2,3,4,5-四氢-1H-吡啶并[4,3-b]氮杂卓 | 233264-75-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 中文名称: 2,3,4,5-四氢-1H-吡啶并[4,3-b]氮杂卓
• 英文名称: 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]azepine
• CAS: 233264-75-0
• 化学式: C₉H₁₂N₂
• mdl: MFCD06656944
• 分子量: 148.208
• InChiKey: FUNKWXDYVOJNKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.444
• 拓扑面积：
  24.9
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] BENZAMIDE DERIVATIVES AS VASOPRESSIN ANTAGONISTS<br/>[FR] DERIVES DE BENZAMIDE ANTAGONISTES VIS-A-VIS DE LA VASOPRESSINE
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：WO1999037637A1

  公开（公告）日：1999-07-29

  (EN) A compound of formula (I) wherein A is an optionally substituted heterocyclic group; R is a lower alkoxy; Z is C=O or CH2; and B is a saturated or unsaturated condensed ring group selected from the group consisting of benzazepinyl, benzodiazepinyl, pyridoazepinyl, pyridodiazepinyl, thienoazepinyl, benzoxazepinyl, benzothiazepinyl, imidazobenzazepinyl, pyridobenzoxazepinyl and indolinyl, each member being optionally substituted, and a salt thereof, which possess vasopressin antagonistic activity and are useful as vasopressin antagonists.(FR) L'invention concerne un composé de formule (I) et un sel de ce composé. Dans ladite formule, A est un groupe hétérocyclique éventuellement substitué, R est alcoxy inférieur, Z est C=O ou CH2; et B est un groupe cyclique condensé saturé ou insaturé choisi dans la série comprenant benzazépinyle, benzodiazépinyle, pyridoazépinyle, pyridodiazépinyle, thiénoazépinyle, benzoxazépinyle, benzothiazépinyle, imidazobenzazépinyle, pyridobenzoxazépinyle et indolinyle, chaque élément étant éventuellement substitué. Ledit composé, qui a une activité antagoniste vis-à-vis de la vasopressine, est utile comme antagoniste vis-à-vis de la vasopressine.

  化合物的化学式为（I），其中A是可选取代的杂环基团；R是较低的烷氧基；Z是C=O或CH2；B是选择自苯并氮杂环基、苯并二氮杂环基、吡啶并氮杂环基、吡啶并二氮杂环基、噻吩并氮杂环基、苯并噁唑杂环基、苯并噻唑杂环基、咪唑苯并氮杂环基、吡啶苯并噁唑杂环基和吲哚基的饱和或不饱和的融合环基团，每个成员均可选取代，以及其盐。该化合物具有抗利尿激素拮抗活性，并可用作抗利尿激素拮抗剂。
• Pyridine derivative
  申请人：Astellas Pharma Inc.

  公开号：US10421762B2

  公开（公告）日：2019-09-24

  The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

  本发明要解决的问题是提供一种适用于药物组合物的化合物，特别是一种用于治疗夜尿症的药物组合物。 本发明者假定，抑制胎盘亮氨酸氨肽酶（P-LAP）（即能裂解 AVP 的氨肽酶）的夜间活性将维持和/或增加内源性 AVP 水平，从而增强抗利尿作用，这将有助于减少夜间排尿次数，并对抑制 P-LAP 的化合物进行了广泛研究。 结果，本发明人发现(2R)-3-氨基-2-[4-（取代的吡啶）-2-基]甲基}-2-羟基丙酸衍生物具有极佳的 P-LAP 抑制活性。本发明者评估了水负荷大鼠的抗利尿作用，发现这些化合物通过抑制 P-LAP 增加了内源性 AVP 水平，从而减少了尿量。因此，本发明提供的化合物有望用作基于 P-LAP 抑制作用的夜尿症治疗剂。
• Process for preparing substituted biphenyls
  申请人：BASF SE

  公开号：US10683256B2

  公开（公告）日：2020-06-16

  The present invention relates to a process for preparing substituted biphenyls via Suzuki coupling using specific phosphorus ligands and a solvent mixture containing water, a non-polar organic solvent and a polar aprotic co-solvent.

  本发明涉及一种利用特定磷配体和含有水、非极性有机溶剂和极性钝化助溶剂的混合溶剂，通过铃木偶联制备取代联苯的工艺。
• Organic reactions carried out in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：US10836688B2

  公开（公告）日：2020-11-17

  The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose.

  本发明涉及一种在有羟基烷基纤维素或烷基纤维素存在的水溶液中进行有机反应的方法。
• Stabilizer composition
  申请人：BASF SE

  公开号：US11001698B2

  公开（公告）日：2021-05-11

  The present invention relates to a stabilizer composition containing at least one sterically hindered amine (HALS) in which the amino group carries a basicity-reducing substituent, at least one antioxidant containing one or more thioether groups and at least one liquid plasticizer containing carboxylate groups. The invention further relates to a polymer composition containing at least one sterically hindered amine (HALS) in which the amino group carries a basicity-reducing substituent, at least one antioxidant containing one or more thioether groups, at least one liquid plasticizer containing carboxylate groups and at least one silyl-terminated polymer, to the use of the stabilizer composition for stabilizing a silyl-terminated polymer or a sealant, adhesive, gasket, knifing filler or coating composition, especially a sealant, adhesive, gasket, knifing filler or coating composition containing a silyl-terminated polymer, against degradation by heat, light and/or oxygen, to the use of the polymer composition as or in a sealant, adhesive, liquid gasket, knifing filler or coating composition, and to a sealant composition or an adhesive composition, or a gasket composition, or a knifing filler composition or a coating composition comprising the polymer composition.

  本发明涉及一种稳定剂组合物，其中至少含有一种氨基带有还原碱性取代基的立体受阻胺（HALS）、至少一种含有一个或多个硫醚基团的抗氧化剂和至少一种含有羧酸基团的液体增塑剂。本发明还涉及一种聚合物组合物，该组合物含有至少一种氨基带有碱性还原取代基的立体受阻胺 （HALS）、至少一种含有一个或多个硫醚基团的抗氧化剂、至少一种含有羧酸基团的液体增塑剂和至少一种硅烷封端聚合物，该稳定剂组合物可用于稳定硅烷封端聚合物或密封剂、粘合剂、垫圈、刀具填料或涂层组合物、稳定剂组合物用于稳定密封剂、粘合剂、垫片、切削填充剂或涂层组合物，特别是含有硅烷基封端聚合物的密封剂、粘合剂、垫片、切削填充剂或涂层组合物，使其不受热、光和/或氧的影响而降解；稳定聚合物组合物作为密封剂、粘合剂、液体垫片、切削填充剂或涂层组合物或在其中使用；稳定包含聚合物组合物的密封剂组合物、粘合剂组合物、垫片组合物、切削填充剂组合物或涂层组合物。