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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。
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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。
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公开(公告)号:US07855215B2
公开(公告)日:2010-12-21
申请号:US11575601
申请日:2005-09-27
申请人: Guido Bold , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W Manley , Carole Pissot Soldermann , Andrea Vaupel
发明人: Guido Bold , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W Manley , Carole Pissot Soldermann , Andrea Vaupel
IPC分类号: A61K31/505 , A61K31/506 , C07D239/02 , C07D401/12 , C07D413/12
CPC分类号: C07D417/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D417/14
摘要: The invention relates to novel compounds of Formula I: wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; A is CRc, S, NRc or O, where Rc is H or lower alkyl; X, Y and Z are each independently selected from N or C—R3, wherein at least two of X, Y and Z are N; and each Ra is independently selected from hydrogen and lower-alkyl; each Rb is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R1, R2, R3 and R4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diary urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
摘要翻译: 本发明涉及式I的新化合物:其中p是1,2或3; n为0,1,2或3; m为0,1,2或3; A是CRc,S,NRc或O,其中Rc是H或低级烷基; X,Y和Z各自独立地选自N或C-R 3,其中X,Y和Z中的至少两个是N; 并且每个R a独立地选自氢和低级烷基; 每个R b是氢或低级烷基; G是基团Ar或代表CN或未取代或取代的低级烷基; Ar是饱和或不饱和的环状基团,其是取代或未取代的,并且可以是五或六元单环或8,9,10,11或12元双环或三环,并且可以含有0,1,2或3个选自 来自O,N和S; 并且其中所述基团的R1,R2,R3和R4具有如本文所定义的含义,其盐,酯,N-氧化物或前药; 以及它们在治疗蛋白激酶依赖性疾病中的应用,它们在制备用于治疗所述疾病的药物组合物中的应用,用于治疗所述疾病的日用脲衍生物的使用方法,包含这些新型二芳基脲 衍生物,制备新型二芳基脲衍生物的方法,上述新型二芳基脲衍生物的使用或使用方法,和/或这些新型二芳基脲衍生物用于动物或人体的治疗。
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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。
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公开(公告)号:US20080039440A1
公开(公告)日:2008-02-14
申请号:US11575601
申请日:2005-09-27
申请人: Guido Bold , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul Manley , Carole Pissot Soldermann , Andrea Vaupel
发明人: Guido Bold , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul Manley , Carole Pissot Soldermann , Andrea Vaupel
IPC分类号: A61K31/506 , A61K31/496 , A61K31/55 , A61P35/00 , C07D401/12 , C07D403/12 , C07D413/14
CPC分类号: C07D417/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D417/14
摘要: The invention relates to novel compounds of Formula I: wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; A is CRc, S, NRc or O, where Rc is H or lower alkyl; X, Y and Z are each independently selected from N or C—R3, wherein at least two of X, Y and Z are N; and each Ra is independently selected from hydrogen and lower-alkyl; each Rb is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R1, R2, R3 and R4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diary urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
摘要翻译: 本发明涉及式I的新化合物:其中p是1,2或3; n为0,1,2或3; m为0,1,2或3; A是CR,C,NR C或O,其中R c是H或低级烷基; X,Y和Z各自独立地选自N或C-R 3,其中X,Y和Z中的至少两个为N; 并且每个R a a独立地选自氢和低级烷基; 每个R b是氢或低级烷基; G是基团Ar或代表CN或未取代或取代的低级烷基; Ar是饱和或不饱和的环状基团,其是取代或未取代的,并且可以是五或六元单环或8,9,10,11或12元双环或三环,并且可以含有0,1,2或3个选自 来自O,N和S; 并且其中基团具有R 1,R 2,R 3和R 4具有如本文所定义的含义 ,其盐,酯,N-氧化物或前药; 以及它们在治疗蛋白激酶依赖性疾病中的应用,它们在制备用于治疗所述疾病的药物组合物中的应用,用于治疗所述疾病的日用脲衍生物的使用方法,包含这些新型二芳基脲 衍生物,制备新型二芳基脲衍生物的方法,上述新型二芳基脲衍生物的使用或使用方法,和/或这些新型二芳基脲衍生物用于动物或人体的治疗。
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公开(公告)号:US20090137804A1
公开(公告)日:2009-05-28
申请号:US11570983
申请日:2005-06-23
申请人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul W. Manley , Joseph Schoepfer , Carsten Spanka
发明人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul W. Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号: A61K31/50 , C07D239/12 , A61P35/00
CPC分类号: C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译: 本发明涉及式(I)化合物,其中取代基X1,R1,R2,R3和R4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物 ,其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途,以及治疗这种疾病的方法。
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7.
公开(公告)号:US20080261973A1
公开(公告)日:2008-10-23
申请号:US12158764
申请日:2006-12-20
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。
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公开(公告)号:US08552002B2
公开(公告)日:2013-10-08
申请号:US11570983
申请日:2005-06-23
申请人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
发明人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号: A01N43/54 , C07D239/02
CPC分类号: C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译: 本发明涉及式(I)化合物,其中取代基X1,R1,R2,R3和R4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物 ,其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途,以及治疗这种疾病的方法。
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公开(公告)号:US20100305113A1
公开(公告)日:2010-12-02
申请号:US12599131
申请日:2008-05-07
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。
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10.
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。
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