N-甲基-N-[(3R)-吡咯烷-3-基]乙酰胺 | 550370-81-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: N-甲基-N-[(3R)-吡咯烷-3-基]乙酰胺
• 英文名称: N-Methyl-N-[(3R)-pyrrolidin-3-YL]acetamide
• CAS: 550370-81-5
• 化学式: C₇H₁₄N₂O
• 分子量: 142.2
• InChiKey: KOEKUQRWTOSZOR-SSDOTTSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-(1H-Pyrazol-4-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene-2-carboxylic acid 、 N-甲基-N-[(3R)-吡咯烷-3-基]乙酰胺 以to give 180 (24.3 mg, M+1 438.1)的产率得到N-methyl-N-{(R)-1-[8-(1H-pyrazol-4-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene-2-carbonyl]-pyrrolidin-3-yl}-acetamide
  参考文献：
  名称：

  BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

  摘要：

  公式I中的苯并噻吩化合物，包括立体异构体、几何异构体、互变异构体、溶剂化物、代谢物和其药学上可接受的盐，其中：Z1为CR1或N；Z2为CR2或N；Z3为CR3或N；Z4为CR4或N；当(i) X1为N且X2为S，(ii) X1为S且X2为N，(iii) X1为CR7且X2为S，(iv) X1为S且X2为CR7，(v) X1为NR8且X2为N，(vi) X1为N且X2为NR8，(vii) X1为CR7且X2为O，(viii) X1为O且X2为CR7，(ix) X1为CR7且X2为C(R7)2，(x) X1为C(R7)2且X2为CR7，(xi) X1为N且X2为O，或(xii) X1为O且X2为N，对于抑制脂质激酶，包括p110α和其他PI3K的亚型，并用于治疗由脂质激酶介导的癌症等疾病有用。本文还公开了使用公式I化合物在哺乳动物细胞中进行体外、体内和原位诊断、预防或治疗此类疾病或相关病理条件的方法。

  公开号：

  US20110076291A1

文献信息

• Melanin Concentrating Hormone Receptor-1 Antagonist Pyridinones
  申请人：Armour R. Duncan

  公开号：US20080085884A1

  公开（公告）日：2008-04-10

  The present invention provides for MCHR1 antagonist compounds of formula (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein the substituents are as defined herein, and the pharmaceutically acceptable salts, solvates and prodrugs thereof, which are useful in treating diseases or conditions wherein antagonism of the MCHR1 receptor is beneficial.

  本发明提供了式（I）的MCHR1拮抗剂化合物及其药用盐、溶剂合物和前药，其中取代基如本文所定义，并且其药用盐、溶剂合物和前药，可用于治疗对MCHR1受体拮抗有益的疾病或症状。
• HETEROAROMATIC COMPOUNDS AS VANIN INHIBITORS
  申请人：Boehringer Ingelheim International GmbH

  公开号：US20200172508A1

  公开（公告）日：2020-06-04

  The present invention encompasses compounds of the formula I which are suitable for the treatment of diseases related to Vanin, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.

  本发明涵盖了适用于治疗与Vanin相关疾病的化合物I的公式，以及制备这些化合物的方法、含有这些化合物的药物制剂，以及它们的使用方法。
• NEW PYRIDONE DERIVATES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
  申请人：Stenkamp Dirk

  公开号：US20080255083A1

  公开（公告）日：2008-10-16

  The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R 1 , R 2 , have the meanings given in claim 1 . Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的化合物，其中B、k、L、U、V、W、X、Y、Z、R1、R2的基团和基团具有权利要求1中所给出的含义。此外，本发明涉及含有至少一种根据本发明的化合物的制药组合物。由于它们的MCH受体拮抗活性，本发明的制药组合物适用于治疗代谢障碍和/或进食障碍，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。
• Pyridazine Derivatives with MCH Antagonistic Activity and Medicaments Comprising These Compounds
  申请人：Lehmann-Lintz Thorsten

  公开号：US20100197908A1

  公开（公告）日：2010-08-05

  The present invention relates to compounds of general formula I wherein the groups and radicals B, W, X, Y, Z, R 1 , R 2 , have the meanings given in claim 1 . Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的化合物，其中基团和基团B、W、X、Y、Z、R1、R2的含义如权利要求书1所述。此外，本发明还涉及含有本发明中至少一种化合物的制药组合物。由于其MCH受体拮抗活性，本发明中的制药组合物适用于治疗代谢性疾病和/或饮食障碍，特别是肥胖症、暴食症、厌食症、暴食症和糖尿病。
• BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
  申请人：Blaquiere Nicole

  公开号：US20110076291A1

  公开（公告）日：2011-03-31

  Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z 1 is CR 1 or N; Z 2 is CR 2 or N; Z 3 is CR 3 or N; Z 4 is CR 4 or N; and where (i) X 1 is N and X 2 is S, (ii) X 1 is S and X 2 is N, (iii) X 1 is CR 7 and X 2 is S, (iv) X 1 is S and X 2 is CR 7 ; (v) X 1 is NR 8 and X 2 is N, (vi) X 1 is N and X 2 is NR 8 , (vii) X 1 is CR 7 and X 2 is O, (viii) X 1 is O and X 2 is CR 7 , (ix) X 1 is CR 7 and X 2 is C(R 7 ) 2 , (x) X 1 is C(R 7 ) 2 and X 2 is CR 7 ; (xi) X 1 is N and X 2 is O, or (xii) X 1 is O and X 2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

  公式I中的苯并噻吩化合物，包括立体异构体、几何异构体、互变异构体、溶剂化物、代谢物和其药学上可接受的盐，其中：Z1为CR1或N；Z2为CR2或N；Z3为CR3或N；Z4为CR4或N；当(i) X1为N且X2为S，(ii) X1为S且X2为N，(iii) X1为CR7且X2为S，(iv) X1为S且X2为CR7，(v) X1为NR8且X2为N，(vi) X1为N且X2为NR8，(vii) X1为CR7且X2为O，(viii) X1为O且X2为CR7，(ix) X1为CR7且X2为C(R7)2，(x) X1为C(R7)2且X2为CR7，(xi) X1为N且X2为O，或(xii) X1为O且X2为N，对于抑制脂质激酶，包括p110α和其他PI3K的亚型，并用于治疗由脂质激酶介导的癌症等疾病有用。本文还公开了使用公式I化合物在哺乳动物细胞中进行体外、体内和原位诊断、预防或治疗此类疾病或相关病理条件的方法。