Use of amino hydrogenated quinazoline compounds and derivatives thereof for abstaining from drug dependence
AssigneeNanning Maple Leaf Pharmaceutical Co., Ltd.
InventorsXinfu Pan, Fanglong Qiu
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Abstract
This invention relates to the use of amino hydrogenated quinazoline compounds and derivatives thereof, such as tetrodotoxin, for abstaining from drug dependence in human. Such compounds are administered by subcutaneous, intramuscular or intravenous injection for abstaining from drug dependence, the said drug is alkaloids and nitrogen-containing non-amino acid compound, for example opium, morphine, heroin and the like. Such compounds without drug dependence and low toxicity and side effect can abstain rapidly from drug dependence.
Claims22
A method of treating drug dependence in a human which comprises administering to the human suffering from drug dependence at least one amino hydrogenated quinazoline having the general formula I in an amount effective to cause said drug dependent human to abstain from drug-dependence ##STR7## wherein R.sub.2 and R.sub.5 each is selected from the group consisting of H, OH, and OAc;
- R.sub.1 is selected from the group consisting of H, C.sub.1 -C.sub.4 alkyl, OH, OR, OC(O)R', NH.sub.2 NHR", and NR"R"' wherein R is C.sub.1 -C.sub.6 alkyl, R' is C.sub.1 -C.sub.3 alkyl, and R", and R"' is C.sub.1 -C.sub.4 alkyl;
- R.sub.3 and R.sub.4 are .dbd.O;
- or
- when R.sub.3 is H, R.sub.4 is selected from the group consisting of:
- --ROH, wherein R is a branched or straight chain C.sub.1 -C.sub.7 alkyl,
- --CH(OH)NHOMe,
- --NAP--gly,
- --NAP--en,
- --CH.sub.2 NH.sub.2,
- --CH.sub.2 NHCH.sub.3,
- --AAG,
- --NMAG, and
- --ANT;
- or when R.sub.3 is OH or OC(O)R wherein R is C.sub.1 -C.sub.3 alkyl, R.sub.4 is selected from the group consisting of
- --CHO,
- --CH.sub.2 --gly,
- --CH.sub.2 --.beta.--Ala,
- --CH.sub.2 --Lys,
- --CH.sub.2 --en,
- --CH.sub.2 --NAP--Lys,
- --CH.sub.2 --NAP--en,
- --CH(OH)CH(NH.sub.2)COOH,
- --NH(CH.sub.2).sub.n COOH,
- --NH(CH.sub.2).sub.n NH.sub.2 and
- NH(CH.sub.2).sub.n CH(NH.sub.2)COOH
- wherein:
- n=1-6,
- en is ethylene,
- NAP is 4-triazo-2-nitrobenzoic amide,
- AAG is 2-triazo-O-aminobenzoic amide,
- NMAG is O-methylaminobenzoic amide,
- ANT is O-aminobenzoic amide.
A method for treating a human suffering from drug dependence, comprising administering to said human a daily dosage between 5 and 300 .mu.g of at least one compound of formula I:
- ##STR11## wherein R.sub.2 and R.sub.5 each is selected from the group consisting of H, OH, and OAc;
- R.sub.1 is selected from the group consisting of H, C.sub.1 -C.sub.4 alkyl, OH, OR, OC(O)R', NH.sub.2 NHR", and NR"R"' wherein R is C.sub.1 -C.sub.6 alkyl, R' is C.sub.1 -C.sub.3 alkyl, and R" and R"' are C.sub.1 -C.sub.4 alkyl;
- R.sub.3 and R.sub.4 are .dbd.O or when R.sub.3 is H, R.sub.4 is selected from the group consisting of:
- --ROH, wherein R is a branched or straight chain C.sub.1 -C.sub.7 alkyl,
- --CH(OH)NHOMe,
- --NAP--gly,
- --NAP--en,
- --CH.sub.2 NH.sub.2,
- --CH.sub.2 NHCH.sub.3,
- --AAG,
- --NMAG, and
- --ANT;
- or wherein R.sub.3 is OH or OC(O)R wherein R is a C.sub.1 -C.sub.3 alkyl and R.sub.4 is selected from the group consisting of
- --CHO,
- --CH.sub.2 --gly,
- --CH.sub.2 --.beta.--Ala,
- --CH.sub.2 --Lys,
- --CH.sub.2 --en,
- --CH.sub.2 --NAP--Lys,
- --CH.sub.2 --NAP--en,
- --CH(OH)CH(NH.sub.2)COOH,
- --NH(CH.sub.2).sub.n COOH,
- --NH(CH.sub.2).sub.n NH.sub.2 and
- --NH(CH.sub.2).sub.n CH(NH.sub.2)COOH;
- wherein
- n=1-6,
- en is ethylene,
- NAP is 4-triazo-2-nitrobenzoic amide,
- AAG is 2-triazo-O-aminobenzoic amide,
- NMAG is O-methylaminobenzoic amide,
- ANT is O-aminobenzoic amide.
Dependencies are inferred from the claim text.