Patent ID: 6706715
Filing Date: 2004-03-16
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula I, wherein:D1 and D2 independently from one another are a hydrogen atom, â€”C(O)â€”(C1-C6)-alkyl, â€”C(O)-aryl, â€”C(O)â€”(C1-C6)-alkyl-aryl, â€”C(O)â€”Oâ€”(C1-C6)-alkyl, â€”C(O)â€”Oâ€”(C1-C6)-alkyl-aryl, â€”C(O)â€”Oâ€”(C1-C6)-aryl or â€”NH2; or D1 is a hydrogen atom, when D2 is â€”OH, â€”Oâ€”C(O)â€”(C1-C6)-alkyl, â€”Oâ€”C(O)-aryl, â€”Oâ€”C(O)â€”(C1-C6)-alkyl-aryl or â€”NH2; or D2 is a hydrogen atom, when D1 is â€”OH, â€”Oâ€”C(O)â€”(C1-C6)-alkyl, â€”Oâ€”C(O)-aryl, â€”Oâ€”C(O)â€”(C1-C6)-alkyl-aryl or â€”NH2; or D1 and D2 together with the nitrogen atom to which they are attached form a cycle of the formula VIII D1 and R4 or D2 and R4 together form a cycle of the formulae VIIIa to VIIId, X1 and X2, independently from one another, are a nitrogen atom, or a carbon atom substituted by R4a, wherein R4a is a hydrogen atom, â€”(C1-C6)-alkyl, â€”OH, â€”Oâ€”(C1-C6)-alkyl, halogen, â€”NH2 or â€”NO2; R4 and R5 independently from one another are a hydrogen atom, â€”(C1-C6)-alkyl, â€”OH, â€”Oâ€”(C1-C6)-alkyl, halogen, â€”NH2 or â€”NO2; X3 is an oxygen atom, sulfur atom or NH; A is â€”X4â€”, â€”N(R3)â€”X4â€”, or â€”Oâ€”X4â€” wherein â€”X4â€” is a covalent bond, â€”CH2â€”, â€”CH(OH)â€”, â€”CH(NH2)â€”, â€”CH(COOH)â€”, â€”CH(CONH2)â€”, â€”CH(CH2â€”OH)â€”, â€”CH(â€”CH2â€”NH2)â€”, â€”CH(â€”CH2â€”COOH)â€” or â€”CH(â€”CH2â€”CONH2)â€”, and wherein R3 is a hydrogen atom, â€”OH or â€”NH2; R1 and R2 together with each of the carbon atoms to which they are attached form aryl, wherein aryl is unsubstituted or mono- or disubstituted independently of one another by R6, or form heteroaryl, wherein heteroaryl is unsubstituted or mono- or disubstituted independently of one another by R6, or form a 3- to 8-membered cyclic group, wherein said cyclic group is saturated or partially saturated and unsubstituted or mono- or disubstituted independently of one another by R6 or &boxH;O, or form a 3- to 8-membered cyclic group, having up to 1, 2, 3 or 4 heteroatoms chosen from nitrogen, sulfur or oxygen, wherein said cyclic group is saturated or partially saturated and unsubstituted or mono- or disubstituted independently of one another by R6 or &boxH;O, wherein R6 is halogen, â€”(CH2)nâ€”OH, wherein n is the integer zero, 1 or 2, â€”(CH2)nâ€”Oâ€”R10, wherein R10 is â€”(C1-C6)-alkyl or â€”(C1-C6)-alkyl-aryl, and n is the integer zero, 1 or 2, â€”(CH2)nâ€”COOR11, wherein R11 is a hydrogen atom, â€”(C1-C6)-alkyl or â€”(C1-C6)-alkyl-aryl, and n is the integer zero, 1 or 2, â€”(CH2)nâ€”C(O)N(H)R12, wherein R12 is a hydrogen atom or â€”(C1-C6)-alkyl, and n is the integer zero, 1 or 2, â€”NO2, â€”N(H)R12a, wherein R12a is a hydrogen atom, formyl, acetyl, sulfonylmethyl, amidosulfonyl or â€”(C1-C6)-alkyl, â€”CF3, â€”SO2â€”R13, wherein R13 is methyl, ethyl or â€”NH2, â€”CN, â€”(C1-C6)-alkyl, â€”(C1-C6)-alkyl-aryl, -heteroaryl, â€”(C1-C6)-alkyl-heteroaryl, or -heterocycloalkyl; B isâ€”N(R7)â€”(CHâ€”(R8))p-aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by an aryl group substituent selected from the group consisting of 1) â€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by &boxH;O, &boxH;S, â€”Oâ€”R10, halogen, aryl or heteroaryl, 2) â€”(C3-C6)-cycloalkyl, wherein cycloalkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by &boxH;O, &boxH;S, â€”Oâ€”R10, halogen, aryl or heteroaryl, 3) â€”CF3, 4) â€”CN, 5) â€”NO2, 6) halogen, 7) â€”C(O)â€”Oâ€”R14, wherein R14 is hydrogen atom or as R6, 8) â€”C(O)â€”(C0-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 9) â€”Oâ€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 10) â€”Oâ€”(C1-C6)-alkyl-aryl, wherein alkyl and aryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 11) â€”Oâ€”(C1-C6)-alkyl-heteroaryl, wherein alkyl and heteroaryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 12) â€”Oâ€”C(O)â€”Sâ€”(C1-C6)-alkyl, 13) â€”Oâ€”C(O)â€”(C1-C6)-alkyl-aryl, wherein alkyl and aryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 14) â€”Oâ€”C(O)â€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 15) â€”Oâ€”C(O)â€”(C1-C6)-alkyl-heteroaryl, wherein alkyl and heteroaryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 16) â€”Oâ€”C(O)-aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 17) â€”Oâ€”C(O)-heteroaryl, wherein heteroaryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 18) â€”Oâ€”C(O)â€”NHâ€”(C1-C6)-alkyl-aryl, wherein alkyl and aryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 19) â€”Oâ€”C(O)â€”NHâ€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 20) â€”Oâ€”C(O)â€”NHâ€”(C1-C6)-alkyl-heteroaryl, wherein alkyl and heteroaryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 21) â€”Oâ€”C(O)â€”NH-aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 22) â€”Oâ€”C(O)â€”NH-heteroaryl, wherein heteroaryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 23) aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 24) â€”O-aryl, wherein â€”O-aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 25) heteroaryl, wherein heteroaryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 26) â€”O-heteroaryl, wherein â€”O-heteroaryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 27) â€”(CH2)râ€”S(O)sâ€”R15, wherein â€”R15 is a) â€”OH, provided that s is only 2, b) â€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, c) aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, d) â€”(C1-C6)-alkyl-aryl, wherein alkyl and aryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by R6, or e) â€”N(R16)2, wherein R16 independently of one another are a hydrogen atom or R15 a) to R15 d), provided that s is only 2, r is the integer zero, 1, 2, or 3, and s is the integer zero, 1 or 2, 28) â€”N(R17)2, wherein R17 independently of one another are a) a hydrogen atom, b) â€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by an aryl group substitutent selected from the group consisting of aryl group substituents 1) to 27), c) aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 27) or two adjacent carbon atoms of the aryl residue form a dioxolan residue, d) â€”(C1-C6)-alkyl-aryl, wherein alkyl and aryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 27) or two adjacent carbon atoms of the aryl residue form a dioxolan residue, e) heteroaryl, wherein heteroaryl is unsubstituted or mono-, di- or trisubstituted independently of one another by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 27) or &boxH;O, f) â€”(C1-C6)-alkyl-heteroaryl, wherein alkyl and heteroaryl independently of one another are unsubstituted or mono-, di- or trisubstituted independently of one another by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 27) or &boxH;O, g) â€”C(O)â€”R18, wherein R18 is 1) a hydrogen atom, 2) â€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 3) aryl, wherein aryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, 4) â€”(C1-C6)-alkyl-aryl, wherein alkyl and aryl independently of one another are unsubstituted or mono-, di- or trisubstituted by R6, or 5) heteroaryl, wherein heteroaryl is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, or 6) â€”(C1-C6)-alkyl-heteroaryl, wherein alkyl and heteroaryl independently of one another are unsubstituted or mono-, di- or trisubstituted by R6, h) â€”C(S)â€”R18, i) â€”C(O)â€”Oâ€”R18, j) â€”C(O)â€”N(R18)2, wherein R18 are independent of one another, k) â€”S(O)â€”R18, l) â€”S(O)2â€”R18, m) â€”S(O)â€”N(R18)2, wherein R18 are independent of one another, n) â€”S(O)2â€”N(R18)2, wherein R18 are independent of one another, o) â€”(C3-C6)-cycloalkyl, or p) both R17 residues form, together with the nitrogen atom to which they each are bonded, a 3- to 8-membered cyclic group, containing up to 1, 2, 3 or 4 heteroatoms chosen from nitrogen, sulfur or oxygen, wherein said cyclic group is saturated or partially saturated, and wherein said cyclic group is unsubstituted or mono-, di- or trisubstituted independently of one another by R6, and (29) â€”C(O)â€”N(R17)2, wherein R17 are independent of one another. or B is â€”N(R17)2, wherein R17 are independent of one another, provided that if there is a single bond between A and B, then A and B are in a cis-conformation to each other; p is the integer zero, 1 or 2; R7 is a hydrogen atom, â€”(C1-C6)-alkyl or â€”OH; R8 is a) a hydrogen atom, b) â€”(C1-C6)-alkyl, wherein alkyl is unsubstituted or mono- to totally substituted by fluorine, c) â€”(C2-C6)-alkenyl, wherein alkenyl is unsubstituted or mono- di- or trisubstituted by fluorine, d) â€”(C2-C6)-alkinyl, wherein alkinyl is unsubstituted or mono- di- or trisubstituted by fluorine, e) â€”(C0-C3)-alkyl-(C3-C6)-cycloalkyl, wherein alkyl is unsubstituted or mono- to totally substituted by fluorine, f) â€”CN, g) aryl, wherein aryl is unsubstituted or mono- or di-substituted by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 28), h) heteroaryl, wherein heteroaryl is unsubstituted, mono- or di-substituted by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 28), or i) â€”(C0-C2)-alkyl-Oâ€”(C1-C6)-alkyl, or B is â€”Oâ€”(CHâ€”(R8))p-aryl, or B is â€”N(R7)â€”(CHâ€”(R8))p-heteroaryl, wherein heteroaryl is unsubstituted or mono- or di-substituted by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 28), or or B is â€”Sâ€”(CHâ€”(R8))p-aryl, wherein aryl is unsubstituted or mono- or di-substituted by an aryl group substituent selected from the group consisting of aryl group substituents 1) to 28); or a stereoisomeric form, or mixture of stereoisomeric forms thereof, or a physiologically tolerable salt of such compound, stereoisomeric form or mixture.