Toyo Jozo Kabushiki Kaisha

Toyo Jozo Company, Ltd.

Akira Asahi

Satoshi Yaginuma

Yukio Suzuki

Masao Yaso

Masaki Takada

Kouichi Kuno

Motoshi Shoda

Mitsuo Hayashi

Kiyofumi Fukukawa

An aldose reductase inhibitor, comprising a compound of the formula (I) ##STR1## or a pharmaceutically acceptable salt thereof as the effective component, in which R is lower alkyl or cyclohexylmethyl and n is 2 or 3. The compounds of formula (I) and salts thereof according to the invention exhibit a superior aldose reductase inhibiting activity with simultaneous high stability, so that they are useful for the prevention and therapy of diabetic complications.

Aldose reductase inhibitor

An aldose reductase inhibitor, comprising a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof as the effective component, in which R denotes an alkyl of C.sub.1-12, ##STR2## wherein X.sub.1 and X.sub.2 are same or different and are hydrogen or halogen, cyclohexylmethyl, cyclohexyl, tetra-hydro-2H-pyran-1-yl-methyl, carboxy-lower alkyl or cyclo-lower alkyl and n is 2 or 3. These compounds exhibit a superior aldose reductase inhibiting activity with simultaneous high stability, and are for use in the prevention and therapy of diabetic complications.

Biphenyl-5,5'-bis-alkanoic acid derivatives, their production and aldose

A physiologically-active novel substance 'aldostatin' having an estimated molecular formula of C.sub.20 H.sub.20 N.sub.2 O.sub.8 is produced by culturing an aldostatin-producing microorganism of the Pseudeurotium, for example, the Pseudeurotium zonatum M4109 strain. Aldostatin inhibits the aldose reductase activity and as a consequence, avoids abnormal accumulation of sorbitol, galactitol, etc. It is therefore effective for the treatment of chronic complications such as cataract, retinopathy and neuropathy caused by diabetes renalis.

Physiologically-active novel substance 'Aldostatin' and production

A substance is provided which has strong enzyme inhibitory activity against thiol proteases such as papain, ficin, bromelain, etc. and which is represented by the following formula: ##STR1## (wherein R is a hydrogen atom or a hydroxyl group), its pharmaceutically acceptable salt or hydrate.

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Shizuoka, Japan

Akira Asahi