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US 2007/0191353 A1Published application
Use of thiadiazoleurea derivatives
OwnerLars Burgdorf, Frank Stieber +7inventors
InventorsLars Burgdorf, Frank Stieber, Hans-Peter Buchstaller, Soheila Anzali, Christiane Amendt, Hartmut Greiner, Matthias Grell, Christian Sirrenberg, Frank Zenke
Life of this patent
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Abstract
Use of compounds of the formula (I), in which Ar1, Ar2 and Z have the meanings indicated in Patent Claim 1, for the prophylaxis and/or treatment of diseases in which the inhibition, regulation and/or modulation of signal transduction by kinases, in particular RAF kinases, plays a role.
Claims15
Use of one or more of the compounds of the formula I
- in which
- Ar1 denotes phenyl, naphthyl, biphenyl or Het, each of which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by R1,
- Ar2 denotes phenyl, naphthyl, biphenyl or Het, each of which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by R2,
- Y denotes O, S, CH—NO2, C(CN)2 or N—R4,
- Z denotes —O—, —S—, —CH2—(CH2)n—, —(CH2)n—CHA-, —CHA-(CH2)n—, —C(═O)—, —CH(OH)—, —(CHA)nO—, —(CH2)nO—, —O(CHA)n-, —O(CH2)n—, —(CH2)nS—, —S(CH2)n—, —(CH2)nNH—, —NH(CH2)n—, —(CH2)nNA-, —NA(CH2)n—, —CHHal- or —C(Hal)2-,
- Het denotes a mono- or bicyclic aromatic heterocycle having 1 to 4 N, O and/or S atoms,
- R1, R2, independently of one another, denote A, Ar′, OR3, SR3, OAr′, SAr′, N(R3)2, NHAr′, Hal, NO2, CN, (CH2)nCOOR3, (CH2)nCON(R3)n, COR3, S(O)mA, S(O)mAr′, NHCOA, NHCOAr′, NHSOmA, NHSOOmAr′, SOmN(R3)2, —O—(CH2)n—N(R3)2, O(CH2)nNHR3, O(CH2)nNA2, O(CH2)nC(CH3)2(CH2)nN(R3)2, NH(CH2)n(CH3)2(CH2)nN(R3)2, O(CH2)nN(R3)SOmA, O(CH2)nN(R3)SOmN(R3)A, O(CH2)nN(R3)SOmAr′, (CH2)nN(R3)SOmA, (CH2)nN(R3)SOmN(R3)A, (CH2)nN(R3)SOmAr′, O(CH2)nSOmA, O(CH2)nSOmN(R3)A, O(CH2)nSOmAr′, (CH2)nSOmA, (CH2)nSOmN(R3)A, (CH2)nSOmAr′, —NH—(CH2)n—NH2, —NH—(CH2)n—NHA, —NH—(CH2)n—NA2, —NA-(CH2)n—NH2, —NA-(CH2)n—NHA, —NA-(CH2)n—NA2, —O—(CH2)n-Het1 or Het1,
- R3 denotes H, A or (CH2)nAr′,
- R4 denotes H, CN, OH, A, (CH2)mAr′, COR3, COAr′, S(O)mA or S(O)mAr′,
- Ar′ denotes phenyl which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by A, Ph, OH, OA, SH, SA, OPh, SPh, NH2, NHA, NA2, NHPh, Hal, NO2, CN, (CH2)nCOOH, (CH2)nCOOA, (CH2)nCONH2, (CH2)nCONHA, CHO, COA, S(O)mA, S(O)mPh, NHCOA, NHCOPh, NHSO2A, NHSO2Ph or SO2NH2,
- Ph denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by A, Hal, CN, COOR, COOH, NH2, NO2, OH or OA,
- Het1 denotes a monocyclic saturated heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NH2, ═NH, ═N—OH, ═N—OA and/or carbonyl oxygen (═O),
- A denotes alkyl having 1 to 10 C atoms, where 1-7 H atoms may also be replaced by F and/or chlorine,
- Hal denotes F, Cl, Br or I,
- n denotes 0, 1, 2, 3, 4 or 5,
- m denotes 0, 1 or 2,
- and pharmaceutically usable derivatives, solvates, salts and stereoisomers thereof, including mixtures thereof in all ratios, for the preparation of a medicament for the prophylaxis and/or treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role.
14 more elements
Compounds general formula VI
- in which
- Ar1 denotes phenyl which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by R1,
- Ar2 denotes phenyl or Het, each of which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by R2,
- Y denotes O,
- Z denotes —O—, —CH2—(CH2)n—, —(CH2)n—CHA-, —CHA-(CH2)n—, —C(═O)—, —CH(OH)—, —CH(OA)-, —(CH2)nO—, —O(CH2)n—, —(CH2)nNH— or —NH(CH2)n—,
- Het denotes a mono- or bicyclic aromatic heterocycle having 1 to 4 N, O and/or S atoms,
- R1, R2, independently of one another, denote A, OR3, Hal, NO2, CN, S(O)mA, O(CH2)nNA2 or Het1,
- R3 denotes H or A,
- Het1 denotes a monocyclic saturated heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NH2, ═NH, ═N—OH, ═N—OA and/or carbonyl oxygen (═O),
- A denotes alkyl having 1 to 10 C atoms, where 1-7 H atoms may also be replaced by F and/or chlorine,
- Hal denotes F, Cl, Br or I,
- n denotes 0, 1, or 2,
- m denotes 0, 1 or 2,
- and pharmaceutically usable derivatives, solvates, salts and stereoisomers thereof, including mixtures thereof in all ratios.
11 more elements
Set (kit) consisting of separate packs of
- a) an effective amount of a compound of the formula I and/or pharmaceutically usable derivatives, solvates and stereoisomers thereof, including mixtures thereof in all ratios,
- and
- b) an effective amount of a further medicament active ingredient.
Dependencies are inferred from the claim text.