Abstract: Described herein are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, W, X, Y, Z, m, n and p are as defined herein. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
Type:
Grant
Filed:
October 25, 2022
Date of Patent:
December 31, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Abdelghani Abe Achab, Zachary G. Brill, Jenny Lorena Rico Duque, Xavier Fradera, Joey L. Methot, Phieng Siliphaivanh, Jing Su, Brandon A. Vara, Erin F. DiMauro
Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
Type:
Grant
Filed:
April 29, 2024
Date of Patent:
December 31, 2024
Assignee:
MERCK SHARP & DOHME LLC
Inventors:
Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
Abstract: An insulin conjugate comprising or consisting of a tetra-valent sugar cluster is described. The tetra-valent sugar cluster is provided by tetra-dentate linker having four arms, wherein each arm of the tetra-dentate linker is independently covalently linked to a ligand comprising or consisting of a saccharide, such as a monosaccharide, disaccharide, trisaccharide, tetrasaccharide, or branched trisaccharide. In particular aspects, the insulin conjugate displays a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose.
Type:
Application
Filed:
November 16, 2022
Publication date:
December 26, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Pei Huo, Songnian Lin, Christopher R. Moyes, Dmitri A. Pissarnitski, Zhiqiang Zhao, David N. Hunter, Yuping Zhu
Abstract: In some examples, a vial-to-syringe converter includes a plunger rod, an adapter including a body having a piercing spike, a receiver and a lumen extending between the spike and the receiver, the body further including at least one laterally-extending flange, and a needle in communication with the receiver and configured to deliver a medicament to a patient's body.
Type:
Application
Filed:
November 1, 2022
Publication date:
December 26, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Daniel A. Bonanno, Eduardo Cristofolli, Cassie Megna, Wail A. Rasheed, Ophelia L. Wells
Abstract: Described herein are compounds of Formula I; and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, m, n, and p are as defined herein. The compounds of Formula I, and pharmaceutically acceptable salts thereof, act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
Type:
Application
Filed:
October 24, 2022
Publication date:
December 26, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Abdelghani Abe Achab, Jenny Lorena Rico Duque, Xavier Fradera, Joey L. Methot, Phieng Siliphaivanh, Brandon A. Vara, Hongjun Zhang
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:
Application
Filed:
September 6, 2024
Publication date:
December 26, 2024
Applicant:
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 method or system for training a convolutional neural network (CNN) for medical imaging analysis. The system pre-trains the CNN's encoder using a dataset of unlabeled 3D medical images. Each 3D image includes an annotated slice delineating a boundary of a lesion and multiple non-annotated 2D slices above and below the annotated slice. The system then fine-tunes the pre-trained encoder using an annotated 2D image dataset. The annotated 2D image dataset includes multiple 2D slices of lesions, each including an annotation that delineates a boundary of a corresponding lesion.
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:
April 8, 2022
Date of Patent:
December 24, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
Abstract: The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 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 cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
Type:
Grant
Filed:
August 5, 2019
Date of Patent:
December 24, 2024
Assignees:
Merck Sharp & Dohme LLC, MSD International GmbH
Inventors:
Michelle Machacek, David Witter, Craig Gibeau, Chunhui Huang, Shuhei Kawamura, David L. Sloman, Phieng Siliphaivanh, Ryan Quiroz, Murray Wan, Sebastian Schneider, Charles S. Yeung, Michael H. Reutershan, Timothy J. Henderson, Jean-Laurent Paparin, Houcine Rahali, Jonathan M. E. Hughes, Sulagna Sanyal, Yingchun Ye, David A. Candito, Patrick S. Fier, Steven M. Silverman
Abstract: Methods of treatment of colorectal cancer can include the administration of the anti-alpha-v integrin (receptor) antibody Abituzumab. Preferably, the methods of treating colorectal cancer can include treating Stage II-IV colorectal cancer, metastatic colorectal cancer, left-sided colorectal cancer and/or left-sided metastatic colorectal cancer, involving the administration of said Abituzumab to patients in need thereof. Abituzumab is also useful for the manufacture of a medicament for treating colorectal cancer, preferably colorectal cancer as defined herein. Abituzumab is further useful for the manufacture of a medicament for treating colorectal cancer in combination with suitable targeted therapy concepts, such as growth factor or growth factor receptor targeting monoclonal antibodies, and/or chemotherapy.
Type:
Grant
Filed:
October 18, 2019
Date of Patent:
December 24, 2024
Assignee:
Merck Patent GmbH
Inventors:
Giorgio Massimini, Ilhan Celik, Josef Straub, Rolf Bruns, Rita Laeufle
Abstract: The invention relates to compounds that can be used in an organic electronic device as an active compound, in particular for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention, and to electronic devices comprising same.
Abstract: A pigment mixture comprising at least two or three interference pigments of different interference colours selected from the colours red, green and blue, suitable for use in paints, coatings, printing inks, security printing inks, plastics, ceramic materials, glasses and in the preparation of pigment preparations, dry preparations and in particular cosmetic formulations.
Type:
Grant
Filed:
January 23, 2019
Date of Patent:
December 24, 2024
Assignee:
MERCK PATENT GMBH
Inventors:
Christoph Schmidt, Carsten Plueg, Uwe Lenz, Sabine Schoen
Abstract: In some examples, an injector includes a base, a housing movable relative to the base, a needle unit disposed within the base, the needle unit comprising at least one piercing needle configured to pierce a pierceable membrane of a drug product container, and at least one microneedle disposed on an opposite side of the at least one piercing needle, and a driving mechanism configured and arranged to drive at least one of the drug product container and the needle unit toward another of the drug product container and the needle unit.
Type:
Application
Filed:
November 1, 2022
Publication date:
December 19, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Daniel A. Bonanno, John B. Cline, Eduardo Cristofolli, Cassie Megna, Wail A. Rasheed, Ophelia L. Wells
Abstract: The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.
Type:
Grant
Filed:
May 13, 2024
Date of Patent:
December 17, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Mary Ann Johnson, Leonardo Resende Allain, W. Mark Eickhoff, Craig B. Ikeda, Chad D. Brown, Francis J. Flanagan, Jr., Rebecca Nofsinger, Melanie J. Marota, Lisa Lupton, Paresh B. Patel, Hanmi Xi, Wei Xu
Abstract: The present invention relates to a method for preparing an optical metal oxide layer, to a formulation for preparing an optical metal oxide layer and to an optical device comprising an optical metal oxide layer. The optical metal oxide layers are particularly suitable for optical applications and may be used in optical devices such as, for example, in diffractive gratings for augmented reality (AR) and/or virtual reality (VR) devices.
Type:
Application
Filed:
October 4, 2022
Publication date:
December 12, 2024
Applicant:
MERCK PATENT GMBH
Inventors:
Oliver DOLL, Hagai ARBELL, Henning SEIM, Oleg CHASHCHIKHIN
Abstract: The present invention relates to a pharmaceutical formulation of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol or pharmaceutically acceptable salt thereof, as well as a method of making same, as well as medical uses thereof.
Type:
Application
Filed:
August 21, 2024
Publication date:
December 12, 2024
Applicant:
Merck Patent GmbH
Inventors:
Simon Geissler, Martina Jeschke, Patrizia Boniforte, Markus Weigandt
Abstract: The present disclosure is directed to benzoxazinone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naive cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
Type:
Application
Filed:
October 10, 2022
Publication date:
December 12, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Abdellatif El Marrouni, Antonella Converso, Ashley Forster
Abstract: The present disclosure provides, among other things, a vaccine composition that includes a squalene nanoemulsion (SNE) adjuvant and HPV virus-like particles (VLPs) of at least one type of human papillomavirus (HPV) selected from the group consisting of HPV types: 6, 11, 16, 18, 26, 31, 33, 35, 39, 45, 51, 52, 53, 55, 56, 58, 59, 66, 68, 73, and 82.
Type:
Application
Filed:
June 6, 2024
Publication date:
December 12, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Patrick L. Ahl, William J. Smith, Randal J. Soukup, Nicole Lea Sullivan, John Gaspar, Julie M. Skinner
Abstract: The present invention relates to purified antibody and antigen-binding fragment compositions that lack sulfated tyrosine on one or more tyrosine residues in the immunoglobulin chains. Purification methods for removing sulfated tyrosine variants from antibody and antigen-binding fragment compositions are also provided.
Abstract: A liquid-crystal (LC) medium based on a mixture of polar compounds, its use for optical, electro-optical and electronic purposes, in particular in LC displays, especially in LC displays of the vertically aligned mode, to an LC display of the vertically aligned mode containing the LC medium, especially an energy-saving LC display and a process of manufacturing the LC display.
Type:
Grant
Filed:
June 1, 2023
Date of Patent:
December 10, 2024
Assignee:
MERCK PATENT GMBH
Inventors:
Harald Hirschmann, Sabine Schoen, Philipp Wucher