Patent ID: 6740663
Filing Date: 2004-05-25
Classification: A61P,C07D

Abstract:
A compound comprising a benzothiepene of Formula I-1 or I-2: or a pharmaceutically acceptable salt, solvate, or prodrug thereofwherein j is 0, 1 or 2; wherein m is 0, 1, 2, 3 or 4; wherein R2A and R2B are independently selected from the group consisting of hydrogen and hydrocarbyl; wherein R3A, R3B, R5A, and R5B are independently selected from the group consisting of hydrogen, alkyl; cycloalkyl; alkenyl; alkynyl; heterocyclyl; quaternary heterocyclyl, oxo; aryl-R5; â€”OR9; â€”NR9R10; â€”SR9; â€”S(O)R9; â€”SO2R9; and â€”SO3R9; wherein R9 and R10 are independently selected from the group consisting of hydrogen; hydrocarbyl; amino; and hydrocarbylamino; wherein R5 is selected from the group consisting of hydrogen; hydrocarbyl, heterocyclyl, outeraryloc; â€”OR9; â€”SR9; â€”S(O)R9; â€”SO2R9; and â€”SO3R9; wherein when R5 is said cycloalkyl, aryl or heterocyclyl, said cycloalkyl, aryl or heterocyclyl are optionally substituted with â€”NHâ€”Xâ€”R or â€”Oâ€”Xâ€”R; wherein X is selected from the group consisting of â€”(C&boxH;O)s-alkyl-; â€”(C&boxH;O)s-alkyl-NHâ€”; â€”(C&boxH;O)s-alkyl-Oâ€”; â€”(C&boxH;O)s-alkyl-(C&boxH;O)t; and a covalent bond, wherein s and t are independently 0 or 1; wherein R is selected from the group consisting of monosaccharides, disaccharides, and polysaccharides, wherein said monosaccharides, disaccharides, and polysaccharides are optionally protected with one or more sugar protecting groups; wherein R9 and R10 are as previously defined; wherein, when R5&ap;H, R5 is optionally substituted with one or more radicals independently selected from the group consisting of halogen; â€”NO2; â€”CN; oxo; hydrocarbyl; â€”OR13; â€”NR13R14; â€”SR13; â€”S(O)R13; â€”SO2R13â€”SO3R13; â€”NR13OR14; â€”NR13NR14R15; â€”CO2R13; â€”OM; â€”SO2OM; â€”SO2NR13R14; â€”C(O)NR13R14; â€”C(O)OM; â€”COR13; â€”NR13C(O)R14; â€”NR13C(O)NR14R15; â€”NR13CO214; â€”OC(O)R13; â€”OC(O)NR13R14; â€”NR13SOR14; â€”NR13SO2R14; â€”NR13SONR14R15; â€”NR13SO2NR14R15; â€”PR13R14; â€”P(O)R13R14; â€”P+R13R14R15Aâˆ’; â€”P(OR13)OR14; â€”S+R13R14Aâˆ’; and â€”N+R13R14R15Aâˆ’; wherein R13, R14, and R15 are independently selected from the group consisting of hydrogen and hydrocarbyl; wherein Aâˆ’ is a pharmaceutically acceptable anion; wherein M is a pharmaceutically acceptable cation; wherein one or more R6 radicals are independently selected from the group consisting of hydrogen; halogen; â€”CN; â€”NO2; hydrocarbyl; â€”R5; â€”OR13; â€”NR13R14; â€”SR13; â€”S(O)R13; â€”S(O)2R13; â€”SO3R13; â€”S+R13R14Aâˆ’; â€”NR13OR14; â€”NR13NR14R15; â€”OM; â€”SO2OM; â€”SO2NR13R14; â€”NR14C(O)R13; â€”C(O)OM; â€”S(O)NR13R14; N+R13R14R15Aâ€”; â€”PR13R14; â€”P(O)R13R14; â€”P+R13R14R15Aâˆ’; amino acid residue; peptide residue; polypeptide residue; and carbohydrate residue; wherein R13, R14, R15, Aâˆ’, and M are as defined above; and wherein, in each instance, said hydrocarbyl may be optionally substituted with one or more groups comprising one or more heteroatoms, and wherein, in each instance, said hydrocarbyl optionally may have one or more carbon atoms replaced by one or more heteroatoms independently selected from the group consisting of oxygen, nitrogen, sulfur, phosphorus and combinations thereof.