公开(公告)号：US20240360157A1

公开(公告)日：2024-10-31

申请号：US18260275

申请日：2022-01-06

Applicant: BIOGEN MA INC.

Inventor： Nathan Genung ,  Tamara Halkina Levin

IPC: C07D519/00 ,  A61K31/5025 ,  A61K31/53

CPC classification number: C07D519/00 ,  A61K31/5025 ,  A61K31/53

Abstract: This disclosure relates to compounds of formula (I′), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the application. The compounds of the present disclosure are capable of inhibiting the activity of tyrosine kinase 2 (TYK2). The disclosure further provides methods of preparing the compounds of the disclosure, and methods for their therapeutic use.

公开(公告)号：US20240360146A1

公开(公告)日：2024-10-31

申请号：US18574511

申请日：2022-06-30

Applicant: HANGZHOU HEALZEN THERAPEUTICS CO., LTD. ,  SHANGHAI INSTITTUTE OF MATERIA, CHINESE ACADEMY OF SCCIENCES

Inventor： Xinglu ZHOU ,  Jia LI ,  Xingguo LIU ,  Yubo ZHOU ,  Miao HU ,  Xiaomin LUO ,  Jiangfeng XIE ,  Weijuan KAN ,  Mingbo SU ,  Yizhe WU

IPC: C07D491/048 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/675 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07F9/6558

CPC classification number: C07D491/048 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/675 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07F9/65583

Abstract: Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof; or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.

公开(公告)号：US20240343704A1

公开(公告)日：2024-10-17

申请号：US18288213

申请日：2022-05-02

Applicant: Ontario Institute for Cancer Research (OICR)

Inventor： Anh Chau ,  Methvin Isaac ,  Babu Joseph ,  Radek Laufer ,  Gennady Poda ,  Michael Prakesch ,  Pandiaraju Subramanian ,  David Uehling ,  Iain Watson ,  Brian Wilson ,  Tao Xin

IPC: C07D401/04 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/695 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07F7/08

CPC classification number: C07D401/04 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/695 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07F7/0836

Abstract: The present application relates to halo-substituted heterocyclic compounds of Formula (I): or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

公开(公告)号：US20240342184A1

公开(公告)日：2024-10-17

申请号：US18757557

申请日：2024-06-28

Applicant: CHINA PHARMACEUTICAL UNIVERSITY

Inventor： Haiping HAO ,  Hong WANG ,  Huiyong SUN ,  Huijian HU ,  Xiaojie PAN ,  Guangji WANG ,  Xiaowei XU ,  Shuang CUI

IPC: A61K31/53 ,  A61K9/08 ,  A61K9/20 ,  A61K9/48 ,  A61K47/26 ,  A61K47/32 ,  A61P1/16

CPC classification number: A61K31/53 ,  A61K9/08 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/26 ,  A61K47/32 ,  A61P1/16

Abstract: Provided in the present invention is the use of an enhancer named as 3C1 in the preparation of an enhancer for the interaction between FXR protein and Caspase 8 protein. The enhancer can promote the interaction between FXR protein and Caspase 8 protein, thereby inhibiting the recruitment of Caspase 8 to apoptosome and blocking its formation, inhibiting the cleavage and activation of Caspase 8, blocking signal transduction of apoptosis, and ultimately inhibiting cell apoptosis. Therefore, the enhancer can be used for preparing a drug for treating liver diseases characterized with hepatocyte apoptosis.

公开(公告)号：US20240335448A1

公开(公告)日：2024-10-10

申请号：US18376981

申请日：2023-10-05

Applicant: Servier Pharmaceuticals LLC

Inventor： Zenon Konteatis ,  Janeta Popovici-Muller ,  Jeremy Travins ,  Robert Zahler ,  Zhenwei Cai ,  Ding Zhou

IPC: A61K31/53 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D251/18 ,  C07D251/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC classification number: A61K31/53 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D251/18 ,  C07D251/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.

公开(公告)号：US20240316025A1

公开(公告)日：2024-09-26

申请号：US18732162

申请日：2024-06-03

Applicant: Terns Pharmaceuticals, Inc.

Inventor： Martijn FENAUX ,  Kevin KLUCHER ,  Christopher T. JONES ,  Thorsten A. KIRSCHBERG

IPC: A61K31/454 ,  A61K31/4439 ,  A61K31/4748 ,  A61K31/53 ,  A61K31/575 ,  A61P1/16

CPC classification number: A61K31/454 ,  A61K31/4439 ,  A61K31/4748 ,  A61K31/53 ,  A61K31/575 ,  A61P1/16

Abstract: Provided herein are methods for treating liver disorders, including non-alcoholic steatohepatitis, and symptoms and manifestations thereof, in a patient which utilize, among others, a combination treatment of an FXR agonist and a THRβ agonist.

公开(公告)号：US12097205B2

公开(公告)日：2024-09-24

申请号：US17293100

申请日：2019-10-23

Applicant: B. Braun Melsungen AG

Inventor： Andreas Arndt ,  Natalie Dück ,  Michael Kurz

IPC: A61K31/53 ,  A61K9/08 ,  A61K47/10 ,  A61K47/18 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34

CPC classification number: A61K31/53 ,  A61K9/08 ,  A61K47/10 ,  A61K47/18 ,  A61K47/186 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34

Abstract: An aqueous composition includes a dihydrotriazine compound of the general formula below,




where



R1 means (i) a phenyl group or phenylalkyl group, (ii) a naphthyl group or naphthylalkyl group, (iii) a heterocyclic group, heterocyclic alkyl group or heterocyclic aminoalkyl group, (iv) an alkyl group having 1 to 16 carbon atoms or (v) a cycloalkyl group or cycloalkylalkyl group,
R1′ means a hydrogen atom bonded to the nitrogen atom at position 1 or 3 of the dihydrotriazine ring,
R2 and R3 each mean a hydrogen atom or a methyl group,
R4 means an alkyl group having 7 to 16 carbon atoms and
the dashed line indicates that a double bond is positioned either between positions 1 and 2 or between positions 2 and 3 of the dihydrotriazine ring, or a tautomer thereof or a salt thereof and
a defoamer.

公开(公告)号：US20240307537A1

公开(公告)日：2024-09-19

申请号：US18451632

申请日：2023-08-17

Applicant: Omeros Corporation

Inventor： Michael Cicirelli ,  Neil S. Cutshall ,  Gregory A. Demopulos ,  George A. Gaitanaris ,  Marc A. Gavin ,  Alexander Gragerov ,  Thomas L. Little ,  Rene Onrust

IPC: A61K39/00 ,  A61K31/17 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4409 ,  A61K31/473 ,  A61K31/495 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K31/53 ,  A61K31/55 ,  A61K39/395 ,  A61K45/06 ,  A61P35/00 ,  C07K16/28 ,  G01N33/574

CPC classification number: A61K39/4643 ,  A61K31/17 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4409 ,  A61K31/473 ,  A61K31/495 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K31/53 ,  A61K31/55 ,  A61K39/39558 ,  A61K45/06 ,  A61P35/00 ,  C07K16/28 ,  G01N33/57488 ,  A61K2039/505 ,  A61K2039/545 ,  C07K2317/76

Abstract: This disclosure is directed to compounds, compositions, and methods for the treatment of various diseases and/or conditions related to G protein-coupled receptor 174 (e.g., cancers).

公开(公告)号：US20240307357A1

公开(公告)日：2024-09-19

申请号：US18671217

申请日：2024-05-22

Applicant: AARHUS UNIVERSITET

Inventor： Thomas Holm PEDERSEN ,  Martin Brandhøj SKOV

IPC: A61K31/4192 ,  A61K31/00 ,  A61K31/165 ,  A61K31/53 ,  A61P21/02

CPC classification number: A61K31/4192 ,  A61K31/00 ,  A61K31/165 ,  A61K31/53 ,  A61P21/02 ,  A61K2300/00

Abstract: The present invention relates to Rufinamide (or active derivatives thereof) for use in the treatment of myotonia, such as myotonia congenita, paramyotonia congenita and myotonic dystrophy. The present invention also relates to a combinatorial composition comprising Rufinamide (or active derivatives thereof) and Lamotrigine (or active derivatives thereof) for use as a medicament.

公开(公告)号：US20240300936A1

公开(公告)日：2024-09-12

申请号：US18568365

申请日：2022-06-09

Applicant: AVELOS THERAPEUTICS INC.

Inventor： Ki Seon BAEK ,  Ja Heouk KHOO ,  Soongyu CHOI ,  Young Whan PARK ,  Simon WARD ,  Darren LE GRAND ,  Ryan WEST ,  Penelope TURNER ,  Samuele MARAMAI ,  Tristan REUILLON

IPC: C07D413/14 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: This invention relates to compounds which are microtubule associated serine/threonine-like kinase (MASTL) inhibitors and the use of the compounds in the treatment of diseases and medical conditions mediated by MASTL, for example in the treatment of cancer and other target related diseases.