公开(公告)号：WO2023089632A1

公开(公告)日：2023-05-25

申请号：PCT/IN2022/051006

申请日：2022-11-16

申请人： COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN. OF SOC. ACT (ACT XXI OF 1860)

发明人： SULOCHANA, Priya ,  SASIDHAR BALAPPA, Somappa ,  KOZHIPARAMBIL GOPALAN, Raghu ,  SREERENJINI, Lakshmi ,  KIZHAKKAN THIRUTHI, Ashitha

IPC分类号： A61P35/00 ,  A61K31/415 ,  C07D231/14

摘要： The present disclosure provides new derivatives of pyrazole amide represented by the formula (Formula I) in which when R= -CH2-, then R1 may be one among benzene, 4-methyl benzene, 4-methoxy benzene, 4-chloro benzene, 4-fluoro benzene, 2-chloro benzene, 3,4-dichloro benzene, 3,5-trifluoromethylbenzene, and when R= -SO2-, then R1 may be one among benzene, 4-methoxy benzene, 4-chloro benzene, 4-bromo benzene, 4-trifluoromethyl benzene, 3-trifluoromethyl benzene, 2-bromo benzene, 2-chlorothiophen, 2,3-dichlorothiophen substituents. The disclosure also relates to compounds of formula (I) for its use as an anticancer agent in triple negative breast cancer (TNBC) cells. The disclosure established the effectiveness of the pyrazole amide derivative of formula I (I-8), against TNBC cells by inducing cell death by various mechanisms through interaction with diverse cellular pathways.

公开(公告)号：WO2023283453A1

公开(公告)日：2023-01-12

申请号：PCT/US2022/036569

申请日：2022-07-08

申请人： DICE ALPHA, INC.

发明人： REILLY, Maureen ,  FATHEREE, Paul R. ,  AQUINO, Claudio ,  FREIDBERG, Michael ,  CHURCH, Timothy J.

IPC分类号： A61P29/00 ,  C07D213/56 ,  C07D231/14 ,  C07D261/18 ,  C07D271/08 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： The disclosure herein provides phenyl acetamide based compounds of Formula (I), (I-a), (II), and pharmaceutical compositions thereof, for the modulation of IL-17A, useful in the treatment of inflammatory conditions such as psoriasis.

公开(公告)号：WO2023280630A1

公开(公告)日：2023-01-12

申请号：PCT/EP2022/067677

申请日：2022-06-28

申请人： BASF SE

发明人： GEBHARDT, Joachim ,  GARIVET, Guillaume Michel Jacques ,  BORATE, Kailaskumar ,  KNOLL, Daniel Maximilian ,  GOETZ, Roland

IPC分类号： C07D231/14 ,  C07C251/40 ,  C07D271/06

摘要： The present invention relates to a process for the preparation of substituted amidoximes of formula I, which can be obtained through reaction of nitrile compounds of formula II with free hydroxylamine in the presence of a solvent.

公开(公告)号：WO2022266357A1

公开(公告)日：2022-12-22

申请号：PCT/US2022/033845

申请日：2022-06-16

申请人： FUSION PHARMACEUTICALS INC. ,  KLINZ, Stephan

发明人： IMBS, Diane-Charlotte ,  LEWKOWICZ, Elodie ,  ROLLAND, Sylvie ,  ROHBAN, Thomas ,  FORBES, John R.

IPC分类号： A61K31/33 ,  C07D403/00 ,  C07D231/14 ,  A61K31/41 ,  A61K31/00

摘要： The present invention relates to a combination comprising a neurotensin receptor binding compound and NAPOX for use for the treatment of a neurotensin receptor overexpressing tumour in a subject.

公开(公告)号：WO2022197577A1

公开(公告)日：2022-09-22

申请号：PCT/US2022/020110

申请日：2022-03-14

申请人： MERCK SHARP & DOHME LLC ,  CHILDERS, Kaleen Konrad ,  ELLIS, J. Michael ,  FULLER, Peter, J. ,  GUNAYDIN, Hakan ,  SCOTT, Jack, D. ,  TANG, Haiqun ,  YEUNG, Charles, S.

发明人： CHILDERS, Kaleen Konrad ,  ELLIS, J. Michael ,  FULLER, Peter, J. ,  GUNAYDIN, Hakan ,  SCOTT, Jack, D. ,  TANG, Haiqun ,  YEUNG, Charles, S.

IPC分类号： A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  C07D231/10 ,  C07D231/12 ,  C07D231/14

摘要： The present invention is directed to certain (hetero)aroyl 4-aminopyrazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：WO2021188769A

公开(公告)日：2021-09-23

申请号：PCT/US2021/022912

申请日：2021-03-18

申请人： ARCUS BIOSCIENCES, INC. [US]/[US]

发明人： BEATTY, Joel Worley ,  DREW, Samuel Lawrie ,  EPPLIN, Matthew ,  FOURNIER, Jeremy Thomas Andre ,  GAL, Balint ,  GUNEY, Tezcan ,  HAELSIG, Karl T. ,  HARDMAN, Clayton ,  JACOB, Steven Donald ,  JEFFREY, Jenna Leigh ,  KALISIAK, Jaroslaw ,  LAWSON, Kenneth Victor ,  LELETI, Manmohan Reddy ,  LINDSEY, Erick Allen ,  MAILYAN, Artur Karenovich ,  MANDAL, Debashis ,  MATA, Guillaume ,  MOON, Hyunyoung ,  POWERS, Jay Patrick ,  ROSEN, Brandon Reid ,  SU, Yongli ,  TRAN, Anh Thu ,  WANG, Zhang ,  YAN, Xuelei ,  YU, Kai

IPC分类号： C07C255/52 ,  C07C317/14 ,  C07C317/22 ,  C07D209/34 ,  C07D213/26 ,  A61P35/00 ,  C07D213/30 ,  C07D213/61 ,  C07D213/64 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/18 ,  C07D215/36 ,  C07D215/48 ,  C07D217/02 ,  C07D231/12 ,  C07D231/14 ,  C07D231/56 ,  C07D237/20 ,  C07D239/28 ,  C07D239/42 ,  C07D241/12 ,  C07D241/20 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/56 ,  C07D265/36 ,  C07D277/24 ,  C07D277/40 ,  C07D277/56 ,  C07D277/62 ,  C07D307/83 ,  C07D307/88 ,  C07D311/58 ,  C07D401/04 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/44

摘要： Compounds that inhibit HIF-2a, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2a.

公开(公告)号：WO2021129565A1

公开(公告)日：2021-07-01

申请号：PCT/CN2020/137963

申请日：2020-12-21

申请人： BEIJING INNOCARE PHARMA TECH CO., LTD.

发明人： CHEN, Xiangyang ,  FENG, Jing

IPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D231/14 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/454 ,  A61P35/00

摘要： The various crystalline forms of (S) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1H-pyrazole-4-carboxamide and the pharmaceutical compositions comprising the crystalline forms are provided.

公开(公告)号：WO2020257261A1

公开(公告)日：2020-12-24

申请号：PCT/US2020/038103

申请日：2020-06-17

申请人： NORTHWESTERN UNIVERSITY

发明人： SCHILTZ, Gary, E ,  JAIN, Atul ,  HAN, Huiying ,  ABDULKADIR, Sarki, A.

IPC分类号： C07D231/14 ,  C07D231/18 ,  C07D233/58 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4164 ,  A61K31/4192 ,  A61P35/00

摘要： Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute tri azoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.

公开(公告)号：WO2020117493A1

公开(公告)日：2020-06-11

申请号：PCT/US2019/062778

申请日：2019-11-22

申请人： FMC CORPORATION ,  FMC AGRO SINGAPORE PTE LTD.

发明人： BOOTH, Steven, T.

IPC分类号： C07D231/14 ,  C07D401/04

摘要： A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride in a continuous process.

公开(公告)号：WO2020084094A1

公开(公告)日：2020-04-30

申请号：PCT/EP2019/079108

申请日：2019-10-24

申请人： ETH ZURICH

发明人： KATAYEV, Dmitry ,  ZHANG, Kun ,  CALVO, Roxan

IPC分类号： C07D311/72 ,  C07C201/08 ,  C07C205/06 ,  C07D239/30 ,  C07D207/40 ,  C07D209/48 ,  C07F5/02 ,  C07D213/61 ,  C07D307/71 ,  C07C209/02 ,  C07C231/12 ,  C07C253/30 ,  C07C315/04 ,  C07C319/20 ,  C07J41/00 ,  C07D209/02 ,  C07D231/14 ,  C07D233/76 ,  C07D233/92 ,  C07D333/12 ,  C07H15/00

摘要： The present invention relates to a process for preparing a nitrated compound, comprising the step of reacting a compound (A) comprising at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein said heteroaromatic ring comprises at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I) wherein Y is selected from the group consisting of hydrogen and nitro.