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1. WO2019196812 - PROTEIN DEGRADATION TARGETING COMPOUND, ANTI-TUMOR APPLICATION, INTERMEDIATE THEREOF AND USE OF INTERMEDIATE

Publication Number WO/2019/196812
Publication Date 17.10.2019
International Application No. PCT/CN2019/081840
International Filing Date 09.04.2019
IPC
C07D 401/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 401/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/454
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
454containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/502
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
50Pyridazines; Hydrogenated pyridazines
502ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/5025
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
50Pyridazines; Hydrogenated pyridazines
5025ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
Applicants
  • 上海科技大学 SHANGHAITECH UNIVERSITY [CN]/[CN]
Inventors
  • 杨小宝 YANG, Xiaobao
  • 姜标 JIANG, Biao
  • 孙仁红 SUN, Renhong
  • 任超伟 REN, Chaowei
  • 孙宁 SUN, Ning
  • 孔莹 KONG, Ying
  • 李岩 LI, Yan
  • 陈金聚 CHEN, Jinju
  • 阴倩倩 YIN, Qianqian
  • 宋肖玲 SONG, Xiaoling
  • 赵全菊 ZHAO, Quanju
  • 仇星 QIU, Xing
Agents
  • 上海胜康律师事务所 SYNCLAW ATTORNEYS
Priority Data
201810312040.809.04.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PROTEIN DEGRADATION TARGETING COMPOUND, ANTI-TUMOR APPLICATION, INTERMEDIATE THEREOF AND USE OF INTERMEDIATE
(FR) COMPOSÉ CIBLANT UNE DÉGRADATION PROTÉIQUE, UTILISATION ANTITUMORALE, INTERMÉDIAIRE DE CELUI-CI ET UTILISATION DE L'INTERMÉDIAIRE
(ZH) 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用
Abstract
(EN)
The present disclosure relates to a compound of formula (I), an anti-tumor use thereof, intermediate compounds thereof of formula (III) and formula (IV), and a use thereof. The compound of formula (I) has a degrading effect on a specific target protein, and is mainly composed of three parts: the first part is Small Molecules Binding Protein (SMBP); the second part is a linker unit (LIN); and the third part is a Ubiquitin Ligase Binding Moiety (LUM), wherein SMBP and LIN are covalently bound, and LIN is covalently bound to ULM. The compounds designed and synthesized by the present disclosure have a wide pharmacological activities, have a function of degrading specific proteins and/or inhibiting activities, and can be used for the treatment of associated tumor.
(FR)
La présente invention concerne un composé de formule (I), une utilisation antitumorale de celui-ci, des composés intermédiaires de celui-ci de formule (III) et de formule (IV), et une utilisation associée. Le composé de formule (I) a un effet de dégradation sur une protéine cible spécifique, et est principalement composé de trois parties : la première partie est une protéine de liaison à petites molécules (SMBP) ; la deuxième partie est une unité de liaison (LIN) ; et la troisième partie est une fraction de Liaison à l'ubiquitine ligase (LUM), SMBP et LIN étant liées de manière covalente, et LIN étant liée de manière covalente à ULM. Les composés fournis et synthétisés par la présente invention ont une large activité pharmacologique, ont une fonction de dégradation de protéines spécifiques et/ou d'inhibition des activités, et peuvent être utilisés pour le traitement d'une tumeur associée. (I), (III), (IV)
(ZH)
本公开涉及式(I)化合物及其抗肿瘤应用,和其中间体式(III)化合物、式(IV)化合物及其应用。式(I)化合物对特定靶蛋白具有降解作用,其主要由三部分组成,第一部分能够结合蛋白的小分子化合物(SMBP,Small Molecules Binding Protein);第二部分LIN是链接单元(Linker);第三部分ULM是具有泛素化功能的配体(ULM,Ubiquitin Ligase BindingMoiety);其中SMBP和LIN共价结合,且LIN与ULM共价结合。本公开设计合成的一系列化合物具有广泛的药理活性,有降解特定蛋白和/或抑制活性的功能,可用于相关的肿瘤治疗。
Also published as
JP2020555408
EP2019786024
Latest bibliographic data on file with the International Bureau