SULPHUR-CONTAINING CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS

L'invention concerne les nouveaux produits de formule (I) : dans laquelle n représente 0 ou 2; R représente pyridyle ou pyrimidinyle substitués par un radical NR1R2, avec l'un de R1 et R2 représente hydrogène ou alkyle, et l'autre de R1 et R2 représente hydrogène ou alkyle éventuellem...

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Hauptverfasser: STROBEL, HARTMUT, RUF, SVEN, RITTER, KURT, HALLEY, FRANK, DAGALLIER, ANNE, CERTAL, VICTOR, VENOT, CORINNE, EL-AHMAD, YOUSSEF
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creator STROBEL, HARTMUT
RUF, SVEN
RITTER, KURT
HALLEY, FRANK
DAGALLIER, ANNE
CERTAL, VICTOR
VENOT, CORINNE
EL-AHMAD, YOUSSEF
description L'invention concerne les nouveaux produits de formule (I) : dans laquelle n représente 0 ou 2; R représente pyridyle ou pyrimidinyle substitués par un radical NR1R2, avec l'un de R1 et R2 représente hydrogène ou alkyle, et l'autre de R1 et R2 représente hydrogène ou alkyle éventuellement substitué, cycloalkyle, hétérocycloalkyle, phényle, pyrimidinyle, pyridyle, et CO-R3 av ec R3 choisi notamment parmi les radicaux aminés, alcoxy, hétérocycloalkyle, aryle, aryloxy et hétéroaryle; tous ces radicaux étant éventuellement substitués; et leurs sels. Cyclic urea compounds (I) are new. Cyclic urea compounds of formula (I) and their racemic, enantiomers, diastereoisomers and addition salts of bases or mineral/organic acids are new. Ra1, Rb1 = methyl; or CRa1Rb1 = cycloalkyl; R = pyridyl (preferred) or pyrimidinyl (both substituted by NR1R2); one of R1, R2 = H or alkyl and the other = T; T = H or alkyl (optionally substituted by OH, alkoxy, aziridyl, azetidinyl, pyrrolidinyl, piperidyl, morpholinyl or piperazinyl (optionally 4-alkylated)), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted)) or C(O)R3; R3 = alkoxy, heterocycloalkyl, aryloxy, (heter)oaryl (all optionally substituted) or NR4R5 (preferred); either one of R4, R5 = H or alkyl and the other = T; or NR4R5 = heterocycle (optionally including another heteroatom like N or O and/or optionally substituted); aryl, phenyl, aryloxy, heteroaryl or the heterocycle NR4R5 may be substituted by 1-3 halo, alkyl, phenyl, NH 2, NHAlk, NR(Alk) 2, C(O)NHAlk or C(O)N(Alk) 2; and n = 0 or 2. [Image] ACTIVITY : Cytostatic; Metabolic; Antiallergic; Antiasthmatic; Prevention: Anticoagulant / Treatment: Thrombolytic; Neuroprotective; Ophthalmological; Antipsoriatic; Antiarthritic; Antirheumatic; Antidiabetic; Muscular-Gen. MECHANISM OF ACTION : Tyrosine protein kinase inhibitor; Insulin like growth factor-1 receptor kinase inhibitor.
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Cyclic urea compounds (I) are new. Cyclic urea compounds of formula (I) and their racemic, enantiomers, diastereoisomers and addition salts of bases or mineral/organic acids are new. Ra1, Rb1 = methyl; or CRa1Rb1 = cycloalkyl; R = pyridyl (preferred) or pyrimidinyl (both substituted by NR1R2); one of R1, R2 = H or alkyl and the other = T; T = H or alkyl (optionally substituted by OH, alkoxy, aziridyl, azetidinyl, pyrrolidinyl, piperidyl, morpholinyl or piperazinyl (optionally 4-alkylated)), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted)) or C(O)R3; R3 = alkoxy, heterocycloalkyl, aryloxy, (heter)oaryl (all optionally substituted) or NR4R5 (preferred); either one of R4, R5 = H or alkyl and the other = T; or NR4R5 = heterocycle (optionally including another heteroatom like N or O and/or optionally substituted); aryl, phenyl, aryloxy, heteroaryl or the heterocycle NR4R5 may be substituted by 1-3 halo, alkyl, phenyl, NH 2, NHAlk, NR(Alk) 2, C(O)NHAlk or C(O)N(Alk) 2; and n = 0 or 2. [Image] ACTIVITY : Cytostatic; Metabolic; Antiallergic; Antiasthmatic; Prevention: Anticoagulant / Treatment: Thrombolytic; Neuroprotective; Ophthalmological; Antipsoriatic; Antiarthritic; Antirheumatic; Antidiabetic; Muscular-Gen. 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Cyclic urea compounds (I) are new. Cyclic urea compounds of formula (I) and their racemic, enantiomers, diastereoisomers and addition salts of bases or mineral/organic acids are new. Ra1, Rb1 = methyl; or CRa1Rb1 = cycloalkyl; R = pyridyl (preferred) or pyrimidinyl (both substituted by NR1R2); one of R1, R2 = H or alkyl and the other = T; T = H or alkyl (optionally substituted by OH, alkoxy, aziridyl, azetidinyl, pyrrolidinyl, piperidyl, morpholinyl or piperazinyl (optionally 4-alkylated)), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted)) or C(O)R3; R3 = alkoxy, heterocycloalkyl, aryloxy, (heter)oaryl (all optionally substituted) or NR4R5 (preferred); either one of R4, R5 = H or alkyl and the other = T; or NR4R5 = heterocycle (optionally including another heteroatom like N or O and/or optionally substituted); aryl, phenyl, aryloxy, heteroaryl or the heterocycle NR4R5 may be substituted by 1-3 halo, alkyl, phenyl, NH 2, NHAlk, NR(Alk) 2, C(O)NHAlk or C(O)N(Alk) 2; and n = 0 or 2. [Image] ACTIVITY : Cytostatic; Metabolic; Antiallergic; Antiasthmatic; Prevention: Anticoagulant / Treatment: Thrombolytic; Neuroprotective; Ophthalmological; Antipsoriatic; Antiarthritic; Antirheumatic; Antidiabetic; Muscular-Gen. 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Cyclic urea compounds (I) are new. Cyclic urea compounds of formula (I) and their racemic, enantiomers, diastereoisomers and addition salts of bases or mineral/organic acids are new. Ra1, Rb1 = methyl; or CRa1Rb1 = cycloalkyl; R = pyridyl (preferred) or pyrimidinyl (both substituted by NR1R2); one of R1, R2 = H or alkyl and the other = T; T = H or alkyl (optionally substituted by OH, alkoxy, aziridyl, azetidinyl, pyrrolidinyl, piperidyl, morpholinyl or piperazinyl (optionally 4-alkylated)), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted)) or C(O)R3; R3 = alkoxy, heterocycloalkyl, aryloxy, (heter)oaryl (all optionally substituted) or NR4R5 (preferred); either one of R4, R5 = H or alkyl and the other = T; or NR4R5 = heterocycle (optionally including another heteroatom like N or O and/or optionally substituted); aryl, phenyl, aryloxy, heteroaryl or the heterocycle NR4R5 may be substituted by 1-3 halo, alkyl, phenyl, NH 2, NHAlk, NR(Alk) 2, C(O)NHAlk or C(O)N(Alk) 2; and n = 0 or 2. [Image] ACTIVITY : Cytostatic; Metabolic; Antiallergic; Antiasthmatic; Prevention: Anticoagulant / Treatment: Thrombolytic; Neuroprotective; Ophthalmological; Antipsoriatic; Antiarthritic; Antirheumatic; Antidiabetic; Muscular-Gen. MECHANISM OF ACTION : Tyrosine protein kinase inhibitor; Insulin like growth factor-1 receptor kinase inhibitor.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
title SULPHUR-CONTAINING CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS
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