Polyamides bearing functionalized side chains useful as water soluble hypolipidemic agents
AssigneeBerlex Laboratories, Inc.
InventorsKent R. Stevens, William V. Taggart
Life of this patent
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Abstract
This invention relates to derivatives of polyanhydroaspartic acid which are non-systemic water soluble polymers and which are intended to be lipid lowering agents. The pharmaceutical compositions/formulations incorporating these compounds are also discussed.
Claims14
The method of inhibiting the growth of gram positive bacteria in a subject in need thereof which comprises administering to said subject a gram positive inhibitory amount of a compound of the following structural Formula II:
- ##STR18## wherein w is the integer 0 or 1;
- y is the integer 1-6;
- z is the integer 0-3;
- t is the integer 0 or 1;
- ##STR19## R is hydrogen, lower alkyl, phenyl or when taken together with R.sub.1 forms a saturated monoheterocyclic ring of from 5 to 6 members;
- R.sub.1, R.sub.2 are the same or independently C.sub.1 -C.sub.10 straight or branched chain alkyl which may be substituted by up to 3 substituents selected from 1 to 2 hydroxyl groups and one ##STR20## group, or when taken together form a saturated heterocyclic ring of from 5 to 6 members which may contain a ##STR21## or --O-- linkage;
- R.sub.3 is methyl, ethyl, benzyl which may be substituted by up to 3 substituents selected from hydroxyl, halogen, methoxy and C.sub.1 -C.sub.6 straight or branched chain alkyl, 1-naphthyl or 2-naphthyl;
- R.sub.4 is a C.sub.1 -C.sub.6 straight or branched chain alkyl which may be substituted by one hydroxyl group;
- R.sub.5, R.sub.6 are the same or independently hydrogen, C.sub.1 -C.sub.4 straight or branched chain alkyl or when taken together form a diheterocyclic ring of from 5 to 6 members;
- R.sub.7, R.sub.8 are the same or independently C.sub.1 -C.sub.6 straight or branched chain alkyl which may be substituted by one hydroxyl group or when taken together with an --O-- linkage form a morpholine ring;
- B is a direct link or a C.sub.1 -C.sub.4 straight or branched chain alkyl;
- n is an integer in the range from about 5 to 500;
- and
- X.sup.- is an anion forming a pharmaceutically acceptable salt.
The method of inhibiting the growth of gram-positive bacteria on a surface which comprises contacting the surface with a gram positive inhibitory amount of a compound of the following structural Formula II:
- ##STR22## wherein w is the integer 0 or 1;
- y is the integer 1-6;
- z is the integer 0-3;
- t is the integer 0 or 1;
- contain a ##STR23## or --O-- linkage;
- R.sub.3 is methyl, ethyl, benzyl which may be substituted by up to 3 substituents selected from hydroxyl, halogen, methoxy and C.sub.1 -C.sub.6 straight or branched chain alkyl, 1-naphthyl or 2-naphthyl;
- R.sub.4 is a C.sub.1 -C.sub.6 straight or branched chain alkyl which may be substituted by one hydroxyl group;
- R.sub.5, R.sub.6 are the same or independently hydrogen, C.sub.1 -C.sub.4 straight or branched chain alkyl or when taken together form a diheterocyclic ring of from 5 to 6 members;
- R.sub.7, R.sub.8 are the same or independently C.sub.1 -C.sub.6 straight or branched chain alkyl which may be substituted by one hydroxyl group or when taken together with an --O-- linkage form a morpholine ring;
- B is a direct link or a C.sub.1 -C.sub.4 straight or branched chain alkyl;
- n is an integer in the range from about 5 to 500;
- and
- X.sup.- is an anion forming a pharmaceutically acceptable salt.
Dependencies are inferred from the claim text.