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1. 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。

2. 发明申请

US20080287427A1 Bicyclic Amides as Kinase Inhibitors 有权
标题翻译：双环酰胺作为激酶抑制剂
公开(公告)号：US20080287427A1
公开(公告)日：2008-11-20
申请号：US11575025
申请日：2005-09-14
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andreas 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 , Andreas Vaupel , Carole Pissot Soldermann , Francois Gessier , Christian Schnell , Amanda Jane Littlewood-Evans , Prasad Koteswara Kapa , Joginder S. Bajwa , Xinglong Jiang
IPC分类号： A61K31/5377 , C07D403/12 , A61K31/506 , C07D213/72 , C07D413/02
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 en 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。

3. 发明授权

US08026247B2 Bicyclic amides as kinase inhibitors 有权
标题翻译：双环酰胺作为激酶抑制剂
公开(公告)号：US08026247B2
公开(公告)日：2011-09-27
申请号：US11575025
申请日：2005-09-14
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andrea Vaupel
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andrea Vaupel
IPC分类号： C07D239/46 , C07D403/12 , C07D413/12 , A61K31/505
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。

4. 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。

5. 发明授权

US07323469B2 7H-pyrrolo[2,3-d]pyrimidine derivatives 失效
标题翻译： 7H-吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07323469B2
公开(公告)日：2008-01-29
申请号：US10783000
申请日：2004-02-20
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
IPC分类号： A61K31/519 , A61K31/497 , C07D487/04 , A61P35/04
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
摘要翻译：本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

6. 发明申请

US20100305113A1 Substituted Imidazopyridazines as Lipid Kinase Inhibitors 审中-公开
标题翻译：取代的咪唑并哒嗪作为脂质激酶抑制剂
公开(公告)号：US20100305113A1
公开(公告)日：2010-12-02
申请号：US12599131
申请日：2008-05-07
申请人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet
发明人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet
IPC分类号： A61K31/542 , C07D487/04 , A61K31/5025 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P37/08 , A61P9/00
CPC分类号： C07D487/04
摘要： The invention relates to novel compounds of the formula I, as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.
摘要翻译：本发明涉及式I的新化合物以及与这些化合物有关的其它发明实施方案。化合物是例如鉴于其抑制蛋白激酶（例如PI3激酶）的能力，可用于动物或人体的治疗。

7. 发明申请

US20080262021A1 1H-Imidazoquinoline Derivatives as Prote In Kinase Inhibitors 审中-公开
标题翻译： 1H-咪唑并喹啉衍生物作为激酶抑制剂中的蛋白质
公开(公告)号：US20080262021A1
公开(公告)日：2008-10-23
申请号：US10579587
申请日：2004-11-19
申请人： Hans-Georg Capraro , Giorgio Caravatti , Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Frederic Stauffer
发明人： Hans-Georg Capraro , Giorgio Caravatti , Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Frederic Stauffer
IPC分类号： A61K31/4745 , C07D471/04 , A61P35/04
CPC分类号： C07D471/04
摘要： The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; 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：本发明涉及用于治疗蛋白激酶依赖性疾病的式（I）的咪唑并喹啉; 包含咪唑并喹啉的药物制剂，特别是用于治疗蛋白激酶依赖性疾病; 新型咪唑并喹啉; 以及制备新的咪唑并喹啉的方法。

8. 发明申请

US20100311729A1 Substituted imidazopyridazines and pyrrolopyrimidines as lipid kinase inhibitors 审中-公开
标题翻译：取代的咪唑并哒嗪和吡咯并嘧啶作为脂质激酶抑制剂
公开(公告)号：US20100311729A1
公开(公告)日：2010-12-09
申请号：US12599143
申请日：2008-05-09
申请人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet , Jiong Lan , Sabrina Pecchi , Joseph Schoepfer
发明人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet , Jiong Lan , Sabrina Pecchi , Joseph Schoepfer
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/5025 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.
摘要翻译：本发明涉及式I化合物，其制备方法，更一般地，这些用于治疗人或动物体的化合物，用于治疗炎性或阻塞性气道疾病，通常在连接中发生的疾病移植或增殖性疾病，该疾病对PI3激酶相关蛋白激酶家族的激酶的抑制作出反应。

9. 发明授权

US06767906B2 2-amino-6-anilino-purines and their use as medicaments 失效
标题翻译： 2-氨基-6-苯胺基嘌呤及其作为药物的用途
公开(公告)号：US06767906B2
公开(公告)日：2004-07-27
申请号：US09927322
申请日：2001-08-10
申请人： Patricia Imbach , Hans-Georg Capraro , Jürg Zimmermann , Giorgio Caravatti , Pascal Furet , Wolfgang Karl-Diether Brill
发明人： Patricia Imbach , Hans-Georg Capraro , Jürg Zimmermann , Giorgio Caravatti , Pascal Furet , Wolfgang Karl-Diether Brill
IPC分类号： C07D47316
CPC分类号： C07D473/16 , C07D473/40
摘要： This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R1 is &agr;) —S(═O)k—NR6R7, in which k is 1 or 2, wherein under the proviso that R6 and R7 cannot be simultaneously hydrogen &agr;1) R6, R7 can be identical or different from one another and represent an aliphatic, carbocyclic, heterocyclic, carbocyclic-aliphatic or heterocyclic-aliphatic radical; hydrogen or lower aliphatic acyl; or &agr;2) R6 and R7 together are an alkylene or alkenylene radical having from 3 up to and including 9 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen, &bgr;) N-(aryl lower alkyl)carbamoyl, or &ggr;) a radical of the formula —NH—S(═O)i—R8, in which i is 1 or 2, R8 is an aliphatic, carbocyclic or heterocyclic radical; or &dgr;) a radical of the formula —NH—C(═O)—R9, and the other variable substituents are as defined herein. The inventive compounds inhibit p34cdc2/cyclin Bcdc13 kinase and protein tyrosine kinase pp60c-src and can be used for treatment of hyperproliferative diseases, for example tumour diseases, and diseases which respond to inhibition of the activity of protein tyrosine kinase pp60c-src, in particular osteoporosis.
摘要翻译：本申请公开了式Iin的2-氨基-6-苯胺基 - 嘌呤衍生物，其中q是1-5，和R1是α）-S（= O）k-NR6R7，其中k是1或2，其中在条件是R6和 R7不能同时为氢α1）R6，R7可以相同或不同，代表脂族，碳环，杂环，碳环脂族或杂环脂族基; 氢或低级脂族酰基; 口服α2）R6和R7一起是具有3个至多且包括9个C原子的亚烷基或亚烯基，其中1-3个C原子可以被氧，硫或氮取代，β）N-（芳基低级烷基）氨基甲酰基（= O）i-R8的基团，其中i为1或2，R8为脂族，碳环或杂环基; 顺式）式-NH-C（= O）-R9的基团，其它可变取代基如本文所定义。本发明化合物抑制p34 /细胞周期蛋白B 激酶和蛋白酪氨酸激酶pp60 ，并且可用于治疗过度增殖性疾病，例如肿瘤疾病和对抑制活性的疾病蛋白酪氨酸激酶pp60 ，特别是骨质疏松症。

10. 发明授权

US07390805B2 4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives 失效
标题翻译： 4-氨基-6-苯基 - 吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07390805B2
公开(公告)日：2008-06-24
申请号：US11686023
申请日：2007-03-14
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
IPC分类号： C07D413/10 , C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/497 , A06P35/04
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
摘要翻译：本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

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