| abstract |
REFERS TO COMPOUNDS DERIVED FROM TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE OF FORMULA (I) WHERE X IS N OR CH; Z1 IS N OR CR1c, WHERE R1c IS H, HALOGEN, OR ALKYL (C1-C6); Z2 IS N OR CR1d, WHERE R1d IS H, ALKYL (C1-C6), ALCOXYL (C1-C6), AMONG OTHERS; R1a IS H, (C1-C6) ALKYL, (C1-C6) ALCOXYL, CN, AMONG OTHERS; R1b IS H, AMINO, ALKYLAMINE (C1-C4), AMONG OTHERS; R1e IS H, HALOGEN, CN, ALKYL (C1-C6), AMONG OTHERS; R2 IS H, (C1-C6) ALKYL; CYCLOALKYL (C3-C7), AMONG OTHERS; R3 IS PHENYL, HETEROARYL, OR PHENYLALKYL (C1-C3); R4 IS HO (C1-C4) ALKYL; R5 IS H, OR R4 AND R5 IN COMBINATION ARE OXO; R6 IS H O BOTH R6 FORMING A CARBONYL. PREFERRED COMPOUNDS ARE: 1- (2- (2,6-DIMETHYLPHENYL) -6- (3-ISOPROPYL-1-METHYL-1H-PYRAZOLE-5-IL) -5,6,7,8-TETRAHYDROPYRIDE [4,3 -d] PYRIMIDIN-4-IL) -2-METHYLPIPERIDIN-4-OL RACEMIC; 2- (2,6-DIMETHYLPHENYL) -4- (3,3-DIMETHYLPIPERIDIN-1-IL) -6- (3-ISOPROPYL-1-METHYL-1H-PYRAZOLE-5-IL) -5,6,7, 8-TETRAHYDROPYRIDE [4,3-d] PYRIMIDINE; (S) -2- (2,6-DIMETHYLPHENYL) -6- (3-ISOPROPYL-1-METHYL-1H-PYRAZOLE-5-IL) -4- (2-METHYLPIPERIDIN-1-IL) -5.6, 7,8-TETRAHYDROPYRIDE [4,3-d] PYRIMIDINE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE MODULATORS OF C5A RECEPTORS OF THE MAMMAL COMPLEMENT AND BEING USEFUL IN THE TREATMENT OF DIABETIC RETINOPATHY, RETINITIS PIGMENTOSA, EYE PENFIGUS |