to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. More particularly, it relates to compounds which exhibit agonist activity for CCK-A receptors thereby enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals.
대표청구항▼
[ We claim:] [1.] A compound of formula (I)EQU R.sup.1 R.sup.2 NCOCH.sub.2 N(R.sup.3)COR.sup.4 (I) physiologically acceptable salts thereof whereinR.sup.1 is C.sub.3-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, phenyl, --(CH.sub.2).sub.p CN or --(CH.sub.2).sub.p COO(C.sub.1-4 alkyl) andR.sup.2
[ We claim:] [1.] A compound of formula (I)EQU R.sup.1 R.sup.2 NCOCH.sub.2 N(R.sup.3)COR.sup.4 (I) physiologically acceptable salts thereof whereinR.sup.1 is C.sub.3-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, phenyl, --(CH.sub.2).sub.p CN or --(CH.sub.2).sub.p COO(C.sub.1-4 alkyl) andR.sup.2 is [C.sub.3-6 alkyl,] C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, benzyl, phenyl, or phenyl mono- or disubstituted independently with C.sub.1-3 alkyl, cyano, hydroxy, dimethylamino, --O(C.sub.1-4 alkyl), --O(CII.sub.2 C.sub.6 II.sub.5), --NH(C.sub.1-4 alkyl), --COO(C.sub.1-4 alkyl), --N(C.sub.1-4 alkyl).sub.2 pyrrolidino, morpholino, halogen, or C.sub.1-3 alkyl substituted by one or more fluorine atoms, or R.sup.1 is C.sub.1-2 alkyl and R.sup.2 is phenyl substituted at the 2- or 4-position with chloro, methyl, methoxy, or methoxycarbonyl;R.sup.4 is a group of formula (III) [ STR 13 ] where n is 0, 1, 2 or 3; p is the integer 0 or 1;q is the integer 0 or 1;r is the integer 0 or 1, provided that when q is 0 then r is 0;R.sup.9 is hydrogen or C.sub.1-10 alkyl;R.sup.5 is C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl, phenyl mono-, di or trisubstituted independently with C.sub.1-4 alkyl, hydroxy, C.sub.1-6 alkoxy, halogen, amino, mono- or di(C.sub.1-6 alkyl)amino, nitro, carboxy, --COO(C.sub.1-4 alkyl), carboxyC.sub.1-6 alkoxy, carboxyC.sub.1-4 alkyl, carboxymethylthio, heteroaryl, mono- or di(C.sub.1-6 alkyl)aminoalkyl, or trifluoromethyl, trifluoromethoxy, C.sub.1-4 alkylthio, --SO.sub.y (C.sub.1-4 alkyl), --SO.sub.v NH(C.sub.1-4 alkyl), --SO.sub.v CF.sub.3 or --SO.sub.v C.sub.6 H.sub.5, --(CH.sub.2).sub.v NO.sub.2, --(CH.sub.2).sub.v CN, --(CH.sub.2).sub.v COOH, --(CH.sub.2).sub.v COO(C.sub.1-4 alkyl), --(CH.sub.2).sub.v SCH.sub.3, --(CH.sub.2).sub.v SOCH.sub.3, --(CH.sub.2).sub.v SO.sub.3 H, CH(C.sub.1-3 alkyl)SO.sub.3 H, CH(C.sub.1-3 alkyl)CO.sub.2 H, (CH.sub.2).sub.v SO.sub.2 CH.sub.3, --(CH.sub.2).sub.v CONH.sub.2, --SCH.sub.2 COOH, --CONH(SO.sub.2 CH.sub.3), --CONH(SO.sub.2 CF.sub.3)--(CH.sub.2).sub.v N(C.sub.1-4 alkyl.sub.2, --(CH.sub.2).sub.v NH(SO.sub.2 CF.sub.3) --CH.sub.3).sub.v N(SO.sub.2 CF.sub.3)(C.sub.1-4 alkyl), --(CH.sub.2).sub.v SO.sub.2 N(HCOC.sub.1-4 alkyl)--(CH.sub.2).sub.v SO.sub.2 N(C.sub.1-4 alkyl), CO(C.sub.1-4 alkyl), --(CH.sub.2).sub.v CONHSO.sub.2 (C.sub.1-4 alkyl), --(CH.sub.2).sub.v CON(C.sub.1-4 alkyl)SO.sub.2 (C.sub.1-4 alkyl), --(CH.sub.2).sub.v NHR.sup.10 or (CH.sub.2).sub.v OR.sup.11 substituents; heteroaryl (provided when R.sub.5 is oxadiazole then R.sup.9 is not hydrogen), heteroaryl substituted with halogen, C.sub.1-6 alkyl, hydroxy, nitro, cyano, carboxy, C.sub.1-6 alkoxy, benzoxy, --COO(C.sub.1-4 alkyl), amino, mono- or di(C.sub.1-6 alkyl)amino, phenyl or benzyl substituents; naphthyl; bicycloheteroaryl or bicycloheteroaryl N-substituted independently with hydroxy, carboxyalkyl, phenyl, heteroaryl, C.sub.1-4 alkoxy or cyano substituents, further provided when n is 1, p is 0, q is 0 and r is 0 then heteroaryl, substituted heteroaryl, bicycloheteroaryl and substituted bicycloheteroaryl are bound at the 3 position, still further provided that when n is 0, p is 1, q is 1 and r is 0 then heteraryl, substituted heteroaryl, bicycloheteroaryl and substituted bicycloheteroaryl are bound at the 2 position:R.sup.10 is hydrogen acetyl, C.sub.1-4 alkyl, SO.sub.3 H, --SO.sub.2 CH.sub.3, --SO.sub.2 CF.sub.3, --SO.sub.2 C.sub.6 H.sub.5, C.sub.1-4 alkoxycarbonylR.sup.11 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, --CH.sub.2 C.sub.6 H.sub.5, --CH.sub.2 COOH, --CH.sub.2, --CII.sub.2 CONH(C.sub.1-4 alkyl), --CH.sub.2 CON(C.sub.1-4 allkyl).sub.2 or [ STR 14 ] v 0, 1 or 2; c is zero or 1R.sup.3 and R.sup.6 together form a linking chain [ STR 15 ] wherein the group Z is linked to the rest of the molecule at the carbon atom substituted by the group R.sup.9 andwherein Z is CH.sub.2, C(CH.sub.3).sub.2, --C(CH.sub.3) or CO, Y is a group selected from S, SO, SO.sub.2, CO or CH.sub.2, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 each represent hydrogen, or R.sup.13 and R.sup.14 together form a double bond and R.sup.12 and R.sup.15 are both hydrogen.
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이 특허에 인용된 특허 (1)
Lowe ; III John A. (Stonington CT), Substituted tetrahydrobenzazepinones.
Elisabeth Defossa DE; Uwe Heinelt DE; Otmar Klingler DE; Gerhard Zoller DE; Hans Matter DE; Fahad A. Al-Obeidi ; Armin Walser ; Peter Wildgoose DE, Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them.
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