公开(公告)号：WO2023086363A2

公开(公告)日：2023-05-19

申请号：PCT/US2022/049367

申请日：2022-11-09

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： FILVAROFF, Ellen ,  HANNA, Bishoy ,  LAMBA, Manisha ,  ARONCHIK, Ida

IPC: A61K9/00 ,  A61K31/472 ,  A61K31/495 ,  A61N5/00 ,  A61P35/00

Abstract: The present application relates generally to methods for treating glioblastoma, or glioblastoma multiforme (GBM), with substituted heterocyclic derivative 4-[2-(cyclopropylmethoxy) -5-methylsulfonylphenyl]-2-methylisoquinolin-l-one, or the pharmaceutically acceptable salt thereof, which is a BET inhibitor.

公开(公告)号：WO2023080765A1

公开(公告)日：2023-05-11

申请号：PCT/KR2022/095004

申请日：2022-01-04

Applicant: (주)셀로스바이오텍

Inventor： 배윤수 ,  정다운

IPC: C07D271/113 ,  A61K31/4245 ,  A61K31/495 ,  A61K45/06 ,  A61P25/28 ,  A61P35/00 ,  C07D413/10

Abstract: 본 발명은 옥사다이아졸 유도체 및 이를 포함하는 NADPH 산화효소(NOX) 관련 질환 예방 또는 치료용 조성물에 관한 것으로, NOX 억제에 대한 우수한 작용을 통해 NADPH 산화효소(NOX) 와 관련된 질환의 치료에 이용될 수 있다.

公开(公告)号：WO2023078180A1

公开(公告)日：2023-05-11

申请号：PCT/CN2022/128331

申请日：2022-10-28

Applicant: 北京微智瑞医药科技有限公司

Inventor： 宁宗超 ,  郭全禄

IPC: A61K9/20 ,  A61K31/198 ,  A61K31/215 ,  A61K31/401 ,  A61K31/495 ,  A61K31/519 ,  A61K31/7048 ,  A61K45/00 ,  A61K47/42 ,  A61K47/38 ,  A61K47/36 ,  A61K47/32 ,  A61K47/10 ,  A61K47/14 ,  A61K47/02 ,  A61K47/26

Abstract: 本发明属于药物技术领域，具体涉及一种微型片剂及其制备方法和制剂。所述微型片剂，组分包括活性成分、填充剂和/或崩解剂，所述微型片剂直径为1-5mm，片重为1-50mg。所述制剂中微型片剂的数量为单个或多个。本发明还提供了微型片剂的制备方法。本发明的微型片剂能够实现小剂量直接给药，剂量精确，使用方便，提高用药依从性；本发明的微型片剂有效解决了含量均匀度问题，同时，降低了工艺的复杂度、难度，更适应于工业化生产。

公开(公告)号：WO2023064768A1

公开(公告)日：2023-04-20

申请号：PCT/US2022/077907

申请日：2022-10-11

Applicant: BAYLOR COLLEGE OF MEDICINE

Inventor： YOUNG, Damian Winston ,  CHAMAKURI, Srinivas ,  SANTINI, Conrad ,  MATZUK, Martin M. ,  TRAN, Kevin A. ,  JAIN, Prashi ,  GUDURU, Shiva Krishna Reddy ,  RAJI, Idris O. ,  SAMUEL, Errol L.G. ,  MACKENZIE, Kevin R.

IPC: C07D241/04 ,  A61K31/495 ,  A61P3/00 ,  A61P9/00 ,  A61P11/00 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00

Abstract: G protein-coupled receptor (GPCR) regulators and methods for their use are provided herein. The GPCR regulators described herein are useful in treating and/or preventing conditions or diseases associated with a GPCR, including ageing, cancer, cardiovascular disorders, hematologic disorders, infectious diseases, inflammatory diseases, metabolic diseases, neurodegenerative disorders, respiratory diseases, or urological disorders. Also provided are methods of regulating a G protein-coupled receptor in a cell using the compounds and compositions described herein.

公开(公告)号：WO2023031115A1

公开(公告)日：2023-03-09

申请号：PCT/EP2022/073941

申请日：2022-08-29

Applicant: DSM IP ASSETS B.V.

Inventor： BENDIK, Igor ,  TOPCHYAN, Araksya ,  BAYNE, Anne-Cecile V. ,  HUG, Hubert Paul ,  LA FATA, Giorgio

IPC: A61K31/495 ,  A61K31/59 ,  A61K31/592 ,  A61K31/593 ,  A61P25/22 ,  A61P25/24 ,  A61P29/00

Abstract: A lack of vitamin D is a possible reason for poor response to vortioxetine treatment. Many vortioxetine low-responders and vortioxetine non-responders benefit from vitamin D supplementation. The pharmaceutical combination of the invention is a pharmaceutical combination for simultaneous or sequential administration comprising vitamin D and vortioxetine. Thereby, vitamin D is preferably cholecalciferol or calcifediol. The preferred vortioxetine is vortioxetine hydrobromide.

公开(公告)号：WO2023031114A1

公开(公告)日：2023-03-09

申请号：PCT/EP2022/073940

申请日：2022-08-29

Applicant: DSM IP ASSETS B.V.

Inventor： BAYNE, Anne-Cecile V. ,  BENDIK, Igor ,  HUG, Hubert Paul ,  LA FATA, Giorgio ,  TOPCHYAN, Araksya

IPC: A61K31/495 ,  A61P25/24

Abstract: The present invention is about a personalised healthcare invention. The inventors have found that there is a functional relationship between a patient´s vitamin D level and his responsiveness to a treatment with vortioxetine. One embodiment of the invention relates to vortioxetine for use in the treatment of a depressive patient who has a healthy vitamin D level. The present invention also relates to a method of purposively selecting patients for treatment with vortioxetine or a pharmaceutically acceptable salt thereof, wherein the concentration of calcifediol is measured ex vivo in blood samples of patients that are suffering from depression, anxiety and/or chronic pain. The preferred vortioxetine is vortioxetine hydrobromide or any other pharmaceutically acceptable salt thereof.

公开(公告)号：WO2023030459A1

公开(公告)日：2023-03-09

申请号：PCT/CN2022/116584

申请日：2022-09-01

Applicant: 中国科学院上海药物研究所 ,  中国科学院武汉病毒研究所

Inventor： 周宇 ,  李佳 ,  张磊砢 ,  姜智冬 ,  臧奕 ,  张宇旻 ,  郑淼 ,  苏明波 ,  冯勃 ,  肖庚富 ,  柳红 ,  蒋华良

IPC: C07D401/06 ,  A61K31/495 ,  A61P31/14

Abstract: 本发明提供了一类含喹啉酮酰胺的化合物及其制备方法、药物组合物和用途，具体地，本发明提供了一种通式I所示结构的喹啉酮酰胺类化合物，及其外消旋体、R-异构体、S-异构体、可药用盐或它们混合物。所述的化合物具有优异的针对3CL蛋白酶的抑制活性，因此可以用于治疗、预防以及缓解与3CL蛋白酶相关的疾病，特别是用于治疗存在3CL蛋白酶的病毒性疾病，如由SARS-CoV-2、SARS-CoV、MERS-CoV、诺如病毒等引发的疾病。

公开(公告)号：WO2023027888A1

公开(公告)日：2023-03-02

申请号：PCT/US2022/039730

申请日：2022-08-08

Applicant: 3+2 PHARMA, LLC

Inventor： RUAN, Fuqiang

IPC: A61K31/33 ,  A61K31/495 ,  C07D471/02 ,  C07D471/04

Abstract: Provided are compounds of formula (la) and (lb), and pharmaceutically acceptable salts thereof. Additionally provided are compositions and pharmaceutical compositions comprising the compounds, therapeutic methods using same for modulating (e.g., inhibiting) CREB binding protein (CBP)/β-catenin mediated signaling in treating a condition, disease or disorder (e.g., fibrosis, cancer, neurological conditions, metabolic disorders (e.g., diabetes, etc.), and skin conditions (dermatitis, psoriasis, scarring, alopecia, etc.) mediated by aberrant CBP/β-catenin signaling, and cosmetic methods for treating skin conditions (e.g., aging, etc.). Additionally provided are methods for enhancing vaccine efficacy using the compounds and compositions. Further provided are methods for efficiently synthesizing an antagonist of CBP/catenin signaling pathway, comprising use, in a penultimate, or last reaction step, of an intermediate 2-propynyl-compound to form a pyrazole derivative (e.g., via 3+2 cycloaddition).

公开(公告)号：WO2023001891A1

公开(公告)日：2023-01-26

申请号：PCT/EP2022/070350

申请日：2022-07-20

Applicant: FUNDACIÓN PROFESOR NOVOA SANTOS ,  SERVIZO GALEGO DE SAÚDE

Inventor： MAYÁN SANTOS, María Dolores ,  CARPINTERO FERNÁNDEZ, Paula ,  GARCÍA YUSTE, Alejandro ,  ACEA NEBRIL, Benigno ,  FONSECA CAPDEVILA, Eduardo

IPC: A61K38/17 ,  A61P35/00 ,  A61K31/495

Abstract: The present invention to connexin 43 (Cx43) for use in the treatment of a type of cancer characterized by the presence of functional retinoblastoma gene (RB), or by the presence of functional RB and also by hyperactivity of CDK4 and CDK6, preferably in combination with a CDK4/6 inhibitor.

公开(公告)号：WO2023001247A1

公开(公告)日：2023-01-26

申请号：PCT/CN2022/107127

申请日：2022-07-21

Applicant: 南京明德新药研发有限公司

Inventor： 付翔宇 ,  丁照中 ,  胡利红 ,  曾旭 ,  江文 ,  黎健 ,  陈曙辉

IPC: C07D403/14 ,  C07D247/02 ,  A61K31/495 ,  A61K31/501 ,  A61K31/506 ,  A61P35/00

Abstract: 一系列哒嗪酮类化合物及其药学上可接受的盐，及其在制备治疗相关疾病的药物中的应用，具体公开了式(IV)化合物及其药学上可接受的盐。