1-[(7-{[4-(2,2,2-trifluoroethoxy)-3-(trifluoromethyl)benzyl]ox y}-2H-chromen-3-yl)methyl]piperidine-4-carboxylic acid hydrochloride | 1228580-11-7

• 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-[(7-{[4-(2,2,2-trifluoroethoxy)-3-(trifluoromethyl)benzyl]ox y}-2H-chromen-3-yl)methyl]piperidine-4-carboxylic acid hydrochloride
• 英文别名: 1-[(7-{[4-(2,2,2-trifluoroethoxy)-3-(trifluoromethyl)phenyl]methoxy}-2H-1-benzopyran-3-yl)methyl]piperidine-4-carboxylic acid monohydrochloride；1-[[7-[[4-(2,2,2-trifluoroethoxy)-3-(trifluoromethyl)phenyl]methoxy]-2H-chromen-3-yl]methyl]piperidine-4-carboxylic acid;hydrochloride
• CAS: 1228580-11-7
• 化学式: C₂₆H₂₅F₆NO₅*ClH
• 分子量: 581.94
• InChiKey: LLYLBEQEAUKJEK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.22
• 重原子数：
  39
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  68.2
• 氢给体数：
  2
• 氢受体数：
  12

文献信息

• MEDICINAL COMPOSITION FOR INHIBITING FORMATION AND/OR ENLARGEMENT OF CEREBRAL ANEURYSM OR SHRINKING SAME
  申请人：Kyoto University

  公开号：EP2990055A1

  公开（公告）日：2016-03-02

  Provided is a pharmaceutical composition which enables the inhibition of formation and/or enlargement of cerebral aneurysm or the regression of cerebral aneurysm. The pharmaceutical composition for the inhibition of formation and/or enlargement of cerebral aneurysm or for the regression of cerebral aneurysm of the present invention, which includes a S1P1 receptor agonist as an active ingredient, enables the inhibition of formation and/or enlargement of cerebral aneurysm or the regression of cerebral aneurysm, and enables the prevention and/or treatment of a disease associated with cerebral aneurysm.

  本发明提供了一种能够抑制脑动脉瘤形成和/或扩大或使脑动脉瘤消退的药物组合物。本发明的抑制脑动脉瘤形成和/或增大或使脑动脉瘤消退的药物组合物，其活性成分包括 S1P1 受体激动剂，可抑制脑动脉瘤形成和/或增大或使脑动脉瘤消退，并可预防和/或治疗与脑动脉瘤相关的疾病。
• MEDICINE FOR PREVENTING OR TREATING OPHTHALMIC DISEASE ASSOCIATED WITH ENHANCED INTRAOCULAR NEOVASCULARIZATION AND/OR INTRAOCULAR VASCULAR PERMEABILITY
  申请人：Kyoto University

  公开号：EP3747471A1

  公开（公告）日：2020-12-09

  Provided is a pharmaceutical for preventing or treating an ophthalmic disease associated with intraocular neovascularization and/or increased intraocular vascular permeability. The inventors of the present invention have made investigations on a pharmaceutical for preventing or treating an ophthalmic disease associated with intraocular neovascularization and/or increased intraocular vascular permeability, and have confirmed that a selective S1P receptor agonist having agonist activity at an S1P1 receptor has an intraocular neovascularization-reducing action and an intraocular vascular permeability-reducing action, thus completing the present invention. A compound or a pharmaceutically acceptable salt thereof of the present invention, which serves as the selective S1P receptor agonist having agonist activity at the S1P1 receptor, has an intraocular neovascularization-reducing action and an intraocular vascular permeability-reducing action, and can be used as a preventive and/or therapeutic agent for, for example, exudative age-related macular degeneration, diabetic retinopathy, diabetic macular edema, myopic choroidal neovascularization, retinal artery occlusion, retinal vein occlusion, or neovascular glaucoma.

  本发明提供了一种用于预防或治疗与眼内新生血管和/或眼内血管通透性增加有关的眼科疾病的药物。本发明的发明者对一种用于预防或治疗与眼内新生血管化和/或眼内血管通透性增加相关的眼科疾病的药物进行了研究，并证实了一种对 S1P1 受体具有激动活性的选择性 S1P 受体激动剂具有降低眼内新生血管化作用和降低眼内血管通透性作用，从而完成了本发明。本发明的化合物或其药学上可接受的盐作为选择性 S1P 受体激动剂，在 S1P1 受体上具有激动活性，具有降低眼内新生血管作用和降低眼内血管通透性作用、本发明可用作渗出性老年性黄斑变性、糖尿病视网膜病变、糖尿病黄斑水肿、近视性脉络膜新生血管、视网膜动脉闭塞、视网膜静脉闭塞或新生血管性青光眼等疾病的预防和/或治疗药物。
• COMPOSITION COMPRISING A SPHINGOSINE-1-PHOSPHATE RECEPTOR 1 AGONIST FOR INHIBITING FORMATION AND/OR ENLARGEMENT OF CEREBRAL ANEURYSM OR FOR SHRINKING IT
  申请人：Kyoto University

  公开号：EP2990055B1

  公开（公告）日：2019-06-05
• US9629834B2
  申请人：——

  公开号：US9629834B2

  公开（公告）日：2017-04-25
• [EN] MEDICINE FOR PREVENTING OR TREATING OPHTHALMIC DISEASE ASSOCIATED WITH ENHANCED INTRAOCULAR NEOVASCULARIZATION AND/OR INTRAOCULAR VASCULAR PERMEABILITY<br/>[FR] MÉDICAMENT POUR PRÉVENIR OU TRAITER UNE MALADIE OPHTALMIQUE ASSOCIÉE À UNE NÉOVASCULARISATION INTRAOCULAIRE ET/OU À UNE PERMÉABILITÉ VASCULAIRE INTRAOCULAIRE ACCRUES<br/>[JA] 眼内血管新生及び／又は眼内血管透過性亢進を伴う眼科疾患の予防又は治療のための医薬
  申请人：UNIV KYOTO

  公开号：WO2019151470A1

  公开（公告）日：2019-08-08

  眼内血管新生及び／又は眼内血管透過性亢進を伴う眼科疾患の予防又は治療のための医薬を提供する。本発明者らは、眼内血管新生及び／又は眼内血管透過性亢進を伴う眼科疾患の予防又は治療のための医薬について検討し、S1P1受容体に対してアゴニスト活性を有する選択的S1P受容体アゴニストが眼内血管新生抑制作用及び眼内血管透過性抑制作用を有することを確認し、本発明を完成した。本発明のS1P1受容体に対してアゴニスト活性を有する選択的S1P受容体アゴニストである化合物又はその製薬学的に許容される塩は眼内血管新生及び眼内血管透過性抑制作用を有し、滲出型加齢黄斑変性、糖尿病網膜症、糖尿病黄斑浮腫、近視性脈絡膜新生血管、網膜動脈閉塞症、網膜静脈閉塞症、又は血管新生緑内障等の予防及び／又は治療剤として使用しうる。