Sanwa Kagaku Kenkyusho Co., Ltd.

Hirosaki University

Noriaki Kato

Masayasu Kurono

Kiichi Sawai

Yasuaki Kondo

Kenji Miura

Toshinao Usui

Takuji Yamaguchi

Kyoichi Asano

Akira Matsubara

Kuniharu Mizuno

Naofumi Terada

Ryoichi Unno

Masato Fukushima

Hiroshi Ozawa

Takahito Jomori

Kaori Taniko

Hiroshi Nagano

Chihiro Hibi

Saori Ogasawara

Soroku Yagihashi

A prophylactic or therapeutic agent for diabetic maculopathy, which can be administered for a long time and exhibits efficacy in a mechanism different from that of existing medicines. The invention relates to a prophylactic or therapeutic agent for diabetic maculopathy, comprising, as an active ingredient, a compound represented by the general formula: wherein X represents a halogen or a hydrogen atom, Rand Rconcurrently or differently represent a hydrogen atom or an optionally substituted C1 to C6 alkyl group, or Rand R, together with a nitrogen atom bound thereto and optionally another nitrogen atom or an oxygen atom, are combined to form a 5- to 6-membered heterocycle. Preferably, the compound is (2S,4S)-6-fluoro -2',5&#x2032;-dioxospiro chroman-4,4&#x2032;-imidazolidine]-2-carboxamide. The invention also provides a model animal with diabetic maculopathy produced by subjecting a diabetic animal to intraocular ischemia/reperfusion to express edema in a retinal visual cell layer or in a macula lutea.

Prophylactic or therapeutic agent for diabetic maculopathy

A prophylactic or therapeutic agent for diabetic maculopathy, which can be administered for a long time and exhibits efficacy in a mechanism different from that of existing medicines. The invention relates to a prophylactic or therapeutic agent for diabetic maculopathy, comprising, as an active ingredient, a compound represented by the general formula: wherein X represents a halogen or a hydrogen atom, Rand Rconcurrently or differently represent a hydrogen atom or an optionally substituted C1 to C6 alkyl group, or Rand R, together with a nitrogen atom bound thereto and optionally another nitrogen atom or an oxygen atom, are combined to form a 5- to 6-membered heterocycle. Preferably, the compound is (2S,4S)-6-fluoro-2',5&#x2032;-dioxospiro[chroman-4,4&#x2032;-imidazolidine]-2-carboxamide. The invention also provides a model animal with diabetic maculopathy produced by subjecting a diabetic animal to intraocular ischemia/reperfusion to express edema in a retinal visual cell layer or in a macula lutea.

Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,

Hydantoin derivatives for treating complications of diabetes

Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivatives, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,

Process for preparing optically active hydantoins

Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group, in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, ##STR3## in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,

Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group, in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitogen or oxygen atom, ##STR3## in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,

Growing community of inventors

Kasugai, Japan

Noriaki Kato