Small molecule inhibitors targeted at BCL-2

A composition comprising a compound of formula:

• 33
• wherein X and Y are each independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine and iodine;
• Z1 and Z2 are each independently O or S;
• A1 and A2 are each independently 1 to 3 substituents and selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COHO, COO(C1-C6)alkyl, COHN, COHN(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• B1, B2, B3 and B4 are each independently 1 to 2 substituents and selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• and pharmaceutically acceptable salts and derivatives thereof.

A composition comprising a compound of formula:

• 34
• wherein X and Y are each independently hydrogen, OR or OR1;
• wherein R and R1 are each independently hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl or trifluoromethyl;
• wherein R2, R3, R4 and R5 are each independently hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2) n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• A and A1 are each independently 1 to 3 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2) n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• and pharmaceutically acceptable salts and derivatives thereof.

A composition comprising a compound of formula:

• 35
• wherein R is selected from the group consisting of NH2, NH((C1-C6)alkyl) and N((C1-C6)alkyl)2;
• A1 is 1 to 4 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2) n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• A2 is 1 to 5 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6) alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• or a pharmaceutically acceptable salt thereof.

A composition comprising a compound of formula:

• 36
• wherein, Z is O or S;
• X is selected from the group consisting of hydrogen and OR, wherein R is selected from the group consisting of hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl and trifluoromethyl;
• A1 and A2 are each independently 1 to 3 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6) alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• and pharmaceutically acceptable salts and derivatives thereof.

A composition comprising a compound of formula:

• 37
• wherein Z is O or S;
• A1 and A2 are each independently 1 or 2 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2) n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F. Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F. Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position it or 2by methyl or benzyl);
• B1 and B2 are each independently 1 to 3 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2) n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position or 2 by methyl or benzyl);
• D1 and D2 are each independently 1 to 4 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2) n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• and pharmaceutically acceptable salts and derivatives thereof.

A composition comprising a compound of formula:

• 38
• wherein X and Y are each independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine and iodine;
• A1 and A2 are each independently 1 to 3 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• B1 and B2 are each independently 1 to 3 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6) alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• and pharmaceutically acceptable salts and derivatives thereof.

A composition comprising a compound of formula:

• 39
• wherein R1 and R2 are each independently hydrogen, OR3 or OR4, NH2, NH((C1-C6)alkyl) or N((C1-C6)alkyl)2;
• wherein R3 and R4 are each independently hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl or trifluoromethyl;
• A1 and A2 are each independently 1 to 4 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2)n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position 1 or 2 by methyl or benzyl);
• B is 1 or 2 substituents selected from the group consisting of hydrogen, hydroxy, branched or straight chain (C1-C6)-alkyl, branched or straight chain (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, phenyl, aryl, (C1-C6)-alkoxy, CZ3 (wherein Z is selected from the group consisting of F, Cl, Br and I), NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NO2, CN, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON((C1-C6)alkyl)2, O—(C1-C6)alkyl (where one, more than one or all hydrogen(s) in the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, O—CH2—Ph, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2, NH—CO—CH3 or N(COOCH2Ph)2), SO2—NH2, SO2NH(C1-C6)alkyl, SO2N((C1-C6)alkyl)2, S—(C1-C6)alkyl, S—(CH2) n-phenyl, SO—(C1-C6)-alkyl, SO—(CH2)n-phenyl, SO2—(C1-C6)-alkyl, SO2—(CH2)n-phenyl (where n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH((C1-C6)alkyl), N((C1-C6)alkyl)2), NH(C1-C7)-acyl, phenyl, biphenylyl, O—(CH2)n-phenyl (where n is 0-6), 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl, 2- or 3-thienyl (wherein the phenyl, biphenylyl, naphthyl, pyridyl, furanyl, thienyl rings may be optionally substituted up to 3 times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O—(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, SO2—CH3, COOH, COO—(C1-C6)-alkyl or CONH2), 1,2,3-triazol-5-yl (wherein the triazol ring may be optionally substituted in position 1, 2 or 3 by methyl or benzyl) or tetrazol-5-yl (wherein the tetrazol ring may be optionally substituted in position1 or 2 by methyl or benzyl);
• and pharmaceutically acceptable salts and derivatives thereof.