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1. 发明授权

US6004967A Psoriasis treatment with quinazoline compounds 失效
标题翻译：用喹唑啉化合物治疗牛皮癣
公开(公告)号：US6004967A
公开(公告)日：1999-12-21
申请号：US927442
申请日：1997-09-11
申请人： Gerald McMahon , Laura Shawver , Blair Narog , Peng Cho Tang , Klaus Peter Hirth
发明人： Gerald McMahon , Laura Shawver , Blair Narog , Peng Cho Tang , Klaus Peter Hirth
IPC分类号： A61K31/517 , A61K31/505
CPC分类号： A61K31/517
摘要： This invention is directed to methods and compositions for treating hyperproliferative skin disorders utilizing a quinazoline derivative as an active ingredient.
摘要翻译：本发明涉及利用喹唑啉衍生物作为活性成分治疗过度增生性皮肤病的方法和组合物。

2. 发明授权

US06908930B2 4-substituted 7-AZA-indolin-2-ones and their use as protein kinase inhibitors 失效
标题翻译： 4-取代的7-AZA-二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途
公开(公告)号：US06908930B2
公开(公告)日：2005-06-21
申请号：US10622787
申请日：2003-07-21
申请人： Congxin Liang , Li Sun , Chung Chen Wei , Peng Cho Tang , Gerald McMahon , Klaus Peter Hirth , Jingrong Cui
发明人： Congxin Liang , Li Sun , Chung Chen Wei , Peng Cho Tang , Gerald McMahon , Klaus Peter Hirth , Jingrong Cui
IPC分类号： A61K31/437 , A61K31/519 , A61K31/5377 , A61P1/00 , A61P1/18 , A61P3/00 , A61P5/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/00 , A61P15/00 , A61P19/00 , A61P25/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1 and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.
摘要翻译：本发明涉及4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途。本文公开的特定的4-取代的7-氮杂 - 二氢吲哚-2-酮是式1及其药学上可接受的盐，溶剂合物，包合物和前药，其中R 1，R 2， R 3，R 3，R 4，X，Y和Z在本文中定义。本发明还涉及包含式1化合物的药物组合物和剂型，以及它们用于治疗和/或预防疾病例如但不限于癌症的方法。

3. 发明授权

US06696448B2 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors 失效
标题翻译： 3-（哌嗪基亚苄基）-2-二氢吲哚酮化合物和衍生物作为蛋白质酪氨酸激酶抑制剂
公开(公告)号：US06696448B2
公开(公告)日：2004-02-24
申请号：US10201593
申请日：2002-07-24
申请人： Peng Cho Tang , Li Sun , Gerald McMahon , Laura Kay Shawver , Klaus Peter Hirth
发明人： Peng Cho Tang , Li Sun , Gerald McMahon , Laura Kay Shawver , Klaus Peter Hirth
IPC分类号： A61K31496
CPC分类号： G06F13/4045
摘要： The present invention relates to novel 3-(piperazinyl-benylidenyl)-2-indolinone compounds and derivatives and physiologically acceptable salts thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及新的3-（哌嗪基 - 亚烯基）-2-二氢吲哚酮化合物及其衍生物及其生理上可接受的盐，其预期调节蛋白酪氨酸激酶的活性，因此可用于预防和治疗蛋白质酪氨酸激酶相关的细胞病症如癌症。

4. 发明授权

US06906093B2 Indolinone combinatorial libraries and related products and methods for the treatment of disease 失效
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：US06906093B2
公开(公告)日：2005-06-14
申请号：US09897755
申请日：2001-07-03
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 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D455/06 , C07D495/04 , G06F13/40 , A61K31/40 , C07D209/02
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D455/06 , C07D495/04 , G06F13/4045
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
摘要翻译：本发明涉及能够调节酪氨酸激酶信号转导以调节，调节和/或抑制异常细胞增殖的有机分子。

5. 发明授权

US06610688B2 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors 失效
标题翻译： 4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途
公开(公告)号：US06610688B2
公开(公告)日：2003-08-26
申请号：US09741737
申请日：2000-12-21
申请人： Congxin Liang , Li Sun , Chung Chen Wei , Peng Cho Tang , Gerald McMahon , Klaus Peter Hirth , Jingrong Cui
发明人： Congxin Liang , Li Sun , Chung Chen Wei , Peng Cho Tang , Gerald McMahon , Klaus Peter Hirth , Jingrong Cui
IPC分类号： C07D48704
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1 and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.
摘要翻译：本发明涉及4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途。本文公开的特定的4-取代的7-氮杂 - 二氢吲哚-2-酮是式1及其药学上可接受的盐，溶剂合物，包合物和前药，其中R1，R2，R3，R4，X，Y和Z如本文所定义。本发明还涉及包含式1化合物的药物组合物和剂型，以及它们用于治疗和/或预防疾病例如但不限于癌症的方法。

6. 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.

7. 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。

8. 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。

9. 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.

10. 发明授权

US5700822A 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：US5700822A
公开(公告)日：1997-12-23
申请号：US457047
申请日：1995-06-01
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。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。

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