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US 8,946,204 B2Granted
Substituted phenylureas and phenylamides as vanilloid receptor ligands
AssigneeGruenenthal GmbH
InventorsRobert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Nils Damann, Sven Frormann, Bernhard Lesch, Derek John Saunders, Jeewoo Lee, Yong-Soo Kim, Myeong-Seop Kim, Hannelore Stockhausen
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Abstract
Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.
Claims19
A compound corresponding to formula (R)
- wherein
- R101, R102 and R103 are each independently selected from the group consisting of H, F, Cl, Br, CFH2, CF2H, CF3, CN, CH2—OH, CH2CH2—OH, CH2—OCH3, CH2CH2—OCH3, OCFH2, OCF2H, OCF3, OH, NH2, a C1-4 alkyl, an O—C1-4 alkyl, a NH—C1-4 alkyl, and a N(C1-4 alkyl)2, wherein the C1-4 alkyl is in each case unsubstituted;
- R2 represents CF3, an unsubstituted C1-4 alkyl or an unsubstituted C3-6 cycloalkyl;
- R7 and R9 are each independently selected from the group consisting of H, F, Cl, Br, CFH2, CF2H, CF3, CN, OH, OCF3, a C1-4 alkyl, and an O—C1-4 alkyl, wherein the C1-4 alkyl is in each case unsubstituted;
- A denotes N, CH or C(CH3);
- q denotes 0, 1 or 2;
- R112 represents H or a C1-4 alkyl, which is unsubstituted or mono-, di- or trisubstituted with 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, OH, ═O and OCH3;
- R113 represents a H, S(═O)2—NH2, a C1-4 alkyl or a S(═O)2—C1-4 alkyl, wherein the C1-4 alkyl is in each case unsubstituted or mono-, di- or trisubstituted with 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, OH, ═O and OCH3;
- or, if q is not 0, then
- R112 and R113 together with the nitrogen atom connecting them form a 3 to 6 membered heterocyclyl, which is unsubstituted or mono-, di- or trisubstituted with 1, 2 or 3 substituents independently selected from the group consisting of F, Cl, Br, CN, CF3, CH3, CH2CH3, CH(CH3)2, tert.-butyl, cyclopropyl, OH, ═O, OCH3, OCF3, NH2, NH(CH3) and N(CH3)2;
- in the form of a free compound or a physiologically acceptable salt thereof, and if applicable, in the form of an individual stereoisomer or a mixture of stereoisomers.
8 more elements
Dependencies are inferred from the claim text.