5-Boc-5-氮杂螺[2.4]庚烷-1-羧酸 | 150543-61-6

• 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: 5-Boc-5-氮杂螺[2.4]庚烷-1-羧酸
• 中文别名: 5-BOC-5-氮杂螺[2.4]庚烷-1-羧酸
• 英文名称: 5-(Tert-butoxycarbonyl)-5-azaspiro[2.4]heptane-1-carboxylic acid
• 英文别名: 5-[(2-methylpropan-2-yl)oxycarbonyl]-5-azaspiro[2.4]heptane-2-carboxylic acid
• CAS: 150543-61-6
• 化学式: C₁₂H₁₉NO₄
• mdl: MFCD12198550
• 分子量: 241.28
• InChiKey: QXRGGYBREHVBNA-UHFFFAOYSA-N

物化性质

• 沸点：
  377.4±25.0 °C(Predicted)
• 密度：
  1.23±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

文献信息

• NAPHTHYRIDINES AS INHIBITORS OF HPK1
  申请人：Genentech, Inc.

  公开号：US20180282328A1

  公开（公告）日：2018-10-04

  Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

  萘啶化合物及其作为HPK1抑制剂的用途被描述。这些化合物在治疗HPK1依赖性疾病和增强免疫反应方面很有用。还描述了抑制HPK1的方法、治疗HPK1依赖性疾病的方法、增强免疫反应的方法以及制备萘啶化合物的方法。
• [EN] MASP INHIBITORY COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS INHIBITEURS DE MASP ET LEURS UTILISATIONS
  申请人：BAYER AG

  公开号：WO2020225095A1

  公开（公告）日：2020-11-12

  The present invention relates to novel Mannose-binding lectin (MBL)-associated serine protease (MASP) inhibitory compounds, as well as analogues and derivatives thereof, to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of renal and cardiovascular disorders and of ischemia reperfusion injuries.

  本发明涉及新型甘霖结合凝集素（MBL）相关丝氨酸蛋白酶（MASP）抑制化合物，以及其类似物和衍生物，以及其制备方法，单独或组合用于治疗和/或预防疾病，以及用于生产药物治疗和/或预防疾病，特别是用于治疗和/或预防肾脏和心血管疾病以及缺血再灌注损伤。
• NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES
  申请人：FUNDACIÓN PARA LA INVESTIGACIÓN MÉDICA APLICADA

  公开号：US20160002246A1

  公开（公告）日：2016-01-07

  It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B 1 is a radical selected from the group consisting of formula (A″), formula (B″), formula (C″), and formula (D″):

  它涉及到一些具有多环结构和羟胺酸基团的化合物，其中多环结构包括至少三个环系统，其中一个环系统是由2至4个环组成的多环环系统；至少一个环是芳香环；结构中包含至少3个氮原子和1个氧原子。它还涉及到它们的制备过程，以及包含它们的制药组合物，以及它们在医学上的应用，特别是在治疗和/或预防伴随认知缺陷或损伤或神经退行性疾病的神经系统疾病中。其中B1是从公式（A''）、公式（B''）、公式（C''）和公式（D''）组成的基团。
• Azaspiroheptanes and octanes and processes for their production
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：EP0550025A1

  公开（公告）日：1993-07-07

  The present invention relates to certain novel azasprio derivatives of following formula(I), which are especially useful as intermediates for the preparation of quinolone carboxylic acid derivatives posssessed with a broad spectrum of potent anti-bacterial activities; and the novel processes for preparing these intermediates. wherein: R₁ isa hydrogen atom, an optionally substituted C₁₋₂₀ alkyl, optionally substituted benzyl, or nitrogen protecting group; R₂ isa hydrogen atom or a methyl group which is preferably substituted at the 4- or 6-position carbon; R₃ is-CO₂H, -CON₃, -NCO, -CONHR₁₀ wherein R₁₀ is a hydrogen atom, a benzyl, C₁₋₈ alkyl, or C₁₋₅ alkoxycarbonyl group, or -(CH₂)mY wherein m is 0 or 1 and Y is a hydroxyl, C₂₋₅ acyloxy, mesyloxy, p-toluensulfonyloxy or amino group which is optionally substituted with one or two C₁₋₄ alkyl radicals, with one C₁₋₄ alkanoyl radical, with one benzoyl radical or with one nitrogen protecting radical metabolizable in vivo; and the carbon atom to which R₃ is attached is a chiral carbon atom which has the stereochemical configuration of (1,3)-R,S, (1,3)-R,R, (1,3)-S,S or (1,3)-S, R; and n is1 or 2.

  本发明涉及下式(I)的某些新型氮杂环丁烷衍生物，这些衍生物特别适用于制备具有广谱强效抗菌活性的喹诺酮羧酸衍生物的中间体；本发明还涉及制备这些中间体的新型工艺。 其中 R₁ 是氢原子、任选取代的 C₁₋₂₀ 烷基、任选取代的苄基或氮保护基团； R₂ 是氢原子或甲基，甲基最好在 4 位或 6 位碳上被取代； R₃是-CO₂H、-CON₃、-NCO、-CONHR₁₀，其中 R₁₀ 是氢原子、苄基、C₁₋₈烷基或 C₁₋₅烷氧基羰基，或-(CH₂)mY，其中 m 是 0 或 1，Y 是羟基、C₂₋₅ 酰氧基、间氧基、其中 m 为 0 或 1，Y 为羟基、酰氧基、间氧基、对甲苯磺酸氧基或氨基，可任选被一个或两个 C₁₋₄烷基、一个 C₁₋₄烷酰基、一个苯甲酰基或一个可在体内代谢的氮保护基取代；与 R₃ 连接的碳原子是手性碳原子，其立体化学构型为 (1,3)-R,S、(1,3)-R,R、(1,3)-S,S 或 (1,3)-S,R；以及 n 为 1 或 2。
• Naphthyridines as inhibitors of HPK1
  申请人：Genentech, Inc.

  公开号：US10407424B2

  公开（公告）日：2019-09-10

  Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

  介绍了萘啶类化合物及其作为 HPK1 抑制剂的用途。这些化合物可用于治疗 HPK1 依赖性疾病和增强免疫反应。还描述了抑制 HPK1 的方法、治疗 HPK1 依赖性疾病的方法、增强免疫反应的方法以及制备萘啶化合物的方法。