Patent ID: 6645992
Filing Date: 2003-11-11
Classification: A61K,A61P,C07C

Abstract:
A compound of formula I, wherein:A is a compound of formula II, â€ƒwherein: R3 is hydrogen, â€”OH, or â€”(C1-C7)-alkyl; R4 and R5, independently of one another, are 1. hydrogen; 2. â€”(C1-C7)-alkyl; 3. â€”OH; 4. â€”Oâ€”(C1-C7)-alkyl; 5. halogen; 6. â€”NH2; or 7. â€”NO2; X1 and X2, are selected from a carbon substituted by R4, wherein R4 is as defined above; D1 and D2, independently of one another, are 1. hydrogen; 2. â€”C(O)â€”(C1-C7)-alkyl; 3. â€”C(O)-aryl; 4. â€”C(O)â€”(C1-C7)-alkyl-aryl; 5. â€”C(O)â€”Oâ€”(C1-C7)-alkyl; 6. â€”C(O)â€”Oâ€”(C1-C7)-alkyl-aryl; or 7. â€”C(O)â€”Oâ€”(C1-C6)-aryl; or D1 is hydrogen, when D2 is 1. â€”OH; 2. â€”Oâ€”C(O)â€”(C1-C7)-alkyl; 3. â€”Oâ€”C(O)-aryl; or 4. â€”Oâ€”C(O)â€”(C1-C7)-alkyl-aryl; or D1 and D2, together with the nitrogen to which they are attached, form a cycle of the formula VIII R1 is 1. hydrogen; 2. â€”(C1-C7)-alkyl; 3. â€”OH; 4. â€”Oâ€”(C1-C7)-alkyl; or 5. â€”Nâ€”(R6)2, wherein R6 is, independently of one another, hydrogen, â€”C(O)-aryl, â€”C(O)â€”(C1-C7)-alkyl-aryl, â€”C(O)â€”(C1-C7)-alkyl, â€”(C1-C7)-alkyl, â€”C(O)â€”N(H)-aryl, â€”C(O)â€”N(H)â€”(C1-C7)-alkyl-aryl, â€”(C1-C6)â€”N(H)-alkyl, â€”C(O)â€”O-aryl, â€”C(O)â€”Oâ€”(C1-C7)-alkyl-aryl, â€”C(O)â€”Oâ€”(C1-C7)-alkyl-, S(O2)-aryl, or â€”S(O2)â€”(C1-C7)-alkyl; R2 is 1. aryl, wherein aryl is unsubstituted or mono- to tri-substituted, independently of one another, by 1.1 â€”CF3; 1.2. halogen; 1.3 â€”OH; 1.4 â€”CN; 1.5 sulfo; 1.6 â€”NO2; 1.7 â€”NH2; 1.8 â€”Oâ€”(C1-C7)-alkyl; 1.9 substituted amino; 1.10 â€”COOH; 1.11 â€”(C1-C7)-alkyl; 1.12 carbamyl; 1.13 carbonyl; 1.14 alkoxycarbonyl; 1.15 methylendioxyl; 1.16 aryloxy, wherein aryloxy is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.15; 1.17 â€”Oâ€”(C1-C7)-alkyl-aryl, wherein aryl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.15; 1.18 Het-group, wherein Het-group is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.15; or 1.19 â€”(C0-C4)-alkyl-aryl, wherein aryl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.15; 2. hydrogen; 3. Het-group, wherein the Het-group is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; 4. â€”(CH2)mâ€”Ynâ€”(CH2)o-aryl, in which m, n, and o are, independently of one another, 0, 1, or 2, provided that at least one of m, n, and o is not 0; aryl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; and Y is â€”Oâ€”, â€”Sâ€”, or â€”Nâ€”(R6) wherein R6 is hydrogen or â€”(C1-C7)-alkyl, provided n is 1, or Y is â€”N(R6)â€”N(R6)â€” wherein R6 is, independently of one another, hydrogen or â€”(C1-C7)-alkyl, or â€”N&boxH;Nâ€”, provided n is 2; or 5. â€”(CH2)mâ€”Ynâ€”(CH2)o-Het-group, in which m, n, and o are, independently of one another, 0, 1, or 2, provided that at least one of m, n, and o is not 0; Het-group is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; and Y is as defined above; or R1 and R2, together with the carbon to which they are bonded, form 1. a â€”(C3-C7)-cycloalkyl, wherein cycloalkyl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; 2. a â€”(C3-C7)-cycloalkyl, wherein cycloalkyl is unsubstituted or mono- to disubstituted, independently of one another, and fused to an aryl- or Het-group-ring, which itself is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; 3. a Het-group, wherein the Het-group is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; or 4. a keto-group, which may partially or totally exist in a hydrated state; provided that, when R1 is as defined above under 3, 4, or 5, then R2 is not directly bonded to formula I via a oxygen-, sulfur- or nitrogen-; B is 1. â€”N(R7)â€”(CHâ€”(R8))p-aryl, in which aryl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.3 and 1.5 to 1.19 above; p is 0, 1, or 2; R7 is 1.1 hydrogen; 1.2 â€”(C1-C7)-alkyl; 1.3 â€”OH; or 1.4 â€”Nâ€”(R6)2, wherein R6 is, independently of one another, hydrogen or â€”(C1-C7)-alkyl; R8 is 1.1 hydrogen; 1.2 â€”(C1-C7)-alkyl; 1.3 â€”(C2-C7)-alkenyl; 1.4 â€”(C2-C7)-alkynyl; 1.5 â€”(C0-C3)-alkyl-(C3-C7)-cycloalkyl; 1.6 â€”CN; 1.7 aryl, aryl is unsubstituted or mono- or di-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; 1.8 a Het-group, wherein the Het-group is unsubstituted or mono- or di-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; 1.9 â€”(CHâ€”(R8))â€” forms a â€”(C3-C7)-cycloalkyl derivative; or 1.10 â€”(C0-C4)-alkyl-Oâ€”(C1-C7)-alkyl; 2. â€”Oâ€”(CHâ€”(R8))p-aryl, wherein aryl, R8, and p are as defined above; 3. â€”N(R7)â€”(CHâ€”(R8))p-Het-group, wherein the Het-group is unsubstituted or mono- or di-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above, and R7, R8, and p are as defined above; 4. â€”N(R9)â€”N(R9â€²)â€”(CHâ€”(R8))q-aryl, in which aryl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; q is 0, 1, or 2; R9 and R9â€² are, independently of one another, hydrogen, â€”(C1-C7)-alkyl, or â€”(C1-C3)-alkyl-aryl; and R8 is as defined above; 5. â€”Oâ€”N(R9)â€”(CHâ€”(R8))q-aryl, in which aryl is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; q is 0, 1, or 2; and R8 and R9 are as defined above; 6. â€”N(R9)â€”N(R9â€²)â€”(CHâ€”(R8))q-Het-group, in which Het-group is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; q is 0, 1, or 2; and R8, R9â€², and R9 are as defined above; or 7. â€”Oâ€”N(R9)â€”(CHâ€”(R8))q-Het-group, in which Het-group is unsubstituted or mono- to tri-substituted, independently of one another, by a substituent as defined by 1.1 to 1.19 above; q is 0, 1, or 2; and R8 and R9 are as defined above; in any stereoisomeric form or mixture thereof in any ratio, or a physiologically tolerable salt thereof.