Compounds

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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C546S114000

Reexamination Certificate

active

07553849

ABSTRACT:
A compound of formula (I)whereinR is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl;R′ is hydrogen, C1-C4alkyl, C1-C3alkoxy; halogen, trifluoromethyl or OCHxFy,R″ is hydrogen, fluoro or chloro, that R″ being fluoro or chloro only when R′ is fluoro or chloro;R3is hydrogen or C1-C5alkylR4is hydrogen, CH2OCOC(CH3)3, pharmaceutically acceptable inorganic or organic cations, or COR4′ wherein R4′ is C1-C5alkyl, phenyl, benzyl or phenethyl;R7is methyl or ethyl;one of A and B is sulphur and the other is C-R2;when A is S, R2is selected from hydrogen and methyl, with the proviso that R2is methyl only when R3is not hydrogen; andwhen B is S, R2is hydrogen;and any tautomer thereof.A pharmaceutical composition comprising a compound of formula (I), a method of treating malignant tumours or diseases resulting from autoimmunity or pathologic inflammation.

REFERENCES:
patent: 5593943 (1997-01-01), Nuebling et al.
patent: 1419772 (2004-05-01), None
patent: WO 94/29295 (1994-12-01), None
patent: WO 00/53610 (2000-09-01), None
patent: WO 03/059912 (2003-07-01), None
patent: WO 2004/019939 (2004-03-01), None
Hans-Peter Buschstaller et al “Synthesis of Novel 2-Aminothiophene-3-carboxylates by Variations of the Gewald Reaction” Chemical Monthly, vol. 132, (2001) pp. 279-293.
R.A.W. Johnstone et al “A Rapid Method of N-Alkylation of Amines” J. Chem. Soc. (C.) (1969) pp. 2223-2224.
John W. Prineas “The neuropathology of multiple sclerosis” Handbook of Clinical Neurology vol. 3 (47) (1985) pp. 213-257.
Hsing-Jang Liu et al “An improved procedure for the preparation of 3-carbomethoxy-4-oxotetrahydrothiopyran, 2- and 4-carbomethoxy-3-oxotetrahydrothiophene” Can. J. Chem. vol. 60, (19982) pp. 437-439.

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