Tic-containing opioid dipeptide derivatives useful as analgesics
AssigneeAstra AB
InventorPeter Schiller
Life of this patent
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Abstract
Use of a compound of the formula I ##STR1## for the manufacture of a medicament for the treatment of pain. The compounds are .delta. opioid agonists and thus useful in the treatment of pain without the requirement of co-application of a .mu. opioid agonist.
Claims4
A method of treating a patient for pain comprising, administering to said patient an effective amount of a compound of formula I:
- ##STR101## wherein R.sub.1 and R.sub.2 is each and independently selected from H;
- ##STR102## R.sub.3, R.sub.4, R.sub.5, R.sub.6 are all H;
- or R.sub.4, R.sub.5, R.sub.6 are all H whereas R.sub.3 is a C.sub.1 -C.sub.6 alkyl;
- or
- R.sub.4 and R.sub.5 are both H, whereas R.sub.3 and R.sub.6 are both a C.sub.1 -C.sub.6 alkyl;
- or
- R.sub.3, R.sub.5, R.sub.6 are all H, whereas R.sub.4 is F, Cl, Br, I, OH, NO.sub.2 or NH.sub.2 ;
- R.sub.7 is a 2-phenylethyl- or a 2-cyclohexylethyl group containing one or more additional substituents in the ortho- or para-position of the ring moiety or at the carbon atom adjacent to the ring moiety, with the proviso that, when R.sub.1 and R.sub.2 are both H, R.sub.7 is not a 2-phenylethyl group substituted in the para position.
A method of treating a patient for pain, comprising administering to said patient an effective amount of a compound of formula I:
- ##STR103## wherein:
- R.sub.1 is selected from H and CH.sub.3 ;
- R.sub.2 is selected from H and CH.sub.3 ;
- R.sub.3 is selected from H and CH.sub.3 ;
- R.sub.4 is H;
- R.sub.5 is H;
- R.sub.6 is selected from H and CH.sub.3 ;
- R.sub.7 isselected from any one of ##STR104## wherein R.sub.8 is selected from H, F, Cl, Br, I, NH.sub.2, NO.sub.2, C.sub.1 -C.sub.6 alkyl, and phenyl;
- and
- R.sub.9 is selected from H, C.sub.1 -C.sub.6 alkyl, --CH.sub.2 OH, and phenyl;
- with the proviso that R.sub.8 and R.sub.9 may not both be H;
- ##STR105## wherein R.sub.10 and R.sub.11 is each and independently selected from H, NO.sub.2, NH.sub.2, F, Cl, Br, I, and C.sub.1 -C.sub.6 alkyl;
- ##STR106## wherein R.sub.12 is selected from C.sub.1 -C.sub.6 alkyl and (--CH.sub.2).sub.n --Ph, wherein n=0-3;
- ##STR107## wherein R.sub.13 and R.sub.14 is each and independently selected from H, C.sub.1 -C.sub.6 alkyl, and --(CH.sub.2).sub.n --Ph wherein n=0-3;
- ##STR108##
A method of treating a patient for pain, comprising administering to said patient an effective amount of a compound selected from the group consisting of:
A method of treating a patient for pain, comprising administering to said patient an effective amount of a compound selected from the group consisting of:
Dependencies are inferred from the claim text.