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    Antivirally active heterocyclic azahexane derivatives
    2.
    发明授权
    Antivirally active heterocyclic azahexane derivatives 失效
    抗病毒活性杂环氮杂己烷衍生物

    公开(公告)号：US6110946A

    公开(公告)日：2000-08-29

    申请号：US108481

    申请日：1998-07-01

    申请人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20 ,  A01K31/44 ,  C07C241/00 ,  C07C261/00 ,  C07D277/04 ,  C07D401/00

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基， R4是通过环碳原子连接的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，亚硫酰基的杂原子 （-SO-）和磺酰基（-SO 2 - ），并且未被取代或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中所提及的含义之一，R 6独立地为R 1， 低级烷氧基羰基或其盐，条件是存在至少一个成盐基团。 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，可以用于例如艾滋病的治疗。 它们具有出色的药效学性质。

    Antivirally active heterocyclic azahexane derivatives
    4.
    发明授权
    Antivirally active heterocyclic azahexane derivatives 失效
    抗病毒活性杂环氮杂己烷衍生物

    公开(公告)号：US5849911A

    公开(公告)日：1998-12-15

    申请号：US831630

    申请日：1997-04-09

    申请人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20 ,  C07D241/02 ,  A61K31/42 ,  C07D263/34 ,  A61K277/54

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl, R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl, R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, and R.sub.6, independently of R.sub.1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述了式I *的化合物，其中R1是低级烷氧基羰基，R2是仲或低级低级烷基或低级烷硫基 - 低级烷基，R3是未被取代或被一个或多个低级烷氧基取代的苯基 自由基或C 4 -C 8环烷基，R 4是苯基或环己基，其各自在4-位上被不饱和杂环基取代，所述不饱和杂环基通过环碳原子键合，具有5至8个环原子，含有1至4个选自 氮，氧，硫，亚磺酰基（-SO-）和磺酰基（-SO 2 - ），并且是未取代的或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2所提及的含义之一， R6独立地为R1，是低级烷氧基羰基或其盐，条件是存在至少一个成盐基团。 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，可以用于例如艾滋病的治疗。 它们具有出色的药效学性质。

    Combinations of HIV protease inhibitors with reverse transcriptase inhibitors
    5.
    发明授权
    Combinations of HIV protease inhibitors with reverse transcriptase inhibitors 有权
    HIV蛋白酶抑制剂与逆转录酶抑制剂的组合

    公开(公告)号：US6166004A

    公开(公告)日：2000-12-26

    申请号：US399627

    申请日：1999-09-20

    申请人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20 ,  A61K31/435 ,  A61K31/41 ,  A61K31/425 ,  C07D257/06 ,  C07D277/02

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基， R4是通过环碳原子连接的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，亚硫酰基的杂原子 （-SO-）和磺酰基（-SO 2 - ），并且未被取代或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中所提及的含义之一，R 6独立地为R 1， 低级烷氧基羰基或其盐，条件是存在至少一个成盐基团。 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，可以用于例如艾滋病的治疗。 它们具有出色的药效学性质。

    Antivirally active heterocyclic azahexane derivatives
    7.
    发明授权
    Antivirally active heterocyclic azahexane derivatives 有权
    抗病毒活性杂环氮杂己烷衍生物

    公开(公告)号：US06300519B1

    公开(公告)日：2001-10-09

    申请号：US09448328

    申请日：1999-11-23

    申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C20904

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基，R 4 是通过环碳原子键合的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，脯氨酰基的杂原子（ -SO-）和磺酰基（-SO 2 - ），并且是未取代的或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中提及的含义之一，R 6独立地为R 1，为低级烷氧基羰基 或其盐，条件是存在至少一种成盐基团。化合物是天冬氨酸逆转录病毒蛋白酶的抑制剂，并且可以用于例如AIDS的治疗。 它们具有出色的药效学性质。

    5-amino-4-hydroxyhexanoic acid derivatives
    8.
    发明授权
    5-amino-4-hydroxyhexanoic acid derivatives 失效
    5-氨基-4-羟基己酸衍生物

    公开(公告)号：US5643878A

    公开(公告)日：1997-07-01

    申请号：US207646

    申请日：1994-03-08

    申请人： Guido Bold ,  Marc Lang ,  Alexander Fassler ,  Hans-Georg Capraro ,  Shripad Bhagwat ,  Peter Schneider ,  Peter van Hoogevest

    发明人： Guido Bold ,  Marc Lang ,  Alexander Fassler ,  Hans-Georg Capraro ,  Shripad Bhagwat ,  Peter Schneider ,  Peter van Hoogevest

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/02 ,  A61K31/535 ,  C07P265/06

    CPC分类号： C07K5/0207 ,  C07K7/02 ,  A61K38/00

    摘要： Compounds of formula I ##STR1## or their hydroxy-protected derivatives, and compounds of formula I' ##STR2## wherein T is an acyl radical of formula Z ##STR3## wherein R.sup.z is unsubstituted or substituted hydrocarbyl wherein at least one carbon atom has been replaced by a hetero atom with the proviso that a hetero atom is not bonded directly to the carbonyl to which the radical R.sup.z is bonded, alkyl having two or more carbon atoms, lower alkenyl, lower alkynyl, aryl or unsubstituted or substituted amino, and wherein the radicals R.sub.1, B.sub.1, R.sub.2, R.sub.3, A.sub.1, A.sub.2 and NR.sub.4 R.sub.5 are as defined in the description, and precursors thereof, are described. The compounds have pharmaceutical activity, for example in the treatment of retroviral diseases, such as AIDS.

    摘要翻译： 式I化合物（I）或其羟基保护的衍生物和式I'化合物（I'）其中T是式Z的酰基（Z），其中R z是未取代的或 取代的烃基，其中至少一个碳原子已经被杂原子替代，条件是杂原子不直接键合到与基团Rz键合的羰基上，具有两个或更多个碳原子的烷基，低级链烯基，低级炔基 ，芳基或未取代或取代的氨基，并且其中基团R 1，B 1，R 2，R 3，A 1，A 2和NR 4 R 5如说明书中所定义，及其前体。 该化合物具有药物活性，例如用于治疗逆转录病毒疾病，例如艾滋病。

    Intermediates for the preparation of peptide analogues
    9.
    发明授权
    Intermediates for the preparation of peptide analogues 失效
    用于制备肽类似物的中间体

    公开(公告)号：US5912352A

    公开(公告)日：1999-06-15

    申请号：US866558

    申请日：1997-05-30

    申请人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Heinz Steiner

    发明人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Heinz Steiner

    IPC分类号： C07C241/02 ,  C07C253/16 ,  C07C255/44 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D213/54 ,  C07D213/55 ,  C07D257/04 ,  C07D277/22 ,  C07D277/30 ,  C07D213/02

    CPC分类号： C07D213/42 ,  C07C253/16 ,  C07C255/44 ,  C07C281/02 ,  C07C281/04 ,  C07D213/54 ,  C07D213/55 ,  C07D257/04 ,  C07D277/30 ,  C07B2200/07 ,  Y02P20/55

    摘要： The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a suitable amino-protecting group,R.sub.2 is unsubstituted or substituted alkyl,R.sub.3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl,R.sub.4, independently of R.sub.1, is hydrogen or a suitable amino-protecting group andm is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds.The precursor is an oxo compound,which is in turn prepared by hydrogenation with a suitable complex hydride or with hydrogen in the presence of a suitable catalyst and acyl migration starting from a hydrazone,which is in turn preferably prepared from a nitrile via an imino compound by means of hydrogenation and reaction with a hydrazine derivative,which is prepared from an aldehyde by reaction with a reactive derivative of a carboxylic acid in the presence of a cyanide salt;and the novel intermediates required therefor.

    摘要翻译： 本发明涉及一种制备式I化合物的新方法，其中R 1为氢或适当的氨基保护基，R 2为未取代或取代的烷基，R 3为氢，芳基，杂环基，未取代或取代的烷基或未取代或取代的 环烷基，独立于R 1的R 4是氢或合适的氨基保护基，m是1至7的数; 并且其中可以存在其它合适的官能团保护基团; 哪些化合物是抗病毒活性的或可以用作药物活性的起始原料，特别是抗病毒化合物。 前体是氧代化合物，其又通过在合适的催化剂存在下用合适的络合氢化物或氢气氢化制备，并且从腙开始进行酰基迁移，其又优选通过亚氨基化合物由腈制备 通过氢化和与肼衍生物反应，肼衍生物通过与氰化物的存在下与羧酸的反应性衍生物反应由醛制备; 和所需的新型中间体。

    Azahexane derivatives as substrate isosters of retroviral asparate proteases
    10.
    发明授权
    Azahexane derivatives as substrate isosters of retroviral asparate proteases 失效
    氮杂己烷衍生物作为逆转录病毒天冬氨酸蛋白酶的底物等价物

    公开(公告)号：US06225345B1

    公开(公告)日：2001-05-01

    申请号：US09068876

    申请日：1998-05-21

    申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

    发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

    IPC分类号： A61K3127

    CPC分类号： C07C271/22 ,  Y10S514/934

    摘要： The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen; or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.

    摘要翻译： 本发明涉及式（I）化合物：其中R 1和R 10各自独立地为低级烷氧基羰基; R 2，R 3和R 4各自独立地为C 1 -C 4烷基，R 7，R 8和R 9各自选自氢和C 1 -C 4烷基，不超过2个基团为氢; 或R 7，R 8和R 9各自独立地为C 1 -C 4烷基，R 2，R 3和R 4各自选自氢和C 1 -C 4烷基，其中1或2个是氢; R5是苯基或环己基; R6为苯基或氰基苯基; 或其盐; 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，并且是有效的，例如针对HIV。