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41. 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。

42. 发明授权

US09315489B2 Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权
标题翻译：用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物
公开(公告)号：US09315489B2
公开(公告)日：2016-04-19
申请号：US14400990
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/04 , A61K31/4427 , C07D403/04 , C07D213/81 , C07D213/85 , C07D317/60 , C07D231/12 , C07D233/38 , C07D233/54 , C07D239/26 , C07D239/30 , C07D239/34 , C07D407/14 , C07D241/12 , C07D241/20 , C07D277/22 , A61K31/381 , A61K31/4025 , A61K31/4418 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D333/38
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式I化合物：其中Y，Y 1，Y 4，Y 5，Y 6，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

43. 发明申请

US20150141427A1 COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 有权
标题翻译：抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物
公开(公告)号：US20150141427A1
公开(公告)日：2015-05-21
申请号：US14400990
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D403/04 , A61K31/505 , C07D239/34 , C07D213/85 , A61K31/4418 , C07D241/20 , A61K31/4965 , C07D241/12 , C07D333/38 , A61K31/381 , A61K31/4025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D239/26
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式I化合物：其中Y，Y 1，Y 4，Y 5，Y 6，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

44. 发明申请

US20150126485A1 BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 有权
标题翻译：用于抑制ABL1，ABL2和BCR-ABL1活性的苯扎明星衍生物
公开(公告)号：US20150126485A1
公开(公告)日：2015-05-07
申请号：US14400992
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D417/14 , A61K31/427 , A61K45/06 , C07D401/14 , A61K31/4439 , A61K31/4025 , C07D413/14 , C07D409/14 , C07D401/04 , A61K31/5377 , C07D403/10 , C07D417/10 , C07D405/14
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制Abelson蛋白（ABL1），Abelson相关蛋白（ABL2）和相关嵌合蛋白（特别是BCR-ABL1）的酪氨酸激酶酶活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

45. 发明授权

US08829195B2 Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权
标题翻译：用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物
公开(公告)号：US08829195B2
公开(公告)日：2014-09-09
申请号：US13892769
申请日：2013-05-13
申请人： Stephanie Kay Dodd , Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Stephanie Kay Dodd , Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/00 , C07D211/72 , C07D211/84 , C07D211/56 , A01N43/40 , A61K31/44 , C07D405/14 , C07D401/10 , C07D401/04 , C07D213/82 , A61K45/06 , C07D403/10 , C07F9/58 , A61K31/4439 , A61K31/506 , C07D401/14
CPC分类号： C07D213/82 , A61K31/4439 , A61K31/506 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07F9/58
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式（I）化合物：其中Y，Y 1，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

46. 发明授权

US09896444B2 Benzamide derivatives for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权
公开(公告)号：US09896444B2
公开(公告)日：2018-02-20
申请号：US15075620
申请日：2016-03-21
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/14 , C07D417/14 , A61K31/4155 , C07D487/10 , C07D405/14 , C07D413/14 , C07D401/04 , C07D403/10 , C07D409/14 , C07D417/10 , A61K31/4025 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.

47. 发明授权

US09458112B2 Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权
标题翻译：用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物
公开(公告)号：US09458112B2
公开(公告)日：2016-10-04
申请号：US15060723
申请日：2016-03-04
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D239/26 , C07D401/04 , A61K31/505 , C07D239/34 , A61K31/506 , C07D241/20 , A61K31/4965 , C07D241/12 , C07D333/38 , A61K31/381 , C07D409/06 , A61K31/4025 , C07D233/56 , A61K31/4164 , C07D277/30 , A61K31/426 , C07D231/12 , A61K31/415 , C07D405/14 , A61K31/4439 , C07D403/04 , C07D317/60 , A61K31/36 , C07D333/22 , A61K31/5377 , A61K45/06
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.

48. 发明授权

US09340537B2 Benzamide derivatives for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权
标题翻译：用于抑制ABL1，ABL2和BCR-ABL1活性的苯甲酰胺衍生物
公开(公告)号：US09340537B2
公开(公告)日：2016-05-17
申请号：US14400992
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D417/10 , C07D417/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D403/10 , C07D409/14 , A61K31/4025 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译：本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制Abelson蛋白（ABL1），Abelson相关蛋白（ABL2）和相关嵌合蛋白（特别是BCR-ABL1）的酪氨酸激酶酶活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。

49. 发明授权

US07638523B2 Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors 有权
标题翻译：含二芳基胺的化合物和组合物，以及它们作为c-kit受体调节剂的用途
公开(公告)号：US07638523B2
公开(公告)日：2009-12-29
申请号：US11933030
申请日：2007-10-31
申请人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
发明人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
IPC分类号： A61K31/505 , A61K31/506 , A61P19/02 , A61P37/08 , A61P9/02 , A61P17/06 , A61P1/04 , A61P1/16 , A61P25/20 , C07D239/42 , C07D403/10 , C07D403/14
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
摘要翻译：本文描述的是包括二芳基胺结构特征的化合物。本文还描述了制备这种化合物的方法，使用这些化合物调节c-kit受体的活性的方法，以及包含这些化合物的药物组合物和药物。本文还描述了使用这些化合物，药物组合物和药物来治疗和/或预防和/或抑制和/或改善与c-kit受体活性相关的病理学和/或症状学疾病或病症的方法。

50. 发明授权

US07563894B2 Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors 有权
公开(公告)号：US07563894B2
公开(公告)日：2009-07-21
申请号：US11932945
申请日：2007-10-31
申请人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
发明人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
IPC分类号： C07D403/10 , C07D403/14 , C07D239/42 , A61K31/505
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

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