Ajinomoto Co., Ltd.

Takashi Kayahara

Tadakiyo Nakagawa

Shunji Takehana

Kazuyuki Sagi

Kaoru Yoshida

Naoyuki Fukuchi

Morikazu Kito

Masataka Shoji

Yumiko Fukuda

Mitsuo Takahashi

Naoyuki Yamada

Akira Takahara

Masaru Takayanagi

Eiichiro Suzuki

Kohki Ishikawa

Fumie Futaki

Kuniya Sakurai

Nobuhisa Shimba

Keiko Gondoh

Kazumi Tashiro

Hiroshi Yamamoto

Masayuki Sugiki

Munetaka Tokumasu

Shingo Makino

Kohichi Fujita

Shunsuke Kageyama

Yuki Kajigaya

Masahiro Yamanashi

Benzamidine derivatives of the following formulae or analogs thereof, i.e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants 

Benzamidine derivatives

It is provided a method for producing a subunit peptide originating from an oligomeric protein having disulfide bonds within a subunit and between subunits. The method comprises producing a subunit originating from an oligomeric protein having disulfide bonds within a subunit and between subunits by the following steps:

Process for producing subunit peptide originating in polymer protein

A method for producing a protein having an antithrombotic activity, which comprises replacing, in a protein that has an amino acid sequence having a homology of not less than 30% to the amino acid sequence of SEQ ID NO: 1 and forms a higher order structure composed of a first &#x3b2; strand (&#x3b2;1), a first a helix (&#x3b1;1), a second &#x3b1; helix (&#x3b1;2), a second &#x3b2; strand (&#x3b2;2), a loop, a third &#x3b2; strand (&#x3b2;3), a fourth &#x3b2; strand (&#x3b2;4) and a fifth &#x3b2; strand (&#x3b2;5) in this order from the amino terminus, at least one amino acid residue in a region from &#x3b1;2 to &#x3b2;2 and/or a region from &#x3b2;3 to &#x3b2;4 so that electric charge of the amino acid residue is changed towards positive direction.

Protein having antithrombotic activity and method for producing the same

Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants or agents for preventing or treating thrombi or emboli.

Aminoisoquinoline derivatives

The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.

Benzodiazepine derivatives

Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.

Benzamidine derivative

A benzamidine derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an effect of inhibiting the blood coagulation based on their excellent effect of inhibiting activated blood-coagulation factor X. Thus, a blood-coagulation inhibitor or an agent for preventing or treating thrombosis or embolism, containing one of those compounds as the active ingredient, is provided.

An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.

Amidinophenylpyruvic acid derivatives

A method for producing a protein having an antithrombotic activity, which comprises replacing, in a protein that has an amino acid sequence having a homology of not less than 30% to the amino acid sequence of SEQ ID NO: 1 and forms a higher order structure composed of a first &bgr; strand (&bgr;1), a first &agr; helix (&agr;1), a second &agr; helix (&agr;2), a second &bgr; strand (&bgr;2), a loop, a third &bgr; strand (&bgr;3), a fourth &bgr; strand (&bgr;4) and a fifth &bgr; strand (&bgr;5) in this order from the amino terminus, at least one amino acid residue in a region from &agr;2 to &bgr;2 and/or a region from &bgr;3 to &bgr;4 so that electric charge of the amino acid residue is changed towards positive direction.

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Kawasaki, Japan

Takashi Kayahara