embedded image ;where R1 in each occurrence is independently H, or C1-C4 alkyl; R2 is a nullity or CH—CH3, R3 is a nullity or C(O)—R6—NH; R6 is C2-C6 alkyl, (CH2CH2—O)n, or (CH(OH)CH2)n; n is an integer of between 1 and 4; R4 is a nullity or NH—R6—C(O); and R5 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, endocannabinoids 1 & 2, 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 peptide transferrin, glucosyl ester, lactic acid, leucine, tryptophan, glutamic acid."/> AMANTADINE, MEMANTINE, AND RIMANTADINE CONJUGATES AND A PHARMACEUTICAL COMPOSITION FOR TREATMENT OF NEURONAL DISORDERS
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AMANTADINE, MEMANTINE, AND RIMANTADINE CONJUGATES AND A PHARMACEUTICAL COMPOSITION FOR TREATMENT OF NEURONAL DISORDERS

机译:金刚烷胺,肉毒杆菌素和雷米他定结合物以及用于治疗神经疾病的药物组合物

摘要

A compound is provided that has the formula (II):; embedded image ;where R1 in each occurrence is independently H, or C1-C4 alkyl; R2 is a nullity or CH—CH3, R3 is a nullity or C(O)—R6—NH; R6 is C2-C6 alkyl, (CH2CH2—O)n, or (CH(OH)CH2)n; n is an integer of between 1 and 4; R4 is a nullity or NH—R6—C(O); and R5 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, endocannabinoids 1 & 2, 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 peptide transferrin, glucosyl ester, lactic acid, leucine, tryptophan, glutamic acid.
机译:提供具有式(II)的化合物: “嵌入式图像” ;其中每次出现的R 1 独立地为H或C 1 -C 4 烷基; R 2 是无效或CH-CH 3 ,R 3 是无效或C(O)-R 6 —NH; R 6 是C 2 -C 6 烷基,(CH 2 CH 2 —O) n 或(CH(OH)CH 2 n ; n为1至4之间的整数; R 4 是无效值或NH-R 6 -C(O);和R 5 是能够穿过血脑屏障的部分,是游离的血清素,多巴胺,血脑屏障(BBB)肽,膜移位肽,TAT肽,内源性大麻素1和2,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,促甲状腺激素,血管紧张素,血管紧张素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,血管活性肠肽转铁蛋白,葡萄糖基酯,乳酸,亮氨酸,色氨酸,谷氨酸。

著录项

  • 公开/公告号US2017035889A1

    专利类型

  • 公开/公告日2017-02-09

    原文格式PDF

  • 申请/专利权人 LANDON C. G. MILLER;

    申请/专利号US201514819959

  • 发明设计人 LANDON C. G. MILLER;

    申请日2015-08-06

  • 分类号A61K47/48;

  • 国家 US

  • 入库时间 2022-08-21 13:45:23

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