Patent ID: 6444664
Filing Date: 2002-09-03
Classification: A61K,A61P,Y10S

Abstract:
A method for treating or preventing atherosclerotic conditions comprising decreasing the synthesis of apolipoprotein(a) or decreasing the plasma level of lipoprotein(a) or increasing the synthesis of apolipoprotein A1 or increasing the plasma level of high-density lipoprotein by administering an effective amount of a compound selected from the group consisting of azepine derivatives having the following formula 1: and of benzoazepine derivatives having the following formula 1a: wherein, in formula 1, A is a group â€”CH&boxH;C(R2)â€”CH&boxH;CHâ€”, â€”Sâ€”C(R2)&boxH;CHâ€”, â€”CH&boxH;C(R2)â€”Sâ€” or an optionally substituted benzo or thieno ring having the following formula 1b: Q is a nitrogen atom (â€”N&boxH;), or an optionally substituted carbon atom (â€”CR4&boxH;), R4 being as defined below; X is a nitrogen, sulphur or oxygen atom, the neighboring bond optionally being a double bond if X is nitrogen; Y is a nitrogen atom (&boxH;Nâ€”) or an optionally substituted carbon atom (&boxH;CRâ€”), having a substituent R wherein R is hydrogen, methyl, ethyl, methoxycarbonyl or ethoxycarbonyl; Z is a nitrogen atom (â€”N&boxH;) or an optionally methyl-substituted carbon atom (â€”CR1&boxH;) having a substituent Râ€² wherein R1is hydrogen, methyl or hydroxymethyl; at least one of Y and Z is a nitrogen atom; R1 is hydrogen, halogen, C1-C6 alkyl, cycloalkylalkyl or cycloalkylalkenyl, trifluoromethyl, hydroxymethyl or aminomethyl, R2 is hydrogen, halogen, trifluoromethyl, nitro, C1-C3 alkyl or the group â€”CH2â€”CH2R2, R2â€² being an optionally substituted phenyl, C1-C3 alkoxycarbonyl, or an aminomethyl or carbamoyl group, the nitrogen atom of the aminomethyl or carbamoyl group optionally being substituted by one or two C1-C3 alkyl groups or optionally being part of a pyrrolidino, piperidino, or morpholino ring; R3 is hydrogen, hydroxyl, methyl or carboxyl; and R4 is hydrogen, halogen, hydroxyl, methyl or methoxy.