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1. 发明授权

US5998615A Anthracyclinone derivatives 失效
标题翻译：蒽环类衍生物
公开(公告)号：US5998615A
公开(公告)日：1999-12-07
申请号：US946578
申请日：1997-10-07
申请人： Antonino Suarato , Jacqueline Lansen , Michele Caruso , Dario Ballinari , Tiziano Bandiera
发明人： Antonino Suarato , Jacqueline Lansen , Michele Caruso , Dario Ballinari , Tiziano Bandiera
IPC分类号： C07D309/10 , A61K31/12 , A61K31/122 , A61K31/135 , A61K31/165 , A61K31/35 , A61K31/351 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/65 , A61P3/00 , A61P25/00 , A61P25/28 , C07C46/00 , C07C50/36 , C07C50/38 , C07C66/00 , C07C225/32 , C07C225/34 , C07C225/36 , C07C233/31 , C07C233/36 , C07C309/65 , C07C309/73 , C07D295/108 , C07D295/112 , C07D317/26 , C07D295/116
CPC分类号： C07D295/112 , A61K31/12 , A61K31/135 , A61K31/445 , A61K31/495 , A61K31/535 , C07C225/32 , C07C225/34 , C07D295/108 , C07D317/26 , C07C2103/44
摘要： The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.
摘要翻译：本发明提供了用式（A）的蒽环类抗生素治疗淀粉样变性的新用途，其中R1，R2，R3，R4和R5是适当的取代基。一些式（A）的化合物是新的。还描述了其制备方法和含有它们的药物组合物。

2. 发明授权

US6096888A Anthracyclinone derivatives and their use in amyloidosis 失效
标题翻译：蒽环类衍生物及其在淀粉样变性中的应用
公开(公告)号：US6096888A
公开(公告)日：2000-08-01
申请号：US395202
申请日：1999-09-14
申请人： Antonino Suarato , Jacqueline Lansen , Michele Caruso , Dario Ballinari , Tiziano Bandiera
发明人： Antonino Suarato , Jacqueline Lansen , Michele Caruso , Dario Ballinari , Tiziano Bandiera
IPC分类号： C07D309/10 , A61K31/12 , A61K31/122 , A61K31/135 , A61K31/165 , A61K31/35 , A61K31/351 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/65 , A61P3/00 , A61P25/00 , A61P25/28 , C07C46/00 , C07C50/36 , C07C50/38 , C07C66/00 , C07C225/32 , C07C225/34 , C07C225/36 , C07C233/31 , C07C233/36 , C07C309/65 , C07C309/73 , C07D295/108 , C07D295/112 , C07D317/26
CPC分类号： C07D295/112 , A61K31/12 , A61K31/135 , A61K31/445 , A61K31/495 , A61K31/535 , C07C225/32 , C07C225/34 , C07D295/108 , C07D317/26 , C07C2103/44
摘要： The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.
摘要翻译：本发明提供了用式（A）的蒽环类抗生素治疗淀粉样变性的新用途，其中R1，R2，R3，R4和R5是适当的取代基。一些式（A）的化合物是新的。还描述了其制备方法和含有它们的药物组合物。

3. 发明授权

US5731313A Use of anthracyclinone derivatives in amyloidosis 失效
标题翻译：蒽环类衍生物在淀粉样变性中的应用
公开(公告)号：US5731313A
公开(公告)日：1998-03-24
申请号：US615182
申请日：1996-04-04
申请人： Antonino Suarato , Jacqueline Lansen , Michele Caruso , Dario Ballinari , Tiziano Bandiera
发明人： Antonino Suarato , Jacqueline Lansen , Michele Caruso , Dario Ballinari , Tiziano Bandiera
IPC分类号： C07D309/10 , A61K31/12 , A61K31/122 , A61K31/135 , A61K31/165 , A61K31/35 , A61K31/351 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/65 , A61P3/00 , A61P25/00 , A61P25/28 , C07C46/00 , C07C50/36 , C07C50/38 , C07C66/00 , C07C225/32 , C07C225/34 , C07C225/36 , C07C233/31 , C07C233/36 , C07C309/65 , C07C309/73 , C07D295/108 , C07D295/112 , C07D317/26
CPC分类号： C07D295/112 , A61K31/12 , A61K31/135 , A61K31/445 , A61K31/495 , A61K31/535 , C07C225/32 , C07C225/34 , C07D295/108 , C07D317/26 , C07C2103/44
摘要： The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.
摘要翻译： PCT No.PCT / EP95 / 02928 Sec。 371日期：1996年4月4日 102（e）日期1996年4月4日PCT提交1995年7月24日PCT公布。出版物WO96 / 04895 日期1996年2月22日本发明提供了用式（A）的蒽环类抗生素治疗淀粉样变性的新用途，其中R1，R2，R3，R4和R5是适当的取代基。一些式（A）的化合物是新的。还描述了其制备方法和含有它们的药物组合物。

4. 发明授权

US06194422B1 Anthracycline derivatives 失效
标题翻译：蒽环类衍生物
公开(公告)号：US06194422B1
公开(公告)日：2001-02-27
申请号：US09341703
申请日：1999-07-27
申请人： Michele Caruso , Daniela Faiardi , Tiziano Bandiera , Jacqueline Lansen , Antonino Suarato
发明人： Michele Caruso , Daniela Faiardi , Tiziano Bandiera , Jacqueline Lansen , Antonino Suarato
IPC分类号： A61K314375
CPC分类号： C07D471/08 , A61K31/435
摘要： The present invention provides imino aza-anthracyclinones and a method of treating amyloidoses using the same.
摘要翻译：本发明提供了亚氨基氮杂蒽环类和使用其的淀粉样变性的治疗方法。

5. 发明授权

US06268362B1 Amino anthracyclinone derivatives and their use in the treatment of amyloidosis 失效
标题翻译：氨基蒽环类衍生物及其在治疗淀粉样变性中的应用
公开(公告)号：US06268362B1
公开(公告)日：2001-07-31
申请号：US09622921
申请日：2000-09-07
申请人： Tiziano Bandiera , Daniele Fancelli , Mario Varasi , Michele Caruso , Jacqueline Lansen , Antonino Suarato
发明人： Tiziano Bandiera , Daniele Fancelli , Mario Varasi , Michele Caruso , Jacqueline Lansen , Antonino Suarato
IPC分类号： A61K315377
CPC分类号： C07D405/06 , C07D211/70
摘要： A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
摘要翻译：式（1）的化合物，其中R 1表示氢，羟基，式OR 7的基团，其中R 7是C 1 -C 6烷基，C 2 -C 6烯基; R2代表氢，羟基，二乙基氨基，哌啶子基，四氢吡啶基或吗啉代，独立的R 3独立地代表氢或羟基，独立地，R 4和R 5独立地表示氢，羟基或与碳原子一起代表羰基; 或R 3和R 4一起表示式（A）的基团，其中R 8和R 9表示C 1 -C 6烷基，R 5表示氢; R6代表氢或任选被甲基，甲氧基或卤素取代的苯基及其药物上可接受的盐，可用于治疗淀粉样变性。还描述了制备方法和药物组合物。

6. 发明授权

US6103700A Fluoro labelled anthracyclinone and anthracycline derivatives 失效
标题翻译：氟标记的蒽环霉素和蒽环类衍生物
公开(公告)号：US6103700A
公开(公告)日：2000-08-15
申请号：US202954
申请日：1998-12-24
申请人： Tiziano Bandiera , Daniele Fancelli , Michele Caruso , Jacqueline Lansen , Antonino Suarato
发明人： Tiziano Bandiera , Daniele Fancelli , Michele Caruso , Jacqueline Lansen , Antonino Suarato
IPC分类号： C07D295/10 , A61K31/435 , A61K31/495 , A61K31/65 , A61K49/00 , A61K49/06 , C07C225/24 , C07D295/104 , C07D295/112 , C07D295/185 , C07D295/22 , C07D295/26 , C07D309/14 , C07D405/12 , C07H15/252 , A61K31/70
CPC分类号： C07D295/185 , A61K49/06 , C07C225/24 , C07D295/112 , C07D295/26 , C07H15/252 , C07C2103/44
摘要： Compounds of formula (A), wherein R.sub.1, R.sub.2, R.sub.3, Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their preparation, and pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP97 / 03234 371 1998年12月14日第 102（e）1998年12月14日日期PCT 1997年6月18日PCT公布。公开号WO97 / 49433 日期：1997年12月31日其中R1，R2，R3，Y和Z为有机取代基的式（A）化合物可用于诊断淀粉样变性; 一些式（A）的化合物是新的。还描述了其制备方法和含有它们的药物组合物。

7. 发明授权

US5985887A Aza-anthracyclinone derivatives 失效
标题翻译：氮杂蒽环衍生物
公开(公告)号：US5985887A
公开(公告)日：1999-11-16
申请号：US496
申请日：1998-02-09
申请人： Michele Caruso , Daniela Faiardi , Tiziano Bandiera , Jacqueline Lansen , Antonino Suarato
发明人： Michele Caruso , Daniela Faiardi , Tiziano Bandiera , Jacqueline Lansen , Antonino Suarato
IPC分类号： C07D451/02 , A61K31/00 , A61K31/435 , A61P25/28 , C07D209/56 , C07D401/06 , C07D451/00 , C07D451/04 , C07D471/08 , C07H15/24 , C07D211/00 , C07D471/00
CPC分类号： C07D401/06 , C07D209/56 , C07H15/24
摘要： Compounds of formula I ##STR1## wherein X.sub.1 and X.sub.2 are C.dbd.O, C.dbd.NH or CH.sub.2, X.sub.3 is CH.sub.2, CO, CHOH, ##STR2## wherein n=2 or, 3 or C.dbd.N(R.sub.9) wherein R.sub.9 is hydroxy or amino-aryl, and each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are hydrogen, halogen or an organic residue, are useful in the treatment of amyloidosis. A process for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP96 / 03237 371日期：1998年2月9日 102（e）1998年2月9日PCT PCT 1996年7月23日PCT公布。公开号WO97 / 06165 日期：1997年2月20日其中X1和X2为C = O，C = NH或CH2，X3为CH2，CO，CHOH的式I化合物，其中n = 2或3或C = N（R9）其中R9为羟基或氨基 - 芳基，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8各自为氢，卤素或有机残基，可用于治疗淀粉样变性。还描述了其制备方法和含有它们的药物组合物。

8. 发明授权

US06589504B1 Compounds and methods for diagnosing and treating amyloid-related conditions 失效
公开(公告)号：US06589504B1
公开(公告)日：2003-07-08
申请号：US09667357
申请日：2000-09-22
申请人： Thomas J. Raub , Geri A. Sawada , Steven P. Tanis , Gregory J. Fici , Allen Edwin Buhl , Donald Bainbridge Carter , Tiziano Bandiera , Jacqueline Lansen , Cesare Pellerano , Luisa Savini
发明人： Thomas J. Raub , Geri A. Sawada , Steven P. Tanis , Gregory J. Fici , Allen Edwin Buhl , Donald Bainbridge Carter , Tiziano Bandiera , Jacqueline Lansen , Cesare Pellerano , Luisa Savini
IPC分类号： A61K5100
CPC分类号： C07D215/38 , A61K31/47 , A61K45/06 , A61K51/0455 , A61K2300/00 , A61K31/00
摘要： The invention provides methods for diagnosing and treating amyloid-related conditions and compounds useful for the same. The invention provides for detecting, imaging, monitoring, diagnosing, and treating conditions characterized by the binding or aggregation of amyloid fibrils. More particularly, the invention relates to using quinolinehydrazone compounds for diagnosing and treating amyloidotic conditions and also as an antioxidant.

9. 发明授权

US06316451B1 Heterocyclyl anthracyclinone derivatives 失效
标题翻译：杂环蒽环类衍生物
公开(公告)号：US06316451B1
公开(公告)日：2001-11-13
申请号：US09623859
申请日：2000-09-26
申请人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Jacqueline Lansen , Mario Varasi
发明人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Jacqueline Lansen , Mario Varasi
IPC分类号： C07D27742
CPC分类号： C07D417/04 , C07D233/88 , C07D277/40 , C07D277/42
摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
摘要翻译：式（1）的化合物，其中R 1是氢，羟基，式OR 5的基团，其中R 5是C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 8环烷基，卤素，可被未被取代或被C1单或二取代的氨基 C 6烷基，C 2 -C 6烯基，芳烷基，酰基或三氟乙酰基; R 2是氢，羟基，NR 6 R 7基团，其中R 6和R 7独立地表示氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或与氮原子一起代表任选取代的C 3 -C 8 杂环 R3是氢，羟基，R4是2-取代的噻唑基或咪唑基系统及其药学上可接受的盐，可用于治疗淀粉样变性。还描述了制备方法和药物组合物。

10. 发明授权

US08119641B2 1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的1H-呋喃并[3,2-C]吡唑化合物
公开(公告)号：US08119641B2
公开(公告)日：2012-02-21
申请号：US12302569
申请日：2007-05-25
申请人： Daniele Fancelli , Maurizio Pulici , Jürgen Moll , Tiziano Bandiera
发明人： Daniele Fancelli , Maurizio Pulici , Jürgen Moll , Tiziano Bandiera
IPC分类号： A61K31/4162 , A61K31/427 , A61K31/496 , C07D491/048 , C07D277/44 , C07D295/135 , C07D417/10 , C07D403/14
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, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; —R5 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，-NHZR5位于与CONH接头的邻位; -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; R3是氢或卤素原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C = O或-C（= O）NH-; -R5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。

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