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US 4,391,816 AGranted
N-(Naphthalenylthioxomethyl)aminoacid derivatives
AssigneeAyerst McKenna and Harrison Ltd.
InventorsKazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
Life of this patent
Estimating the term…
Abstract
Herein disclosed are N-(naphthalenylthioxomethyl)aminoacid derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
Claims19
A compound of formula I ##STR4## wherein R.sup.1 is lower alkyl, carboxymethyl, phenyl or phenyl substituted with a substituent selected from halo, lower alkyl or lowe alkoxy;
- R.sup.2 is hydrogen or lower alkyl;
- n is the integer O, 1 or 2;
- or
- n is the integer O and R.sup.1 and R.sup.2 form a (CH.sub.2).sub.3 bridge to complete a pyrrolidine ring with the nitrogen and carbon to which R.sup.1 and R.sup.2 are joined;
- and
- R.sup.3 is a halo substituent at position 3, 5, 6 or 7 of the naphthalene ring, or
- R.sup.3 is two or three substituents on the naphthalene ring selected from the group consisting of 4-lower alkoxy-5-[di(lower alkyl)aminosulfonyl] and 3-halo-4-lower alkoxy-5-[(di(lower alkyl)aminosulfonyl];
- with the proviso that when R.sup.1 is lower alkyl, then R.sup.3 is a halo substituent at position 3, 6 or 7 of the naphthalene ring or R.sup.3 is two or three substituents as defined herein, or a therapeutically acceptable salt thereof with an organic or inorganic base.
5 more elements
A compound of the formula ##STR5## wherein R.sup.1 is lower alkyl, carboxymethyl, phenyl or phenyl substituted with a substituent selected from halo, lower alkyl or lower alkoxy;
- R.sup.2 is hydrogen or lower alkyl;
- n is the integer O, 1 or 2;
- or
- n is the integer O and R.sup.1 and R.sup.2 form a (CH.sub.2).sub.3 bridge to complete a pyrrolidine ring with the nitrogen and carbon to which R.sup.1 and R.sup.2 are joined;
- and
- R.sup.3 is a halo substituent at position 3, 5, 6 or 7 of the naphthalene ring, or
- R.sup.3 is two or three substituents on the naphthalene ring selected form the group consisting of 4-lower alkoxy-5-[di(lower alkyl)aminosulfonyl] and 3-halo-4-lower alkoxy-5-[di(lower alkyl)aminosulfonyl];
- with the proviso that when R.sup.1 is lower alkyl, then R.sup.3 is a halo substituent at position 3, 6 or 7 of the naphthalene ring or R.sup.3 is two or three substituents as defined herein;
- and R.sup.4 is lower alkyl or ar(lower)alkyl.
6 more elements
Dependencies are inferred from the claim text.