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US 7,956,085 B2Granted
1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof
AssigneeSanofi-Aventis Deutschland GmbH
InventorsWendelin Frick, Heiner Glombik, Stefan Theis, Hubert Heuer, Hans-Ludwig Schaefer, Werner Kramer
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Abstract
This invention relates to Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof.
Claims15
A compound of formula I
- wherein
- X is NH;
- R1 is (C1-C6)-alkyl;
- R2, is OH;
- R2′ is H;
- R3, R3′, R4, R4′, R5, R5′, are, independently of one another, H, Cl, Br, I, OH, —(CH2)—OH, CF3, NO2, N3, CN, S(O)p—R6, O—S(O)p—R6, (C1-C6)-alkylene-S(O)p—R6, (C1-C6)-alkylene-O —S(O)p—R6, COOH, COO(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, (C1-C6)-alkyl, (C2-C6)alkenyl, (C2-C6)-alkynyl, O—(C1-C6)-alkyl, where one, more than one, or all hydrogen(s) in the alkyl radicals may be replaced by fluorine;
- phenyl, —(CH2)-phenyl, —(CH2)2-phenyl, O-phenyl, O—(CH2)m-phenyl, —(CH2)—O—(CH2)m-phenyl, where the phenyl ring may be substituted one 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;
- wherein at least one of the radicals R3, R3′, R4, R4′, R5, R5′ has the meaning of (C1-C6)-alkylene-O —S(O)p—R6 and another has the meaning of —O—(CH2)m-phenyl, where the phenyl ring may be substituted one 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;
- R6 is H, OH, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)2;
- n is 2, 3, 4, 5 or 6;
- m is 1, 2, 3, 4, 5 or 6;
- P is 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof.
10 more elements
A compound of the formula
- or a pharmaceutically acceptable salt thereof.
A compound of the formula
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.