首页> 外国专利> Compounds mercaptoacetilamino - 1.5 - 3 - oxo - Azepan useful as inhibitors of Matrix Metalloproteinases,Pharmaceutical Composition and uses for the manufacture of Medicines for the treatment of diseases that respond to inhibition of Matrix Metalloproteinases

Compounds mercaptoacetilamino - 1.5 - 3 - oxo - Azepan useful as inhibitors of Matrix Metalloproteinases,Pharmaceutical Composition and uses for the manufacture of Medicines for the treatment of diseases that respond to inhibition of Matrix Metalloproteinases

机译:巯基乙酰胺基-1.5-3-氧代-氮杂环庚烷化合物,可用作基质金属蛋白酶的抑制剂,药物组合物,以及用于制备治疗对基质金属蛋白酶抑制有反应的疾病的药物

摘要

Described are compounds of the formula (i), where R1 is alkyl group C1 - C6, a W - M - (CH2), or a group Q - Z - (CH2) where W is phthalimido m; Z is a link or Oxy, NR6 NR6, C (OR), (OR), nr6c NHC (NR6), OC (NR6),HNC (OR) or so2nr6; Q is Hydrogen, or ung and N - (CH2) where Hydrogen is N - aryl - and C6, C9 C10, heteroariloc3 -, - C (o) - or6, n 2 (r6), morpholino, pirrolidino piperidino, R2 is alkyl or isoindolilo; C1 C4A Group - (CH2) P - heteroaryl C3 C9, or a Group (CH2) P - ar1donde AR1 is phenyl or substituted naftiloopc ionalmente; R3 is Hydrogen, C1 to C6 alkyl -, - ch2sch2nhcoch3 Group, a - (CH2) n -,A Group - (CH2) M - B or - CH2 - Group D - R7 where C6 C10 is aryl, heteroaryl or C3 C9, Cyclohexyl; b - N (R7) 2, guanidine, nitroguanidino,- C (o) - C (o) or or6 NR6; and D is Oxy or Uncle; R4 is Hydrogen or a Group - (CH2) M - S (o) x 2 (r6); R5 is Hydrogen,C1 - C6 alkyl R4 and R5 or taken along with the nitrogen Atom to which they are ancladosforman piperidino, pirrolidino, or isoindolilo; eshidrogeno alq uilo R6 and R7 is C1 - C6; Hydrogen or c1-c4 alkyl,Or a Group - (CH2) where p ar ar is optionally substituted phenyl onaftilo; R8 is Hydrogen, - C (o) R7, a group C (o) - (CH2) Q - K - A - S - group G, where K is selected from the group formed poramino,Uilamino Alq, fenilalquilamino, Heterocycles, and substituted Heterocycles; g is chosen from the group consisting of formula (ii); or otrosalquilo R12 to R16 are between - (CH2) V1 is pair; or,O or NH; V2 is n or CH; V3 is a link or - C (o) - (CH2); V4 is - W -, r, S, nr7 or CN (R11); X and x are each independientementech or a Salt, N;Stereoisomer or pharmaceutically acceptable hydrate.Derivatives are included in a Pharmaceutical Composition and use in produce Medicines to treat diseases that respond to inhibition of metal Protein of the Matrix.
机译:描述了式(i)的化合物,其中R 1是烷基C 1 -C 6,W M-(CH 2)或基团Q -Z-(CH 2),其中W是邻苯二甲酰亚胺基m; Z是链或Oxy,NR6 NR6,C(OR),(OR),nr6c NHC(NR6),OC(NR6),HNC(OR)或so2nr6; Q是氢或ung和N-(CH2),其中氢是N-芳基-和C6,C9,C10,杂芳基3-,-C(o)-or6,n 2(r6),吗啉代,吡咯烷基哌啶子基,R2是烷基或isoindolilo; C1C4A基团-(CH2)P-杂芳基C3C9,或基团(CH2)P-芳基AR1是苯基或取代的萘环; R3是氢,C1-C6烷基-,-ch2sch2nhcoch3基团,a-(CH2)n-,A基团-(CH2)M-B或-CH2-基团D-R7,其中C6C10是芳基,杂芳基或C3环己基; b-N(R7)2,胍,硝基胍基,-C(o)-C(o)或or6 NR6; D是Oxy或叔叔; R4是氢或-(CH2)MS-(x)(r6)基团R 5是氢,C 1 -C 6烷基,R 4和R 5或与氮原子一起使用的是Ancladosforman piperidino,pirrolidino或isoindolilo; eshidrogeno alq uilo R6和R7为C1-C6;氢或c 1 -c 4烷基,或基团-(CH 2),其中p ar ar是任选取代的苯基onf aftilo; R 8是氢,-C(o)R 7,是基团C(o)-(CH2)Q-K-A-S-G组,其中K选自形成的基团:poramino,Uilamino Alq,fenilalquilamino,杂环和取代的杂环; g选自式(ii);或otrosalquilo R12至R16之间-(CH2)V1为对;或或者,O或NH; V2为n或CH; V3是链接或-C(o)-(CH2); V4是-W-,r,S,nr7或CN(R11); X和x分别是独立性或盐,N;立体异构体或药学上可接受的水合物。衍生物包括在药物组合物中,并用于生产治疗对基质金属蛋白的抑制有响应的疾病的药物。

著录项

  • 公开/公告号AR009363A1

    专利类型

  • 公开/公告日2000-04-12

    原文格式PDF

  • 申请/专利权人 AVENTIS HOLDINGS INC.;

    申请/专利号AR1997P104242

  • 发明设计人

    申请日1997-09-17

  • 分类号C07K5/078;A61K38/05;A61P19/02;A61P35/00;A61P9/10;A61P27/02;A61P1/02;A61P11/00;

  • 国家 AR

  • 入库时间 2022-08-22 01:57:35

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