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21. 发明授权

US06649635B2 Heteroarylcarboxamide compounds active against protein tyrosine kinase related disorders 失效
公开(公告)号：US06649635B2
公开(公告)日：2003-11-18
申请号：US09948090
申请日：2001-09-07
申请人： Gerald McMahon , Peng Cho Tang , Laura Kay Shawver , Klaus Peter Hirth
发明人： Gerald McMahon , Peng Cho Tang , Laura Kay Shawver , Klaus Peter Hirth
IPC分类号： A61K31443
CPC分类号： C07D277/32 , C07D261/18 , C07D401/12 , C07D413/12
摘要： The present invention relates to novel heteroaryl-carboxamides which modulate the activity of protein tyrosine kinases and therefore are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders including cancer.

22. 发明授权

US06596878B2 Methods and compositions for inhibiting cell proliferative disorders 失效
标题翻译：用于抑制细胞增殖性疾病的方法和组合物
公开(公告)号：US06596878B2
公开(公告)日：2003-07-22
申请号：US09953933
申请日：2001-09-18
申请人： Hui Chen , Aviv Gazit , Alexander Levitzki , Klaus Peter Hirth , Elaina Mann , Laura K. Shawver , Jianming Tsai , Peng Cho Tang
发明人： Hui Chen , Aviv Gazit , Alexander Levitzki , Klaus Peter Hirth , Elaina Mann , Laura K. Shawver , Jianming Tsai , Peng Cho Tang
IPC分类号： C07D23138
CPC分类号： C07D241/52 , A61K31/245 , A61K31/277 , A61K31/415 , A61K31/4184 , A61K31/4402 , A61K31/498 , A61K31/517 , C07C229/60 , C07C255/36 , C07C255/37 , C07C255/41 , C07C255/42 , C07C255/66 , C07C311/27 , C07C317/46 , C07C327/44
摘要： The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.
摘要翻译：本发明涉及化合物及其抑制受体酪氨酸激酶活性的用途。本发明优选用于治疗细胞增殖性疾病，例如以过度活动或不适当活性HER2或EGFR为特征的癌症。

23. 发明授权

US5990141A Treatment of platelet derived growth factor related disorders such as cancers 失效
标题翻译：治疗血小板衍生生长因子相关疾病如癌症
公开(公告)号：US5990141A
公开(公告)日：1999-11-23
申请号：US370574
申请日：1995-01-06
申请人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers , Fairooz F. Kabbinavar , Dennis Slamon , Peng Cho Tang
发明人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers , Fairooz F. Kabbinavar , Dennis Slamon , Peng Cho Tang
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物也抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。下面描述特征化合物A10（参见图1a）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

24. 发明授权

US5958959A Treatment of platelet derived growth factor related disorders such as cancers 失效
标题翻译：治疗血小板衍生生长因子相关疾病如癌症
公开(公告)号：US5958959A
公开(公告)日：1999-09-28
申请号：US457051
申请日：1995-06-01
申请人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Axel Ullrich , Reiner Lammers
发明人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Axel Ullrich , Reiner Lammers
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDFG-R superfamily and are selective for members of the PDGF-R superfamily. The PDGF-R superfamily includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物还抑制PDFG-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。以下描述特征化合物A10（参见图1a）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

25. 发明授权

US5932602A Treatment of platelet derived growth factor related disorders such as cancers 失效
公开(公告)号：US5932602A
公开(公告)日：1999-08-03
申请号：US456735
申请日：1995-06-01
申请人： Klaus Peter Hirth , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Janis Haimichael , Axel Ullrich , Reiner Lammers
发明人： Klaus Peter Hirth , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Janis Haimichael , Axel Ullrich , Reiner Lammers
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50 , A61K31/175
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

26. 发明授权

US08143271B2 Compounds and methods for kinase modulation, and indications therefor 失效
公开(公告)号：US08143271B2
公开(公告)日：2012-03-27
申请号：US13216200
申请日：2011-08-23
申请人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Chao Zhang , Jiazhong Zhang , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Hanna Cho
发明人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Chao Zhang , Jiazhong Zhang , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Hanna Cho
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

27. 发明授权

US07202265B2 Indolinone combinatorial libraries and related products and methods for the treatment of disease 有权
标题翻译：吲哚酮组合文库及相关产品及治疗方法
公开(公告)号：US07202265B2
公开(公告)日：2007-04-10
申请号：US10784917
申请日：2004-02-24
申请人： Peng Cho Tang , Connie Li Sun , Gerald McMahon , Klaus Peter Hirth , Laura Kay Shawver
发明人： Peng Cho Tang , Connie Li Sun , Gerald McMahon , Klaus Peter Hirth , Laura Kay Shawver
IPC分类号： A61K31/404 , C07D403/06
CPC分类号： C07D209/34
摘要： The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1′ position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.
摘要翻译：本发明涉及能够调节，调节和/或抑制蛋白激酶信号转导的有机分子。这些化合物可用于治疗与未调节的蛋白激酶信号转导相关的疾病，包括细胞增殖性疾病如癌症，动脉粥样硬化，关节炎和再狭窄以及诸如糖尿病的代谢疾病。本发明具有抑制蛋白激酶及相关产物和方法的吲哚啉酮化合物。可以通过向3 - [（吲哚-3-基）亚甲基] -2-二氢吲哚酮，特别是在吲哚环的1'位置添加化学取代基来获得对FLK蛋白激酶特异性的抑制剂。特异性抑制FLK和血小板衍生生长因子蛋白激酶的吲哚酮化合物可以含有四氢吲哚或环戊基-b-吡咯部分。被取代基修饰的吲哚啉酮化合物，特别是在羟吲哚环的5位，可以有效地激活蛋白激酶。本发明还具有酪氨酸激酶抑制剂和相关产物和方法的新型水溶性吲哚啉酮化合物。

28. 发明授权

US06316479B1 Isoxazole-4-carboxamide compounds active against protein tryosine kinase related disorders 失效
标题翻译：对抗蛋白质软糖激酶相关疾病活性的异恶唑-4-甲酰胺化合物
公开(公告)号：US06316479B1
公开(公告)日：2001-11-13
申请号：US09081917
申请日：1998-05-19
申请人： Gerald McMahon , Peng Cho Tang , Laura Kay Shawver , Klaus Peter Hirth
发明人： Gerald McMahon , Peng Cho Tang , Laura Kay Shawver , Klaus Peter Hirth
IPC分类号： A61K3142
CPC分类号： C07D277/32 , C07D261/18 , C07D401/12 , C07D413/12
摘要： The present invention relates to novel isoxazole-4-carboxamides which modulate the activity of protein tyrosine kinases and therefore are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders including cancer.
摘要翻译：本发明涉及调节蛋白酪氨酸激酶活性的新型异恶唑-4-甲酰胺，因此预期可用于治疗包括癌症在内的异常蛋白酪氨酸激酶活性驱动的疾病。

29. 发明授权

US6147106A Indolinone combinatorial libraries and related products and methods for the treatment of disease 失效
公开(公告)号：US6147106A
公开(公告)日：2000-11-14
申请号：US915366
申请日：1997-08-20
申请人： Peng Cho Tang , Li Sun , Gerald McMahon , Klaus Peter Hirth , Laura Kay Shawver
发明人： Peng Cho Tang , Li Sun , Gerald McMahon , Klaus Peter Hirth , Laura Kay Shawver
IPC分类号： C07D209/34 , A61K31/404 , C07D403/06
CPC分类号： C07D209/34
摘要： The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1' position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.

30. 发明授权

US5942385A Method for molecular diagnosis of tumor angiogenesis and metastasis 失效
标题翻译：肿瘤血管生成和转移的分子诊断方法
公开(公告)号：US5942385A
公开(公告)日：1999-08-24
申请号：US624858
申请日：1996-03-21
申请人： Klaus Peter Hirth
发明人： Klaus Peter Hirth
IPC分类号： C12N15/09 , C12N5/08 , C12Q1/02 , C12Q1/68 , G01N33/53 , G01N33/574 , C12Q1/00 , C07H21/04
CPC分类号： C12Q1/6886 , C12Q2600/112
摘要： The invention is directed to methods of assessing the molecular stage of an disease characterized by abnormal angiogenesis. More particularly, the invention is directed to a method of determining the metastatic potential of a tumor by determining the presence of specific molecular markers. The invention is based in part on the discovery that the key marker for determining the eventual metastasis of a tumor is vascular endothelia growth factor. Knowledge of the particular markers present in a tumor condition allows the physician to tailor cancer treatment and manage the disease condition.
摘要翻译：本发明涉及评估以异常血管发生为特征的疾病的分子阶段的方法。更具体地，本发明涉及通过确定特定分子标记物的存在来确定肿瘤的转移潜力的方法。本发明部分基于用于确定肿瘤的最终转移的关键标记物是血管内皮生长因子的发现。了解存在于肿瘤状况中的特定标记物允许医师定制癌症治疗并控制疾病状况。

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