(6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-3,4,6,7-tetrahydroimidazo[4,5-c]pyridin-1-ium-6-carboxylate

• 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: (6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-3,4,6,7-tetrahydroimidazo[4,5-c]pyridin-1-ium-6-carboxylate
• 化学式: C31H32N4O3
• 分子量: 508.6
• InChiKey: YSTVFDAKLDMYCR-NDEPHWFRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  78.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• 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。
• METHOD OF TREATING ABNORMAL TISSUE PROLIFERATION BY ADMINISTERING AN ANGIOTENSIN II ANTAGONIST
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0625902A1

  公开（公告）日：1994-11-30
• 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.
• METHOD FOR INHIBITING THE INDUCTION AND FORMATION OF OSTEOCLASTS
  申请人：Morishita Ryuuichi

  公开号：US20120046327A1

  公开（公告）日：2012-02-23

  Methods for (i) inhibiting the induction and formation of osteoclasts, (ii) inhibiting RANKL expression in osteoblasts, (ii) inhibiting the activation of osteoclasts and (iv) inhibiting a decrease in bone density by administering to a warm-blooded animal in need thereof a pharmacologically effective amount of a compound selected from the group consisting of olmesartan and olmesartan medoxomil, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof.
• METHOD OF TREATMENT OR PROPHYLAXIS INFTAMMATORY PAIN
  申请人：Novartis AG

  公开号：US20160052925A1

  公开（公告）日：2016-02-25

  A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin II receptor 2 (AT 2 receptor) antagonists is disclosed. The AT 2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain.