4-[(4-iodophenyl)oxy]-1-(1-methylethyl)piperidine | 684249-46-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 4-[(4-iodophenyl)oxy]-1-(1-methylethyl)piperidine
• 英文别名: 1-isopropyl-4-(4-iodophenoxy)piperidine；4-(4-iodophenoxy)-1-isopropylpiperidine；4-(4-iodophenoxy)-1-propan-2-ylpiperidine
• CAS: 684249-46-5
• 化学式: C₁₄H₂₀INO
• 分子量: 345.223
• InChiKey: RPNUOKVVEDMYMV-UHFFFAOYSA-N

物化性质

• 沸点：
  366.6±37.0 °C(Predicted)
• 密度：
  1.431±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-[(4-iodophenyl)oxy]-1-(1-methylethyl)piperidine 、 N-Boc-哌嗪 在 palladium diacetate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 、 sodium t-butanolate 作用下， 以 甲苯 为溶剂， 反应 3.17h， 以66%的产率得到1,1-dimethylethyl 4-(4-{[1-(1-methylethyl)-4-piperidinyl]oxy}phenyl)-1-piperazinecarboxylate
  参考文献：
  名称：

  [EN] SUBSTITUTED PIPERAZINES, (1,4) DIASZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS
  [FR] PIPERAZINES, (1,4) DIAZEPINES, ET 2,5-DIAZABICYCLO (2.2.1) HEPTANES SUBSTITUES EN TANT QU'ANTAGONISTES DE L'HISTAMINE H1 ET/OU H3 OU ANTAGONISTES INVERSES DE L'HISTAMINE H3

  摘要：

  本发明涉及具有药理活性的新型哌嗪和氮杂七元环衍生物，其制备方法，含有它们的组合物以及它们在治疗包括阿尔茨海默病在内的神经退行性疾病中的应用。

  公开号：

  WO2004035556A1
• 作为产物：
  描述：

  N-Boc-4-羟基哌啶 在 三乙酰氧基硼氢化钠 、 sodium hydride 、 溶剂黄146 、 三氟乙酸 作用下， 以 1,1-二氯乙烷 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 20.5h， 生成 4-[(4-iodophenyl)oxy]-1-(1-methylethyl)piperidine
  参考文献：
  名称：

  [EN] PLK-4 INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
  [FR] INHIBITEURS DE PLK4 ET MÉTHODE DE TRAITEMENT DU CANCER À L'AIDE DE CEUX-CI

  摘要：

  这项发明涉及一种由以下结构式（I）和（II）表示的化合物及其药学上可接受的盐：（结构式（I））；（结构式（IV））。由该结构式表示的化合物是激酶抑制剂，因此在此披露用于癌症治疗。结构式中变量的定义在此提供。

  公开号：

  WO2012048411A1

文献信息

• [EN] 4- (4-(HETEROCYCLYLALKOXY}PHENYL)-1-(HETEROCYCLYL-CARBONYL)PIPERIDINE DERIVATIVES AND RELATED COMPOUNDS AS HISTAMINE H3 ANTAGONISTS FOR THE TREATMENT OF NEUROLOGICAL DISEASES SUCH AS ALZHEIMER'S<br/>[FR] DERIVES DE 4-(4-(HETEROCYCLYLALKOXY)PHENYL-1-(HETEROCYCLYL-CARBONYL)PIPERIDINE ET COMPOSES ASSOCIES SERVANT D'ANTAGONISTES D'HISTAMINE H3 DESTINES AU TRAITEMENT DE TROUBLES NEUROLOGIQUES
  申请人：GLAXO GROUP LTD

  公开号：WO2004089373A1

  公开（公告）日：2004-10-21

  The present invention provides, in a first aspect, a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: R1 represents -C1-6 alkyl-O-C1-6 alkyl, -C3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl and other groups; X represents a bond, O, CO, OCH2, CH2O or SO2; Z represents CO, CONR10 or SO2; R10 represents hydrogen, C1-6 alkyl, -C3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl; A represents a single or a double bond; m and n independently represent 0, 1 or 2; R2 represents hydrogen, C1-6 alkyl or C1-6 alkoxy; R3 represents halogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, cyano, amino, -COC1-6 alkyl, -SO2C1-6 alkyl or trifluoromethyl; R4 represents -(CH2)q-NR11R12 or a group of formula (i) wherein all the other substituents are as defined in claim 1. Compounds of formula (I) and their pharmaceutically acceptable salts have affinity for and are antagonists and/or inverse agonists of the histamine H3 receptor and are believed to be of potential use in the treatment of neurological diseases including Alzheimer's disease.

  本发明在第一方面提供了一个式(I)的化合物或其药学上可接受的盐，其中：R1代表-C1-6烷基-O-C1-6烷基，-C3-8环烷基，芳基，杂环烷基，杂芳基和其他基团；X代表键，O，CO，O ，CH2O或SO2；Z代表CO，CONR10或SO2；R10代表氢，C1-6烷基，-C3-8环烷基，芳基，杂环烷基，杂芳基；A代表单键或双键；m和n独立地代表0，1或2；R2代表氢，C1-6烷基或C1-6烷氧基；R3代表卤素，C1-6烷基，羟基，C1-6烷氧基，氰基，氨基，-COC1-6烷基，-SO2C1-6烷基或三氟甲基；R4代表-(CH2)q-NR11R12或一个式(i)的基团，其中所有其他取代基的定义如权利要求1所述。式(I)的化合物及其药学上可接受的盐具有亲和力，并且是组织胺H3受体的拮抗剂和/或逆向激动剂，被认为在治疗包括阿尔茨海默病在内的神经系统疾病中具有潜在用途。
• PYRAZOLE DERIVATIVE
  申请人：Nakamura Toshio

  公开号：US20100113776A1

  公开（公告）日：2010-05-06

  A novel pyrazole derivative of the following formula having a histamine H3 receptor antagonistic effect: or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation comprising the same as an active ingredient is effective for prevention or treatment of dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.

  以下公式的新型吡唑酮衍生物具有组胺H3受体拮抗作用： 或其药用可接受盐，或包含其作为活性成分的药物制剂，对预防或治疗痴呆症、阿尔茨海默病、注意力缺陷多动障碍、精神分裂症、进食障碍、肥胖症、糖尿病、高脂血症、睡眠障碍、嗜睡症、睡眠呼吸暂停综合征、昼夜节律紊乱、抑郁症、过敏性鼻炎或其他疾病具有有效性。
• 4-(4-(Heterocyclylakoxy) phenyl-1-(heterocyclyl-carbonyl) piperidine derivavites and related compounds as histamine h3 antagonists for the treatment of neurological diseases such as alzheimer's
  申请人：Bamford James Mark

  公开号：US20060205774A1

  公开（公告）日：2006-09-14

  The present invention relates to novel phenyl piperidinyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

  本发明涉及具有药理活性的新型苯基哌啶衍生物，其制备过程，含有它们的组合物以及它们在神经和精神障碍治疗中的应用。
• SUBSTITUTED PIPERAZINES, (1,4) DIAZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS
  申请人：Ancliff Rachael

  公开号：US20100075953A1

  公开（公告）日：2010-03-25

  The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.

  本发明涉及具有药理活性的新型哌嗪和氮杂七环衍生物，其制备过程，包含它们的组合物以及它们在治疗神经退行性疾病，包括阿尔茨海默病中的应用。
• PHENYLPYRROLE DERIVATIVE
  申请人：TAISHO PHARMACEUTICAL CO., LTD.

  公开号：US20140330010A1

  公开（公告）日：2014-11-06

  Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds. Specifically, there are provided phenylpyrrole compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: Formula (I) [wherein Q refers to a group represented by the following formula (A) or (B):

  提供了一些新型化合物，这些化合物可用于预防或治疗痴呆症、阿尔茨海默病、注意力缺陷多动障碍、精神分裂症、癫痫、中枢性惊厥、肥胖症、糖尿病、高脂血症、嗜睡症、特发性嗜睡症、行为诱导性睡眠不足综合症、睡眠呼吸暂停综合症、昼夜节律紊乱、睡眠障碍、睡眠相关运动障碍、失眠症和抑郁症，或过敏性鼻炎，或这些化合物的药物可接受的盐。具体而言，提供了下式（I）所表示的苯基吡咯化合物或其药物可接受的盐：式（I）[其中Q是由下式（A）或（B）表示的基团：