公开(公告)号：WO2023088233A1

公开(公告)日：2023-05-25

申请号：PCT/CN2022/131893

申请日：2022-11-15

Applicant: INSILICO MEDICINE IP LIMITED

Inventor： CHENG, Xin ,  QIN, Luoheng ,  REN, Feng

IPC: C07D413/06 ,  C07D413/12 ,  A61P35/00 ,  A61K31/41 ,  A61K31/40

Abstract: Described herein are KAT6A inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of a disease or disorder associated with KAT6A.

公开(公告)号：WO2023026060A1

公开(公告)日：2023-03-02

申请号：PCT/GB2022/052204

申请日：2022-08-26

Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS

Inventor： AITKEN, Laura ,  GUNN-MOORE, Frank ,  SMITH, Terry K

IPC: C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D413/06 ,  A61K31/401 ,  A61K31/404 ,  A61K31/41 ,  A61K31/498 ,  A61P25/28 ,  A61P35/00

Abstract: The present invention concerns Amyloid Binding Alcohol Dehydrogenase (ABAD) inhibitors (I) or (II) that interact non- competitively with nicotinamide adenine dinucleotide + H (NADH). Inhibition of ABAD is useful in the treatment or prophylaxis of disease, including Alzheimer's disease (AD) and cancer. Accordingly, the present invention also concerns ABAD inhibitors for use as a medicament, specifically for use in the treatment of Alzheimer's disease and/or cancer.

公开(公告)号：WO2023018643A1

公开(公告)日：2023-02-16

申请号：PCT/US2022/039689

申请日：2022-08-08

Applicant: ABBVIE INC.

Inventor： CUSACK, Kevin, Patrick ,  HOEMANN, Michael, Zeller ,  KINSMAN, David, Andrew ,  OSMAN, Sami ,  STAMBULI, James, Patrick ,  ARGIRIADI, Maria, Anastasia ,  O'REILLY, Ciaran ,  DEXTER, Hannah ,  FORDYCE, Euan ,  ST. GALLAY, Steve

IPC: C07D401/06 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/455 ,  A61P29/00

Abstract: Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, useful as RIPK1 inhibitors, and pharmaceutical compositions comprising same. Further provided are methods of use and preparation. (I)

公开(公告)号：WO2023281271A1

公开(公告)日：2023-01-12

申请号：PCT/GB2022/051760

申请日：2022-07-08

Applicant: VICORE PHARMA AB

Inventor： PETERSEN, Nadia Nasser ,  HALLBERG, Anders ,  LARHED, Mats ,  FEX, Tomas ,  OHLSSON, Bengt

IPC: C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  C07D409/06 ,  A61P9/10 ,  A61P13/12 ,  A61P37/00 ,  A61P11/00 ,  A61K31/4178

Abstract: There is provided pharmaceutical compounds of formula I, wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3, X and Z have meanings given in the description, which compounds are useful in the treatment of autoimmune and/or fibrotic diseases, including interstitial lung diseases, such as idiopathic pulmonary fibrosis and sarcoidosis.

公开(公告)号：WO2022241286A1

公开(公告)日：2022-11-17

申请号：PCT/US2022/029304

申请日：2022-05-13

Applicant: GLOBAL BLOOD THERAPEUTICS, INC.

Inventor： WANG, Xiang ,  FUJIMORI, Shinji ,  NELSON, Todd, Daniel ,  PARRA RIVERA, Ana, Cristina ,  MUNDAL, Devon ,  GRAETZ, Benjamin ,  FRICK, Morin

IPC: C07D413/06

Abstract: The present disclosure relates to processes for preparing a compound of formula (I). The disclosure also provides compounds that are synthetic intermediates.

公开(公告)号：WO2022189856A1

公开(公告)日：2022-09-15

申请号：PCT/IB2022/000106

申请日：2022-03-08

Applicant: ABIONYX PHARMA SA

Inventor： DASSEUX, Jean-Louis Henri

IPC: C07D231/12 ,  C07D233/64 ,  C07D249/06 ,  C07D263/32 ,  C07D277/22 ,  C07D333/10 ,  C07D333/52 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  A61P1/16 ,  A61P13/12

Abstract: This invention provides compounds, for example, of Formulae (A)-(H) and (J)-(AA) and pharmaceutically acceptable salts, solvates, esters, amides, and prodrugs thereof. The invention further provides pharmaceutical compositions comprising a compound of the invention, and a pharmaceutically acceptable carrier or vehicle. The compounds and compositions disclosed herein are useful for treating or preventing various diseases and conditions, for example liver disease such as liver fibrosis, fatty liver disease, non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH), and kidney diseases such as acute kidney injury (AKI).

公开(公告)号：WO2022125849A1

公开(公告)日：2022-06-16

申请号：PCT/US2021/062733

申请日：2021-12-10

Applicant: ARKUDA THERAPEUTICS [US]/[US]

Inventor： BURNETT, Duane A. ,  LANTER, James C.

IPC: C07D405/06 ,  A61P25/00 ,  A61K31/4725 ,  C07D405/14 ,  C07D413/06 ,  C07D491/052 ,  C07D491/107 ,  C07D493/08 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10 ,  C07D513/04 ,  A61P3/00 ,  A61P29/00 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/553 ,  A61K31/541 ,  A61K31/542

Abstract: Provided herein are compounds that modulate progranulin and methods of using the compounds in progranulin-associated disorders, such as Frontotemporal lobe dementia (FTLD).

公开(公告)号：WO2022122882A1

公开(公告)日：2022-06-16

申请号：PCT/EP2021/084927

申请日：2021-12-09

Applicant: LUXEMBOURG INSTITUTE OF SCIENCE AND TECHNOLOGY (LIST) [LU]/[LU]

Inventor： VERGE, Pierre ,  ADJAOUD, Antoine ,  PUCHOT, Laura

IPC: C07D265/16 ,  C07D413/06 ,  C09J177/00 ,  C08G65/48 ,  C08G73/02

Abstract: The invention relates to a process for producing a benzoxazine containing free aliphatic hydroxyl groups and monoester comprising the steps of: a) a reaction of a phenolic acid derivative with a monofunctional oligomer or molecule at a temperature of from 80°C to 200°C, during 12h-48h, in a presence of a Bronsted type acid catalyst, resulting in a monophenol terminated oligomer or molecule and b) reaction of the monophenol terminated oligomer or molecule of step a) with a mixture of an amino-alcohol, a primary amine derivative and paraformaldehyde at a temperature range of from 80°C to 100°C, from 1h to 48h, under stirring.

公开(公告)号：WO2022099658A1

公开(公告)日：2022-05-19

申请号：PCT/CN2020/128838

申请日：2020-11-13

Applicant: 大连理工大学 ,  深圳迈瑞生物医疗电子股份有限公司

Inventor： 樊江莉 ,  陈庚文 ,  夏天平 ,  叶燚 ,  张子千 ,  姚起超

IPC: C09B23/02 ,  C07D417/06 ,  C07D413/06

Abstract: 本发明公开了一种菁类化合物、含菁类化合物染料以及菁类化合物的应用。菁类化合物具有通式I的结构。其中，X选自由C(CH3)2、O、S和Se组成的组。R1和R2各自独立地选自由H、C1-C18烷基、苯基、OR6和卤素组成的组、R3和R4各自独立地选自由C1-C18烷基、C1-C18羧基、C1-C18羟基、C1-C18NR5R6、苄基和取代苄基组成的组，其中取代苄基的取代基选自由C1-C18烷基、CN、COOH、NH2、NO2、OH、SH、C1-C6烷氧基、C1-C6烷基氨基、C1-C6酰氨基、卤素和C1-C6卤代烷基组成的组。R5和R6各自独立地选自由H和C1-C18烷基组成的组。Y-为负离子。根据本发明的菁类化合物，具有良好的活细胞通透性，能够在不破坏细胞膜的情况进入细胞对核酸进行染色；且激发光为波长较小的蓝绿色光。

公开(公告)号：WO2022071777A1

公开(公告)日：2022-04-07

申请号：PCT/KR2021/013401

申请日：2021-09-29

Applicant: 연세대학교 산학협력단

Inventor： 최재영 ,  한균희 ,  남궁완 ,  박성하 ,  박무석 ,  유태현 ,  송두나

IPC: C07D413/06 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/519 ,  A61P11/00 ,  C07D417/06 ,  C07D495/04

Abstract: 본 발명은 펜드린 억제 활성을 갖는 화합물의 의약 용도에 관한 것으로, 하기 화학식 1 또는 2로 표시되는 화합물, 이의 E- 또는 Z-이성질체, 이의 광학이성질체, 이의 전구체, 이의 약학적으로 허용가능한 염, 이의 용매화물 또는 이의 2종의 이성질체 혼합물 및 이의 펜드린 억제 활성을 이용한 호흡기 질환 예방, 개선 또는 치료용 조성물 및 이뇨용 조성물을 제공한다. [화학식 1] [화학식 2]