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1. 发明申请

WO1995028392A1 CHELANT COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO1995028392A1
公开(公告)日：1995-10-26
申请号：PCT/GB1995000833
申请日：1995-04-12
申请人： NYCOMED IMAGING A/S , COCKBAIN, Julian , VARADARAJAN, John , WATSON, Alan, David , BERG, Arne
发明人： NYCOMED IMAGING A/S , COCKBAIN, Julian
IPC分类号： C07D257/02
CPC分类号： A61K49/06 , C07C237/08 , C07D255/02 , C07D257/02 , C07D259/00 , C07D273/00
摘要： The invention provides amphiphilic compounds of the formula (I) Ch-(-L-Ar-(-AH)n)m (where Ch is a hydrophilic chelant moiety or a salt or a chelate thereof); each L is an optionally oxo substituted C2-25-alkylene linker wherein at least one CH2 moiety is replaced by a group X (e.g. L may include a chain sequence, an X (CH2CH2X )u (where u is a positive integer) such as X CH2CH2X , CH2X CH2CH2X CH2CH2X , CH2X CH2CH2X CH2CH2X CH2CH2X , etc.), and wherein L is optionally interrupted by a metabolizable group M but with the provisos that the terminus of L adjacent Ch is CH2 and that the terminus of L adjacent Ar is X or a CH2 group adjacent or separated by one CH2 from a group X (thus, for example the L-Ar linkage may be L -X -Ar, L -CH2-Ar, L -X CH2-Ar or L -X CH2CH2-Ar, where L is the residue of L; each Ar is an aryl ring optionally substituted by or having fused thereto a further aryl ring; each AH is a protic acid group, preferably an oxyacid, e.g. a carbon, sulphur or phosphorus oxyacid or a salt thereof; each X is O, S, NR or PR , preferably no more than 3 X groups being present in L; each R is hydrogen, alkyl or aryl; and m and n are positive integers, m being for example 1 to 4, especially 1 or 2 and n being for example 1, 2 or 3) which are especially suited for use in diagnostic imaging of the hepatobiliary system.
摘要翻译：本发明提供式（I）Ch - （ - L-Ar - （ - AH）n）m（其中Ch是亲水性螯合剂部分或其盐或螯合物）的两亲化合物; 每个L是任选氧代取代的C2-25-亚烷基接头，其中至少一个CH 2部分被基团X 1取代（例如L可以包括链序列，X 1（CH 2 CH 2 X 1）u（其中u是正整数），例如X 1 CH 2 CH 2 X 1，CH 2 X 1 CH 2 CH 2 X 1 CH 2 CH 2 X 1，CH 2 X 1 CH 2 CH 2 X 1 CH 2 CH 2 X 1 CH 2 CH 2 X 1等），并且其中L任选地被可代谢基团M中断，但条件是邻近Ch的L的末端是CH 2，并且L相邻的Ar的末端是X 1或与一个CH 2相邻或分隔的CH2基团基团X 1（因此，例如L-Ar键可以是L 1 -X 1 -Ar，L 1 -CH 2 -Ar，L 1 -X 1 CH 2 - Ar或L 1 -X 1 CH 2 CH 2 -Ar，其中L 1是L的残基;每个Ar是任选被另外的芳基环取代或与其稠合的芳基;每个AH是质子酸基团，优选含氧酸，例如碳，硫或磷的含氧酸或其盐;每个X 1为O，S，NR 1或PR 1，优选不超过3个X 1为存在于升; 每个R 1是氢，烷基或芳基; m和n为正整数，m为例如1至4，特别是1或2，n为例如1,2或3），其特别适用于肝胆系统的诊断成像。

2. 发明申请

WO9509848A3 POLYAZACYCLOALKANES AS DICHELANTS 审中-公开
标题翻译：聚四环素作为狄更斯
公开(公告)号：WO9509848A3
公开(公告)日：1995-07-27
申请号：PCT/GB9402115
申请日：1994-09-29
申请人： NYCOMED SALUTAR INC , COCKBAIN JULIAN R M , CARVALHO JOAN , FELLMANN JERE DOUGLAS , WATSON ALAN DAVID , KOO MICHAEL
发明人： CARVALHO JOAN , FELLMANN JERE DOUGLAS , WATSON ALAN DAVID , KOO MICHAEL
IPC分类号： G01R33/28 , A61B5/055 , A61K31/395 , A61K31/495 , A61K49/00 , A61K49/06 , A61K51/00 , A61N5/00 , A61P39/00 , A61P39/02 , A61P43/00 , C07D255/02 , C07D257/02 , C07D273/00 , C07D285/00 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07F5/00 , C07F9/547 , C07F9/6524 , C07H23/00 , C09K3/00
CPC分类号： C07D295/15 , A61K49/122 , C07D257/02 , C07D273/08 , C07D403/14 , 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 (V) (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 or a group CR 2Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR 2Y; each Y is a group CO2H, PO3H, SO3H, CONR 2, CON(OR )R , CNS or CONR NR 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 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, other than an unsubstituted carbonylaminoethylaminocarbonyl 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.

3. 发明申请

WO1995009848A2 POLYAZACYCLOALKANES AS DICHELANTS 审中-公开
标题翻译：聚四环素作为狄更斯
公开(公告)号：WO1995009848A2
公开(公告)日：1995-04-13
申请号：PCT/GB1994002115
申请日：1994-09-29
申请人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian, Roderick, Michaelson , CARVALHO, Joan , FELLMANN, Jere, Douglas , WATSON, Alan, David , KOO, Michael
发明人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian, Roderick, Michaelson
IPC分类号： C07D257/02
CPC分类号： C07D295/15 , A61K49/122 , C07D257/02 , C07D273/08 , C07D403/14 , 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 (V) (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 or a group CR 2Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR 2Y; each Y is a group CO2H, PO3H, SO3H, CONR 2, CON(OR )R , CNS or CONR NR 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 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, other than an unsubstituted carbonylaminoethylaminocarbonyl 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（Ⅴ）化合物（其中每个X可以相同或不同的是NZ，O或S，至少两个X为NZ;每个Z为基团R 1或基团CR 1 2Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 2Y; 每个Y是CO 2 H，PO 3 H，SO 3 H，CONR 2，CON（OR 1）R 1，CNS或CONR 1 NR 1，优选COOH; m是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，是氢原子或任选被一个或多个羟基和/或烷氧基; D是分子量小于1000，优选小于500的未取代的羰基氨基乙基氨基羰基以外的桥连基，通过至少一个酰胺键或酯键连接两个大环）和盐和金属螯合物。

4. 发明申请

WO1996011023A1 LIPOSOMAL AGENTS 审中-公开
标题翻译：药物代理
公开(公告)号：WO1996011023A1
公开(公告)日：1996-04-18
申请号：PCT/GB1995002378
申请日：1995-10-09
申请人： NYCOMED SALUTAR INC. , COCKBAIN, Julian, Roderick, Michaelson , GARRITY, Martha , VARADARAJAN, John , WATSON, Alan, David
发明人： NYCOMED SALUTAR INC. , COCKBAIN, Julian, Roderick, Michaelson
IPC分类号： A61K49/00
CPC分类号： A61K49/1812 , A61K51/1234
摘要： There is provided a liposomal agent comprising liposomes having bound to a membrane thereof a chelated diagnostically or therapeutically effective metal ion, the chelating agent binding said metal ion having a macrocyclic chelant moiety with attached to a single ring atom thereof a lipophilic membrane associating moiety.
摘要翻译：提供了包含与其膜结合螯合的诊断或治疗有效金属离子的脂质体的脂质体试剂，所述螯合剂将具有大环螯合剂部分的所述金属离子与亲环体膜缔合部分连接。

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