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Method for inhibiting the Enzyme beta lactamase Class D in the treatment of bacterial infection in a patient

机译:在患者的细菌感染治疗中抑制D类酶β内酰胺酶的方法

摘要

Penemes alkylidene 6 Tricyclic inhibitors of Enzymes with activity as a class D beta lactamase hydrolyse beta lactam Antibiotics, and as such serve as the primary cause of Bacterial Resistance when combined with beta lactam Antibiotics, the compounds of This provided an effective treatment against bacterial infections that threaten Life.Provided are compounds of formula (1) are useful for the treatment of bacterial infections that are associated with this Enzyme Class D: One, where a and B denote Hydrogen and optionally substituted heteroaryl FUSED tricyclic Group; and X is s or or.Claim 1: a method to inhibit Enzymes of Class D in the treatment of Class D to inhibit enzymes in the treatment of bacterial infection in a patient in need thereof, characterized by understanding provide an effective amount of a compound of formula (1),Where: one of a and B denote Hydrogen and the other a tricyclic FUSED heteroaryl Group optionally substituted; X is s or R5 is H, alkyl or cycloalkyl C1 - C5 - 6, 6 -, and alquiloc1 6chr30co; R3 is Hydrogen, alkyl C1 - C5 - 6 6, cycloalkyl, optionally substituted aryl or heteroaryl optional Mind replaced; or a pharmaceutically acceptable Salt or Ester is hydrolyzed in vivo.
机译:Penemesalkidene 6酶的三环抑制剂,具有D类内酰胺酶水解β-内酰胺抗生素的活性,因此与β-内酰胺抗生素结合使用时,是细菌耐药的主要原因,此化合物可有效抵抗细菌感染提供了威胁生命的式(1)化合物,其可用于治疗与该酶D类相关的细菌感染:一个,其中a和B表示氢和任选取代的杂芳基FUSED三环基团;权利要求1:在需要治疗的患者中抑制D类酶治疗D类酶以抑制酶治疗细菌感染的方法,其特征在于理解提供有效量的化合物式(1)中,a和B之一表示氢,另一个表示任选取代的三环FUSED杂芳基。 X是s或R5是H,烷基或环烷基C1-C5-6、6-和alquiloc1 6chr30co; R3为氢,烷基C1-C5-6,环烷基,任选取代的芳基或杂芳基任选被取代;或药学上可接受的盐或酯在体内水解。

著录项

  • 公开/公告号AR054467A1

    专利类型

  • 公开/公告日2007-06-27

    原文格式PDF

  • 申请/专利权人 WYETH;

    申请/专利号AR2006P102292

  • 申请日2006-06-01

  • 分类号A61K31/43;A61K31/424;A61K31/429;A61P31/04;

  • 国家 AR

  • 入库时间 2022-08-21 20:59:37

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