Tropicamide hydrochloride | 958623-78-4

• 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: Tropicamide hydrochloride
• 英文别名: N-ethyl-3-hydroxy-2-phenyl-N-(pyridin-4-ylmethyl)propanamide;hydrochloride
• CAS: 958623-78-4
• 化学式: C17H21ClN2O2
• 分子量: 320.8
• InChiKey: JQIPVEBSCXNGIG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.63
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  53.4
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] TOPICAL TREATMENT OF CATARACTS IN DOGS<br/>[FR] TRAITEMENT TOPIQUE DE LA CATARACTE CHEZ LES CHIENS
  申请人：KADOR PETER F

  公开号：WO2010065024A1

  公开（公告）日：2010-06-10

  The topical treatment of cataracts in dogs is a composition having an aldose reductase inhibitor (ARI) in a topical carrier. The ARI is preferably 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4'-imidazolidine]-2',5'-dione, referred to as 2R-methyl sorbinil. The topical carrier is formed from EDTA and deionized water containing about 2.5% carbomer, 1.5% glycerin, 0.02% EDTA and 0.1% benzalkonium chloride mixed to form a uniform emulsion. The concentration of the ARI in the topical carrier is preferably about 5-6%. The treatment includes administering to a dog an effective amount of the composition for preventing the formation of cataracts, reversing the formation of cataracts, and for treating diabetic retinopathy and pathological conditions resulting from diabetes affecting the cornea, iris, ciliary bodies, etc. The composition is preferably administered in the form of about two to four eye drops daily.

  翻译结果如下： 犬白内障的局部治疗是一种具有醛糖还原酶抑制剂（ARI）的局部载体的组合物。 ARI 最好是 2R，4S-6-氟-2-甲基-螺[色酮-4,4'-咪唑啉]-2'，5'-二酮，称为 2R-甲基索比林。局部载体由 EDTA 和去离子水形成，含约 2.5％ 的卡波姆，1.5％ 的甘油，0.02％ 的 EDTA 和 0.1％ 的苯扎氯铵混合形成均匀乳液。 ARI 在局部载体中的浓度最好约为5-6％。治疗包括向犬中投与有效量的该组合物，以预防白内障的形成，逆转白内障的形成，并治疗糖尿病视网膜病变和糖尿病影响角膜，虹膜，睫状体等的病理情况。该组合物最好以每日约两到四滴眼药水的形式投与。
• Amelioration of cataracts, macular degeneration and other ophthalmic diseases
  申请人：Matier L. William

  公开号：US20050131025A1

  公开（公告）日：2005-06-16

  Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age-related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula: where R 1 and R 2 are, independently, H or C 1 to C 3 alkyl; R 3 and R 4 are, independently C 1 to C 3 alkyl; and where R 1 and R 2 , taken together, or R 3 and R 4 , taken together, or both may be cycloalkyl; R 5 is H, OH, or C 1 to C 6 alkyl; R 6 is or C 1 to C 6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl; R 7 is C 1 to C 6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R 6 and R 7 , or R 5 , R 6 and R 7 , taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.

  本发明涉及可用于阻止白内障、老视、黄斑变性和其他视网膜病变、青光眼、葡萄膜炎以及各种角膜疾病的眼科可接受的组合物。该组合物还可用作预防性治疗，以预防或延迟年龄相关的眼部疾病的发展，包括白内障、老视、青光眼和黄斑变性。该组合物包括一种药用可接受的载体或稀释剂和至少一种具有以下式子的化合物：其中R1和R2独立地为H或C1到C3烷基；R3和R4独立地为C1到C3烷基；而R1和R2一起取代，或R3和R4一起取代，或两者都可以是环烷基；R5为H、OH或C1到C6烷基；R6为C1到C6烷基、烯基、炔基或取代的烷基或烯基；R7为C1到C6烷基、烯基、炔基或取代的烷基或烯基，或者R6和R7，或者R5、R6和R7一起形成一个具有3到7个原子的环烷或杂环。
• [EN] MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE<br/>[FR] COMPOSÉS DE LACTONE MACROCYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：ELIXIR MEDICAL CORP

  公开号：WO2009114010A1

  公开（公告）日：2009-09-17

  The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula (I) wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, -OH, -OP(O)Me2, (II), (III), -O-(CH2)n-OH and -O-(CH2)m-O-(CH2)o-CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of (IV) and (V) wherein each M8 is independently a member selected from the group consisting Of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of (VI), (VII) and (VIII); and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.

  本发明提供了一种制药组合物，该组合物包括一种药用可接受的赋形剂和一种式(I)的化合物，其中R1、R2、R3、R5、R6、R8、M1、M2、M3、M4、M5、M6和M7各自独立地选择自H、C1-6烷基、OH和C1-6羟基烷基的群体中的一种；R4、R7和R9各自独立地选择自C1-6烷氧基和OH的群体中的一种；R10选择自H、-OH、-OP(O)Me2、(II)、(III)、-O-(CH2)n-OH和-O-(CH2)m-O-(CH2)o-CH3的群体中的一种，其中下标n和m各自独立地从2到8，下标o从1到6；L1和L4各自独立地选择自(VI)和(VII)的群体中的一种，其中每个M8各自独立地选择自C1-6烷基、OH和C1-6羟基烷基的群体中的一种；L2和L3各自独立地选择自(VI)、(VII)和(VIII)的群体中的一种；以及其盐、水合物、异构体、代谢物、N-氧化物和前药。
• Topical treatment of cataracts in dogs
  申请人：Kador Peter F.

  公开号：US20090082415A1

  公开（公告）日：2009-03-26

  The topical treatment of cataracts in dogs is a composition having an aldose reductase inhibitor (ARI) in a topical carrier. The ARI is preferably 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4′-imidazolidine]-2′,5′-dione, referred to as 2R-methyl sorbinil, having the structure: The topical carrier is formed from EDTA and deionized water containing about 2.5% carbomer, 1.5% glycerin, 0.02% EDTA and 0.1% benzalkonium chloride mixed to form a uniform emulsion. The concentration of the ARI in the topical carrier is preferably about 5-6%. The treatment includes administering to a dog an effective amount of the composition for preventing the formation of cataracts, reversing the formation of cataracts, and for treating diabetic retinopathy and pathological conditions resulting from diabetes affecting the cornea, iris, ciliary bodies, etc. The composition is preferably administered in the form of about two to four eye drops daily.

  犬类白内障的局部治疗是一种具有醛糖还原酶抑制剂（ARI）的局部载体组成的药物。 ARI 最好是 2R,4S-6-氟-2-甲基-螺[色酮-4,4'-咪唑啉]-2',5'-二酮，称为 2R-甲基索比林，其结构式为：局部载体由 EDTA 和去离子水组成，含有约2.5％的卡波姆，1.5％的甘油，0.02％的 EDTA 和 0.1％苯扎氯铵混合形成均匀乳液。在局部载体中的 ARI 浓度最好约为5-6％。治疗包括向犬类施用有效量的该组成物，以预防白内障的形成，逆转白内障的形成，并治疗糖尿病视网膜病变和由糖尿病影响角膜，虹膜，睫状体等的病理情况。该组成物最好以每天约两到四滴眼药水的形式施用。
• Use of at least one hydroxylamine compound for the treatment of eye disease
  申请人：Othera Holding, Inc.

  公开号：EP2052720A2

  公开（公告）日：2009-04-29

  Uses for the treatment or prevention of a number of ocular diseases or disorders are disclosed. In particular, uses are disclosed for the amelioration of diabetic retinophaty and other retinopathies, as well as uveitis, presbyopia, dry eye, glaucoma, blepharitis and rosacea of the eye. The uses comprise administration of a composition comprising an ophtalmalogically acceptable carrier or diluent and a hydroxylamine compound in a therapeutically sufficient amount to prevent, retard the development or reduce the symptoms of one or more of the ophthalmic conditions.

  已公开的用途包括治疗或预防多种眼部疾病或失调。 特别是公开了用于改善糖尿病视网膜病变和其他视网膜病变，以及葡萄膜炎、老花眼、干眼症、青光眼、眼睑炎和酒渣鼻的用途。 这些用途包括施用由眼科可接受的载体或稀释剂和羟胺化合物组成的组合物，其治疗量足以预防、延缓一种或多种眼科疾病的发展或减轻其症状。