公开(公告)号：WO2023062049A1

公开(公告)日：2023-04-20

申请号：PCT/EP2022/078329

申请日：2022-10-12

申请人： F. HOFFMANN-LA ROCHE AG ,  HOFFMANN-LA ROCHE INC.

发明人： AMOUSSA, Machoud ,  BENZ, Joerg ,  BLAISING, Julie Elisabeth Françoise ,  GIROUD, Maude ,  GRETHER, Uwe ,  KROLL, Carsten ,  KUHN, Bernd ,  MARTIN, Rainer E. ,  O'HARA, Fionn Susannah ,  PUELLMANN, Bernd ,  RITTER, Martin ,  ROMBACH, Didier ,  SCHMID, Philipp Claudio ,  WITTWER, Matthias Beat

IPC分类号： C07D487/10 ,  C07D498/10 ,  A61K31/407 ,  A61K31/4166 ,  A61K31/424

摘要： The invention provides new MAGL inhibitors having the general formula (I) wherein the variables are as described herein, compositions including the compounds,processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：WO2022195102A1

公开(公告)日：2022-09-22

申请号：PCT/EP2022/057227

申请日：2022-03-18

申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITE D'ORLEANS

发明人： MORISSET-LOPEZ, Séverine ,  SUZENET, Franck ,  GUILLAUMET, Gérald ,  DEAU, Emmanuel ,  ROBIN, Elodie ,  EL KHAMLICHI, Chayma ,  REVERCHON-ASSADI, Flora ,  HERVOUET-COSTE, Nadège ,  MADOURI, Fahima ,  HIEBEL, Marie-Aude ,  LE-BESCONT, Julie

IPC分类号： A61K31/454 ,  A61K31/496 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  A61K31/4166 ,  A61K31/4178 ,  A61K31/506 ,  A61K31/53 ,  A61K31/551 ,  C07D233/70 ,  C07D235/26 ,  C07D401/12 ,  C07D403/12 ,  C07D487/04

摘要： The present invention relates to a compound having the following formula (I) wherein: - R and R' are, independently from each other, H or (C1-C6)alkyl groups, or form together with the carbon atoms carrying them a (C6-C10)aryl group; - R2 is selected from the group consisting of: H, (C1-C6)alkyl group, halo(C1-C6)alkyl group, aryl, and heteroaryl; - A1 is a linker; - R'' is either a group (A-1) or a group (A-2) for use in the treatment of a brain disorder involving modified 5-HT7R-mediated signaling, especially for use in the treatment of pain or inflammation or in the treatment of multiple sclerosis, or for use to induce hypothermia.

公开(公告)号：WO2022173853A1

公开(公告)日：2022-08-18

申请号：PCT/US2022/015851

申请日：2022-02-09

申请人： XENON PHARMACEUTICALS INC. ,  RABINOWITZ, Stephen S.

发明人： JOHNSON, JR, James Philip

IPC分类号： A61K31/435 ,  A61K9/00 ,  A61K31/165 ,  A61K31/19 ,  A61K31/4015 ,  A61K31/41 ,  A61K31/4166 ,  A61P25/00 ,  A61P25/08

摘要： In certain embodiments, the present disclosure is directed to methods and uses for treating seizure disorders in a human in need thereof, wherein the methods and uses comprise conjointly administering N-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide (Compound A) and an antiseizure medication (ASM) to the human in amounts that are therapeutically effective when conjointly administered. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

公开(公告)号：WO2022077095A1

公开(公告)日：2022-04-21

申请号：PCT/CA2021/050472

申请日：2021-04-09

申请人： XENON PHARMACEUTICALS INC.

发明人： BEATCH, Gregory N. ,  NAMDARI, Rostam

IPC分类号： A61K31/635 ,  A61K31/4166 ,  A61P25/08 ,  C07D233/02 ,  C07D417/12

摘要： Provided are methods for treating diseases or conditions associated with Nav1.6 activity in a patient, comprising administering to said patient (S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2-fluoro-5-methyl-N(thiazol-4-yl)benzenesulfonamide or a pharmaceutically acceptable salt thereof, wherein the patient is also being administered a strong inducer of cytochrome P450 3A4 (CYP3A4).

公开(公告)号：WO2021248093A1

公开(公告)日：2021-12-09

申请号：PCT/US2021/036038

申请日：2021-06-04

申请人： HENRY FORD HEALTH SYSTEM

发明人： GHOSH, Jagadananda ,  MONGA, Jitender

IPC分类号： A61K31/4178 ,  A61K31/4166 ,  A61K45/06 ,  A61P35/00

摘要： The present invention discloses daclatasvir (DCV) for use in the treatment and/or prevention of cancer, preferably lung cancer and/ or prostate cancer, more preferably enzalutamide-resistant prostate cancer.

公开(公告)号：WO2021247977A1

公开(公告)日：2021-12-09

申请号：PCT/US2021/035863

申请日：2021-06-04

申请人： CELGENE QUANTICEL RESEARCH, INC.

发明人： DE ALVARO, Juan ,  PARRA-PALAU, Josep Lluis ,  NIKOLOVA, Zariana ,  DI MARTINO, Jorge ,  FILVAROFF, Ellen ,  ARONCHIK, Ida ,  MALATESTA, Martina

IPC分类号： A61K31/4166 ,  A61K31/513 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  A61P35/04

摘要： The present application relates generally to methods for treating prostate cancer with a lysine specific demethylase-1 (LSD-1) inhibitor, wherein the lysine specific demethylase-1 (LSD-1) inhibitor resensitizes the prostate cancer cells to androgen receptor pathway inhibitor (ARPI) treatment.

公开(公告)号：WO2021224313A1

公开(公告)日：2021-11-11

申请号：PCT/EP2021/061816

申请日：2021-05-05

申请人： DISRUPTIVE MATERIALS PHARMA AB

发明人： ÅSBERG, Peter ,  FAGERBERG, Jonas ,  IVARSSON, Caroline

IPC分类号： A61K9/14 ,  A61K31/4035 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61P35/00 ,  A61P17/06

摘要： The present invention is directed to a solid and substantially amorphous active pharmaceutical ingredient, to an oral pharmaceutical formulation comprising said substantially amorphous active pharmaceutical ingredient, as well as to a method for the manufacture of the same. The invention is also directed to the use of a particulate anhydrous and substantially amorphous mesoporous magnesium carbonate (MMC) to stabilize an active pharmaceutical ingredient (API).

公开(公告)号：WO2021190346A1

公开(公告)日：2021-09-30

申请号：PCT/CN2021/080926

申请日：2021-03-16

申请人： 纳莹（上海）生物科技有限公司

发明人： 张大生

IPC分类号： C07D233/96 ,  C07D233/66 ,  C07D233/70 ,  A61K31/00 ,  A61K31/4164 ,  A61K31/4166

摘要： 一种荧光染料及其制备方法和用途，荧光染料对粘度响应敏感并且特异，本底荧光低等优点，还可以作为荧光激活点亮型探针，用于蛋白、酶或核酸的荧光标记、定量或检测。

公开(公告)号：WO2021114315A1

公开(公告)日：2021-06-17

申请号：PCT/CN2019/125455

申请日：2019-12-14

申请人： SHANGHAI EAST HOSPITAL

发明人： CHEN, Yihan ,  LIANG, Dandan ,  LIU, Yi ,  SAKYA, Subas Man ,  LI, Li ,  ZHANG, Fulei ,  ZHOU, Huixing ,  HE, Xiaoyu

IPC分类号： A61K31/4166 ,  A61K31/4178 ,  C07D233/96 ,  A61P9/00 ,  A61P9/10

摘要： Provided herein is the use of heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, disclosed is the use of compounds of formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug thereof; and application thereof. Definition of each group in the formula can be found in the specification for details.

公开(公告)号：WO2021071451A1

公开(公告)日：2021-04-15

申请号：PCT/TR2020/050493

申请日：2020-06-05

申请人： İZMİR YÜKSEK TEKNOLOJİ ENSTİTÜSÜ

发明人： ŞANLI MOHAMED, Gülşah

IPC分类号： B01J23/00 ,  B01J23/06 ,  B01J37/02 ,  B01J31/00 ,  A61K31/4166 ,  A61K31/4439 ,  A61P35/00 ,  A61P5/28 ,  A61P13/08

摘要： The invention, in order to be used in the healthcare industry provided by biotechnology-nanotechnology, a targeted dual cytotoxic effective nano-metallo system for the treatment of non-metastasized castration-resistant prostate cancer, containing apalutamid@ZIF-8 nanoparticles, using the ZIF-8 framework for accumulation of zinc ion in prostate tumor tissue within the apalutamid@ZIF-8 nanoparticles, using metal-organic skeletons for direct delivery of zinc ion to tumor tissue for prostate cancer, zinc and apalutamide gives the dual effect is characterized by combining with a single formulation in nano size.