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1. 发明申请

WO2011057960A1 CRYSTALLINE CDC7 INHIBITOR SALTS 审中-公开
标题翻译：结晶CDC7抑制剂盐
公开(公告)号：WO2011057960A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/066873
申请日：2010-11-05
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , ZAMPIERI, Massimo , VANOTTI, Ermes , CIVAROLI, Paola , FORNARETTO, Maria, Gioia
发明人： ZAMPIERI, Massimo , VANOTTI, Ermes , CIVAROLI, Paola , FORNARETTO, Maria, Gioia
IPC分类号： C07D403/04 , A61K31/506 , A61P35/00
CPC分类号： C07D403/04
摘要： The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide.
摘要翻译：本发明涉及CDC7或CDC7 / CDKs抑制剂的新结晶盐，相应游离碱的新结晶形式，其制备方法，这些新盐形式的水合物，溶剂化物和多晶型物的用途在治疗和含有它们的药物组合物。这样的结晶盐选自5-（2-氨基 - 嘧啶-4-基）-2-（2,4-二氯 - 苯基）-2-羟基丙酸的L-天冬氨酸盐，半富马酸盐，盐酸盐，马来酸盐，甲磺酸盐，硫酸盐，L-酒石酸盐或磷酸盐，苯基）-1H-吡咯-3-甲酸酰胺。

2. 发明申请

WO2009133170A1 PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES 审中-公开
标题翻译：制备5-（2-氨基 - 嘧啶-4-基）-2-亚甲基-1H-吡咯-3-羧酸的方法
公开(公告)号：WO2009133170A1
公开(公告)日：2009-11-05
申请号：PCT/EP2009/055262
申请日：2009-04-30
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , D'ANELLO, Matteo , BATTISTINI, Carlo , FORNARETTO, Maria Gioia , VANOTTI, Ermes
发明人： D'ANELLO, Matteo , BATTISTINI, Carlo , FORNARETTO, Maria Gioia , VANOTTI, Ermes
IPC分类号： C07D403/04
CPC分类号： C07D403/04
摘要： The present invention relates to a process for the preparation of 5-(2-amino- pyrimidin-4-yl)-2-aryl-lH-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-lH-pyrrole-3-carboxamides are described and claimed in WO2007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-lH-pyrrole-3- carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
摘要翻译：本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。在WO2007110344中描述和要求保护的5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺，其也公开了其制备方法。这些化合物可以有利地通过允许以高产率和纯度以及有限数量的步骤获得所需产物的方法制备。合成起始于氰基吡咯衍生物，其特征在于5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲腈的最终水解。根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

3. 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。

4. 发明申请

WO2008104475A1 ISOQUINOLINOPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的活性氧化丙烯吡咯烷酮
公开(公告)号：WO2008104475A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/051948
申请日：2008-02-18
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , VANOTTI, Ermes , MENICHINCHERI, Maria , SCOLARO, Alessandra
发明人： VANOTTI, Ermes , MENICHINCHERI, Maria , SCOLARO, Alessandra
IPC分类号： A61K31/437
CPC分类号： C07D471/04 , C07D471/14
摘要： Heteroarylpyridinone derivatives represented by formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions comprising them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.
摘要翻译：由式（I）表示的杂芳基吡啶酮衍生物，其中R 1，R 2，R 3，R 4，R 4，并且X如说明书，其组成，及其使用方法中所定义。特别地，描述了异喹啉基吡咯并吡啶酮，包含它们的药物组合物及其在治疗癌症和细胞增殖障碍中作为治疗剂的用途。

5. 发明申请

WO2009013126A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的取代的吲哚酚衍生物
公开(公告)号：WO2009013126A1
公开(公告)日：2009-01-29
申请号：PCT/EP2008/058861
申请日：2008-07-08
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , LOMBARDI BORGIA, Andrea , MENICHINCHERI, Maria , ORSINI, Paolo , PANZERI, Achille , PERRONE, Ettore , VANOTTI, Ermes , NESI, Marcella , MARCHIONNI, Chiara
发明人： LOMBARDI BORGIA, Andrea , MENICHINCHERI, Maria , ORSINI, Paolo , PANZERI, Achille , PERRONE, Ettore , VANOTTI, Ermes , NESI, Marcella , MARCHIONNI, Chiara
IPC分类号： C07D231/56 , A61K31/33 , A61P35/00
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole derivatives of formula (I) 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 deregulated protein kinase activity, like cancer.
摘要翻译：公开了本说明书中定义的式（I）的取代的吲唑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; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

6. 发明申请

WO2008065054A1 TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES 审中-公开
标题翻译：三聚吲哚和（4,5-二羟基）吲哚
公开(公告)号：WO2008065054A1
公开(公告)日：2008-06-05
申请号：PCT/EP2007/062762
申请日：2007-11-23
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , VANOTTI, Ermes , CALDARELLI, Marina , CASUSCELLI, Francesco , FORTE, Barbara , MENICHINCHERI, Maria , SCOLARO, Alessandra , TRAQUANDI, Gabriella , VIANELLO, Paola
发明人： VANOTTI, Ermes , CALDARELLI, Marina , CASUSCELLI, Francesco , FORTE, Barbara , MENICHINCHERI, Maria , SCOLARO, Alessandra , TRAQUANDI, Gabriella , VIANELLO, Paola
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4162 , A61K31/4745 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, ----- means either simple or double carbon-carbon bond and R 1 , R 2 and R 3 are as defined in the specification. Further objects of the invention are a process 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, in particular Cdc7 and AKT kinase activity, like cancer.
摘要翻译：本发明提供式（I）的三环吲哚和（4,5-二氢）吲哚或其药学上可接受的盐：其中环A表示稠合吡唑，吡啶或嘧啶，-----表示简单或双碳 - 碳键和R 1，R 2和R 3是如说明书中所定义的。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。事实上，式（I）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，特别是Cdc7和AKT激酶活性，如癌症。

7. 发明申请

WO2002090358A1 DISUBSTITUTED 7,9-GUANINIUM HALIDES AS TELOMERASE INHIBITORS 审中-公开
标题翻译：作为TELOMERASE抑制剂的7,9-角质酸
公开(公告)号：WO2002090358A1
公开(公告)日：2002-11-14
申请号：PCT/EP2001/006625
申请日：2001-06-08
申请人： PHARMACIA ITALIA S.p.A. , BARGIOTTI, Alberto , ERMOLI, Antonella , MENICHINCHERI, Maria , VANOTTI, Ermes , BONOMINI, Luisella , FRETTA, Antonella
发明人： BARGIOTTI, Alberto , ERMOLI, Antonella , MENICHINCHERI, Maria , VANOTTI, Ermes , BONOMINI, Luisella , FRETTA, Antonella
IPC分类号： C07D473/18
CPC分类号： C07D473/18
摘要： The present invention relates to benzylmethyl and/or naphtylmethyl disubstituted 7,9-guaninium halides possessing antitumor activity, to pharmaceutical compositions comprising them and to a process for preparing the same. Furthermore, these compounds are expected to enhance the efficacy of other chemotherapeutic agents, in the treatment of cancer.
摘要翻译：本发明涉及具有抗肿瘤活性的苄基甲基和/或萘甲基二取代的7,9-胍卤化物，包括它们的药物组合物及其制备方法。此外，预期这些化合物可以增强其他化学治疗剂在癌症治疗中的功效。

8. 发明申请

WO2003055861A1 BENZOCYCLODECANE DERIVATIVES WITH ANTITUMOR ACTIVITY 审中-公开
标题翻译：具有抗肿瘤活性的苯并四氢吡喃衍生物
公开(公告)号：WO2003055861A1
公开(公告)日：2003-07-10
申请号：PCT/EP2002/014514
申请日：2002-12-18
申请人： PHARMACIA ITALIA SPA , ANGIOLINI, Mauro , DUCKI, Sylvie , MENICHINCHERI, Maria , MONGELLI, Nicola , VANOTTI, Ermes , CIOMEI, Marina
发明人： ANGIOLINI, Mauro , DUCKI, Sylvie , MENICHINCHERI, Maria , MONGELLI, Nicola , VANOTTI, Ermes , CIOMEI, Marina
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07C45/673 , C07C49/747 , C07C67/08 , C07C67/29 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07C2602/12 , C07D213/56 , C07D263/32 , C07D277/30 , C07H15/203 , C07C69/16
摘要： A compound which is a benzocyclodecane of the formula I wherein: ----- at positions 8-9 and 11-12 independently represents a single or double bond, -R1 is =O, or -OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH=CHR8, R8 is aryl or heterocyclyl;-R2 and -R3 are H, =O or -OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then -R4 represents=O, =CH2, =CHCOOR10, R10 is C1-C10 alkyl or aryl; =CH(OCH3), -OR9; -CH2OR11, R11 is H or a sugar residue, -COR12 , R12 is H, -OH or -OR10; or when at position 11-12 there is a double bond, then -R4 is -CH2OR11 or -COR12; - R5 and -R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6 alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R1 and R4 =O, then one of R2, R3, R5, R6 and R13 is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.
摘要翻译：作为式I的苯并环十一烷的化合物，其中： - 在8-9和11-12位，独立地表示单键或双键，-R1为=或-OR7，R7为H，C1- C7烷酰基，苯甲酰基，C1-C10烷基，C2-C10烯基或COCH = CHR8，R8是芳基或杂环基; -R2和-R3是H，= O或-OR9，R9是H，C1-C7烷酰基或苯甲酰基; 当在11-12位存在单键时，则-R 4表示= O，= CH 2，= CHCOOR 10，R 10是C 1 -C 10烷基或芳基; = CH（OCH 3），-OR 9; -CH 2 OR 11，R 11为H或糖残基，-COR 12，R 12为H，-OH或-OR 10; 或者当在11-12位存在双键时，则-R 4是-CH 2 OR 11或-COR 12; -R 5和-R 6是H或当在8-9位存在单键时，一起形成环丙烷环; R 13是H或1-3个选自C 1 -C 6烷基，C 2 -C 6烯基，苯基，苯基C 1 -C 6烷基，卤素，羟基，C 1 -C 6烷氧基，芳氧基，氰基，硝基，氨基，C 1 -C 10烷基氨基，芳基氨基，C 1 -C 7烷酰基氨基，芳酰氨基，羟基羰基，氨基羰基，C 1 -C 6烷基羰基，C 1 -C 6烷基氨基磺酰基和芳基氨基磺酰基; 条件是如果R1和R4 = O，则R2，R3，R5，R6和R13之一不是H原子; 或其药学上可接受的盐。这些苯并环十一烷衍生物具有抗肿瘤活性; 还提供了其制备方法和新的中间体，含有它们的药物组合物及其在预防，控制和治疗癌症中的用途。

9. 发明申请

WO2007096334A1 PYRROLOPYRROLONES 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
公开(公告)号：WO2007096334A1
公开(公告)日：2007-08-30
申请号：PCT/EP2007/051570
申请日：2007-02-19
申请人： PFIZER ITALIA SRL , VANOTTI, Ermes , MARTINA, Katia , MENICHINCHERI, Maria , D'ALESSIO, Roberto
发明人： VANOTTI, Ermes , MARTINA, Katia , MENICHINCHERI, Maria , D'ALESSIO, Roberto
IPC分类号： C07D487/04 , A61P35/00 , A61K31/407
CPC分类号： C07D487/04
摘要： Compounds represented by formula (I) wherein A, R 1 , R 2 , R 3 , and R 4 are as defined in the specification, compositions thereof, and methods of use thereof.
摘要翻译：由式（I）表示的化合物，其中A，R 1，R 2，R 3和R 4，如说明书，其组合物及其使用方法中所定义。

10. 发明申请

WO2007071621A1 HETEROARYLPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的异氟烷基吡咯烷酮
公开(公告)号：WO2007071621A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/069761
申请日：2006-12-15
申请人： PFIZER ITALIA Srl , VANOTTI, Ermes , FORTE, Barbara , MARTINA, Katia , MENICHINCHERI, Maria , CIRLA, Alessandra , ORSINI, Paolo
发明人： VANOTTI, Ermes , FORTE, Barbara , MARTINA, Katia , MENICHINCHERI, Maria , CIRLA, Alessandra , ORSINI, Paolo
IPC分类号： C07D471/04 , A61K31/444 , A61K31/506 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds represented by formuia (I) wherein A, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification or a pharmaceutically acceptable salt or solvate thereof, compositions thereof, and methods of use thereof.
摘要翻译：由式（I）表示的化合物，其中A，R 1，R 2，R 3，R 4， R 5和R 6如说明书或其药学上可接受的盐或溶剂化物，其组合物及其使用方法中所定义。

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