Abstract: The present invention relates to novel 5-azaindazole derivatives of formula (I), as described and defined herein, and pharmaceutically acceptable salts, solvates and prodrug thereof, as well as pharmaceutical compositions comprising such compounds. The 5-azaindazole derivatives according to the invention have been found to be highly effective dual A2A/A2B adenosine receptor antagonists, and can thus be used as therapeutic agents, particularly in the treatment or prevention of hyperproliferative or infectious diseases or disorders.
Type:
Application
Filed:
October 24, 2024
Publication date:
February 13, 2025
Applicant:
MERCK PATENT GMBH
Inventors:
Anne-Laure BLAYO, Baptiste MANTEAU, Camille AMALRIC, Stanislas MAYER, Stephan SCHANN, Mickaƫl FER
Abstract: Monovalent IL-12 heterodimeric Fc proteins that display attenuated potency at the IL-12 receptor compared to wild-type IL-12 and have an extended half-life compared to wild-type IL-12 are described. The monovalent heterodimeric IL-12 heterodimeric Fc proteins comprise a heterodimer comprising an IL-12p35 subunit first Fc domain fusion protein and an IL-p40 subunit second Fc domain fusion protein IL-12 and Fc domains wherein the first and second Fc domains comprise modifications that facilitate heterodimerization of the first Fc domain to the second Fc domain.
Type:
Application
Filed:
August 8, 2024
Publication date:
February 13, 2025
Applicant:
MERCK SHARP & DOHME LLC
Inventors:
Mehabaw Getahun Derebe, Ghassan N. Fayad, Veronica M. Juan, Mike Lee, Ji Hea Park, Piyali Saha, Fan Zhang
Abstract: Provided are novel Pyrazolopyrimidine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are as defined herein. Also provided are compositions comprising at least one Pyrazolopyrimidine Derivative, and methods of using the Pyrazolopyrimidine Derivatives for treating or preventing a herpesvirus infection in a patient.
Type:
Application
Filed:
December 13, 2022
Publication date:
February 13, 2025
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Kira A. Armacost, Andrew J. Cooke, Christopher Douglas Cox, Brendan M. Crowley, Marc A. Labroli, Michael A. Plotkin, Izzat T. Raheem, Kelly-Ann S. Schlegel, Anthony W. Shaw, David M. Tellers
Abstract: A silicon precursor compound according to Formula I as described herein is used to form a silicon-containing thin film having excellent quality. A preparation method therefor, and a silicon-containing thin film preparation method using the silicon precursor compound are also described.
Abstract: A semiconducting light emitting nanoparticle is described having a core and shell structure. The particle has a core and an outer layer or shell. The outer layer covers at least part of the core and contains a metal cation and a divalent anion. Additionally, one or more organic moieties are directly attached to the anion of the outer layer by covalent bond. The divalent anion is Se2?, S2?, Te2?, O2? or a combination thereof. The metal cation can be a monovalent, cation, trivalent, or tetravalent cation. Also, a process for synthesizing the semiconducting light emitting nanoparticle is described.
Type:
Grant
Filed:
April 23, 2020
Date of Patent:
February 11, 2025
Assignee:
MERCK PATENT GMBH
Inventors:
Elizaveta Kossoy, Shany Neyshtadt, Sanaa Khalil, Alex Rabkin, Jessica Benjamini Ettedgui
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:
July 18, 2024
Date of Patent:
February 11, 2025
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Mary Ann Johnson, Leonardo R. 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 refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and an amino acid ethyl ester like L-phenylalanine ethyl ester or L-methionine ethyl ester, wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to amino acid ethyl ester is from 1:0.3 to 1:3.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.
Type:
Grant
Filed:
July 2, 2019
Date of Patent:
February 11, 2025
Assignee:
MERCK PATENT GMBH
Inventors:
Rudolf Moser, Viola Groehn, Ruth Boehni Stamm, Fritz Blatter, Martin Szelagiewicz
Abstract: Method and system to analyze biomasses in a bioreactor (3) via a computer (2) with a system software (5), the bioreactor (3) having at least one sensor (6) to measure the biomasses and which has a data connection to the computer (2) managed by a data interface provided by the system software (5), wherein the system software (5) provides a data conversion model (8) to analyze real time raw data about permittivity measured by and transmitted from the at least one sensor (6) to the computer (2) to calculate specific cell parameters of cells in the biomasses.
Abstract: The present invention provides a number of process improvements related to the conjugation of capsular polysaccharides from Streptococcus pneumoniae to a carrier protein. These processes are serotype specific and include acid hydrolysis, addition of sodium chloride to the reductive amination reaction, and addition of sucrose to dissolve polysaccharides. Polysaccharide-protein conjugates prepared using the processes of the invention can be included in multivalent pneumococcal conjugate vaccines.
Abstract: Disclosed herein are biomarkers that correlate with responses to an anti-ILT4 and anti-PD-1 combination therapy. A biomarker that can differentiate responders from non-responders to this combination therapy can potentially be used to select human subjects who have a higher probability to benefit from such a combination therapy. In one embodiment, a combined positive score (CPS) for PD-L 1 expression in a tumor sample from a human subject is used as a biomarker to differentiate a responder from a non-responder to an anti-ILT4 and anti-PD-1 combination therapy. In another embodiment, a T-cell-inflamed gene expression profile (TcellinfGEP) score is used as a biomarker to differentiate a responder from a non-responder to an anti-ILT4 and anti-PD-1 combination therapy.
Type:
Application
Filed:
December 15, 2022
Publication date:
February 6, 2025
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Rachel Allison Altura, Jared Lunceford, Julia F. Markensohn, Leah Suttner, Douglas C. Wilson
Abstract: The present application concerns compounds for use in electronic devices, processes for preparing the compounds, and electronic devices comprising the compounds.
Type:
Grant
Filed:
December 17, 2019
Date of Patent:
February 4, 2025
Assignee:
Merck Patent GmbH
Inventors:
Elvira Montenegro, Teresa Mujica-Fernaud, Florian Maier-Flaig, Frank Voges, Christian Wirges
Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
Type:
Grant
Filed:
March 8, 2019
Date of Patent:
February 4, 2025
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Abdelghani Abe Achab, Matthew L. Childers, Jared N. Cumming, Christian Fischer, Symon Gathiaka, Hakan Gunaydin, Charles A. Lesburg, Derun Li, Min Lu, Anandan Palani, Rachel L. Palte, Qinglin Pu, David L. Sloman, Sung-Sau So, Chunrui Sun, Hongjun Zhang
Abstract: The new media exhibit a ferroelectric nematic phase preferably at ambient temperature. They preferably comprise one or more compounds selected from the group of compounds of formulae IA, IB and IC, in which the variable groups have the meanings indicated in the text and in the claims. Use of the media for providing ferroelectric nematic materials and a method of operation of an electro-optical device are presented. The media may be useful for energy-saving displays and electrical appliances.
Type:
Grant
Filed:
November 30, 2021
Date of Patent:
February 4, 2025
Assignee:
MERCK PATENT GMBH
Inventors:
Matthias Bremer, Atsutaka Manabe, Martin Kraska
Abstract: The present invention is directed to pro drugs of 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
December 13, 2023
Date of Patent:
February 4, 2025
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Sachin Mittal, Jason W. Skudlarek, Izzat T. Raheem
Abstract: The invention relates, in part, to single domain antibody constructs. In particular, the invention relates, in part, to single domain antibody constructs that include a non-blocking ?-PDL1 VHH that would provide minimal disruption of the PD-1/?PD-L1 binding interaction. The invention further relates to a method for detecting cell-cell interactions using the VHH sequences provided herein.
Type:
Application
Filed:
December 1, 2022
Publication date:
January 30, 2025
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Edward P. Bowman, Olugbeminiyi O. Fadeyi, Rob C. Oslund
Abstract: The crosslinked peptidomimetic macrocycles disclosed herein comprise an alkene or alkyne staple and a poly-amino acid C-terminal tail. These crosslinked peptidomimetic macrocycles have improved binding to MDM2 and MDMX (aka MDM4), are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.
Type:
Application
Filed:
November 23, 2022
Publication date:
January 30, 2025
Applicants:
Merck Sharp & Dohme LLC, MSD International GmbH, Agency for Science, Technology and Research
Inventors:
Hubert Josien, Arun Chandramohan, Charles William Johannes, Christopher J. Brown, Srinivasaraghavan Kannan, Anthony William Partridge, Chandra Shekhar Verma, Lin Yan, Tsz Ying Yuen
Abstract: Disclosed are compounds of Formula I, or a salt thereof: where A, B, D, X, R1, R2 and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
Type:
Grant
Filed:
June 30, 2022
Date of Patent:
January 28, 2025
Assignee:
MERCK SHARP & DOHME LLC
Inventors:
Harold B. Wood, Hubert B. Josien, Thomas Joseph Tucker, Angela Dawn Kerekes, Ling Tong, Abbas M. Walji, Anilkumar G. Nair, Fa-Xiang Ding, Elisabetta Bianchi, Danila Branca, Chengwei Wu, Yusheng Xiong, Sookhee Nicole Ha, Jian Liu, Sobhana Babu Boga
Abstract: The present invention relates to immunoglobulins that bind ADAMTS5 and more in particular to polypeptides, that comprise or essentially consist of one or more such immunoglobulins. The invention also relates to constructs comprising such immunoglobulins, such as immunoglobulin single variable domains (ISVDs) or polypeptides as well as nucleic acids encoding such immunoglobulins or polypeptides; to methods for preparing such immunoglobulins, polypeptides and constructs; to host cells expressing or capable of expressing such immunoglobulins or polypeptides; to compositions, and in particular to pharmaceutical compositions, that comprise such immunoglobulins, polypeptides, constructs, nucleic acids and/or host cells; and to uses of immunoglobulins, polypeptides, constructs, nucleic acids, host cells and/or compositions, in particular for prophylactic and/or therapeutic purposes, such as the prophylactic and/or therapeutic purposes mentioned herein.
Type:
Grant
Filed:
January 19, 2022
Date of Patent:
January 28, 2025
Assignees:
Merck Patent GmbH, ABLYNX NV
Inventors:
Marie-Ange Buyse, Guy Hermans, Sven Lindemann, Hans Guehring, Ralf Guenther, Roland Kellner