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    1H-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases
    1.
    发明授权
    1H-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases 有权
    1H-咪唑并[4,5-c]喹啉衍生物在治疗蛋白激酶依赖性疾病中的应用

    公开(公告)号：US07998972B2

    公开(公告)日：2011-08-16

    申请号：US10515126

    申请日：2003-05-20

    申请人： Carlos Garcia-Echeverria ,  Hans-Georg Capraro ,  Pascal Furet

    发明人： Carlos Garcia-Echeverria ,  Hans-Georg Capraro ,  Pascal Furet

    IPC分类号： A61K31/4166 ,  A61K31/4188 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoloquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.

    摘要翻译： 本发明涉及咪唑并喹啉及其盐在治疗蛋白激酶依赖性疾病中的用途，以及用于制备用于治疗所述疾病的药物制剂，用于治疗蛋白激酶依赖性疾病的咪唑并喹啉， 所述疾病包括将咪唑并喹啉给予包含咪唑并喹啉的温血动物，特别是用于治疗蛋白激酶依赖性疾病的新型咪唑并喹啉的药物制剂，以及制备新的咪唑并喹啉的方法。

    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors
    2.
    发明申请
    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors 审中-公开
    磺酰胺苯胺衍生物作为Janus激酶抑制剂

    公开(公告)号：US20080261973A1

    公开(公告)日：2008-10-23

    申请号：US12158764

    申请日：2006-12-20

    申请人： Hans-Georg Capraro ,  Bernard Coupez ,  Pascal Furet ,  Paul W. Manley ,  Carole Pissot Soldermann

    发明人： Hans-Georg Capraro ,  Bernard Coupez ,  Pascal Furet ,  Paul W. Manley ,  Carole Pissot Soldermann

    IPC分类号： C07D473/32 ,  C07D487/04 ,  A61K31/52 ,  A61K31/5377

    CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D487/04 ,  C07D519/00

    摘要： The invention relates to sulphonamidoanilines of formula I, wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R1 represents NR4R5 or OR4, wherein R4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R5 represents hydrogen or unsubstituted or substituted alky, or R4 and R5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R2 is hydrogen, lower alkenyl or alkyl, R3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of diseases, a method for the treatment of such a disease and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a proliferative disease.

    摘要翻译： 本发明涉及式I的磺酰氨基苯胺，其中A是N或CH，W，X，Y和Z是N或CH，条件是三个符号W，X和Y中的至少一个表示CH， 1表示NR 4 R 5或OR 4，其中R 4表示任选取代的烷基， 任选包含一个或两个氮原子或氧原子的任选取代的环烷基或取代的芳基，R 5表示氢或未取代或取代的烷基，或R 4和R 3， 与它们所连接的氮一起代表任选取代的五元或六元含氮单环，任选取代的含氮完全饱和双环，或含有一个或两个 氮原子，R 2是氢，低级烯基或烷基，R 3是未被取代的或被卤素单 - ，二 - 或三取代的烷基; 烯基或芳基，及其盐; 其制备方法，它们在人体或动物体内的治疗中的应用，单独使用或与一种或多种其它药学活性化合物组合用于治疗疾病，治疗这种疾病的方法和 使用这种化合物单独或与一种或多种其它药学活性化合物组合，用于制备用于治疗增殖性疾病的药物制剂。

    Antivirally active heterocyclic azahexane derivatives
    4.
    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。

    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。

    5-amino-4-hydroxyhexanoic acid derivatives
    6.
    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。