N,r-2,c-4,c-6-2,4,6-tetramethylpiperidine | 860113-58-2

• 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: N,r-2,c-4,c-6-2,4,6-tetramethylpiperidine
• 英文别名: N,r-2,c-4,t-6-2,4,6-tetramethylpiperidine；N,r-2,t-4,c-6-2,4,6-tetramethylpiperidine；1,2,4,6-tetramethyl-piperidine；1,2,4,6-Tetramethyl-piperidin；1,2,4,6-Tetramethylpiperidine
• CAS: 860113-58-2
• 化学式: C₉H₁₉N
• 分子量: 141.257
• InChiKey: HGOBOOSDBONHTB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  2,4,6-三甲哌啶 、 碘甲烷 生成 N,r-2,c-4,c-6-2,4,6-tetramethylpiperidine
  参考文献：
  名称：

  v. Auwers, Journal fur praktische Chemie (Leipzig 1954), 1922, vol. <2> 105, p. 110

  摘要：

  DOI：

文献信息

• [EN] SPIRO[CYCLOPENTANE-1,3'-INDOLIN]-2'-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS<br/>[FR] DÉRIVÉS SPIRO[CYCLOPENTANE-1,3'-INDOLIN]-2'-ONE UTILISÉS EN TANT QU'INHIBITEURS DE BROMODOMAINES
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2018109650A1

  公开（公告）日：2018-06-21

  The present invention provides spiro[cyclopentaneane-1,3'-indolin]-2'-one derivatives of formula (I), which are therapeutically useful, more particularly as bromodomain inhibitors. (I) wherein Cy, R1, R2, L and 'm' have the meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use as bromodomain inhibitors in the treatment and prevention of the associated diseases or disorders. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the spiro[cyclopentane-1,3'-indolin]-2'-one derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefore.

  本发明提供了式(I)的螺[环戊烷-1,3'-吲哚]-2'-酮衍生物，其在治疗上具有用途，更具体地作为溴结构域抑制剂。其中Cy、R1、R2、L和'm'在说明书中给出的含义，以及它们的药学上可接受的盐或药学上可接受的立体异构体，在治疗和预防疾病或紊乱方面具有用途，特别是它们作为溴结构域抑制剂在治疗和预防相关疾病或紊乱方面的用途。本发明还提供了该化合物的制备以及包括至少一种式(I)的螺[环戊烷-1,3'-吲哚]-2'-酮衍生物的药物配方，以及药学上可接受的载体、稀释剂或赋形剂。
• METHODS FOR FORMING SATURATED (HETERO)CYCLIC BORYLATED HYDROCARBONS AND RELATED COMPOUNDS
  申请人：BOARD OF TRUSTEES OF MICHIGAN STATE UNIVERSITY

  公开号：US20180051042A1

  公开（公告）日：2018-02-22

  The disclosure relates to methods for forming at least partially saturated cyclic and heterocyclic borylated hydrocarbons, as well as related compounds, which can be precursor compounds in the synthesis of any of a variety of pharmaceutical or medicinal compounds with a desired structure and/or stereochemistry for drug synthesis or drug candidate evaluation. The methods generally include reduction of an unsaturated cyclic or heterocyclic borylated hydrocarbon having a boron-containing substituent at an sp 2 -carbon, where such reduction converts the sp 2 -carbon to an sp 3 -carbon at the point of attachment of the boron-containing substituent. The methods can exhibit a selectivity for syn-addition during reduction, which can provide stereospecific products, such as when the unsaturated cyclic or heterocyclic reactant is multiply substituted with boron groups and/or other functional groups.

  本发明涉及用于形成至少部分饱和的环状和杂环硼化烃的方法，以及相关的化合物，这些化合物可以是合成多种具有所需结构和/或立体化学的药物或药用化合物的前体化合物。这些方法通常包括将具有sp2碳上含硼取代基的不饱和环状或杂环硼化烃还原，这样的还原将sp2碳转化为与含硼取代基连接点上的sp3碳。这些方法在还原过程中可表现出对顺式加成的选择性，从而可以提供立体特异性产物，例如当不饱和环状或杂环反应物上多元取代硼基团和/或其他功能基团时。
• NOVEL COMPOUNDS
  申请人：Hauel Norbert

  公开号：US20110294775A1

  公开（公告）日：2011-12-01

  Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases. The following is exemplary:

  新颖的化合物，可用于治疗急性疼痛、内脏疼痛、神经痛、炎症/疼痛受体介导的疼痛、肿瘤疼痛和头痛疾病。以下是示例：
• CARBOSTYRIL DERIVATIVES
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP0450066A1

  公开（公告）日：1991-10-09

  This invention relates to carbostyril derivatives represented by general formula (1), a process for their preparation, and an agent for inhibiting agglutination of platelets containing them as an active ingredient, wherein A represents a lower alkylene group, R1 represents a substituted or unsubstituted cycloalkyl-lower alkyl group, a cycloalkyl group, a tetrahydropyranyl* lower alkyl group, a lower alkylenedioxy-substituted lower alkyl group, a substituted phenyl-lower alkyl group or a lower alkyl-substituted piperidinyl-lower alkyl group, R2 represents a substituted or unsubstituted 5- or 6-membered, saturated or unsaturated heterocyclic-lower alkyl group, a tetrahydropyranylthio-lower alkyl group, a pyridylthio-lower alkyl group, a lower alkylene-dioxy-substituted lower alkyl group or a substituted or unsubstituted lower alkyl group, and the carbon-to-carbon bond between the 3- position and the 4-position of the carbostyril skeleton represents either a single or a double bond.

  本发明涉及通式(1)代表的碳化二氢吡啶衍生物、其制备工艺以及含有其作为活性成分的抑制血小板凝集的制剂，其中A代表低级亚烷基，R1代表取代或未取代的环烷基-低级烷基、环烷基、四氢吡喃基*低级烷基、低级亚烷基-二氧基取代的低级烷基、取代的苯基-低级烷基或低级烷基-取代的哌啶基-低级烷基、R2 代表取代或未取代的 5 或 6 元、饱和或不饱和杂环低级烷基、四氢吡喃硫基低级烷基、吡啶硫基低级烷基、亚烷基二氧基取代的低级烷基或取代或未取代的低级烷基，碳四吡啶骨架的 3 位和 4 位之间的碳-碳键代表单键或双键。
• Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：EP2357173A1

  公开（公告）日：2011-08-17

  Die vorliegende Erfindung betrifft Alkin-Verbindungen der allgemeinen Formel I in der die Gruppen und Reste A, B, W, X, Y, Z, R1 und R2 die in Anspruch 1 angegebenen Bedeutungen aufweisen. Ferner betrifft die Erfindung Arzneimittel enthaltend mindestens ein erfindungsgemäßes Alkin. Auf Grund der MCH-Rezeptor antagonistischen Aktivität eignen sich die erfindungsgemäßen Arzneimittel zur Behandlung von metabolischen Störungen und/oder Essstörungen, insbesondere von Obesitas, Bulimie, Anorexie, Hyperphagia und Diabetes.

  本发明涉及通式 I 的炔化合物 其中基团 A、B、W、X、Y、Z、R1 和 R2 具有权利要求 1 中给出的含义。本发明还涉及含有至少一种根据本发明的炔类化合物的药物。由于具有 MCH 受体拮抗活性，根据本发明的药物适用于治疗代谢紊乱和/或饮食失调，特别是肥胖症、贪食症、厌食症、多食症和糖尿病。