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

WO2009156315A1 PYRAZOLO-QUINAZOLINES 审中-公开
标题翻译：吡唑并喹唑啉
公开(公告)号：WO2009156315A1
公开(公告)日：2009-12-30
申请号：PCT/EP2009/057512
申请日：2009-06-17
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , CALDARELLI, Marina , ANGIOLINI, Mauro , COLOMBO, Riccardo , DISINGRINI, Teresa , NUVOLONI, Stefano , POSTERI, Helena , SALSA, Matteo , SILVAGNI, Marco
发明人： CALDARELLI, Marina , ANGIOLINI, Mauro , COLOMBO, Riccardo , DISINGRINI, Teresa , NUVOLONI, Stefano , POSTERI, Helena , SALSA, Matteo , SILVAGNI, Marco
IPC分类号： C07D487/04 , A61K31/517 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , C07D239/70
摘要： The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C 3 -C 7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C 3 -C 7 cycloalkyl as substituent of a carboxamide at 3 position of the molecula framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. 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：本发明涉及吡唑并 - 喹唑啉，其特征在于在8位的邻位取代的芳基氨基，杂环基氨基或C3-C7环烷基氨基残基，作为分子3位的羧酰胺取代基的芳基，杂环基或C 3 -C 7环烷基框架。本发明的化合物调节蛋白激酶的活性，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是MPS1 / TTK。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，以及利用包含这些化合物的药物组合物治疗疾病的方法。

2. 发明申请

WO2014067960A3 FUNCTIONALIZED 9-BROMO-CAMPTOTHECIN DERIVATIVES 审中-公开
公开(公告)号：WO2014067960A3
公开(公告)日：2014-05-08
申请号：PCT/EP2013/072633
申请日：2013-10-29
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BERIA, Italo , CARUSO, Michele , SALSA, Matteo , FAIARDI, Daniela
IPC分类号： C07D491/22 , A61K31/4745 , A61P35/00
摘要： The present invention relates to new functionalized 9-bromo- camptothecin derivatives (I) which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of these functionalized 9-bromo-camptothecin derivatives in the preparation of conjugates.

3. 发明申请

WO2012013557A1 ISOXAZOLO-QUINAZOLINES AS MODULATORS OF PROTEIN KINASE ACTIVITY 审中-公开
标题翻译：作为蛋白激酶活性的调节剂的ISOXAZOLO-QUINAZOLINES
公开(公告)号：WO2012013557A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/062453
申请日：2011-07-20
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , CALDARELLI, Marina , BERIA, Italo , COLOMBO, Nicoletta , PIUTTI, Claudia , SALSA, Matteo , TRAQUANDI, Gabriella
发明人： CALDARELLI, Marina , BERIA, Italo , COLOMBO, Nicoletta , PIUTTI, Claudia , SALSA, Matteo , TRAQUANDI, Gabriella
IPC分类号： C07D498/02 , A61K31/517 , A61P35/00
CPC分类号： A61K31/519 , A61K45/06 , A61N5/10 , C07D498/02 , C07D498/04
摘要： The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these 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取代异恶唑并喹唑啉，因此可用于治疗由失调蛋白激酶活性引起的疾病，特别是人MPS1和PERK。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。

4. 发明申请

WO2014072220A1 SUBSTITUTED PYRIMIDINYL AND PYRIDINYL-PYRROLOPYRIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 审中-公开
标题翻译：取代的吡咯烷酮和吡啶基吡咯烷酮，其制备方法及其作为激酶抑制剂的用途
公开(公告)号：WO2014072220A1
公开(公告)日：2014-05-15
申请号：PCT/EP2013/072793
申请日：2013-10-31
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： MENICHINCHERI, Maria , ANGIOLINI, Mauro , BERTRAND, Jay Aaron , CARUSO, Michele , POLUCCI, Paolo , QUARTIERI, Francesca , SALOM, Barbara , SALSA, Matteo , ZUCCOTTO, Fabio
IPC分类号： C07D471/04 , A61K31/506 , A61P35/00
CPC分类号： C07D471/04 , A61K31/496 , A61K31/506 , A61K45/06 , A61N5/10
摘要： The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及调节蛋白激酶活性的取代的嘧啶基和吡啶基吡咯并吡喃酮化合物，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是RET家族激酶。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，以及使用含有这些化合物的药物组合物治疗疾病的方法。

5. 发明申请

WO2013149946A1 FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的功能性三硝吲哚衍生物
公开(公告)号：WO2013149946A1
公开(公告)日：2013-10-10
申请号：PCT/EP2013/056733
申请日：2013-03-28
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BERIA, Italo , CARUSO, Michele , LUPI, Vittoria , ORSINI, Paolo , SALSA, Matteo
IPC分类号： C07D495/04 , A61K31/407 , A61P35/00
CPC分类号： A61K47/48338 , A61K31/496 , A61K45/06 , A61K47/65 , C07D495/04
摘要： The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates. Formula (I) or (II) wherein R 1 and R 2 taken together form a group (D) or (G): wherein R 5 is hydrogen or C 1 -C 4 alkyl; R 3 and R 4 are independently hydrogen, C 1 -C 4 alkyl or C 1 -C 4 hydroxyalkyi; n is 0, 1 or 2; each of X is independently -O-, -S- or -NR 4 -; each of Y is independently -CH = or -N=; R 7 and R 8 are independently hydrogen, halogen, hydroxy, C 1 -C 4 alkoxy, cyano, -NHCOOR 3 , -C(NH)NH 2 or -NR 3 R 4 ; A is -O-, -NH- or -CO-; L is null or a conditionally-cleavable moiety; W is null or a self-immolative moiety comprising one or more self-immolative groups; Z is null or a peptidic, non peptidic or hybrid peptidic and non peptidic linker; RM is null or a reactive moiety; R 6 is a leaving group; A 1 is null or A; L 1 is hydrogen or L.
摘要翻译：本发明涉及具有细胞毒活性并且可用于治疗疾病如癌症和细胞增殖病症的式（I）或（II）的新的功能化噻吩并吲哚衍生物。本发明还涉及这些官能化的噻吩并吲哚衍生物在共轭物的制备中的用途。式（I）或（II）其中R 1和R 2一起形成基团（D）或（G）：其中R 5是氢或C 1 -C 4烷基; R3和R4独立地是氢，C1-C4烷基或C1-C4羟基烷基; n为0,1或2; X各自独立地为-O - ， - S-或-NR 4 - ; 每个Y独立地是-CH =或-N =; R7和R8独立地是氢，卤素，羟基，C1-C4烷氧基，氰基，-NHCOOR3，-C（NH）NH2或-NR3R4; A是-O - ， - NH-或-CO-; L为无效或条件可切割部分; W是无效的或包含一个或多个自褪色基团的自褪色部分; Z是无效或肽，非肽或杂交肽和非肽接头; RM为无效或反应性部分; R6是离职团体 A1为null或A; L1是氢或L.

6. 发明申请

WO2012073217A1 PROCESS FOR THE PREPARATION OF MORPHOLINYL ANTHRACYCLINE DERIVATIVES 审中-公开
标题翻译：制备吗啉酰基蒽醌衍生物的方法
公开(公告)号：WO2012073217A1
公开(公告)日：2012-06-07
申请号：PCT/IB2011/055410
申请日：2011-12-01
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , CARUSO, Michele , LUPI, Vittoria , SALSA, Matteo
发明人： CARUSO, Michele , LUPI, Vittoria , SALSA, Matteo
IPC分类号： C07H19/24 , A61K31/706 , A61P35/00
CPC分类号： C07H15/244 , C07H1/00 , C07H19/24
摘要： The present invention provides a process for the preparation of a morpholinyl anthracycline derivative in good yields and purity, including 3'-deamino-3"-4'-anhydro- [2"(S)-methoxy-3"(R)-hydroxy-4"-morpholinyl] doxorubicin (1).
摘要翻译：本发明提供以良好的产率和纯度制备吗啉基蒽环类衍生物的方法，包括3'-脱氨基-3“-4'-脱水 - [2”（S） - 甲氧基-3“（R） - 羟基 -4“ - 吗啉基]多柔比星（1）。

7. 发明申请

WO2023083716A1 ANTHRACYCLINE DERIVATIVE LINKER REAGENTS, ANTIBODY-DRUG CONJUGATES AND METHODS 审中-公开
公开(公告)号：WO2023083716A1
公开(公告)日：2023-05-19
申请号：PCT/EP2022/080834
申请日：2022-11-04
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： SALSA, Matteo , GASPARRI, Fabio , ORSINI, Paolo , VALSASINA, Barbara
IPC分类号： A61K47/68 , A61P35/00 , C07D498/14 , C07H15/24 , C07H15/252
摘要： The present invention provides anthracycline-linker reagents for the preparation of therapeutic antibody-drug conjugate (ADC) compounds. The present invention also provides therapeutic antibody-drug conjugate (ADC) compounds comprising anthracycline drug moieties, with biological activity against cancer cells. The compounds may inhibit tumor growth in mammals and may be useful for treating human cancer patients. Aspects of the invention include methods of making, methods of preparing, methods of synthesis, methods of conjugation, and methods of purification of the anthracycline-linker reagents and of the antibody-drug conjugate compounds.

8. 发明申请

WO2013149948A1 NEW ALKYLATING AGENTS 审中-公开
标题翻译：新碱性剂
公开(公告)号：WO2013149948A1
公开(公告)日：2013-10-10
申请号：PCT/EP2013/056743
申请日：2013-03-28
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BERIA, Italo , CARUSO, Michele , LUPI, Rosita , ORSINI, Paolo , SALSA, Matteo , PANZERI, Achille
IPC分类号： C07D495/04 , A61K31/407 , A61P35/00
CPC分类号： A61K31/407 , A61K31/496 , A61K38/05 , A61K38/06 , A61K45/06 , A61K47/545 , C07D495/04 , C07K5/06017 , C07K5/0804
摘要： The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
摘要翻译：本发明涉及一类新颖的烷化剂，其包含与DNA结合部分连接的噻吩并吲哚部分，其具有细胞毒活性，并且可用于治疗疾病如癌症，细胞增殖病症和病毒感染。本发明还提供了制备这些化合物的方法，包含它们的药物组合物和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。本发明还涉及这种新型烷基化剂在制备缀合物中的用途。

9. 发明申请

WO2010009124A2 ANTHRACYCLINE DERIVATIVE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS 审中-公开
标题翻译：蒽环衍生物缀合物，其制备方法及其作为抗肿瘤化合物的用途
公开(公告)号：WO2010009124A2
公开(公告)日：2010-01-21
申请号：PCT/US2009/050537
申请日：2009-07-14
申请人： GENENTECH, INC. , NERVIANO MEDICAL SCIENCES S.R.L. , BERIA, Italo , CARUSO, Michele , FLYGARE, John, A. , LUPI, Vittoria , PEREGO, Rita , POLAKIS, Paul , POLSON, Andrew , SALSA, Matteo , SPENCER, Susan, D. , VALSASINA, Barbara
发明人： BERIA, Italo , CARUSO, Michele , FLYGARE, John, A. , LUPI, Vittoria , PEREGO, Rita , POLAKIS, Paul , POLSON, Andrew , SALSA, Matteo , SPENCER, Susan, D. , VALSASINA, Barbara
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
摘要： The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
摘要翻译：本发明涉及治疗上有用的蒽环类抗生素与载体如多克隆和单克隆抗体，天然或合成来源的蛋白质或肽的缀合物; 它们的制备方法，含有它们的药物组合物以及它们在治疗某些哺乳动物肿瘤中的用途。

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