Substituted 3,4-dihydro-pyrimido[1,2-a]pyrimidine and 3,4-dihydro-pyrazino[1,2-a]pyrimidine derivatives are new. The substituted 3,4-dihydro-pyrimido[1,2-a]pyrimidine and 3,4-dihydro-pyrazino[1,2-a]pyrimidine derivatives are compounds of formula (I) and their salts: [Image] Y : CR8; and Z : N; or Y : N; and Z : CR9; R1,R2H; OR10; SH; SR10; or alkyl, cycloalkyl, heterocyclyl, aryl, aralkyl or heteroaryl-alkyl; R3,R4H; or alkyl, cycloalkyl, aryl, heteroaryl, aralkyl or heteroaryl-alkyl; or R1 or R2+R3 or R4W; W : a'-(CH2)3-10-b'; a'-CH=CH-CH2-b'; a'-CH=CH-CH2-CH2-b'; a'-CH2-CH=CH-CH2-b'; a'-CH2-CH2-CH=CH-CH2-CH2-b'; a'-O-(CH2)2-6-b'; or a group of formula (a)-(e); R1 or R2 and R3 or R4H or alkyl; a' : bond to a; b' : bond to b; X : CH2; O; or S; R5alkyl, cycloalkyl, heterocyclyl, aryl, aralkyl or heteroaryl-alkyl; C(O)R11; CO2H; or CO2R12 R6-R9H; F; Cl; Br; I; CN; NH2; NH(alkyl); N(alkyl)2; NH(aralkyl); N(aralkyl)2; NH-aryl; N(aryl)2; NHR13; NO2; OH; SH; O-alkyl; S(O)0-2-alkyl; O-aryl; S(O)0-2-aryl; aralkoxy; S(O)0-2-aralkyl; CO2H; C(O)R14; alkyl; CF3; cycloalkyl; heterocyclyl; aryl; or heteroaryl; or R6+R7Q; or R6+R9T; R10alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, aralkyl or heteroaryl-alkyl; R11NH2; NH(alkyl; N(alkyl)2; NH(aralkyl); N(aralkyl)2; NH-aryl; N(aryl)2; cycloalkyl; aryl; heteroaryl; aralkyl; or heteroaryl-alkyl; R12alkyl; cycloalkyl; or aralkyl; R13C(O)CH3; C(O)phenyl; or C(O)OtBu; R14H; NH2; NH(alkyl); N(alkyl)2; NH(aralkyl); N(aralkyl)2; NH-aryl; N(aryl)2; alkyl; cycloalkyl; aryl; aralkyl; O-alkyl; O-cycloalkyl; O-aryl or O-aralkyl; Q : g'-CR15=CR16-CR17=CR18-d'; T : g'-CR19=CR20-CR21=CR22-e' or g'-N=CR20-CR21=N-e'; g' : bond to g; d' : bond to d; R15-R22H; F; Cl ; Br; I; OH; CN; alkyl; or CO2H; alkyl, cycloalkyl and heterocyclyl are saturated or unsaturated and alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are optionally mono- or poly-substituted; provided that R1 and R2 are not both H; and R1 or R2 is H or 1-12C alkyl when the other of R1 and R2 = aryl. [Image] Full definitions are given in the DEFINITIONS Field. An independent claim is also included for the preparation of compounds (I). - ACTIVITY : Analgesic; antipruritic; antidiarrheal. - MECHANISM OF ACTION : None given in the source material.
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