| abstract |
These derivatives of formula (1), act as phosphodiesterase IV inhibitors and can be used for the treatment of osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, diseases, autoimmune, myocardial diseases and AIDS. Claim 1: Compounds of the formula (1) wherein: R1, R2 are in each case, independently of each other, H, OH, OR8, -SR8, -SOR8, -SO2R8, or Hal; R1 and R2 are also together -OCH2O- or -OCH2CH2O-; R3, R3 'are in each case, independently of each other, H, A "R7, COA" R7, COOA "R7, CONH2, CONHA''R7, WITH (A" R7) (A "') R7, CONR10Het, NH2 , NHA "R7, N (A" R7) (A "'R7), NCOA''R7 or NCOOA''R7; V, W are oxygen, or hydrogen substituents, with the proviso that, when V means O, W is H, H, and vice versa; B is an aromatic isocyclic or heterocyclic radical, which is unsubstituted or which may be mono, di or trisubstituted by R4, R5 and / or R6; X is N or CR3, R4, R5, R6 are in each case, independently of each other, H, A''R7, OH, OA''R7, NO2, NH2, NHA''R7, N (A''R7) (A '' 'R7), NHCOA''R7, NHCOOA''R7, NHCONH2, NHCONHA''R7, NHCON (A''R7) (A' '' R7), Hal, COOH, COOA''R7, CONH2 , CONHA''R7, CON (A''R7) (A '' 'R7); or a remainder of the group of formulas (2); R7 is H, COOH, COOA, CONH2, CONHA, CONAA ', NH2, NHA, NAA', NCOA, NCOOA, OH or OA; R8 is A, C3-7 cycloalkyl, C4-8 alkylenecycloalkyl or C2-8 alkenyl; R9 is C1-10 alkyl, C3-7 cycloalkyl, C4-8 alkylenecycloalkyl or C2-8 alkenyl, where one, two or three CH2 groups may be replaced by O, S, SO, SO2, NH, NMe, NEt and / or by groups -CH = CH- and / or 1-7 atoms of H may be replaced by F and / or Cl; Y is C1-10 alkylene or C2-8 alkenylene, where one, two or three CH2 groups can be replaced by O, S, SO, SO2, NH or NR9 and / or 1-7 H atoms can be replaced by F and / or Cl; A, A 'are in each case, independently of each other, C1-10 alkyl or C2-8 alkenyl, where one, two or three CH2 groups may be replaced by O, S, SO, SO2, NH or NR9 and / or 1 -7 atoms of H may be replaced by F and / or Cl, or aryl or Het; A and A 'are also together a C2-7 alkylene chain, where one, two or three CH2 groups can be replaced by O, S, SO, SO2, NH or NR9, NCOR9 or NCOOR9; A '', A '' 'in each case, independently of each other, are absent, they are C1-10 alkylene, C2-8 alkenylene or C3-7 cycloalkylene, where one, two or three CH2 groups can be replaced by O, S , SO, SO2, NH or NR9 and / or 1-7 H atoms may be replaced by F and / or Cl; A '' and A '' 'are also together a C2-7 alkylene chain, where one, two or three CH2 groups can be replaced by O, S, SO, SO2, NH or NR9, NCOR9 or NCOOR9; aryl is phenyl, naphthyl, fluorenyl, or unsubstituted or mono, di or trisubstituted biphenyl by Hal, R11, OR10, N (R10) 2, NO2, CN, COOR10, CON (R10) 2, NR10COR10, NR10CON (R10) 2, NR10SO2A, COR10, SO2N (R10) 2, S (O) mR11, R10 is H or C1-6 alkyl; R11 is C1-6 alkyl; Het is a saturated, unsaturated or aromatic mono or bicyclic heterocycle with 1 or 2 atoms of N, O and / or S, which is unsubstituted or mono or disubstituted by carbonyl oxygen, Hal, R11, OR10, N (R10) 2, NO2, CN, COOR10, CON (R10) 2, NR10COR10, NR10CON (R10) 2, NR10SO2R11, COR10, SO2NR10 and / or S (O) mR11; Hal is F, Cl, Br or I; m is 0, 1 or 2; as well as derivatives, solvates and stereoisomers thereof for pharmaceutical use, including mixtures thereof in all proportions. |