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1. 发明申请

WO2007110344A1 PYRIDYL- AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE- AND FURANE-DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的吡啶并吡啶并吡啶并 - 吡咯并 - 呋喃衍生物
公开(公告)号：WO2007110344A1
公开(公告)日：2007-10-04
申请号：PCT/EP2007/052587
申请日：2007-03-19
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , VANOTTI, Ermes , CALDARELLI, Marina , CIRLA, Alessandra , FORTE, Barbara , ERMOLI, Antonella , MENICHINCHERI, Maria , PILLAN, Antonio , SCOLARO, Alessandra
发明人： VANOTTI, Ermes , CALDARELLI, Marina , CIRLA, Alessandra , FORTE, Barbara , ERMOLI, Antonella , MENICHINCHERI, Maria , PILLAN, Antonio , SCOLARO, Alessandra
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , A61K31/435 , A61K31/495 , A61P35/00
CPC分类号： C07D409/14 , A61K31/4439 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/06 , A61N5/10 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04
摘要： The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中G，W，R 2，R 3，R 4， R 5和R 6如本说明书中所定义。本发明的另外的目的是制备式（I）化合物，包含它们的药物组合物和治疗细胞增殖性疾病的方法的方法和中间体。事实上，式（I）化合物在治疗中可用于治疗与蛋白激酶活性失调相关的疾病，如癌症。

2. 发明申请

WO1990003970A1 N-IMIDAZOLYL- AND N-IMIDAZOLYLMETHYL-DERIVATIVES OF SUBSTITUTED BICYCLIC COMPOUNDS 审中-公开
标题翻译：取代的双环化合物的N-咪唑并 - 和N-咪唑烷基甲基衍生物
公开(公告)号：WO1990003970A1
公开(公告)日：1990-04-19
申请号：PCT/EP1989001159
申请日：1989-10-03
申请人： FARMITALIA CARLO ERBA S.R.L. , CARGANICO, Germano , COZZI, Paolo , PILLAN, Antonio , SALVATI, Patricia , FERTI, Corrado
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D233/56
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention relates to new N-imidazolyl and N-imidazolylmethyl derivatives of bicyclic compounds having general formula (I), wherein A is an alpha or beta group, in which R3 is hydrogen or C1-C6 alkyl, or a psi group, in which each of R4 and R5 independently is hydrogen or C1-C5 alkyl; Z is -CH2-, -O- or -S-; n is zero or 1; each of R and R1 is independently hydrogen or C1-C6 alkyl; R2 is -COCH2OH, -CH2OR', -COOR', -CONR'R'' or -CH=CH-COOR', in which each of R' and R'' independently is hydrogen or C1-C6 alkyl, and the pharmaceutically acceptable salts thereof; and wherein: a) when n is zero, then Z is -CH2- or -O-; whereas when n is one, then Z is -CH2-, -O- or -S-; b) when A is alpha or beta in which R3 is hydrogen, then n is one; and c) when, at the same time, A is beta in which R3 is hydrogen, Z is -CH2-, n is one and R2 is -COOR' wherein R' is as defined above, then at least one of R and R1 is other than hydrogen, which are useful in the treatment of diseases related to an enhancement of TxA2 synthesis.
摘要翻译：本发明涉及具有通式（I）的双环化合物的新的N-咪唑基和N-咪唑基甲基衍生物，其中A是α或β基团，其中R3是氢或C1-C6烷基或psi基团，其中R4和R5各自独立地为氢或C1-C5烷基; Z是-CH 2 - ， - O-或-S-; n为零或1; R和R 1各自独立地为氢或C 1 -C 6烷基; R 2是-COCH 2 OH，-CH 2 OR'，-COOR'，-CONR'R“或-CH = CH-COOR'，其中R'和R”各自独立地是氢或C 1 -C 6烷基，可接受的盐; 并且其中：a）当n为0时，Z为-CH 2 - 或-O-; 而当n为1时，则Z为-CH 2 - ， - O-或-S-; b）当A是其中R 3是氢时的α或β，则n是1; 和c）当同时A为β，其中R 3为氢时，Z为-CH 2 - ，n为1，R 2为-COOR'，其中R'如上定义，则R和R 1中的至少一个不同于氢，其可用于治疗与增强TxA2合成相关的疾病。

3. 发明申请

WO2005014572A8 PYRIMIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的吡咯烷酮衍生物
公开(公告)号：WO2005014572A8
公开(公告)日：2006-03-09
申请号：PCT/EP2004008853
申请日：2004-08-06
申请人： PHARMACIA ITALIA SPA , VANOTTI ERMES , D ALESSIO ROBERTO , TIBOLLA MARCELLINO , VARASI MARIO , MONTAGNOLI ALESSIA , SANTOCANALE CORRADO , ORSINI PAOLO , PILLAN ANTONIO
发明人： VANOTTI ERMES , D ALESSIO ROBERTO , TIBOLLA MARCELLINO , VARASI MARIO , MONTAGNOLI ALESSIA , SANTOCANALE CORRADO , ORSINI PAOLO , PILLAN ANTONIO
IPC分类号： A61K31/506 , A61K31/513 , A61K31/52 , A61K41/00 , A61K45/06 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/00 , C07D471/04 , C07D519/00 , C07D401/04
CPC分类号： C07D471/04 , A61K31/506 , A61K31/513 , A61K31/52 , A61K41/00 , A61K45/06 , A61K2300/00
摘要： Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
摘要翻译：公开了本说明书中定义的式（1）的嘧啶基吡咯衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

4. 发明申请

WO1992011240A1 PYRIDYL DERIVATIVES OF SUBSTITUTED BICYCLIC COMPOUNDS AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：取代双环化合物的吡啶衍生物及其制备方法
公开(公告)号：WO1992011240A1
公开(公告)日：1992-07-09
申请号：PCT/EP1991002104
申请日：1991-11-07
申请人： FARMITALIA CARLO ERBA S.R.L. , COZZI, Paolo , PILLAN, Antonio , BERTONE, Leone , SALVATI, Patricia
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D213/55
CPC分类号： C07D213/55 , C07D213/56
摘要： The present invention relates to new pyridyl derivatives of bicyclic compounds having general formula (I) wherein the symbol ------ represents a single or double bond; m is an integer of 1 to 3; R is hydrogen or a C1-C6 alkyl group; R1 is a -(CH2)n-COR3 group, wherein n is zero or an integer of 1 to 3 and R3 is an -OR4 or -N(R4R5) group in which each of R4 and R5 independently is hydrogen, C1-C6 alkyl optionally substituted by phenyl or phenyl; or a -(CH2)p-OR4 group wherein p is zero or an integer of 1 to 4 and R4 is as defined above; R2 is hydrogen or C1-C4 alkyl; or a pharmaceutically acceptable salt thereof; and wherein, when at the same time the symbol ------ is a single bond and R1 is a -(CH2)n-COR3 group in which n is as defined above and R3 is an OR4 group wherein R4 is hydrogen or unsubstituted C1-C6 alkyl, then at least one of R and R2 is other than hydrogen, which are useful in the treatment of diseases related to an enhancement of TxA2 synthesis.
摘要翻译：本发明涉及具有通式（I）的双环化合物的新的吡啶基衍生物，其中符号表示单键或双键; m为1〜3的整数。 R是氢或C 1 -C 6烷基; R1是 - （CH2）n-COR3基团，其中n是0或1〜3的整数，R3是-OR4或-N（R4R5）基团，其中R4和R5各自独立地是氢，C1-C6 任选被苯基或苯基取代的烷基; 或 - （CH 2）p-OR 4基团，其中p为0或1至4的整数，并且R 4如上所定义; R2是氢或C1-C4烷基; 或其药学上可接受的盐; 并且其中当符号同时为单键并且R 1为其中n如上述定义的 - （CH 2）n -COR 3基团，且R 3为OR 4基团，其中R 4为氢或未取代的C 1 -C 6烷基，那么R和R 2中的至少一个不是氢，其可用于治疗与增强TxA2合成相关的疾病。

5. 发明申请

WO2005014572A1 PYRIMIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的吡咯烷酮衍生物
公开(公告)号：WO2005014572A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008853
申请日：2004-08-06
申请人： PHARMACIA ITALIA S.P.A. , VANOTTI, Ermes , D'ALESSIO, Roberto , TIBOLLA, Marcellino , VARASI, Mario , MONTAGNOLI, Alessia , SANTOCANALE, Corrado , ORSINI, Paolo , PILLAN, Antonio
发明人： VANOTTI, Ermes , D'ALESSIO, Roberto , TIBOLLA, Marcellino , VARASI, Mario , MONTAGNOLI, Alessia , SANTOCANALE, Corrado , ORSINI, Paolo , PILLAN, Antonio
IPC分类号： C07D401/04
CPC分类号： C07D471/04 , A61K31/506 , A61K31/513 , A61K31/52 , A61K41/00 , A61K45/06 , A61K2300/00
摘要： Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
摘要翻译：公开了本说明书中定义的式（1）的嘧啶基吡咯衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

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