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. 发明授权

US09102704B2 Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines 有权
标题翻译：用于制备吡咯并苯并二氮杂卓的合成方法和中间体
公开(公告)号：US09102704B2
公开(公告)日：2015-08-11
申请号：US14351166
申请日：2012-10-12
申请人： SPIROGEN SÀRL
发明人： Philip Wilson Howard , Arnaud Tiberghien
IPC分类号： C07K5/062 , C07F7/18 , C07D401/12 , C07D409/12 , C07D413/12 , C07D487/04 , C07D207/20 , C07D207/24 , C07D207/27 , C07D519/00
CPC分类号： C07K5/06052 , C07D207/20 , C07D207/24 , C07D207/27 , C07D401/12 , C07D409/12 , C07D413/12 , C07D487/04 , C07D519/00 , C07F7/1804 , Y02P20/55
摘要： A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(═O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(═O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(═O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.
摘要翻译：式I的化合物，其中：R 7选自：ORA，其中RA选自C 1-4饱和烷基，任选被苯基取代，可以带有氯取代基，吡啶基和呋喃基; 氯 NH2; -CH 2 -O-C（= O）Me; R8是OProto，其中Proto是与Rc正交的硅基氧保护基; R9选自H，甲基和甲氧基; R 5选自CF 3，（CF 2）3 CF 3，CH 3和（式2），R c选自：（i）C（= O）-ORC1，其中RC1为饱和C 1-4烷基; （ii）-CH 2 -O-C（= O）RC 2，其中RC 2是甲基或苯基; （iii）CH2-O-Si-（RSi1）（RSi2）（RSi3），其中RSi1，RSi2，RSi3独立地选自C1-6饱和烷基和苯基; 和（iv）C（-YRC3）（-YRC4），其中每个Y独立地为O或S，并且其中RC3和RC4独立地为饱和C 1-4烷基，或一起形成C 2-3亚烷基。

2. 发明申请

US20150126495A1 PYRROLOBENZODIAZEPINES 有权
公开(公告)号：US20150126495A1
公开(公告)日：2015-05-07
申请号：US14397843
申请日：2013-04-30
申请人： UCL BUSINESS PLC , SPIROGEN SÀRL
发明人： Philip Wilson Howard , David Edwin Thurston , Khondaker Mirazur Rahman , Peter William Taylor
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound of formula (I) or a salt or solvate thereof, wherein the dotted double bond indicates the presence of a single or double bond between C2 and C3; R2 is selected from —H, —OH, ═O, ═CH2, —CN, —R, OR, halo, dihalo, ═CHR, ═CHRR′, —O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, nitro, Me3Sn and halo; where R and R′ are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and QRQ respectively, where Q is selected from O, S and NH and RQ is H or C1-7 alkyl or H and SOxM, where x is 2 or 3, and M is a monovalent pharmaceutically acceptable cation; A is selected from (A1), (A2), (A3), (A4) or (A5) where X1 and Y1 are selected from: CH and NH; CH and NMe; N and NMe; CH and S; N and S; N and O; and CH and O, respectively; X2 and Y2 are selected from: CH and NH; CH and NMe; N and NMe; CH and S; N and S; N and O; and CH and O, respectively; Z1 is selected from O and S; Z2 is selected from CH and N; F is selected from a single bond and -(E-F1)m-; each E is independently selected from a single bond, and —C(═O)—NH—; each F1 is independently a C3-20 heteroarylene group; m is 1, 2 or 3; G is selected from hydrogen, C1-4alkyl, —C(═O)—O—C1-4alkyl, —(CH2)n—C3-20 heterocycloalkyl, and —O—(CH2)n—C3-20 heterocycloalkyl group; each n is 0-4; provided that A2 is not A2′, where X1 and Y1 of A2′ are selected from: CH and NMe; COH and NMe; CH and S; N and NMe; N and S, respectively; and provided that A3 is not A3′, where X2 and Y2 of A3′ are selected from: CH and NMe; COH and NMe; CH and S; N and NMe; N and S, respectively; B is either a single bond or (B1), where X and Y of B1 are selected from: CH and NMe; COH and NMe; CH and S; N and NMe; N and S, respectively; and R1 is C1-4 alkyl.

3. 发明授权

US09821074B2 Pyrrolobenzodiazepines and conjugates thereof 有权
公开(公告)号：US09821074B2
公开(公告)日：2017-11-21
申请号：US14208374
申请日：2014-03-13
申请人： Spirogen Sàrl , Genentech, Inc.
发明人： Philip Wilson Howard , John A. Flygare , Thomas Pillow , Binqing Wei
IPC分类号： A61K47/48 , A61K31/5517 , C07D519/00 , C07D487/04
CPC分类号： A61K47/6869 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , A61P35/00 , C07D487/04 , C07D487/16 , C07D519/00
摘要： Conjugate compounds of formula (A): wherein: R2 is where R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 alkyl ester; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R′ are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR′, R and R′ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring; wherein R16, R17, R19, R20, R21 and R22 are as defined for R6, R7, R9, R10, R11 and R2 respectively; wherein Z is CH or N; wherein T and T′ are independently selected from a single bond or a C1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X′ is 3 to 12 atoms; and X and X′ are independently selected from O, S and N(H).

4. 发明授权

US09266894B2 Pyrrolobenzodiazepines as unsymmetrical dimeric PBD compounds for inclusion in targeted conjugates 有权
公开(公告)号：US09266894B2
公开(公告)日：2016-02-23
申请号：US14346006
申请日：2012-09-20
申请人： SPIROGEN SÀRL
发明人： Philip Wilson Howard
IPC分类号： C07D487/04 , C07D519/00 , A61K47/48 , C07K5/062 , C07K5/065 , C07K5/078
摘要： A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.

5. 发明申请

US20150344482A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 有权
标题翻译：。。。。。。。。。。。。
公开(公告)号：US20150344482A1
公开(公告)日：2015-12-03
申请号：US14654065
申请日：2013-12-20
申请人： SPIROGEN SÀRL
发明人： Philip Wilson HOWARD
IPC分类号： C07D487/04 , A61K31/5517 , A61K47/48
CPC分类号： C07D487/04 , A61K31/5517 , A61K47/6801 , A61K47/6851 , A61K47/6889
摘要： A compound with the formula I: and salts and solvates thereof.
摘要翻译：具有式I的化合物及其盐和溶剂化物。

6. 发明申请

US20150158869A1 PYRROLOBENZODIAZEPINES AS UNSYMMETRICAL DIMERIC PBD COMPOUNDS FOR INCLUSION IN TARGETED CONJUGATES 有权
标题翻译：作为非对称双极性PBD化合物，用于包含在目标结合物中的吡咯烷酮
公开(公告)号：US20150158869A1
公开(公告)日：2015-06-11
申请号：US14346006
申请日：2012-09-20
申请人： SPIROGEN SÀRL
发明人： Philip Wilson Howard
IPC分类号： C07D487/04 , A61K47/48 , C07K5/062
CPC分类号： C07D487/04 , A61K47/54 , A61K47/55 , A61K47/60 , C07D519/00 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06156 , C07K5/06165
摘要： A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.
摘要翻译：具有式I的化合物，其中：R2为式II，其中Q选自OH，SH和NRN，RN选自H，甲基和乙基，以及由该化合物制备的药物接头和药物偶联物。

7. 发明申请

US20150133435A1 PYRROLOBENZODIAZEPINES 有权
标题翻译： PYRROBOBENZODIAZEPINES
公开(公告)号：US20150133435A1
公开(公告)日：2015-05-14
申请号：US14397842
申请日：2013-04-30
申请人： SPIROGEN SÀRL , UCL BUSINESS PLC
发明人： Philip Wilson Howard , David Edwin Thurston , Khondaker Mirazur Rahman
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolobenzodiazepine (PBDs) having a (1-methyl-1H-pyrrol-3-yl)phenyl based amino residue were found to be highly effective compounds having improved cytotoxicity ad DNA binding properties.
摘要翻译：发现具有（1-甲基-1H-吡咯-3-基）苯基氨基残基的吡咯并苯并二氮杂（PBD）是具有改善的细胞毒性和DNA结合特性的高效化合物。

8. 发明申请

US20140286970A1 PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES 有权
标题翻译：。。IA IA。。。。。。。。。。
公开(公告)号：US20140286970A1
公开(公告)日：2014-09-25
申请号：US14351168
申请日：2012-10-12
申请人： SEATTLE GENETICS, INC. , SPIROGEN SÀRL
发明人： Scott Jeffrey , Patrick Burke , Philip Wilson Howard
IPC分类号： A61K47/48 , C07D471/04
CPC分类号： A61K31/5517 , A61K47/55 , A61K47/6803 , A61K47/6849 , A61K47/6889 , A61P35/00 , C07D487/04
摘要： A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of formula wherein: (a) R10 is H, and R11 is OH, ORA, where RA is saturated C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is S02M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation, or both M together are a divalent pharmaceutically acceptable cation.
摘要翻译：选自下式的化合物或其药学上可接受的盐或溶剂合物或其结合物其中：（a）R 10是H，R 11是OH，ORA，其中RA是饱和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SO 2 M，其中z为2或3，M为一价药学上可接受的阳离子，或两者均为二价药学上可接受的阳离子。

9. 发明申请

US20150315196A1 UNSYMMETRICAL PYRROLOBENZODIAZEPINES-DIMERS FOR USE IN THE TREATMENT OF PROLIFERATIVE AND AUTOIMMUNE DISEASES 有权
标题翻译：用于治疗增生性和自身免疫性疾病的非对称吡咯烷酮双胍
公开(公告)号：US20150315196A1
公开(公告)日：2015-11-05
申请号：US14654070
申请日：2013-12-20
申请人： SPIROGEN SÀRL
发明人： Philip Wilson HOWARD
IPC分类号： C07D487/04 , C07K5/062 , A61K47/22
CPC分类号： C07D487/04 , A61K47/22 , C07K5/06026
摘要： A compound of formula I: or a pharmaceutically acceptable salt or solvate thereof.
摘要翻译：式I化合物或其药学上可接受的盐或溶剂合物。

10. 发明申请

US20140275522A1 SYNTHESIS METHOD AND INTERMEDIATES USEFUL IN THE PREPARATION OF PYRROLOBENZODIAZEPINES 有权
标题翻译：合成方法和中间体有用于制备吡咯烷酮
公开(公告)号：US20140275522A1
公开(公告)日：2014-09-18
申请号：US14351166
申请日：2012-10-12
申请人： SPIROGEN SÀRL
发明人： Philip Wilson Howard , Arnaud Tiberghien
IPC分类号： C07K5/062 , C07F7/18
CPC分类号： C07K5/06052 , C07D207/20 , C07D207/24 , C07D207/27 , C07D401/12 , C07D409/12 , C07D413/12 , C07D487/04 , C07D519/00 , C07F7/1804 , Y02P20/55
摘要： A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(═O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(═O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(═O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.
摘要翻译：式I的化合物，其中：R 7选自：ORA，其中RA选自C 1-4饱和烷基，任选被苯基取代，可以带有氯取代基，吡啶基和呋喃基; 氯 NH2; -CH 2 -O-C（= O）Me; R8是OProto，其中Proto是与Rc正交的硅基氧保护基; R9选自H，甲基和甲氧基; R 5选自CF 3，（CF 2）3 CF 3，CH 3和（式2），R c选自：（i）C（= O）-ORC1，其中RC1是饱和C 1-4烷基; （ii）-CH 2 -O-C（= O）RC 2，其中RC 2是甲基或苯基; （iii）CH2-O-Si-（RSi1）（RSi2）（RSi3），其中RSi1，RSi2，RSi3独立地选自C1-6饱和烷基和苯基; 和（iv）C（-YRC3）（-YRC4），其中每个Y独立地为O或S，并且其中RC3和RC4独立地为饱和C 1-4烷基，或一起形成C 2-3亚烷基。

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