Patent ID: 6339082
Filing Date: 2002-01-15
Classification: A61P,C07D

Abstract:
A compound selected from the group consisting of a compound of the formula wherein R1 is â€”CONHâ€”Aâ€”Bâ€”COR6, A is a divalent, optionally unsaturated hydrocarbon of 1 to 12 carbon atoms unsubstituted or substituted by Z, B is selected from the group consisting of phenylene, a single bond and â€”CHZâ€”, Z is selected from the group consisting of hydrogen, â€”D0-6â€”NHâ€”Raâ€”Rb, â€”D0-6â€”NHâ€”SO2â€”Rc, â€”D0-6â€”NHâ€”CO2â€”Rc, â€”D0-6â€”NHâ€”COâ€”Rc, â€”D0-6â€”NHâ€”SO2â€”NHâ€”Rc, â€”D0-6NHâ€”COâ€”NHâ€”Rc, â€”Dâ€”0-6â€”CO2â€”Rc, â€”D0-6â€”SO2â€”Rc, â€”D0-6â€”COâ€”Rc and â€”D0-6â€”Rc, D is a divalent, optionally unsaturated hydrocarbon of 0 to 6 carbon atoms, Ra, Rb and Rc are individually selected from the group consisting of hydrogen, â€”(CH2)0-3â€”Ar, â€”(CH2)0-3â€”Alk and â€”(CH2)0-3â€”Het, Ar is carbocyclic aryl of 6 to 18 carbon atoms, Het is saturated or unsaturated, aromatic or non-aromatic heterocycle of 1 to 9 carbon atoms and 1 to 5 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, Alk is saturated or unsaturated alkyl and cycloalkyl of up to 12 carbon atoms, the Ar, Alk and Het being optionally substituted or Ra and Rb together with the nitrogen to which they are attached form an aromatic or non-aromatic, saturated or unsaturated, optionally substituted heterocycle optionally containing at least one further heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, R6 is selected from the group consisting of â€”OH, â€”OAlk, â€”OAr, â€”NH2, â€”NHAlk, â€”N(Alk)2 and acyl of an L- or D-amino acid, R2 and R3 are individually selected from the group consisting of hydrogen, â€”OH, â€”OAlk and â€”Oâ€”(CH2)0-3â€”Ar or R2 and R3 form a ring â€”Oâ€”(CRdRc)nâ€”Oâ€”, n is an integer from 1 to 5, Rd and Re are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and phenyl, R4 is selected from the group consisting of hydrogen, halogen, â€”OH, â€”NH2, â€”NO2, â€”CN, acyl and acyloxy of an organic carboxylic acid of 1 to 12 carbon atoms and alkyl, alkenyl, alkynyl, alkylthio, alkoxy, alkylamino, dialkylamino, dialkylaminoalkyl and dialkylaminoalkoxy, all of up to 6 carbon atoms, R5 is selected from the group consisting of hydrogen, â€”OH, halogen, â€”Alk and â€”Oâ€”(CH2)0-3â€”Ar, G is selected from the group consisting of â€”NRaRb, â€”Het, and â€”NRhâ€”SO2â€”Rc, Rh is hydrogen, or Alk, Hetâ€² is (J) is the remainder of an aromatic or non-aromatic, saturated or unsaturated, mono or bicyclic, optionally substituted heterocycle of 1 to 9 carbon atoms and 2 to 5 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, X is selected from the group consisting of O&boxH;, S&boxH; and &boxH;NH, the dotted lines are an optional second bond, R1, R2 and R3 are in 8, 9 or 10 position of the tricycle and its salts with non-toxic, pharmaceutically acceptable acids and bases.