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11. 发明授权

US4874779A Mitomycin phosphate derivatives 失效
标题翻译：丝裂霉素磷酸酯衍生物
公开(公告)号：US4874779A
公开(公告)日：1989-10-17
申请号：US213201
申请日：1988-06-29
申请人： Peter D. Senter
发明人： Peter D. Senter
IPC分类号： A61K31/675 , A61P35/00 , C07F9/6561
CPC分类号： C07F9/6561
摘要： Disclosed herein are N.sup.7 -alkylphosphate derivatives of mitomycin C and porfiromycin showing antitumor activity against transplanted human tumor and reduced toxicity relative to the parent N.sup.7 -alkanol mitomycin compounds.
摘要翻译：本文公开了丝裂霉素C和卟吩霉素的N7-烷基磷酸酯衍生物，其显示针对移植的人肿瘤的抗肿瘤活性，并且相对于母体N7-链烷醇丝裂霉素化合物的毒性降低。

12. 发明授权

US08703714B2 Monomethylvaline compounds capable of conjugation to ligands 有权
标题翻译：能与配体结合的单甲基缬氨酸化合物
公开(公告)号：US08703714B2
公开(公告)日：2014-04-22
申请号：US13098391
申请日：2011-04-29
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Toni Beth Kline
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Toni Beth Kline
IPC分类号： A61K38/08 , A61K47/48
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
摘要翻译：制备包括MeVal-Val-Dil-Dap-Norephedrine（MMAE）和MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽，并通过各种接头包括马来酰亚胺酰基val-cit-PAB连接到配体上。所得配体药物偶联物在体外和体内都是活性的。

13. 发明授权

US08557780B2 Monomethylvaline compounds capable of conjugation to ligands 有权
公开(公告)号：US08557780B2
公开(公告)日：2013-10-15
申请号：US13098393
申请日：2011-04-29
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki
IPC分类号： A61K38/00 , A61K38/04 , A61K38/08 , C07K5/027 , C07K7/02 , C07K17/02 , C07K17/06 , A61P35/00
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

14. 发明申请

US20120141510A1 MONOMETHYLVALINE COMPOUNDS CAPABLE OF CONJUGATION TO LIGANDS 审中-公开
公开(公告)号：US20120141510A1
公开(公告)日：2012-06-07
申请号：US13397661
申请日：2012-02-15
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , B32B1/02 , C07K16/00
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6803 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

15. 发明授权

US07964566B2 Monomethylvaline compounds capable of conjugation to ligands 有权
标题翻译：能与配体结合的单甲基缬氨酸化合物
公开(公告)号：US07964566B2
公开(公告)日：2011-06-21
申请号：US11833959
申请日：2007-08-03
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K38/00 , A61K38/02 , C07K2/00
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
摘要翻译：制备包括MeVal-Val-Dil-Dap-Norephedrine（MMAE）和MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽，并通过各种接头包括马来酰亚胺酰基val-cit-PAB连接到配体上。所得配体药物偶联物在体外和体内都是活性的。

16. 发明申请

US20090111756A1 Monomethylvaline Compounds Having Phenylalanine Carboxy Modifications at the C-Terminus 有权
标题翻译：在C-末端具有苯丙氨酸羧基修饰的单甲基缬氨酸化合物
公开(公告)号：US20090111756A1
公开(公告)日：2009-04-30
申请号：US11994459
申请日：2006-07-07
申请人： Svetlana O. Doronina , Toni Beth Kline , Scott Jeffrey , Peter D. Senter , Damon Meyer
发明人： Svetlana O. Doronina , Toni Beth Kline , Scott Jeffrey , Peter D. Senter , Damon Meyer
IPC分类号： C07K7/06 , C07K16/46 , A61K38/08 , C12N5/06 , A61P35/00
CPC分类号： A61K47/48415 , A61K38/00 , A61K39/3955 , A61K47/6811 , A61K2039/505 , C07K5/0205 , C07K7/02 , C07K16/2866 , C07K2317/76 , Y02A50/40 , Y02A50/401 , Y02A50/406 , Y02A50/48
摘要： Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) having a carboxylic acid equivalent at the C-terminal phenylalanine were prepared and attached to ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
摘要翻译：制备具有C-末端苯丙氨酸羧酸当量的MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽类似物，并通过各种接头包括马来酰亚氨基己酰基val-cit-PAB连接到配体上。所得配体药物偶联物在体外和体内都是活性的。

17. 发明申请

US20080248051A1 MONOMETHYLVALINE COMPOUNDS CAPABLE OF CONJUGATION TO LIGANDS 有权
公开(公告)号：US20080248051A1
公开(公告)日：2008-10-09
申请号：US11833961
申请日：2007-08-03
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/44 , A61P35/00
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

18. 发明授权

US07091186B2 p-Amidobenzylethers in drug delivery agents 有权
标题翻译：药物递送剂中的对 - 二苯基醚
公开(公告)号：US07091186B2
公开(公告)日：2006-08-15
申请号：US09963103
申请日：2001-09-24
申请人： Peter D. Senter , Brian E. Toki
发明人： Peter D. Senter , Brian E. Toki
IPC分类号： C07K5/06
CPC分类号： A61K47/6889
摘要： Compounds of the formulae LAn-Z-X—WwD and BZ-X—WwD wherein: D is a drug moiety; L is a ligand; B is a blocking group; A is an optional acyl unit; Z is an amino acid or a peptide residue; X is an aminobenzyl ether self-immolative spacer group; W is an optional second self-immolative group; n is an integer of 0 or 1; and w is an integer of 0 or 1, and compositions of said compounds with pharmaceutically acceptable carrier, diluent and/or excipient, and methods of delivery the drug D via the compounds.
摘要翻译：公式的化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> L A -ZXW _{w D和B ZXW D < ？in-line-formula description =“In-line formula”end =“tail”？>其中：D是药物部分; L是配体; B是封闭组; A是任选的酰基单元; Z是氨基酸或肽残基; X为氨基苄基醚自消除间隔基; W是可选的第二个自焚组; n为0或1的整数; w为0或1的整数，所述化合物与药学上可接受的载体，稀释剂和/或赋形剂的组合物，以及通过化合物递送药物D的方法。}

19. 发明授权

US5338678A Expression of DNA sequences encoding a thermally stable cytosine deaminase from saccharomyces 失效
标题翻译：表达编码来自酵母菌的热稳定胞嘧啶脱氨酶的DNA序列
公开(公告)号：US5338678A
公开(公告)日：1994-08-16
申请号：US531646
申请日：1990-06-01
申请人： Peter D. Senter , Peter C. D. Su , Hans Marquardt , Martha S. Hayden , Peter Linsley
发明人： Peter D. Senter , Peter C. D. Su , Hans Marquardt , Martha S. Hayden , Peter Linsley
IPC分类号： C12N15/09 , C12N1/00 , C12N9/78 , C12N15/55 , C12R1/865 , C12N5/00 , C07H15/12 , C12N1/20 , C12N15/00
CPC分类号： C12N9/78
摘要： Thermally stable cytosine deaminase (CDase), and the gene coding therefor, is disclosed as well as methods of isolating, purifying, and recombinantly producing the same. The thermally stable CDase can be isolated from Saccharomyces cerevisiae. The yeast isolated enzyme has a molecular weight of approximately 32 kDa, as determined by gel filtration chromatography, and is composed of two subunits, each with a molecular weight of about 17 kDa. Thermally stable yeast CDase so purified shows no significant sequence homology with other known sequenced proteins.
摘要翻译：公开了热稳定的胞嘧啶脱氨酶（CDase）及其编码基因，以及分离，纯化和重组产生其的方法。热稳定的CDase可以从酿酒酵母中分离出来。酵母分离的酶具有通过凝胶过滤色谱法测定的约32kDa的分子量，由两个分子量约17kDa的亚基组成。如此纯化的热稳定酵母CDase与其他已知的测序蛋白质没有显着的序列同源性。

20. 发明授权

US4569789A Acid-cleavable compound, use in protein conjugates and drug delivery systems 失效
标题翻译：可酸切割化合物，用于蛋白质缀合物和药物递送系统
公开(公告)号：US4569789A
公开(公告)日：1986-02-11
申请号：US727550
申请日：1985-04-26
申请人： Walter A. Blattler , John M. Lambert , Peter D. Senter
发明人： Walter A. Blattler , John M. Lambert , Peter D. Senter
IPC分类号： C07K14/00 , A61K31/194 , A61K31/195 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K38/00 , A61K38/36 , A61K39/00 , A61K39/395 , A61K45/00 , A61K47/48 , A61P35/00 , C07C229/42 , C07C323/36 , C07D207/44 , C07D207/452 , C07D405/00 , C07D405/12 , C07H15/252 , C07K1/107 , C07K1/113 , C07K9/00 , C07K14/415 , C07K16/00 , C07D519/00 , C07D521/00
CPC分类号： C07D207/452 , C07D405/12
摘要： Amino-sulfhydryl cross-linking reagents that are cleavable under mildly acidic conditions are disclosed. Also disclosed are methods of making the cross-linkers, as well as methods of using the cross-linkers, e.g., to deliver a biologically active substance across the membranes of selected cells in a heterogeneous cell population; once inside the cell the active substance is released, intact, by the transient, mild acidity of certain cell structures. Finally, a method of characterizing complex multi-chain protein structures is disclosed.
摘要翻译：公开了在弱酸性条件下可切割的氨基 - 巯基交联试剂。还公开了制备交联剂的方法，以及使用交联剂的方法，例如将生物活性物质跨越异种细胞群体中所选细胞的膜递送; 一旦在细胞内，活性物质通过某些细胞结构的瞬时，温和的酸度被完全释放。最后，公开了一种表征复合多链蛋白结构的方法。

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