首页> 外国专利> Derivatives of imidazo 2,1-b 1,3,4 thiadiazole, Pharmaceutical compositions containing Same, and Method for preparing them, and Use thereof for the treatment of tumors and other diseases induced by Kinases

Derivatives of imidazo 2,1-b 1,3,4 thiadiazole, Pharmaceutical compositions containing Same, and Method for preparing them, and Use thereof for the treatment of tumors and other diseases induced by Kinases

机译:咪唑并[2,1-b] [1,3,4]噻二唑的衍生物,含有该衍生物的药物组合物及其制备方法及其在治疗由激酶引起的肿瘤和其他疾病中的用途

摘要

The pyridan [2,1-b] [1,3,4] p-thiodiazepine derivative in formula (1), R1 is a monosexual anthrax (or an unsubstituted monosexual or non heterosexual) or an unsubstituted double cycle (consisting of 1-4 n, or Y / or S atoms), each of which can be replaced by at least one substitute "Hal", "CH2) nor3, - co-r3 selected from group A, -Co-nr3r3, - Co-N (R3) 2, - (CH2) nnr3r3, - (CH2) NN (R3) 2 and so2n (R3) 2; R2 is A'o CYC; R3 is an independent representation,In R1, a 'and CYC: H, a, oh, OA, ACIO or carboarilo alternative; a represents each other independently,In R1 and R3: non separator or separator tar containing 1-10 C atoms, one or two non adjacent CH2 groups may be replaced by N and / or NH; and / or in addition, 1-7 atoms of h may be replaced by Hal Oh, mofulin and / or ammonia; and a 'indicates that non separator tar or branch has 1-10 C atoms, Among them, 1-7 H atoms can be replaced by CYC, R3, NR3, n (R3), 2, het1 and optional anthrax; het1 is independent of each other,R1 and a ': saturated, unsaturated, unsaturated or preferred singlet or bicyclic heteromorphism, replaced by 1 to 4 N, O and / or S atoms, optionally = O; CYC is expressed independently of each other,R2, R3 and a ': cyclopentanediol with 3-7 C atoms, which can be replaced by - R3, NR3 or - n (R3) 2; Hal independently represents each other,in R1 and A: F, Cl, Br or I; and n is 0, 1, 2, 3 or 4; and / or its physiologically acceptable salts. They are TGF-beta receptor I kinase inhibitors and can be used, inter alia, for the treatment of tumors.
机译:式(1)中的吡啶并[2,1-b] [1,3,4]对硫二氮杂衍生物,R1是单性炭疽(或未取代的单性或非异性)或未取代的双环(由1-组成) 4个n或Y /或S原子),每个原子均可被至少一个取代基“ Hal”,“ CH2)nor3,-选自A组的co-r3,-Co-nr3r3,-Co-N( R3)2,-(CH2)nnr3r3,-(CH2)NN(R3)2和so2n(R3)2; R2是A'o CYC; R3是独立表示,在R1中,a'和CYC:H,a在R 1和R 3中:含1-10个碳原子的非分隔物或分隔物焦油,一个或两个不相邻的CH 2基团可以被N和/或NH取代;和/或另外,h的1-7个原子可以被Hal Oh,mofulin和/或氨水取代;并且'表示非分隔物的焦油或分支具有1-10个碳原子,其中1-7个H原子可以用CYC,R3,NR3,n(R3),2,het1和可选的炭疽代替; het1彼此独立,R1和' :饱和的,不饱和的,不饱和的或优选的单线或双环异态,被1-4个N,O和/或S原子取代,可选地= O; CYC彼此独立地表示,R 2,R 3和具有3-7个碳原子的':环戊二醇,可以被-R 3,NR 3或-n(R 3)2取代; Hal在R1和A中彼此独立地表示:F,Cl,Br或I; n为0、1、2、3或4;和/或其生理上可接受的盐。它们是TGF-β受体I激酶抑制剂,并且可以尤其用于治疗肿瘤。

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