公开(公告)号：WO2023077218A1

公开(公告)日：2023-05-11

申请号：PCT/CA2022/051611

申请日：2022-11-01

Applicant: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIVERSITY

Inventor： LI, Chao-Jun ,  LI, Jianbin ,  HUANG, Chia-Yu

IPC: C07D401/04 ,  B01J31/28 ,  B01J35/00 ,  C07D213/22 ,  C07D213/71 ,  C07D213/81 ,  C07D215/06 ,  C07D215/12 ,  C07D215/14 ,  C07D217/26 ,  C07D221/12 ,  C07D235/08 ,  C07D239/88 ,  C07D241/44 ,  C07D277/56 ,  C07D277/64 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14 ,  C07D453/02 ,  C07D471/04 ,  C07D473/40

Abstract: There is provided a process for alkylating a substrate with a photocatalytic system. The process comprises providing a mixture containing an acid, and a substrate (an organic compound). Then, an organophotoredox catalyst of formula Ia is contact with the mixture. Finally, the organophotoredox catalyst is activated with a light irradiation to alkylate the substrate and form a carbon covalent bond.

公开(公告)号：WO2023077070A1

公开(公告)日：2023-05-04

申请号：PCT/US2022/078879

申请日：2022-10-28

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： CLARKE, Adam James ,  FRIENDS, Todd J. ,  MATHUR, Arvind ,  MYERS, Michael C. ,  LI, Jianqing ,  PINTO, Donald J.P. ,  PABBISETTY, Kumar Balashanmuga ,  SU, Shun ,  VOKITS, Benjamin P. ,  BARRE, Durga Buchi Raju ,  SMITH, II, Leon M. ,  ORWAT, Michael J. ,  SHAW, Scott A. ,  KUMAR, Sreekantha Ratna ,  POTTURI, Hima Kiran

IPC: C07D213/82 ,  C07D215/54 ,  C07D217/26 ,  C07D231/20 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D311/24 ,  C07D333/38 ,  C07D401/06 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07D491/20 ,  C07D498/04 ,  A61K31/4412 ,  A61P9/10

Abstract: The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension). Formula (I)

公开(公告)号：WO2023072969A1

公开(公告)日：2023-05-04

申请号：PCT/EP2022/079842

申请日：2022-10-25

Applicant: PERHA PHARMACEUTICALS

Inventor： DEAU, Emmanuel ,  GEORGE, Pascal ,  MEIJER, Laurent ,  MIEGE, Frédéric ,  ARCHAMBAUD, Sylvie

IPC: A61P3/00 ,  A61P3/10 ,  A61P19/02 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P31/00 ,  A61P31/12 ,  A61P31/16 ,  A61P31/18 ,  A61P31/22 ,  A61P33/00 ,  A61P33/06 ,  A61P35/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention relates to a compound of formula (I) wherein A, B, C, D and E are selected from the group consisting of =CH- and -N=, R2 is selected from a hydrogen atom, a (C1-C4)alkyl group and a (C3-C6)cycloalkyl group, R1 represents a (C4-C6)alkyl group, a (C3-C8)cycloalkyl group, a bridged (C6-C10)cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C1-C3)alkanediyl group, and R' represents, a (C3-C8)heterocycloalkyl group, or a (C3-C8)heteroaryl group, or a R'-L- group wherein L is a (C1-C3)alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome, Alzheimer's disease, dementia and/or tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; tendinopathy and osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia, infections and for regulating body temperature.

公开(公告)号：WO2023066834A1

公开(公告)日：2023-04-27

申请号：PCT/EP2022/078767

申请日：2022-10-17

Applicant: CHIESI FARMACEUTICI S.P.A.

Inventor： CARZANIGA, Laura ,  RANCATI, Fabio ,  RIZZI, Andrea ,  GHIDINI, Eleonora ,  IOTTI, Nicolò ,  MAZZUCATO, Roberta ,  LEVANTO, Stefano ,  WHITTAKER, Ben Paul

IPC: C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  A61P1/16 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P27/02 ,  A61K31/4025

Abstract: The present invention relates to compounds of formula (I) inhibiting Discoidin Domain Receptors (DDR inhibitors), methods of preparing such compounds, intermediate compounds useful in such preparations, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful for instance in the treatment of many disorders associated with DDR mechanisms.

公开(公告)号：WO2023046885A1

公开(公告)日：2023-03-30

申请号：PCT/EP2022/076491

申请日：2022-09-23

Applicant: ATROGI AB

Inventor： BENGTSSON, Tore ,  PELCMAN, Benjamin

IPC: C07D207/08 ,  C07D401/06 ,  A61K31/40 ,  A61K31/4439 ,  A61P1/16 ,  A61P3/10

Abstract: There is provided herein compounds of formula I and pharmaceutically acceptable salts thereof, wherein R1, ring A and the ring containing Q1 to Q5 have meanings as provided in the description. There is also provided medical uses of such compounds.

公开(公告)号：WO2023031319A1

公开(公告)日：2023-03-09

申请号：PCT/EP2022/074293

申请日：2022-09-01

Applicant: AXXAM S.P.A.

Inventor： CATALANI, Maria Pia ,  PEVARELLO, Paolo ,  SODANO, Mariangela

IPC: C07D405/06 ,  C07D403/10 ,  C07D401/06 ,  C07D249/12 ,  A61K31/4196 ,  A61P11/08 ,  A61P25/04 ,  A61P25/18 ,  A61P25/28 ,  A61P27/02 ,  A61P35/00 ,  A61P37/00

Abstract: The present invention relates to novel 2,4-dihydro-3H-1,2,4-triazol-3-one compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

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：WO2023016562A1

公开(公告)日：2023-02-16

申请号：PCT/CN2022/112259

申请日：2022-08-12

Applicant: 浙江同源康医药股份有限公司

Inventor： 梁阿朋 ,  李钧 ,  吴豫生 ,  陈少卿 ,  刘广斌 ,  尹洲 ,  董胜利 ,  李美华

IPC: C07D215/48 ,  C07D471/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D241/44 ,  C07D487/04 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/55 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02

Abstract: 本发明涉及多环类化合物及其用途。具体地，本发明化合物具有式I所示结构，其中各基团和取代基的定义如说明书中所述；本发明还公开了所述化合物的制备方法及其在调节和治疗与YAP/TEAD的异常活性所导致的相关疾病方面的用途。

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.