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    • 1. 发明申请
    • PYRAZOLO [4, 3-D]PYRIMIDINES, PROCESSES FOR THEIR PREPARATION AND METHODS OF USE
    • 吡咯并[4,3-D]吡啶,其制备方法和使用方法
    • WO2004098608A1
    • 2004-11-18
    • PCT/EP2004/004855
    • 2004-05-06
    • ÚSTAV EXPERIMENTALNI BOTANIKY AKADEMIE VED CESKE REPUBLIKYMORAVCOVÁ, DanielaHAVLICEK, LiborKRYSTOF, VladimirLENOBEL, RenéBINAROVÁ, PavlaMLEJNEK, PetrVOJTESEK, BorekULDRIJAN, StjepanSCHMÜLLING, ThomasSTRNAD, Miroslav
    • MORAVCOVÁ, DanielaHAVLICEK, LiborKRYSTOF, VladimirLENOBEL, RenéBINAROVÁ, PavlaMLEJNEK, PetrVOJTESEK, BorekULDRIJAN, StjepanSCHMÜLLING, ThomasSTRNAD, Miroslav
    • A61K31/505
    • C07D487/04
    • The invention relates to 3-, 7-disubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I (I), and pharmaceutically acceptable salts thereof, wherein R3 is selected from the group consisting of alkyl, cycloalkyl, , cycloalkyl alkyl, cycloheteroalkyl alkyl, cycloheteroalkyl, aryl, heterocycle, heteroaryl, arylalkyl, heteroarylalkyl, and heteroalkyl, wherein each of the groups may optionally be substituted, R7 is selected from the group consisting of halogen, hydroxyl, hydroxylamino, amino, carboxyl, cyano, nitro, amido, sulfo, sulfamido, carbamino, unsubstituted or substituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroarylakyl, substituted or unsubstituted cycloalkyl alkyl, substituted or unsubstituted cycloheteroalkyl alkyl; R7'-X- wherein X is an -NH-, -N(alkyl)-, -0- or -S- moiety and R7' is selected from the group consisting of H, alkyl, cycloalkyl, aryl, alkylcycloalkyl, arylalkyl, heterocycle, heterocyclealkyl, substituted alkyl, substituted cycloalkyl, substituted aryl, substituted arylalkyl, substituted heterocycle, substituted heteroaryl, substituted heteroarylalkyl, substituted heteroalkyl, substituted cycloalkyl alkyl and substituted cycloheteroalkyl alkyl, wherein the groups are preferably substituted by more than one halogen, hydroxyl, amino, mercapto, carboxyl, cyano, nitro, amido, sulfo, sulfamido, carbamino, alkyl, alkoxy, and substituted alkyl group.
    • 本发明涉及由通式I(I)表示的3-,7-二取代的吡唑并[4,3-d]嘧啶及其药学上可接受的盐,其中R 3选自烷基,环烷基,环烷基 烷基,环杂烷基烷基,环杂烷基,芳基,杂环,杂芳基,芳基烷基,杂芳基烷基和杂烷基,其中每个基团可任选被取代,R 7选自卤素,羟基,羟基氨基,氨基,羧基,氰基, 取代或未取代的芳烷基,取代或未取代的杂烷基,取代或未取代的杂芳基烷基,取代或未取代的环烷基烷基,取代或未取代的环杂烷基烷基;取代或未取代的芳基烷基, 其中X是-NH-,-N(烷基) - , - O-或-S-部分,并且R 7'选自H,烷基,环烷基,芳基,烷基环烷基,芳基烷基, 杂环,杂环烷基,取代的烷基,取代的环烷基,取代的芳基,取代的芳基烷基,取代的杂环,取代的杂芳基,取代的杂芳基烷基,取代的杂烷基,取代的环烷基烷基和取代的环杂烷基烷基,其中基团优选被多于一个的卤素,羟基, 氨基,巯基,羧基,氰基,硝基,酰胺基,磺基,氨基磺酰氨基,氨基氨基,烷基,烷氧基和取代的烷基。
    • 5. 发明申请
    • NOVEL PYRAZOLO[4,3-D]PYRIMIDINES, PROCESSES FOR THEIR PREPARATION AND METHODS FOR THERAPY
    • 新型吡咯并[4,3-D]吡嗪类,其制备方法和治疗方法
    • WO2003082872A1
    • 2003-10-09
    • PCT/EP2003/003207
    • 2003-03-27
    • USTAV EXPERIMENTALNI BOTANIKY AV CR (INSTITUTE OF EXPERIMENTAL BOTANY ACADEMY OF SCIENCES OF THE CZECH REPUBLIC)MORAVCOVÁ, DanielaHAVLICEK, LiborKRYSTOF, VladimirLENOBEL, RenéSTRNAD, Miroslav
    • MORAVCOVÁ, DanielaHAVLICEK, LiborKRYSTOF, VladimirLENOBEL, RenéSTRNAD, Miroslav
    • C07D487/04
    • C07D487/04
    • The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula (I), and pharmaceutically acceptable salts thereof, wherein, R3 is an optionally substituted alkyl, cycloalkyl, cycloheteroalkyl, cycloalkyl alkyl, aryl or alkylaryl group; R5 is halogen, -NHNH 2 , -NHOH, NHCONH 2 , guanylo (NH-C(NH)NH 2 ) an optionally substituted C 1 -C 6 alkyl, alkenyl, alkinyl, C 3 -C 15 cycloalkyl, R f (C 3 -C 15 cycloalkyl), heterocycle, heteroalkyl, aryl, heteroaryl, arylalkyl, cycloheteroalkyl, cycloheteroalkyl alkyl, heteroarylalkyl group, the group -C(O)-R a , -C(O)NR b R c - SO 3 R d , or -NHC(O)R e , wherein R a and R f are an optionally substituted C 1 -C 6 alkyl, alkenyl, or alkinyl group, R b , R c and R d are independently selected from the group consisting of H, optionally substituted C 1 -C 6 alkyl, alkenyl, or alkinyl group, and R e is a hydroxy, amino, alkoxy, alkylamino, optionally substituted C 1 -C 6 alkyl, alkenyl or alkinyl group; or the group -X-R 5' , wherein X is -NH-, -O-, -S- or -N(alkyl)- and R 5' is hydrogen, an optionally substituted C 1 -C 6 alkyl, alkenyl, alkinyl, C 3 -C 15 cycloalkyl, Rf(C 3 -C 15 cycloalkyl), aryl, heterocycle, hetero C 1 -C 6 alkyl, arylalkyl, heteroaryl, cycloheteroalkyl, cycloheteroalkyl alkyl, or heteroarylalkyl group, the group -C(O)-R a , -C(O)NR b R c , -SO 3 R d , or -NHC(O)R e , wherein R a , R b , R c , R d , R e and R f have the above meaning, and R7 is halogen, -NHNH 2 , NHOH, NHCONH 2 , guanylo (NH-C(NH)NH 2 ) or the group -X-R 7 , wherein X has the above meaning and the meaning of R 7 , is as defined for R 5' .
    • 本发明涉及由通式(I)表示的3-,5-,7-三取代的吡唑并[4,3-d]嘧啶及其药学上可接受的盐,其中R 3是任选取代的烷基,环烷基,环杂烷基, 环烷基烷基,芳基或烷基芳基; R5是卤素,-NHNH2,-NHOH,NHCONH2,胍基(NH-C(NH)NH2),任意取代的C1-C6烷基,烯基,炔基,C3-C15环烷基,Rf(C3-C15环烷基),杂环, ,芳基,杂芳基,芳基烷基,环杂烷基,环杂烷基烷基,杂芳基烷基,基团-C(O)-Ra,-C(O)NRbRc-SO3Rd或-NHC(O)Re,其中Ra和Rf是任选取代的 C 1 -C 6烷基,烯基或炔基,R b,R c和R d独立地选自H,任选取代的C 1 -C 6烷基,烯基或炔基,Re是羟基,氨基,烷氧基,烷基氨基 ,任选取代的C 1 -C 6烷基,烯基或炔基; 或基团-X-R5',其中X是-NH-,-O - , - S-或-N(烷基) - ,并且R 5'是氢,任选取代的C 1 -C 6烷基,烯基,炔基, C 15环烷基,R f(C 3 -C 15环烷基),芳基,杂环,杂C 1 -C 6烷基,芳烷基,杂芳基,环杂烷基,环杂烷基烷基或杂芳基烷基,基团-C(O)-R a,-C(O)NR b R c ,-SO 3 R d或-NHC(O)R e,其中R a,R b,R c,R d,R e和R f具有上述含义,并且R 7是卤素,-NHNH 2,NHOH,NHCONH 2,胍基(NH-C(NH) )或-X-R7基团,其中X具有上述含义并且R7的含义如R5'所定义。