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21. 发明授权

US6143740A Heregulin antagonists and methods for their use 失效
标题翻译：促胰岛素拮抗剂及其使用方法
公开(公告)号：US6143740A
公开(公告)日：2000-11-07
申请号：US308396
申请日：1999-08-16
申请人： Dajun Yang , Shaomeng Wang , Alan P. Kozikowski , Marc E. Lippman
发明人： Dajun Yang , Shaomeng Wang , Alan P. Kozikowski , Marc E. Lippman
IPC分类号： C07D498/18 , A61K31/34 , A61K31/395 , A61K31/495 , A61K31/496 , A61K31/551 , A61K31/655 , A61P35/00 , A61P43/00 , C07D498/08 , A61K31/33 , C07K1/00 , C07K16/00
CPC分类号： A61K31/708 , A61K31/395 , A61K31/495 , A61K31/496 , A61K31/551 , A61K31/655 , A61K31/704 , A61K31/7076 , C07D498/08
摘要： The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R.sub.1, and R.sub.2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.______________________________________ ##STR1## ______________________________________ Compounds R.sub.1 = ______________________________________ A1 --OH A2 --OH A3 --OH A4 --OH A5 --OH A6 --OH A7 --OH - A8 ##STR2## ______________________________________ Compounds R.sub.2 = ______________________________________ A1 #STR3## - A2 #STR4## - A3 #STR5## - A4 #STR6## - A5 #STR7## - A6 #STR8## - A7 #STR9## - A8 --H ______________________________________ Compounds IC.sub.50 (1) IC.sub.50 (2) ______________________________________ A1 10 uM 1 uM A2 10 uM 3 uM A3 10 uM 3 uM A4 50 uM 5 uM A5 >500 uM >50 uM A6 >500 uM >50 uM A7 >200 uM >50 uM A8 >500 M >50 uM ______________________________________
摘要翻译： PCT No.PCT / US97 / 21474 Sec。 371日期1999年8月16日 102（e）1999年8月16日PCT 1997年11月19日PCT公布。第WO98 / 21956号公报日期1998年5月28日本发明提供抑制癌细胞生长，从而治疗癌症的方法，包括向患有癌症的哺乳动物施用有效量的式（I）化合物，其中R1和R2的变量具有在本说明书中定义的含义。本发明还提供新的式（I）化合物以及可用于制备式（I）化合物的新型药物组合物和中间体。该图示出了本发明化合物和一些利福霉素类似物的结构和结合活性。 - 化合物R1 = -Al-OH-A2-OH-A3-OH-A4-OH-A5-OH-A6-OH-A7 -OH - - A8化合物R2 = 图像 - - A2 - - A3 - - A4 GE> - - A7 - - A8 -H - 化合物IC50（1）IC50（2） - A1 10 uM 1 uM - A2 10 uM 3 uM - A3 10 uM 3 uM - A4 50 uM 5 uM - A5> 500 uM> 50 uM - A6> 500 uM> 50 uM - A7> 200 uM> 50 uM - A8> 500 M> 50 uM -

22. 发明授权

US07910621B2 Small molecule antagonists of XIAP family proteins 失效
标题翻译： XIAP家族蛋白的小分子拮抗剂
公开(公告)号：US07910621B2
公开(公告)日：2011-03-22
申请号：US10594200
申请日：2005-03-22
申请人： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
发明人： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
IPC分类号： A61K31/352 , C07D311/30
CPC分类号： C07C235/84 , C07C50/28 , C07C50/30 , C07D311/30
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
摘要翻译：本发明涉及XIAP家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供了塞林和其他XIAP抑制剂以及使用这些化合物作为XIAP家族蛋白的抗凋亡作用的拮抗剂的方法。本发明还提供了治疗疾病和病理（例如肿瘤性疾病）的方法。

23. 发明授权

US07427689B2 ErbB-2 selective small molecule kinase inhibitors 失效
标题翻译： ErbB-2选择性小分子激酶抑制剂
公开(公告)号：US07427689B2
公开(公告)日：2008-09-23
申请号：US10343267
申请日：2001-07-30
申请人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
发明人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
IPC分类号： C07C205/00
CPC分类号： A61K31/216 , A61K31/00 , A61K31/192
摘要： A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(p-nitrophenyl)-2-propynoate.
摘要翻译：化合物的erbB-2激酶抑制的新方法通过计算建模和数据处理鉴定，和/或合理和从头药物设计提供了化合物结合erbB-2激酶分子，并且其可以用作erbB-2激酶激动剂或拮抗剂。这些化合物特别用于治疗癌症，特别是乳腺癌，并且可以单独使用或与其它化学治疗剂，特别是与赫氏原，人源化抗HER-2抗体或放射治疗组合使用。例示的具体化合物是“化合物B17”=甲基 - （对硝基苯基）-2-丙炔酸酯。

24. 发明申请

US20080021095A1 Small Molecule Antagonists of Xiap Family Proteins 失效
标题翻译：霞科家族蛋白的小分子拮抗剂
公开(公告)号：US20080021095A1
公开(公告)日：2008-01-24
申请号：US10594200
申请日：2005-03-22
申请人： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
发明人： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
IPC分类号： A61K31/353 , A61K31/122 , A61P35/00 , C07C49/603 , C07D311/30 , C12N5/06
CPC分类号： C07C235/84 , C07C50/28 , C07C50/30 , C07D311/30
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
摘要翻译：本发明涉及XIAP家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供了塞林和其他XIAP抑制剂以及使用这些化合物作为XIAP家族蛋白的抗凋亡作用的拮抗剂的方法。本发明还提供了治疗疾病和病理（例如肿瘤性疾病）的方法。

25. 发明申请

US20070219194A1 PHENYLALANINE DERIVATIVES 有权
标题翻译：苯乙烯胺衍生物
公开(公告)号：US20070219194A1
公开(公告)日：2007-09-20
申请号：US11749499
申请日：2007-05-16
申请人： Terrence Burke , Yang Gao , Zhu-jun Yao , Dajun Yang
发明人： Terrence Burke , Yang Gao , Zhu-jun Yao , Dajun Yang
IPC分类号： A61K31/5377
CPC分类号： C07K5/0819 , A61K38/00 , C07C271/22 , C07D265/32 , C07K5/0812 , C07K5/0827
摘要： The present invention provides phenylalanine derivatives that inhibit SH2 domain binding with a phosphoprotein. These derivatives include compounds of the formula: W—Y-(AA)n-Z wherein n is 0 to 15; Y is a phenylalanyl radical having a phenyl ring, an amine end, and a carboxyl end, the phenyl ring having one or more substituents, e.g., hydroxyl, carboxyl, formyl, carboxyalkyl, carboxyalkyloxy, dicarboxyalkyl, dicarboxyalkyloxy, dicarboxyhaloalkyl, dicarboxyhaloalkyloxy, and phosphonoalkyl, or phosphonohaloalkyl; W is a moiety attached to the nitrogen of Y and is, e.g., alkylcarbonyl, oxalyl, alkylaminooxalyl, arylaminooxalyl, arylalkylaminooxalyl, or alkoxyoxalyl; AA is an amino acid, the amine end of which is attached to the carboxyl end of Y; and Z is an arylalkylamino or arylheterocyclyl alkylamino; or a salt thereof; with the proviso that W is not arylalkylamino when the phenyl ring of phenylalanyl contains a phosphonoalkyl or phosphonohaloalkyl substituent at a position para to the alkylamido group and the ortho and meta positions are unsubstituted. The present invention further provides precursors suitable for preparing the phenylalanine derivatives and a method for the preparation of the precursors. The present invention further provides conjugates comprising a precursor and a conjugant that are covalently linked. These conjugates have biological and/or pharmacological properties.
摘要翻译：本发明提供抑制与磷蛋白结合的SH2结构域的苯丙氨酸衍生物。这些衍生物包括下式的化合物：其中n为0至15的W-Y-（AA）n-n -Z; Y是具有苯环，胺末端和羧基端的苯丙氨酰基，苯环具有一个或多个取代基，例如羟基，羧基，甲酰基，羧基烷基，羧基烷氧基，二羧基烷基，二羧基烷氧基，二羧基卤代烷基，二羧基卤代烷氧基和膦酰基烷基，或膦酰卤代烷基; W是连接到Y的氮的部分，例如烷基羰基，草酰基，烷基氨基草酰基，芳基氨基草酰基，芳基烷基氨基草酰基或烷氧基草酰基; AA是氨基酸，其末端连接到Y的羧基末端; Z是芳基烷基氨基或芳基杂环基烷基氨基; 或其盐; 条件是当苯丙氨酰基的苯环在烷基酰氨基的对位位置含有膦酰基烷基或膦酰卤代烷基取代基时，W不是芳烷基氨基，邻位和间位是未取代的。本发明还提供适用于制备苯丙氨酸衍生物的前体和前体的制备方法。本发明进一步提供包含共价连接的前体和共轭物的缀合物。这些缀合物具有生物学和/或药理学性质。

26. 发明授权

US07226991B1 Phenylalanine derivatives 有权
标题翻译：苯丙氨酸衍生物
公开(公告)号：US07226991B1
公开(公告)日：2007-06-05
申请号：US09937150
申请日：2000-03-23
申请人： Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
发明人： Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
IPC分类号： C07K5/08
CPC分类号： C07K5/0812 , A61K38/00 , C07K7/06
摘要： Disclosed herein are phenylalanine derivative compounds of the following formula W—Y—(AA)n—Z wherein Y is a phenylalanyl radical, AA is an amino acid, n is an integer of 1 to 15, and substituent variables W and Z are as described herein. The compounds can be used to inhibit SH2 binding with phosphoproteins, and to inhibit proliferation of tumor cells.
摘要翻译：本文公开的是下式的苯丙氨酸衍生物化合物：α-in-line-formula description =“In-line formula”end =“lead”？> WY-（AA）n -Z < -line-formula description =“In-line Formulas”end =“tail”？>其中Y是苯丙氨酰基，AA是氨基酸，n是1到15的整数，取代基变量W和Z如上所述这里。该化合物可用于抑制与磷蛋白结合的SH2，并抑制肿瘤细胞的增殖。

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