tropan-3-yl-acetic acid | 90978-73-7

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: tropan-3-yl-acetic acid
• 英文别名: Tropan-3-yl-essigsaeure；(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)acetic acid；3α-Tropan-essigsaeure；Tropan-3α-essigsaeure；2-(8-Methyl-8-azabicyclo[3.2.1]octan-3-yl)acetic acid
• CAS: 90978-73-7
• 化学式: C₁₀H₁₇NO₂
• 分子量: 183.25
• InChiKey: CFLMZWGSEVZEHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tropan-3-yl-acetic acid 、 4H-benzo[e]thieno[3,4-b][1,4]diazepin-9(10H)-one 生成 endo-4,9-dihydro-4-[(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)acetyl]-10H-thieno[3,4-b][1,5]benzodiazepin-10-one
  参考文献：
  名称：

  Thienobenzodiazepinones, pharmaceutical compositions thereof and method

  摘要：

  这项发明涉及以下结构的新化合物：其中R.sub.1为氢或含有1至4个碳原子的烷基；R.sub.2为卤素、氢或含有1至4个碳原子的烷基；R为(1-甲基-4-哌啶基)甲基、(1-甲基-1,2,5,6-四氢-4-吡啶基)甲基、1-甲基-1,2,5,6-四氢-4-吡啶基、(1-甲基-4-哌啶基亚)-甲基或(8-甲基-8-氮杂双环[3.2.1]辛-3-基)-甲基，其中每个基在杂环环上可以选择性地有一个额外的甲基取代基，并且其无毒、药理学上可接受的酸盐。这些化合物及其盐可用作抗溃疡剂。

  公开号：

  US04424225A1
• 作为产物：
  描述：

  托品酮 在 乙酸铵 、 盐酸 、 palladium on activated charcoal 、 溶剂黄146 作用下， 生成 tropan-3-yl-acetic acid
  参考文献：
  名称：

  Zirkle et al., Journal of Organic Chemistry, 1962, vol. 27, p. 1269,1277

  摘要：

  DOI：

文献信息

• M3 Muscarinic Acetylcholine Receptor Antagonists
  申请人：Busch-Petersen Jakob

  公开号：US20080234315A1

  公开（公告）日：2008-09-25

  The present invention is directed to novel Muscarinic Acetylcholine receptor antagonists of Formula (I), pharmaceutical compositions and methods of using them. Compounds of Formula (I) are, inter alia, wherein: R1 and R2 are, independently, selected from the group consisting of 3-thienyl, pyridyl, benzyl, pyrimidyl, thiazolyl, isothiazolyl and C 3-7 cycloalkyl.

  本发明涉及一种新的肌动蛋白乙酰胆碱受体拮抗剂，其化学式为(I)，以及使用它们的药物组合物和方法。其中，化合物(I)包括但不限于以下结构：其中：R1和R2分别独立地选择自3-噻吩基、吡啶基、苄基、嘧啶基、噻唑基、异噻唑基和C3-7环烷基的群。
• Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with a Cyclic Amino Group As Crf Antagonists
  申请人：Nakazato Atsuro

  公开号：US20080280928A1

  公开（公告）日：2008-11-13

  [PROBLEM TO BE SOLVED] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following a [I] has a high affinity for CRF receptors and/or δ receptors, and is effective against diseases in which CRF is considered to be involved.

  【问题需解决】本发明的目的是提供一种针对CRF受体的拮抗剂和/或δ受体的激动剂，其作为治疗或预防CRF参与的疾病，如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、脑梗塞、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、癫痫、皮炎、精神分裂症、疼痛等方面的治疗或预防药物。 【解决方案】一种通过以下a[I]所代表的环状氨基基团取代的吡咯吡嘧啶或吡咯吡啶衍生物具有高亲和力，可用于CRF受体和/或δ受体，并对CRF参与的疾病具有治疗作用。
• PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES SUBSTITUTED WITH A CYCLIC AMINO GROUP AS CRF ANTAGONISTS
  申请人：NAKAZATO Atsuro

  公开号：US20110124862A1

  公开（公告）日：2011-05-26

  [Problem to be Solved] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [Solution] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following formula [I] has a high affinity for CRF receptors and/or δ receptors, and is effective against diseases in which CRF is considered to be involved.

  【待解决的问题】本发明的目的是提供一种CRF受体的拮抗剂和/或δ受体的激动剂，作为治疗或预防CRF参与的疾病（如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈病、进食障碍、高血压、胃肠疾病、药物依赖、脑梗塞、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、癫痫、皮炎、精神分裂症、疼痛等）的有效药物。 【解决方案】以下式[I]所表示的带有环状氨基基团的吡咯吡嘧啶或吡咯吡啶衍生物具有高亲和力，可作为CRF受体和/或δ受体的拮抗剂，对于CRF参与的疾病具有治疗效果。
• Salts of endo-8-methyl-8-syn-alkyl-8-azoniabicyclo-(3.2.1)-octane-3-alkylcarboxylates, process for their preparation and therapeutic compositions containing them
  申请人：VALEAS S.p.A. INDUSTRIA CHIMICA E FARMACEUTICA

  公开号：EP0042365A1

  公开（公告）日：1981-12-23

  The invention relates to new salts of endo-8-methyl-8-syn- atkyl-8-azoniabicycio-[3.2.1 ]-octane-3-atkylcarboxylates, of formula: in which R1 is a linear or branched alkyl radical of 2-5 C atoms, a cycloalkyl radical of 3-6 C atoms, or a phenyl-alkyl radical, R3 and R4, which can be the same or different, are alkyl radicals of 1-6 C atoms, X is a halide ion. The new compounds are potent spasmolytics.

  本发明涉及内-8-甲基-8-鞘氨酰-8-氮杂双环-[3.2.1 ]-辛烷-3-烷基羧酸盐的新盐，其式如下： 其中 R1 是 2-5 个 C 原子的直链或支链烷基、3-6 个 C 原子的环烷基或苯基烷基，R3 和 R4（可以相同或不同）是 1-6 个 C 原子的烷基，X 是卤化物离子。 新化合物是强效的解痉剂。
• Indole derivatives and processes for preparation thereof
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0403882A2

  公开（公告）日：1990-12-27

  A compound of the formula : wherein R1 is lower alkyl and R2 and R3 are each hydrogen, lower alkyl or linked together to form a bond; or R1 and R2 are linked together to form lower alkylene and R3 is hydrogen, and R4 is azabicyclo(C5-Cl2)alkyl(lower)alkyl or its N-oxide, each of which may be substituted by lower alkyl, provided that R4 is N-oxide of azabicyclo(C5-C12(lower)alkyl, which may be substituted by lower alkyl when R1 is lower alkyl and R2 and R3 are each hydrogen or lower alkyl, and pharmaceutically acceptable salt thereof, processes for their preparation and pharmaceutical compositions comprising them as active ingredient in association with a pharmaceutically acceptable carrier or excipient.

  式中的化合物 式中 R1 是低级烷基 R2 和 R3 分别为氢、低级烷基或连接在一起形成键；或 R1 和 R2 连接在一起形成低级亚烷基，且 R3 为氢，以及 R4 是氮杂双环(C5-Cl2)烷基（低级）烷基或其 N-氧化物，其中每个可被低级烷基取代，条件是 R4 是氮杂双环(C5-C12(低级)烷基的 N-氧化物，当 R1 是低级烷基且 R2 和 R3 各为氢或低级烷基时，该氮杂双环(C5-C12(低级)烷基可被低级烷基取代、 及其药学上可接受的盐、 它们的制备工艺以及由它们作为活性成分与药学上可接受的载体或赋形剂组成的药物组合物。