4-Imidazo[1,2-a]pyrimidin-2-ylbenzoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-Imidazo[1,2-a]pyrimidin-2-ylbenzoic acid
• 化学式: C₁₃H₉N₃O₂
• 分子量: 239.23
• InChiKey: JSVXKWRXNBRMCX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] 4-(1-PIPERIDINY)-BUTYLCARBOXAMIDE AS D3 DOPAMINE RECEPTOR SUBTYPE SELECTIVE LIGANDS<br/>[FR] 4-(1-PIPERIDINY)-BUTYLCARBOXAMIDE UTILES COMME LIGANDS SELECTIFS DU SOUS-TYPE DU RECEPTEUR D3 DE LA DOPAMINE
  申请人：RICHTER GEDEON VEGYESZET

  公开号：WO2003028725A1

  公开（公告）日：2003-04-10

  The present invention relates to new D3 dopamine receptor subtype selective ligands of Formula (I), wherein R1 and R2 represent independently a substituent selected from hydrogen, halogen, C1-6alkyl, C1-6 alkoxy, cyano, hydroxy, trifluoromethyl, C1-6alkylsulfonyloxy, trifluoromethanesulfonyloxy, optionally substituted C1-6alkanoyloxy, amino, aminoalkyl, carboxy, aminocarbonyl, N-hydroxycarbamimidoyl, carbamimidoyl, hydroxycarbamoyl, thiocarbamoyl, sulfamoyl or mono or bicyclic heterocyclic group; Y represents an oxygen atom or NH or CH2 or OCH2 group; Q represents an optionally substituted C1-6alkyl, aryl, heteroaryl, heteroaralkyl or heteroaralkenyl group, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or the salts and/or hydrates and/or solvates thereof, to the process for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc.), drug (e.g. alcohol, cocaine and nicotine, opioids, etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit/hyperactivity disorder in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's disease, neuroleptic induced parkinsonism, tardive dyskinesias) anxiety, sexual disorders, sleep disorders, emesis, aggression, autism, pain, ophthalmological diseases (e.g. glaucoma, etc.).
• [EN] 4-(4-SUBSTITUTED PIPERAZINYL-1YL)-BUTYLCARBOXAMIDES AS D3 DOPAMINE SUBTYPE SELECTIVE LIGANDS<br/>[FR] 4-(PIPERAZINYL-1YLE SUBSTITUE EN 4)-BUTYLCARBOXAMIDES UTILISES EN TANT QUE LIGANDS SELECTIFS DU SOUS-TYPE DE LA DOPAMINE D3
  申请人：RICHTER GEDEON VEGYESZET

  公开号：WO2003028728A1

  公开（公告）日：2003-04-10

  The present invention relates to new D3 dopamine receptor subtype selective ligands of Formula (I), wherein R1, R2 and R3 independently represent substituents selected from hydrogen, halogen, C1-6alkyl, C1-6alkoxy, cyano, hydroxy, trifluoromethyl, C1-6alkylsulfonyloxy, trifluoromethanesulfonyloxy, optionally substituted C1-6alkanoyloxy, amino, aminoalkyl, carboxy, aminocarbonyl, N-hydroxycarbamimidoyl, carbamimidoyl, hydroxycarbamoyl, thiocarbamoyl, sulfamoyl, optionally substituted phenyl or naphthyl, optionally substituted mono or bicyclic heterocyclic group, two adjacent groups of R1, R2 and R3 may combine to form an optionally substituted fused mono or bicyclic heterocyclic group, with the exception of compounds wherein a) R1= R2 = R3 = H, b) R1 = R2= H and R3 = C1-6alkoxy in the position 2 or R3 is in the position 4 of the piperazinylphenyl moiety, c) R1 = H and R2 = R3 = C1-6alkoxy; Q represents an optionally substituted C1-6alkyl, C1-6alkenyl, phenyl or heteroaryl group.