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1. 发明授权

US5972307A Dichelants 失效
公开(公告)号：US5972307A
公开(公告)日：1999-10-26
申请号：US898376
申请日：1997-07-22
申请人： Joan Carvalho , Alan D. Watson , Jere D. Fellmann , Michael Koo
发明人： Joan Carvalho , Alan D. Watson , Jere D. Fellmann , Michael Koo
IPC分类号： A61K49/00 , A61K49/06 , C07C237/06 , C07C237/10 , C07C237/12 , C07D241/06 , C07D257/02 , C07D295/185 , C07D403/14 , C07F9/6524 , C07F19/00 , A61K51/04 , A61B5/055 , C07D225/00 , C07F5/00
CPC分类号： C07D241/06 , A61K49/0002 , A61K49/06 , C07C237/06 , C07C237/10 , C07C237/12 , C07D257/02 , C07D295/185 , C07D403/14 , C07F19/005 , C07F9/6524
摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups;and D is a bridging group having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.
摘要翻译：本发明涉及双耳，特别是具有通过含有酯或酰胺键的桥连接的两个大环螯合剂基团的化合物，特别是式Vb化合物（其中每个X可以相同或不同，为至少NZ，O或S，至少两个X为NZ;每个Z为基团R 1或基团CR 12 Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 12Y;每个Y为CO 2 H，PO 3 H，SO 3 H，CONR 12， CON（OR1）R1，CNS或CONR1NR12，优选COOH; m为0或1或2，优选1;每个n为2或3，优选2; q为1或2，优选1;每个R 1可以相同或不同的是氢原子或任选被一个或多个羟基和/或烷氧基取代的烷基; D是分子量小于1000，优选小于500的桥连基团，至少通过至少连接两个大环一个酰胺或酯键）及其盐和金属螯合物。

2. 发明授权

US5650133A Macrocyclic polyaza dichelates linked through ring nitrogens via an amide or ester functionality 失效
标题翻译：通过环氮化合物通过酰胺或酯官能团连接的大环多氮化合物
公开(公告)号：US5650133A
公开(公告)日：1997-07-22
申请号：US226760
申请日：1994-04-12
申请人： Joan Carvalho , Alan D. Watson , Jere D. Fellmann , Michael David Koo
发明人： Joan Carvalho , Alan D. Watson , Jere D. Fellmann , Michael David Koo
IPC分类号： A61K49/00 , A61K49/06 , C07D257/02 , C07D403/14 , C07F9/6524 , A61K51/04 , A61B5/055 , C07D225/00 , C07F5/00
CPC分类号： C07D403/14 , A61K49/0002 , A61K49/06 , C07D257/02 , C07F9/6524
摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups;and D is a bridging group having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.
摘要翻译：本发明涉及双耳，特别是具有通过含有酯或酰胺键的桥连接的两个大环螯合剂基团的化合物，特别是具有式Vb的化合物（其中每个可以相同或不同的X可以是NZ，O或S ，至少两个X为NZ;每个Z为基团R 1或基团CR 12 Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 12Y;每个Y为CO 2 H，PO 3 H，SO 3 H ，CONR12，CON（OR1）R1，CNS或CONR1NR12，优选COOH; m为0或1或2，优选1;每个n为2或3，优选2; q为1或2，优选1; 相同或不同的是氢原子或任选被一个或多个羟基和/或烷氧基取代的烷基; D是分子量小于1000，优选小于500的桥连基，连接两个大环通过至少一个酰胺或酯键）及其盐和金属螯合物。

3. 发明授权

US5976493A Metabolically cleavable dendrimeric polychelants 失效
公开(公告)号：US5976493A
公开(公告)日：1999-11-02
申请号：US702693
申请日：1996-11-08
申请人： Lawrence Margerum , Joan Carvalho , Martha Garrity , Jere Douglas Fellmann
发明人： Lawrence Margerum , Joan Carvalho , Martha Garrity , Jere Douglas Fellmann
IPC分类号： A61K49/00 , A61K49/08 , A61K49/12 , A61K51/06 , C07D259/00 , C08G83/00 , C09K3/00 , A61K51/04 , A61B5/055
CPC分类号： A61K49/124 , A61K49/085 , A61K49/12 , A61K51/065 , C07D259/00 , C08G83/00 , Y10S424/16
摘要： The invention provides polychelant compounds which are useful for example in diagnostic imaging procedures and which are degradable in vivo to release excretable fragments. Such compounds conveniently are of the formula (I): R.sup.1 (X.sup.1 R.sup.2 ((X.sup.2).sub.p L).sub.n).sub.m (where X.sup.1 is a linker moiety metabolically cleavable to release R.sup.1 X.sup.3.sub.m and X.sup.4 R.sup.2 ((X.sup.2).sub.p L).sub.n fragments where X.sup.3 and X.sup.4 are the cleavage residues of X.sup.1 ; R.sup.1 X.sup.3.sub.m is a biotolerable polymer, preferably a substantially monodisperse polymer and especially one with a molecular weight below 40,000 D, particularly below 30,000 D and especially below 20,000 D, for example a first to sixth generation dendrimer; X.sup.4 R.sup.2 ((X.sup.2).sub.p L).sub.n is a polychelant fragment having a molecular weight below 40,000 D, preferably below 30,000 D, especially below 20,000 D, each such moiety preferably being the same; p is 0 or 1; X.sup.2, where present, is a linker moiety metabolically cleavable to release a monochelant fragment; each L is a macrocyclic chelant moiety, wherein the macrocyclic skeleton preferably has 9 to 25 ring members and preferably is an optionally oxygen or sulphur interrupted polyazacycloalkane; R.sup.2 ((X.sup.2).sub.p).sub.n is a straight chain or branched backbone moiety, preferably providing a chain of up to 20 atoms between each L group and the X.sup.1 moiety to which it is joined and a chain of up to 25 atoms between each pair of L groups linked thereby, such chains conveniently being nitrogen and/or oxygen and/or sulphur interrupted carbon chains; each n is an integer having a value of at least 2, preferably a value of 2 to 25, especially 2 to 12; and each m is an integer having a value of at least 2, preferably a value of up to 200, especially 3 to 100, such that the total number of L groups in the polychelant of formula (I) is at least 20, preferably 50 to 200), having a molecular weight of at least 30,000 D, preferably at least 40,000 D, and especially preferably 50,000 to 150,000 D, and metal chelates and salts thereof.

4. 发明授权

US06207660B1 Texaphyrin conjugates and uses thereof 失效
标题翻译：特拉法林缀合物及其用途
公开(公告)号：US06207660B1
公开(公告)日：2001-03-27
申请号：US09325890
申请日：1999-06-04
申请人： Jonathan L. Sessler , Darren Magda , Tarak Mody , Pavel Anzenbacher, Jr. , Joan Carvalho
发明人： Jonathan L. Sessler , Darren Magda , Tarak Mody , Pavel Anzenbacher, Jr. , Joan Carvalho
IPC分类号： C07D48722
CPC分类号： A61K41/0038 , A61K41/0033 , A61K41/0076 , A61K47/546
摘要： Texaphyrin/chemotherapeutic drug conjugates, optionally including a platinum(II) or platinum(IV) metal chelating site and/or complex, are useful for treating atheroma, tumors and other neoplastic tissue, neovascular-related diseases, as well as other conditions that are typically responsive to chemotherapy, radiation sensitization and photodynamic therapy.
摘要翻译：任意包括铂（II）或铂（IV）金属螯合位点和/或络合物的特拉法林/化疗药物偶联物可用于治疗动脉粥样化，肿瘤和其他肿瘤组织，新生血管相关疾病以及其它条件通常对化学疗法，辐射敏化和光动力疗法有反应。

5. 发明授权

US5958373A Polychelants as contrast enhancing agents 失效
标题翻译： Polychelants作为对比增强剂
公开(公告)号：US5958373A
公开(公告)日：1999-09-28
申请号：US615241
申请日：1996-06-13
申请人： Martha Garrity , Shaun Paul Crofts , Joan Carvalho , Per Strande , Harald Dugstad
发明人： Martha Garrity , Shaun Paul Crofts , Joan Carvalho , Per Strande , Harald Dugstad
IPC分类号： A61K31/395 , A61K49/00 , A61K49/04 , A61P39/02 , C07D257/02 , C07D519/00 , A61B5/055
CPC分类号： A61K49/0002 , C07D257/02 , Y10S514/836
摘要： The present invention provides a polychelant compound of formula (VII), (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ; B is (CR.sup.1 Y) or --N(CR.sup.1.sub.2 Y)--; each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z being a group CR.sup.1.sub.2 Y; each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2 ; m is 0 or 1 or 2; each n is 2 or 3; q is 0 or 1 when B is (CR.sup.1 Y) and 2 when B is N(CR.sup.1.sub.2 Y); p is an integer having a value of at least 2; each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl, aryl or aralkyl group optionally substituted by one or more hydroxy or alkoxy groups, or two R.sup.1 groups on ring atoms or in Z groups together represent a linker group L; each L which may be the same or different represents a bond or an organic linker group having a molecular weight of less than 1000 and salts and chelates thereof. These compounds, especially the diand trichelates with paramagnetic or heavy metal ions are especially useful as diagnostic imaging contrast agents.
摘要翻译： PCT No.PCT / GB94 / 01931 Sec。 371日期：1996年6月13日 102（e）日期1996年6月13日PCT 1994年9月6日PCT公布。公开号WO95 / 07270 日期：1995年3月16日本发明提供了式（VII）所示的聚合物化合物，其中每个X可以相同或不同，为NZ，O或S，至少两个X为NZ; B为（CR1Y）或 - N（CR12Y） - ;各Z为基团R1或基团CR12Y，至少一个Z为基团CR12Y;每个Y为CO 2 H，PO 3 H，SO 3 H，CONR 12，CON（OR 1）R 1，CNS或CONR1NR 12; m 是0或1或2;每个n是2或3;当B是（CR1Y）时，q是0或1，当B是N（CR12Y）时，q是2; p是具有至少2的整数;每个R1 可以相同或不同的是氢原子或任选被一个或多个羟基或烷氧基取代的烷基，芳基或芳烷基，或在环原子上或Z基团中的两个R 1基团一起表示连接基团L;每个L 可以相同或不同，表示分子量小于1000的键或有机连接基团及其盐和螯合物，这些化合物，特别是具有顺磁性或重金属离子的二联体三聚体是特别的作为诊断成像造影剂有效。

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