发明授权
EP1370543B1 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
有权
广谱2-(取代的氨基) - 苯并噻唑磺酰胺HIV蛋白酶抑制剂
- 专利标题: BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
- 专利标题(中): 广谱2-(取代的氨基) - 苯并噻唑磺酰胺HIV蛋白酶抑制剂
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申请号: EP02729930.4申请日: 2002-02-14
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公开(公告)号: EP1370543B1公开(公告)日: 2006-10-25
- 发明人: SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , GETMAN, Daniel , VERSCHUEREN, Wim, Gaston , VENDEVILLE, Sandrine , DE BETHUNE, Marie-Pierre , DE KERPEL, Jan, Octaaf, Antoon , MOORS, Samuel, Leo, Christiaan , DE KOCK, Herman, Augustinus , VOETS, Marieke, Christiane, Johanna
- 申请人: Tibotec Pharmaceuticals Ltd.
- 申请人地址: Unit 4, Block 4B, Blanchardstown Corporate Park Blanchardstown, Dublin 15 IE
- 专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人地址: Unit 4, Block 4B, Blanchardstown Corporate Park Blanchardstown, Dublin 15 IE
- 代理机构: Daelemans, Frank F.R.
- 优先权: EP01200529 20010214; US287758P 20010502
- 国际公布: WO2002083657 20021024
- 主分类号: C07D277/82
- IPC分类号: C07D277/82
摘要:
The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het?1, Het2; R¿1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8-C1-6?alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1-6alkanediyl-C(=O)-, C1-6alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2-; R5 is H, OH, C1-6alkyl, Het?1C¿1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het?1, Het1O, Het2, Het2¿O, aryl, arylO, C¿1-6?alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R?6¿ may also be C¿1-6?alkyl, Het?1C¿1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het?1 or Het2¿. 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.
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