2,3-Dihydro-pyrano[2,3-B]pyridin-4-one | 1196153-27-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡喃吡啶类
• 英文名称: 2,3-Dihydro-pyrano[2,3-B]pyridin-4-one
• 英文别名: 2,3-dihydropyrano[2,3-b]pyridin-4-one
• CAS: 1196153-27-1
• 化学式: C₈H₇NO₂
• mdl: MFCD09834583
• 分子量: 149.15
• InChiKey: BRXWJQKRZSDABL-UHFFFAOYSA-N

物化性质

• 沸点：
  305.7±31.0 °C(Predicted)
• 密度：
  1.274±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  39.2
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Heterocyclic derivatives as metabotropic glutamate receptor modulators
  申请人：Merz Pharma GmbH & Co. KGaA

  公开号：EP2650284A1

  公开（公告）日：2013-10-16

  The invention relates to heterocyclic derivatives of formula I as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.

  这项发明涉及公式I的杂环衍生物及其药学上可接受的盐。该发明还涉及制备这类化合物的方法。该发明的化合物是mGluR5调节剂，因此对于控制和预防急性和/或慢性神经系统疾病是有用的。
• [EN] ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS D'ÉTHYNYLE A TITRE DE MODULATEURS DU RÉCEPTEUR MÉTABOTROPIQUE DU GLUTAMATE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2017009275A1

  公开（公告）日：2017-01-19

  The present invention relates to compounds of formula I wherein R1 is lower alkyl; R2 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; n is 0, 1 or 2; V/U are independently from each other O or CH2, wherein V and U cannot be simultaneously O; L is a five or six membered heteroaryl group, selected from or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

  本发明涉及式I的化合物，其中R1为较低的烷基；R2为苯基或吡啶基，吡啶基中的N原子可能位于不同位置；n为0、1或2；V/U分别为O或CH2，其中V和U不能同时为O；L为选自五元或六元杂环芳基团的杂环芳基团，选择自药用盐或酸加盐，对于外消旋混合物，或对应的对映体和/或光学异构体和/或立体异构体。这些化合物可用于治疗帕金森病、焦虑症、呕吐、强迫症、自闭症、神经保护、癌症、抑郁症和2型糖尿病。
• Substituted pyrano[2,3-B]pyridine derivatives as cannabinoid-1 receptor modulators
  申请人：Debenham John S.

  公开号：US20080207666A1

  公开（公告）日：2008-08-28

  Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

  结构式（I）的新化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，并可用于治疗、预防和抑制CB1受体介导的疾病。本发明的化合物可用作中枢作用药物，治疗精神病、记忆障碍、认知障碍、阿尔茨海默病、偏头痛、神经病、神经炎性疾病，包括多发性硬化症和吉兰-巴雷综合征，以及病毒性脑炎、脑血管意外和头部创伤的炎症后遗症、焦虑症、压力、癫痫、帕金森病、亨廷顿病运动障碍和精神分裂症。这些化合物还可用于治疗物质滥用障碍、肥胖或进食障碍，以及哮喘、便秘、慢性肠假性梗阻、肝硬化、非酒精性脂肪肝病（NAFLD）、非酒精性脂肪性肝炎（NASH）和促进清醒。
• Azolidinedione derivatives
  申请人：PFIZER INC.

  公开号：EP0306251A2

  公开（公告）日：1989-03-08

  A series of novel spiro-heteroazolones derived from a 2,3-dihydropyrano[2,3-b]pyridine ring system have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical member compounds include spiro-imides, spiro-oxazolidinediones, spiro-thiazolidinediones and spiroimidazolidinediones derived from the aforesaid ring system. (4'S)(2'R)-6'-Chloro-2',3'-dihydro-2'-methyl-spiro-[imidazolidine-4,4'-4'H-py- rano[2,3-b]pyridine]-2,5-dione represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.

  我们制备出了一系列新型螺杂环唑酮类化合物，它们来自 2,3-二氢吡喃并[2,3-b]吡啶环系统，包括其药学上可接受的盐类。这些化合物可作为醛糖还原酶抑制剂用于治疗，以控制某些慢性糖尿病并发症。典型的成员化合物包括由上述环系统衍生的螺烷基亚胺、螺烷基噁唑烷二酮、螺烷基噻唑烷二酮和螺烷基咪唑烷二酮。(4'S)(2'R)-6'-氯-2',3'-二氢-2'-甲基-螺-[咪唑烷-4,4'-4'H-吡喃并[2,3-b]吡啶]-2,5-二酮代表了一种典型的优选成员化合物。本文提供了用已知起始原料制备所有这些化合物的方法。
• Ethynyl derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US10189848B2

  公开（公告）日：2019-01-29

  The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

  本发明涉及代谢型谷氨酸受体 4 (mGluR4) 的正性异位调节剂 (PAM)，可用于治疗帕金森病、焦虑、呃逆、强迫症、自闭症、神经保护、癌症、抑郁症和 2 型糖尿病等疾病。