苯乙胺,4-氨基-a-甲基-,(aR)- | 736081-33-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 苯乙胺,4-氨基-a-甲基-,(aR)-
• 英文名称: 4-[(2R)-2-Aminopropyl]aniline
• CAS: 736081-33-7
• 化学式: C₉H₁₄N₂
• 分子量: 150.22
• InChiKey: UXAZIFYAGDKABZ-SSDOTTSWSA-N

物化性质

• 沸点：
  280.6±15.0 °C(Predicted)
• 密度：
  1.035±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  52
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• [EN] AMINOETHYLAROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR<br/>[FR] COMPOSES AMINOETHYLAROMATIQUES PERMETTANT DE TRAITER DES TROUBLES REPONDANT A UNE MODULATION DU RECEPTEUR D3 DE LA DOPAMINE
  申请人：ABBOTT GMBH & CO KG

  公开号：WO2006040179A1

  公开（公告）日：2006-04-20

  The present invention relates to aromatic compounds of the formula (I) wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated Cl-C4­-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4­-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-­C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3­-C4-alkenyl, or R1a and R2 together are (CH2)n with n being 2, 3 or 4, or R1a and R2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are independently of each other H, C1-C4-alkyl or fluorinated C1-C4-alkyl or R2a and R2 together are (CH2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

  本发明涉及公式（I）的芳香族化合物，其中Ar为苯基或芳香族5-或6-成员C-键合杂环基，其中Ar可能携带1个基团Ra，Ar也可能携带1个或2个基团Rb；X为N或CH；E为CR6R7或NR3；R1为C1-C4-烷基，C3-C4-环烷基，C3-C4-环烷基甲基，C3-C4-烯基，氟代的Cl-C4-烷基，氟代的C3-C4-环烷基，氟代的C3-C4-环烷基甲基，氟代的C3-C4-烯基，甲酰基或C1-C3-烷基羰基；R1a为H，C1-C4-烷基，C3-C4-环烷基，C3-C4-环烷基甲基，C3-C4-烯基，氟代的C1-C4-烷基，氟代的C3-C4-环烷基，氟代的C3-C4-环烷基甲基，氟代的C3-C4-烯基，或R1a和R2一起为（CH2）n，其中n为2、3或4，或R1a和R2a一起为（ ）n，其中n为2、3或4；R2和R2a彼此独立为H，C1-C4-烷基或氟代的C1-C4-烷基，或R2a和R2一起为（ ）m，其中m为1、2、3、4或5；R3为H或C1-C4-烷基；R6、R7彼此独立地选自H、氟、C1-C4-烷基和氟代的C1-C4-烷基，或一起形成一个( )p的基团，其中p为2、3、4或5；以及其生理耐受的酸盐。该发明还涉及使用公式（I）的化合物或其药学上可接受的盐来制备用于治疗可用多巴胺D3受体配体治疗的医疗疾病的药物组合物。
• [EN] COMPOSITIONS COMPRISING TRYPSIN-CLEAVABLE AMPHETAMINE PRODRUGS AND INHIBITORS THEREOF<br/>[FR] COMPOSITIONS COMPRENANT DES PROMÉDICAMENTS DE TYPE AMPHÉTAMINE CLIVABLES PAR TRYPSINE ET LEURS INHIBITEURS
  申请人：PHARMACOFORE INC

  公开号：WO2011133347A1

  公开（公告）日：2011-10-27

  Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

  提供药物组合物及其使用方法，其中药物组合物包括一种苯丙胺前药，可提供苯丙胺或苯丙胺类似物的酶控释放。该组合物还可以包括一个酶抑制剂，与介导苯丙胺前药中的苯丙胺或苯丙胺类似物的酶相互作用，以减弱苯丙胺前药的酶解裂。
• COMPOSITIONS FOR REDUCING RISK OF ADVERSE EVENTS CAUSED BY DRUG-DRUG INTERACTIONS
  申请人：JENKINS Thomas E.

  公开号：US20120232066A1

  公开（公告）日：2012-09-13

  The present disclosure provides a composition comprising a GABA A agonist and a GI enzyme inhibitor. The present disclosure also provides a composition comprising (a) a GI enzyme inhibitor and (b) a first drug that interacts with a second drug to produce an adverse effect when the second drug is co-ingested as a GI enzyme-cleavable prodrug with the first drug. Such an interaction can be additive or synergistic.

  本公开提供一种包含GABAA激动剂和GI酶抑制剂的组合物。本公开还提供一种包含（a）GI酶抑制剂和（b）第一药物的组合物，当第二药物以GI酶可切割的前药形式与第一药物共同摄入时，第一药物与第二药物相互作用产生不良效应。这种相互作用可以是加成的或协同的。
• [EN] PROCESS FOR THE SYNTHESIS OF AMPHETAMINE DERIVATIVES<br/>[FR] PROCÉDÉ POUR LA SYNTHÈSE DE DÉRIVÉS D'AMPHÉTAMINE
  申请人：ARCHIMICA INC

  公开号：WO2010042120A1

  公开（公告）日：2010-04-15

  The invention relates to a process for preparing acylated amphetamine, methamphetamine and dexamphetamine derivatives by reacting the parent amine with the to be coupled acid or a salt of the to be coupled acid which acid is protected or not protected, in the presence of an alkylphosphonic acid anhydride as coupling agent and - provided the acid (V2) was protected - the cleavage of the protecting group(s), in a one-pot reaction or in two or more separate steps.

  该发明涉及一种制备酰化苯丙胺、甲基苯丙胺和右旋苯丙胺衍生物的过程，通过将母体胺与待偶联酸或待偶联酸的盐（该酸受保护或未受保护）在辛基膦酸酐作为偶联剂的存在下反应，并且 - 假设酸（V2）受保护 - 解除保护基的，在一个锅反应中或在两个或更多独立步骤中。
• [EN] COMPOSITIONS COMPRISING ENZYME-CLEAVABLE AMPHETAMINE PRODRUGS AND INHIBITORS THEREOF<br/>[FR] COMPOSITIONS COMPRENANT DES PROMÉDICAMENTS DE TYPE AMPHÉTAMINE CLIVABLES PAR ENZYME ET LEURS INHIBITEURS
  申请人：PHARMACOFORE INC

  公开号：WO2011133348A1

  公开（公告）日：2011-10-27

  Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

  提供了药物组合物及其使用方法，其中药物组合物包括一种苯丙胺前药，该前药提供苯丙胺或苯丙胺类似物的酶控释放。该组合物还可以包括一种酶抑制剂，与介导苯丙胺前药中的苯丙胺或苯丙胺类似物的酶相互作用，以减轻苯丙胺前药的酶催化裂解。