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1. 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。

2. 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）。

3. 发明公开

EP2303332A2 ANTHRACYCLINE DERIVATIVE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS 有权
标题翻译： ANTHRACYCLINKONJUGATE，对于其方法及其作为抗肿瘤药
公开(公告)号：EP2303332A2
公开(公告)日：2011-04-06
申请号：EP09790394.2
申请日：2009-07-14
申请人： Genentech, Inc. , NERVIANO MEDICAL SCIENCES S.R.L.
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.

4. 发明授权

EP2303332B1 ANTHRACYCLINE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS 有权
标题翻译： ANTHRACYCLINKONJUGATE，对于其方法及其作为抗肿瘤药
公开(公告)号：EP2303332B1
公开(公告)日：2014-12-31
申请号：EP09790394.2
申请日：2009-07-14
申请人： Genentech, Inc. , NERVIANO MEDICAL SCIENCES S.R.L.
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

5. 发明申请

WO2014177441A1 NEW MORPHOLINYL ANTHRACYCLINE DERIVATIVES 审中-公开
标题翻译：新型吗啉酰蒽醌衍生物
公开(公告)号：WO2014177441A1
公开(公告)日：2014-11-06
申请号：PCT/EP2014/058262
申请日：2014-04-23
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BERIA, Italo , CARUSO, Michele , LUPI, Vittoria
IPC分类号： C07D498/14 , A61K31/5383 , A61P35/00
CPC分类号： C07H9/00 , A61K31/7034 , A61K31/704 , A61K45/06 , C07D498/14
摘要： The present invention relates to new morpholinyl anthracycline derivatives 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 compositions containing them.
摘要翻译：本发明涉及具有细胞毒活性并可用于治疗疾病如癌症，细胞增殖病症和病毒感染的新的吗啉基蒽环类衍生物。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。

6. 发明申请

WO2016071418A1 FUNCTIONALIZED MORPHOLINYL ANTHRACYCLINE DERIVATIVES 审中-公开
标题翻译：官能化的吗啉代蒽醌衍生物
公开(公告)号：WO2016071418A1
公开(公告)日：2016-05-12
申请号：PCT/EP2015/075749
申请日：2015-11-04
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BERIA, Italo , CARUSO, Michele , LUPI, Vittoria
IPC分类号： C07D498/14 , A61K31/5383 , A61P35/00
CPC分类号： A61K31/5383 , A61K45/06 , A61K47/542 , A61K47/545 , A61K47/64 , C07D498/14 , A61K2300/00
摘要： The present invention relates to new functionalized morpholinyl anthracycline derivatives 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 compositions containing them. The invention also relates to the use of these derivatives in the preparation of conjugates. The morpholinyl anthracycline derivatives are of the formula Ant-L-W-Z-RM (I) wherein RM is null or a reactive moiety; Z is null or a peptidic, non peptidic or hybrid - peptidic and non peptidic - linker; W is null or a self-immolative system, comprising one or more self-immolative groups; L is null or a conditionally-cleavable moiety; Ant is an anthracycline moiety selected from the formulas (II), (III), (IV) and (V), wherein the wavy line indicates the attachment to the conditionally-cleavable moiety L, or to the self-immolative system W, or to the linker Z, or to the reactive moiety RM; provided that at least one of L, W, Z and RM is not null; R 1 is halogen or NR4R5; R2 is OR6, NR7R8 or an optionally substituted group selected from straight or branched C 1 C 4 alkyl-, NR7R8-C 1 C 4 alkyl- and R60-C 1 C 4 alkyl-; R4 and R5 are independently hydrogen, a monosubstituted-benzyl, a disubstituted-benzyl, or an optionally substituted group selected from straight or branched C 1 -C 6 alkyl, NR7R8-C 1 -C 6 alkyl-, R60-C 1 -C 6 alkyl-, R7R8N-C 1 -C 6 alkylcarbonyl-, R60-C 1 -C 6 alkylcarbonyl-, R7R8N-C 1 -C 6 alkoxycarbonyl- and R60-C 1 -C 6 alkoxycarbonyl-; or R4 and R5, taken together with the nitrogen atom to which they are bound, form a heterocyclyl substituted with R4', wherein R4' is hydrogen or a group selected from straight or branched C 1 -C 6 alkyl and NR7R8-C 1 -C 6 alkyl-; R15 is null or an optionally substituted bivalent group selected from -NR7-C 1 -C 6 alkyl*, -O-C 1 -C 6 alkyl*, -NR7-C 1 -C 6 alkylcarbonyl*, -O-C 1 -C 6 alkylcarbonyl*, -NR7-C 1 -C 6 alkoxycarbonyl* and -O-C 1 -C 6 alkoxycarbonyl*, wherein * indicates the point of attachment to -NH-Ant; R6, R7 and R8 are independently hydrogen or an optionally substituted straight or branched C 1 -C 6 alkyl; or a pharmaceutically acceptable salt thereof.
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，细胞增殖病症和病毒感染的新的功能化吗啉基蒽环类衍生物。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。本发明还涉及这些衍生物在制备缀合物中的用途。吗啉基蒽环类衍生物具有下式：其中RM为无效或反应性部分的Ant-L-W-Z-RM（I） Z是无效或肽，非肽或杂交 - 肽和非肽 - 接头; W是无效的或自我毁灭的系统，包括一个或多个自我毁灭的团体; L为无效或条件可切割部分; 蚂蚁是选自式（II），（III），（IV）和（V））的蒽环类部分，其中波浪线表示与条件可切割部分L的连接，或者指自分泌系统W，或到接头Z或反应性部分RM; 条件是L，W，Z和RM中的至少一个不为空; R1是卤素或NR4R5; R2是OR6，NR7R8或选自直链或支链C1C4烷基 - ，NR7R8-C1C4烷基 - 和R60-C1C4烷基 - 的任选取代基; R4和R5独立地是氢，单取代的苄基，二取代的苄基或选自直链或支链C1-C6烷基，NR7R8-C1-C6烷基 - ，R60-C1-C6烷基 - ，R7R8N-C1-C6烷基羰基 - ，R60-C1-C6烷基羰基 - ，R7R8N-C1-C6烷氧基羰基 - 和R60-C1-C6烷氧基羰基 - ; 或R4和R5与它们所连接的氮原子一起形成被R4'取代的杂环基，其中R4'是氢或选自直链或支链C1-C6烷基和NR7R8-C1-C6烷基的基团; R 15为无效或选自-NR 7 -C 1 -C 6烷基*，-O-C 1 -C 6烷基*，-NR 7 -C 1 -C 6烷基羰基*，-O-C 1 -C 6烷基羰基*，-NR 7 -C 1 -C 6烷氧基羰基* 和-O-C 1 -C 6烷氧基羰基*，其中*表示与-NH-Ant的连接点; R6，R7和R8独立地是氢或任选取代的直链或支链C 1 -C 6烷基; 或其药学上可接受的盐。

7. 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.

8. 发明公开

EP2836493A1 FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER 有权
标题翻译： FUNKTIONALISIERTE THIENOINDOLDERIVATE ZUR BEHANDLUNG VON KREBS
公开(公告)号：EP2836493A1
公开(公告)日：2015-02-18
申请号：EP13713180.1
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 R1 and R2 taken together form a group (D) or (G): wherein R5 is hydrogen or C1-C4 alkyl; R3 and R4 are independently hydrogen, C1-C4 alkyl or C1-C4 hydroxyalkyl; n is 0, 1 or 2; each of X is independently —O—, —S— or —NR4—; each of Y is independently —CH═ or —N═; R7 and R8 are independently hydrogen, halogen, hydroxy, C1-C4 alkoxy, cyano, —NHCOOR3, —C(NH)NH2 or —NR3R4; 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; R6 is a leaving group; A1 is null or A; L1 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障碍的式（I）或（II）的新的官能化噻吩并吲哚衍生物。本发明还涉及这些官能化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 - ; Y中的每一个独立地为-CH =或-N =; R 7和R 8独立地是氢，卤素，羟基，C 1 -C 4烷氧基，氰基，-NHCOOR 3，-C（NH）NH 2或-NR 3 R 4; 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为零或A; L1是氢或L.

9. 发明授权

EP2646456B1 PROCESS FOR THE PREPARATION OF MORPHOLINYL ANTHRACYCLINE DERIVATIVES 有权
标题翻译：用于生产吗啉衍生物
公开(公告)号：EP2646456B1
公开(公告)日：2015-01-21
申请号：EP11805950.0
申请日：2011-12-01
申请人： Nerviano Medical Sciences S.r.l.
发明人： CARUSO, Michele , LUPI, Vittoria , SALSA, Matteo
IPC分类号： C07H19/24 , A61K31/706 , A61P35/00 , C07H15/244
CPC分类号： C07H15/244 , C07H1/00 , C07H19/24

10. 发明公开

EP3215513A1 FUNCTIONALIZED MORPHOLINYL ANTHRACYCLINE DERIVATIVES 有权转让
标题翻译：功能化吗啉基蒽环衍生物
公开(公告)号：EP3215513A1
公开(公告)日：2017-09-13
申请号：EP15788447.9
申请日：2015-11-04
申请人： Nerviano Medical Sciences S.r.l.
发明人： BERIA, Italo , CARUSO, Michele , LUPI, Vittoria
IPC分类号： C07D498/14 , A61K31/5383 , A61P35/00
CPC分类号： A61K31/5383 , A61K45/06 , A61K47/542 , A61K47/545 , A61K47/64 , C07D498/14 , A61K2300/00
摘要： The present invention relates to new functionalized morpholinyl anthracycline derivatives 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 compositions containing them. The invention also relates to the use of these derivatives in the preparation of conjugates. The morpholinyl anthracycline derivatives are of the formula Ant-L-W-Z-RM (I) wherein RM is null or a reactive moiety; Z is null or a peptidic, non peptidic or hybrid—peptidic and non peptidic—linker; W is null or a self-immolative system, comprising one or more self-immolative groups; L is null or a conditionally-cleavable moiety; Ant is an anthracycline moiety selected from the formulas (II), (III), (IV) and (V), wherein the wavy line indicates the attachment to the conditionally-cleavable moiety L, or to the self-immolative system W, or to the linker Z, or to the reactive moiety RM; provided that at least one of L, W, Z and RM is not null; R1 is halogen or NR4R5; R2 is OR6, NR7R8 or an optionally substituted group selected from straight or branched C1-C4alkyl-, NR7R8-C1-C4alkyl- and R60-C1-C4alkyl-; R4 and R5 are independently hydrogen, a monosubstituted-benzyl, a disubstituted-benzyl, or an optionally substituted group selected from straight or branched C1-C6alkyl, NR7R8-C1-C6alkyl-, R60-C1-C6alkyl-, R7R8N—C1-C6alkylcarbonyl-, R60-C1-C6alkylcarbonyl-, R7R8N—C1-C6alkoxycarbonyl- and R60-C1-C6alkoxycarbonyl-; or R4 and R5, taken together with the nitrogen atom to which they are bound, form a heterocyclyl substituted with R4′, wherein R4′ is hydrogen or a group selected from straight or branched C1-C6alkyl and NR7R8-C1-C6alkyl-; R15 is null or an optionally substituted bivalent group selected from —NR7-C1-C6alkyl*, —O—C1-C6alkyl*, —NR7-C1-C6alkylcarbonyl*, —O—C1-C6alkylcarbonyl*, —NR7-C1-C6alkoxycarbonyl* and —O—C1-C6alkoxycarbonyl*, wherein * indicates the point of attachment to —NH-Ant; R6, R7 and R8 are independently hydrogen or an optionally substituted straight or branched C1-C6alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有细胞毒性活性并可用于治疗诸如癌症，细胞增殖性病症和病毒感染等疾病的新型功能化吗啉基蒽环类衍生物。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。本发明还涉及这些衍生物在制备缀合物中的用途。吗啉基蒽环类衍生物的结构式为Ant-L-W-Z-RM（I），其中RM为无效或反应性部分; Z不存在或为肽，非肽或杂化的肽和非肽 - 接头; W不存在或包含一个或多个自我牺牲基团的自毁系统; L为无效或有条件可切割的部分; Ant是选自式（II），（III），（IV）和（V）的蒽环类部分，其中波浪线表示与条件可切割的部分L或自身降解系统W的连接，或连接体Z或反应性部分RM; 条件是L，W，Z和RM中的至少一个不为空; R1是卤素或NR4R5; R 2是OR 6，NR 7 R 8或选自直链或支链C 1 -C 4烷基 - ，NR 7 R 8 -C 1 -C 4烷基 - 和R 60 -C 1 -C 4烷基 - 的任选取代的基团; R 4和R 5独立地为氢，单取代的苄基，二取代的苄基或任选取代的选自直链或支链C 1 -C 6烷基，NR 7 R 8 -C 1 -C 6烷基 - ，R 60 -C 1 -C 6烷基 - ，R 7 R 8 N -C 1 -C 6烷基羰基 - ，R60-C1-C6烷基羰基 - ，R7R8N-C1-C6烷氧基羰基 - 和R60-C1-C6烷氧基羰基 - 或者R 4和R 5与它们所连接的氮原子一起形成被R 4'取代的杂环基，其中R 4'为氢或选自直链或支链C 1 -C 6烷基和NR 7 R 8 -C 1 -C 6烷基的基团; R15为空或选自-NR7-C1-C6烷基*，-O-C1-C6烷基*，-NR7-C1-C6烷基羰基*，-O-C1-C6烷基羰基*，-NR7-C1-C6烷氧基羰基* 和-O-C1-C6烷氧基羰基*，其中*表示与-NH-Ant的连接点; R6，R7和R8独立地为氢或任选取代的直链或支链C1-C6烷基; 或其药学上可接受的盐。

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