Mochida Pharmaceutical Co., Ltd.

Hodogaya Chemical Co., Ltd.

Akio Uemura

Ei Mochida

Kazuo Kato

Hiroki Tokunaga

Akinori Haga

Ryo Tanaka

Hideaki Morishita

Nobuo Ohzawa

Yasuyuki Kunihiro

Michio Ichimura

Atsushi Nii

This invention relates to novel vectors and host cells containing nucleic acids coding for a polypeptide having thrombin binding ability, anticoagulant activity and thrombolytic activity. The polypeptide can be efficiently produced in large quantities by means of genetic recombination techniques using the vectors and host cells of the present invention. Since the polypeptide exhibits anticoagulant activity and thrombolytic activity without generating side effects such as bleeding tendencies, it can be applied effectively to the prevention and treatment of hypercoagulability-related diseases.

Recombinant DNA vectors, including plasmids, and host cells for

This invention relates to a novel polypeptide which is obtained by means of genetic recombination DNA techniques and has thrombin binding ability, anticoagulant activity and thrombolytic activity. The polypeptide of the present invention can be produced in a large quantity and efficiently by means of genetic recombination techniques. Since the polypeptide of the present invention exhibits anticoagulant activity and thrombolytic activity without generating side effects such as bleeding tendency, it can be applied effectively to the prevention and treatment of hypercoagulability-related diseases.

Truncated thrombomodulin, recombinant production thereof, and

This invention relates to a novel anticoagulant substance in human urine, a process for its preparation and a pharmaceutical composition comprising the said substance for the prevention and/or treatment of diseases related to the disorders in blood coagulation system.

Anticoagulant substance obtained from urine

This invention relates to a novel glycoprotein with anticoagulant activity in human urine, a process for its preparation and a pharmaceutical composition comprising the said glycoprotein for the prevention and/or treatment of diseases related to the disorders in the blood coagulation system.

Anticoagulant substance obtained from urine and process for the

The present invention relates to intermediate compounds to produce novel 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites. The present invention is based on two characters. One is the selection of acyl substituents of 2,3-dihydro-4(1H)-quinolinone at 1-position, namely propionyl, t-butylcarbonyl, benzoyl, 2-bromobenzoyl, 4-chlorobenzoyl, 2-methylbenzoyl, 2-ethylbenzoyl, 2,3-dimethoxybenzoyl, 2,4-dichlorobenzoyl, 4-chloro-2-methyl benzoyl or 2-chloro-4-nitrobenzoyl. The other is the selection of substituents and positional specificity at 6- or 7-position, namely halogen atom, methoxy, trifluoromethyl or dimethylamino group. 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives which are made from the intermediate compounds of the present invention have potent hypotensive, antioedematous and diuretic effect as well as an activity to remove ascites, and are extremely useful for the treatment of diseases and disorders mentioned above.

Intermediate compounds of 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime

The present invention relates to novel 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime-O-sulfonic acid compound, processes for producing said compounds, intermediate compounds to produce said compounds and compositions containing said compounds with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites. The present invention is based on the selection of 1-acyl-7-halo-2,3-dihydro-4(1H)-quinolinone-4-oxime-O-sulfonic acid compounds, namely heterocyclic-or fused heterocyclic- carbonyl derivatives at 1 position. The compounds of the present invention containing these substituents have potent hypotensive, antioedematous and diuretic effect as well as an activity to remove ascites and are extremely useful for the treatment of diseases and disorders mentioned above.

1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives, process for

The present invention relates to novel 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives, processes for producing said derivatives, intermediate compounds to produce said derivatives, processes to produce said intermediate compounds, and compositions containing said derivatives with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites. The present invention is based on the selection of 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives, namely O-sulfate, O-mesylate, O-methylphosphate and O-carboxymethyl ether, especially O-sulfate of 4-oxime. The compounds of the present invention containing these substituents have potent hypotensive, anti-oedematous and diuretic effect as well as an activity to remove ascites and are extremely useful for the treatment of diseases and disorders mentioned above.

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Mishima, Japan

Akio Uemura