4-amino-5-chloro-N-(2-pyrrolidinylmethyl)-2,3-dihydrobenzo[b]furan-7-carboxamide

• 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: 4-amino-5-chloro-N-(2-pyrrolidinylmethyl)-2,3-dihydrobenzo[b]furan-7-carboxamide
• 英文别名: 4-amino-5-chloro-N-(pyrrolidin-2-ylmethyl)-2,3-dihydro-1-benzofuran-7-carboxamide
• 化学式: C₁₄H₁₈ClN₃O₂
• 分子量: 295.769
• InChiKey: MPECLPSCJHXWNO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  76.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Formulations of adenosine a1 agonists
  申请人：——

  公开号：US20030018008A1

  公开（公告）日：2003-01-23

  The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and a 5HT 3 antagonist or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

  本发明提供了一种治疗与疼痛相关的症状并缓解相关症状的方法，包括向哺乳动物，包括人类，施用腺苷A1受体激动剂或其生理上可接受的盐或溶剂以及5HT3拮抗剂或其生理上可接受的盐或溶剂。本发明还提供了包含这些组合物的药物配方和患者包。
• Use of 5-hydroxytryptamine-antagonists in the treatment of mental disorders originating in childhood
  申请人：GLAXO GROUP LIMITED

  公开号：EP0450757A2

  公开（公告）日：1991-10-09

  The invention relates to the use of a compound which acts as an antagonist of 5-HT at 5-HT₃ receptors in the treatment of autism or another disorder originating in childhood in which there is mental retardation.

  本发明涉及一种在 5-HT₃ 受体上作为 5-HT 拮抗剂的化合物在治疗自闭症或另一种源于儿童期的精神发育迟滞疾病中的应用。
• Use of benzobicyclic carboxamides for the manufacture of a medicament for use as analgesic
  申请人：Erbamont Inc.

  公开号：EP0507637A2

  公开（公告）日：1992-10-07

  A compound of the formula (I) or a pharmaceutically acceptable salt thereof is used for the manufacture of a medicament for the treatment of algesia. Z represents the carbon and hydrogen atoms necessary to complete a substituted or unsubstituted, saturated or unsaturated, 5- to 7-membered ring. R1, R2, and R3 may be the same or different and represent a member selected from hydrogen, lower alkyl, cycloalkyl, lower alkoxy, amino, lower alkyl substituted amino, acylamido, sulfonamido, halogen, and nitro. A represents a moiety selected from formulae (II), (III), (IV), (V), (VI) and (VII) W represents a single boad or the carbon and hydrogen atoms necessary to complete a 3- to 8-membered saturated or unsaturated ring. Y represents a single bond or the carbon and hydrogen atoms necessary to complete a 4 to 8 membered saturated or unsaturated ring R6 is selected from hydrogen, lower alkyl, phenyl, phenalkyl, fluorine-substituted alkyl, propargyl, and allyl, R7 and R8 may be the same or different and are selected from lower alkyl, and lower hydroxyalkyl, M1 and M2 are the same or different and represent hydrogen or methyl, R11 and R12 are the same or different and represent lower alkyl, cycloalkyl, or phenalkyl. n is 0 or an integer of 1 to 3. When Z represents the atoms accessary to complete a 2,3,4,5-tetrahydro-1-benzoxepin ring, R1 may not equal hydrogen, amino, or alkylamino and R2 may not equal hydrogen or halogen. When Z represents the atoms necessary to complete a 2,2-dimethyl-2,3-dihydrobenzofuran ring, R1, R2 and may not simultaneously equal hydrogen and when R2 is flourine, R1 and R3 may not equal hydrogen. When Z represents the atoms necessary to complete a 2,2-dimethyl or a 2,2-diethyl 3,4-dihydrobenzopyran ring, R2 may not equal fluorine or chlorine when R1 and R3 are hydrogen.

  式 (I) 的化合物或其药学上可接受的盐可用于制造治疗鹅口疮的药物。 Z 代表完成取代或未取代的、饱和或不饱和的 5 至 7 元环所需的碳原子和氢原子。R1、R2 和 R3 可以相同或不同，并代表选自氢、低级烷基、环烷基、低级烷氧基、氨基、低级烷基取代的氨基、酰氨基、磺酰氨基、卤素和硝基的成员。A 代表选自式(II)、(III)、(IV)、(V)、(VI)和(VII)的分子。 W 代表单键或完成 3 至 8 元饱和或不饱和环所需的碳原子和氢原子。R6 选自氢、低级烷基、苯基、苯烷基、氟代烷基、丙基和烯丙基，R7 和 R8 可以相同或不同，选自低级烷基和低级羟烷基，M1 和 M2 可以相同或不同，代表氢或甲基，R11 和 R12 可以相同或不同，代表低级烷基、环烷基或苯烷基。当 Z 代表完成 2,3,4,5-四氢-1-苯并氧杂卓环所需的原子时，R1 不可为氢、氨基或烷基氨基，R2 不可为氢或卤素。当 Z 代表完成 2,2-二甲基-2,3-二氢苯并呋喃环所需的原子时，R1、R2 和不得同时等于氢，当 R2 为面粉碱时，R1 和 R3 不得等于氢。当 Z 代表完成 2,2-二甲基或 2,2-二乙基 3,4-二氢苯并呋喃环所需的原子时，当 R1 和 R3 为氢时，R2 可能不等于氟或氯。
• Process for the preparation of substituted benzofuran derivatives
  申请人：PHARMACIA S.p.A.

  公开号：EP0496064A1

  公开（公告）日：1992-07-29

  The present invention relates to a process for the preparation of a compound of the following formula (I) wherein one of R₁ and R₂ is hydrogen or halogen and the other is independently, an amino group or a C₂-C₄ alkanoyl amino group; R₃ is hydrogen; a linear or branched alkyl, C₁-C₄ alkoxy or C₂-C₄ alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C₁-C₄ alkyl group; A is a group -(CH₂)n-Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms and n is zero or an integer of 1 to 3; and the symbol ....¯ represents a single or double bond and the pharmaceutically acceptable salts thereof. The compounds of the invention can be useful as 5HT3 receptor antagonists.

  本发明涉及一种下式（I）化合物的制备工艺 其中 R₁ 和 R₂ 中的一个是氢或卤素，另一个独立地是氨基或 C₂-C₄ 烷酰基氨基； R₃ 是氢；直链或支链烷基、C₁-C₄ 烷氧基或 C₂-C₄ 烷氧羰基；卤素；或未被 C₁-C₄ 烷基取代或被 C₁-C₄ 烷基取代的苯基； A是基团-(CH₂)n-Het，其中Het是含有一个或两个氮原子的任选取代的杂单环或杂双环，n是零或1至3的整数；符号....¯代表单键或双键及其药学上可接受的盐。 本发明的化合物可用作 5HT3 受体拮抗剂。
• USE OF ONDANSETRON IN THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF TREMOR
  申请人：GLAXO GROUP LIMITED

  公开号：EP0851756B1

  公开（公告）日：2003-01-15