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1. 发明申请

WO2011130616A1 PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的吡罗昔康唑
公开(公告)号：WO2011130616A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032668
申请日：2011-04-15
申请人： SPIROGEN LIMITED , SEATTLE GENETICS, INC. , HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
IPC分类号： C07D519/00 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04 , A61K47/6803 , A61K47/6849 , A61K47/6851 , C07D519/00
摘要： Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
摘要翻译：吡咯并苯并二氮杂二聚体I在一个单体单元上具有C2-C3双键和C2位上的芳基，C2-C3双键和C2位上的共轭双键或三键或C2位烷基在其他单体单元上，以及这些化合物的共轭物。

2. 发明申请

WO2011130598A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：WO2011130598A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032632
申请日：2011-04-15
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , FLYGARE, John, A. , GUNZNER, Janet, L. , POLAKIS, Paul , POLSON, Andrew , RAAB, Helga, E. , SPENCER, Susan, D.
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , FLYGARE, John, A. , GUNZNER, Janet, L. , POLAKIS, Paul , POLSON, Andrew , RAAB, Helga, E. , SPENCER, Susan, D.
IPC分类号： A61K47/48 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04 , A61K47/6849 , A61K47/6855 , A61K47/6869 , C07D519/00
摘要： Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
摘要翻译：公开了用于制备作为通过N10位置连接的PBD分子的缀合物的缀合物和化合物，以及缀合物用于治疗包括癌症在内的增殖性疾病的用途。

3. 发明申请

WO2011128650A1 INTERMEDIATES USEFUL FOR THE SYNTHESIS OF PYRROLOBENZODIAZEPINES 审中-公开
标题翻译：中间体用于合成紫杉酚的中间体
公开(公告)号：WO2011128650A1
公开(公告)日：2011-10-20
申请号：PCT/GB2011/000588
申请日：2011-04-15
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud
IPC分类号： C07D207/20 , C07D207/22 , C07D207/24 , C07D487/04
CPC分类号： C07D207/24 , C07D207/20 , C07D207/22 , C07D487/04
摘要： A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
摘要翻译：式（I）化合物：其基本上不含任何相应的式（IB）化合物：制备此类化合物的方法以及该化合物的进一步转化。

4. 发明申请

WO2013053873A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2013053873A1
公开(公告)日：2013-04-18
申请号：PCT/EP2012/070233
申请日：2012-10-12
申请人： SPIROGEN SÀRL , SEATTLE GENETICS, INC.
发明人： HOWARD, Philip Wilson , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick
IPC分类号： C07D487/04 , C07D519/00 , A61K31/5517 , A61P35/00
CPC分类号： A61K47/48338 , A61K47/48092 , A61K47/549 , A61K47/65 , C07D487/04 , C07D519/00 , C07H15/22
摘要： A compound with the formula (I), wherein: R 2 is of formula (II), where X is selected from the group comprising: OH, SH, CO 2 H, COH, N=C=O, NHNH 2 , CONHNH 2 , formula (A), formula (B), NHR N , wherein R N is selected from the group comprising H and C 1-4 alkyl; R C1 , R C2 and R C3 are independently selected from H and unsubstituted C 1-2 alkyl; and either: R 12 is selected from the group consisting of: (ia) C 5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C 1-7 alkyl, C 3-7 heterocyclyl and bis-oxy-C 1-3 alkylene; (ib) C 1-5 saturated aliphatic alkyl; (ic) C 3-6 saturated cycloalkyl; (id) formula (C), wherein each of R 21 , R 22 and R 23 are independently selected from H, C 1-3 saturated alkyl, C 2-3 alkenyl, C 2-3 alkynyl and cyclopropyl, where the total number of carbon atoms in the R 12 group is no more than 5; (ie) formula (D), wherein one of R 25a and R 25b is H and the other is selected from: phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; and (if) formula (E), where R 24 is selected from: H; C 1-3 saturated alkyl; C 2-3 alkenyl; C 2-3 alkynyl; cyclopropyl; phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', nitro, Me 3 Sn and halo; where R and R' are independently selected from optionally substituted C 1-12 alkyl, C 3-20 heterocyclyl and C 5-20 aryl groups; R 7 is selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NHRR', nitro, Me 3 Sn and halo; either: (a) R 10 is H, and R 11 is OH, OR A , where R A is C 1-4 alkyl; (b) R 10 and R 11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R 10 is H and R 11 is SO z M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R" is a C 3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, and/or aromatic rings; Y and Y' are selected from O, S, or NH; R 6' , R 7' , R 9' are selected from the same groups as R 6 , R 7 and R 9 respectively and R 10' and R 11' are the same as R 10 and R 11 , wherein if R 11 and R 11' are SO z M, M may represent a divalent pharmaceutically acceptable cation.
摘要翻译：具有式（I）的化合物，其中：R 2为式（II），其中X选自OH，SH，CO 2 H，COH，N = C = O，NHNH 2，CONHNH 2，式（A），式（B），NHRN，其中RN选自H和C 1-4烷基; RC1，RC2和RC3独立地选自H和未取代的C 1-2烷基; R 12选自：（ia）C5-10芳基，任选被一个或多个选自以下的取代基取代：卤素，硝基，氰基，醚，C 1-7烷基，C 3-7 杂环基和双 - 氧基-C 1-3亚烷基; （ib）C 1-5饱和脂肪族烷基; （ic）C3-6饱和环烷基; （id）式（C），其中R 21，R 22和R 23各自独立地选自H，C 1-3饱和烷基，C 2-3烯基，C 2-3炔基和环丙基，其中R 12中的总碳原子数组别不超过5; （即）式（D），其中R25a和R25b之一是H，另一个选自：苯基，该苯基任选被选自卤素，甲基，甲氧基的基团取代; 吡啶基; 和噻吩基; 和（如果）式（E），其中R 24选自：H; C1-3饱和烷基; C2-3烯基; C2-3炔基; 环丙基; 苯基，该苯基任选被选自卤素，甲基，甲氧基的基团取代; 吡啶基; 和噻吩基; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，硝基，Me 3 Sn和卤素; 其中R和R'独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基; R 7选自H，R，OH，OR，SH，SR，NH 2，NHR，NHRR'，硝基，Me 3 Sn和卤素; 或者：（a）R 10是H，R 11是OH，ORA，其中RA是C 1-4烷基; （b）R 10和R 11在它们所结合的氮原子和碳原子之间形成氮 - 碳双键; 或（c）R 10为H且R 11为SOzM，其中z为2或3，M为一价药学上可接受的阳离子; R“是C3-12亚烷基，该链可以被一个或多个杂原子和/或芳环中断; Y和Y'选自O，S或NH; R 6'，R 7'，R 9' 选自与R6，R7和R9分别相同的基团，R10'和R11'与R10和R11相同，其中如果R11和R11'是SOzM，M可以表示二价药学上可接受的阳离子。

5. 发明授权

EP2751111B1 Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases 有权
标题翻译：不对称性双 - （5H-吡咯并[2,1-c] [1,4]苯并二氮杂_-5-on）衍生自体免疫印度尼西亚
公开(公告)号：EP2751111B1
公开(公告)日：2017-04-26
申请号：EP12772782.4
申请日：2012-10-12
申请人： MedImmune Limited , Seattle Genetics, Inc.
发明人： HOWARD, Philip Wilson , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick
IPC分类号： C07D487/04 , C07D519/00 , A61K31/5517 , A61P35/00
CPC分类号： A61K47/48338 , A61K47/48092 , A61K47/549 , A61K47/65 , C07D487/04 , C07D519/00 , C07H15/22

6. 发明公开

EP2558475A1 PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES 审中-公开
标题翻译： EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN
公开(公告)号：EP2558475A1
公开(公告)日：2013-02-20
申请号：EP11716755.1
申请日：2011-04-15
申请人： Spirogen Sàrl , Seattle Genetics, Inc.
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
IPC分类号： C07D519/00 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04 , A61K47/6803 , A61K47/6849 , A61K47/6851 , C07D519/00
摘要： Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit are claimed as are conjugates of these compounds.
摘要翻译：吡咯并苯并二氮杂二聚体I在一个单体单元上具有C2-C3双键和C2位上的芳基，C2-C3双键和C2位上的共轭双键或三键或C2位烷基作为这些化合物的共轭物，要求保护其它单体单元。

7. 发明公开

EP2751111A1 PYRROLOBENZODIAZEPINES 有权
标题翻译：非对称型双（5H-吡咯并[2,1-C] [1,4]苯并二氮杂-5-酮），用于增殖性疾病或自身免疫疾病的治疗衍生物
公开(公告)号：EP2751111A1
公开(公告)日：2014-07-09
申请号：EP12772782.4
申请日：2012-10-12
申请人： Spirogen Sàrl , Seattle Genetics, Inc.
发明人： HOWARD, Philip Wilson , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick
IPC分类号： C07D487/04 , C07D519/00 , A61K31/5517 , A61P35/00
CPC分类号： A61K47/48338 , A61K47/48092 , A61K47/549 , A61K47/65 , C07D487/04 , C07D519/00 , C07H15/22
摘要： A compound with the formula (I), wherein: R
2 is of formula (II), where X is selected from the group comprising: OH, SH, CO
2 H, COH, N=C=O, NHNH
2 , CONHNH
2 , formula (A), formula (B), NHR
N , wherein R
N is selected from the group comprising H and C
1-4 alkyl; R
C1 , R
C2 and R
C3 are independently selected from H and unsubstituted C
1-2 alkyl; and either: R
12 is selected from the group consisting of: (ia) C
5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C
1-7 alkyl, C
3-7 heterocyclyl and bis-oxy-C
1-3 alkylene; (ib) C
1-5 saturated aliphatic alkyl; (ic) C
3-6 saturated cycloalkyl; (id) formula (C), wherein each of R
21 , R
22 and R
23 are independently selected from H, C
1-3 saturated alkyl, C
2-3 alkenyl, C
2-3 alkynyl and cyclopropyl, where the total number of carbon atoms in the R
12 group is no more than 5; (ie) formula (D), wherein one of R
25a and R
25b is H and the other is selected from: phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; and (if) formula (E), where R
24 is selected from: H; C
1-3 saturated alkyl; C
2-3 alkenyl; C
2-3 alkynyl; cyclopropyl; phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; R
6 and R
9 are independently selected from H, R, OH, OR, SH, SR, NH
2 , NHR, NRR', nitro, Me
3 Sn and halo; where R and R' are independently selected from optionally substituted C
1-12 alkyl, C
3-20 heterocyclyl and C
5-20 aryl groups; R
7 is selected from H, R, OH, OR, SH, SR, NH
2 , NHR, NHRR', nitro, Me
3 Sn and halo; either: (a) R
10 is H, and R
11 is OH, OR
A , where R
A is C
1-4 alkyl; (b) R
10 and R
11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R
10 is H and R
11 is SO
z M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R" is a C
3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, and/or aromatic rings; Y and Y' are selected from O, S, or NH; R
6' , R
7' , R
9' are selected from the same groups as R
6 , R
7 and R
9 respectively and R
10' and R
11' are the same as R
10 and R
11 , wherein if R
11 and R
11' are SO
z M, M may represent a divalent pharmaceutically acceptable cation.

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