Antivirally active heterocyclic azahexane derivatives

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United States of America Patent

PATENT NO 6300519
SERIAL NO

09448328

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl, R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl, R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, and R.sub.6, independently of R.sub.1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

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Patent Owner(s)

Patent OwnerAddress
NOVARTIS CORPORATION608 FIFTH AVENUE NEW YORK NY 10020

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bold, Guido Gipf-Oberfrick, CH 82 1203
Capraro, Hans-Georg Rheinfelden, CH 36 614
Fassler, Alexander Macclesfield, GB 14 179
Khanna, Satish Chandra Bottmingen, CH 15 173
Lang, Marc Mulhouse, FR 40 533

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