Amide compounds and use thereof

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

C514S303000, C514S337000, C514S349000, C546S113000, C546S119000, C546S280100, C546S279700, C546S282700, C546S309000

Reexamination Certificate

active

06933305

ABSTRACT:
The present invention relates to an amide compound of the formulawherein R1is a hydrogen and the like, R2is a hydrogen and the like, X is SO2and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.

REFERENCES:
patent: 6218410 (2001-04-01), Uehata et al.
patent: 11-130751 (1999-05-01), None
patent: 2000-63274 (2000-02-01), None
patent: 98/06433 (1998-02-01), None
Sasaki et al. Pharmacology & Therapeutics. 2002, 93:225-232.
Loge et al. Journal of Enzyme Inhibition and Medicinal Chemistry, 2002, 17(6): 381-290.
H. Nagumo et al., “Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells”, Am. J. Physiol. Cell. Physiol., vol. 278, No. 1, Jan. 2000, C57-65.

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