4-(2-氯苯基)哌啶盐酸盐 | 82211-92-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 4-(2-氯苯基)哌啶盐酸盐
• 英文名称: 4-(2-chloro-phenyl)piperidine hydrochloride
• 英文别名: 4-(2-Chlorophenyl)piperidine hydrochloride；4-(2-chlorophenyl)piperidine;hydrochloride
• CAS: 82211-92-5
• 化学式: C₁₁H₁₄ClN*ClH
• 分子量: 232.153
• InChiKey: BALIJVUSWGOXBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.23
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  12
• 氢给体数：
  2
• 氢受体数：
  1

安全信息

• 海关编码：
  2933399090
• 危险性防范说明：
  P261,P280,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H332,H335

反应信息

• 作为反应物：
  描述：

  1-甲基-2-甲酰苯并咪唑 、 4-(2-氯苯基)哌啶盐酸盐 在 三乙酰氧基硼氢化钠 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 、 1,2-二氯乙烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 32.0h， 生成 2-((4-(2-chlorophenyl)piperidin-1-yl)methyl)-1-methyl-1H-benzo-[d]imidazole
  参考文献：
  名称：

  1-[(1-Methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis

  摘要：

  A novel series of mGluR2 positive allosteric modulators (PAMs), 1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines, is herein disclosed. Structure-activity relationship studies led to potent, selective mGluR2 PAMs with excellent pharmacokinetic profiles. A representative lead compound (+)-17e demonstrated dose-dependent inhibition of methamphetamine-induced hyperactivity and mescaline-induced scratching in mice, providing support for potential efficacy in treating psychosis.

  DOI：

  10.1021/jm101414h
• 作为产物：
  描述：

  tert-butyl 4-(2-nitrophenyl)-5,6-dihydropyridine-1(2H)-carboxylate 在 palladium 10% on activated carbon 吡啶 、 盐酸 、 水 、 甲酸铵 、 sodium hydroxide 、 sodium nitrite 作用下， 以 1,4-二氧六环 、 industrial methylated spirit 、 乙醇 、 二氯甲烷 、 水 为溶剂， 反应 8.0h， 生成 4-(2-氯苯基)哌啶盐酸盐
  参考文献：
  名称：

  [EN] (4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE
  [FR] COMPOSÉS DE (4-PHÉNYL-PIPÉRIDIN-1-YL)-[5-1H-PYRAZOL-4-YL)-THIOPHÉN-3-YL]-MÉTHANONE ET LEUR UTILISATION

  摘要：

  本发明一般涉及治疗化合物领域。更具体地说，本发明涉及某些（4-苯基-哌啶-1-基）-[5-(1 H-吡唑-4-基)-噻吩-3-基]-甲酮化合物，其中包括抑制11β-羟基甾酮脱氢酶1（11β-HSD1）的作用。本发明还涉及包含这些化合物的药物组合物，以及利用这些化合物和组合物在体外和体内抑制11β-羟基甾酮脱氢酶1的用途；治疗通过抑制11β-羟基甾酮脱氢酶1而得到改善的疾病；治疗代谢综合征，其中包括2型糖尿病和肥胖等疾病，以及相关疾病，包括胰岛素抵抗、高血压、脂质紊乱和缺血性（冠状动脉）心脏病等心血管疾病；治疗轻度认知障碍和早期痴呆等中枢神经系统疾病，包括阿尔茨海默病等。

  公开号：

  WO2011033255A1

文献信息

• SULTAM DERIVATIVES
  申请人：Anderson Kevin W.

  公开号：US20110124686A1

  公开（公告）日：2011-05-26

  The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.

  本发明涉及符合式1的化合物，具有细胞毒活性。这些化合物可用于治疗癌症。
• [EN] TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS<br/>[FR] INHIBITEURS DE SÉCRÉTION DE PROTÉINE À BASE DE TRIAZACYCLODODÉCANSULFONAMIDE ("TCD")
  申请人：KEZAR LIFE SCIENCES

  公开号：WO2019178510A1

  公开（公告）日：2019-09-19

  Provided herein are triazacyclododecansulfonamide ("TCD")-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.

  本文提供了基于三氮杂环十二烷磺酰胺（"TCD"）的蛋白质分泌抑制剂，例如Sec61的抑制剂，其制备方法，相关的药物组合物，以及使用它们的方法。例如，本文提供了符合Formula（I）的化合物及其药用盐和包括它们的组合物。本文披露的化合物可以用于治疗炎症和/或癌症等疾病。
• [EN] BENZOSUBERONYLPIPERIDINE COMPOUNDS AS ANALGESICS<br/>[FR] COMPOSES DE BENZOSUBERONYLPIPERIDINE COMME ANALGESIQUES
  申请人：SMITHKLINE BEECHAM SPA

  公开号：WO2001083454A1

  公开（公告）日：2001-11-08

  Compounds of formula (I) or a derivative thereof, wherein; R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl; R1 is hydrogen or R; R2 is hydroxy, C¿1-6?alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R?3¿ is hydrogen or C¿1-6?alkyl; R?4 and R5¿ are each independently selected from the list consisting of perhaloC¿1-6?alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; with the proviso that, when R?3¿ is hydrogen, then R?4 and R5¿ are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo; are ligands of the ORL-1 receptor and are useful in therapy.

  式(I)或其衍生物的化合物，其中：R为C1-6烷基，C3-7环烷基，C1-6烷氧基，羟基，卤素，C1-6烯基，C1-6炔基，氨基，C1-6烷基氨基，二（C1-6烷基）氨基，羟基C1-6烷基，C1-6烷氧基C1-6烷基，氨基C1-6烷基，（C1-6烷基）氨基C1-6烷基，二（C1-6烷基）氨基C1-6烷基；R1为氢或R；R2为羟基，C1-6烷氧基，氨基，C1-6烷基氨基，二（C1-6烷基）氨基；R3为氢或C1-6烷基；R4和R5各自独立地从以下列表中选择：全卤素C1-6烷基，氢，卤素，C1-6烷基，C1-6烷氧基，羟基，氨基，C1-6烷基氨基，二（C1-6烷基）氨基，羟基C1-6烷基，C1-6烷氧基C1-6烷基，氨基C1-6烷基，（C1-6烷基）氨基C1-6烷基，二（C1-6烷基）氨基C1-6烷基，芳基和COX，其中X可以是羟基，C1-6烷氧基，C1-6烷基，氨基，C1-6烷基氨基或二（C1-6烷基）氨基；但是，当R3为氢时，R4和R5不同时为氢；其中任何烷基或含有此类基团的任何基团的烷基部分均可被卤素取代一次或多次；是ORL-1受体的配体，并且在治疗中有用。
• Benzosuberonylpiperdine compounds as analgesics
  申请人：——

  公开号：US20040029917A1

  公开（公告）日：2004-02-12

  Compounds of formula (I) or a derivative thereof, wherein; R is C 1-6 allkyl, C 3-7 cycloalkyl, C 1-6 alkoxy, hydroxy, halo, C 1-6 alkenyl, C 1-6 allkynyl, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, hydroxyC 1-6 alkyl, C 1-6 akoxyC 1-6 alkyl, aminoC 1-6 allkyl, (C 1-6 allkyl)aminoC 1-6 alkyl, di(C 1-6 allkyl)aminoC 1-6 alkyl; R 1 is hydrogen or R; R 2 is hydroxy, C 1-6 alkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino; R 3 is hydrogen or C 1-6 alkyl; R 4 and R 5 are each independently selected from the list consisting of perhaloC 1-6 alkyl, hydrogen, halo, C 1-6 alkyl, C 1-6 alkoxy, hydroxy, amino, C 1-6 akylamino, di(C 1-4 alkyl)amino, hydroxyC 1-6 alkyl, C 1-6 akoxyC 1-6 alkyl, aminoC 1-6 allkyl, (C 1-4 alkyl)aminoC 1-6 alkyl, di(C 1-4 alkyl)aminoC 1-4 alkyl, aryl, and COX wherein X may be hydroxy, C 1-6 alkoxy, C 1-6 alkyl, amino, C 1-6 alkylamino, or di(C 1-6 allkyl)amino; with the proviso that, when R 3 is hydrogen, then R R 4 and R 5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo; are ligands of the ORL-1 receptor and are useful in therapy. 1

  式(I)或其衍生物的化合物，其中：R是C1-6烷基，C3-7环烷基，C1-6烷氧基，羟基，卤素，C1-6烯基，C1-6炔基，氨基，C1-6烷基氨基，二（C1-6烷基）氨基，羟基C1-6烷基，C1-6烷氧基C1-6烷基，氨基C1-6烷基，（C1-6烷基）氨基C1-6烷基，二（C1-6烷基）氨基C1-6烷基；R1是氢或R；R2是羟基，C1-6烷氧基，氨基，C1-6烷基氨基，二（C1-6烷基）氨基；R3是氢或C1-6烷基；R4和R5各自独立地选自以下列表中的物种：全卤素C1-6烷基，氢，卤素，C1-6烷基，C1-6烷氧基，羟基，氨基，C1-6烷基氨基，二（C1-4烷基）氨基，羟基C1-6烷基，C1-6烷氧基C1-6烷基，氨基C1-6烷基，（C1-4烷基）氨基C1-6烷基，二（C1-4烷基）氨基C1-4烷基，芳基，和COX，其中X可以是羟基，C1-6烷氧基，C1-6烷基，氨基，C1-6烷基氨基或二（C1-6烷基）氨基；但是，当R3是氢时，R、R4和R5不能同时为氢；其中任何烷基或含有此类基团的任何基团的烷基部分可以被卤素取代一次或多次；是ORL-1受体的配体，并且在治疗中有用。
• (4-Phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone Compounds and Their Use
  申请人：Webster Scott Peter

  公开号：US20120172393A1

  公开（公告）日：2012-07-05

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

  本发明涉及治疗化合物领域。更具体地说，本发明涉及某些(4-苯基哌啶-1-基)-[5-(1H-吡唑-4-基)-噻吩-3-基]-甲酮化合物，其中包括抑制11β-羟化类固醇脱氢酶1型(11β-HSD1)的化合物。本发明还涉及包含此类化合物的制药组合物的使用，以及在体外和体内使用此类化合物和组合物以抑制11β-羟化类固醇脱氢酶1型；治疗由抑制11β-羟化类固醇脱氢酶1型改善的疾病；治疗代谢综合征，包括2型糖尿病和肥胖症等疾病，以及相关疾病，包括胰岛素抵抗、高血压、脂质代谢异常和心血管疾病，如缺血性(冠状)心脏病；治疗轻度认知障碍和早期痴呆等中枢神经系统疾病，包括阿尔茨海默病等。