1-(Ethoxycarbonyloxy)ethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(tetrazol-5-yl)phenyl]phenyl}-methylimidazole-5-carboxylate | 144689-80-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(Ethoxycarbonyloxy)ethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(tetrazol-5-yl)phenyl]phenyl}-methylimidazole-5-carboxylate
• 英文别名: 1-(ethoxycarbonyloxy)ethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[4-[2-(tetrazole-5-yl)phenyl]phenyl]methylimidazole-5-carboxylate；1-ethoxycarbonyloxyethyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
• CAS: 144689-80-5
• 化学式: C₂₉H₃₄N₆O₆
• 分子量: 562.626
• InChiKey: INQBJYBQZUVSCB-UHFFFAOYSA-N

物化性质

• 沸点：
  783.8±70.0 °C(Predicted)
• 密度：
  1.30±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  41
• 可旋转键数：
  14
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  154
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• 1-Biphenylimidazole derivatives, their preparation and their therapeutic use
  申请人：Sankyo Company Limited

  公开号：EP0503785A1

  公开（公告）日：1992-09-16

  Compounds of formula (I): in which: R¹ is alkyl or alkenyl; R² and R³ are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R⁴ is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula -SiRaRbRc, in which Ra, Rb and Rc are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R⁵ is carboxy or a group of formula -CONR⁸R⁹, in which R⁸ and R⁹ are hydrogen atoms or alkyl, or R⁸ and R⁹ together form alkylene; R⁶ is hydrogen, alkyl, alkoxy or halogen; R⁷ is carboxy or tetrazol-5-yl; and pharmaceutically acceptable salts and esters thereof have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. They may be prepared, inter alia, by reacting a biphenylmethyl compound with an imidazole compound.

  式(I)的化合物中：其中，R¹是烷基或烯基；R²和R³是氢、烷基、烯基、环烷基、芳基烷基、芳基或与环烷基融合的芳基；R⁴是氢、烷基、酰基烷基、烯酰基烷基、芳基羰基、烷氧羰基、四氢吡喃基、四氢硫吡喃基、四氢噻吩基、四氢呋喃基、式为-SiRaRbRc的基团，其中Ra、Rb和Rc是烷基或芳基、烷氧甲基、（烷氧基）甲基、卤代烷氧甲基、芳基烷基、芳基或酰氧甲氧羰基；R⁵是羧基或式为-CONR⁸R⁹的基团，其中R⁸和R⁹是氢原子或烷基，或R⁸和R⁹一起形成亚烷基；R⁶是氢、烷基、烷氧基或卤素；R⁷是羧基或四唑-5-基；其药学上可接受的盐和酯具有降压活性，可用于治疗和预防高血压。它们可以通过将联苯甲基化合物与咪唑化合物反应制备而成。
• PHARMACEUTICAL FOR PREVENTION OR TREATMENT OF BONE METABOLIC DISEASE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP1884240A1

  公开（公告）日：2008-02-06

  The present invention provides a medicament for preventing or treating bone metabolic diseases, comprising as an active ingredient an angiotensin II receptor antagonist. A prophylactic or therapeutic agent for bone metabolic diseases, comprising as an active ingredient a compound represented by the following general formula (I), a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof: wherein R1 represents a C1-C4 alkyl group; R2 and R3 are the same or different and each represent a hydrogen atom or a C1-C4 alkyl group; R4 represents a hydrogen atom or a C1-C4 alkyl group; R5 represents a hydrogen atom, a C1-C4 alkyl group, a C2-C5 alkanoyloxymethyl or 1-(C2-C5 alkanoyloxy)ethyl group, a C1-C4 alkoxycarbonyloxymethyl or 1-(C1-C4 alkoxycarbonyloxy)ethyl group, a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl group, a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl or a phthalidyl group; and R6 represents a carboxy group or a tetrazole-5-yl group.

  本发明提供了一种预防或治疗骨代谢疾病的药物，其活性成分包括血管紧张素 II 受体拮抗剂。 一种预防或治疗骨代谢疾病的药物，其活性成分包括由下通式(I)代表的化合物、其药理学上可接受的盐或其药理学上可接受的酯： 其中 R1 代表 C1-C4 烷基； R2 和 R3 相同或不同，各自代表氢原子或 C1-C4 烷基； R4 代表氢原子或 C1-C4 烷基； R5代表氢原子、C1-C4烷基、C2-C5烷酰氧基甲基或1-(C2-C5烷酰氧基)乙基、C1-C4烷氧基羰酰氧基甲基或1-(C1-C4烷氧基羰酰氧基)乙基、(5-甲基-2-氧代-1,3-二氧戊烯-4-基)甲基、(5-苯基-2-氧代-1,3-二氧戊烯-4-基)甲基或酞酰基；以及 R6 代表羧基或四唑-5-基。
• MEDICINAL AGENT FOR PREVENTION OR TREATMENT OF ALZHEIMER'S DISEASE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2174666A1

  公开（公告）日：2010-04-14

  The present invention provides a medicament for preventing or treating Alzheimer's disease or mild cognitive impairment which is an early state of cognitive impairment including Alzheimer's disease, comprising an angiotensin II receptor blocker as an active ingredient. A prophylactic or therapeutic agent for Alzheimer's disease or mild cognitive impairment which is an early state of cognitive impairment including Alzheimer's disease, comprising an angiotensin II receptor blocker as an active ingredient.

  本发明提供了一种预防或治疗阿尔茨海默病或轻度认知障碍（包括阿尔茨海默病在内的认知障碍的早期状态）的药物，其活性成分包括血管紧张素II受体阻滞剂。 一种阿尔茨海默病或轻度认知障碍（包括阿尔茨海默病在内的认知障碍的早期状态）的预防或治疗药物，包含一种血管紧张素 II 受体阻滞剂作为活性成分。
• Pharmaceutical for prevention or treatment of bone metabolic disease
  申请人：Morishita Ryuuichi

  公开号：US20090082411A1

  公开（公告）日：2009-03-26

  A method for treating a bone metabolic disease by administering to a human a pharmacologically effective amount of an angiotensin II receptor antagonist which is a compound of the following formula (I), a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof: wherein R 1 represents a C 1 -C 4 alkyl; R 2 and R 3 are the same or different and each represent hydrogen or a C 1 -C 4 alkyl; R 4 represents hydrogen or a C 1 -C 4 alkyl; R 5 represents hydrogen, a C 1 -C 4 alkyl, a C 2 -C 5 alkanoyloxymethyl, 1 -(C 2 -C 5 alkanoyloxy)ethyl, a C 1 -C 4 alkoxycarbonyloxymethyl, 1 -(C 1 -C 4 alkoxycarbonyloxy)ethyl, a ( 5 -methyl- 2 -oxo- 1,3 -dioxolen- 4 -yl)methyl, a ( 5 -phenyl- 2 -oxo- 1,3 -dioxolen- 4 -yl)methyl or a phthalidyl; and R 6 represents a carboxy or a tetrazole- 5 -yl.
• MEDICAL AGENT FOR PREVENTION OR TREATMENT OF ALZHEIMER 'S DISEASE
  申请人：Morishita Ryuichi

  公开号：US20100130567A1

  公开（公告）日：2010-05-27

  A method of treating or preventing Alzheimer's disease or mild cognitive impairment which is an early state of cognitive impairment including Alzheimers' disease by administering a pharmacologically effective amount of an angiotensin II receptor blocker. A method of improving cerebral circulation or cerebral blood flow disorder by administering a pharmacologically effective amount of an angiotensin II receptor blocker. A method of treating or preventing amyloid β-induced brain disfunction by administering a pharmacologically effective amount of an angiotensin II receptor blocker.