Patent ID: 6503934
Filing Date: 2003-01-07
Classification: A61P,C07D

Abstract:
A compound of formula (I): in any of its stereoisomeric forms, or in a mixture thereof in any ratio, or a physiologically tolerated salt of any of the foregoing, in which:R1 is 1. phenyl, 2. phenyl which is mono- to trisubstituted by: 2.1. â€”(C1-C6)-alkyl, wherein alkyl is straight-chain, cyclic, or branched, 2.2. â€”OH, 2.3. â€”Oâ€”C(O)â€”(C1 -C6)-alkyl-, 2.4. â€”Oâ€”(C1-C6)-alkyl, 2.5. methylenedioxo, 2.6. halogen, 2.7. â€”CF3, 2.8. â€”CN, 2.9. â€”NO2, 2.10. â€”C(O)â€”OH, 2.11. â€”C(O)â€”Oâ€”(C1-C6)-alkyl, or 2.12. R3â€”(R4)Nâ€”, wherein R3 and R4 are identical or different and are a hydrogen atom or (C1-C6)-alkyl, or 3. a heteroaromatic from the following group 3.1 to 3.15, which is unsubstituted or substituted as described under 2.1 to 2.12, 3.1. pyrrole, 3.2. pyrazole, 3.3. imidazole, 3.4. triazole, 3.5. thiophene, 3.6. thiazole, 3.7. oxazole, 3.8. isoxazole, 3.9. pyridine, 3.10. pyrimidine, 3.11. indole, 3.12 benzothiophene, 3.13. benzimidazole, 3.14. benzoxazole, or 3.15. benzothiazole; R3 is 1. a hydrogen atom or 2. â€”(C1-C6)-alkyl; R2 is 1. â€”(C1-C7)-alkyl, wherein alkyl is branched or unbranched and is mono- or disubstituted as described above under 2.2 to 2.12, or is substituted by a heteroalkyl ring or by a (C3-C7)-cycloalkyl, wherein the heteroalkyl ring or the (C3-C7)-cycloalkyl is unsubstituted or is mono- or disubstituted as described above under 2.1 to 2.12, 2. â€”(C2-C10)-alkenyl, wherein alkenyl is straight-chain or branched, 3. â€”(C3-C7)-cycloalkyl, wherein cycloalkyl is unsubstituted or is mono- or disubstituted as described above under 2.1 to 2.12, 4. phenyl, wherein phenyl is unsubstituted or mono- or disubstituted as described above under 2.1 to 2.12, 5 â€”(CH2)m-phenyl, wherein phenyl is unsubstituted or mono- or disubstituted as described above under 2.1 to 2.12, and m is the integer 1, 2, 3, 4, 5, or 6, or wherein one hydrogen atom of the â€”(CH2)m radical is replaced by â€”OH, 6. â€”(CH2)n-heteroaryl, wherein heteroaryl is as defined under 3.1 to 3.15, and is unsubstituted or substituted as described above under 2.1 to 2.12, and n is the integer zero, 1, 2, 3, 4, 5, or 6, 7. â€”(C2-C6)-alkyl-Oâ€”R6, wherein R6 is a hydrogen atom, benzyl, allyl, or (C1-C6)-alkyl, and wherein the alkyl radical is straight chain or branched, 8. â€”(C2-C6)-alkyl-C(O)â€”OR6, wherein R6 is as defined above, 9. â€”C(R8,R7)â€”C(O)â€”X, wherein R8 has the same meaning as R3 above, R7 is the radical of an &agr;-amino acid, or R8 and R7 (together with the carbon atom to which they are bonded) form a 4- to 7-membered ring, and X is â€”OH, NHR6, or â€”OR6, wherein R6 is as defined above, or 10. R2 and R3 (together with the nitrogen to which they are bonded) form a 4- to 7-membered ring, wherein at least one of the carbon atoms is optionally replaced by â€”Oâ€”, â€”Sâ€” or â€”NHâ€”, and wherein one, two or three of the carbon atoms in the ring are unsubstituted or mono- or disubstituted by 10.1 (C1-C2)-alkyl, 10.2 phenyl, 10.3 â€”OH, 10.4 &boxH;O, 10.5 â€”C(O)â€”Oâ€”(C1-C6)-alkyl, 10.6 â€”C(O)-phenyl, wherein phenyl is unsubstituted or substituted as described above under 2.1 to 2.12, 10.7 â€”C(O)â€”(C1-C6)-alkyl, or 10.8 â€”Câ€”(O)â€”OR3, wherein R3 is a hydrogen atom or (C1-C6)-alkyl, and optionally 10.9 two carbon atoms in the ring form part of an additional phenyl radical, which is unsubstituted or substituted as described above under 2.1 to 2.12, or wherein the hydrogen atom in the â€”NHâ€” optionally present is unsubstituted or is substituted by (a) (C1-C3)-alkyl, (b) â€”C(O)â€”R3, wherein R3 is as defined above, (c) â€”(CH2)o-phenyl, wherein phenyl is unsubstituted or mono- or disubstituted as described under 2.1 to 2.12, and o is the integer zero, one, or two, (d) benzoyl, which is unsubstituted or substituted as described above under 2.1 to 2.12, or (e) â€”C(O)â€”Oâ€”(C1-C6)-alkyl; provided that, when R1 is phenyl and R2 is phenyl, R3 is other than hydrogen.