embedded imagewhere R1 is embedded imageM is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium (II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium (II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium (II):transporter ligand."/> Compound and method of treating neurogenic conditions using non-steroidal anti-inflammatory drug complexes
首页> 外国专利> Compound and method of treating neurogenic conditions using non-steroidal anti-inflammatory drug complexes

Compound and method of treating neurogenic conditions using non-steroidal anti-inflammatory drug complexes

机译:使用非甾体抗炎药复合物治疗神经源性疾病的化合物和方法

摘要

A complex is provided for the treatment of neurogenic conditions having the formula: embedded imagewhere R1 is embedded imageM is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium (II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium (II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium (II):transporter ligand.
机译:提供了一种用于治疗具有以下化学式的神经源性病症的复合物:<化学id =“ CHEM-US-00001”> <图像alt =“嵌入式图像” file =“ US20060142181A1-20060629-C00001.GIF” he =“ 12.11mm” id =“ EMI-C00001” imgContent =“ chem” imgFormat =“ GIF” wi =“ 52.24mm” /> 其中R 1 “嵌入式图像” M是金属离子Ca(II),Mg(II),Cu(II)或Ni(II); n是1或2的整数; R是BBB肽,转铁蛋白,膜转运蛋白肽,TAT肽,缓激肽,β-内啡肽,蛙皮素,降钙素,胆囊收缩素,脑啡肽,强啡肽,胰岛素,胃泌素,P物质,神经降压素,胰高血糖素,促胰液素,促生长素抑制素,胃动素,血管加压素,催产素,催乳素,促甲状腺素,血管紧张素,甘丙肽,神经肽Y,促甲状腺激素释放激素,促性腺激素释放激素,生长激素释放激素,黄体生成激素,血管活性肠肽葡萄糖酸盐,L-乳酸,L-亮氨酸,L-色氨酸和L-谷氨酸; R通过羧酸部分与M偶联。镁(II)代表优选的金属离子,因为已知镁具有神经保护作用。金属离子部分地被非甾族抗炎药螯合,该药物不抑制血小板活性,包括水杨酸盐和布洛芬酸盐。该复合物还包括在跨血脑屏障转运中起作用的配体。制备本发明络合物的方法包括将含有羧酸根基团的配体化学计量加入到金属离子的溶液中。在金属离子为镁(II)的情况下,非甾体抗炎配体:镁(II):转运体配体之间的化学计量比为1:1:1。

著录项

  • 公开/公告号US2006142181A1

    专利类型

  • 公开/公告日2006-06-29

    原文格式PDF

  • 申请/专利权人 LANDON C.G. MILLER;

    申请/专利号US20040023240

  • 发明设计人 LANDON C.G. MILLER;

    申请日2004-12-27

  • 分类号A61K38/28;A61K38/23;A61K38/11;

  • 国家 US

  • 入库时间 2022-08-21 21:46:31

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号