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1. 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。

2. 发明申请

US20090318410A1 IMIDAZOPYRIDAZINES AS LIPID KINASE INHIBITORS 审中-公开
标题翻译：作为脂质激酶抑制剂的咪唑吡啶
公开(公告)号：US20090318410A1
公开(公告)日：2009-12-24
申请号：US12442418
申请日：2007-10-29
申请人： Hans-Georg Capraro , Pascal Furet , Patricia Imbach , Frédéric Stauffer
发明人： Hans-Georg Capraro , Pascal Furet , Patricia Imbach , Frédéric Stauffer
IPC分类号： A61K31/5025 , C07D487/04 , A61K31/5377
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。

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。

5. 发明申请

US20090286779A1 PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS 审中-公开
标题翻译：作为脂质激酶抑制剂的吡唑并嘧啶
公开(公告)号：US20090286779A1
公开(公告)日：2009-11-19
申请号：US12442606
申请日：2007-09-27
申请人： Patricia Imbach , Frederic Stauffer , Pascal Furet , Hans-Georg Capraro
发明人： Patricia Imbach , Frederic Stauffer , Pascal Furet , Hans-Georg Capraro
IPC分类号： A61K31/5377 , C07D487/04 , C07D401/12 , C07D413/14 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to novel—at least 3,5-disubstituted-pyrazolo[1,5-a]pyrimidines of the formula I, wherein the symbols R1 to R4 are as defined in the specification, tautomers thereof or N-oxides thereof, or (preferably pharmaceutically acceptable) salts thereof, or hydrates or solvates thereof, as well as to related embodiments. The compounds are useful inter alia as protein kinase inhibitors, and thus e.g. useful in the treatment of diseases that respond to an inhibition of kinases of the PI3-kinase-related protein kinase family, especially lipid kinases and/or PI3 kinase (PI3K) and/or mTOR and/or DNA protein kinase and/or ATM and/or ATR and/or hSMG-1.
摘要翻译：本发明涉及式I的至少3,5-二取代 - 吡唑并[1,5-a]嘧啶，其中符号R1至R4如本说明书中所定义，其互变异构体或其N-氧化物，或（优选药学上可接受的）盐，或其水合物或溶剂化物，以及相关实施方案。所述化合物尤其可用作蛋白激酶抑制剂，可用于治疗响应抑制PI3激酶相关蛋白激酶家族，特别是脂质激酶和/或PI3激酶（PI3K）和/或mTOR和/或DNA蛋白激酶和/或ATM的激酶的疾病，以及 /或ATR和/或hSMG-1。

6. 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。

7. 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。

8. 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。

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

US20060058324A1 4-Amino-5-phenyl-7-cyclohexyl-pyrrolo 2,3-d pyrimidine derivatives 审中-公开
标题翻译： 4-氨基-5-苯基-7-环己基 - 吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US20060058324A1
公开(公告)日：2006-03-16
申请号：US10534427
申请日：2003-11-11
申请人： Hans-Georg Capraro , Pascal Furet , Carlos Garcia-Echeverria
发明人： Hans-Georg Capraro , Pascal Furet , Carlos Garcia-Echeverria
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04
摘要： The invention relates to new 4-amino-5-phenyl-7-cyclohexyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for 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 a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound, alone or in combination with one or more other pharmaceutically active compounds, for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.
摘要翻译：本发明涉及新的4-氨基-5-苯基-7-环己基 - 吡咯并[2,3-d]嘧啶衍生物，其制备方法，其在治疗人或动物体的方法中的应用，单独或与一种或多种其它药学活性化合物组合用于治疗疾病，特别是增殖性疾病如肿瘤疾病的用途，用于治疗哺乳动物，特别是人类中的这些疾病的方法，以及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特别是增殖性疾病如肿瘤的药物组合物（药物）的用途。

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