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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

WO2010017035A2 INHIBITORS OF IAP 审中-公开
标题翻译： IAP抑制剂
公开(公告)号：WO2010017035A2
公开(公告)日：2010-02-11
申请号：PCT/US2009/051522
申请日：2009-07-23
申请人： GENENTECH, INC. , DUDLEY, Dannette , FLYGARE, John, A. , NDUBAKU, Chudi
发明人： DUDLEY, Dannette , FLYGARE, John, A. , NDUBAKU, Chudi
IPC分类号： C07D403/12 , C07D403/10 , A61K31/4025 , A61P35/00
CPC分类号： C07D403/12 , C07D207/16 , C07D513/04 , C07K5/0804
摘要： The invention provides novel compounds that are inhibitors of IAPs having the general formula: wherein X 1 , X 2 , X 3 , Y, A, R 1 , R 2 , R 3 , R 4 , R 4' , R 5 , R 5' , R 6 and R 6' are as described herein. The compouds of the invention may be used to induce apoptosis in cells (or sensitise cells to apoptosis) in which IAPs are overexpressed or otherwise implicated in resistance to normal apoptotic processes. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment cancers.
摘要翻译：本发明提供了新型化合物，其为具有以下通式的IAP抑制剂：其中X 1，X 2，X 3， Y，A，R 1，R 2，R 3，R 4，R 4，R 4， 4'，R 5，R 5，R 6和R 6' 如本文所述。本发明的化合物可用于诱导细胞凋亡（或使细胞对细胞凋亡敏感），其中IAP过表达或以其他方式牵涉抗正常细胞凋亡过程。因此，化合物可以以药学上可接受的组合物提供并用于治疗癌症。

3. 发明申请

WO2016044560A1 PYRROLOBENZODIAZEPINES AND ANTIBODY DISULFIDE CONJUGATES THEREOF 审中-公开
标题翻译：吡罗昔康唑及其抗体结合蛋白
公开(公告)号：WO2016044560A1
公开(公告)日：2016-03-24
申请号：PCT/US2015/050634
申请日：2015-09-17
申请人： GENENTECH, INC.
发明人： FLYGARE, John, A. , PILLOW, Thomas, H.
IPC分类号： C07D487/04 , A61K39/44 , A61P35/00
CPC分类号： C07K16/28 , A61K47/6803 , A61K47/6855 , A61K47/6889 , C07D487/04 , C07D519/00 , C07K16/18 , C07K16/2803 , C07K16/2851 , C07K16/32 , C07K2317/40 , C07K2317/522 , C07K2317/567
摘要： A compound of formula (I), wherein Y is selected from a single bond, and a group of formulae (A1) or (A2), where N shows where the group binds to the N10 of the PBD moiety.
摘要翻译：其中Y选自单键的式（I）化合物和式（A1）或（A2）的基团，其中N表示该基团与PBD部分的N10结合。

4. 发明申请

WO2013055987A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：WO2013055987A1
公开(公告)日：2013-04-18
申请号：PCT/US2012/059864
申请日：2012-10-12
申请人： SPIROGEN SÀRL , GENENTECH, INC.
发明人： FLYGARE, John, A. , GUNZNER-TOSTE, Janet, L. , PILLOW, Thomas , HOWARD, Philip, Wilson , MASTERSON, Luke
IPC分类号： A61K47/48 , C07D487/04 , C07D519/00 , A61P35/00
CPC分类号： A61K47/48384 , A61K47/6803 , A61K47/6849 , C07D487/04 , C07D519/00
摘要： A conjugate of formula (A): the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R 2 is independently selected from H, OH, =0, =CH 2 , CN, R, OR, =CH-R D , =C(R D ) 2 , 0-S0 2 -R, C0 2 R and COR, and optionally further selected from halo or dihalo; where R D is independently selected from R, C0 2 R, COR, CHO, C0 2 H, and halo; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', NO 2, Me 3 Sn and halo; R 7 is independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', N02, Me 3 Sn and halo; Y is selected from a single bond, and a group of formulae A1 or A2: where N shows where the group binds to the N10 of the PBD moiety; R L1 and R L2 are independently se!ected from H and methyl, or together with the carbon atom to which they are bound form a cyclopropylene group; CBA represents a cell binding agent; Q is independently selected from O, S and NH; R 11 is either H, or R or, where Q is O, S0 3 M, where M is a metal cation; R and R' are each independently selected from optionally substituted C 1-12 alkyl, C 3-20 heterocyclyl and C 5-20 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 Z-metfibered heteracyciie ring; wherein R 12 R 16 , R 19 and R 17 are as defined for R 2 , R 6 , R 9 and R 7 respectively: wherein R" is a C 3-12 alky!ene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H}; NMe and/or aromatic rings, e.g. benzene or pyridine, which rings are optional y substituted; X and X' are independently selected from O, S and N(H).
摘要翻译：式（A）的缀合物：虚线表示在C1和C2或C2和C3之间任选存在双键; R2独立地选自H，OH，= O，= CH2，CN，R，OR，= CH-RD，= C（RD）2,0-SO2-R，CO 2 R和COR，并且任选地进一步选自卤素或二卤; 其中RD独立地选自R，CO 2 R，COR，CHO，CO 2 H和卤素; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; Y选自单键和式A1或A2的基团：其中N表示基团结合PBD部分的N10的位置; RL1和RL2独立地由H和甲基取代，或与它们所结合的碳原子一起形成环亚丙基; CBA代表细胞结合剂; Q独立地选自O，S和NH; R 11是H或R，或其中Q是O，SO 3 M，其中M是金属阳离子; R和R'各自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，并且任选地相对于NRR'基团，R和R'与它们所连接的氮原子一起形成任选取代的4-，5- 6-或Z-元纤维杂化环; 其中R 12 R 16，R 19和R 17分别如对R 2，R 6，R 9和R 7所定义：其中R“为C 3-12烷基，该链可以被一个或多个杂原子（例如O，S，N H}; NMe和/或芳环，例如苯或吡啶，该环是任选的y取代的; X和X'独立地选自O，S和N（H）。

5. 发明申请

WO2010080478A1 COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：化合物和使用方法
公开(公告)号：WO2010080478A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068400
申请日：2009-12-17
申请人： GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
发明人： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
IPC分类号： A61K31/535
CPC分类号： C07D417/14 , C07D417/12 , C07D487/04
摘要： In one aspect, the present invention provides for a compound of Formula (I) in which, the variables X 1 , X 2a , X 2b , X 2c , R 1 , B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula (I) as well as methods for using compounds of Formula (I) for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
摘要翻译：一方面，本发明提供式（I）的化合物，其中变量X1，X2a，X2b，X2c，R1，B，L，E，A和下标n如本文所定义。在另一方面，本发明提供包含式（I）化合物的药物组合物以及使用式（I）化合物治疗由表达特征的疾病和病症（例如癌症，血小板增多症等）的方法或过度表达Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。

6. 发明申请

WO2014159981A2 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：WO2014159981A2
公开(公告)日：2014-10-02
申请号：PCT/US2014/025564
申请日：2014-03-13
申请人： SPIROGEN SARL , GENENTECH, INC.
发明人： HOWARD, Philip, Wilson , FLYGARE, John, A. , PILLOW, Thomas , WEI, Binqing
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: R 2 is, where R 36a and R 36b are independently selected from H, F, C 1-4 saturated aikyl, C 2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C 1-4 alkyl amido and C 1-4 alkyl ester; or, when one of R 36a and R 36b is H, the other is selected from nitrile and a C 1-4 aikyl ester; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', NO 2 , Me 3 Sn and halo; R 7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', NO 2 , Me 3 Sn 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; R A4 is a C 1-6 alkylene group; either (a) R 10 is H, and R 11 is OH, OR A , where R A is C 1-4 aikyl; or (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 OSO z M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R' are each independently selected from optionally substituted C 1-12 alkyl, C 3-20 heterocyclyl and C 5-20 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 R 16 , R 17 , R 19 , R 20 , R 21 and R 22 are as defined for R 6 , R 7 , R 9 , R 10 , R 11 and R 2 respectively; wherein Z is CH or N; wherein T and T' are independently selected from a single bond or a C 1-9 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).
摘要翻译：式（A）的共轭化合物：其中：R 2为，其中R 36a和R 36b独立地选自H，F，C 1-4饱和的烷基，C 2-3链烯基，该烷基和烯基任选被选自C 1 -4-烷基酰氨基和C 1-4烷基酯; 或者当R 36a和R 36b之一为H时，另一个选自腈和C 1-4烷基酯; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; Y选自式A1，A2，A3，A4，A5和A6：L是连接到细胞结合剂的连接体; CBA是细胞结合剂; n为0〜48的整数; RA4是C1-6亚烷基; （a）R 10是H，R 11是OH，ORA，其中RA是C 1-4烷基; 或（b）R 10和R 11在与它们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OSOzM，其中z为2或3，M为单价药学上可接受的阳离子; R和R'各自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，并且任选地相对于基团NRR'，R和R'与它们所在的氮原子一起连接形成任选取代的4-，5-，6-或7-元杂环; 其中R16，R17，R19，R20，R21和R22分别如R6，R7，R9，R10，R11和R2所定义; 其中Z是CH或N; 其中T和T'独立地选自单键或C1-9亚烷基，该链可以被一个或多个杂原子间隔。 O，S，N（H），NMe，条件是X和X'之间的最短原子链中的原子数为3至12个原子; X和X'独立地选自O，S和N（H）。

7. 发明申请

WO2010080503A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：杂环化合物和使用方法
公开(公告)号：WO2010080503A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068496
申请日：2009-12-17
申请人： GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , CZABOTAR, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , HASVOLD, Lisa, A. , PETROS, Andrew, M. , SOUERS, Andrew, J. , TAO, Zhi-Fu , WANG, Le , WANG, Xilu , DESHAYES, Kurt
发明人： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , CZABOTAR, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , HASVOLD, Lisa, A. , PETROS, Andrew, M. , SOUERS, Andrew, J. , TAO, Zhi-Fu , WANG, Le , WANG, Xilu , DESHAYES, Kurt
IPC分类号： A01N43/00
CPC分类号： C07D417/14 , C07D471/06 , C07D473/00 , C07D487/04 , C07D495/04 , C07D513/04 , C07D513/06
摘要： In one aspect, the present invention provides for a compound of Formula I; in which the variable X 1a , X 1b , X 1c , X 1d , Q, A, R 1 , B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
摘要翻译：一方面，本发明提供式I的化合物; 其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n具有如本文所述的含义。另一方面，本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症（例如癌症，血小板增多症等）的方法的Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。

8. 发明申请

WO2006069063A1 PYRROLIDINE INHIBITORS OF IAP 审中-公开
标题翻译：吡咯啉抑制剂IAP
公开(公告)号：WO2006069063A1
公开(公告)日：2006-06-29
申请号：PCT/US2005/046161
申请日：2005-12-19
申请人： GENENTECH, INC. , COHEN, Frederick , TSUI, Vickie Hsiao-wei , LY, Cuong , FLYGARE, John, A.
发明人： COHEN, Frederick , TSUI, Vickie Hsiao-wei , LY, Cuong , FLYGARE, John, A.
IPC分类号： C07D417/04 , C07D417/14 , A61K31/427 , A61P35/00
CPC分类号： C07D471/04 , C07D417/04 , C07D417/14
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I), wherein A,Q,X 1 ,X 2 ,Y,R 1 ,R 2 ,R 3 ,R 4 ,R 4’ ,R 5 ,R 6 and R 6’ are described herein.
摘要翻译：本发明提供了新的IAP抑制剂，其可用作治疗恶性肿瘤的治疗剂，其中化合物具有通式（I），其中A，Q，X 1，X 2， >，Y，R _{1 ，R _{2 ，R _{3 ，R _{4 ，R _{4' 本文描述了R 5，R 6和R 6'。}}}}}

9. 发明申请

WO2004072641A1 COMPOSITIONS AND METHODS FOR ENHANCING APOPTOSIS 审中-公开
标题翻译：组合物和增强抗病毒的方法
公开(公告)号：WO2004072641A1
公开(公告)日：2004-08-26
申请号：PCT/US2003/003799
申请日：2003-02-07
申请人： GENENTECH, INC.
发明人： FAIRBROTHER, Wayne, J. , DESHAYES, Kurt , FISCHER, Saloumeh , FLYGARE, John, A. , FRANKLIN, Matthew, C. , VUCIC, Domagoj
IPC分类号： G01N33/53
CPC分类号： C07K14/4747 , A61K38/00 , C07K5/0806 , C07K5/0827 , C07K5/1008 , G01N2500/04 , G01N2510/00
摘要： The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same.
摘要翻译：本发明涉及用于增强哺乳动物细胞凋亡的物质组合物，以及使用这些物质组合物的方法。

10. 发明公开

EP2968596A2 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 有权
标题翻译：吡咯并苯并二氮杂及其偶联物
公开(公告)号：EP2968596A2
公开(公告)日：2016-01-20
申请号：EP14761432.5
申请日：2014-03-13
申请人： MEDIMMUNE LIMITED , Genentech, Inc.
发明人： HOWARD, Philip, Wilson , FLYGARE, John, A. , PILLOW, Thomas , WEI, Binqing
IPC分类号： A61K47/48 , A61K31/5517 , 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).
摘要翻译：式（A）的偶联化合物：其中：R 2是，其中：R 36a和R 36b独立地选自H，F，C 1-4饱和烷基，C 2-3烯基，其中烷基和烯基任选被选自C 1-4烷基酰胺基和C 1-4烷基酯的基团; 或者当R 36a和R 36b中的一个是H时，另一个选自腈和C 1-4烷基酯; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; Y选自式A1，A2，A3，A4，A5和A6：L是与细胞结合剂连接的接头; CBA是细胞结合剂; n是在0至48范围内选择的整数; R A4是C 1-6亚烷基; （a）R 10为H，且R 11为OH，OR A，其中R A为C 1-4烷基; 或（b）R 10和R 11在它们所键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OSO zM，其中z为2或3且M为单价药学上可接受的阳离子; R和R'各自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，并且任选地与基团NRR'，R和R'一起与氮原子一起形成它们连接形成任选取代的4-，5-，6-或7-元杂环; 其中R 16，R 17，R 19，R 20，R 21和R 22分别与R 6，R 7，R 9，R 10，R 11和R 2的定义相同; 其中Z是CH或N; 其中T和T'独立地选自单键或C 1-9亚烷基，该链可被一个或多个杂原子例如 O，S，N（H），NMe，条件是在X和X'之间的最短原子链中的原子数是3至12个原子; X和X'独立地选自O，S和N（H）。

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