专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2012143248A1 SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的替代吡咯烷基吡啶
公开(公告)号：WO2012143248A1
公开(公告)日：2012-10-26
申请号：PCT/EP2012/056266
申请日：2012-04-05
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , BRASCA, Maria Gabriella , BANDIERA, Tiziano , BERTRAND, Jay Aaron , GNOCCHI, Paola , MIRIZZI, Danilo , NESI, Marcella , PANZERI, Achille
发明人： BRASCA, Maria Gabriella , BANDIERA, Tiziano , BERTRAND, Jay Aaron , GNOCCHI, Paola , MIRIZZI, Danilo , NESI, Marcella , PANZERI, Achille
IPC分类号： C07D403/04 , A61K31/506 , A61P35/00
CPC分类号： A61K31/506 , C07D403/04 , C07D405/14 , C07F5/025
摘要： The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
摘要翻译：本发明涉及调节蛋白激酶活性的式（I）的取代的嘧啶基 - 吡咯化合物，因此可用于治疗由失调蛋白激酶活性引起的疾病，尤其是Janus激酶。本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物。

2. 发明申请

WO2007068619A1 SUBSTITUTED PYRAZOLO [4,3-C] PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活性的取代的吡唑并[4,3-C]吡啶衍生物
公开(公告)号：WO2007068619A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/069285
申请日：2006-12-06
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , POLUCCI, Paolo , VILLA, Manuela , NESI, Marcella , ANGIOLINI, Mauro , VARASI, Mario
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , POLUCCI, Paolo , VILLA, Manuela , NESI, Marcella , ANGIOLINI, Mauro , VARASI, Mario
IPC分类号： C07D471/04 , A61P35/00 , A61K31/496 , A61K31/437 , A61K31/5355
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine 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 dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的吡唑并[4,3-c]吡啶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。

3. 发明申请

WO2008074749A9 INDAZOLE DERIVATIVES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2008074749A9
公开(公告)日：2008-06-26
申请号：PCT/EP2007/063998
申请日：2007-12-14
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , NESI, Marcella , PERRONE, Ettore , BOSSI, Roberto , POLUCCI, Paolo
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , NESI, Marcella , PERRONE, Ettore , BOSSI, Roberto , POLUCCI, Paolo
IPC分类号： A61K31/4162 , A61P35/00
摘要： Substituted indazole derivativesof 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 dysregulated protein kinase activity, like cancer formula (I).

4. 发明申请

WO2007068637A1 SUBSTITUTED PYRROLO-PYRAZOLE 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吡咯并吡唑衍生物
公开(公告)号：WO2007068637A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/069373
申请日：2006-12-06
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , PERRONE, Ettore , BERIA, Italo , FANCELLI, Daniele , GALVANI, Arturo
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , PERRONE, Ettore , BERIA, Italo , FANCELLI, Daniele , GALVANI, Arturo
IPC分类号： C07D487/04 , A61P35/00 , A61K31/41 , A61K31/496 , A61K31/5355
CPC分类号： C07D487/04
摘要： Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and 5 pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的取代吡咯并 - 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5种药物组合物。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。

5. 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。

6. 发明申请

WO2007009898A1 1H-THIENO[2,3-C]PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译： 1H-THIENO [2,3-C]吡唑化合物作为激酶抑制剂有用
公开(公告)号：WO2007009898A1
公开(公告)日：2007-01-25
申请号：PCT/EP2006/064055
申请日：2006-07-10
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , FANCELLI, Daniele , MOLL, Juergen , PULICI, Maurizio , QUARTIERI, Francesca , BANDIERA, Tiziano
发明人： FANCELLI, Daniele , MOLL, Juergen , PULICI, Maurizio , QUARTIERI, Francesca , BANDIERA, Tiziano
IPC分类号： C07D495/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D495/04
摘要： There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent -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 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 organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are also 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：提供式（I）的噻吩并[2,3-c]吡唑衍生物，其中A是芳基或杂芳基环，取代基-NHZR 5在其上与CONH的邻位位置连接; R 1和R 2相同或不同，彼此独立地表示氢原子或有机基团; 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是氢或有机基团; 或异构体，互变异构体，载体，代谢物，前药及其药学上可接受的盐。还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相关的疾病，如癌症。

7. 发明申请

WO2007099171A2 BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译： BICYCLO-PYRAZOLES活性为激酶抑制剂
公开(公告)号：WO2007099171A2
公开(公告)日：2007-09-07
申请号：PCT/EP2007/052024
申请日：2007-03-02
申请人： PFIZER ITALIA S.R.L. , BANDIERA, Tiziano , BERTRAND, Jay Aaron , PEVARELLO, Paolo , PERRONE, Ettore , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , ANGIOLINI, Mauro , FANCELLI, Daniele
发明人： BANDIERA, Tiziano , BERTRAND, Jay Aaron , PEVARELLO, Paolo , PERRONE, Ettore , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , ANGIOLINI, Mauro , FANCELLI, Daniele
IPC分类号： C07D487/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/496 , A61K31/5377
摘要： A compound having formula (I): wherein: R, A, R 1 and R 2 , are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof
摘要翻译：具有式（I）的化合物：其中：R，A，R 1和R 2如本说明书中所定义，及其药物配方和使用方法其

8. 发明申请

WO2012167133A2 INHIBITORS OF ANANDAMIDE TRANSPORT AND THEIR THERAPEUTIC USES 审中-公开
标题翻译： ANANDAMIDE运输的抑制剂及其治疗用途
公开(公告)号：WO2012167133A2
公开(公告)日：2012-12-06
申请号：PCT/US2012/040531
申请日：2012-06-01
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , IIT - ISTITUTO ITALIANO DI TECNOLOGIA , PIOMELLI, Daniele , FU, Jin , BOTTEGONI, Giovanni , CAVALLI, Andrea , BANDIERA, Tiziano
发明人： PIOMELLI, Daniele , FU, Jin , BOTTEGONI, Giovanni , CAVALLI, Andrea , BANDIERA, Tiziano
IPC分类号： A61K31/502 , A61K31/495 , A61P29/00 , A61P25/00
CPC分类号： C07D237/34 , A61K31/495 , A61K31/502 , C07K14/435 , C12N15/11 , G01N33/5008
摘要： Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.
摘要翻译：提供了对应于FLAT，细胞内anandamide降解酶的部分胞质变体，脂肪酸酰胺水解酶-1（FAAH-1）的核酸和多肽序列。 FLAT没有酰胺酶活性，但是结合内源性抗生素Aandamide并促进其转运到细胞中。鉴定了用于抑制anandamide转运的化学支架。本发明的组合物在体外阻止氨酰胺内化，在体内中断anandamide失活，并在炎症性疼痛的小鼠模型中引起严重的CB1大麻素受体介导的镇痛。因此，本发明还提供了用于治疗其中调节anandamide转运有益的病症的方法和药物组合物。

9. 发明申请

WO2008145398A1 4-ARYLPYRROLE SUBSTITUTED 2-INDOLINE DERIVATIVES ACTIVE AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂活化的4-ARYLPYRROLE取代的2-吲哚衍生物
公开(公告)号：WO2008145398A1
公开(公告)日：2008-12-04
申请号：PCT/EP2008/004342
申请日：2008-05-31
申请人： PFIZER ITALIA S.R.L. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , PAOLUCCI, Paolo , ORRENIUS, Christian , GALVANI, Arturo
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , PAOLUCCI, Paolo , ORRENIUS, Christian , GALVANI, Arturo
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , A61K31/404 , A61P35/00
CPC分类号： C07D403/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to certain 4-arylpyrrole substituted 2-indolinone compounds of Formula (I), which modulate the activity of protein kinases (PKs). The compounds of this invention are therefore useful in treating disorders related to dysregulated PK activity The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及调节蛋白激酶（PK）活性的式（I）的某些4-芳基吡咯取代的2-二氢吲哚酮化合物。因此，本发明的化合物可用于治疗与失调的PK活性相关的疾病。本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用包含这些化合物的药物组合物治疗疾病的方法。

10. 发明申请

WO2013028570A2 META-SUBSTITUTED BIPHENYL PERIPHERALLY RESTRICTED FAAH INHIBITORS 审中-公开
标题翻译： META取代的联苯外周限制性FAAH抑制剂
公开(公告)号：WO2013028570A2
公开(公告)日：2013-02-28
申请号：PCT/US2012/051478
申请日：2012-08-17
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , UNIVERSITA DEGLI STUDI DI URBINO "Carlo Bo" , UNIVERSITA DEGLI STUDI DI PARMA , PIOMELLI, Daniele , MORENO-SANZ, Guillermo , BANDIERA, Tiziano , MOR, Marco , TARZIA, Giorgio
发明人： PIOMELLI, Daniele , MORENO-SANZ, Guillermo , BANDIERA, Tiziano , MOR, Marco , TARZIA, Giorgio
IPC分类号： C07C233/06 , C07C233/23 , C07D309/14 , A61K31/165 , A61P29/00
CPC分类号： C07C271/56 , C07C269/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D309/14
摘要： The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.
摘要翻译：本发明提供制备和使用脂肪酸酰胺水解酶（FAAH）的外周限制性抑制剂的方法。本发明提供抑制FAAH活性并增加中枢神经系统（CNS）外的anandamide水平的化合物和组合物。本发明还提出了抑制FAAH的方法以及用于治疗诸如但不限于疼痛，炎症，免疫病症，皮炎，粘膜炎，外周感觉神经元的过度反应性，神经性皮炎和膀胱过动症的病症的方法。因此，本发明还提供了用于治疗其中外周FAAH的选择性抑制（与CNS FAAH相反）会有益的病症的化合物，方法和药物组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式