1-Boc-4-(4-溴苯氨基)-哌啶 | 443998-65-0

• 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: 1-Boc-4-(4-溴苯氨基)-哌啶
• 中文别名: 4-(4-溴苯基)氨基-1-(叔丁氧羰基)哌啶；1-N-BOC-4-(4-溴-苯氨基)-哌啶；4-[(4-溴苯基)氨基]哌啶-1-羧酸叔丁酯；1-BOC-4-(4-溴苯氨基)-哌啶
• 英文名称: tert-butyl 4-((4-bromophenyl)amino)piperidine-1-carboxylate
• 英文别名: 4-(4-Bromophenyl)amino-1-(tert-butoxycarbonyl)piperidine；tert-butyl 4-(4-bromoanilino)piperidine-1-carboxylate
• CAS: 443998-65-0
• 化学式: C₁₆H₂₃BrN₂O₂
• mdl: MFCD07785997
• 分子量: 355.275
• InChiKey: ZDCRNXMZSKCKRF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.562
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-Boc-4-(4-溴苯氨基)-哌啶 在 Pd catalyst 、 三乙酰氧基硼氢化钠 、 sodium carbonate 、 溶剂黄146 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 26.0h， 生成 (1-Cyclopentyl-piperidin-4-yl)-(3'-trifluoromethyl-biphenyl-4-yl)-amine
  参考文献：
  名称：

  Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

  摘要：

  Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure-activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound I exhibited oral efficacy in chronic (28 d) rodent models at 3-30 mpk showing significant reduction in food intake and weight gain relative to controls.

  DOI：

  10.1021/jm0503852
• 作为产物：
  描述：

  N-叔丁氧羰基-4-哌啶酮 、 4-溴苯胺 生成 1-Boc-4-(4-溴苯氨基)-哌啶
  参考文献：
  名称：

  Erythropoietin production accelerator

  摘要：

  本发明涉及一种预防或治疗由于红细胞生成素减少引起的病理状态，或用于贫血，慢性贫血，肾性贫血，再生障碍性贫血或纯红细胞再生障碍的药物，该药物包含以下式（1）所表示的环状胺化合物作为活性成分：其中，R1，R2和R3各自独立地表示氢原子，卤素原子，羟基，烷基，卤代烷基，烷氧基，烷硫基，羧基，烷氧羰基或烷酰基；W1和W2各自独立地表示N或CH；X表示O，NR4，CONR4或NR4CO；R4表示氢原子，或烷基，烯基，炔基，取代或未取代芳基，取代或未取代杂芳基，取代或未取代芳基甲基，或取代或未取代杂芳基甲基基团；l，m和n各自表示0或1的数字，或其盐或溶剂化物。

  公开号：

  US20060040986A1

文献信息

• Cyclic amine compounds and pharmaceutical composition containing the same
  申请人：KOWA CO., LTD.

  公开号：US20040010147A1

  公开（公告）日：2004-01-15

  A cyclic amine compound represented by the following general formula (1): 1 wherein, R 1 , R 2 and R 3 each independently represent a hydrogen atom or an alkoxy group; W 1 and W 2 each independently represent N or CH; X represents O, NR 4 , CONR 4 or NR 4 CO; R 4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.

  以下是通用公式（1）表示的一个环胺化合物： 其中， R 1 ，R 2 和R 3 分别独立地表示氢原子或烷氧基； W 1 和W 2 分别独立地表示N或CH； X表示O，NR 4 ，CONR 4 或NR 4 CO； R 4 表示氢原子，或烷基，芳基，杂芳基，芳基烷基或杂芳基烷基； l，m和n分别表示0或1的数字， 提供其盐和水合物。 这些化合物对细胞粘附和细胞浸润均具有抑制作用，并可用作抗哮喘剂，抗过敏剂，抗风湿剂，抗动脉硬化剂，抗炎剂，抗干燥综合征剂等。
• [EN] 1, 4-SUBSTITUTED PIPERIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE PIPÉRIDINE 1,4-SUBSTITUÉS
  申请人：CEPHALON INC

  公开号：WO2016205633A1

  公开（公告）日：2016-12-22

  Described herein are 1,4-substituted piperidine compounds according to Formula (I) that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

  本文描述了按照式（I）的1,4-取代哌啶化合物，这些化合物已经表现出作为脂肪酸合成酶抑制剂的活性。本文还描述了含有所述1,4-取代哌啶化合物的药物组合物，以及通过给予所述化合物或药物配方中的一个或多个来治疗由脂肪酸合成酶介导的疾病的方法。本文还描述了合成所述化合物的方法，包括所述的1,4-取代哌啶化合物和在这些合成中有用的合成中间体。
• [EN] 3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE 3-(PYRAZOLYL)-1H-PYRROLO[2,3-B]PYRIDINE EN TANT QU'INHIBITEURS DE KINASE
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2014006554A1

  公开（公告）日：2014-01-09

  The present application relates to novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.

  本申请涉及一种新型的3-(吡唑基)-lH-吡咯并[2,3-b]吡啶衍生物，其化学式为(I)，作为蛋白激酶抑制剂。该发明特别涉及化合物的化学式(I)、化合物的制备以及其药物组成。该发明还涉及药用可接受的盐和组合物，包括所述新型的3-(吡唑基)-lH-吡咯并[2,3-b]吡啶衍生物及其在治疗各种疾病中的应用。
• Piperidine derivatives useful as CCR5 antagonists
  申请人：Schering Corporation

  公开号：US20040010008A1

  公开（公告）日：2004-01-15

  The present invention provides a compound of the formula 1 or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , R 9 , R 10 , A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

  本发明提供了一种具有化学式1的化合物或其药用可接受的盐或溶剂，其中R1、R2、R3、R9、R10、A和B如规范中定义。本发明还提供了含有本发明化合物的药物组合物，以及使用本发明化合物进行治疗的方法。该发明还涉及使用本发明化合物与一种或多种抗病毒或其他在治疗人类免疫缺陷病毒（HIV）中有用的药物的组合。该发明还涉及使用本发明化合物单独或与另一种药物组合在治疗实体器官移植排斥、移植物宿主病、关节炎、类风湿性关节炎、炎症性肠病、特应性皮炎、银屑病、哮喘、过敏或多发性硬化症中。
• [EN] TRIAZOLE DERIVATIVES WITH ANTIFUNGAL ACTIVITY<br/>[FR] DÉRIVÉS TRIAZOLES À ACTIVITÉ ANTIFONGIQUE
  申请人：KING S COLLEGE LONDON

  公开号：WO2021156636A1

  公开（公告）日：2021-08-12

  Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, Q2, L1 and n are as defined herein. The compounds have antifungal properties and are useful in the treatment of fungal infections, including infections that are resistant to conventions anti-fungal agents. Q1 is selected from: (Formulae Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ii, Ij and Ik) wherein * indicates the point of attachment to L1.

  揭示了公式(I)的化合物及其药学上可接受的盐，其中R1、R2、Q2、L1和n的定义如本文所述。这些化合物具有抗真菌性能，并可用于治疗真菌感染，包括对传统抗真菌药物产生耐药性的感染。Q1选自:(公式Ia、Ib、Ic、Id、Ie、If、Ig、Ih、Ii、Ij和Ik)，其中*表示与L1的连接点。