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1.发明授权Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides 有权制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法公开(公告)号：US08399668B2
公开(公告)日：2013-03-19
申请号：US12989518
申请日：2009-04-30
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-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-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-1H-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。
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2.发明申请PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES 有权制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-羧酸的方法公开(公告)号：US20110040090A1
公开(公告)日：2011-02-17
申请号：US12989518
申请日：2009-04-30
IPC分类号： C07D403/04 , C07D207/416
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-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in W02007110344, 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-1H-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。 5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺在WO2007110344中进行了描述和要求保护，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。
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公开(公告)号：US20120245189A1
公开(公告)日：2012-09-27
申请号：US13508648
申请日：2010-11-05
IPC分类号： A61K31/506 , A61P35/00 , C07D403/04
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。
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公开(公告)号：US08658662B2
公开(公告)日：2014-02-25
申请号：US13508648
申请日：2010-11-05
IPC分类号： A01N43/54 , A61K31/505
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。
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公开(公告)号：US08673893B2
公开(公告)日：2014-03-18
申请号：US13611679
申请日：2012-09-12
申请人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/415 , A61K31/535 , A61K31/445
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。
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公开(公告)号：US08293762B2
公开(公告)日：2012-10-23
申请号：US12528656
申请日：2008-02-18
IPC分类号： A61K31/4745 , C07D471/12
CPC分类号： C07D471/04 , C07D471/14
摘要： Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions including 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 5和X如说明书，其组成，及其使用方法所定义。 特别地，描述了异喹啉吡咯并吡啶酮，包括它们的药物组合物及其作为治疗癌症和细胞增殖障碍的治疗剂的用途。
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公开(公告)号：US20100292207A1
公开(公告)日：2010-11-18
申请号：US12668745
申请日：2008-07-08
申请人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/416 , C07D403/12 , C07D231/56 , C07D405/14 , C07D405/12 , C07D413/14 , C07D403/14 , C07D413/12 , A61K31/497 , A61K31/5513 , A61K31/454 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P27/02 , A61P17/06 , A61P35/04 , A61P9/00 , A61P11/00
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。
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公开(公告)号：US5767282A
公开(公告)日：1998-06-16
申请号：US776607
申请日：1997-02-20
申请人： Cesare Gennari , Nicola Mongelli , Ermes Vanotti , Anna Vulpetti
发明人： Cesare Gennari , Nicola Mongelli , Ermes Vanotti , Anna Vulpetti
IPC分类号： C07D263/04 , C07D263/06 , C07D263/16 , C07D263/26 , C07D305/14 , C07D413/12
CPC分类号： C07D263/04 , C07D263/16 , C07D305/14 , C07D413/12 , Y02P20/55
摘要： A process of making taxane derivatives by reacting Baccatin III derivatives with an oxazolidine which contains a thioester substituent at the 4-position.
摘要翻译： PCT No.PCT / EP96 / 02409 Sec。 371日期1997年2月20日 102（e）1997年2月20日PCT PCT 1996年6月4日PCT公布。 出版物WO97 / 00870 日期1997年1月9日通过使Baccatin III衍生物与在4位含有硫酯取代基的恶唑烷反应制备紫杉烷衍生物的方法。
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公开(公告)号：US20050288238A1
公开(公告)日：2005-12-29
申请号：US10878212
申请日：2004-06-28
申请人： Mauro Angiolini , Sylvie Ducki , Maria Menichincheri , Nicola Mongelli , Ermes Vanotti , Marina Ciomei
发明人： Mauro Angiolini , Sylvie Ducki , Maria Menichincheri , Nicola Mongelli , Ermes Vanotti , Marina Ciomei
IPC分类号： A61K31/225 , A61K31/704 , C07C67/02 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07D213/55 , C07D233/54 , C07D263/32 , C07D277/30 , C07H15/24
CPC分类号： C07D233/64 , C07C67/08 , C07C67/29 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07C2602/12 , C07D213/55 , C07D263/32 , C07D277/30 , 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.
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公开(公告)号：US4939282A
公开(公告)日：1990-07-03
申请号：US622177
申请日：1984-06-19
IPC分类号： C07C50/38 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C45/00 , C07C46/00 , C07C50/36 , C07C67/00 , C07D407/04 , C07H15/252
CPC分类号： C07D407/04 , C07H15/252
摘要： A new process for the preparation of 6-deoxyanthracyclinones of general formula I: ##STR1## wherein R represents a hydrogen atom, a hydroxy group or a lower alkoxy group is described. The process provides a total synthesis of the 6-deoxyanthracyclinones of formula I using 1,2,3,6-tetrahydro-phthalate as starting material. The obtained racemic mixture of the compounds of formula I, if desired, can be submitted to optical resolution by the conventional method of conversion to diastereomeric derivatives using a chiral resolving agent. Alternatively, the racemic mixture can be used as such for the condensation with a suitably protected halosugar derivative to obtain alpha glycosidic derivatives of formula XV: ##STR2## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolisis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.
摘要翻译： 描述了制备通式I的6-脱氧尿嘧啶的新方法：其中R表示氢原子，羟基或低级烷氧基。 该方法提供使用1,2,3,6-四氢邻苯二甲酸酯作为起始原料的式I的6-脱氧蒽环类的全合成。 如果需要，所得到的式I化合物的外消旋混合物可以通过使用手性拆分剂转化成非对映体衍生物的常规方法进行光学拆分。 或者，外消旋混合物可以直接用于与适当保护的卤糖衍生物的缩合，以获得式XV的α糖苷衍生物：其中R 1表示氢原子或羟基，R 2和R 3之一表示 氢原子，R2和R3中的另一个表示氢原子或羟基，X是氢原子或三氟乙酰基。 式XV的α-糖苷类的N-三氟乙酰基7S：9S和7R：9R衍生物可以通过硅胶色谱分离，得到在温和的碱性水解后，所需的7S：9Sα-糖苷（R1 = H）为游离 碱，并且最终可以通过已知的方法转化成它们相应的多柔比星衍生物（R1 = OH）。
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