3-(Amino-or aminoalkyl) pyridinone derivatives and their use for the treatment of HIV related diseases

A compound having the formula (1)

• 247
• wherein:
• Q represents —NR1R2 or —R0NR1R2 wherein:
• R0 represents C1-6 alkanediyl;
• R1 and R2 each independently represent C1-6alkyl or C3-6alkenyl;
• said C1-6alkyl and C3-6alkenyl may be substituted with one, two or three substituents selected from hydroxy, C1-4alkyloxy, C1-4alkylthio, aryloxy, arylthio, amino, mono- or di(C1-4alkyl)amino and aryl;
• or
• R1 and R2 taken together may form a bivalent radical —R1-R2— wherein —R1-R2 — represents —(CH2)2—O—(CH2)2—, —(CH2)2—NR7—(CH2)2, —(CH2)2—CH(NHR7)—(CH2)2— or —(CH2)n wherein R7 represents hydrogen or C1-4alkyl and n represents 2, 3, 4, 5 or 6;
• R3 represents aryl or a monocyclic or bicyclic heterocycle selected from pyridinyl, pyrimidinyl, thiazolinyl, furanyl, thienyl, imidazolyl, benzoxazolyl, benzothiazolyl, benzimidazolyl;
• said monocyclic or bicyclic heterocycle may optionally be substituted with one, two or three substituents each independently selected from hydroxy, C1-4alkyl, C1-4alkoxy, halo, trifluoromethyl, dimethylenoxy or phenyl,
• R4 and R5 each independently represent hydrogen, C1-6alkyl, C3-6alkenyl, C1-4alkoxy, C1-4alkyloxyC1-4alkyl, amino, mono- or di(C1-4alkyl) amino, formyl, C1-4alkylcarbonyl carboxyl, C1-4 alkyloxycarbonyl, or C1-4alkyl aminocarbonyl;
• wherein C1-6alkyl and C3-6alkenyl may be substituted with one, two or three substituents selected from hydroxy, C1-4alkyloxy, C1-4alkyl thio, aryloxy, arylthio, amino, mono- or di(C1-4alkyl)amino and aryl;
• or R4 and R5 taken together form a bivalent radical of formula —R4-R5— wherein —R4-R5— represents —CH═CH—CH═CH— or —(CH2)t, wherein t represents 3 or 4;
• R6represents hydrogen, hydroxy, C1-4alkyloxy, c1-6alkyl, C3-6alkenyl, aryl, C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or alkylaryl;
• Y represents O or S;
• X represents a radical of formula:
• —(CH2)p (a)
• or
• —(CH2)q—Z—(CH2)r (b)
• wherein p represents 1, 2, 3, 4 or 5;
• q represents 0, 1, 2, 3, 4 or 5;
• r represents 0, 1, 2 or 3;
• Z represents NR8, C(═O), CHOH, CHNR8R9;
• CF2, O, S or CH═CH;
• wherein R8 and R9 each independently represent hydrogen or C1-4 alkyl;
• or a N-oxide, a stereochemically isomeric form or a pharmaceutically acceptable addition salt thereof.