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    • 2. 发明申请
    • NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS
    • 新型环状尿素衍生物及其制备方法和作为激酶抑制剂的药物用途
    • WO2006010641A3
    • 2006-10-26
    • PCT/EP2005008720
    • 2005-07-25
    • AVENTIS PHARMA SASTROBEL HARTMUTRUF SVENLESUISSE DOMINIQUENEMECEK CONCEPTIONEL-AHMAD YOUSSEFGUESSREGEN STEFANLEBRUN ANNERITTER KURTBENARD DIDIERHITTINGER AUGUSTINBOUCHARD HERVE
    • STROBEL HARTMUTRUF SVENLESUISSE DOMINIQUENEMECEK CONCEPTIONEL-AHMAD YOUSSEFGUESSREGEN STEFANLEBRUN ANNERITTER KURTBENARD DIDIERHITTINGER AUGUSTINBOUCHARD HERVE
    • C07D401/06A61K31/4166C07D401/14
    • C07D403/04
    • The invention relates to products of formula (I): in which p = 0, 1 and 2; A = aryl, heteroaryl, carbocycle or heterocycle; X = single bond; -N(R6)-; -NH-alk-; alkylene; -O-; -C(O)-; -S(O)n-; -N(R6)-C(O)-; -NH-CO-alk-, -N(R6)-C(O)-N(R6')-; -N(R6)-C(S)-N(R6')-; -N(R6)-C(O)O-; -N(R6)-SO2-; -N(R6)-SO2-N(R6')-; -C(O)-N(R6)-; -SO2-NR6-; and -C(O)O-; L1 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene; all optionally substituted; R1 = hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; -SO2R9, -C(O)R9; -C(O)OR9,-C(O)NR10R11, -C(S)NR10R11,-SO2NR10R11; R2 = hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, either R1 and R2 with N, or NR1R2 with L1 may form a saturated or unsaturated heterocycle possibly containing O, N, S; R3 = hydrogen; halogen; alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylenedioxy, heterocycle, aryl and heteroaryl, all optionally substituted; S(O)n-alkyl; amino, alkylamino, dialkylamino, with dialkylamino optionally forming with N a cycle, all optionally substituted; R4, R4' and R4''= hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, oxo; with two from among R4, R4' and R4'' possibly forming with C a ring possibly containing O, N or S; L2 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, -O-, -NR17-, -C(O)-, SO2; Y = N-heterocycle possibly containing O, N or S; R5 = hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
    • 本发明涉及式(I)的产物:其中p = 0,1和2; A =芳基,杂芳基,碳环或杂环; X =单键; -N(R 6) - ; -NH-烷 - ; 亚; -O-; -C(O) - ; -儿子-; -N(R 6)-C(O) - ; -NH-CO-alk-,-N(R 6)-C(O)-N(R 6') - ; -N(R6)-C(S)-N(R6' ) - ; -N(R 6)-C(O)O-; -N(R 6)-SO 2 - ; -N(R6)-SO2-N(R6' ) - ; -C(O)-N(R6) - ; -SO 2 NR 6 - ; 和-C(O)O-; L1 =单键,亚烷基,亚烯基,亚炔基,亚环烷基,亚苯基,亚杂芳基; 全部任选被取代; R1 =氢,烷基,烯基,炔基或环烷基,芳基,杂芳基,芳基烷基,杂芳基烷基; -SO 2 R 9,-C(O)R 9; -C(O)OR 9,-C(O)NR 10 R 11,-C(S)NR 10 R 11,-SO 2 NR 10 R 11; R 2 =氢,烷基,烯基,炔基,环烷基,R 1和R 2与N或NR 1 R 2与L 1可以形成可能含有O,N,S的饱和或不饱和杂环; R3 =氢; 卤素; 烷基,烯基,炔基,环烷基,烷氧基,亚烷基二氧基,杂环,芳基和杂芳基,全部任选被取代; S(O)n-烷基; 氨基,烷基氨基,二烷基氨基,任选与N环形成的二烷基氨基,全部任选被取代; R4,R4'和R4“=氢,卤素,烷基,烯基,炔基,环烷基,芳基,杂芳基,氧代; 其中R4,R4'和R4“中的两个可能与C形成可能含有O,N或S的环; L2 =单键,亚烷基,亚烯基,亚炔基,亚环烷基,-O - , - NR17-,-C(O) - ,SO2; Y =可能含有O,N或S的N-杂环; R5 =氢,卤素,烷基,烯基,炔基,环烷基,芳基,芳基烷基,杂芳基,杂芳基烷基; 所有这些基团任选地被取代,这些产物以所有异构形式和盐作为医药产品。
    • 3. 发明申请
    • NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS
    • 新型循环尿素衍生物,其制备方法及其作为激酶抑制剂的药物用途
    • WO2006010641A2
    • 2006-02-02
    • PCT/EP2005/008720
    • 2005-07-25
    • AVENTIS PHARMA S.A.STROBEL, HartmutRUF, SvenLESUISSE, DominiqueNEMECEK, ConceptionEL-AHMAD, YoussefGUESSREGEN, StefanLEBRUN, AnneRITTER, KurtBENARD, DidierHITTINGER, AugustinBOUCHARD, Hervé
    • STROBEL, HartmutRUF, SvenLESUISSE, DominiqueNEMECEK, ConceptionEL-AHMAD, YoussefGUESSREGEN, StefanLEBRUN, AnneRITTER, KurtBENARD, DidierHITTINGER, AugustinBOUCHARD, Hervé
    • C07D401/06C07D401/14
    • C07D403/04
    • The invention relates to products of formula (I): in which p = 0, 1 and 2; A = aryl, heteroaryl, carbocycle or heterocycle; X = single bond; -N(R6)-; -NH-alk-; alkylene; -O-; -C(O)-; -S(O)n-; -N(R6)-C(O)-; -NH-CO-alk-, -N(R6)-C(O)-N(R6')-; -N(R6)-C(S)-N(R6')-; -N(R6)-C(O)O-; -N(R6)-SO2-; -N(R6)-SO2-N(R6')-; -C(O)-N(R6)-; -SO2-NR6-; and -C(O)O-; L1 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene; all optionally substituted; R1 = hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; -SO2R9, -C(O)R9; -C(O)OR9,-C(O)NR10R11, -C(S)NR10R11,-SO2NR10R11; R2 = hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, either R1 and R2 with N, or NR1R2 with L1 may form a saturated or unsaturated heterocycle possibly containing O, N, S; R3 = hydrogen; halogen; alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylenedioxy, heterocycle, aryl and heteroaryl, all optionally substituted; S(O)n-alkyl; amino, alkylamino, dialkylamino, with dialkylamino optionally forming with N a cycle, all optionally substituted; R4, R4' and R4''= hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, oxo; with two from among R4, R4' and R4'' possibly forming with C a ring possibly containing O, N or S; L2 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, -O-, -NR17-, -C(O)-, SO2; Y = N-heterocycle possibly containing O, N or S; R5 = hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
    • 本发明涉及式(I)的产物:其中p = 0,1和2; A =芳基,杂芳基,碳环或杂环; X =单键; -N(R 6) - ; -NH-烷 - ; 亚; -O-; -C(O) - ; -儿子-; -N(R 6)-C(O) - ; -NH-CO-烷基,-N(R 6)-C(O)-N(R 6') - ; -N(R6)-C(S)-N(R6' ) - ; -N(R 6)-C(O)O-; -N(R 6)-SO 2 - ; -N(R6)-SO2-N(R6' ) - ; -C(O)-N(R6) - ; -SO 2 NR 6 - ; 和-C(O)O-; L1 =单键,亚烷基,亚烯基,亚炔基,亚环烷基,亚苯基,亚杂芳基; 全部任意取代; R 1 =氢,烷基,烯基,炔基或环烷基,芳基,杂芳基,芳基烷基,杂芳基烷基; -SO 2 R 9,-C(O)R 9; -C(O)OR 9,-C(O)NR 10 R 11,-C(S)NR 10 R 11,-SO 2 NR 10 R 11; R 2 =氢,烷基,烯基,炔基,环烷基,R 1和R 2与N或NR 1 R 2与L 1可以形成可能含有O,N,S的饱和或不饱和杂环; R3 =氢; 卤素; 烷基,烯基,炔基,环烷基,烷氧基,亚烷基二氧基,杂环,芳基和杂芳基,全部被取代; S(O)n-烷基; 氨基,烷基氨基,二烷基氨基,二烷基氨基,任选地以N a个周期形成,全部任选被取代; R 4,R 4'和R 4“=氢,卤素,烷基,烯基,炔基,环烷基,芳基,杂芳基,氧代; 其中R4,R4和R4之间的两个可能形成可能含有O,N或S的C环; L2 =单键,亚烷基,亚烯基,亚炔基,亚环烷基,-O-,-NR17-,-C(O) - ,SO2; Y =可能含有O,N或S的N-杂环; R5 =氢,卤素,烷基,烯基,炔基,环烷基,芳基,芳基烷基,杂芳基,杂芳基烷基; 所有这些基团任选被取代,这些产物是所有异构体形式和盐,作为药用产品。