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1. 发明授权

US09278981B2 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：US09278981B2
公开(公告)日：2016-03-08
申请号：US14400987
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 , Erich Alois Spieser
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 , Erich Alois Spieser
IPC分类号： A61K31/4439 , C07D498/08 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D401/10 , C07D403/10 , C07D413/10 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/10 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/551 , A61K31/553 , A61K45/06 , C07D491/107
CPC分类号： C07D498/08 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/551 , A61K31/553 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/10 , C07D491/107
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 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，R，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。

2. 发明授权

US07977323B2 C2-C5-alkyl-imidazole-bisphosphonates 有权
标题翻译： C2-C5-烷基 - 咪唑 - 双膦酸盐
公开(公告)号：US07977323B2
公开(公告)日：2011-07-12
申请号：US12323696
申请日：2008-11-26
申请人： Sven Weiler , Leo Widler , Jean Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/02
CPC分类号： C07F9/6506
摘要： C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C2-C5-烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在药物制剂的制备中的用途，它们描述了用于治疗疾病，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。该化合物具有式I化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或盐。

3. 发明申请

US20090171639A1 Method to identify modulators for human 3alpha-hydroxysteroid dehydrogenase 审中-公开
标题翻译：识别人3α-羟基类固醇脱氢酶调节剂的方法
公开(公告)号：US20090171639A1
公开(公告)日：2009-07-02
申请号：US11823308
申请日：2007-06-26
申请人： Philipp Floersheim , Christian Ostermeier , Doncho Uzunov , Wolfgang Jahnke
发明人： Philipp Floersheim , Christian Ostermeier , Doncho Uzunov , Wolfgang Jahnke
IPC分类号： G06G7/58 , C12N9/04
CPC分类号： C12Q1/32 , G01N2500/04
摘要： 3 α-hydroxysteroid dehydrogenase (3α-HSD) plays a central role in the metabolism and action of steroid hormones and neurosteroids (steroids synthesized in the central nervous system). The high resolution structure of human type III 3α-HSD crystallized in complex with cofactor NADP is determined by X-ray diffraction. Furthermore the active site is determined. The structure coordinates of the enzyme may be used to design and select novel classes of modulators to human type III 3α-HSD.
摘要翻译： 3α-羟基类固醇脱氢酶（3alpha-HSD）在类固醇激素和神经甾体（在中枢神经系统中合成的类固醇）的代谢和作用中起着核心作用。通过X射线衍射测定与辅因子NADP复合结晶的人III型3α-HSD的高分辨率结构。此外，确定活性位点。酶的结构坐标可用于设计和选择人类III型3α-HSD的新型调节剂。

4. 发明申请

US20180134695A1 COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 审中-公开
公开(公告)号：US20180134695A1
公开(公告)日：2018-05-17
申请号：US15867679
申请日：2018-01-10
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： C07D417/14 , C07D487/10 , C07D401/14 , A61K31/427 , A61K31/5377 , A61K31/4025 , C07D417/10 , C07D409/14 , C07D401/04 , C07D413/14 , C07D405/14 , A61K45/06 , A61K31/4439 , C07D403/10 , A61K31/4155
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.

5. 发明申请

US20160185733A1 COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 审中-公开
公开(公告)号：US20160185733A1
公开(公告)日：2016-06-30
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 , C07D239/34 , C07D401/04 , 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 , A61K31/505
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.

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明申请

US20110257131A1 PHENYLALKYL-IMIDAZOLE-BISPHOSPHONATE COMPOUNDS 审中-公开
标题翻译：苯基 - 咪唑 - 二磷酸酯化合物
公开(公告)号：US20110257131A1
公开(公告)日：2011-10-20
申请号：US13141249
申请日：2009-12-21
申请人： Simona Cotesta , Wolfgang Jahnke , Jean-Michel Rondeau , Sven Weiler , Leo Widler
发明人： Simona Cotesta , Wolfgang Jahnke , Jean-Michel Rondeau , Sven Weiler , Leo Widler
IPC分类号： A61K31/675 , A61P19/00 , A61P43/00 , C07F9/572
CPC分类号： C07F9/6506
摘要： (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are disclosed. The compounds are able to inhibit excessive or inappropriate bone resorption. The compounds are of the formula I, wherein one of R1 and R2 are as defined in the specification, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译：（未取代或取代的苯基） - 烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在制备药物制剂中的用途，它们在疾病治疗中的应用，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。这些化合物能够抑制过量或不适当的骨吸收。化合物是式I化合物，其中R 1和R 2之一如说明书中所定义，并且可以为酯的形式的游离形式和/或盐。

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