Tetrahydropyracrimycin | 35783-62-1

• 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: Tetrahydropyracrimycin
• 英文别名: Tetrahydropyracrimycin A；3-pyrrolidin-2-yl-propionamide；3-(Pyrrolidin-2-yl)propanamide；3-pyrrolidin-2-ylpropanamide
• CAS: 35783-62-1
• 化学式: C₇H₁₄N₂O
• mdl: MFCD19204952
• 分子量: 142.201
• InChiKey: MMCMQHRSBRWQPT-UHFFFAOYSA-N

物化性质

• 沸点：
  326.3±15.0 °C(Predicted)
• 密度：
  1.018±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.857
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• SUBSTITUTED PIPERAZINYL-PHENYL-OXAZOLIDINONE DERIVATIVES AND THEIR USE AS ANTI-BACTERIAL AGENTS
  申请人：ZENECA LIMITED

  公开号：EP0918769A1

  公开（公告）日：1999-06-02
• [EN] SUBSTITUTED PIPERAZINYL-PHENYL-OXAZOLIDINONE DERIVATIVES AND THEIR USE AS ANTI-BACTERIAL AGENTS<br/>[FR] DERIVES SUBSTITUES DE PIPERAZINYLE-PHENYLE-OXAZOLIDINONE ET LEUR UTILISATION EN TANT QU'AGENTS ANTIBACTERIENS
  申请人：——

  公开号：WO1998001446A1

  公开（公告）日：1998-01-15

  [EN] The invention concerns a compound of formula (I) wherein, for example: R<1> is of the formula -NHC(=O)R wherein R is for example (1-4C)alkyl; R<2> and R<3> are independently hydrogen or fluoro; R<4> and R<5> are independently hydrogen or methyl; R<6> is a 6-membered heteroaryl ring containing 2 or 3 ring nitrogen atoms as the only ring heteroatoms, and optionally substituted by substituents selected from (1-4C)alkyl (optionally substituted), halo, trifluoromethyl, (1-4C)alkylS(O)n- (wherein n is 0, 1 or 2), (1-4C)alkylS(O)2amino, (1-4C)alkanoylamino, carboxy, hydroxy, amino, (1-4C)alkylamino, di-(1-4C)alkylamino, (1-4C)alkoxycarbonyl, carbamoyl, N-(1-4C)alkylcarbamoyl, di-(N-(1-4C)alkyl)carbamoyl [wherein the (1-4C)alkyl group or groups in the last two-mentioned carbamoyl substituents is optionally substituted by hydroxy, (1-4C)alkoxy or (1-4C)alkoxycarbonyl], (2-4C)alkenyl (optionally substituted by carboxy or (1-4C)alkoxycarbonyl), (1-4C)alkoxy, cyano or nitro; pharmaceutically-acceptable salts, suitable N-oxides and in-vivo-hydrolysable esters thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
  [FR] L'invention concerne un composé représenté par la formule (I) dans laquelle, par exemple: R<1> représente la formule -NHC(=O)R dans laquelle R représente, par exemple, alkyle C1-C4; R<2> et R<3> représentent hydrogène ou fluoro; R<4> et R<5> représentent indépendamment hydrogène ou méthyle; R<6> représente une chaîne hétéroaryle à 6 éléments contenant 2 ou 3 atomes d'azote en tant que seuls hétéroatomes de chaîne, et éventuellement substitué par des substituants sélectionnés dans alkyle C1-C4 (éventuellement substitué), halo, trifluorométhyle, alkyle C1-C4 S(O)n- (dans laquelle n est 0, 1 ou 2), alkyle C1-C4 S(O)2amino, alkanoylamino C1-C4, carboxy, hydroxy, amino, alkylamino C1-C4, dialkylamino C1-C4, alkoxycarbonyle C1-C4, carbamoyle, N-alkylcarbamoyle C1-C4, di-(N-alkyle C1-C4)carbamoyle [dans laquelle le ou les groupes alkyle C1-C4 dans les deux derniers substituants de carbamoyle sont éventuellement substitués par hydroxy, alkoxy C1-C4 ou alkoxycarbonyle C1-C4], alkényle C2-C4 (éventuellement substitué par carboxy ou alkoxycarbonyle C1-C4), alkoxy C1-C4, cyano ou nitro; ses sels acceptables sur le plan pharmaceutique, ses N-oxydes appropriés et ses esters hydrolysables in-vivo; leurs procédés de préparation; des compositions pharmaceutiques les contenant et leur utilisation en tant qu'agents antibactériens.
• [EN] INHIBITORS OF STAT3 AND USES THEREOF<br/>[FR] INHIBITEURS DU STAT3 ET LEURS UTILISATIONS
  申请人：UNIV TEXAS

  公开号：WO2010118309A2

  公开（公告）日：2010-10-14

  Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.