Process for preparation of cytostatic compounds

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United States of America Patent

PATENT NO 4410459
SERIAL NO

06293611

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl and R.sup.3 is .alpha.-ethyl; or R.sup.4 is hydrogen and R.sup.3 is .beta.-ethyl; R' is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety; R.sup.1 is methoxy and R.sup.2 is acetyl, provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl. These compounds and N-desmethyl-N- ethoxy- methyl -vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formula R'--OH (III) Pharmaceutical compositions containing compounds of the general formula /I/ as active ingredients are also within the scope of invention.

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Patent Owner(s)

Patent OwnerAddress
RICHTER GEDEON VEGYESZETI GYAR RTBUDAPEST

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Acs, Tibor Budapest, HU 6 15
Dancsi, Lajos Budapest, HU 17 50
Dezseri, Eszter Budapest, HU 5 19
Eckhardt, Sandor Budapest, HU 8 25
Fekete, Gyorgy Budapest, HU 20 124
Gorog, Sandor Budapest, HU 27 85
Hindi, Ivan Budapest, HU 2 12
Honty, Katalin Budapest, HU 7 25
Kerpel-Fronius, Sandor Budapest, HU 3 14
Keve, Tibor Budapest, HU 31 85
Relle, nee Somfai Zsuzsanna Budapest, HU 1 6
Sugar, Janos Budapest, HU 7 22
Szabo, Lajos Budapest, HU 46 113
Szantay, Csaba Budapest, HU 57 142

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