公开(公告)号：US12180219B2

公开(公告)日：2024-12-31

申请号：US18649712

申请日：2024-04-29

Applicant: Merck Sharp & Dohme LLC

Inventor： Feng Xu ,  Zhuqing Liu ,  Richard Desmond ,  Jeonghan Park ,  Alexei Kalinin ,  Birgit Kosjek ,  Hallena Strotman ,  Hongmei Li ,  Johannah Moncecchi

IPC: C07D207/08 ,  C07C215/30 ,  C07D207/12 ,  C07D487/04 ,  C12P17/10

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.

公开(公告)号：US12180152B2

公开(公告)日：2024-12-31

申请号：US17876138

申请日：2022-07-28

Applicant: Ozchela Inc.

Inventor： Min-Kyung Lee ,  Jin-Kak Lee ,  Won-Seok Han

IPC: C07D241/04 ,  A61K31/235 ,  A61K31/277 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/5375 ,  C07C15/52 ,  C07C63/331 ,  C07C229/68 ,  C07C253/30 ,  C07C255/35 ,  C07C255/37 ,  C07C255/41 ,  C07C255/42 ,  C07D207/08 ,  C07D213/79 ,  C07D213/80 ,  C07D221/00 ,  C07D265/30 ,  C07D295/155 ,  C07D295/192

Abstract: This invention relates to a stilbene derivative and a method of preparing the same, and more particularly to a novel stilbene derivative for inhibiting the function of cyclophilin, which is effective at the prevention of cyclophilin-related diseases or at the treatment of symptoms of such diseases, and to a method of preparing the same.

公开(公告)号：US12162818B2

公开(公告)日：2024-12-10

申请号：US17575027

申请日：2022-01-13

Applicant: The Regents of the University of California ,  The United States Government represented by the Department of Veterans Affairs

Inventor： Matthew Rettig ,  Michael E. Jung ,  D. Elshan Nakath G. Ralalage ,  Jiabin An

IPC: C07C225/16 ,  A61P35/00 ,  C07C33/48 ,  C07C49/223 ,  C07C235/34 ,  C07C235/78 ,  C07C321/20 ,  C07D207/08 ,  C07D211/32 ,  C07D241/04 ,  C07D265/30 ,  C07D303/32 ,  C07D303/40 ,  C07D307/52 ,  C07D333/24

Abstract: The present disclosure provides compounds of Formula (VIIb) and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

公开(公告)号：US20240300955A1

公开(公告)日：2024-09-12

申请号：US18508594

申请日：2023-11-14

Applicant: Merck Sharp & Dohme LLC

Inventor： Feng XU ,  Zhuqing LIU ,  Richard DESMOND ,  Jeonghan PARK ,  Alexei KALININ ,  Birgit KOSJEK ,  Hallena STROTMAN ,  Hongmei LI ,  Johannah MONCECCHI

IPC: C07D487/04 ,  C07C215/30 ,  C07D207/08 ,  C07D207/12 ,  C12P17/10

CPC classification number: C07D487/04 ,  C07C215/30 ,  C07D207/08 ,  C07D207/12 ,  C12P17/10

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.

公开(公告)号：US12084416B2

公开(公告)日：2024-09-10

申请号：US17422500

申请日：2020-01-13

Applicant: Zydus Lifesciences Limited

Inventor： Rajiv Sharma ,  Sameer Agarwal

IPC: C07D207/48 ,  C07D205/04 ,  C07D207/08 ,  C07D211/24 ,  C07D211/96 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D417/04 ,  C07D417/06

CPC classification number: C07D207/48 ,  C07D205/04 ,  C07D207/08 ,  C07D211/24 ,  C07D211/96 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D417/04 ,  C07D417/06

Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions in which interleukin 1β activity is implicated.

公开(公告)号：US20240245784A1

公开(公告)日：2024-07-25

申请号：US18409330

申请日：2024-01-10

Applicant: ARBUTUS BIOPHARMA CORPORATION

Inventor： James HEYES ,  Richard J. HOLLAND ,  Alan D. MARTIN ,  Mark WOOD

IPC: A61K47/54 ,  A61K31/713 ,  A61K47/59 ,  A61K47/60 ,  C07C235/10 ,  C07C237/08 ,  C07H15/08 ,  C07H15/18 ,  C07H15/26 ,  C07H21/00 ,  C07J51/00 ,  C07J63/00 ,  C12N15/113 ,  C07D207/08 ,  C07D207/12 ,  C07D211/42 ,  C12N15/11 ,  C12N15/87

CPC classification number: A61K47/549 ,  A61K31/713 ,  A61K47/554 ,  A61K47/59 ,  A61K47/60 ,  C07C235/10 ,  C07C237/08 ,  C07H15/08 ,  C07H15/18 ,  C07H15/26 ,  C07H21/00 ,  C07J51/00 ,  C07J63/008 ,  C12N15/113 ,  C07D207/08 ,  C07D207/12 ,  C07D211/42 ,  C12N15/111 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/346 ,  C12N2310/351 ,  C12N2320/32

Abstract: The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).

公开(公告)号：US20240182412A1

公开(公告)日：2024-06-06

申请号：US18335836

申请日：2023-06-15

Applicant: ReNAgade Therapeutics Management Inc.

Inventor： Muthusamy Jayaraman ,  Stephen Scully

IPC: C07D207/08 ,  C07D211/34 ,  C07D401/06

CPC classification number: C07D207/08 ,  C07D211/34 ,  C07D401/06

Abstract: The present disclosure details various lipids, compositions, and/or methods of optimized systems and delivery vehicles for the delivery of nucleic acid sequences, polypeptides or peptides for use in vaccinating against infectious agents.

公开(公告)号：US11926633B2

公开(公告)日：2024-03-12

申请号：US17272369

申请日：2019-08-26

Applicant: SUZHOU PENGXU PHARMATECH CO., LTD

Inventor： Peng Wang ,  Pixu Li ,  Qiang Wei ,  Wen Cheng ,  Hao Wu

IPC: C07D487/14 ,  C07D207/08 ,  C07D207/16 ,  C07D241/20 ,  C07D487/04

CPC classification number: C07D487/14 ,  C07D207/08 ,  C07D207/16 ,  C07D241/20 ,  C07D487/04

Abstract: The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III),






wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.

公开(公告)号：US11896672B2

公开(公告)日：2024-02-13

申请号：US16092685

申请日：2017-04-11

Applicant: ARBUTUS BIOPHARMA CORPORATION

Inventor： James Heyes ,  Richard J. Holland ,  Alan D. Martin ,  Mark Wood

IPC: A61K47/54 ,  A61K31/713 ,  C12N15/113 ,  A61K47/60 ,  C07C237/08 ,  C07H15/18 ,  C07C235/10 ,  C07H15/26 ,  C07J51/00 ,  C07H15/08 ,  A61K47/59 ,  C07J63/00 ,  C07H21/00 ,  C07D211/42 ,  C07D207/08 ,  C07D207/12 ,  C12N15/11 ,  C12N15/87

CPC classification number: A61K47/549 ,  A61K31/713 ,  A61K47/554 ,  A61K47/59 ,  A61K47/60 ,  C07C235/10 ,  C07C237/08 ,  C07H15/08 ,  C07H15/18 ,  C07H15/26 ,  C07H21/00 ,  C07J51/00 ,  C07J63/008 ,  C12N15/113 ,  C07D207/08 ,  C07D207/12 ,  C07D211/42 ,  C12N15/111 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/346 ,  C12N2310/351 ,  C12N2320/32 ,  C12N2310/321 ,  C12N2310/3521 ,  C12N2310/322 ,  C12N2310/3533

Abstract: The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).

公开(公告)号：US20230312473A1

公开(公告)日：2023-10-05

申请号：US18194423

申请日：2023-03-31

Applicant: Genentech, Inc. ,  Hoffmann-La Roche Inc.

Inventor： Fabienne HOFFMANN-EMERY ,  Manuel KONRATH ,  Christian LAUTZ ,  Katrin Monika NIEDERMANN ,  Jonathan Ugo ORCEL ,  Diane Elizabeth CARRERA

IPC: C07D213/61 ,  C07D207/08 ,  C07D207/16 ,  C07D239/38 ,  C07D491/08

CPC classification number: C07D213/61 ,  C07D207/08 ,  C07D207/16 ,  C07D239/38 ,  C07D491/08 ,  C07B2200/13

Abstract: Processes for preparing biheteroaryl compounds are provided, including the biheteroaryl compound 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine. Among other advantages, the processes provide for: the use of solvents that are relatively non-toxic and inexpensive; reduced usage of expensive precious metal catalysts; reaction temperature reduction in certain steps; the use of relatively non-toxic oxidation agents; the use of inexpensive transition metal catalysts; a reduction of molar ratios of certain reactants thereby improving process efficiency while reducing cost and waste; significantly higher reactant concentrations in certain steps; elimination of the need for multiple chromatographic purification steps; elimination of the need for certain extraction steps using organic solvent; and provide for higher yield and improved purity.