2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine | 70769-69-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine
• 英文别名: 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine
• CAS: 70769-69-6
• 化学式: C₁₂H₁₅N
• 分子量: 173.258
• InChiKey: OOERPQACTFFTHC-UHFFFAOYSA-N

物化性质

• 沸点：
  292.3±9.0 °C(Predicted)
• 密度：
  1.040±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine 、 碘甲烷 、 calcium carbonate 、 丙酮 生成 1-methyl-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine
  参考文献：
  名称：

  URBINA G. A., SYNTH. COMMUN., 1979, 9, NO 4, 245-250

  摘要：

  DOI：
• 作为产物：
  描述：

  1-(1H-inden-2-yl)pyrrolidine 在 palladium 10% on activated carbon lithium aluminium tetrahydride 、 氢气 、 溶剂黄146 作用下， 以 四氢呋喃 、 甲醇 、 水 、 溶剂黄146 为溶剂， 20.0~130.0 ℃ 、300.01 kPa 条件下， 反应 9.25h， 生成 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine
  参考文献：
  名称：

  [EN] ARYL- AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE
  [FR] DÉRIVÉS ARYLECARBONYLE ET HÉTÉROARYLCARBONYLE D'HEXAHYDROINDÉNOPYRIDINE ET D'OCTAHYDROBENZOQUINOLINE

  摘要：

  本发明涉及由公式I定义的化合物，其中变量R1、R2、R3、R4和m如权利要求1中定义的那样，具有有价值的药理活性。特别是，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以受到该酶抑制影响的疾病，例如代谢性疾病，特别是2型糖尿病、肥胖症和血脂异常。

  公开号：

  WO2011057054A1

文献信息

• ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE
  申请人：Eckhardt Matthias

  公开号：US20110136800A1

  公开（公告）日：2011-06-09

  The present invention relates to compounds defined by formula I wherein the variables R 1 , R 2 , R 3 , R 4 , and m are defined as in claim 1 , possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

  本发明涉及由以下公式I定义的化合物，其中变量R1、R2、R3、R4和m的定义如权利要求书中，具有有价值的药理活性。特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以受到该酶抑制影响的疾病，如代谢性疾病，特别是2型糖尿病、肥胖症和血脂异常。
• [EN] CRYSTALLINE FORMS OF HYDROCHLORIDE SALT OF (4A-R,9A-S) -1- (1H - BENZOIMIDAZOLE- 5 -CARBONYL) -2, 3, 4, 4A, 9, 9A - HEXAHYDRO -1H- INDENO [2, 1 -B] PYRIDINE- 6 -CARBONITRILE AND THEIR USE AS HSD 1 INHIBITORS<br/>[FR] FORMES CRISTALLINES DU SEL DE TYPE CHLORHYDRATE DU (4A-R,9A-S)-1-(1H-BENZIMIDAZOLE-5-CARBONYL)-2,3,4,4A,9,9A-HEXAHYDRO-1H-INDÉNO[2,1-B]PYRIDINE-6-CARBONITRILE ET LEUR UTILISATION COMME INHIBITEURS D'HSD1
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012061708A1

  公开（公告）日：2012-05-10

  The present invention relates to crystalline compounds of the following structural formula (II) possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

  本发明涉及具有以下结构式（II）的晶体化合物，具有有价值的药理活性。特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以受到该酶抑制影响的疾病，如代谢性疾病，特别是2型糖尿病、肥胖症和血脂异常。
• [EN] 6-AMINO(AZA)INDANE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECPTOR<br/>[FR] COMPOSES DE 6-AMINO(AZA)INDANE 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：WO2006040177A1

  公开（公告）日：2006-04-20

  The present invention relates to 6-amino(aza)indane compound 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 I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR 3; R1 is 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, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.

  本发明涉及公式(I)的6-氨基(氮)茚化合物，其中Ar为苯基或芳香5-或6-成员C-键合杂芳基，其中Ar可能携带1个基团Ra，Ar还可能携带1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，氟化的C1-C4-烷基，氟化的C3-C4-环烷基，氟化的C3-C4-环烷基甲基，氟化的C3-C4-烯基，甲酰基或C1-C3-烷基羰基；R1a为H或R1a和R2或R1a和R2a一起为(CH2)n，其中n为1、2、3或4；R2和R2a各自独立地为H、CH3、 F、CHF2或CF3；R3为H或C1-C4-烷基；以及这些化合物的生理耐受性酸盐。该发明还涉及包含至少一种公式(I)化合物或其药学上可接受的盐的制药组合物，以及用于治疗可通过多巴胺D3受体配体治疗的医疗疾病的方法，该方法包括给予至少一种公式(I)化合物或其药学上可接受的盐的有效量。
• Antiparasitic terpene alkaloids
  申请人：Chubb A. Nathan

  公开号：US20070185101A1

  公开（公告）日：2007-08-09

  The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an, antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.

  本发明涉及新型萜类生物碱及其作为抗寄生虫剂的用途。本发明还涉及一种抗寄生虫剂，其包含本发明中的萜类生物碱化合物作为抗寄生虫制剂中的有效成分。更具体地，本发明涉及萜类生物碱（1S，2R，4aS，5R，8R，8aR）-2-（乙酰氧基）-8a-羟基-3，8-二甲基-5-（1-甲基乙烯基）-1,2,4a,5,6,7,8,8a-八氢萘-1-基（2S，3aR，9bR）-6-氯-9b-羟基-5-甲基-1,2,3,3a,5,9b-六氢吡咯[2,3-c] [2,1]苯并噁唑-2-羧酸酯的衍生物。还公开了包含该物质的药物组合物。
• ARYL- AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE
  申请人：Vitae Pharmaceuticals, Inc./Boehringer-Ingelheim

  公开号：US20160272590A1

  公开（公告）日：2016-09-22

  The present invention relates to compounds defined by formula I wherein the variables R 1 , R 2 , R 3 , R 4 , and m are defined as in claim 1 , possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

  本发明涉及由公式I定义的化合物，其中变量R1、R2、R3、R4和m的定义如权利要求书中所述，具有有价值的药理活性。特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以受到该酶抑制影响的疾病，例如代谢性疾病，特别是2型糖尿病、肥胖症和血脂异常。