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    • 4. 发明授权
    • Ocular hypotensive agent
    • 眼降血压药
    • US5639773A
    • 1997-06-17
    • US269675
    • 1994-07-01
    • Keiji KuboTakahiro OgawaTakaaki Deguchi
    • Keiji KuboTakahiro OgawaTakaaki Deguchi
    • A61K31/41A61K31/415A61K31/695
    • A61K31/415
    • This invention relates to an ocular hypotensive agent which comprises a compound represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon residue that may be bound via a hetero atom; R.sup.2 represents hydrogen or a hydrocarbon residue that may have a substituent; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X is a covalent bond between the 2 benzene rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n represents 1 or 2; ring A is a benzene ring having 1 or 2 optional substituents in addition to the group represented by COOR.sup.2, or a pharmaceutically acceptable salt thereof.
    • 本发明涉及一种眼降血压药,其包含由下式表示的化合物:其中R 1表示氢或可经由杂原子结合的任选取代的烃残基; R 2表示氢或可以具有取代基的烃残基; R3表示能够形成阴离子或能够改变的基团的基团; X是相邻的亚苯基和苯基之间的线性部分的2个苯环或链长为1〜2个原子的间隔基之间的共价键; n表示1或2; 除了由COOR2表示的基团之外,环A是具有1或2个任选取代基的苯环或其药学上可接受的盐。
    • 5. 发明授权
    • Ophthalmic composition for lowering intraocular pressure
    • 用于降低眼内压的眼用组合物
    • US5538974A
    • 1996-07-23
    • US378244
    • 1995-01-24
    • Takahiro OgawaTakaaki Deguchi
    • Takahiro OgawaTakaaki Deguchi
    • A61K31/55A61K31/495A61K31/39
    • A61K31/55
    • An ophthalmic composition comprising a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each a hydrogen, a halogen, a hydroxyl, a lower alkyl or a lower alkoxy, R.sup.3 and R.sup.4 are each a hydrogen, an optionally substituted lower alkyl, an optionally substituted cycloalkyl or an optionally substituted aralkyl, or form, together with the adjacent nitrogen atom, an optionally substituted ring, X is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally esterified or amidized carboxyl, Y is >C.dbd.O or >CH--OR.sup.5 wherein R.sup.5 is a hydrogen, an acyl or an optionally substituted carbamoyl, m is an integer of from 0 to 2, and n is an integer of from 1 to 6, or a salt thereof, and a method for the treatment of glaucoma, comprising administering said compound or a salt thereof.
    • 一种眼用组合物,其包含式IMA的化合物,其中R 1和R 2各自为氢,卤素,羟基,低级烷基或低级烷氧基,R 3和R 4各自为氢,任选取代的低级烷基, 任选取代的环烷基或任选取代的芳烷基,或与相邻氮原子一起形成任选取代的环,X为氢,任选取代的低级烷基,任选取代的芳基或任选酯化或酰胺化的羧基,Y为> C = O或> CH-OR 5,其中R5是氢,酰基或任选取代的氨基甲酰基,m是0-2的整数,n是1至6的整数,或其盐,和 治疗青光眼的方法,包括给予所述化合物或其盐。