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US 6,150,524 AGranted
Morphine derivatives with analgesic activity
AssigneeCeNes Limited
InventorsMichael Hartmann, Dagmar Stimmeder, Steinar Engelsen, Andreas Koch, Franz Rovenszky, Peter Kremminger, Michael Hutzinger
Life of this patent
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Abstract
Morphine derivatives of formula (I), process for perparing them and their use and use as analgesics. ##STR1##
Claims9
A morphinan derivative of the formula ##STR6## wherein D denotes a straight-chained or branched, optionally halogenated C.sub.1-4 -alkyl group,
- the dotted line represent a chemical bond indicating that the compound is a morphine or 7,8-dihydromorphine derivative,
- P denotes a group --C(L) (R.sub.1) (R.sub.2),
- L denotes a group --A.sub.1 --(C(R.sub.3) (R.sub.4)).sub.k --A.sub.2 --B
- k is an integer from 0 to 5;
- R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another denote hydrogen, a straight-chained or branched, C.sub.1-4 -alkyl group, a C.sub.2-4 -alkenyl group, or a group --(CH.sub.2).sub.x --OR.sub.7, --(CH.sub.2).sub.x --OC(O)R.sub.7, (CH.sub.2).sub.x --F, (CH.sub.2).sub.x --Cl, (CHF).sub.x --F, (CHCl).sub.x --Cl, (CF.sub.2).sub.x --F, (CCl.sub.2).sub.x --Cl,
- x is an integer from 0 to 2,
- A.sub.1 and A.sub.2 independently of each other denote a group --(CH.sub.2).sub.m --,
- m is an integer from 0 to 4,
- B is a hydrogen atom or a group X, and
- X denotes a group --(CH.sub.2).sub.n --OH, --(CH.sub.2).sub.n --CO.sub.2 R.sub.7, --(CH.sub.2).sub.n --CN, --(CH.sub.2).sub.n --CONR.sub.5 OR.sub.6, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n --OR.sub.5, --(CH.sub.2).sub.n --COR.sub.5, --(CH.sub.2).sub.n --OC(O)R.sub.7, --(CH.sub.2).sub.n --CONR.sub.5 OR.sub.6, --(CH.sub.2 O.sub.n --NR.sub.5 C(O)R.sub.6, --(CH.sub.2).sub.n --SR.sub.5, --(CH.sub.2).sub.n S(O)R.sub.5, --(CH.sub.2).sub.n --S(O).sub.2 NR.sub.5 R.sub.6, --(CH.sub.2).sub.n --NR.sub.5 R.sub.6, --(CH.sub.2).sub.n --NHC(O)R.sub.5, --(CH.sub.2).sub.n --NHS(O).sub.2 R.sub.5, --(CH.sub.2).sub.n --F, --(CH.sub.2).sub.n --Cl, --(CH.sub.2).sub.n --Br, --(CH.sub.2).sub.n --NO.sub.2
- n is an integer from 0 to 4,
- R.sub.5, R.sub.6 and R.sub.7 independently of one another denote hydrogen or a straight-chained or branched C.sub.1-4 -alkyl group, a C.sub.2-4 -alkenyl group or an aryl or benzyl group, or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.