公开(公告)号：WO2022238737A1

公开(公告)日：2022-11-17

申请号：PCT/IB2021/054167

申请日：2021-05-14

Applicant: APRINOIA THERAPEUTICS LIMITED

Inventor： JANG, Ming-Kuei ,  TEMPEST, Paul ,  LIN, Yih-Shyan

IPC: A61K47/55 ,  A61P25/28 ,  C07D417/14 ,  A61K47/545

Abstract: The present disclosure provides compounds comprising an E3 ubiquitin ligase binding moiety and an alpha-synuclein protein binding moiety for use in the treatment of neurodegenerative diseases, in particular synucleinopathies.

公开(公告)号：WO2021197303A1

公开(公告)日：2021-10-07

申请号：PCT/CN2021/083862

申请日：2021-03-30

Applicant: 东莞市东阳光生物药研发有限公司 ,  广东东阳光药业有限公司

Inventor： 杨福斌 ,  李松 ,  王海龙 ,  王仲清 ,  郑宝液 ,  郭林峰 ,  李平珠

IPC: C07C67/08 ,  C07C69/34 ,  C07C67/313 ,  C07C69/67 ,  C07D207/48 ,  A61K47/54 ,  A61K38/28 ,  A61K38/26 ,  A61P3/10 ,  A61K47/543 ,  A61K47/545

Abstract: 本发明提出了一种制备长链脂肪二酸单苄酯的方法。该方法包括：1)将长脂肪链二酸进行酯化反应，以便获得长脂肪链二苄酯；2)将长脂肪链二苄酯进行水解反应，以便获得长链脂肪二酸单苄酯；其中，所述长脂肪链二酸具有式(A)所示的结构，X为6～32的整数。该方法，相对于现有技术，反应试剂廉价易得、操作简便、产品相关杂质含量低、中间体纯化简单，生产周期短，收率高，成本低，产生"废液"少，没有固废生成，环保压力低。

公开(公告)号：WO2022150555A2

公开(公告)日：2022-07-14

申请号：PCT/US2022/011560

申请日：2022-01-07

Applicant: DESIGN THERAPEUTICS, INC.

Inventor： ANSARI, Aseem ,  BHAT, Abhi ,  JEFFRIES, Sean ,  SHAH, Pratik ,  ZHANG, Chengzhi

IPC: A61K31/785 ,  A61K47/545 ,  C07D495/14 ,  A61K31/00 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

Abstract: The present disclosure relates to compounds and methods for modulating the expression of fxn, and treating diseases and conditions in which fxn plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a trinucleotide repeat sequence GAA; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence GAA; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.

公开(公告)号：WO2022082108A1

公开(公告)日：2022-04-21

申请号：PCT/US2021/055434

申请日：2021-10-18

Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.

Inventor： GOLDMAN, Aaron ,  SENGUPTA, Shiladitya ,  NATARAJAN, Siva Kumar

IPC: A61K31/437 ,  A61K47/545 ,  A61K47/64

Abstract: Described herein are HSP-90 inhibitors conjugated to lipids, compositions comprising the conjugates, and methods of use thereof for treating cancer.

公开(公告)号：WO2021123013A1

公开(公告)日：2021-06-24

申请号：PCT/EP2020/086811

申请日：2020-12-17

Applicant: JOHANNES GUTENBERG-UNIVERSITÄT MAINZ

Inventor： RÖSCH, Frank ,  LAHNIF, Hanane ,  GRUS, Tilman

IPC: A61K47/54 ,  A61K47/68 ,  A61K51/04 ,  A61K103/00 ,  A61P35/00 ,  A61K47/542 ,  A61K47/545 ,  A61K47/547 ,  A61K47/548 ,  A61K51/0402 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0489 ,  A61K51/0497

Abstract: Ein Smart-Drug-Delivery-System für duale nuklearmedizinisch-cytotoxische Theranostik umfasst – eine erste Verbindung mit der Struktur: oder – eine zweite Verbindung mit der Struktur Chel—S—TV und eine dritte Verbindung mit der Struktur CT—L—TV; wobei in der ersten, zweiten und dritten Verbindung Chel ein Rest eines Chelators für die Komplexierung eines Radioisotops; CT ein Rest einer cytotoxischen Verbindung; TV ein biologischer Targetingvektor; L1 und L jeweils ein Linker; S1, S2 und S jeweils ein Spacer ist.

公开(公告)号：WO2022007153A1

公开(公告)日：2022-01-13

申请号：PCT/CN2020/112583

申请日：2020-08-31

Applicant: 福建医科大学孟超肝胆医院（福州市传染病医院）

Inventor： 张晓龙 ,  曾永毅 ,  刘小龙 ,  丁磊

IPC: A61K9/51 ,  A61K47/42 ,  A61K47/22 ,  A61K47/02 ,  A61K39/00 ,  A61P35/00 ,  A61K38/415 ,  A61K41/0057 ,  A61K41/0071 ,  A61K47/545 ,  A61K47/61 ,  A61K47/6929 ,  A61K47/6939 ,  A61K49/0036 ,  A61K49/0045 ,  B82Y40/00 ,  B82Y5/00

Abstract: 一种同时包载光敏剂和蛋白质的肿瘤靶向纳米药物及其在制备抗肿瘤药物中的应用，该肿瘤靶向纳米药物是利用金属有机框架包载疏水性光敏剂和蛋白质药物，并采用改性剂进行修饰而构成。所述肿瘤靶向纳米药物具有肿瘤细胞主动靶向及肿瘤微环境响应释放药物的特性，并能在荧光成像的同时实现光动力治疗和蛋白质治疗的协同治疗，从而达到良好的诊断与治疗效果。

公开(公告)号：WO2021252446A1

公开(公告)日：2021-12-16

申请号：PCT/US2021/036335

申请日：2021-06-08

Applicant: UNITED THERAPEUTICS CORPORATION ,  MANNKIND CORPORATION

Inventor： BATRA, Hitesh ,  GUO, Liang ,  POISSON, Patrick ,  TUMMALA, Sri Harsha ,  HARRIS, Elizabeth Ann

IPC: C07D241/08 ,  A61K31/4965 ,  A61P11/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P11/06 ,  A61P25/02 ,  A61P17/02 ,  A61K31/192 ,  A61K31/5575 ,  A61K47/545

Abstract: Provided are novel treprostinil based compounds, methods of treatment using the same, and their methods of making.

公开(公告)号：WO2021248048A8

公开(公告)日：2021-12-09

申请号：PCT/US2021/035972

申请日：2021-06-04

Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGY

Inventor： CHUANG, Shih-Hsien ,  SUN, Wei-Ting ,  LAILEE, Ying-Shuan ,  LAI, Chun-Liang ,  LIN, Wun-Huei ,  WEI, Win-Yin ,  TSAI, Shih-Chong ,  YU, Cheng-Chou ,  HUANG, Chao-Yang

IPC: A61K47/68 ,  C07K16/32 ,  C07K16/46 ,  A61K47/545 ,  A61K47/6803 ,  A61K47/6817 ,  A61K47/6851 ,  A61K47/6889 ,  A61P35/00

Abstract: The present disclosure provides an immunoconjugate includes an antibody comprising an antigen-binding fragment that specifically binds to an epitope in mesothelin, an N-glycan binding domain and an N-glycan; a linker linking to the N-glycan; and a payload A and a payload B conjugated to the linker, respectively; wherein the payload A and the payload B are the same or different. A pharmaceutical composition comprises the immunoconjugate and a method for treating cancer are also provided in the disclosure.

公开(公告)号：WO2021127456A1

公开(公告)日：2021-06-24

申请号：PCT/US2020/066040

申请日：2020-12-18

Applicant: RAIN THERAPEUTICS INC.

Inventor： WAGMAN, Allan S.

IPC: A61K47/54 ,  A61P35/00 ,  A61K47/545 ,  C07D239/94 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/10

Abstract: The present disclosure relates to prodrugs of pan-HER, HER2, HER4 and/or EGFR (HER1) inhibitory agents. The prodrugs can be covalently bonded to attenuating moieties such as reductive triggers (e.g., chemical moieties that can be cleaved in vivo). The prodrugs are useful in methods of treatment of the human or animal body.

公开(公告)号：WO2021255524A1

公开(公告)日：2021-12-23

申请号：PCT/IB2021/000419

申请日：2021-06-16

Applicant: BIOASIS TECHNOLOGIES, INC.

Inventor： RATHJEN, Deborah ,  TIAN, Mei, Mei

IPC: A61K47/66 ,  A61P25/28 ,  C07K14/47 ,  C07K14/705 ,  C07K14/79 ,  C07K19/00 ,  C07K7/08 ,  A61K38/1709 ,  A61K38/1787 ,  A61K38/185 ,  A61K47/545 ,  A61K47/64

Abstract: Disclosed are therapeutic payloads comprising p97 fragments coupled with active agents having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, to facilitate delivery of therapeutic or diagnostic agents across the BBB. The therapeutic payloads can be effective in the treatment of frontotemportal dementia (FTD). Methods of treating frontotemporal dementia (FTD) and pharmaceutical compositions are also disclosed.