3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine | 146396-08-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine
• 英文别名: 3-(,3,4-dichlorophenyl)-3-(2-hydroxy-ethyl)piperidine；3-(2-Hydroxyethyl)-3-(3,4-dichlorophenyl)-piperidine；(+)-2-[3-(3,4-dichlorophenyl)piperidin-3-yl]ethanol；3-(2-hydroxyethyl)-3-(3,4-dichlorophenyl)piperidine；3-(3,4-Dichlorophenyl)-3-(2-hydroxyethyl)piperidine；2-[3-(3,4-Dichlorophenyl)piperidin-3-yl]ethanol
• CAS: 146396-08-9
• 化学式: C₁₃H₁₇Cl₂NO
• 分子量: 274.19
• InChiKey: NFEQUCGNNCYRCD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine 在 sodium carbonate 作用下， 以 水 、 乙酸乙酯 为溶剂， 生成 1-(3,4,5-trimethoxy-benzoyl)-3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine
  参考文献：
  名称：

  Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases

  摘要：

  本发明涉及一种新颖的4-(1H-苯并咪唑-2-基)[1,4]二氮杂环庚烷衍生物及其立体异构体，以及其药学上可接受的盐，其作为组胺受体拮抗剂和速激肽受体拮抗剂具有用途。这些拮抗剂在过敏性鼻炎的治疗中有用，包括季节性鼻炎和鼻窦炎；炎症性肠病，包括克罗恩病和溃疡性结肠炎；哮喘；支气管炎；以及呕吐。

  公开号：

  US20010034343A1
• 作为产物：
  描述：

  3,4-二氯苯乙腈 在 盐酸 、 sodium hydroxide 、 sodium borohydrid 、 硫酸 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 水 为溶剂， 生成 3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine
  参考文献：
  名称：

  Substituted piperidines useful for the treatment of allergic diseases

  摘要：

  本发明涉及一种新型的取代哌啶衍生物，其化学式为其立体异构体和药学上可接受的盐，可用作组胺受体拮抗剂和速激肽受体拮抗剂。这类拮抗剂在治疗过敏性疾病中很有用，包括：季节性鼻炎、过敏性鼻炎和鼻窦炎。

  公开号：

  US06329392B1

文献信息

• [EN] QUATERNARY PIPERIDINE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS QUATERNAIRES DE PIPÉRIDINE ET LEURS UTILISATIONS
  申请人：ASTRAZENECA AB

  公开号：WO2010071575A1

  公开（公告）日：2010-06-24

  This invention generally relates to quaternary piperidine compounds, particularly substituted 3-phenylpiperidine compounds and salts thereof. This invention also relates to pharmaceutical compositions comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), and processes for making such a compound.

  这项发明通常涉及四元哌啶化合物，特别是取代的3-苯基哌啶化合物及其盐。这项发明还涉及包括这种化合物的药物组合物、这种化合物的用途（包括治疗方法和药物制剂等），以及制备这种化合物的方法。
• Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases
  申请人：Aventis Pharmaceuticals Inc.

  公开号：US06211199B1

  公开（公告）日：2001-04-03

  The present invention relates to novel substituted piperidine derivatives of formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

  本发明涉及一种新型的取代哌啶衍生物，其化学式为（1），其立体异构体以及药学上可接受的盐，这些衍生物可用作组胺受体拮抗剂和速激肽受体拮抗剂。这些拮抗剂在过敏性鼻炎的治疗中很有用，包括季节性鼻炎和鼻窦炎；炎症性肠病，包括克罗恩病和溃疡性结肠炎；哮喘；支气管炎；以及呕吐。
• Substituted 4-(1H-benzimidazol-2-yl)&lsqb;1,4&rsqb;diazepanes useful for the treatment of allergic disease
  申请人：Aventis Pharmaceuticals Inc.

  公开号：US06194406B1

  公开（公告）日：2001-02-27

  The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

  本发明涉及新颖的4-(1H-苯并咪唑-2-基)[1,4]二氮杂环庚烷衍生物的化合物（1）及其立体异构体，以及其药学上可接受的盐，这些化合物可用作组胺受体拮抗剂和速激肽受体拮抗剂。这些拮抗剂在过敏性鼻炎的治疗中很有用，包括季节性鼻炎和鼻窦炎；炎症性肠病，包括克罗恩病和溃疡性结肠炎；哮喘；支气管炎；以及呕吐。
• 1-azoniabicyclo[2.2.1] heptanes and pharmaceutical compositions in which
  申请人：Sanofi

  公开号：US05554763A1

  公开（公告）日：1996-09-10

  The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a .omega.-C.sub.1 -C.sub.4 -alkoxy(C.sub.2 -C.sub.4)alkyl, or a .omega.-C.sub.2 -C.sub.4 -alkanoyloxy (C.sub.1 -C.sub.4)alkyl;. Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form an azabicyclic or azatricyclic system optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

  该发明涉及以下结构的四元碱性酰胺：其中Ar是可选择取代的单、双或三环芳香族或杂芳族基团；T是直接键、羟甲亚基、烷氧基甲亚基（其中烷氧基是C.sub.1 -C.sub.4）、或C.sub.1 -C.sub.5 烷基亚基；Ar'是未取代或单或多取代的苯基、噻吩基、苯并噻吩基、萘基或吲哚基；R是氢或C.sub.1 -C.sub.4 烷基，或.ω.-C.sub.1 -C.sub.4 烷氧基(C.sub.2 -C.sub.4)烷基，或.ω.-C.sub.2 -C.sub.4 烷酰氧基(C.sub.1 -C.sub.4)烷基；Q是氢；或者Q和R一起形成1,2-乙烯基、1,3-丙烷基或1,4-丁烷基；Am.sup..sym.是基团：其中X.sub.1、X.sub.2和X.sub.3与它们连接的氮原子一起形成一个可能被苯基或苄基取代的氮杂双环或氮杂三环系统；A.sup..crclbar.是一种药用可接受的阴离子。这些化合物可用于制备用于治疗涉及缓激肽系统的病理状况的药物。
• 1-azoniabicyclo\x9b2.2.1!heptanes, method of preparing them and
  申请人：Sanofi

  公开号：US05679693A1

  公开（公告）日：1997-10-21

  The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tricyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl;. Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-AZONIABICYCLO\x9b2.2.1!HEPTANE optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

  该发明涉及公式为##STR1##的四元碱性酰胺，其中Ar是一个可选择取代的单环、双环或三环芳香或杂芳基团；T是直链键，羟甲亚基，烷氧甲亚基，其中烷氧基是C.sub.1 -C.sub.4，或C.sub.1 -C.sub.5-烷基亚基；Ar'是未取代或单取代或多取代的苯基，噻吩基，苯噻吩基，萘基或吲哚基；R是氢或C.sub.1 -C.sub.4-烷基，或C.sub.1 -C.sub.4-ω-烷氧基(C.sub.2 -C.sub.4)烷基，或C.sub.2 -C.sub.4-ω-烷酰氧基(C.sub.1 -C.sub.4)烷基；Q是氢；或者Q和R一起形成1,2-乙烯，1,3-丙烯或1,4-丁烯基团；Am.sup..sym.是基团##STR2##其中X.sub.1、X.sub.2和X.sub.3与它们连接的氮原子一起形成一个1-AZONIABICYCLO\x9b2.2.1!HEPTANE，该环可选择由苯基或苄基取代；A.sup..crclbar.是一种药用可接受的阴离子。这些化合物可用于制备用于治疗涉及Tachykinin系统的病理条件的药物。