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    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    6.
    发明申请
    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
    BROADSPECTRUM 2-（取代氨基） - 苯并噻唑磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：WO02081478A2

    公开(公告)日：2002-10-17

    申请号：PCT/EP0204012

    申请日：2002-04-09

    Applicant: TIBOTEC PHARM LTD ,  SURLERAUX DOMINIQUE LOUIS NEST ,  VENDEVILLE SANDRINE MARIE HELE ,  VERSCHUEREN WIM GASTON ,  DE BETHUNE MARIE-PIERRE T M M ,  DE KOCK HERMAN AUGUSTINUS ,  TAHRI ABDELLAH ,  ERRA SOLA MONTSERRAT

    Inventor： SURLERAUX DOMINIQUE LOUIS NEST ,  VENDEVILLE SANDRINE MARIE HELE ,  VERSCHUEREN WIM GASTON ,  DE BETHUNE MARIE-PIERRE T M M ,  DE KOCK HERMAN AUGUSTINUS ,  TAHRI ABDELLAH ,  ERRA SOLA MONTSERRAT

    IPC: A61K31/423 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07D263/58 ,  C07D413/04 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04

    CPC classification number: C07D413/04 ,  C07D263/58 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04

    Abstract: 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, Het1, Het2; R1 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-C1-6alkanediyl-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, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, 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; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 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.

    Abstract translation: 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各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3 -7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 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 -S（= O）2; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代的C 1 1-6; A是C 1-6烷二基，-C（= O） - ， - C（= S） - ， - S（= O）2 - ，C 1-6烷二基-C（= O） - ，C 1-6烷二基-C ） - 或C 1-6烷二基-S（= O）2 - ; R 5是H，OH，C 1-6烷基，Het 1 C 1-6烷基，Het 2 C 1-6烷基，任选取代的氨基C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 10，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在-A-不是C 1-6烷二基的情况下，则R6还可以是C 1-6烷基，Het 1 C 1-4烷基，Het 1 OC 1-4烷基，Het 2 C 1-4烷基，Het 2 OC 1-4烷基，芳基C 1-4烷基，芳基OC 1-4烷基或氨基C 1-4烷基; 其中R6的定义中的每个氨基可任选被取代; -A-R6是羟基C 1-6烷基; R5和-A-R6与它们所连接的氮原子一起也可以形成Het1或Het2。 它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。 它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

    AMINO NICOTINIC AND ISONICOTINIC ACID DERIVATIVES AS DHODH INHIBITORS
    8.
    发明申请
    AMINO NICOTINIC AND ISONICOTINIC ACID DERIVATIVES AS DHODH INHIBITORS 审中-公开
    氨基酸和异柠檬酸衍生物作为DHODH抑制剂

    公开(公告)号：WO2008077639A1

    公开(公告)日：2008-07-03

    申请号：PCT/EP2007/011401

    申请日：2007-12-21

    Applicant: LABORATORIOS ALMIRALL, S.A. ,  CASTRO PALOMINO LARIA, Julio Cesar ,  ERRA SOLA, Montserrat ,  LOZOYA TORIBIO, Maria Estrella ,  NAVARRO ROMERO, Eloisa

    Inventor： CASTRO PALOMINO LARIA, Julio Cesar ,  ERRA SOLA, Montserrat ,  LOZOYA TORIBIO, Maria Estrella ,  NAVARRO ROMERO, Eloisa

    IPC: C07D213/79 ,  C07D213/80 ,  A61K31/465 ,  A61P35/00

    CPC classification number: C07D213/79 ,  C07D213/80

    Abstract: A compound of formula (I) wherein : - one of the groups G 1 represents a nitrogen atom or a group CR c and the other represents a group CR c ; - G 2 represents a nitrogen atom or a group CR d ; - R 1 represents a group selected from hydrogen atoms, halogen atoms, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R 2 represents a group selected from hydrogen atoms, halogen atoms, hydroxyl groups, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R a , R b and R c independently represent groups selected from hydrogen atoms, halogen atoms, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R d represents a group selected from hydrogen atoms, halogen atoms, hydroxyl groups, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - one of the groups G 3 and G 4 is a nitrogen atom and the other is a CH group; - M is a hydrogen atom or an pharmaceutically acceptable cation with the proviso that, when at least one of the groups R a and R b represent a hydrogen atom and G 2 is a group CR d , then Rd represents a groups selected from C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, C 3-8 cycloalkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; and the pharmaceutically acceptable salts and N-oxides thereof.

    Abstract translation: 式（I）的化合物，其中：基团G 1中的一个表示氮原子或基团CR c，另一个表示基团CR ; G 2表示氮原子或基团CR 11; R 1表示选自氢原子，卤素原子，C 1-4烷基的基团，其可任选被1,2或3个选自卤素原子的取代基取代 和羟基，以及可以被1,2或3个选自卤素原子和羟基的取代基任选取代的C 3-8环烷基; R 2表示选自氢原子，卤素原子，羟基，C 1-4烷基的基团，其可任选被1,2或3个选自以下的取代基取代 可以任选被1,2或3个选自卤素原子和羟基的取代基取代的C 1-4烷氧基和C 3-8烷基， 可以任选地被1,2或3个选自卤素原子和羟基的取代基取代的环烷基; R a，R b和R c独立地表示选自氢原子，卤素原子，C 1-4烷基的基团， 可以任选被1,2或3个选自卤素原子和羟基的取代基取代的亚烷基，和可以被1,2或3个取代基任意取代的C 1-4烷氧基 选自卤素原子和羟基; -R d表示选自氢原子，卤素原子，羟基，C 1-4烷基的基团，其可任选被1,2或3个选自下列的取代基取代： 可以任选地被1,2或3个选自卤素原子和羟基的取代基取代的C 1-4烷氧基和C 3-8烷氧基， 其可任选被1,2或3个选自卤素原子和羟基的取代基取代; G 3和G 4之一是氮原子，另一个是CH基团; - M是氢原子或药学上可接受的阳离子，条件是当基团R a和R b中的至少一个表示氢原子时，G 2 是基团CR d，则Rd表示选自C 1-4烷氧基的基团，其可任选被1,2或3个取代基 选自卤素原子和羟基的取代基，可以任选被1,2或3个选自卤素原子和羟基的取代基取代的C 3-8环烷氧基; 及其药学上可接受的盐和N-氧化物。

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