L-组氨酰-L-脯氨酰胺二氢溴酸盐 | 59760-04-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: L-组氨酰-L-脯氨酰胺二氢溴酸盐
• 英文名称: L-Histidyl-L-prolinamide dihydrobromide
• 英文别名: (2S)-1-[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carboxamide;dihydrobromide
• CAS: 59760-04-2
• 化学式: C11H19Br2N5O2
• 分子量: 413.11
• InChiKey: VEUXRROWTMGTCK-CDEWPDHBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.09
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  118
• 氢给体数：
  5
• 氢受体数：
  4

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  alpha-(2-Oxo-1-azetidinyl)acetic acid 、 L-组氨酰-L-脯氨酰胺二氢溴酸盐 生成 (2S)-1-[(2S)-3-(1H-imidazol-5-yl)-2-[[2-(2-oxoazetidin-1-yl)acetyl]amino]propanoyl]pyrrolidine-2-carboxamide
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Histidyl peptide derivatives
  申请人：Japan Tobacco Inc.

  公开号：US05151497A1

  公开（公告）日：1992-09-29

  Novel peptide derivatives of the following formula ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable acid addition salts thereof and analogous copounds thereof. Since the derivatives and their pharmaceutically acceptable acid addition salts of the present invention possess stronger actions on central nervous system (e.g. antagonistic action against hypothermia, locomotor stimulant action, signal reflex stimulant action), they are of use as a therapeutic medicament for central nervous disorders such as impaired consciousness, depression, hypomnesia, the like in association association with schizophrenia, melancholia, senile dementia, sequelae of cerebrovascular disorders, head trauma, epilepsy and spinocerebellar degeneracy.

  以下是该句子的中文翻译： 新型的肽衍生物符号如规范中所定义的以下公式： ##STR1## 其中每个符号如规范所定义，其药物可接受的酸盐衍生物和类似化合物。由于本发明的衍生物及其药物可接受的酸盐具有更强的中枢神经系统作用（例如对抗低体温、运动刺激作用、信号反射刺激作用），因此它们可用作治疗中枢神经系统障碍的药物，例如与精神分裂症、忧郁症、老年性痴呆、脑血管疾病后遗症、头部外伤、癫痫和脊髓小脑变性相关的意识障碍、记忆障碍等。
• CNS active substituted azetidinone compounds
  申请人：Yamanouchi Pharmaceutical Co., Ltd.

  公开号：US04719207A1

  公开（公告）日：1988-01-12

  Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.4 represents a group other than a hydrogen atom and provided that either R.sup.3 or R.sup.4 represents a group other than a hydrogen atom. The compounds have strong CNS action.

  本发明提供了具有以下式子的取代氮杂环戊酮化合物：##STR1## 其中R1和R2中的一个代表取代的低碳基，偶氮基，氨基，低酰胺基，巯基或低烷基硫基，另一个代表氢基，或者两个都代表氢原子或低烷基基团；R3代表氢原子或由以下式子表示的基团：##STR2## （其中X代表##STR3## （其中R5代表氢原子或低烷基基团），Y代表羟基，低烷氧基，氨基，单或双低烷基氨基基团）；R4代表氢原子，取代或未取代的低烷基基团或由以下公式表示的基团：--CH.sub.2 CO--A（其中A代表氨基或由以下式子表示的基团：##STR4## （其中X和Y如上定义），前提是当R1和R2都是氢原子时，至少R4代表除氢原子外的基团，并且R3或R4中的任一代表除氢原子外的基团。这些化合物具有强烈的中枢神经系统作用。
• Novel peptides and process for preparing the same and pharmaceutical composition
  申请人：Tanabe Seiyaku Co., Ltd.

  公开号：EP0134582A2

  公开（公告）日：1985-03-20

  A compound of the formula: wherein A is a group of the formula: R1 and R' are the same or different and each hydrogen atom, nitro, amino, a protected amino, hydroxy or lower alkoxy, Y is oxygen atom or a group of the formula: -NR3-, R3 is hydrogen atom or lower alkyl. X is methylene or sulphur atom and the dotted line is an optional double bond, or a pharmaceutically acceptable acid addition salt thereof is useful as a medicine for the treatment of consciousness disorders. Also processes for the preparation of these compounds are disclosed.

  式的化合物： 其中 A 是式中的基团： R1 和 R'相同或不同，各自为氢原子、硝基、氨基、受保护氨基、羟基或低级烷氧基、 Y 是氧原子或式中的基团：-NR3-、 R3 是氢原子或低级烷基。 X 是亚甲基或硫原子，以及 虚线为任选双键，或其药学上可接受的酸加成盐，可作为治疗意识障碍的药物。此外，还公开了制备这些化合物的工艺。
• Dihydroorotic acid derivatives, processes for their preparing and pharmaceutical composition containing them
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0168042A2

  公开（公告）日：1986-01-15

  There are disclosed 1-Methy)-4,5-dihydroorotyl-histidyl-prolinamide or a pharmaceutically acceptable acid addition salt thereof, processes for their preparation and pharmaceutical compositions containing them. The prolinamide and the parmaceutically acceptable acid addition salts thereof are useful for the treatment of central nervous system disorder.

  本发明公开了1-甲基-4,5-二氢烟酰-组氨酰-脯氨酰胺或其药学上可接受的酸加成盐、其制备工艺以及含有它们的药物组合物。 脯氨酰胺及其药学上可接受的酸加成盐可用于治疗中枢神经系统疾病。
• Substituted azetidinone compounds, their preparation, and medicaments containing them
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0171159A1

  公开（公告）日：1986-02-12

  Compounds of the following general formula (1) and salts thereof are useful pharmaceuticals having central nervous system activitv: wherein one of R1 and R2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or both represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom or a group shown by formula: [wherein X represents (wherein R5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group]; and R4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula -CH2CO-A [wherein A represents an amino group or a group shown by formula (wherein X and Y are as defined above)]; provided that (a) at least one of R3 and R4 is other than a hydrogen atom and (b) when R1 and R2 are both hydrogen atoms at least R4 is other than a hydrogen atom.

  以下通式(1)的化合物及其盐类是具有中枢神经系统活性的有用药物： 其中 R1 和 R2 中的一个代表取代的低级烷基、叠氮基、氨基、低级酰氨基、巯基或低级烷硫基，另一个代表氢基，或二者均代表氢原子或低级烷基；R3 代表氢原子或式(1)所示的基团： [其中 X 代表 (其中 R5 代表氢原子或低级烷基），Y 代表羟基、低级烷氧基、氨基、单或双低级烷基氨基]；以及 R4 代表氢原子、取代或未取代的低级烷基或式 -CH2CO-A 所示的基团[其中 A 代表氨基或式所示的基团 (其中 X 和 Y 如上定义）]；条件是 (a) R3 和 R4 中至少有一个不是氢原子，以及 (b) 当 R1 和 R2 都是氢原子时，至少 R4 不是氢原子。