6,7,8,9-tetrahydro-dibenzofuran-3-ol | 34855-67-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 6,7,8,9-tetrahydro-dibenzofuran-3-ol
• 英文别名: 3-Hydroxy-6,7,8,9-tetrahydro-dibenzofuran；6,7,8,9-Tetrahydrodibenzofuran-3-ol
• CAS: 34855-67-9
• 化学式: C₁₂H₁₂O₂
• 分子量: 188.226
• InChiKey: NZQLDDRKACJBHY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  33.4
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
  申请人：CAO Bin

  公开号：US20100075994A1

  公开（公告）日：2010-03-25

  The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本发明涉及一系列取代二氢和四氢噁唑嘧啶酮，具体地说，涉及一系列式(I)的2-取代-2,3-二氢-噁唑并[3,2-a]嘧啶-7-酮和2-取代-2,3,5,6-四氢-噁唑并[3,2-a]嘧啶-7-酮： 其中p、n、X、Y、R1、R2、R3、R4、R5、R6、R7和R8如本文所定义。本发明还涉及制备这些化合物的方法，包括新颖的中间体。本发明的化合物是代谢型谷氨酸受体（mGluR）的调节剂，特别是mGluR2受体。因此，本发明的化合物在药物制剂中具有用途，特别是在治疗和/或预防各种中枢神经系统疾病（CNS）方面，包括但不限于急性和慢性神经退行性疾病、精神病、癫痫、焦虑、抑郁、偏头痛、疼痛、睡眠障碍和呕吐。
• NOVEL TRICYCLIC COMPOUNDS HAVING SATURATED RINGS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0997458A1

  公开（公告）日：2000-05-03

  Compounds represented by general formula (I) or their salts, having β3 -adrenoceptor agonism and being efficacious when employed in drugs for treating and preventing diabetes, obesity, hyperlipemia, etc. wherein R represents hydrogen or methyl; R1 represents hydrogen, halogeno, hydroxy, benzyloxy, amino or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4', or nitro (wherein R3 represents hydrogen, methyl, SO2R5, formyl or CONHR6'; R5 represents lower alkyl, benzyl or NR4R4'; R4 and R4' may be the same or different and each represents hydrogen, lower alkyl or benzyl; and R6' represents hydrogen or lower alkyl); R6 represents hydrogen or lower alkyl; n is 1 or 2; X represents secondary nitrogen, oxygen or sulfur; and when n is 1, then one of R7 and R8 represents hydrogen while another represents hydrogen, amino, acetylamino or hydroxy, or when n is 2, then R8 represents hydrogen while R7 represents hydrogen, amino, acetylamino or hydroxy.

  通式(I)所代表的化合物或其盐类，具有 β3-肾上腺素受体激动作用，在用于治疗和预防糖尿病、肥胖症、高血脂症等药物时具有疗效。其中 R 代表氢或甲基；R1 代表氢、卤素、羟基、苄氧基、氨基或羟甲基；R2 代表氢、羟甲基、NHR3、SO2NR4R4'或硝基（其中 R3 代表氢、甲基、SO2R5、甲酰基或 CONHR6'；R5 代表低级烷基、苄基或 NR4R4'；R4 和 R4'可以相同或不同，各自代表氢、低级烷基或苄基；和 R6' 代表氢或低级烷基）；R6 代表氢或低级烷基；n 为 1 或 2；X 代表仲氮、氧或硫；当 n 为 1 时，则 R7 和 R8 中的一个代表氢，而另一个代表氢、氨基、乙酰氨基或羟基，或当 n 为 2 时，则 R8 代表氢，而 R7 代表氢、氨基、乙酰氨基或羟基。
• NOVEL HETEROCYCLIC COMPOUNDS AND DRUG COMPOSITIONS CONTAINING THE SAME
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1142883A1

  公开（公告）日：2001-10-10

  The present invention is directed to a compound of the general formula (I): wherein R1 represents a hydrogen atom, a methyl group or SO2R3; R2 represents O, S or H2; R2' represents O or H2; R3 represents a lower alkyl group or NH4R4'; R4 and R4' may be the same or different and represent a hydrogen atom, a lower alkyl group or a benzyl group; R5 represents a hydrogen atom or a lower alkyl group; k and m are zero or 1; A represents the general formula (II) or (III): X1 represents a secondary nitrogen atom, an oxygen atom, a sulfur atom or a methylene group; n is 1 or 2; X2 represents a secondary nitrogen atom, an oxygen atom or a sulfur atom; and, R6, R7 and R8 are a hydrogen atom or the like; and a salt thereof. The compound of the present invention provides a pharmaceutical composition for treating and preventing β3-associated diseases, such as diabetes, obesity and hyperlipidemia. The composition is particularly suitable for oral administration.

  本发明涉及通式（I）的化合物： 其中 R1 代表氢原子、甲基或 SO2R3；R2 代表 O、S 或 H2；R2'代表 O 或 H2；R3 代表低级烷基或 NH4R4'；R4 和 R4'可以相同或不同，并代表氢原子、低级烷基或苄基；R5 代表氢原子或低级烷基；k 和 m 为 0 或 1；A 代表通式（II）或（III）： X1代表仲氮原子、氧原子、硫原子或亚甲基；n为1或2；X2代表仲氮原子、氧原子或硫原子；以及，R6、R7和R8为氢原子或类似物；及其盐。本发明的化合物提供了一种药物组合物，用于治疗和预防与β3相关的疾病，如糖尿病、肥胖症和高脂血症。该组合物特别适合口服给药。
• US6172099B1
  申请人：——

  公开号：US6172099B1

  公开（公告）日：2001-01-09
• US8642603B2
  申请人：——

  公开号：US8642603B2

  公开（公告）日：2014-02-04