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    Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors
    1.
    发明授权
    Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors 失效
    支链杂环取代苯基含磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07763641B2

    公开(公告)日：2010-07-27

    申请号：US10499221

    申请日：2002-12-20

    申请人： Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Abdellah Tahri ,  Samuel Leo Christiaan Moors ,  Montserrat Erra Sola

    发明人： Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Abdellah Tahri ,  Samuel Leo Christiaan Moors ,  Montserrat Erra Sola

    IPC分类号： A61K31/42 ,  A61K31/44 ,  A61K31/425 ,  C07D277/54

    CPC分类号： C07D231/12 ,  C07C311/18 ,  C07C2603/18 ,  C07D233/64 ,  C07D233/88 ,  C07D263/32 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, —(R7a)n—M—R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and —A—R6; and on (ii) a nitrogen atom if present by hydroxy or —A—R6. 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.

    摘要翻译： 本发明涉及具有式（I）的化合物，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Haryl是具有3至14个环成员的芳族单环，双环或三环杂环， 含有一个或多个选自氮，氧和硫的杂原子环成员，并且其可任选地在（i）一个或多个碳原子上被C 1-6烷基，卤素，羟基，任选单或二取代的氨基，硝基，氰基，卤代 烷基，羧基，C 3-7环烷基，任选的单或二取代的氨基羰基，甲硫基，甲基磺酰基，芳基， - （R 7a）n-M-R 7b，Het 1和Het 2; 其中任何氨基官能团上的任选取代基独立地选自R5和-A-R6; 和（ii）如果存在羟基或-A-R 6的氮原子。 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。

    BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    2.
    发明申请
    BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 有权
    BROADSPECTRUM 2-氨基苯并噻唑磺酰胺艾滋病毒蛋白酶抑制剂

    公开(公告)号：US20100029632A1

    公开(公告)日：2010-02-04

    申请号：US12575216

    申请日：2009-10-07

    申请人： Dominique Louis Nestor Ghislain SURLERAUX ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T.M.M.G. De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    发明人： Dominique Louis Nestor Ghislain SURLERAUX ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T.M.M.G. De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    IPC分类号： A61K31/5383 ,  A61K31/421 ,  C12N7/04 ,  A61K31/426 ,  A61K31/436 ,  A61K31/4439 ,  A61K31/505 ,  A61P31/12

    CPC分类号： C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula 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; R5 and R6 are H or C1-6alkyl. 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.

    摘要翻译： 本发明涉及具有式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） - ， - NR8-C（-O） - ， - O-C1-6烷二基-C（ - ） - ，-NR8-C1-6烷二基-C （-O） - ， - S（-O）2 - ， - O（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; R4是H，C1-4烷基OC（-O），羧基，氨基C（-O），单或二（C1-4烷基）氨基C（-O），C3-7环烷基，C2-6烯基，C2-6炔基或任选取代的C1 -6-烷基; R5和R6是H或C1-6烷基。 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。

    Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors
    5.
    发明授权
    Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors 有权
    Bropectpectrum 2-氨基 - 苯并恶唑磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07863306B2

    公开(公告)日：2011-01-04

    申请号：US12575216

    申请日：2009-10-07

    申请人： Dominique Louis Nestor Ghislain Surleraux ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T. M. M. G. De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    发明人： Dominique Louis Nestor Ghislain Surleraux ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T. M. M. G. De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    IPC分类号： A61K31/423

    CPC分类号： C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula 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; R5 and R6 are H or C1-6alkyl. 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.

    摘要翻译： 本发明涉及具有式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） - ， - O-C（= O） - ， - NR8-C（= O） - ， - O-C1-6烷二基-C（= O） - ，-NR8-C1-6烷二基 -C（= O） - ， - S（= O）2 - ， - O-S（= 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; R4是H，C1-4烷基OC（= O），羧基，氨基C（= O），单或二（C1-4烷基）氨基C（= O），C3-7环烷基，C2-6烯基，C2-6炔基或任选取代的C1 -6-烷基; R5和R6是H或C1-6烷基。 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。

    Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors
    6.
    发明授权
    Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors 失效
    Broadspecturm 2-氨基 - 苯并唑磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07622490B2

    公开(公告)日：2009-11-24

    申请号：US10474485

    申请日：2002-05-10

    申请人： Dominique Louis Nestor Ghislain Surleraux ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T. M. M. G De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    发明人： Dominique Louis Nestor Ghislain Surleraux ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T. M. M. G De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    IPC分类号： A61K31/423 ,  C07D263/58

    CPC分类号： C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula 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, C3-7 cycloalkyl, 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)—, —C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR9-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), C3-7 cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. 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.

    摘要翻译： 本发明涉及具有式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） - ， - C 1-6烷二基-C（ - ） - ， - NR 8 -C 1-6烷二基-C （-O）2 - ， - S（-O）2 - ， - NR 9 -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 C 1-6烷基; R5和R6是H或C1-6烷基。 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。

    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    7.
    发明申请
    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 失效

    公开(公告)号：US20070135447A1

    公开(公告)日：2007-06-14

    申请号：US11626183

    申请日：2007-01-23

    申请人： Dominique Louis SURLERAUX ,  Sandrine Marie Vendeville ,  Wim Gaston Verschueren ,  Marie Pierre De Bethune ,  Herman De Kock ,  Abdellah Tahri ,  Montserrat Erra Sola

    发明人： Dominique Louis SURLERAUX ,  Sandrine Marie Vendeville ,  Wim Gaston Verschueren ,  Marie Pierre De Bethune ,  Herman De Kock ,  Abdellah Tahri ,  Montserrat Erra Sola

    IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/427 ,  A61K31/423 ,  A61K31/4439

    CPC分类号： C07D413/04 ,  C07D263/58 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04

    摘要： The present invention concerns the compounds having the formula 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.

    (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
    9.
    发明授权
    (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
    （苯并二恶烷，苯并呋喃或苯并吡喃）衍生物

    公开(公告)号：US06495547B1

    公开(公告)日：2002-12-17

    申请号：US09641485

    申请日：2000-08-18

    申请人： Piet Tom Bert Paul Wigerinck ,  Wim Gaston Verschueren ,  Marc Francis Josephine Schroven ,  Marcel Frans Leopold De Bruyn

    发明人： Piet Tom Bert Paul Wigerinck ,  Wim Gaston Verschueren ,  Marc Francis Josephine Schroven ,  Marcel Frans Leopold De Bruyn

    IPC分类号： C07D40514

    CPC分类号： C07D405/12 ,  C07D405/14

    摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen. sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

    摘要翻译： 式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk1是任选被羟基，C 1-4烷氧基或C 1-4烷基羰基氧基取代的C 1-6烷二基; -Z1-Z2-是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻碳原子上时，R 1和R 2一起可以形成二价基; R4是氢或C1-6烷基; A是式-NR6-Alk2-（b-1）或-N-哌啶基 - （CH2）m（b-2）的二价基团，其中m是0或1; R5是一种基团，其中n是1或2; p1为0，p2为1或2; 或p1为1或2，p2为0; X是氧。 硫或= NR9; Y是氧或硫; R7是氢，C1-6烷基，C3-6环烷基，苯基或苯基甲基; R8是C1-6烷基，C3-6环烷基苯基或苯基甲基; R9是氰基，C1-6烷基，C3-6环烷基，C1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。 公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。