阿西司特 | 1184521-48-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 阿西司特
• 英文名称: Acitazanolast hydrate
• 英文别名: 2-oxo-2-[3-(2H-tetrazol-5-yl)anilino]acetic acid;hydrate
• CAS: 1184521-48-9
• 化学式: C9H9N5O4
• 分子量: 251.2
• InChiKey: LEZMUVNSMYOTNL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.93
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  122
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  ethyl 2-oxo-2-[3-(2H-tetrazol-5-yl)anilino]acetate 生成 阿西司特
  参考文献：
  名称：

  SAVAKI, SEXEHJ;OTAKEH, YASUXIRO;XASIMOTO, MITSUMASA;ABEH, TORU;XORIO, JOS+

  摘要：

  DOI：

文献信息

• PERCUTANEOUS ABSORPTION PREPARATION FOR TREATING OPHTHALMIC DISEASE, USE THEREOF AND METHOD FOR MIGRATION OF OPHTHALMIC REMEDY INTO TOPICAL TISSUE IN EYE
  申请人：Nichiban Company Limited

  公开号：EP1591110A1

  公开（公告）日：2005-11-02

  A transdermal drug delivery system for treatment of ophthalmic diseases comprising a structure that a plaster layer containing a remedy for ophthalmic diseases is provided on a support, wherein the system is applied to a skin surface including a front surface of an eyelid to administer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow. Use of the transdermal drug delivery system for treatment of ophthalmic diseases, comprising applying the transdermal drug delivery system to a skin surface including a front surface of an eyelid to transfer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow, and a method for transferring the remedy for ophthalmic diseases to the ophthalmic topical tissue.

  一种用于治疗眼科疾病的透皮给药系统，包括在支架上设置含有眼科疾病治疗药物的石膏层的结构，其中将该系统应用于包括眼睑前表面在内的皮肤表面，以通过经皮渗透将石膏层中的眼科疾病治疗药物给药到眼科局部组织，而基本上不通过全身血流给药。用于治疗眼科疾病的透皮给药系统，包括将透皮给药系统应用于包括眼睑前表面在内的皮肤表面，通过经皮渗透将膏药层中的眼科疾病治疗剂转移至眼科局部组织，而无需通过全身血流给药，以及将眼科疾病治疗剂转移至眼科局部组织的方法。
• THERAPEUTIC AGENT FOR OPHTHALMIC DISEASE
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1859795A1

  公开（公告）日：2007-11-28

  An agent for the prevention, treatment and/or inhibition of progression of an ophthalmic disease and an agent for the protection of an optic nerve, each of which comprises (2R)-2-propyloctanoic acid or a salt or prodrug thereof in which an amount per dose is from 0.3 ng to 5000 mg. The agents are useful for an ophthalmic disease, such as glaucoma, cataract, retinal detachment, muscae volitantes, age-related macular degeneration, diabetic retinopathy, macular edema, myopia, asthenopia, dry eye, amaurosis fugax, choked disc, papillitis optica, retrobulbar neuritis, toxic amblyopia, optic atrophy, higher visual pathway lesion, internuclear ophthalmoplegia, gaze palsy and ischemic optic neuropathy.

  一种用于预防、治疗和/或抑制眼科疾病进展的制剂和一种用于保护视神经的制剂，其中每种制剂都包含(2R)-2-丙辛酸或其盐或原药，每剂量的用量为 0.3 纳克至 5000 毫克。这些制剂可用于治疗眼科疾病，如青光眼、白内障、视网膜脱离、眼底肌肉萎缩、老年性黄斑变性、糖尿病视网膜病变、黄斑水肿、近视、散光、干眼症、眼底肌肉萎缩、黄斑水肿、视网膜脱离、眼底肌肉萎缩、干眼症、眼底病、窒息性眼底病、视乳头炎、球后神经炎、中毒性弱视、视神经萎缩、高级视觉通路病变、核间性眼肌麻痹、凝视麻痹和缺血性视神经病变。
• Therapeutic agent for opthalmic disease
  申请人：Ono Pharmaceutical Co., Ltd.

  公开号：EP2072047A1

  公开（公告）日：2009-06-24

  Use of (2R)-2-propyloctanoic acid, a salt thereof or a prodrug thereof for the manufacture of an agent for the prevention, treatment and/or inhibition of progression of an ophthalmic disease selected from the group consisting of glaucoma, cataract, retinal detachment, muscae volitantes, age-related macular degeneration, diabetic retinopathy, macular edema, myopia, asthenopia, dry eye, amaurosis fugax, choked disc, papillitis optica, retrobulbar neuritis, toxic amblyopia, optic atrophy, higher visual pathway lesion, internuclear ophthalmoplegia, gaze palsy and ischemic optic neuropathy, in which an amount per dose is from 0.3 ng to 500 mg.

  糖尿病视网膜病变、黄斑水肿、近视、散光、干眼症、眼底病、窒息性视盘炎、视乳头炎、球后神经炎、中毒性弱视、视神经萎缩、高级视觉通路病变、核间性眼肌麻痹、凝视麻痹和缺血性视神经病变，其中每剂量的用量为 0.3 毫微克至 500 毫克。
• Therapeutic agent for ophthalmic disease
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP2266559A1

  公开（公告）日：2010-12-29

  The present invention provides an agent comprising (2R)-2-propyloctanoic acid or a salt thereof for use in the prevention, treatment and/or inhibition of symptom progression of subject of an ophthalmic disease selected from the group consisting of glaucoma, cataract, retinal detachment, muscae volitantes, age-related macular degeneration, diabetic retinopathy, macular edema, myopia, asthenopia, choked disc, papillitis optica, retrobulbar neuritis, toxic amblyopia, optic atrophy, higher visual pathway lesion, internuclear ophthalmoplegia, gaze palsy and ischemic optic neuropathy, wherein the agent is administered intravenously for from one day to 7 days at a dose of from 2 mg to 12 mg per 1 kg of body weight of a patient, orally in an amount per dose of from 300 mg to 1200 mg for from one day to five years or by ocular instillation in an amount per dose of from 0.3 ng to 1 mg for from one day to one year.

  本发明提供了一种包含(2R)-2-丙辛酸或其盐的制剂，用于预防、治疗和/或抑制选自青光眼、白内障、视网膜脱离、蕈样病变、老年性黄斑变性、糖尿病视网膜病变、黄斑水肿、近视、散光、窒盘、视乳头炎、球后神经炎、中毒性弱视、视神经萎缩、高级视觉通路病变、核间性眼肌麻痹、凝视麻痹和缺血性视神经病变等眼科疾病的症状进展、其中，该制剂静脉注射的剂量为每 1 公斤体重 2 毫克至 12 毫克，持续 1 天至 7 天；口服的剂量为每剂量 300 毫克至 1200 毫克，持续 1 天至 5 年；眼部灌注的剂量为每剂量 0.3 毫微克至 1 毫克，疗程为一天至一年。
• 動脈瘤の予防及び／又は治療薬
  申请人：キッセイ薬品工業株式会社

  公开号：JP2008019221A

  公开（公告）日：2008-01-31

  【課題】 動脈瘤の予防及び／又は治療薬を提供する。【解決手段】 ケミカルメディエーター遊離抑制薬を有効成分とする動脈瘤の予防及び／又は治療薬。トラニラスト、フマル酸ケトチフェン、クロモグリク酸ナトリウム、レピリナスト、ペミロラストカリウム、イブジラスト及びアシタザノラスト水和物等のケミカルメディエーター遊離抑制薬は、動脈瘤の発生や進展を抑制するため、動脈瘤の予防及び／又は治療薬として用いることができる。【選択図】図１

  问题】提供一种预防和/或治疗动脉瘤的药物。其有效成分为化学介质释放抑制剂。化学介质释放抑制剂，如曲尼司特、富马酸酮替芬、色甘酸钠、利匹司特、吡米司特钾、伊布司特和水合阿昔他诺司特，可用作动脉瘤的预防和/或治疗药物，因为它们能抑制动脉瘤的发生和发展。它们可用作动脉瘤的预防和/或治疗药物。[图 1.