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1. 发明申请

US20160279261A1 PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF 审中-公开
公开(公告)号：US20160279261A1
公开(公告)日：2016-09-29
申请号：US15182429
申请日：2016-06-14
申请人： Ho Huat Lee , Moana Tercel , Genentech, Inc.
发明人： Ho Huat Lee , Moana Tercel , John A. Flygare , Janet Gunzner-Toste , Thomas H. Pillow , Brian Safina , Leanna Staben , Vishal Verma , BinQing Wei , Guiling Zhao
IPC分类号： A61K47/48 , C07K16/30 , C07K16/28
CPC分类号： C07K16/30 , A61K47/6803 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07K16/28 , C07K16/2851 , C07K16/2863 , C07K2317/24 , C07K2317/56 , C07K2317/76
摘要： This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.

2. 发明授权

US06251933B1 Seco precursors of cyclopropylindolines and their use as prodrugs 失效
标题翻译：环丙基吲哚啉的山梨醇前体及其作为前药的用途
公开(公告)号：US06251933B1
公开(公告)日：2001-06-26
申请号：US09319771
申请日：1999-06-11
申请人： William Alexander Denny , Moana Tercel , Graham John Atwell , Jared Milbank
发明人： William Alexander Denny , Moana Tercel , Graham John Atwell , Jared Milbank
IPC分类号： A61K31404
CPC分类号： C07D403/12 , C07D209/10 , C07D209/12
摘要： A compound which is a 6-substituted seco indoline of the formula (I): wherein: X is halogen or OSO2R where R represents H or C1-5 alkyl optionally substituted with from 1 to 4 hydroxyl, acid (COOH) or amino groups which amino may be optionally substituted by one or two C1-5 alkyl groups; Y is N02, N3, NHOH, NHR, NRR, N═NR, N(O)RR, SR or SSR, where R is defined as above, but that in the case where Y is SSR or N═NR, then R can also be another moiety of formula (I); or Y is a group of formula:
摘要翻译：化合物，其为式（I）的6-取代的仲二氢吲哚：其中：X为卤素或OSO2R，其中R为H或任选被1至4个羟基，酸（COOH）或氨基取代的C 1-5烷基，氨基可以任选地被一个或两个C 1-5烷基取代; Y是N 2，N 3，NHOH，NHR，NRR，N = NR，N（O）RR，SR或SSR，其中R如上所定义，在Y是SSR或N = NR的情况下，R也可以是式（I）的另一部分;或Y是下式的基团：

3. 发明授权

US5872129A Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents 失效
标题翻译：硝基苄基芥末季盐及其作为缺氧选择性细胞毒性剂的用途
公开(公告)号：US5872129A
公开(公告)日：1999-02-16
申请号：US903937
申请日：1997-07-31
申请人： William Alexander Denny , William Robert Wilson , Moana Tercel
发明人： William Alexander Denny , William Robert Wilson , Moana Tercel
IPC分类号： A61K31/14 , A61K31/415 , A61K47/48 , A61P35/00 , A61P43/00 , C07C209/12 , C07C211/63 , C07C211/64 , C07C217/58 , C07C237/30 , C07C309/69 , C07C317/32 , C07C323/32 , C07D233/95 , A61K31/38 , A61K31/40
CPC分类号： A61K47/48338 , C07C211/63 , C07C217/58 , C07C317/32 , C07D233/95
摘要： ##STR1## Nitrobenzyl mustard quaternary salts of formula (I), and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR
1 R
3 -- or CR
1 ═CR
2 -- (where R
1 and R
2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO
2 R; Q is lower alkyl (optionally substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or ether groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO
2 , SO
2 R, CONHR, R, OR, SR, CF
3 and aza (ring --CH-- replared by --N═); with the proviso that when Y=Cl or Br, Q=Me, and X=--CH
2 -- then Ar≠2-nitrophanyl or 4-nitrophenyl.
摘要翻译：（I）式（I）的硝基苄基芥末季盐及其药学上可接受的盐，其制备方法及其作为缺氧选择性细胞毒性剂的化学治疗用途。其中X表示连接基-CR1R3-或CR1 = CR2-（其中R1和R2分别为H，低级烷基，苯基或硝基苯基; Y为卤素或OSO2R; Q为低级烷基（任选被烷基和/或醚取代）基团并含有最多6个碳原子）或硝基苯基; Ar表示单环或双环芳族单元，R是任选被烷基和/或醚基取代的低级烷基，并且可以含有至多8个碳原子，Z表示一个或多个 NO 2，SO 2 R，CONHR，R，OR，SR，CF 3和氮杂（环-CH-被-N =取代）;条件是当Y = Cl或Br时，Q = Me，X = 然后是Ar NOTEQUAL 2-硝基苯甲酰基或4-硝基苯基。

4. 发明申请

US20080119442A1 Nitrobenzindoles and Their use in Cancer Therapy 失效
标题翻译：硝基苯并吲哚及其在癌症治疗中的应用
公开(公告)号：US20080119442A1
公开(公告)日：2008-05-22
申请号：US11666014
申请日：2005-10-21
申请人： William Alexander Denny , William Robert Wilson , Ralph James Stevenson , Moana Tercel , Graham John Atwell , Shangjin Yang , Adam Vorn Patterson , Frederik Bastlaan Pruijn
发明人： William Alexander Denny , William Robert Wilson , Ralph James Stevenson , Moana Tercel , Graham John Atwell , Shangjin Yang , Adam Vorn Patterson , Frederik Bastlaan Pruijn
IPC分类号： A61K31/675 , C07D403/02 , C07D209/56 , C07F9/547
CPC分类号： C07F9/5728 , C07D209/60 , C07D403/06 , C07F9/65583
摘要： The present invention relates generally to nitro-1,2-dihydro-3H-benzo[e]indoles and related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本发明一般涉及硝基-1,2-二氢-3H-苯并[e]吲哚及其相关类似物及其制备方法，以及它们作为用于癌症治疗的缺氧选择性药物和放射增敏剂的用途，其单独或与辐射和/或其他抗癌药物。

5. 发明授权

US07718688B2 Nitrobenzindoles and their use in cancer therapy 失效
标题翻译：硝基苯并吲哚及其在癌症治疗中的应用
公开(公告)号：US07718688B2
公开(公告)日：2010-05-18
申请号：US11666014
申请日：2005-10-21
申请人： William Alexander Denny , William Robert Wilson , Ralph James Stevenson , Moana Tercel , Graham John Atwell , Shangjin Yang , Adam Vorn Patterson , Frederik Bastlaan Pruijn
发明人： William Alexander Denny , William Robert Wilson , Ralph James Stevenson , Moana Tercel , Graham John Atwell , Shangjin Yang , Adam Vorn Patterson , Frederik Bastlaan Pruijn
IPC分类号： A61K31/403 , C07D209/60
CPC分类号： C07F9/5728 , C07D209/60 , C07D403/06 , C07F9/65583
摘要： The present invention relates generally to nitro-1,2-dihydro-3H-benzo[e]indoles and related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本发明一般涉及硝基-1,2-二氢-3H-苯并[e]吲哚及其相关类似物及其制备方法，以及它们作为用于癌症治疗的缺氧选择性药物和放射增敏剂的用途，其单独或与辐射和/或其他抗癌药物。

6. 发明授权

US6130237A Condensed N-aclyindoles as antitumor agents 失效
标题翻译：浓缩的N-亚氨基吲哚作为抗肿瘤剂
公开(公告)号：US6130237A
公开(公告)日：2000-10-10
申请号：US266966
申请日：1999-03-12
申请人： William A. Denny , Moana Tercel , Graham J. Atwell
发明人： William A. Denny , Moana Tercel , Graham J. Atwell
IPC分类号： C07D209/60 , C07D487/04 , C07D209/10
CPC分类号： C07D487/04 , C07D209/60
摘要： The invention provides compounds of general formula (I), wherein: X is halogen or OSO.sub.2 R, where R represents H or is unsubstituted or hydroxy-or amino-substituted lower alkyl; Y is a nitro or amine group or a substituted derivative thereof; W is selected from the structures of formulae (Ia, Ib or Ic), where E is --N.dbd. or --CH.dbd., G is O, S, or NH, and Q is either up to three of R, OR, NRR, NO.sub.2, CONHR, NHCOR or NHCONHR, or is an additional group of formulae (Ia, Ib or Ic) and HET represents a 5- or 6-membered carbocycle or heterocycle; and A and B collectively represent a fused benzene or 2-CO.sub.2 R pyrrole ring. In one embodiment, the group Y is an amine derivative substituted by a group which is a substrate for a nitroreductase or carboxypeptidase enzyme such that one of said enzymes is able to bring about removal of that group. ##STR1##
摘要翻译：本发明提供通式（I）的化合物，其中：X为卤素或OSO 2 R，其中R为H或未取代的或羟基或氨基取代的低级烷基; Y是硝基或胺基或其取代的衍生物; W选自式（Ia，Ib或Ic）的结构，其中E为-N =或-CH =，G为O，S或NH，Q为R，OR，NRR， NO2，CONHR，NHCOR或NHCONHR，或另外一组式（Ia，Ib或Ic），HET表示5-或6-元碳环或杂环; A和B统称为稠合苯或2-CO 2 R吡咯环。在一个实施方案中，基团Y是被作为硝基还原酶或羧肽酶的底物的基团取代的胺衍生物，使得所述酶之一能够导致该基团的去除。

7. 发明授权

US5985909A Cyclopropylindoles and their seco precursors, and their use as prodrugs 失效
标题翻译：环丙基吲哚及其分子前体，以及它们作为前药的用途
公开(公告)号：US5985909A
公开(公告)日：1999-11-16
申请号：US11883
申请日：1998-02-18
申请人： William Alexander Denny , Moana Tercel
发明人： William Alexander Denny , Moana Tercel
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P35/00 , C07D209/14 , C07D209/42 , C07D401/14
CPC分类号： C07D401/14 , C07D209/42
摘要： The present invention provides compounds of formula (I) and (II) which may be used as anticancer drugs.
摘要翻译： PCT No.PCT / NZ96 / 00083 Sec。 371日期1998年2月18日 102（e）1998年2月18日PCT PCT 1996年8月19日PCT公布。出版物WO97 / 07097 日期：1997年2月27日本发明提供可用作抗癌药物的式（I）和（II）化合物。

8. 发明授权

US5691371A Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents 失效
标题翻译：硝基苄基芥末季盐及其作为缺氧选择性细胞毒性剂的用途
公开(公告)号：US5691371A
公开(公告)日：1997-11-25
申请号：US525785
申请日：1995-09-27
申请人： William Alexander Denny , William Robert Wilson , Moana Tercel
发明人： William Alexander Denny , William Robert Wilson , Moana Tercel
IPC分类号： A61K31/14 , A61K31/415 , A61K47/48 , A61P35/00 , A61P43/00 , C07C209/12 , C07C211/63 , C07C211/64 , C07C217/58 , C07C237/30 , C07C309/69 , C07C317/32 , C07C323/32 , C07D233/95
CPC分类号： A61K47/48338 , C07C211/63 , C07C217/58 , C07C317/32 , C07D233/95
摘要： Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.
摘要翻译： PCT No.PCT / NZ94 / 00046 Sec。 371 1995年9月27日第 102（e）1995年9月27日PCT PCT 1994年5月24日PCT公布。第WO94 / 27954号公报日期1994年12月8日公式（I）的硝基苄基芥末季盐及其药学上可接受的盐，其制备方法及其作为缺氧选择性细胞毒性剂的化学治疗用途。其中X表示连接基-CR1R2-或CR1 = CR2-（其中R1和R2分别为H，低级烷基，苯基或硝基苯基; Y为卤素或OSO2R; Q为低级烷基（任选被烷基和/或醚取代）基团并含有最多6个碳原子）或硝基苯基; Ar表示单环或双环芳族单元，R是任选被烷基和/或其它基团取代的低级烷基，并且可含有至多8个碳原子，Z表示一个或多个 NO 2，SO 2 R，CONHR，R，OR，SR，CF 3和氮杂（环-CH =被-N =取代）;条件是当H-Cl或Br，Q = Me和X = CH 2 Ar注释2-硝基苯基或4-硝基苯基。

9. 发明授权

US5556874A 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties 失效
公开(公告)号：US5556874A
公开(公告)日：1996-09-17
申请号：US438616
申请日：1995-05-10
申请人： Ellen M. Dobrusin , Howard D. H. Showalter , William A. Denny , Brian D. Palmer , Gordon W. Rewcastle , Moana Tercel , Andrew M. Thompson
发明人： Ellen M. Dobrusin , Howard D. H. Showalter , William A. Denny , Brian D. Palmer , Gordon W. Rewcastle , Moana Tercel , Andrew M. Thompson
IPC分类号： C07D209/30 , C07D209/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , A61K31/40 , C07D209/10
CPC分类号： C07D401/12 , C07D209/30 , C07D209/42 , C07D405/12 , C07D409/12 , C07D471/04
摘要： 2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.

10. 发明授权

US5464861A 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties 失效
标题翻译：抑制蛋白酪氨酸激酶的2-硫代吲哚（硒代吲哚）和相关的二硫化物（硒化物）并具有抗肿瘤特性
公开(公告)号：US5464861A
公开(公告)日：1995-11-07
申请号：US094792
申请日：1993-08-09
申请人： Ellen M. Dobrusin , Howard D. H. Showalter , William A. Denny , Brian D. Palmer , Gordon W. Rewcastle , Moana Tercel , Andrew M. Thompson
发明人： Ellen M. Dobrusin , Howard D. H. Showalter , William A. Denny , Brian D. Palmer , Gordon W. Rewcastle , Moana Tercel , Andrew M. Thompson
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/44 , A61P9/00 , A61P9/10 , A61P31/12 , A61P35/00 , A61P43/00 , C07D209/30 , C07D209/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D209/04
CPC分类号： C07D401/12 , C07D209/30 , C07D209/42 , C07D405/12 , C07D409/12 , C07D471/04
摘要： 2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.
摘要翻译： 2-硫代吲哚（2-硒吲哚）和类似的2-二氢吲哚硫酮（2-吲哚啉硒酮）和多硫化物（硒化物）化合物，其盐，生产方法，其生产中的中间体，含有所述化合物的药物组合物和抑制蛋白激酶依赖性的方法公开了哺乳动物中的疾病或使用所述组合物治疗哺乳动物的异常细胞生长。

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