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1. 发明授权

US07998972B2 1H-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases 有权
标题翻译： 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。

2. 发明申请

US20080261973A1 Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors 审中-公开
标题翻译：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。

3. 发明授权

US07091346B1 Purine derivatives and processes for their preparation 失效
标题翻译：嘌呤衍生物及其制备方法
公开(公告)号：US07091346B1
公开(公告)日：2006-08-15
申请号：US09051827
申请日：1996-10-22
申请人： Jürg Zimmermann , Hans-Georg Capraro , Patricia Imbach , Pascal Furet
发明人： Jürg Zimmermann , Hans-Georg Capraro , Patricia Imbach , Pascal Furet
IPC分类号： C07D473/40 , C07D473/16 , A61K31/52 , A61P35/00 , A61P17/06
CPC分类号： C07D473/16
摘要： 2-Amino-6-anilino-purine derivatives of the formula 1 in which the symbols are as defined in claim 1 are described. These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and can be used for treatment of hyperproliferative diseases, for example tumour diseases.
摘要翻译：描述了其中符号如权利要求1中所定义的式1的2-氨基-6-苯胺基 - 嘌呤衍生物。这些化合物抑制p34cd2细胞周期蛋白Bclc13激酶，并可用于治疗过度增殖性疾病，例如肿瘤疾病。

4. 发明授权

US06300519B1 Antivirally active heterocyclic azahexane derivatives 有权
标题翻译：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. 发明授权

US6166004A Combinations of HIV protease inhibitors with reverse transcriptase inhibitors 有权
标题翻译： 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。

6. 发明授权

US5643878A 5-amino-4-hydroxyhexanoic acid derivatives 失效
标题翻译： 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。

7. 发明授权

US5354761A Bipyridyls 失效
标题翻译：联吡啶
公开(公告)号：US5354761A
公开(公告)日：1994-10-11
申请号：US69660
申请日：1993-06-01
申请人： Jaroslav Stanek , Giorgio Caravatti , Hans-Georg Capraro , Jorg Frei
发明人： Jaroslav Stanek , Giorgio Caravatti , Hans-Georg Capraro , Jorg Frei
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61P33/02 , C07D213/78 , C07D213/81 , C07D213/83 , C07D401/04
CPC分类号： C07D213/78 , C07D213/81 , C07D213/83
摘要： Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.
摘要翻译：其中Y，Z，S，S'，m，n和R 1 -R 4如说明书中所定义的式I化合物（I）具有有价值的药物性质，并且尤其对抗原生动物感染是有效的。它们是以本身已知的方式准备的。

8. 发明授权

US5238941A Arylhydrazones and pharmaceutical compositions thereof 失效
标题翻译：芳腙及其药物组合物
公开(公告)号：US5238941A
公开(公告)日：1993-08-24
申请号：US849262
申请日：1992-03-11
申请人： Jaroslav Stanek , Giorgio Caravatti , Jorg Frei , Hans-Georg Capraro
发明人： Jaroslav Stanek , Giorgio Caravatti , Jorg Frei , Hans-Georg Capraro
IPC分类号： C07C281/18 , C07C337/08 , C07D213/78 , C07D239/30 , C07D401/04
CPC分类号： C07D213/78 , C07C281/18 , C07C337/08 , C07D239/30 , C07D401/04
摘要： Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
摘要翻译：其中A，X 1，X 2，X 3，X 4，Y，Z和R 1至R 6具有说明书中给出的含义的式I化合物（I）具有有价值的药物性质，尤其对肿瘤有效。它们是以本身已知的方式准备的。

9. 发明申请

US20110301157A1 BICYCLIC AMIDES AS KINASE INHIBITORS 审中-公开
标题翻译：双酚A作为激酶抑制剂
公开(公告)号：US20110301157A1
公开(公告)日：2011-12-08
申请号：US13211765
申请日：2011-08-17
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andrea Vaupel , Carole Pissot Soldermann , Francois Gessier , Christian Schnell , Amanda Jane Littlewood-Evans , Prasad Koteswara Kapa , Joginder S. Bajwa , Xinglong Jiang
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andrea Vaupel , Carole Pissot Soldermann , Francois Gessier , Christian Schnell , Amanda Jane Littlewood-Evans , Prasad Koteswara Kapa , Joginder S. Bajwa , Xinglong Jiang
IPC分类号： A61K31/538 , A61K31/496 , A61K31/505 , C07D413/12 , C07D413/14 , C07D401/14 , C07D239/34 , A61K31/506 , C07D401/12 , A61P17/06 , A61P29/00 , A61P11/06 , A61P9/00 , A61P25/28 , A61P35/02 , A61P35/00 , C07D403/12 , A61P3/10 , A61P37/00 , A61P41/00 , A61K31/5377
CPC分类号： C07D239/47 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及式（I）化合物及其在治疗动物或人体中的用途，包括式I化合物的药物组合物和式I化合物在制备药物组合物中的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病。

10. 发明申请

US20100041662A1 Heterocyclic compounds as antiinflammatory agents 审中-公开
标题翻译：杂环化合物作为抗炎剂
公开(公告)号：US20100041662A1
公开(公告)日：2010-02-18
申请号：US12311393
申请日：2007-10-29
申请人： Sandrine Ferrand , Fraser Glickman , Catherine Leblanc , Cathy Ritchie , Duncan Shaw , Nikolaus Johannes Stiefl , Pascal Furet , Patricia Imbach , Frédéric Stauffer , Hans-Georg Capraro , François Gessier , Christoph Gaul , Pameia A. Albaugh , Greg Chopiuk
发明人： Sandrine Ferrand , Fraser Glickman , Catherine Leblanc , Cathy Ritchie , Duncan Shaw , Nikolaus Johannes Stiefl , Pascal Furet , Patricia Imbach , Frédéric Stauffer , Hans-Georg Capraro , François Gessier , Christoph Gaul , Pameia A. Albaugh , Greg Chopiuk
IPC分类号： A61K31/5025 , C07D487/00
CPC分类号： C07D487/04
摘要： A compound of Formula Ia or Ib in free or salt or solvate form, where R1, R2, R3, R4, R5 R20, R24, R25, X, Y and Z have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. These compounds are also useful for treating diseases mediated by the Pi3k receptor, the JAK-2 receptor and the TRK receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式Ia或Ib的游离或盐或溶剂合物形式的化合物，其中R1，R2，R3，R4，R5，R20，R24，R25，X，Y和Z具有说明书中指出的含义，可用于治疗疾病由ALK-5和/或ALK-4受体介导。这些化合物也可用于治疗由Pi3k受体，JAK-2受体和TRK受体介导的疾病。还描述了含有化合物的药物组合物和用于制备化合物的方法。

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