公开(公告)号：WO2023046198A1

公开(公告)日：2023-03-30

申请号：PCT/CN2022/121712

申请日：2022-09-27

Applicant: 中国医药研究开发中心有限公司

Inventor： 殷惠军 ,  胡远东 ,  陈士柱 ,  闫旭 ,  田卫学 ,  常江 ,  许世民 ,  付健民 ,  邓伟 ,  姚振海 ,  霍涛 ,  田振华 ,  吴国盛 ,  贾丽 ,  钱苏

IPC: C07D241/18 ,  C07D241/20 ,  C07D403/12 ,  C07D403/04 ,  C07D471/18 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/538 ,  A61P35/00 ,  A61P35/02

Abstract: 一种磺胺酮类化合物及其制备方法和医药用途。特别地，涉及通式（I）所示的磺胺酮类化合物，其制备方法，包含其的药物组合物，以及其作为含Src同源区2结构域蛋白酪氨酸磷酸酶2（SHP2）抑制剂的用途，特别是用于预防或治疗与SHP2活性相关的疾病的用途。通式（I）中各基团的定义与说明书中相同。

公开(公告)号：WO2021181221A1

公开(公告)日：2021-09-16

申请号：PCT/IB2021/051814

申请日：2021-03-04

Applicant: CELLIDO THERAPEUTICS B.V.

Inventor： DRUKKER, Micha ,  GROSCH, Markus Oliver

IPC: A61K31/00 ,  A61K31/136 ,  A61K31/407 ,  A61K31/453 ,  A61K31/538 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/08 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/06 ,  G01N33/50

Abstract: The present disclosure describes compounds that can promote the disintegration of complexes containing long non-coding RNA (lncRNA) in vivo. The present disclosure provides a method of using small molecules to treat human diseases, wherein the small molecules are used to disintegrate nuclear condensates comprising lncRNAs. Further, the present disclosure provides an in vitro method of identifying small molecules for the treatment of human diseases associated with lncRNA.

公开(公告)号：WO2021158820A1

公开(公告)日：2021-08-12

申请号：PCT/US2021/016663

申请日：2021-02-04

Applicant: OREGON HEALTH & SCIENCE UNIVERSITY

Inventor： GIBBS, Summer, L. ,  WANG, Lei, G. ,  BARTH, Connor, W.

IPC: A61K31/538 ,  C07D265/38 ,  A61K47/36 ,  A61K49/00

Abstract: Nerve-specific fluorophore formulations of Formula (I) for direct or systemic administration are described. The formulations can be used in fluorescence-guided surgery (FGS) to aid in nerve preservation during surgical interventions.

公开(公告)号：WO2021141041A1

公开(公告)日：2021-07-15

申请号：PCT/JP2021/000184

申请日：2021-01-06

Applicant: 大日本住友製薬株式会社

Inventor： 三平　和明 ,  石山　健夫 ,  池田　篤史 ,  石川　泰三 ,  樋口　真人 ,  田桑　弘之 ,  ▲高▼堂　裕平

IPC: A61K45/00 ,  A61P21/02 ,  A61P21/04 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D237/14 ,  C07D237/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D491/048 ,  C07D491/08 ,  C07D491/107 ,  C07D513/04 ,  C07D487/04 ,  C07D487/10 ,  C07D519/00 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551

Abstract: 電位依存性ナトリウムチャネル（Ｎａｖ）を活性化することによるタウオパチーの治療剤および／または予防剤が提供される。Ｎａｖ活性化剤を有効成分とする、タウオパチーの治療剤および／または予防剤。

公开(公告)号：WO2021084498A1

公开(公告)日：2021-05-06

申请号：PCT/IB2020/060217

申请日：2020-10-30

Applicant: JANSSEN BIOTECH, INC.

Inventor： CISAR, Justin ,  KUDUK, Scott ,  WANG, Aihua ,  ZHANG, Zhuming ,  WANG, Chao-yuan

IPC: C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  A61K31/4709 ,  A61K31/4196 ,  A61K31/517 ,  A61K31/538 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06

Abstract: The present invention discloses compounds formula (I): (I) wherein X is CH; R2 is (AA) R3 is (BB) The present compounds of formula (I) are dihydroorotate dehydrogenase (DHODH) inhibitors, and are useful for the treatment of inflammatory disorders, autoimmune disorders and cancer, such as e.g. lymphomas, leukemias, carcinomas, and sarcomas. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 61 to 101; examples 1 to 24; tables 1 and 2). An exemplary compound is e.g. 7-(4-ethyl-3-(hydroxymethyl)-5- oxo-4,5-dihydro-1H-1,2,4-triazol-l-yl)-6-fluoro-3-(3-fluorophenyl) -1-isopropylquinolin-4(1H)-one (example 1): (CC)

公开(公告)号：WO2021014014A1

公开(公告)日：2021-01-28

申请号：PCT/EP2020/071038

申请日：2020-07-24

Applicant: SENSORION

Inventor： DYHRFJELD-JOHNSEN, Jonas

IPC: A61K31/538 ,  A61P25/00 ,  A61P27/00

Abstract: The present invention relates to the therapeutic use of azasetron or an analogue thereof for treating and/or preventing a lesion in the central auditory nervous system (CANS). The inventors show that treatment of lesions in the CANS with azasetron allows reducing the loss of neurons in the brainstem.

公开(公告)号：WO2020136276A1

公开(公告)日：2020-07-02

申请号：PCT/EP2019/087122

申请日：2019-12-27

Applicant: UNIVERSITÉ LIBRE DE BRUXELLES

Inventor： AMIGHI, Karim ,  WAUTHOZ, Nathalie ,  ROSIÈRE, Rémi

IPC: A61K38/28 ,  A61K9/14 ,  A61K31/58 ,  A61P5/50 ,  A61P11/08 ,  A61P35/00 ,  A61K33/243 ,  A61K9/00 ,  A61K31/137 ,  A61K31/192 ,  A61K31/40 ,  A61K31/439 ,  A61K31/46 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/538 ,  A61K31/7048

Abstract: Dry powder inhalation formulation comprising at least one API and a lipid matrix comprising at least one triglyceride chosen in the group consisting of monohydroxystearin, dihydroxystearin, trihydroxystearin and their mixture and its manufacturing method.

公开(公告)号：WO2020046335A1

公开(公告)日：2020-03-05

申请号：PCT/US2018/048821

申请日：2018-08-30

Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE, INC.

Inventor： CUERVO, Ana Maria ,  GAVATHIOTIS, Evripidis

IPC: C07D241/42 ,  C07D265/36 ,  A61K31/498 ,  A61K31/538

Abstract: Compounds and pharmaceutically acceptable salts thereof of Formula I are disclosed. Certain compounds and salts of Formula I are active as CMA modulators. The disclosure provides pharmaceutical compositions containing a compound of Formula I.

公开(公告)号：WO2019243526A1

公开(公告)日：2019-12-26

申请号：PCT/EP2019/066384

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOMÉ-NEBREDA, José Manuel ,  TRABANCO-SUÁREZ, Andrés, Avelino ,  MARTINEZ-VITURRO, Carlos Manuel ,  DELGADO-JIMÉNEZ, Francisca ,  CONDE-CEIDE, Susana ,  VEGA RAMIRO, Juan, Antonio

IPC: C07D401/14 ,  C07D471/04 ,  A61P25/28 ,  C07D405/14 ,  C07D491/048 ,  C07D491/056 ,  C07D498/04 ,  A61K31/5365 ,  A61K31/536 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/436

Abstract: The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.

公开(公告)号：WO2019090085A8

公开(公告)日：2019-05-09

申请号：PCT/US2018/058969

申请日：2018-11-02

Applicant: CALICO LIFE SCIENCES LLC ,  ABBVIE INC.

Inventor： MARTIN, Kathleen, Ann ,  SIDRAUSKI, Carmela ,  FROST, Jennifer, M. ,  TONG, Yunsong ,  XU, Xiangdong ,  CHUNG, Seungwon ,  ZHANG, Qingwei, I. ,  SHI, Lei ,  MURAUSKI, Kathleen ,  DART, Michael, J. ,  RANDOLPH, John, T.

IPC: C07C233/00 ,  C07C235/00 ,  C07C237/00 ,  A61P19/00 ,  A61P25/00 ,  A61P3/00 ,  A61P21/00 ,  A61P29/00 ,  A61P35/00 ,  A61K31/16 ,  A61K31/165 ,  A61K31/538 ,  A61K31/352 ,  A61K31/36 ,  A61K31/498 ,  C07D311/66 ,  C07D319/20 ,  C07D405/12 ,  C07D413/06 ,  C07D265/36 ,  C07D493/04 ,  C07D207/22 ,  C07D209/42 ,  C07D307/84

Abstract: Provided herein are compounds of formula (I), compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions. (Formula I).