Benzamidine derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S212010, C514S424000, C546S192000, C540S484000, C548S541000

Reexamination Certificate

active

07030138

ABSTRACT:
A compound of a formula (1) and pharmacologically acceptable salts thereof:wherein R1represents hydrogen, halogen, alkyl or hydroxyl; R2represents hydrogen or halogen; R3represents hydrogen, alkyl, hydroxyl, carboxyalkyl, alkoxycarbonylalkyl, alkylsulfonyl, alkoxycarbonylalkylsulfonyl, craboxyalkylsulfonyl or carboxyalkylcarbonyl; each of R4and R5represents hydrogen, halogen, alkyl, carbamoyl, alkoxy, carboxyl, alkoxycarbonyl, monoalkylcarbamoyl or dialkylcarbamoyl; R6represents a heterocycle, hydrogen, alkyl, cycloalkyl, aralkyl, carboxyalkyl, alkoxycarbonyalkyl, aliphatic or aromatic acyl, carbamoyl, alkylsulfonyl, aryl, formimidoyl, 1-iminoalkyl, N-alkylforminidoyl or iminoarylmethyl; each of R7and R8represents hydrogen or alkyl; n represents 0, 1 or 2. The compound exhibits excellent activated blood coagulation factor X inhibitory activity and prevents or treats blood coagulation-related diseases.

REFERENCES:
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English-language International Preliminary Examination Report transmitted on Nov. 4, 2003 of International Application No. PCT/JP02/03355; Applicants: Sankyo Company, Limited.
E.L. Smith et al.,Principles of Biochemistry: Mammalian Biochemistry, 7thEdition, McGraw-Hill, Inc. (1983), pp. 16 to 37.
Sebastian Harder and Petra Thürmann, “Clinically Important Drug Interactions with Anticoagulants”,Clin. Pharmacokinet, 30, 416 to 444 (1996).
Marc Verstraete and Pierre Zoldhelyi, “Novel Antithrombotic Drugs in Development”,Drugs, 49, 856 to 884 (1995).

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