5,5-dimethyl-5,6,7,8-tetrahydronaphthalen-2-ol | 51438-95-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 5,5-dimethyl-5,6,7,8-tetrahydronaphthalen-2-ol
• 英文别名: 1,1-Dimethyl-6-hydroxy-1,2,3,4-tetralin；1,1-Dimethyl-6-tetralol；1,1-Dimethyl-tetralol-(6)；5,5-dimethyl-5,6,7,8-tetrahydro-2-naphthol；5,5-dimethyl-7,8-dihydro-6H-naphthalen-2-ol
• CAS: 51438-95-0
• 化学式: C₁₂H₁₆O
• 分子量: 176.258
• InChiKey: JKROICWEDYNFMA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  5,5-dimethyl-5,6,7,8-tetrahydronaphthalen-2-ol 在 乙醇 、 potassium carbonate 作用下， 以 甲醇 、 丙酮 为溶剂， 反应 193.0h， 生成 (S)-2-(5,5-dimethyl-5,6,7,8-tetrahydro-naphthalen-2-yloxymethyl)-6-ethyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-one
  参考文献：
  名称：

  [EN] SUBSTITUTED DIHYDRO BENZOCYCLOALKYLOXYMETHYL OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
  [FR] DIHYDRO-BENZOCYCLOALKYL-OXYMÉTHYL-OXAZOLOPYRIMIDINONES SUBSTITUÉES, LEUR PRÉPARATION ET LEUR UTILISATION

  摘要：

  本发明涉及一系列取代二氢苯并环烷氧甲基噁唑嘧啶酮化合物，其化学式为（I），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，本发明的化合物可作为药物剂，特别是在治疗和/或预防各种中枢神经系统疾病（CNS）方面有用，包括但不限于急性和慢性神经退行性疾病、精神病、认知缺陷疾病、癫痫、焦虑、抑郁、偏头痛、疼痛、睡眠障碍和呕吐。

  公开号：

  WO2011034830A1
• 作为产物：
  描述：

  4-甲基-3-戊烯酸 在 三氯化铝 作用下， 反应 2.0h， 生成 5,5-dimethyl-5,6,7,8-tetrahydronaphthalen-2-ol
  参考文献：
  名称：

  Alkylation of Phenol with a Homoallylic Halide

  摘要：

  DOI：

  10.1021/ja00903a047

文献信息

• [EN] GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE<br/>[FR] INHIBITEURS DE GLYCOLATE OXYDASE POUR LE TRAITEMENT D'UNE MALADIE
  申请人：BIOMARIN PHARM INC

  公开号：WO2020257487A1

  公开（公告）日：2020-12-24

  Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.

  本文描述了化合物、制备这种化合物的方法、含有这种化合物的药物组合物和药物，以及使用这种化合物治疗或预防与甘氧酸代谢缺陷相关的疾病或紊乱的方法，例如与甘氧酸氧化酶（GO）或草酸代谢变化相关的疾病或紊乱。这些疾病或紊乱包括与产生过多草酸相关的甘氧酸代谢紊乱，例如原发性高草酸尿症。
• Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
  申请人：Inoue Tadashi

  公开号：US20060100460A1

  公开（公告）日：2006-05-11

  This invention provides a compound of the formula (I): wherein R 1 represents a (C 1 -C 6 )alkyl group; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C 1 -C 6 ) alkyl group or a (C 1 -C 6 ) alkoxy group; R 3 , R 4 , R 5 and R 6 each independently represents a hydrogen atom, a (C 1 -C 6 ) alkyl, or a halogen atom; R 7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C 1 -C 6 ) alkyl group optionally substituted with a piperidino group, a (C- 1 -C 6 )alkoxy group optionally substituted with a 3-7 membered cycloalkyl ring, a hydroxy(C 1 -C 6 )alkoxy group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy group, a halo (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkylthio group, a (C 1 -C 6 )alkylsulfinyl group or a (C 1 -C 6 )alkylsulfonyl group; R 5 represents a (C 1 -C 6 )alkyl group, a halo(C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy group, a hydroxy(C 1 -C 6 )alkoxy group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl group or a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy group; or R 7 and R 8 , when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy group and a hydroxy(C 1 -C 6 )alkyl group; and R 9 represents a hydrogen atom or a halogen atom; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor, such as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula (I).

  这项发明提供了一种化合物，其化学式为（I）：其中R1代表（C1-C6）烷基基团；R2代表氢原子、卤原子、羟基、（C1-C6）烷基基团或（C1-C6）氧烷基基团；R3、R4、R5和R6分别独立地代表氢原子、（C1-C6）烷基或卤原子；R7代表氢原子、卤原子、羟基、（C1-C6）烷基基团，可选地取代有哌啶基团的（C1-C6）烷基基团，可选地取代有3-7个成员的环烷基环的（C-1-C6）氧烷基基团，羟基（C1-C6）氧烷基基团，（C1-C6）氧烷基（C1-C6）烷基基团，（C1-C6）氧烷基（C1-C6）氧烷基基团，卤代（C1-C6）烷基基团，（C1-C6）烷基硫基基团，（C1-C6）烷基亚硫基基团或（C1-C6）烷基砜基基团；R8代表（C1-C6）烷基基团，卤代（C1-C6）烷基基团，（C1-C6）氧烷基基团，羟基（C1-C6）氧烷基基团，（C1-C6）氧烷基（C1-C6）烷基基团或（C1-C6）氧烷基（C1-C6）氧烷基基团；或者R7和R8，当相邻时，与它们连接的碳原子一起形成一个5-8成员的脂环或杂环环，其中脂环或杂环环未取代或取代有一个或多个选自羟基、（C1-C6）烷基、（C1-C6）氧烷基和羟基（C1-C6）烷基的取代基；R9代表氢原子或卤原子；或其药学上可接受的盐或溶剂。这些化合物可用于治疗由VR1受体过度激活引起的疾病症状，如哺乳动物中的疼痛等。本发明还提供了一种包含化合物（I）的药物组成物。
• 2-Aminomethyl phenol derivative and process for preparing thereof
  申请人：Ono Pharmaceutical Co., Ltd.

  公开号：US04254056A1

  公开（公告）日：1981-03-03

  A 2-aminomethyl phenol derivative of the formula (I): ##STR1## wherein X is a halogen atom; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different are each a hydrogen atom or a straight or branched chain alkyl group having 1 to 4 carbon atoms; n is 2, 3, 4 or 5 and a pharmaceutically acceptable acid addition salt thereof are disclosed. Also disclosed is a process for preparing such derivative or a pharmaceutically acceptable acid addition salt thereof.

  本发明公开了一种公式(I)的2-氨甲基苯酚衍生物：##STR1## 其中，X是卤素原子；R1、R2、R3和R4可以相同也可以不同，分别是氢原子或1到4个碳原子的直链或支链烷基；n为2、3、4或5，以及其药学上可接受的酸加盐。还公开了制备这种衍生物或其药学上可接受的酸加盐的方法。
• SUBSTITUTED DIHYDRO BENZOCYCLOALKYLOXYMETHYL OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
  申请人：SHER Rosy

  公开号：US20120184566A1

  公开（公告）日：2012-07-19

  The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 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, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本发明涉及一系列取代二氢苯并环烷氧甲基噁唑嘧啶酮化合物，其化学式为(I)：其中n，R1，R2，R3，R4，R5和R6如本文所定义。本发明还涉及制备这些化合物的方法，包括新型中间体。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，本发明的化合物在制药领域中有用，特别是在治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经退行性病变，精神病，认知缺陷障碍，惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐等方面。
• Substituted dihydro benzocycloalkyloxymethyl oxazolopyrimidinones, preparation and use thereof
  申请人：Sher Rosy

  公开号：US09051331B2

  公开（公告）日：2015-06-09

  The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 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, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本发明涉及一系列取代的二氢苯并环烷氧甲基噁唑嘧啶酮化合物，其化学式为（I）：其中n，R1，R2，R3，R4，R5和R6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性谷氨酸受体（mGluR）的调节剂，特别是mGluR2受体。因此，本发明的化合物在医药领域中有用途，特别是在治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经退行性疾病，精神病，认知缺陷障碍，惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐等方面。