Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, A, and B are as defined herein. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.
Type:
Application
Filed:
March 27, 2024
Publication date:
October 10, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
David A. Candito, Anthony Donofrio, Ronald Dale Ferguson, II, George Madalin Giambasu, Anmol Gulati, Andrew M. Haidle, Brett A. Hopkins, William P. Kaplan, Ping Liu, Michaelyn C. Lux, Xiao Mei Zheng, Ryan D. Otte, Alexander Pasternak, Elsie C. Yu
Abstract: The invention provides compositions of anti-PD-1 antibodies or antigen-binding fragments thereof with less than or equal to about 3.0% oxidation of Met105 in the CDRH3 heavy chain region, and methods of obtaining the purified compositions. The invention also provides compositions comprising anti-PD-1 antibody main species and acidic species thereof, wherein the amount of acidic species is about 1.0-12.0%.
Type:
Grant
Filed:
January 27, 2022
Date of Patent:
October 8, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Mark A. Brower, Chung-Jr Huang, Brian Wai Kwan, William Nicholas Napoli, Bhumit A. Patel, Nuno J. Dos Santos Pinto, Douglas Dennis Richardson, II, Sen Xu
Abstract: A microinjection system and apparatus comprising stationary trough chips having wells and troughs to allow for efficient organoid microinjections are described.
Type:
Application
Filed:
September 7, 2022
Publication date:
October 3, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Jason A. Cassaday, Erik C. Hett, Stephen H. Kasper, Linda Adelle Lieberman, Sina Mohammadi, Carolina D. Morell-Perez, Clifford Sampson, Brian Andrews Squadroni
Abstract: Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
Type:
Application
Filed:
May 23, 2024
Publication date:
October 3, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Yeon-Hee Lim, Jianming Bao, James P. Roane
Abstract: The present invention relates to anti-human metapneumovirus (hMPV) antibodies, as well as use of such antibodies in the treatment of viral infections. The invention also includes antigenic hMPV proteins and immunogenic compositions comprising such antigenic hMPV proteins, and the use of such antigenic hMPV proteins and related compositions for preventing or treating viral infection in a subject.
Type:
Application
Filed:
February 8, 2022
Publication date:
October 3, 2024
Applicant:
MERCK SHARP & DOHME LLC
Inventors:
Zhifeng CHEN, Kara S. COX, Arthur FRIDMAN, Jennifer Dawn GALLI, Hua-Poo SU, Aimin TANG, Kalpit VORA, Zhiyun WEN, Xiao XIAO, Lan ZHANG
Abstract: The present disclosure provides a method of treating cancer or von Hippel-Lindau (VHL) disease with a safe and effective therapeutic dose of belzutifan in a patient in need thereof, comprising: (i) determining the belzutifan metabolic status (BMS) of the patient to determine whether the patient has a low metabolizer status, medium metabolizer status, or fast metabolizer status and (ii) (a) if the patient has the medium or fast metabolizer status, administering belzutifan to the patient at a standard therapeutic dose of 120 mg: or (ii) (b) if the patient has the low metabolizer status, administering belzutifan, to the patient at a therapeutic dose below that of the standard therapeutic dosc.
Type:
Application
Filed:
August 8, 2022
Publication date:
October 3, 2024
Applicant:
MERCK SHARP & DOHME LLC
Inventors:
Thomas J. BATEMAN, Aparna CHHIBBER, Eunkyung KAUH, Dhananjay Devidas MARATHE, Peter M. SHAW, Rachel MARCEAU WEST
Abstract: The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAG3 as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the antibodies and fragments (e.g., including anti-PD1 antibodies) are included in the invention. Methods for treating or preventing cancer or infection using such compositions are also provided. In addition, methods for recombinant expression of the antibodies and fragments are part of the present invention.
Type:
Grant
Filed:
February 11, 2022
Date of Patent:
October 1, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Linda Liang, Laurence Fayadat-Dilman, Rene De Waal Malefyt, Gopalan Raghunathan
Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
Type:
Grant
Filed:
May 15, 2020
Date of Patent:
October 1, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi
Abstract: The invention relates to compounds which are suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds.
Type:
Grant
Filed:
August 31, 2020
Date of Patent:
October 1, 2024
Assignee:
Merck KGaA
Inventors:
Amir Parham, Philipp Stoessel, Christian Ehrenreich
Abstract: A liquid-crystal (LC) material having negative dielectric anisotropy and the use thereof for optical, electro-optical and electronic purposes, such as for example in LC displays, in particular energy saving displays based on the ECB, IPS or FFS effect, where the liquid crystal medium contains one or more compounds of formula I and one or more compounds compounds of formulae IIA, IIB, IIC and IID
Type:
Grant
Filed:
June 22, 2023
Date of Patent:
October 1, 2024
Assignee:
MERCK PATENT GMBH
Inventors:
Chi-Shun Huang, Sven Christian Laut, Hee-Kyu Lee, Minghui Yang, Harald Hirschmann, Kuang-Ting Chou, Shih-Chieh Hung, Alexander Hahn, Philipp Wucher
Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
Type:
Grant
Filed:
January 25, 2022
Date of Patent:
October 1, 2024
Assignee:
MERCK & CIE
Inventors:
Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
Abstract: This disclosure relates to methods for treating solid tumors in a patient identified as having metastatic triple negative breast cancer, glioblastoma, metastatic pancreatic ductal adenocarcinoma, metastatic soft tissue sarcoma, or metastatic non-squamous non-small cell lung carcinoma, comprising administering an anti-ILT3 antigen binding protein, or antigen binding fragment, and an anti-PD1 antigen binding protein, or antigen binding fragment, to the patient every three weeks (Q3W).
Type:
Application
Filed:
March 17, 2022
Publication date:
September 26, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Philip E. Brandish, Mei Chen, Andrey Loboda, Michael Nebozhyn, III, Cai Wu, Daping Zhang, Jie Zhang-Hoover
Abstract: Tricyclic heterocycles are disclosed. These heterocyclic compounds are useful as TEAD binders and/or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases, in particular cancer.
Type:
Application
Filed:
May 5, 2021
Publication date:
September 26, 2024
Applicants:
Merck Patent GmbH, Cancer Research Technology Ltd.
Inventors:
Timo HEINRICH, Sarah Schlesiger, Jakub Gunera, Emma Carswell, Lisa Koetzner, Andreas Blum
Abstract: The invention is related to multivalent immunogenic compositions comprising more than one S. pneumoniae polysaccharide protein conjugates, wherein each of the conjugates comprises a polysaccharide from an S. pneumoniae serotype conjugated to a carrier protein, wherein the serotypes of S. pneumoniae are as defined herein. Also provided are methods for inducing a protective immune response in a human patient comprising administering the multivalent immunogenic compositions of the invention to the patient. The multivalent immunogenic compositions are useful for providing protection against S. pneumoniae infection and diseases caused by S. pneumoniae. The compositions of the invention are also useful as part of treatment regimes that provide complementary protection for patients that have been vaccinated with a multivalent vaccine indicated for the prevention of pneumococcal disease.
Type:
Grant
Filed:
November 9, 2023
Date of Patent:
September 24, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
William J. Smith, Patrick McHugh, Michael Albert Winters, Julie M. Skinner, Jian He, Luwy Musey, Chitrananda Abeygunawardana, Yadong Adam Cui, Michael J. Kosinski
Abstract: The disclosed subject matter relates to a rinse and methods of use thereof for removing an edge protection layer and residual hardmask components (e.g., metals) from the edge and at least one proximate surface of a wafer/substrate where the rinse includes acetic acid and/or a halogenated acetic acid of structure (A) wherein R1 and R2 are independently hydrogen or a halogen and R3 is a halogen and (ii) a compound having structure (B) wherein each of Ra, Rb, Rc, Rd, Re, Rf, Rg and Rh may independently be hydrogen, a substituted or an unsubstituted alkyl group, a substituted or an unsubstituted halogenated alkyl group, a substituted or an unsubstituted alkyl carbonyl group, a halogen, and a hydroxy group.
Type:
Grant
Filed:
July 6, 2020
Date of Patent:
September 24, 2024
Assignee:
Merck Patent GmbH
Inventors:
M. Dalil Rahman, Salem Mullen, JoonYeon Cho
Abstract: The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Type:
Application
Filed:
March 14, 2022
Publication date:
September 19, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Kaleen Konrad Childers, J. Michael Ellis, Peter H. Fuller, Anmol Gulati, Hakan Gunaydin, Solomon D. Kattar, Ravi Kurukulasuriya, Joey L. Methot, Gregori J. Morriello, Santhosh Neelamkavil, Blair T. Lapointe, Vladimir Simov, Charles S. Yeung
Abstract: Provided herein are IL-2 muteins that bind to the IL-2 receptor ? subunit but do not have measurable binding to the IL-2 receptor a subunit. Also provided are compositions, kits, methods, and uses involving such IL-2 muteins.
Type:
Application
Filed:
July 21, 2022
Publication date:
September 19, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Juan C. Alvarez, Alan C. Cheng, Ghassan N. Fayad, Brian E. Hall, Veronica M. Juan, Peter S. Kim, Sheila H. Ranganath, Venkataraman Sriraman, Gary C. Starling, Nicole C. Walsh
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:
October 28, 2019
Date of Patent:
September 17, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Dane Clausen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Guoqing Li, Theodore A. Martinot, Alexander Pasternak, David Sloman, Li Xiao, Wensheng Yu, Rui Zhang
Abstract: The present invention relates to an enzymatic synthesis of 4?-ethynyl-2?-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
Type:
Application
Filed:
May 28, 2024
Publication date:
September 12, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Mark A. Huffman, Anna Fryszkowska, Joshua N. Kolev, Paul N. Devine, Kevin R. Campos, Matthew Truppo, Christopher C. Nawrat
Abstract: Therapeutic combinations of immunoconjugates that bind to FOLR1 (e.g., IMGN853) with anti-PD-1 antibodies or antigen-binding fragments thereof (e.g., pembrolizumab) are provided. Methods of administering the combinations to treat cancers, e.g., ovarian, peritoneal, or fallopian tube cancers, with greater clinical efficacy and/or decreased toxicity are also provided.