专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US5516772A K-252 derivatives which enhance neurotrophin-induced activity 失效
标题翻译：增强神经营养因子诱导活性的K-252a衍生物
公开(公告)号：US5516772A
公开(公告)日：1996-05-14
申请号：US307530
申请日：1994-09-16
申请人： Marcie A. Glicksman , Robert L. Hudkins , David P. Rotella , Nicola T. Neff , Chikara Murakata
发明人： Marcie A. Glicksman , Robert L. Hudkins , David P. Rotella , Nicola T. Neff , Chikara Murakata
IPC分类号： C07D487/22 , A61K31/40 , A61K31/407 , A61K31/55 , A61P21/02 , A61P25/00 , A61P25/16 , A61P25/28 , C07D487/14 , C07D498/22
CPC分类号： C07D487/14 , A61K31/40 , A61K31/55
摘要： Disclosed are derivatives of the indolocarbazole alkaloid K-252a of the Formulae I-VI, useful for enhancing neurotrophin-induced activity of neurotrophin responsive cells. A particularly preferred neurotrophin is NT-3, and a particularly preferred neurotrophin responsive cell is one which comprises a trk receptor. The enhanced neurotrophin-induced activity occasioned by the disclosed K-252a derivatives may be determined by the following assays: ChAT activity; DRG neuronal survival; or cell division (mitogenesis).
摘要翻译：公开了式I-VI的吲哚咔唑生物碱K-252a的衍生物，其可用于增强神经营养因子诱导的神经营养因子应答细胞的活性。特别优选的神经营养因子是NT-3，特别优选的神经营养因子应答细胞是包含_t受体的细胞因子。所公开的K-252a衍生物引起的增强的神经营养因子诱导的活性可以通过以下测定法测定：ChAT活性; DRG神经元存活; 或细胞分裂（mitogenesis）。

12. 发明授权

US5206400A Diastereomeric mono- and di-substituted diamino cyclohexane compounds and the method of preparation thereof 失效
标题翻译：非对映体单和二取代二氨基环己烷化合物及其制备方法
公开(公告)号：US5206400A
公开(公告)日：1993-04-27
申请号：US882258
申请日：1986-07-07
申请人： Donald T. Witiak , David P. Rotella
发明人： Donald T. Witiak , David P. Rotella
IPC分类号： C07C215/42 , C07F15/00
CPC分类号： C07C215/42 , C07F15/0093 , C07C2101/14
摘要： One aspect of the present invention relates to a process of making cyclohexane-1,2-di(O)-4,5-di(N) diastereomers which are useful as a synthons for various diastereoisomeric pharmaceutical systems. The present invention also relates to the stereoisomer compounds which are derived from retro-synthetic analysis. In another aspect, the present invention relates to novel antineoplastic Pt(II) complexes derived from the stereoisomers and the processes for making such Pt(II) complexes. Mono- and di-hydroxyl substitution on the cyclohexane ring renders the organoplatinum complex relatively more water soluble, thereby facilitating intravenous administration. The Pt(II) complexes of the present invention are less nephrotoxic than cisplatin and are readily excreted via the kidney due to their enhanced water solubility. In a composition aspect, the present invention encompasses novel pharmaceutical compositions comprising the novel Pt(II) complexes in an amount sufficient to have an antineoplastic effect in an animal or patient.
摘要翻译：本发明的一个方面涉及可用作各种非对映体药物体系的合成子的环己烷-1,2-二（O）-4,5-二（N）非对映异构体的方法。本发明还涉及衍生自复合分析的立体异构体化合物。另一方面，本发明涉及衍生自立体异构体的新型抗肿瘤性Pt（II）络合物和制备这种Pt（II）络合物的方法。环己烷环上的单羟基和二羟基取代使得有机铂复合物相对更易溶于水，从而便于静脉内给药。本发明的Pt（II）配合物与顺铂相比肾毒性较低，由于其水溶性增强，容易通过肾脏排出。在组合物方面，本发明包括新颖的药物组合物，其包含新颖的Pt（II）配合物，其量足以在动物或患者中具有抗肿瘤作用。

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