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1.发明授权Expression of DNA sequences encoding a thermally stable cytosine deaminase from saccharomyces 失效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
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。
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公开(公告)号：US5545548A
公开(公告)日：1996-08-13
申请号：US262238
申请日：1994-06-20
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。
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3.发明授权Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease 有权药物共轭物及其用于治疗癌症，自身免疫性疾病或传染病的用途公开(公告)号：US08906376B2
公开(公告)日：2014-12-09
申请号：US12880028
申请日：2010-09-10
CPC分类号： A61K47/48246 , A61K47/64 , A61K47/642 , A61K47/6817 , A61K47/6851 , A61K47/6867 , C07K5/0205
摘要： Drug-Linker-Ligand Conjugates are disclosed in which a Drug is linked to a Ligand via a peptide-based Linker unit. In one embodiment, the Ligand is an Antibody. Drug-Linker compounds and Drug compounds are also disclosed. Methods for treating cancer, an autoimmune disease or an infectious disease using the compounds and compositions of the invention are also disclosed.
摘要翻译： 公开了药物 - 接头 - 配体结合物，其中药物通过基于肽的接头单元与配体连接。 在一个实施方案中，配体是抗体。 还公开了药物连接剂化合物和药物化合物。 还公开了使用本发明的化合物和组合物治疗癌症，自身免疫疾病或感染性疾病的方法。
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4.发明授权Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus 有权在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：US08871720B2
公开(公告)日：2014-10-28
申请号：US11994459
申请日：2006-07-07
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。
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公开(公告)号：US20120027784A1
公开(公告)日：2012-02-02
申请号：US13189452
申请日：2011-07-22
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 , C07K17/00
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.
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公开(公告)号：US07964567B2
公开(公告)日：2011-06-21
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
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.
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7.发明授权Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease 有权药物共轭物及其用于治疗癌症，自身免疫性疾病或传染病的用途公开(公告)号：US07659241B2
公开(公告)日：2010-02-09
申请号：US10522911
申请日：2003-07-31
CPC分类号： A61K47/48246 , A61K47/64 , A61K47/642 , A61K47/6817 , A61K47/6851 , A61K47/6867 , C07K5/0205
摘要： Compounds and compositions are disclosed in which a Drug unit (D) is linked to a Ligand unit (L). In an exemplary embodiment, the compound is of the formula LAa-Ww-Yy-D)p Ia or a pharmaceutically acceptable salt thereof, where A is a stretcher unit, W is an amino acid unit, Y is a spacer unit, D is of the formula and a, w, y, p and R2-R10 are as disclosed in the specification. Methods for treating cancer, autoimmune disease, and infectious disease using the compounds and compositions of the invention are also disclosed.
摘要翻译： 公开了化合物和组合物，其中药物单元（D）与配体单元（L）连接。 在一个示例性实施方案中，该化合物具有式L
Aa-Ww-Yy-D）p Ia或其药学上可接受的盐，其中A是担架单元，W是氨基 酸单元，Y是间隔单元，D具有下式：a，w，y，p和R 2 -R 10如说明书中所公开的。 还公开了使用本发明的化合物和组合物治疗癌症，自身免疫疾病和感染性疾病的方法。
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公开(公告)号：US07098308B2
公开(公告)日：2006-08-29
申请号：US10979923
申请日：2004-11-01
IPC分类号： C07K7/00
CPC分类号： C07K5/0202 , A61K38/00 , A61K47/6811 , C07K5/0205
摘要： Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.
摘要翻译： 公开了五肽化合物。 这些化合物具有生物活性，例如细胞毒性。 还公开了具有靶向基团和五肽阴离子的前体药物及其前体物质。 例如，具有可用作连接靶向试剂（例如抗体）的反应位点的反应性连接体的前体，如所公开的。
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公开(公告)号：US4904768A
公开(公告)日：1990-02-27
申请号：US199731
申请日：1988-05-27
申请人： Mark G. Saulnier , Peter D. Senter , John F. Kadow
发明人： Mark G. Saulnier , Peter D. Senter , John F. Kadow
IPC分类号： C07H17/04 , A61K20060101 , A61K31/365 , A61K31/366 , A61K31/44 , A61K31/66 , A61K31/661 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P35/00 , A61P35/04 , C07F20060101 , C07H20060101 , C07H3/02 , C07H15/00 , C07H15/24
CPC分类号： C07H17/04 , Y10S514/908
摘要： Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.
摘要翻译： 4'-去甲表鬼臼毒素葡糖苷的磷酸酯衍生物是新的抗肿瘤剂，其盐提供高水溶性的药物优点。
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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。
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