Patent ID: 6608101
Filing Date: 2003-08-19
Classification: A61K,A61P,C07C,C07D

Abstract:
A compound of the formula (I): or its pharmaceutically acceptable salt, wherein:i) the wavy line indicates that the compound can be in the form of the E or Z isomer; ii) R22 and R23 are independently hydrogen or (C1-C4)alkyl; iii) R2&agr;, R3&agr;, R4&agr;, R5&agr;, R6&agr;, R2&bgr;, R3&bgr;, R4&bgr;, R5&bgr; and R6&bgr; are independently hydrogen, alkyl, carbocycle, aryl, heteroaryl, heterocycle, cycloalkyl, alkoxy, aryloxy, arylalkoxy, heteroaryloxy, heteroarylalkoxy, alkylthio, alkylamino, aminoalkyl, haloalkylthio, acyl, haloalkyl, aryloxy, amido, acylamino, amino, dialkylamino, aminodialkyl, trifluoroalkoxy, alkylsulfonyl, haloalkylsulfonyl, aminocarbonyl, alkenyl, alkynyl, halogen, hydroxyl, thiol, cyano, nitro, sulfonic acid, sulfonate, sulfate, sulfinic acid, sulfenic acid, sulfamide, sulfonamide, sulfoxide, metal sulfinate, phosphate, phosphonate, metal phosphonate, phosphinate, alditol, carbohydrate, amino acid, OC(R1)2CO2H, SC(R1)2CO2H, NHC(R1)2CO2H, COâ€”R2, CO2R1, polyoxyalkylene, polyol alkyl, oxyalkylamino, alkylcarbonylalkyl, lower alkyl S(O)-lower alkyl, lower alkyl-S(O)2-lower alkyl; hydroxyalkyl, aralkoxy, heteroaryl lower alkoxy, heterocyclo lower alkoxy, heteroaryloxy, heterocycleoxy, aralkyl lower thioalkyl, heteroaralkyl lower thioalkyl, heterocycloalkyl lower thioalkyl, heteroaryl lower alkyl, heterocyclo lower alkyl, heteroarylthio lower alkyl, arylthio lower alkyl, heterocyclothio lower alkyl, heteroarylamino lower aikyl, heterocycloamino lower alkyl, arylsulfinyl lower alkyl, arylsulfonyl lower alkyl, any of which can be optionally substituted with a moiety that does not adversely affect the biological properties of the molecule; â€”C(O)(CH2)2CO2âˆ’M+, â€”SO3M+, or -lower alkyl-Oâ€”R, wherein R is PO2(OH)âˆ’M+, PO3(OH)âˆ’M+ or â€”SO3M+, wherein M+ is a pharmaceutically acceptable cation; -lower alkylcarbonyl-lower alkyl; carboxy lower alkyl; -lower alkylamino-lower alkyl; N,N-di-substituted amino lower alkyl-, wherein the substituents each independently represent lower alkyl; iv) R1 is H, lower alkyl, an optionally substituted carbocycle, aryl, heteroaryl, heterocycle, alkylaryl, alkylheteroaryl, alkylheteroaryl or alkylheterocycle; v) R2 is an optionally substituted alkyl, alkenyl, alkynyl, aryl, carbocycle, heteroaryl, heterocycle, alkylaryl, alkylheteroaryl, alkylheteroaryl or alkylheterocycle; vi) alternatively, R22 and R6&agr; or R23 and R6&agr; can join together to form a bridged carbocycle, aryl, heterocycle or heteroaromatic; vii) R2&agr; and R3&agr;, R3&agr; and R4&agr;, R4&agr; and R5&agr;, R5&agr; and R6&agr;, R2&bgr; and R3&bgr;, R3&bgr; and R4&bgr;, R4&bgr; and R5&bgr; or R5&bgr; and R6&bgr; can independently join to form a bridged compound selected from the group consisting of an optionally substituted carbocycle, an optionally substituted cycloalkenyl, an optionally substituted cycloalkylcarbonyl, an optionally substituted cycloalkenylcarbonyl; an optionally substituted aryl, an optionally substituted heterocylic or an optionally substituted heteroaromatic, or alkylenedioxy or wherein the ring can include a carbonyl, cyclic ester, amide, amine, sulfonate, or phosphonate; viii) at least one of R2&agr;, R3&agr;, R4&agr;, R5&agr;, R6&agr;, R2&bgr;, R3&bgr;, R4&bgr;, R5&bgr; or R6&bgr; is, or R2&agr; and R3&agr;, R3&agr; and R4&agr;, R4&agr; and R5&agr;, R5&agr; and R6&agr;, R2&bgr; and R3&bgr;, R3&bgr; and R4&bgr;, R4&bgr; and R5&bgr; or R5&bgr; and R6&bgr; come together to be, an optionally substituted saturated or unsaturated thienyl or benzothienyl; and ix) at least one of R2&agr;, R3&agr;, R4&agr;, R5&agr;, or R6&agr;, and at least one of R2&bgr;, R3&bgr;, R4&bgr;, R5&bgr; or R6&bgr; is a substituent other than hydrogen.