Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2006-02-28
2006-02-28
Wilson, James O. (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S343000, C514S326000, C514S423000, C549S539000, C546S193000, C546S279100, C560S121000, C564S163000, C564S245000
Reexamination Certificate
active
07005437
ABSTRACT:
The present invention relates to new substituted aryl and heteroaryl derivatives of general formulawhereinA, Ar, n, X, Y1, Y2, Y3, Y4, R1and R5are defined as in claim1, the prodrugs, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. Thus, the compounds of the above general formula I wherein R5does not contain a cyano group have, in particular, an antithrombotic effect and a selective factor Xa-inhibiting effect with generally improved compatibility. The compounds of the above general formula I wherein R5contains a cyano group are valuable intermediate products for preparing the antithrombotic compounds of general formula I.
REFERENCES:
patent: WO 97/30971 (1997-08-01), None
patent: WO 00/35859 (2000-06-01), None
patent: WO 00/71512 (2000-11-01), None
patent: WO 01/10823 (2001-02-01), None
Hcaplus 129:275676, “Synthesis of cinnamaldehydes by oxidation of arylpropenes with 2,3-dichloro-5,6-dicyanoquinone”, 1998, 52(9), pp. 1177-1182.
R. Rai et al; Perspectives on Factor Xa Inhibition; Current Medicinal Chemistry 2001, vol. 8 pages 101-119; Bentham Science Publishers, Ltd.
Fevig, J.M. et al: “Preparation of meta-amidino-N,N-disunstituted anilines as potent inhibitors of coagulation factor Xa” Bioorganic & Medicinal Chemistry Letters, Oxford, GB, Bd. 8, Nr. 22, Nov. 17, 1998, Seiten 3143-3146, XP004143716 ISSN: 0960-894X.
Nar Herbert
Priepke Henning
Ries Uwe
Stassen Jean-Marie
Wienen Wolfgang
Boehringer Ingelheim Pharma KG
Devlin Mary-Ellen M.
Morris Michael P.
Robinson Binta M.
Stempel Alan R.
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