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1. 发明申请

WO2007138017A1 1H-FURO[3,2-C] PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译： 1H-FURO [3,2-C]吡唑化合物作为激酶抑制剂有用
公开(公告)号：WO2007138017A1
公开(公告)日：2007-12-06
申请号：PCT/EP2007/055113
申请日：2007-05-25
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , FANCELLI, Daniele , PULICI, Maurizio , MOLL, Jurgen , BANDIERA, Tiziano
发明人： FANCELLI, Daniele , PULICI, Maurizio , MOLL, Jurgen , BANDIERA, Tiziano
IPC分类号： C07D491/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D491/048
摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, - NHZR 5 is at the ortho position to the CONH linker; - R 1 and R 2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R 3 is a hydrogen or halogen atom or an organic group; R 4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C=O, or -C(=O)NH-; - R 5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A 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, in particular Aurora kinases activity or IGF-1R activity, like cancer.
摘要翻译：如描述中定义的式（I）的呋喃并[3,2-c]吡唑衍生物及其药学上可接受的盐，其中A是芳基或杂芳基环，-NHZR 5 位置到CONH接头; R 1和R 2相同或不同，彼此独立地表示氢原子或有机残基; R 3是氢或卤素原子或有机基团; R 4是氢或卤素原子或有机基团; Z是直接键合，> C = O或-C（= O）NH-; R 5是氢或任选取代的有机基团或其异构体，互变异构体，载体，代谢物，前药及其药学上可接受的盐。公开了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，特别是Aurora激酶活性或IGF-1R活性相关的疾病，如癌症。

2. 发明申请

WO2005005427A1 PYRROLO[3,4-c]PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译： PYRROLO [3,4-c]作为激酶抑制剂活化的吡唑衍生物
公开(公告)号：WO2005005427A1
公开(公告)日：2005-01-20
申请号：PCT/EP2004/007515
申请日：2004-07-08
申请人： PHARMACIA ITALIA S.P.A. , FANCELLI, Daniele , FORTE, Barbara , MOLL, Jurgen , VARASI, Mario , VIANELLO, Paola
发明人： FANCELLI, Daniele , FORTE, Barbara , MOLL, Jurgen , VARASI, Mario , VIANELLO, Paola
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolo[3,4-c]pyrazole 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）的吡咯并[3,4-c]吡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。

3. 发明申请

WO2002074036A2 SUBSTITUTED BENZOPYRANONES AS TELOMERASE INHIBITORS 审中-公开
标题翻译：作为TELOMERASE抑制剂的取代苯并噻喃酮
公开(公告)号：WO2002074036A2
公开(公告)日：2002-09-26
申请号：PCT/EP2002/002783
申请日：2002-03-12
申请人： PHARMACIA ITALIA SPA , BARGIOTTI, Alberto , BONOMINI, Luisella , MENICHINCHERI, Maria , MOLL, Jurgen , POLUCCI, Paolo , SONCINI, Chiara , VANOTTI, Ermes
发明人： BARGIOTTI, Alberto , BONOMINI, Luisella , MENICHINCHERI, Maria , MOLL, Jurgen , POLUCCI, Paolo , SONCINI, Chiara , VANOTTI, Ermes
IPC分类号： A61K31/352 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61K31/498 , A61P35/00 , A61P43/00 , C07D311/30 , C07D405/04 , C07D413/04 , C07D417/04
CPC分类号： C07D405/04 , A61K31/352 , C07D311/30 , C07D413/04 , C07D417/04
摘要： The present invention relates to benzopyranone derivative, to methods for treating telomerase-modulated diseases, in particular cancers, with said derivatives, to a process for their preparation, to their use as medicaments and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及苯并吡喃酮衍生物，涉及用于治疗端粒酶调节的疾病，特别是癌症与所述衍生物的方法，其制备方法，用作药物和包含它们的药物组合物。

4. 发明申请

WO2008052931A1 A METHOD OF ADMINISTERING AN ANTITUMOR COMPOUND 审中-公开
标题翻译：施用抗微生物化合物的方法
公开(公告)号：WO2008052931A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/061491
申请日：2007-10-25
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , LAFFRANCHI, Bernard , MOLL, Jurgen , BOLOGNA, Fabrina , COMIS, Silvia
发明人： LAFFRANCHI, Bernard , MOLL, Jurgen , BOLOGNA, Fabrina , COMIS, Silvia
IPC分类号： A61K31/4162 , A61P35/00
CPC分类号： A61K31/4162
摘要： The present invention provides a method of treating a mammal, including humans, suffering from tumour, comprising administering Compound 1 of the formula A or a pharmaceutically acceptable salt thereof, to said mammal by intravenous infusion, characterised in that Compound 1 is conveniently administered employing particular schedules, infusion times and doses which allow a more efficacious treatment. Compound 1 of formula A is an aurora inhibitor, chemical name N-{5-[(2R)-2-methoxy- 2-phenylethanoyl]-1,4,5,6-tetrahydropyrrolo[3,4-c] pyrazol-3-yl}-4-(4-methylpiperazin-1-yl) benzamide, and the method is preferably for the treatment of patients having solid tumours or hematopoietic malignant tumours. The use of Compound 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient, in the manufacture of a medicament for the treatment of tumours employing particular schedules, infusion times and doses, as well as the use of Compound 1 for treatment of tumours in the same manner are also provided.
摘要翻译：本发明提供了一种治疗患有肿瘤的哺乳动物（包括人）的方法，其包括通过静脉内输注向所述哺乳动物施用式A化合物1或其药学上可接受的盐，其特征在于化合物1通过特别方法施用时间表，输液时间和剂量，可进行更有效的治疗。式A的化合物1是化学名称为N- {5 - [（2R）-2-甲氧基-2-苯基乙酰基] -1,4,5,6-四氢吡咯并[3,4-c]吡唑-3 - 基} -4-（4-甲基哌嗪-1-基）苯甲酰胺，该方法优选用于治疗患有实体瘤或造血恶性肿瘤的患者。化合物1或其药学上可接受的盐和药学上可接受的载体或赋形剂在制备用于治疗使用特定时间表，输注时间和剂量的肿瘤的药物中的用途以及化合物1用于也提供以相同方式治疗肿瘤。

5. 发明申请

WO2007113198A3 USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS 审中-公开
标题翻译：使用激酶抑制剂治疗特异性抗肿瘤药物
公开(公告)号：WO2007113198A3
公开(公告)日：2008-03-20
申请号：PCT/EP2007053013
申请日：2007-03-29
申请人： NERVIANO MEDICAL SCIENCES SRL , FANCELLI DANIELE , ISACCHI ANTONELLA , MODUGNO MICHELE , MOLL JURGEN , RUSCONI LUISA , SONCINI CHIARA , LUPI ROSITA
发明人： FANCELLI DANIELE , ISACCHI ANTONELLA , MODUGNO MICHELE , MOLL JURGEN , RUSCONI LUISA , SONCINI CHIARA , LUPI ROSITA
IPC分类号： A61K31/4162 , A61K31/44 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/44
摘要： The invention provides low molecular weight compounds, namely 1H-thieno[2,3- c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor- resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
摘要翻译：本发明提供了低分子量化合物，即1H-噻吩并[2,3-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。

6. 发明申请

WO0136602A3 PAK5 A MEMBER OF THE P21-ACTIVATED KINASE (PAK) PROTEIN FAMILY, NUCLEIC ACIDS AND METHODS RELATED TO THE SAME 审中-公开
标题翻译： PAK5 P21激活的激酶（PAK）蛋白家族成员，核酸及其相关方法
公开(公告)号：WO0136602A3
公开(公告)日：2001-10-04
申请号：PCT/EP0010736
申请日：2000-11-14
申请人： PHARMACIA & UPJOHN SPA , DAHLBERG MATS , MOLL JURGEN , GALVANI ARTURO
发明人： DAHLBERG MATS , MOLL JURGEN , GALVANI ARTURO
IPC分类号： G01N33/50 , A61K38/46 , A61K39/00 , A61K39/395 , A61K48/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61P37/06 , C07K16/40 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/10 , C12N9/12 , C12N15/09 , C12P21/08 , C12Q1/48 , C12Q1/68 , G01N33/15 , G01N33/53 , A61K38/45 , A61K121/00 , C12N1/14 , C12N1/20 , C12N15/54 , C12N15/63
CPC分类号： C12N9/1205 , A61K39/00 , C12Y207/01037
摘要： The present invention provides a human polypeptide homolog of P21-activated kinase (PAK) polynucleotides which identify and encode PAK5 serine/threonine kinase. In addition, the inventon provides expression vectors, host cells and methods for its production. The invention also provides methods for the identification of PAK5 agonists/antagonists, useful for the treatment of human diseases and conditions.
摘要翻译：本发明提供鉴定和编码PAK5丝氨酸/苏氨酸激酶的P21活化激酶（PAK）多核苷酸的人多肽同源物。此外，本发明提供表达载体，宿主细胞及其生产方法。本发明还提供了用于鉴定可用于治疗人类疾病和病症的PAK5激动剂/拮抗剂的方法。

7. 发明申请

WO2007113212A3 USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS 审中-公开
标题翻译：使用激酶抑制剂治疗特异性肿瘤
公开(公告)号：WO2007113212A3
公开(公告)日：2008-01-24
申请号：PCT/EP2007053041
申请日：2007-03-29
申请人： NERVIANO MEDICAL SCIENCES SRL , FANCELLI DANIELE , ISACCHI ANTONELLA , MODUGNO MICHELE , MOLL JURGEN , RUSCONI LUISA , SONCINI CHIARA , LUPI ROSITA
发明人： FANCELLI DANIELE , ISACCHI ANTONELLA , MODUGNO MICHELE , MOLL JURGEN , RUSCONI LUISA , SONCINI CHIARA , LUPI ROSITA
IPC分类号： A61K31/4162 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/454 , A61K31/496 , A61K31/5377
摘要： The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
摘要翻译：本发明提供了低分子量化合物，即四氢吡咯并[3,4-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。因此，这些化合物也是ATP竞争性的酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂的T315I ABL突变体。本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP袋的化合物，特别是T315I突变体ABL激酶的筛选方法。

8. 发明申请

WO2007113212A2 USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS 审中-公开
标题翻译：使用激酶抑制剂治疗特异性抗肿瘤药物
公开(公告)号：WO2007113212A2
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053041
申请日：2007-03-29
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
发明人： FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
IPC分类号： A61K31/4162 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/454 , A61K31/496 , A61K31/5377
摘要： The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
摘要翻译：本发明提供了低分子量化合物，即四氢吡咯并[3,4-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。

9. 发明申请

WO2007113198A2 USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS 审中-公开
标题翻译：使用激酶抑制剂治疗特异性抗肿瘤药物
公开(公告)号：WO2007113198A2
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053013
申请日：2007-03-29
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
发明人： FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
IPC分类号： A61K31/4162 , A61K31/44 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/44
摘要： The invention provides low molecular weight compounds, namely 1H-thieno[2,3- c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor- resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
摘要翻译：本发明提供了低分子量化合物，即1H-噻吩并[2,3-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。

10. 发明申请

WO02074036A3 SUBSTITUTED BENZOPYRANONES AS TELOMERASE INHIBITORS 审中-公开
标题翻译：取代的苯并吡喃酮作为端粒酶抑制剂
公开(公告)号：WO02074036A3
公开(公告)日：2002-12-05
申请号：PCT/EP0202783
申请日：2002-03-12
申请人： PHARMACIA ITALIA SPA , BARGIOTTI ALBERTO , BONOMINI LUISELLA , MENICHINCHERI MARIA , MOLL JURGEN , POLUCCI PAOLO , SONCINI CHIARA , VANOTTI ERMES
发明人： BARGIOTTI ALBERTO , BONOMINI LUISELLA , MENICHINCHERI MARIA , MOLL JURGEN , POLUCCI PAOLO , SONCINI CHIARA , VANOTTI ERMES
IPC分类号： A61K31/352 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61K31/498 , A61P35/00 , A61P43/00 , C07D311/30 , C07D405/04 , C07D413/04 , C07D417/04 , A61K31/35 , C07F7/18
CPC分类号： C07D405/04 , A61K31/352 , C07D311/30 , C07D413/04 , C07D417/04
摘要： The present invention relates to benzopyranone derivative, to methods for treating telomerase-modulated diseases, in particular cancers, with said derivatives, to a process for their preparation, to their use as medicaments and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及苯并吡喃酮衍生物，涉及用所述衍生物治疗端粒酶调节的疾病，特别是癌症的方法，它们的制备方法，它们作为药物的用途以及包含它们的药物组合物。

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