Taisho Pharmaceutical Co., Ltd.

Taiho Pharmaceutical Company Limited

Scios Nova, Inc.

Nobuhiko Katunuma

Takashi Adachi

Barbara Cordell

Tetsuji Asao

Sadafumi Omura

Kazunori Hanada

James W Schilling, Jr

Yukio Tada

Yoshimitsu Suda

Kiyoshi Oguma

Masaharu Tamai

Tomohiro Yamashita

Epoxysuccinamide derivative or salt thereof, and medicine comprising the

Pharmaceutical compositions containing a 57 amino acid protease inhibitor and uses for those compositions are taught. The protease inhibitor is referred to as A4i which is associated with Alzheimer's disease. In addition to the A4i protease, other analogs are taught as are pharmaceutical compositions containing such analogs and their uses in treating a variety of abnormalities associated with Kunitz-type basic protease inhibitors. For example, it has been found that pharmaceutical compositions containing A4i protease and analogs thereof inhibit plasmin and tryptase, and also inhibit pancreatic trypsin, alpha-chymotrypsin, tissue kallikrein and serum kallikrein. In that certain diseases are associated with a general release of proteases such as trypsin, chymotrypsin and elastase into the circulatory system pharmaceutical compositions containing A4i and analogs thereof can be used in the management of such diseases.

Methods of treatment using Alzheimer's amyloid polypeptide derivatives

A peptide having an amino acid sequence of the following formula ##STR1## is provided as an inhibitor of trypsin and trypsin-like serine proteases.

Peptide serine protease inhibitor

This invention is directed to novel peptide derivatives. Said peptide derivatives are useful as a substrate for the activity assay of enzymes of the group EC 3. 4. 22, for example, cathepsin L, cathepsin B and cathepsin H. Said peptide derivatives which contain L-methionine radical are prepared according to the methods conventional in peptide chemistry. As typical examples are mentioned D-leucyl-L-tyrosyl-L-methionine-.beta.-naphthylamide formate, .beta.-alanyl-L-tyrosyl-L-methionine-.beta.-naphthylamide formate and succinyl-L-tyrosyl-L-methionine-p-nitroanilide.

Peptide derivatives

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Tokushima, Japan

Nobuhiko Katunuma