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公开(公告)号：US5053226A
公开(公告)日：1991-10-01
申请号：US73500
申请日：1987-07-15
申请人： Michael G. Rosenblum , James L. Murray , Peter J. Kelleher , Robert A. Newman , Abdul R. Khokhar
发明人： Michael G. Rosenblum , James L. Murray , Peter J. Kelleher , Robert A. Newman , Abdul R. Khokhar
CPC分类号： C07K16/44 , A61K47/48676 , C07K16/468 , A61K38/00
摘要： The present invention relates to monoclonal antibodies specifically binding platinum (II) complex. The monoclonal antibodies of the present invention are characteristically produced by antibody-producing cell lines such as hybridomas. These cell lines may result, for example, from fusion of a neoplastic cell with an antibody-producing animal cell obtained from an animal immunized against a platinum (II) complex. The cellular fusion products include cell lines forming monoclonal antibody specifically binding platinum (II) complex in competition with an antibody produced by: hybridoma strain 1C.sub.1 H.sub.2 A.sub.5, deposited with the American Type Culture Collection, Rockville, MD on May 1, 1987 and having ATCC accession number HB 9411; strain 3A.sub.2 A.sub.1 ; strain 1A.sub.6 A.sub.2 ; strain 3A.sub.6 B.sub.1 or strain 1B.sub.1. The cell lines of the present invention are preferably continuous murine hybridoma cell lines which secrete recoverable quantities of monoclonal antibody, particularly a monoclonal antibody which is of an IgG or IgM isotype.
摘要翻译： 本发明涉及特异性结合铂（II）复合物的单克隆抗体。 本发明的单克隆抗体的特征在于产生抗体的细胞系如杂交瘤。 这些细胞系可以例如来自肿瘤细胞与获自抗铂（II）复合物的动物获得的产生抗体的动物细胞的融合。 细胞融合产物包括形成特异性结合铂（II）复合物的单克隆抗体的细胞系，与1987年5月1日保藏于美国典型培养物保藏中心，Rockville，MD的杂交瘤菌株1C1H2A5产生的抗体竞争，并具有ATCC登录号 HB 9411; 菌株3A2A1; 菌株1A6A2; 菌株3A6B1或菌株1B1。 本发明的细胞系优选分泌可回收量的单克隆抗体，特别是IgG或IgM同种型的单克隆抗体的连续鼠杂交瘤细胞系。
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公开(公告)号：USRE30971E
公开(公告)日：1982-06-15
申请号：US119656
申请日：1980-02-20
IPC分类号： A61K31/28 , A61K31/282 , A61P35/00 , B01J31/00 , C07F15/00
CPC分类号： C07F15/0093
摘要： This invention relates to a compound of platinum having the structure: ##STR1## in which X and Y are halogenoid groups which are the same or different and are preferably both chloride but may be other halide or pseudohalide such as cyanate, thiocyanate and azide or other similar groups, and A and B are the same or different branched chain aliphatic amine groups co-ordinated to the Pt through their N atoms.
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3.发明授权Delivery and activation through liposome incorporation of diaminocyclohexane platinum(II) complexes 失效通过二氨基环己烷铂（II）配合物的脂质体掺入递送和活化公开(公告)号：US07029696B2
公开(公告)日：2006-04-18
申请号：US10750382
申请日：2003-12-30
CPC分类号： A61K31/282 , A61K9/127
摘要： Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula where R1 is diaminocycloalkyl, and R2 and R3 each have the formula where R4, R5, and R6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having the formula R1—Pt—X2 (II) where X is halogen.
摘要翻译： 公开了抗肿瘤组合物，以及制备组合物的方法和使用它们抑制哺乳动物肿瘤生长的方法。 本发明可以利用具有下式的铂络合物的脂内酯转化：其中R 1是二氨基环烷基，R 2和R 3各自具有 其中R 4，R 5和R 6各自独立地为具有1至约10个碳原子的烃部分转化为络合物 具有公式<？in-line-formula description =“In-line Formulas”end =“lead”？> R＆lt; 1＆gt; -Pt-X＆lt; 2＆gt;（II） ？in-line-formula description =“In-line Formulas”end =“tail”？>其中X是卤素。
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公开(公告)号：US5384127A
公开(公告)日：1995-01-24
申请号：US998413
申请日：1992-12-29
申请人： Roman Perez-Soler , Insook Han , Abdul R. Khokhar
发明人： Roman Perez-Soler , Insook Han , Abdul R. Khokhar
CPC分类号： A61K9/127 , A61K31/28 , C07F15/0093
摘要： Lipophilic complexes having the structureDACH--Pt--R.sub.2where DACH is diaminocyclohexane, and where R is a linear alkyl carboxylato group having from about 5 to about 18 carbon atoms, have desirable stability when entrapped within lipid bilayers, and exhibit high entrapment efficiency and in vivo antitumor activity.
摘要翻译： 其中DACH是二氨基环己烷的结构DACH-Pt-R2的亲脂性络合物，其中R是具有约5至约18个碳原子的直链烷基羧酸基团，当被捕获在脂质双层内时具有期望的稳定性，并且表现出高的捕获效率和 体内抗肿瘤活性。
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5.发明授权Diamine platinum(IV) complexes having mixed carboxylate ligands as antitumor agents 失效将具有混合的羧酸盐配体的铂（IV）配合物二胺作为抗肿瘤剂
公开(公告)号：US5288887A
公开(公告)日：1994-02-22
申请号：US978788
申请日：1992-11-19
CPC分类号： C07F15/0093
摘要： Platinum(IV) complexes with mixed carboxylato ligands having the formula: ##STR1## where X.sup.1 and X.sup.2 are carboxylato, or are jointly dicarboxylato, where .sup.1 Y and Y.sup.2 are carboxylato, and where Z is either diaminocyclohexane or ethylenediamine, have been found to have desirable antitumor activity, as well as relatively low levels of toxicity.
摘要翻译： 已经发现，铂（IV）络合物与具有下式的混合羧基配位体：其中X1和X2是羧基或羧基共轭二羧酸，其中Z是二氨基环己烷或乙二胺，其中Z是二氨基环己烷或乙二胺， 所需的抗肿瘤活性，以及较低的毒性水平。
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公开(公告)号：US5178876A
公开(公告)日：1993-01-12
申请号：US709122
申请日：1991-05-31
CPC分类号： A61K31/28 , A61K9/127 , C07F15/0093
摘要： The present invention involves the synthesis and use of new platinum compounds. These new platinum compounds are easy to encapsulate in liposomes at high efficiencies. They are further characterized as platinum (II) four coordinate complex having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are carboxylato monoanions bearing a hydrophobic radical function or a single carboxylato dianion bearing a hydrophobic radical function and R.sub.3 is a vicinal diaminoalkane or vicinal diaminocycloalkane. The complex is substantially soluble in methanol or chloroform and substantially insoluble in water. Said complex may be incorporated into phospholipid liposomes. Such platinum complexes encapsulated in phospholipid liposomes are useful for chemotherapy of platinum complex-sensitive tumors.
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7.发明授权
公开(公告)号：US5011959A
公开(公告)日：1991-04-30
申请号：US932176
申请日：1986-11-17
IPC分类号： A61K31/28 , A61K33/24 , A61P35/00 , C07C211/65 , C07C229/16 , C07C239/18 , C07D307/24 , C07F15/00 , C07H7/033 , C07H23/00
CPC分类号： C07H23/00 , C07F15/0093
摘要： The present invention comprises a water-soluble square-planar cis-platinum(II) four-coordinate complex having the formula:trans-R,R-DACH Pt(II) X.sub.2ortrans-R,R-DACH Pt(II) Ywherein X is a monovalvent cation, two of which are present, selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethyglycinato; wherein Y is a divalent cation selected from the group consisting of citraconato, 1,1-cyclobutanedicarboxylato, 1,1-cyclopropanedicarboxylato, isocitratolactone and Z-iminodiacetato where Z is bound to the nitrogen and is ethyl, propyl, Isopropyl, n-butyl, sec-butyl, ter-butyl, n-amyl, isoamyl or OH.In one preferred aspect the water-soluble square-planar cis-platinum(II) four-coordinate complex has the formula:trans-R,R-DACH Pt(II) X.sub.2wherein X is a monovalent cation. Two X substituents are present in the platinum complex. These X substituents are preferably selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethylglycinato. Both X substituents are usually identical butmay be different.
摘要翻译： 本发明包括具有下式的水溶性正方形顺式 - 铂（II）四配位络合物：反式-R，R-DACH Pt（II）X2或反式-R，R-DACH Pt（II）Y 其中X是单价阳离子，其中两个存在，选自环丙烷羧酸盐，莽草酸，蔗糖内酯，半乳糖醛酸和N，N-二甲基甘氨酸; 其中Y是选自柠康酸，1,1-环丁烷二羧酸，1,1-环丙烷二羧酸，异柠檬酸内酯和Z-亚氨基二乙酸的二价阳离子，其中Z与氮结合，是乙基，丙基，异丙基，正丁基， 仲丁基，叔丁基，正戊基，异戊基或OH。 在一个优选的方面，水溶性正方形顺式 - 铂（II）四配位络合物具有下式：反式-R，R-DACH Pt（II）X2，其中X是一价阳离子。 铂络合物中存在两个X取代基。 这些X取代基优选选自环丙烷羧酸，莽草酸，蔗糖内酯，半乳糖醛酸和N，N-二甲基甘氨酸。 两个X取代基通常是相同的，但可以是不同的。
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公开(公告)号：US5434256A
公开(公告)日：1995-07-18
申请号：US316139
申请日：1994-09-30
申请人： Abdul R. Khokhar , Zahid H. Siddik
发明人： Abdul R. Khokhar , Zahid H. Siddik
IPC分类号： C07F15/00 , A61K31/555
CPC分类号： C07F15/0093
摘要： Novel 1,4 and 1,2-diaminocyclohexane platinum IV complexes have been synthesized that show activity in vivo against tumor models resistant to cis-platin and tetraplatin. The novel complexes include the chloro, acetate, trifluoroacetate, propionate, butyrate, pentanoate, hexanoate and heptanoate as leaving ligands and 1,4 or 1,2-DACH-amine ligands. The complexes showed good in vitro cytotoxic activity against murine leukemia L1210/0, L1210/DDP and L1210/DACH. High in vivo activity was shown against L1210 leukemia cells and against cis-platin resistant L1210/DDP. Excellent antitumor activity against M5076 was also exhibited by the new complexes. Additionally, the platinum complexes did not elicit any indication of nephrotoxicity in the in vivo tests.
摘要翻译： 已经合成了新的1,4和1,2-二氨基环己烷铂IV络合物，其在体内表现出对顺铂和四铂的抗肿瘤模型的活性。 新型络合物包括离开配体和1,4或1,2-DACH-胺配体的氯，乙酸酯，三氟乙酸酯，丙酸酯，丁酸酯，戊酸酯，己酸酯和庚酸酯。 该配合物对鼠白血病L1210 / 0，L1210 / DDP和L1210 / DACH显示出良好的体外细胞毒活性。 针对L1210白血病细胞和抗顺铂耐药性L1210 / DDP显示出高体内活性。 新配合物也展示了抗M5076的抗肿瘤活性。 此外，铂络合物在体内测试中没有引起肾毒性的任何迹象。
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9.发明授权
公开(公告)号：US5041581A
公开(公告)日：1991-08-20
申请号：US914591
申请日：1986-10-07
CPC分类号： A61K31/28 , A61K9/127 , C07F15/0093
摘要： The present invention involves the synthesis and use of new platinum compounds. These new platinum compounds are easy to encapsulate in liposomes at high efficiencies. They are further characterized as platinum (II) four coordinate complex having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are carboxylato monoanions bearing a hydrophobic radical function or a single carboxylato dianion bearing a hydrophobic radical function and R.sub.3 is a vicinal diaminoalkane or vicinal diaminocycloalkane. The complex is substantially soluble in methanol or chloroform and substantially insoluble in water. Said complex may be incorporated into phospholipid liposomes. Such platinum complexes encapsulated in phospholipid liposomes are useful for chemotherapy of platinum complex-sensitive tumors.
摘要翻译： 本发明涉及合成和使用新的铂化合物。 这些新的铂化合物容易以高效率包封在脂质体中。 它们被进一步表征为具有下式的铂（II）四配位络合物：其中R1和R2是具有疏水基官能团的羧基单阴离子或具有疏水基功能的单羧酸二阴离子，R3是连位二氨基烷烃或连位二氨基环烷烃 。 该配合物基本上可溶于甲醇或氯仿，基本上不溶于水。 所述复合物可以掺入磷脂脂质体中。 封装在磷脂脂质体中的这种铂络合物可用于铂复合物敏感性肿瘤的化疗。
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10.发明授权Delivery and activation through liposome incorporation of diaminocyclohexane platinum(II) complexes 失效通过二氨基环己烷铂（II）配合物的脂质体掺入递送和活化公开(公告)号：US06696079B2
公开(公告)日：2004-02-24
申请号：US09168799
申请日：1998-10-08
IPC分类号： A61K9127
CPC分类号： A61K31/282 , A61K9/127
摘要： Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula where R1 is diaminocycloalkyl, and R2 and R3 each have the formula where R4, R5, and R6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having the formula R1—Pt—X2 (II) where X is halogen.
摘要翻译： 公开了抗肿瘤组合物，以及制备组合物的方法和使用它们抑制哺乳动物肿瘤生长的方法。 本发明可以利用具有下式的铂络合物的脂质体内转化：R1是二氨基环烷基，R2和R3各自具有式R 4，R 5和R 6各自独立地为具有1至约10个碳原子的烃部分， 其中X是卤素。
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