N-acetyl-methylpyrrolidine | 124929-52-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: N-acetyl-methylpyrrolidine
• 英文别名: 1-(3-Methylpyrrolidin-1-yl)ethanone
• CAS: 124929-52-8
• 化学式: C₇H₁₃NO
• 分子量: 127.186
• InChiKey: RVZZDKDDOIOTEX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  1-[3-(Pyridin-2-ylsulfanylmethyl)-pyrrolidin-1-yl]-ethanone 在 nickel boride 、 硼酸 作用下， 以64%的产率得到N-acetyl-methylpyrrolidine
  参考文献：
  名称：

  The use of acyl derivatives of -hydroxy-2-thiopyridone in a simple synthesis of pyrrolidines and tetrahydrofurans

  摘要：

  DOI：

  10.1016/s0040-4039(00)99175-5

文献信息

• FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
  申请人：Corkey Britton Kenneth

  公开号：US20120289493A1

  公开（公告）日：2012-11-15

  The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R 1 , X 1 , X 2 , Y and R 2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

  本公开涉及一类为钠通道抑制剂的化合物，以及它们在治疗各种疾病状态中的应用，包括心血管疾病和糖尿病。在特定实施例中，该化合物的结构由式I给出： 其中Q、R1、X1、X2、Y和R2如本文所述，以及制备和使用该化合物的方法，以及含有该化合物的药物组合物。
• [EN] AMIDO-THIOPHENE COMPOUNDS AND THEIR USE AS 11-BETA-HSD1 INHIBITORS<br/>[FR] COMPOSÉS AMIDO-THIOPHÈNE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE 11-BÊTA-HSD1
  申请人：UNIV EDINBURGH

  公开号：WO2009074789A1

  公开（公告）日：2009-06-18

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene 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. Formula (I).

  本发明一般涉及治疗化合物领域。更具体地，本发明涉及某些酰胺噻吩化合物，其中包括抑制11β-羟基类固醇脱氢酶1（11β-HSD1）。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-羟基类固醇脱氢酶1；治疗通过抑制11β-羟基类固醇脱氢酶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、脂质紊乱和心血管疾病，如缺血性（冠状）心脏病；治疗中枢神经系统疾病，如轻度认知障碍和早期痴呆，包括阿尔茨海默病等。公式（I）。
• Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826
  申请人：Bennett Stuart Norman Lile

  公开号：US20110092526A1

  公开（公告）日：2011-04-21

  A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.

  公式(I)的化合物：以及药理可接受的盐，其中变量组在内部定义；它们用于抑制11βHSD1，制造它们的过程以及包含它们的药物组合物也在本文中描述。
• AMINOPYRIDINE AND CARBOXYPYRIDINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
  申请人：Allen Jennifer R.

  公开号：US20100160280A1

  公开（公告）日：2010-06-24

  Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , X 1 , X 2 , and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , X 1 , X 2 , and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

  吡啶和嘧啶化合物： 或者是根据说明书中定义的药用可接受盐，其中m、n、R1、R2、R3、R4、R5、R6、R7、X1、X2、X3、X4、X5、X6、X7、X8和Y都有所定义； 或者是根据说明书中定义的药用可接受盐，其中环A、m、n、y、R2、R3、R4、R5、R6、R7、R8、R9、X1、X2和环A都有所定义； 或者是根据说明书中定义的药用可接受盐，其中m、n、y、R2、R3、R4、R5、R6、R7、R9、X1、X2和环A都有所定义；含有它们的组合物以及制备这类化合物的方法。还提供了通过抑制PDE10治疗可治疗的疾病或病症的方法，例如肥胖、非胰岛素依赖型糖尿病、精神分裂症、双相情感障碍、强迫症等。
• [EN] PYRIDAZINE DERIVATIVES AS FACTOR XIA INHIBITORS<br/>[FR] DÉRIVÉS DE LA PYRIDAZINE INHIBITEURS DU FACTEUR XIA
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2009114677A1

  公开（公告）日：2009-09-17

  The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

  本发明提供了式（I）的化合物：或其立体异构体、互变异构体或药学上可接受的盐，其中变量A、L1、L2、R2、R11和M如本文所定义。这些化合物是选择性因子XIa抑制剂或fXIa和血浆激肽原的双重抑制剂。本发明还涉及包含这些化合物的药物组合物以及使用它们治疗血栓栓塞和/或炎症性疾病的方法。