Spiro[indoline-2,4-piperidin]-3-one | 1050596-44-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Spiro[indoline-2,4-piperidin]-3-one
• 英文别名: spiro[indoline-2,4'-piperidine]-3-one；spiro[indole-2,4'-piperidin]-3(1H)-one；1,3-Dihydrospiro[indole-2,4'-piperidine]-3-one；spiro[1H-indole-2,4'-piperidine]-3-one
• CAS: 1050596-44-5
• 化学式: C₁₂H₁₄N₂O
• 分子量: 202.256
• InChiKey: LOEMFMJJJALSDD-UHFFFAOYSA-N

物化性质

• 沸点：
  390.4±42.0 °C(Predicted)
• 密度：
  1.23±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-醛基四氢吡喃 、 Spiro[indoline-2,4-piperidin]-3-one 在 三乙酰氧基硼氢化钠 、 溶剂黄146 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以29%的产率得到N-(tetrahydro-2H-pyran-4-ylmethyl)spiro[indoline-2,4'-piperidin]-3-one
  参考文献：
  名称：

  Discovery and structure-activity relationships of spiroindolines as novel inducers of oligodendrocyte progenitor cell differentiation

  摘要：

  A novel series of spiroindoline derivatives was discovered for use as inducers of oligodendrocyte progenitor cell (OPC) differentiation, resulting from optimization of screening hit 1. Exploration of structure-activity relationships led to compound 18, which showed improved potency (rOPC EC50 = 0.0032 mu M). Furthermore, oral administration of compound 18 significantly decreased clinical severity in an experimental autoimmune encephalomyelitis (EAE) model.

  DOI：

  10.1016/j.bmc.2020.115348
• 作为产物：
  描述：

  ethyl 4-(2-bromophenylamino)-4-cyano-1-piperidinecarboxylate 在 氧气 盐酸 、 三乙基硼 、 水 、 三正丁基氢锡 作用下， 以 甲苯 为溶剂， 反应 66.0h， 生成 Spiro[indoline-2,4-piperidin]-3-one
  参考文献：
  名称：

  WO2008/103126

  摘要：

  公开号：

文献信息

• Novel Combination of Compounds to be Used in the Treatment of Airway Diseases, Especially Chronic Obstructive Pulmonary Disease (COPD) and Asthma
  申请人：Eriksson Tomas

  公开号：US20110124613A1

  公开（公告）日：2011-05-26

  The present invention provides a pharmaceutical product comprising, in combination of, (a) a (therapeutically effective) dose of a first active ingredient, which is a compound of formula (I) or a pharmaceutically acceptable salt thereof; and (b) a (therapeutically effective) dose of a second active ingredient, which is a glucocorticoid receptor agonist; and optionally, (c) a (therapeutically effective) dose of a third active ingredient, which is a β 2 -agonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treating treatment of airway diseases, especially chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kit in treatment of airway diseases such as COPD and asthma.

  本发明提供一种药物产品，其中包括以下组合物：(a)第一活性成分的(治疗有效)剂量，该成分是公式(I)的化合物或其药学上可接受的盐；和(b)第二活性成分的(治疗有效)剂量，该成分是糖皮质激素受体激动剂；可选的，(c)第三活性成分的(治疗有效)剂量，该成分是β2-激动剂。本发明还涉及包含该组合物的药物组合物以及通过给予该组合物治疗哺乳动物的呼吸道疾病，特别是慢性阻塞性肺疾病(COPD)和哮喘的方法。本发明还涉及一种包含该组合物的工具包以及在治疗COPD和哮喘等呼吸道疾病中使用该工具包的用途。
• NOVEL COMBINATION OF COMPOUNDS TO BE USED IN THE TREATMENT OF AIRWAY DISEASES, ESPECIALLY CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) AND ASTHMA
  申请人：AstraZeneca AB

  公开号：EP2120935A1

  公开（公告）日：2009-11-25
• [EN] NOVEL COMBINATION OF COMPOUNDS TO BE USED IN THE TREATMENT OF AIRWAY DISEASES, ESPECIALLY CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) AND ASTHMA<br/>[FR] NOUVELLE COMBINAISON DE COMPOSÉS UTILISÉS DANS LE TRAITEMENT DES MALADIES DES VOIES AÉRIENNES, EN PARTICULIER LA BRONCHOPNEUMOPATHIE CHRONIQUE OBSTRUCTIVE (COPD) ET L'ASTHME
  申请人：ASTRAZENECA AB

  公开号：WO2008103126A1

  公开（公告）日：2008-08-28

  [EN] The present invention provides a pharmaceutical product comprising, in combination of, (a) a (therapeutically effective) dose of a first active ingredient, which is a compound of formula (I) or a pharmaceutically acceptable salt thereof; and (b) a (therapeutically effective) dose of a second active ingredient, which is a glucocorticoid receptor agonist; and optionally, (c) a (therapeutically effective) dose of a third active ingredient, which is a ß₂-agonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treating treatment of airway diseases, especially chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kit in treatment of airway diseases such as COPD and asthma.
  [FR] La présente invention concerne un produit pharmaceutique combinant (a) une dose thérapeutiquement efficace d'un premier ingrédient actif qui est un composé représenté par la formule (I) ou un sel pharmaceutiquement acceptable de celui-ci; et (b) une dose thérapeutiquement efficace d'un deuxième ingrédient actif qui est un agoniste du récepteur des glucocorticoïdes, et éventuellement (c) une dose thérapeutiquement efficace d'un troisième ingrédient actif qui est un agoniste ß₂. L'invention concerne également des compositions pharmaceutiques contenant ladite combinaison et des méthodes de traitement des maladies des voies aériennes, en particulier la bronchopneumopathie chronique obstructive (COPD) et l'asthme, chez des mammifères par administration de ladite combinaison. L'invention concerne également un kit contenant ladite combinaison et l'utilisation dudit kit dans le traitement des maladies des voies aériennes telles que la bronchopneumopathie chronique obstructive (COPD) et l'asthme.
• [EN] DGK TARGETING COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS DE CIBLAGE DE DGK ET UTILISATIONS ASSOCIÉES
  申请人：[en]ARVINAS OPERATIONS, INC.

  公开号：WO2023150186A1

  公开（公告）日：2023-08-10

  Disclosed herein are compounds of Formula (A), or a pharmaceutically acceptable salt thereof, which inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα). These compounds are useful in the treatment of proliferative diseases (e.g., cancer) and viral infections.
• WO2008/103126
  申请人：——

  公开号：——

  公开（公告）日：——