首页> 外国专利> The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein RSUB1/SUB and RSUB8/SUB each are H, optionally substituted CSUB1-6/SUBalkyl, CSUB2-6/SUBalkenyl, CSUB3-7/SUBcycloalkyl, aryl, HetSUP1/SUP, HetSUP2/SUP; RSUB1/SUB may also be a radical of formula (RSUB11a/SUBRSUB11b/SUB)NC(RSUB10a/SUBRSUB10b/SUB)CRSUB9/SUB-; t is 0, 1 or 2; RSUB2/SUB is H or CSUB1-6/SUBalkyl; L is -C(=O)-, -O-C(=O)-, -NRSUB8/SUB-C(=O)-, -O-CSUB1-6/SUBalkanediyl-C(=O)-, -NRSUB8/SUB-CSUB1-6/SUBalkanediyl-C(=O)-, -S(=O)SUB2/SUB-, -O-S(=O)SUB2/SUB-, -NRSUB8/SUB

The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein RSUB1/SUB and RSUB8/SUB each are H, optionally substituted CSUB1-6/SUBalkyl, CSUB2-6/SUBalkenyl, CSUB3-7/SUBcycloalkyl, aryl, HetSUP1/SUP, HetSUP2/SUP; RSUB1/SUB may also be a radical of formula (RSUB11a/SUBRSUB11b/SUB)NC(RSUB10a/SUBRSUB10b/SUB)CRSUB9/SUB-; t is 0, 1 or 2; RSUB2/SUB is H or CSUB1-6/SUBalkyl; L is -C(=O)-, -O-C(=O)-, -NRSUB8/SUB-C(=O)-, -O-CSUB1-6/SUBalkanediyl-C(=O)-, -NRSUB8/SUB-CSUB1-6/SUBalkanediyl-C(=O)-, -S(=O)SUB2/SUB-, -O-S(=O)SUB2/SUB-, -NRSUB8/SUB

机译：本发明涉及具有式（I）的N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R _{1 和R _{8 分别为H，任选取代的C _{1-6 烷基，C _{2-6 烯基，C _{3-7 环烷基，芳基，Het < SUP> 1 ，Het ^{2 ; R _{1 也可以是式（R _{11a R _{11b ）NC（R _{10a R _{10b ）CR _{9 -; t是0、1或2; R _{2 是H或C _{1-6 烷基; L是-C（= O）-，-OC（= O）-，-NR _{8 -C（= O）-，-OC _{1-6 烷二基- C（= O）-，-NR _{8 -C _{1-6 烷二基-C（= O）-，-S（= O）_{2 -，-OS（= O）_{2 -，-NR _{8
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The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Rand Reach are H, optionally substituted Calkyl, Calkenyl, Ccycloalkyl, aryl, Het, Het; Rmay also be a radical of formula (RR)NC(RR)CR-; t is 0, 1 or 2; Ris H or Calkyl; L is -C(=O)-, -O-C(=O)-, -NR-C(=O)-, -O-Calkanediyl-C(=O)-, -NR-Calkanediyl-C(=O)-, -S(=O)-, -O-S(=O)-, -NR-S(=O); Ris Calkyl, aryl, Ccycloalkyl, CcycloalkylCalkyl, or arylCalkyl; Ris H, CalkylOC(=O), carboxyl, aminoC(=O), mono- or di(Calkyl)aminoC(=O), Ccycloalkyl, Calkenyl, Calkynyl or optionally substituted Calkyl; formula (II) is formula (III) or formula (IV) ; Rand Ris Calkenyl, Calkynyl, Ccycloalkyl or Calkyl, optionally substituted on one or more atoms; Rand Rmay also be hydrogen, aryl, Het, Het; Ris hydrogen or Calkyl optionally substituted on one ore more carbon atoms. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

机译：本发明涉及具有式（I）的化合物，其N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中Rand Reach为H，任选取代的C烷基，烯基，C环烷基，芳基，Het，Het ; R可能也是式（RR）NC（RR）CR-的基团; t是0、1或2;氢或C 1-4烷基; L是-C（= O）-，-OC（= O）-，-NR-C（= O）-，-O-烷二基-C（= O）-，-NR-烷二基-C（= O） -，-S（= O）-，-OS（= O）-，-NR-S（= O）; C 1 -C 6烷基，芳基，C环烷基，C环烷基C烷基或芳基C烷基;氢，C烷基OC（＝ O），羧基，氨基C（＝ O），单或二（C烷基）氨基C（＝ O），C环烷基，C烯基，炔基或任选取代的C烷基;式（II）为式（III）或式（IV）;任选地在一个或多个原子上取代的Rand Ris烯基，炔基，C环烷基或C烷基; Rand Rmay也可以是氢，芳基，Het，Het;氢或任选被一个或多个碳原子取代的C 1-6烷基。它还涉及它们作为广谱HIV蛋白酶抑制剂的用途，其制备方法以及包含它们的药物组合物和诊断试剂盒。它还涉及其与另一种抗逆转录病毒剂的组合，以及它们在测定中作为参考化合物或试剂的用途。

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公开/公告号EA010486B1

专利类型
公开/公告日2008-10-30

原文格式PDF
申请/专利权人 TIBOTECPHARMACEUTICALSLTD.;
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申请/专利号EA20050000350
发明设计人 TAHRIABDELLAH;WIGERINCKPIETTOMBERTPAUL;
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申请日2003-08-14
分类号C07D493/04;C07D209/34;A61K31/40;A61P31/18;
国家 EA
入库时间 2022-08-21 20:08:15

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