Mochida Pharmaceutical Co., Ltd.

Kaken Pharmaceutical Company, Ltd.

Ichitomo Miwa

Jun Okuda

Kazuo Kato

Ei Mochida

Katsuaki Kato

Kimihiro Murakami

Kazuhiro Inagaki

Mitsuru Nakayama

Tokunaru Horie

The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

Hydantoin derivatives

The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives and pharmaceutical compositions containing at least one of hydantoin derivatives as hypoglycemic as well as hypolipidemic agents. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites. The compounds of the present invention represent a satisfactory hypoglycemic as well as hypolipidemic activity. These compounds are extremely useful for the treatment and/or prevention of diabetes mellitus with or without hyperlipidemia. It is indicated that the compounds of the present invention are useful for the treatment and/or prevention of diabetic complications such as somatic or autonomic neuropathy, cataract, retinopathy, nephropathy or microangiopathy. It is also indicated that the compounds of the present invention are useful for the treatment and/or prevention of hyperlipidemia.

The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.

Hydantoin derivatives as aldose reductase inhibitors

An inhibitor of aldose reductase which contains, as the effective ingredient, a flavone derivative having the following formula: ##STR1## wherein R.sub.1 is hydrogen atom or hydroxyl group, R.sub.2 is hydroxyl group or methoxyl group or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The inhibitor is useful for preventing, reducing or treating complications of diabetes.

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Nagoya, Japan

Ichitomo Miwa