专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2002096430A1 CEPHALOSPORIN DERIVATIVES AS ANTI-CANCER AGENTS 审中-公开
标题翻译： CEPHALOSPORIN衍生物作为抗癌剂
公开(公告)号：WO2002096430A1
公开(公告)日：2002-12-05
申请号：PCT/NL2002/000356
申请日：2002-05-31
申请人： KYLIX B.V. , BARKER, Nicholas , VON KRIES, Jens, Peter , BROHM, Dirk, Eckart , KRäMER, Timo, Alexander , STIEBER, Frank
发明人： BARKER, Nicholas , VON KRIES, Jens, Peter , BROHM, Dirk, Eckart , KRäMER, Timo, Alexander , STIEBER, Frank
IPC分类号： A61K31/54
CPC分类号： C07D501/00 , C07D279/06
摘要： The invention relates to a compound and/or pharmaceutically acceptable salts, esters, hydrates or solvates thereof, having the structural formula (1) or (2): (Please insert formulas 1 and 2)wherein:- X and Y are independently selected from the group comprising: H,C,N,O,S or alkyl,- W is selected from the group comprising: NH 2 , NH-R 1 , NH-CO-R 1 , NH-CO-Cn-O-R 1 , | R 4 NH-CO-Cn-R 1 , NH-CO-O-Cn-R 1 , NH-CO-Cn-S-R 1 , NH-CO-Cn-NH- R 1 | | | | R 4 R 4 R 4 R 4 wherein R 4 is optional, and n = 1-12, preferably 1-6 and more preferably 1-4- V is selected from the group comprising: H, C, N, O, S or a terminal alkyl group, whereby when V is a terminal alkyl group, X and R 2 are nothing,- Z is selected from the group comprising: S, S = O, O = S = O,- Q is selected from the group comprising: H, or R 1 , R 2 , R 3 , or R 4 - R 1 , R 2 , R 3 , or R 4 are independently selected from the group comprising: H, alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxycarbonyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl.
摘要翻译：本发明涉及具有结构式（1）或（2）的化合物和/或其药学上可接受的盐，酯，水合物或溶剂化物：（请插入式1和2）其中：-X和Y独立地选自所述基团包括：H，C，N，O，S或烷基，-W选自：NH 2，NH-R 1，NH-CO-R 1，NH-CO-Cn-O-R 1， R4 NH-CO-Cn-R1，NH-CO-O-Cn-R1，NH-CO-Cn-S-R1，NH-CO-Cn-NH-R1 | | | | R4 R4 R4 R4其中R4是任选的，n = 1-12，优选1-6，更优选1-4-V选自H，C，N，O，S或末端烷基，当V是末端烷基时，X和R 2不是-Z选自S，S = O，O = S = O，-Q选自H或R 1， R 2，R 3或R 4 -R 1，R 2，R 3或R 4独立地选自H，烷基，烯基，炔基，环烷基，烷氧基，烷氧基羰基，芳基，芳基烷基，杂芳基，杂环烷基。

2. 发明申请

WO0119353A3 AGENTS FOR TREATING HUMAN DISEASES, ESPECIALLY FOR TREATING TUMORS SUCH AS COLONIC CANCERS AND MELANOMAS OR FOR REGENERATING TISSUE AND PROMOTING HAIR GROWTH 审中-公开
标题翻译：手段治疗人类疾病，特别用于治疗肿瘤的治疗和HOW结肠癌黑素瘤或FOR再生组织和毛发生长。促进
公开(公告)号：WO0119353A3
公开(公告)日：2002-03-28
申请号：PCT/DE0003104
申请日：2000-09-07
申请人： MAX DELBRUECK CENTRUM , BIRCHMEIER WALTER , VON KRIES JENS PETER
发明人： BIRCHMEIER WALTER , VON KRIES JENS-PETER
IPC分类号： G01N33/50 , A61K31/05 , A61K31/06 , A61K31/122 , A61K31/136 , A61K31/336 , A61K31/40 , A61K31/402 , A61K31/4025 , A61K31/407 , A61K31/415 , A61K31/44 , A61K31/45 , A61K31/454 , A61K31/47 , A61K31/4725 , A61K31/4745 , A61K31/475 , A61K31/546 , A61K31/55 , A61K31/566 , A61K31/7008 , A61K38/00 , A61K38/17 , A61K45/00 , A61P17/14 , A61P35/00 , G01N33/15 , G01N33/53 , G01N33/566 , C07K14/47 , G01N33/574
CPC分类号： A61K31/47 , A61K31/415 , A61K31/44 , A61K38/1709
摘要： The invention relates to agents for treating human diseases which are based on substances that specifically influence the binding of beta -catenin on LEF-1/TCF- transcription factors, APC or conductin/axin. The invention particularly relates to the identification and use of hydrophobic pockets on the molecular surface in the proximity of the essential binding points for the binding partners of ss-catenin with the aim of optimizing these substances. The invention also relates to the use of the substances, preferably for treating tumors such as colonic cancers and melanomas or for regenerating tissue and promoting hair growth.
摘要翻译：本发明涉及用于药剂的人类疾病的物质的基础特异性影响β-连环蛋白的结合到LEF-1 / TCF转录因子，APC或conductin /轴蛋白上的治疗。特别地，它涉及鉴定和分子表面上使用的疏水口袋中必不可少的结合位点，β连环蛋白与这些物质最优化的目标结合配偶体的附近。本发明还涉及使用该物质，优选用于肿瘤如黑色素瘤和Kolonarazinomen或组织再生，和促进Haarwuches的的治疗。

3. 发明申请

WO9942481A3 AGENTS FOR TREATING HUMAN ILLNESSES BASED ON beta -CATENIN, AND THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：手段治疗人类疾病，起价从β-连环蛋白，生产和需求
公开(公告)号：WO9942481A3
公开(公告)日：2000-02-10
申请号：PCT/DE9900554
申请日：1999-02-22
申请人： MAX DELBRUECK CENTRUM , BIRCHMEIER WALTER , VON KRIES JENS PETER
发明人： BIRCHMEIER WALTER , VON KRIES JENS-PETER
IPC分类号： G01N33/53 , A61K38/00 , A61K45/00 , A61P17/14 , A61P35/00 , A61P43/00 , C07K14/47 , C07K19/00 , G01N33/543 , A61K38/17 , G01N33/00
CPC分类号： C07K14/4702 , A61K38/00
摘要： beta -catenin is a central molecule of the Wnt signal path. Increasing beta -catenin in the cell leads to the translocation in the cell nucleus and to the interaction with transcription factors of the LEF-1/TCF family. This can lead to colonic cancers and melenomas (oncogenic signal path). However, beta -catenin also interacts with the tumor-suppressor genes APC, conductin and E-cadherin which have a contrary effect on the cell (anti-oncogenic effect). The invention relates to peptides derived from LEF-1-/TCF-4-transcription factors and analogous molecules in the treatment of tumors, especially for treating colonic cancers and melanomas. These peptides and analogous molecules influence the interaction between beta -catenin and LEF-1/TCF. The invention can be used in the fields of pharmaceuticals and medicine. The invention essentially relates to peptides, said peptides comprising the parts of the LEF-1/TCF-4-transcription factors, and to the variants and mutations thereof. The peptides are preferably comprised of 10-40 amino acids from the N-terminal area of LEF-1 or TCF-4. The invention also relates to peptides or analogous molecules derived from the armadillo region of beta -catenin which were identified as interaction domains with LEF-1/TCF, APC, conductin and E-cadherin. These peptides or analogous molecules can likewise inhibit the interaction between beta -catenin and LEF-1/TCF, or in the case of APC or conductin, can increase the concentration of beta -catenin in the cell. These last molecules can be used in order to influence the formation of tissue and organs, for example, in order to promote hair growth.
摘要翻译： β-连环蛋白是Wnt信号传导途径的关键分子。在单元格中的β-连环蛋白的增加导致易位进入细胞核并与LEF-1 / TCF家族的转录因子相互作用。这可能会导致结肠癌和黑素瘤（致癌信号传导途径）。但β-联蛋白也与肿瘤抑制APC，Conductin和E-钙粘蛋白，其施加在细胞（抗致癌作用）产生不利影响相互作用。本发明涉及LEF-1 / TCF-4转录因子来源的肽和在肿瘤治疗类似物分子，特别是用于结肠癌和黑素瘤的治疗。这些肽和类似物分子影响β-连环蛋白和LEF-1 / TCF之间的相互作用。本发明的应用领域是医药工业和医药。本发明的一个重要组成部分是包括所述LEF-1 / TCF-4的转录因子，以及它们的变体和突变体的部分的肽。它们优选包括从LEF-1和TCF的N末端区域10-40个氨基酸。4 此外，本发明提供的肽或类似分子，选自β-连环蛋白的犰狳区域已被确定为相互作用结构域到LEF-1 / TCF，APC，E-cadherin和Conductin包括衍生。这些肽或类似物分子还可以抑制β-连环蛋白和LEF-1 / TCF，或之间的相互作用，如在APC或conductin的情况下，增加在细胞中β-连环蛋白的浓度。后面的这些分子可以用于影响组织和器官的形成，例如用于促进头发的生长。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式