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1. WO2020135442 - FAK INHIBITOR AND DRUG COMBINATION THEREOF

Publication Number WO/2020/135442
Publication Date 02.07.2020
International Application No. PCT/CN2019/128030
International Filing Date 24.12.2019
IPC
C07D 403/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/506 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
506not condensed and containing further heterocyclic rings
CPC
A61K 31/4439
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
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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 31/506
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
A61K 31/519
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
519ortho- or peri-condensed with heterocyclic rings
A61K 31/53
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
53having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5377
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
Applicants
  • 成都海创药业有限公司 HINOVA PHARMACEUTICALS INC. [CN]/[CN]
Inventors
  • 杜武 DU, Wu
  • 李宇 LI, Yu
  • 温坤 WEN, Kun
  • 李兴海 LI, Xinghai
  • 陈元伟 CHEN, Yuanwei
Agents
  • 成都高远知识产权代理事务所(普通合伙) GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP)
Priority Data
201811614990.227.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) FAK INHIBITOR AND DRUG COMBINATION THEREOF
(FR) INHIBITEUR DE FAK ET COMBINAISON DE MÉDICAMENTS ASSOCIÉE
(ZH) 一种FAK抑制剂及其联合用药物
Abstract
(EN)
A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. Moreover, the deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment. (I)
(FR)
La présente invention concerne un composé deutéré représenté par la formule (I) ou un isomère optique, un tautomère, un sel pharmaceutiquement acceptable, un promédicament, un hydrate ou un solvate de celui-ci. Par comparaison avec un composé avant deutération, le composé deutéré présente une meilleure pharmacocinétique, une concentration de médicament plasmatique maximale plus élevée, une très bonne exposition, une demi-vie plus longue, et présente une excellente performance métabolique. De plus, le composé deutéré peut inhiber de manière efficace l'activité de FAK, et présente une bonne perspective d'application dans la préparation d'inhibiteurs de FAK et/ou de médicaments pour le traitement du cancer. De plus, l'utilisation du composé deutéré en combinaison avec un médicament anticancéreux (tel qu'un inhibiteur de PD-1) peut atteindre un effet synergique, ce qui permet d'améliorer de manière significative l'effet d'élimination de tumeur, et de fournir un meilleur choix pour le traitement clinique du cancer. (I)
(ZH)
一种式(I)所示的氘代化合物或其光学异构体、互变异构体、药学上可接受的盐、前药、水合物或溶剂合物。与氘代前的化合物相比,氘代化合物显示了更优的药代动力学,更高的最高血药浓度,更高的暴露量和更长的半衰期,具有更加优异的代谢性能。而且,氘代化合物能够有效抑制FAK活性,在制备FAK抑制剂和/或治疗癌症的药物中具有非常好的应用前景。同时,氘代化合物与抗癌药物(比如PD-1抑制剂)联合使用能够发挥协同增效的作用,显著提高肿瘤抑制效果,为临床治疗癌症提供了更好的选择。 (I)
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