Senju Pharmaceutical Co., Ltd.

Takeda Chemical Industries, Inc.

Takaaki Deguchi

Takahiro Ogawa

Kazumi Ogata

Takahiro Sakaue

Keiji Kubo

Katsuhiro Inada

Yoshifumi Ikejiri

Yuuichi Isowaki

Pharmaceutical composition for use in glaucoma treatment

The present invention provides an ophthalmic preparation for reducing intraocular pressure comprising 2-[3-dimethyl-amino-2-(2-carboxyethoxy)propionyloxy]-2'-methoxybibenzyl or a salt thereof, which preparation exhibits intraocular pressure reducing activity, without exerting effects on the central nervous system, and can advantageously be used as a prophylactic and therapeutic agent for ocular hypertension and glaucoma bringing about elevated intraocular pressure.

Ophthalmic preparations for reducing intraocular pressure

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.

Ocular hypotensive agent

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 &gt;C.dbd.O or &gt;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.

Ophthalmic composition for lowering intraocular pressure

A hypotensive agent and antiglaucoma agent which comprise a compound represented by the following formula: ##STR1## (wherein R.sub.1 is hydrogen, or a lower alkyl or lower alkoxy group; R.sub.2 is an isopropylamino, tert-butylamino, 2-(2-methoxyphenyl)ethyl-1-amino, 4-(2-methoxyphenyl)!-1-piperazinyl or 4-piperonyl-1-piperazinyl group, provided however that in the case of R.sub.1 being hydrogen, R.sub.2 is neither isopropylamino nor tert-butylamino group) or its pharmacologically acceptable salt.

Growing community of inventors

Kobe, Japan

Takaaki Deguchi