outputs the estimated morphology and the estimated PSD for the set of particles.
    Type: Grant
    Filed: September 10, 2018
    Date of Patent: January 28, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Roberto Irizarry
  • Patent number: 10544222
    Abstract: The present invention provides multispecific molecules, e.g., comprising more than one ISVD or Nanobody, that bind to PD1 and CTLA4. These molecules have been engineered so as to reduce the incidence of binding by pre-existing antibodies in the bodies of a subject administered such a molecule. Methods for increasing immune response, treating cancer and/or treating an infectious disease with such molecules are provided.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: January 28, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Juha Punnonen, Edward Bowman, Maribel Beaumont, Marie-Ange Buyse, Carlo Boutton, Bruno Dombrecht, Bjorn Victor, David Vlerick, Robert A. Kastelein
  • Patent number: 10544147
    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: Grant
    Filed: March 24, 2017
    Date of Patent: January 28, 2020
    Assignee: 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
  • Patent number: 10538497
    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: Grant
    Filed: December 12, 2016
    Date of Patent: January 21, 2020
    Assignee: 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
  • Patent number: 10537589
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: January 21, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • Publication number: 20200017909
    Abstract: The present invention provides genetic markers on human chromosome 6 that are associated with a beneficial response to a treatment that targets Clostridium difficile (C. difficile) toxin B (TcdB), e.g. a TcdB antibody. These TcdB treatment response markers are useful, inter alia, to identify patients who are most likely to benefit from treatment with a treatment that 5 targets TcdB in methods of treating patients having a disease susceptible to treatment with a TcdB antibody, and in methods for selecting the most appropriate therapy for such patients. The invention also provides antibodies, drug products, and kits useful with the TcdB Treatment response markers of the invention.
    Type: Application
    Filed: December 7, 2017
    Publication date: January 16, 2020
    Applicants: Merck Sharp & Dohme Corp., Beijing Genomics Institute at Shenzhen
    Inventors: Peter M. Shaw, Devan V. Mehrotra, Rebecca L. Blanchard, Judong Shen, Robin Mogg, Mary Beth Dorr, Junhua Li, Xun Xu
  • Publication number: 20200017524
    Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, Y, Z, R1, R7A, R7B and R8 are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: December 1, 2017
    Publication date: January 16, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Tao Yu, Sherman T. Waddell, John A. McCauley
  • Patent number: 10532068
    Abstract: Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)a-(G)b; wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P)c-(L)d-(G)e; wherein P is a peptide and each occurrence of P is independently selected from Table 2; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: January 14, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Thomas J. Tucker, David M. Tellers, Boyoung Kim, Rob Burke, Kathleen B. Calati, Matthew G. Stanton, Rubina G. Parmar, Jeffrey G. Aaronson, Weimin Wang
  • Publication number: 20200010463
    Abstract: The present invention relates to oxazolidinone Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
    Type: Application
    Filed: March 15, 2018
    Publication date: January 9, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jing Su, Lihu Yang, Takao Suzuki
  • Publication number: 20200010449
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Application
    Filed: September 19, 2019
    Publication date: January 9, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul G. Bulger, Kevin M. Belyk, John Limanto, Guy R. Humphrey
  • Publication number: 20200010525
    Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed in the presence of a water miscible organic modifier and at an elevated temperature followed by reverse phase chromatography performed in the presence of a water miscible organic modifier and at an elevated temperature.
    Type: Application
    Filed: August 27, 2019
    Publication date: January 9, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, Michael P. Coleman, Shibu T. George, Michael A. Rauscher, Mark C. Sleevi, Kartoa Chow
  • Publication number: 20200009251
    Abstract: This disclosure provides pharmaceutical compositions comprising ceftolozane, pharmaceutical compositions comprising ceftolozane and tazobactam, methods of preparing those compositions, and related methods and uses of these compositions.
    Type: Application
    Filed: September 18, 2019
    Publication date: January 9, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph TERRACCIANO, Nicole Miller DAMOUR, Chun JIANG, Giovanni FOGLIATO, Giuseppe Alessandron DONADELLI, Dario RESEMINI
  • Patent number: 10526336
    Abstract: The present invention is directed to fused heteroaryl derivative 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 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: December 18, 2015
    Date of Patent: January 7, 2020
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Douglas C. Beshore, Na Meng, Yunfu Luo
  • Patent number: 10526363
    Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: January 7, 2020
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: John Simon Edwards, Peter Richard Mullens, Edward Cleator, Bryon L. Simmons, Courtney K. Maguire, Jeremy Peter Scott, Nobuyoshi Yasuda, Yong-Li Zhong, Lisa F. Frey, Peter G. Dormer, Andrew Brunskill, Artis Klapars, Pu Qian, Yi Zhang, Baoqiang Wan, Eric Ashley
  • Publication number: 20200002407
    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: Application
    Filed: June 7, 2019
    Publication date: January 2, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: KALPIT A. VORA, KARA S. COX, AIMIN TANG, ZHIFENG CHEN, DANIEL DISTEFANO, LAN ZHANG, HUA-POO SU
  • Patent number: 10519115
    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: November 10, 2014
    Date of Patent: December 31, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Purakkattle Biju, Steven L. Colletti, Qun Dang, Pawan Dhondi, Candido Gude, Hubert Josien, Nam Fung Kar, Anilkumar G. Nair, Ravi P. Nargund, De-Yi Yang, Cheng Zhu