N-acetyl-D-phenylglycinebenzylamide | 1026267-15-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-acetyl-D-phenylglycinebenzylamide
• 英文别名: N-Acetyl-D,L-phenylglycine-N-benzylamide；2-(N-acetylanilino)-N-benzylacetamide
• CAS: 1026267-15-1
• 化学式: C₁₇H₁₈N₂O₂
• 分子量: 282.342
• InChiKey: BTIJZMNCIDPMSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  49.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-t-Boc-L-phenylglycine-N-benzylamide 以2.99 g (66%)的产率得到N-acetyl-D-phenylglycinebenzylamide
  参考文献：
  名称：

  Amino acid derivative anticonvulsant

  摘要：

  本发明涉及以下结构的化合物 ##STR1##

  公开号：

  US05654301A1

文献信息

• Lacosamide (SPM 927) for treating myalgia, e.g. fibromyalgia
  申请人：SCHWARZ PHARMA AG

  公开号：EP1754476A1

  公开（公告）日：2007-02-21

  The present invention is directed to the use of a class of peptide compounds for treating non-inflammatory musculoskeletal pain.

  本发明涉及使用一类肽化合物治疗非炎性肌骨疼痛。
• Uses for amino acid anticonvulsants
  申请人：——

  公开号：US20020086828A1

  公开（公告）日：2002-07-04

  The present invention is directed to the use of compounds of the formula: 1 for treating pain, in particular neuropathic pain, bipolar disease and migraine headaches.

  本发明涉及使用式1化合物治疗疼痛，特别是神经病性疼痛、双相情感障碍和偏头痛。
• Novel use of peptide class of compound for treating non neuropathic inflammatory pain
  申请人：——

  公开号：US20030171300A1

  公开（公告）日：2003-09-11

  The present invention concerns the use of compounds of the Formula (I) for treating different types and symptoms of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDS) and are useful as specific analgesics.

  本发明涉及使用式(I)化合物治疗哺乳动物不同类型和症状的急性和慢性疼痛，特别是非神经病性炎症性疼痛。待治疗的疼痛可能是慢性炎症性疼痛、类风湿关节炎疼痛和/或继发性炎症性骨关节炎疼痛。这些化合物表现出镇痛特性，与阿片类和非甾体抗炎药（NSAIDS）等经典镇痛药物不同，并可用作特异性镇痛药物。
• Anticonvulsant composition containing amino acid derivative and use of said amino acid derivative
  申请人：RESEARCH CORPORATION TECHNOLOGIES, INC.

  公开号：EP0263506A2

  公开（公告）日：1988-04-13

  The present invention relates to an anticonvulsant composition comprising a compound of the formula: where R, R₁, R₂ and R₃ and n are as defined in claim 1 as effective ingredient, together with a pharmaceutically acceptable carrier, said composition being useful in the treatment of epilepsy and other CNS disorders, and the use of the above effective ingredient in the preparation of an anticonvulsant medicament.

  本发明涉及一种抗惊厥组合物，该组合物包含一种式化合物： 其中 R、R₁、R₂ 和 R₃ 及 n 如权利要求 1 中所定义，作为有效成分，与药学上可接受的载体一起使用，所述组合物可用于治疗癫痫和其他中枢神经系统疾病，以及将上述有效成分用于制备抗惊厥药物。
• New uses for amino acid anticonvulsants for treatment of migraine
  申请人：Research Corporation Technologies, Inc

  公开号：EP1486205A1

  公开（公告）日：2004-12-15

  The present invention describes the use of a compound of the following formula (I) for the manufacture of a medicament effective in the treatment or prevention of migraine headaches of a mammal:    wherein Ris hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl lower alkyl, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with at least one electron withdrawing or electron donating group; R1is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, heterocyclic lower alkyl, heterocyclic, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with an electron donating or an electron withdrawing group; R2 and R3are independently hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, halogen, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, or Z-Y; R2 and R3 are optionally substituted with at least one electron withdrawing or electron donating group; Zis O, S, S(O)a, NR4 or PR4; Yis hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, heterocyclic, heterocyclic lower alkyl, and Y is optionally substituted with an electron donating or electron withdrawing group, or ZYtaken together is NR4NR5R7, NR4OR5, ONR4R7, OPR4R5, PR4OR5, SNR4R7, NR4SR7, SPR4R5, PR4SR7, NR4PR5R6, PR4NR5R7, NR4C(=O)R5, S(C=O)R5, NR4C(=O)OR5, or S(C=O)OR5, R4, R5 and R6are independently hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl, or lower alkynyl, each optionally substituted with an electron withdrawing or an electron donating group; R7is COOR8, COR8, hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl or lower alkynyl, each optionally substituted with an electron withdrawing or electron donating group; R8is hydrogen, lower alkyl or aryl lower alkyl, the aryl or alkyl group is optionally substituted with an electron withdrawing or an electron donating group; nis 1-4; and ais 1-3.

  本发明描述了下式（I）化合物在制造有效治疗或预防哺乳动物偏头痛的药物中的用途： 其中 Ris氢或低级烷基、低级烯基、低级炔基、芳基、芳基低级烷基、杂环基、杂环低级烷基、低级烷基杂环基、低级环烷基、低级环烷基低级烷基，各自任选被至少一个取电子或供电子基团取代； R1 为氢或低级烷基、低级烯基、低级炔基、低级芳烷基、芳基、杂环低级烷基、杂环、低级烷基杂环、低级环烷基、低级环烷基低级烷基，各自可选地被一个电子捐赠基团或一个电子撤回基团取代； R2 和 R3 独立地为氢、低级烷基、低级烯基、低级炔基、低级芳烷基、芳基、卤素、杂环、杂环低级烷基、低级烷基杂环、低级环烷基、低级环烷基低级烷基或 Z-Y； R2 和 R3 可任选被至少一个析电子或供电子基团取代； Z 是 O、S、S(O)a、NR4 或 PR4； Y 是氢、低级烷基、芳基、芳基低级烷基、低级烯基、低级炔基、杂环、杂环低级烷基，且 Y 可选择被一个电子捐赠基团或电子撤回基团取代，或 ZY合起来是 NR4NR5R7、NR4OR5、ONR4R7、OPR4R5、PR4OR5、SNR4R7、NR4SR7、SPR4R5、PR4SR7、NR4PR5R6、PR4NR5R7、NR4C(=O)R5、S(C=O)R5、NR4C(=O)OR5 或 S(C=O)OR5、 R4、R5 和 R6 独立地为氢或低级烷基、芳基、芳基低级烷基、低级烯基或低级炔基，各自可选地被一个取电子基团或一个供电子基团取代； R7 是 COOR8、COR8、氢或低级烷基、芳基、芳基低级烷基、低级烯基或低级炔基，各自任选被一个取电子或捐电子基团取代； R8 是氢、低级烷基或芳基低级烷基，芳基或烷基可任选被一个取电子或捐电子基团取代； n 是 1-4；和 ais 1-3。