公开(公告)号：US12234265B2

公开(公告)日：2025-02-25

申请号：US18068867

申请日：2022-12-20

Applicant: Merck Sharp & Dohme LLC

Inventor： Lan Zhang ,  Arthur Fridman ,  Eberhard Durr ,  Andrew Bett

IPC: C07K14/135 ,  A61K39/155 ,  C12N7/00 ,  A61K39/00

Abstract: The disclosure relates to stable RSV F proteins and immunogenic compositions containing the same, as well as methods of using the immunogenic compositions and compositions comprising the RSV F proteins.

公开(公告)号：US20250051341A1

公开(公告)日：2025-02-13

申请号：US18720152

申请日：2022-12-13

Applicant: Merck Sharp & Dohme LLC

Inventor： 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

IPC: C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61P31/22

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.

公开(公告)号：US20250034211A1

公开(公告)日：2025-01-30

申请号：US18712016

申请日：2022-11-23

Applicant: Merck Sharp & Dohme LLC ,  MSD International GmbH ,  Agency for Science, Technology and Research

Inventor： Hubert Josien ,  Arun Chandramohan ,  Charles William Johannes ,  Christopher J. Brown ,  Srinivasaraghavan Kannan ,  Anthony William Partridge ,  Chandra Shekhar Verma ,  Lin Yan ,  Tsz Ying Yuen

IPC: C07K7/56 ,  A61K38/00 ,  A61K45/06 ,  A61P35/00

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.

公开(公告)号：US20250026759A1

公开(公告)日：2025-01-23

申请号：US18764441

申请日：2024-07-05

Applicant: Merck Sharp & Dohme LLC

Inventor： Michael J. Breslin ,  Antonella Converso ,  Abdellatif El Marrouni ,  Ashley Forster ,  David N. Hunter ,  Anthony W. Shaw ,  William D. Shipe ,  Yunlong Zhang

IPC: C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61P31/18 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

Abstract: The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve 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).

公开(公告)号：US20250011789A1

公开(公告)日：2025-01-09

申请号：US18690562

申请日：2022-09-08

Applicant: Aligos Therapeutics, Inc. ,  Merck Sharp & Dohme LLC

Inventor： N. Tilani S. De Costa ,  Xuan Luong ,  Aneerban Bhattacharya ,  Leonid Beigelman ,  Jerome Deval ,  Saul Martinez Montero

IPC: C12N15/113 ,  A61K45/06 ,  A61P1/16

Abstract: Disclosed herein are short interfering nucleic acid (siNA) molecules comprising modified nucleotides and uses thereof. The siNA molecules may be double stranded and comprise modified nucleotides selected from 2′—O-methyl nucleotides and 2′-fluoro nucleotides. Further disclosed herein are siNA molecules comprising additional modification including a phosphorylation blocker, conjugated moiety, or 5′-stabilized end cap. The siNA molecules may reduce or inhibit the production of hydroxysteroid dehydrogenase.

公开(公告)号：US20250002448A1

公开(公告)日：2025-01-02

申请号：US18689149

申请日：2022-09-19

Applicant: MERCK SHARP & DOHME LLC

Inventor： Ian M. Bell ,  Brendan M. Crowley ,  James Fells ,  Patrick Bazzini ,  Jean-Marie Contreras ,  Fabrice Garrido ,  Belinda C. Huff ,  Christophe Joseph ,  Christophe Morice ,  Dharam Paul ,  Aurelie Witzel

IPC: C07C233/60 ,  A61K31/165 ,  A61K31/337 ,  A61K31/343 ,  A61K31/44 ,  A61K31/443 ,  A61K45/06 ,  C07C233/59 ,  C07D213/30 ,  C07D305/08 ,  C07D307/94 ,  C07D405/12 ,  C07D407/12

Abstract: The present disclosure relates to compounds of formula (I) that are useful as modulators of a7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease. Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.

公开(公告)号：US20250000994A1

公开(公告)日：2025-01-02

申请号：US18532359

申请日：2023-12-07

Applicant: Merck Sharp & Dohme LLC ,  Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.

Inventor： Junyou Ge ,  Xiaoping Jin ,  Yina Diao ,  Yalan Yang ,  Yujie Fu ,  Dian Jing ,  Hongbo Zhong ,  Omobolaji Akala ,  Elliot Keith Chartash ,  Maria Catherine Pietanza ,  Bin Zhao

IPC: A61K47/68 ,  A61K31/282 ,  A61K33/243 ,  A61K39/395 ,  A61P35/00

Abstract: The present disclosure relates to methods of treating a cellular proliferative disorder (e.g., cancer) comprising administering: (a) an anti-human PD-1 antibody or antigen binding fragment thereof; and (b) an Immunoconjugate of Formula (I): wherein: Ab is an antibody that binds to Trop-2; and n is an integer from 1 to 10. Also disclosed are therapeutic combinations and kits containing such agents for the treatment of cancers.

公开(公告)号：US12178842B2

公开(公告)日：2024-12-31

申请号：US18051250

申请日：2022-10-31

Applicant: MERCK SHARP & DOHME LLC

Inventor： Hubert Josien ,  Abbas Walji ,  Harold B. Wood ,  Fa-Xiang Ding ,  Jian Liu ,  Thomas Joseph Tucker ,  Michael Man-Chu Lo ,  Liangqin Guo

IPC: A61K38/00 ,  A61K38/12 ,  A61P3/06 ,  C07K9/00

Abstract: Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 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.

公开(公告)号：US20240425524A1

公开(公告)日：2024-12-26

申请号：US18702524

申请日：2022-10-24

Applicant: Merck Sharp & Dohme LLC

Inventor： Abdelghani Abe Achab ,  Jenny Lorena Rico Duque ,  Xavier Fradera ,  Joey L. Methot ,  Phieng Siliphaivanh ,  Brandon A. Vara ,  Hongjun Zhang

IPC: C07D519/00 ,  A61K31/438 ,  A61K31/4709 ,  A61K31/519 ,  C07D471/20

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.

公开(公告)号：US20240409531A1

公开(公告)日：2024-12-12

申请号：US18698450

申请日：2022-10-10

Applicant: Merck Sharp & Dohme LLC

Inventor： Abdellatif El Marrouni ,  Antonella Converso ,  Ashley Forster

IPC: C07D413/06 ,  A61K31/538 ,  A61K45/06 ,  C07D265/36

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).