公开(公告)号：WO2023078946A1

公开(公告)日：2023-05-11

申请号：PCT/EP2022/080576

申请日：2022-11-02

Applicant: ZIPHIUS VACCINES NV

Inventor： VALEMBOIS, Sophie ,  HAQUE, AKM, Ashiqul ,  SAHU, Itishri ,  MC CAFFERTY, Séan ,  CARDON, Christiaan

IPC: A61K9/51 ,  C07D241/04 ,  A61K47/24 ,  A61K47/22 ,  A61K47/28 ,  C07D295/15

Abstract: The current invention relates to ionizable lipid-like compound according to Formula (I) or pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The present invention also provides a lipid nanoparticle comprising an ionizable lipid-like compound according to Formula (I) and one or more RNA molecules, as well as a pharmaceutical composition or vaccine, comprising such lipid nanoparticles.

公开(公告)号：WO2022167866A1

公开(公告)日：2022-08-11

申请号：PCT/IB2022/000055

申请日：2022-02-07

Applicant: RAPPTA THERAPEUTICS OY

Inventor： TRAINOR, George, L. ,  RABAL GRACIA, Maria, Obdulia ,  FOURMOIS, Laura ,  GHERBOVET, Olga ,  CACHOUX, Frederic

IPC: C07C311/17 ,  C07C311/18 ,  C07D207/09 ,  C07D207/10 ,  C07D211/96 ,  C07D213/62 ,  C07D231/12 ,  C07D241/04 ,  C07D265/30 ,  C07D307/04 ,  C07D307/52 ,  C07D333/08 ,  C07D333/28 ,  C07D401/12 ,  C07D487/18 ,  A61P29/00 ,  A61P35/00 ,  A61K31/19

Abstract: The present disclosure relates in part to chemical modulators of protein phosphatase 2A (PP2A), comprising formula (I). The compounds of the present disclosure are useful in treating, preventing, and/or ameliorating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease, and cardiac hypertrophy.

公开(公告)号：WO2022159855A1

公开(公告)日：2022-07-28

申请号：PCT/US2022/013604

申请日：2022-01-25

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： GREEN, Jordan, J. ,  KARLSSON, Johan ,  TZENG, Stephany, Yi ,  LULY, Kathryn, M. ,  RUI, Yuan ,  WILSON, David ,  KOZIELSKI, Kristen

IPC: C07C381/00 ,  C07D241/04 ,  C07C321/14 ,  A61K31/78 ,  C07C69/54 ,  A61P35/00

Abstract: Nanocarriers are engineered to realize the potential of RNA therapeutics. This work reports the design of photo-crosslinked bioreducible nanoparticles (XbNPs) for stable siRNA encapsulation in high serum conditions, shielded surface charge, efficient intracellular trafficking, and triggered cytosolic RNA release. These attributes of XbNPs leads to robust siRNA-mediated knockdown in cancer cells and potent systemic siRNA delivery to tumors in the lungs.

公开(公告)号：WO2022140643A1

公开(公告)日：2022-06-30

申请号：PCT/US2021/065021

申请日：2021-12-22

Applicant: BAYLOR COLLEGE OF MEDICINE ,  YOUNG, Damian, Winston ,  SEMERCI, Fatih

Inventor： MALETIC-SAVATIC, Mirjana ,  KANDEL, Prasanna ,  CHAMAKURI, Srinivas

IPC: C07D401/06 ,  C07D401/14 ,  C07D241/04 ,  A61P25/00 ,  A61P35/00 ,  A61K31/496

Abstract: Small molecules acting through the ligand binding domain of nuclear receptor TLX (NR2E1) are disclosed, as well as the use thereof for promoting neurogenesis and treating disorders associated with nuclear receptor TLX, including neurological disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula II as described herein, and pharmaceutically acceptable salts or isomers thereof.

公开(公告)号：WO2022125370A1

公开(公告)日：2022-06-16

申请号：PCT/US2021/061583

申请日：2021-12-02

Applicant: IMBRIA PHARMACEUTICALS, INC. [US]/[US]

Inventor： PATEL, Jaikrishna ,  CHAMBERLIN, Paul

IPC: A61K31/455 ,  A61K31/495 ,  A61K31/496 ,  C07D241/02 ,  C07D241/04 ,  C07D401/12

Abstract: The invention provides methods of treating heart failure with reduced ejection fraction (HFrEF), heart failure with preserved ejection fraction (HFpEF), heart failure associated with hibernating myocardium, and hypertrophic cardiomyopathy (HCM) using modified forms of trimetazidine such as CV-8972 and CV-8814.

公开(公告)号：WO2022057522A1

公开(公告)日：2022-03-24

申请号：PCT/CN2021/111782

申请日：2021-08-10

Applicant: 京东方科技集团股份有限公司 ,  合肥鑫晟光电科技有限公司

Inventor： 马健 ,  任文明 ,  詹成勇 ,  张然

IPC: G02F1/1337 ,  G02F1/13 ,  C08L79/08 ,  C07D307/60 ,  C07D309/32 ,  C07D241/04

Abstract: 一种液晶取向剂，包括至少一种聚合物，选自聚酰亚酸和由所述聚酰亚酸闭环后获得的一组聚酰亚胺中的至少一种；聚酰亚酸包括如式(I)所示的第一双酐和如式(II)或(III)所示的第一二胺生成的第一链段结构。X 1为无定形链段；第一二胺中如式(II)所示，Y 1选自单键、O、NH、S、一个或多个不饱和双键和取代或未取代的脂肪环、芳环、杂环和稠环中的任一个，一个A 1和一个A 2分别选自C，并均与Y 1结合，其余A 1和A 2分别独立地选自CH、CR和N中的任一个；第一二胺中如式(III)所示，Z 1选自取代或未取代的脂肪环、芳环、杂环和稠环中的任一个，A 3和A 4分别独立地选自CH、CR和N中的任一个。

公开(公告)号：WO2022011732A1

公开(公告)日：2022-01-20

申请号：PCT/CN2020/103308

申请日：2020-07-21

Applicant: 凯莱英生命科学技术（天津）有限公司

Inventor： 洪浩 ,  洪亮 ,  陶建 ,  胡忠 ,  张岩 ,  朱建林 ,  王波辉 ,  戴瑞智 ,  王俊强

IPC: C07D241/04

Abstract: 本发明提供了一种吡嗪-2-甲酸乙酯的连续加氢方法。该连续加氢方法包括：将吡嗪-2-甲酸乙酯与氢气的混合物进行分散，以形成含有50nm～5mm小液滴的气液混合物作为反应原料；将反应原料连续地输入固定床反应器中进行催化氢化反应，并连续地排出哌嗪-2-甲酸乙酯，同时沿物料的流动方向，将固定床反应器分为至少两个控温段，且后一个控温段的温度低于前一个控温段的温度。上述强制分散过程能够使反应原料在催化氢化反应过程中进行高性能传质，提高反应原料的充分反应程度，并缩短反应时间。沿物料的流动方向，将固定床反应器进行分段控温段，能有效移除热量积蓄和控制反应器中的反应状态，提高目标产品的收率、纯度和产品性能稳定性。

公开(公告)号：WO2021175913A1

公开(公告)日：2021-09-10

申请号：PCT/EP2021/055315

申请日：2021-03-03

Applicant: STICHTING HET NEDERLANDS KANKER INSTITUUT – ANTONI VAN LEEUWENHOEK ZIEKENHUIS ,  UNIVERSITEIT LEIDEN ,  ACADEMISCH ZIEKENHUIS LEIDEN (H.O.D.N. LUMC) ,  PIVOT PARK SCREENING CENTRE B.V.

Inventor： VAN DER STELT, Marcelis ,  JIANG, Ming ,  MOHR, Florian, David ,  VAN BOECKEL, Constant, Adriaan, Anton ,  HUIZENGA, Mirjam, Cornelia, Wellemina ,  AMEDI, Avand

IPC: C07D241/04 ,  C07D295/108 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P35/00 ,  A61K31/495

Abstract: Provided are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof: Also provided are compositions comprising compounds of formula (I). The compounds and compositions are also provided for use as medicaments, for example as medicaments useful in the treatment of a condition modulated by monoacylglycerol lipase (MAGL). Also provided are the use of compounds and compositions for the inhibition of monoacylglycerol lipase (MAGL).

公开(公告)号：WO2021055376A1

公开(公告)日：2021-03-25

申请号：PCT/US2020/050924

申请日：2020-09-15

Applicant: DICE ALPHA, INC.

Inventor： FATHEREE, Paul R. ,  LINSELL, Martin S. ,  JACOBSEN, John R. ,  VAN DER LINDEN, Wouter A. ,  CHURCH, Timothy J. ,  AQUINO, Claudio ,  PAULICK, Margot G.

IPC: C07D241/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  A61K31/496 ,  A61P35/00

Abstract: The disclosure herein provides compounds and pharmaceutical compositions for the modulation of IL-17A useful for the treatment of inflammatory conditions, such as psoriasis.

公开(公告)号：WO2019236699A1

公开(公告)日：2019-12-12

申请号：PCT/US2019/035572

申请日：2019-06-05

Applicant: CRINETICS PHARMACEUTICALS, INC.

Inventor： HAN, Sangdon ,  ZHU, Yunfei ,  KIM, Sun Hee ,  ZHAO, Jian ,  WANG, Shimiao

IPC: C07D241/04 ,  C07D401/10 ,  C07D401/14 ,  C07D453/02

Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.