首页> 外国专利> Deformilasa peptidyl inhibitors (PDF), useful for the treatment of tuberculosis, and Pharmaceutical compositions containing them.

Deformilasa peptidyl inhibitors (PDF), useful for the treatment of tuberculosis, and Pharmaceutical compositions containing them.

机译:可用于治疗肺结核的变形甲状肽抑制剂(PDF),以及含有它们的药物组合物。

摘要

Claim 1: a compound of the formula (1) or a pharmaceutically acceptable Salt, Ester or prodrug thereof wherein: N is 1 or 2; X is CH2, s or CHF; r1 is - n or - cho (o) C (o) NH (OH); R2 is alkyl, alquilcicloalquilo or alkylaryl or R2 represents a cycloalkyl Group,Where the C adjacent to the carbonyl Group is part of the cycloalkyl Ring; R3 is a Substituent of the formula (2) or (3) or tetrazolilo perimidinilo, 2 - or 4 - fenilimidazol thiocyanatoacetate; where is NH, o, S, or NR4; a, B, D and e each independently selected CHN or CR5; or a and B and D and e are CH Merge and form part of a Ring or a Heterocyclic aryl n with 5 or 6 members is hidroxialquilo alkyl; R4 or R5, heteroalquilo; heterocycle is haloalquilo, optionally substituted with an alkyl group, halogen, alkyl, amino, cyano, Nitro, aryl alkoxy,, Haloalcoxi - co2r7 - so2r8,,,NHC (R9) or - nhso2r9; or two groups together form a heterocycle containing 5 or 6 members, optionally substituted with one or more halogens and FUSED to the 6 members of the ring substituents (1); R6 is amino or alkoxy; R7 is H, alkyl, nhr10, R8 is nr10r11 or NH2. Alkyl aryl, Heterocyclic Or is aryl or heteroaryl amino; R9 and R10 and R11 each independently is an alkyl group,Alquenilo, alquinilo or aryl.
机译:权利要求1:式(1)化合物或其药学上可接受的盐,酯或前药,其中:N为1或2;和X为CH 2,s或CHF; r1是-n或-胆(o)C(o)N​​H(OH); R 2是烷基,烷氧基环烷基或烷基芳基,或R 2代表环烷基,其中与羰基相邻的C是环烷基环的一部分; R3为式(2)或(3)的取代基或四唑基哌啶子基2-或4-苯甲酰咪唑硫氰酸根合乙酸酯; NH,o,S或NR4在哪里; a,B,D和e各自独立选择的CHN或CR5; a和B,D和e为CH合并并形成环或杂环芳基的一部分,其中5或6元为环的是杂环基烷基; R4或R5,杂芳基;杂环是卤代烷基,任选地被烷基,卤素,烷基,氨基,氰基,硝基,芳基烷氧基,卤代烷氧基-co2r7-so2r8,NHC(R9)或-nhso2r9取代;或两个基团一起形成含有5或6个成员的杂环,该杂环任选地被一个或多个卤素取代,并稠合到环取代基(1)的6个成员上; R6是氨基或烷氧基; R 7为H,烷基,nhr 10,R 8为nr 10r11或NH 2。烷基芳基,杂环或为芳基或杂芳基氨基; R 9和R 10和R 11各自独立地为烷基,烷基,烷基或芳基。

著录项

  • 公开/公告号AR058769A1

    专利类型

  • 公开/公告日2008-02-20

    原文格式PDF

  • 申请/专利权人 NOVARTIS AG;

    申请/专利号AR2006P105821

  • 发明设计人

    申请日2006-12-27

  • 分类号C07D403/04;C07D403/14;C07D413/04;C07D413/14;C07D417/04;C07D471/04;C07D487/04;C07D498/04;C07D491/04;A61K31/4184;A61K31/437;A61K31/497;A61K31/416;A61K31/422;A61K31/424;A61K31/427;A61K31/357;A61P31/06;

  • 国家 AR

  • 入库时间 2022-08-21 20:08:57

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