3-Amino-1-phenyl-3-cyclohexyl-propanol-(1) | 124065-53-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 3-Amino-1-phenyl-3-cyclohexyl-propanol-(1)
• 英文别名: 1-phenyl-1-cyclohexyl-3-amino-propanol；3-Amino-1-cyclohexyl-1-phenylpropan-1-ol
• CAS: 124065-53-8
• 化学式: C₁₅H₂₃NO
• 分子量: 233.354
• InChiKey: AIGPYLMSTKCARC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• New amidino derivatives
  申请人：ISTITUTO DE ANGELI S.p.A.

  公开号：EP0309424A2

  公开（公告）日：1989-03-29

  New pharmacologically active amidino derivatives as muscarinic receptor blocking agents which are useful for the treatment of gastrointestinal disorders of the following formula wherein R represents hydrogen atom, Ci-5 alkyl, aryl, an amino group optionally substituted by one or two C1-5 alkyl; R1 represents hydrogen atom, C1-8 alkyl, aralkyl; A represents Ci-5 alkyl substituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl, carboxamide; or a saturated 6-membered heterocyclic ring containing one nitrogen atom N-substituted by COR2 where R2 is a methyl substituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl, hydroxy; or where R3 is hydrogen atom and R4 is C1-5 alkyl substitued by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl, carboxamide, or by hydroxy optionally esterified with a cycloalkylcarboxylic acid, or R3 and R4, together with the nitrogen atom to which they are attached, form a saturated 5- to 7-membered heterocyclic ring, optionally containing one or two nitrogen atoms or an endocyclic carboxamido group optionally comprising in its inside -CH2-CH2- or being the heterocyclic ring substituted by a Ci-5 alkyl substituted in turn by 2 or 3 radicals, which may be identical or different from each other, selected from Ci-s alkyl, aryl, cycloalkyl or hydroxy, or byarylalkylene, or by -ORs where Rs is -OCR6 where R6 is methyl substituted by 2 or 3 radicals, which may be identical or different from each other, selected from a saturated or unsaturated C1-5 alkyl, aryl, cycloalkyl, hydroxy Ci-5 alkyl, hydroxy, or unsaturated 6-membered heterocyclic ring, provided that at least one between R and A is amino group or The tautomers and the acid addition salts of these compounds, as well as the process for the preparation of the compounds of formula (I) and pharmaceutical compositions containing them are also described.

  作为毒蕈碱受体阻断剂的新型药理活性脒衍生物，可用于治疗下式所示的胃肠道疾病 式中 R 代表氢原子、C1-5 烷基、芳基、任选被一个或两个 C1-5 烷基取代的氨基； R1 代表氢原子、C1-8 烷基、芳基； A 代表 被 2 个或 3 个基团取代的 Ci-5 烷基，这些基团可以是相同的，也可以是不同的 或彼此不同，选自芳基、环烷基、羧酰胺 或含有一个氮原子的饱和 6 元杂环，该氮原子由 COR2 取代，其中 R2 是由 2 或 3 个基取代的甲基，这些基可以相同或不同，选自芳基、环烷基、羟基；或 其中 R3 是氢原子，R4 是被 2 或 3 个基团取代的 C1-5 烷基，这些基团可以彼此相同或不同，选自芳基、环烷基、羧酰胺，或由羟基任选与环烷基羧酸酯化，或 R3 和 R4 与它们连接的氮原子一起形成饱和的 5-7 元杂环，可任选含有一个或两个氮原子或内环羧酰胺基团，可任选在其内部包含 -CH2- - 或 被一个依次被 2 或 3 个基取代的 Ci-5 烷基取代的杂环，这些基可以彼此相同或不同，选自 Ci-s 烷基、芳基、环烷基或羟基，或芳烷基，或被 -ORs 取代，其中 Rs 为 -OCR6 ，R6 为被 2 或 3 个基取代的甲基、这些基团可以彼此相同或不同，选自饱和或不饱和的 C1-5 烷基、芳基、环烷基、羟基 Ci-5烷基、羟基或不饱和的 6 元杂环，条件是 R 和 A 之间至少有一个基团是氨基，或 此外，还描述了这些化合物的同系物和酸加成盐，以及式（I）化合物和含有它们的药物组合物的制备过程。