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1. 发明申请

WO1993002045A1 HYDROXAMATE AND HYDRAZIDE DERIVATIVES OF POLYAMINES AND THEIR MEDICAL USE AS CHELATING AGENTS 审中-公开
标题翻译：聚氨酯的氢氧化物和氢化衍生物及其作为螯合剂的医药用途
公开(公告)号：WO1993002045A1
公开(公告)日：1993-02-04
申请号：PCT/EP1992001598
申请日：1992-07-16
申请人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED SALUTAR, INC. , HIMMELSBACH, Richard, J. , RONGVED, Pål , KLAVENESS, Jo , STRANDE, Per , DUGSTAD, Harald
发明人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED SALUTAR, INC.
IPC分类号： C07C243/34
CPC分类号： C07C243/34 , C07C259/06 , C07D257/02
摘要： The present invention provides a compound of formula (I): A[X(CR R )n]mXA or a chelate complex of salt thereof, for use as therapeutic or diagnostic agent wherein in formula (I), each of the groups R and R may independently represent a hydrogen atom or an alkyl or alkoxy group, optionally carrying one or more substituents selected from hydroxy, alkoxy and aryl groups; each X independently represents an oxygen or sulphur atom or a group NA; each A independently represents a hydrogen atom or an alkyl group optionally substituted by a group Y; each Y represents a hydrogen atom, or a group Z, COZ, SO3R , CSZ, PO2Z or B; or one or more pairs of A groups on different X moieties may together form a group [(CR R )nX ]p (CR R )n or a group A on a mid-chain nitrogen may represent a group [(CR R )nX ]p (CR R )nX A where p represents an integer of 0 to 6, and each X independently represents an oxygen or sulphur atom or a group NA where A is as defined for A but may not form part of a group attached to more than one nitrogen atom; or two adjacent groups R and/or A may together form a homo- or heterocyclic saturated or unsaturated 5-7 membered ring containing 0, 1 or 2 ring heteroatoms selected from oxygen, nitrogen and sulphur; m is an integer of 2 to 8; n is an integer of 2 to 4.
摘要翻译：本发明提供式（I）化合物：A [X（CR 1 R 2）n] m X A或其盐的螯合络合物，其用作治疗或诊断剂，其中式（I）， R 1和R 2中的每一个可以独立地表示氢原子或烷基或烷氧基，任选携带一个或多个选自羟基，烷氧基和芳基的取代基; 每个X独立地表示氧或硫原子或基团NA; 每个A独立地表示氢原子或任选被基团Y取代的烷基; 每个Y表示氢原子，或基团Z，COZ，SO 3 R 6，CSZ，PO 2 Z或B; 或不同X部分上的一对或多对A基团可以一起形成基团[（CR 1 R 2）n X 1] p（CR 1 R 2）n或基团中链氮可以表示基团[（CR 1 R 2）n X 1] p（CR 1 R 2）n X 1 A，其中p表示0至6的整数并且每个X 1独立地表示氧或硫原子或NA <1，其中A 1如对A所定义，但不能形成与多于一个氮原子连接的基团的一部分; 或两个相邻基团R 1和/或A可以一起形成含有0,1或2个选自氧，氮和硫的环杂原子的均聚或杂环饱和或不饱和5-7元环; m为2〜8的整数， n为2〜4的整数。

2. 发明申请

WO1993000930A1 IMPROVEMENTS IN OR RELATING TO CONTRAST AGENTS 审中-公开
标题翻译：改进或与对比剂相关
公开(公告)号：WO1993000930A1
公开(公告)日：1993-01-21
申请号：PCT/EP1992001477
申请日：1992-07-03
申请人： HOLMES, Michael, John , NYCOMED AS , BERG, Arne , KLAVENESS, Jo , STRANDE, Per , STUBBERUD, Lars
发明人： HOLMES, Michael, John , NYCOMED AS
IPC分类号： A61K49/00
CPC分类号： A61K49/226 , A61K49/223
摘要： Ultrasound contrast agents comprising a microbubble-generating suspension of a microparticulate X-ray contrast agent in a liquid carrier medium.
摘要翻译：超声造影剂包括在液体载体介质中产生微粒X射线造影剂的微泡产生悬浮液。

3. 发明申请

WO1990007491A1 IODINATED ESTERS 审中-公开
标题翻译：碘化物
公开(公告)号：WO1990007491A1
公开(公告)日：1990-07-12
申请号：PCT/EP1990000053
申请日：1990-01-08
申请人： HOLMES, Michael, John , NYCOMED A/S , KLAVENESS, Jo , STRANDE, Per
发明人： HOLMES, Michael, John , NYCOMED A/S
IPC分类号： C07C233/88
CPC分类号： C07C237/46 , A61K49/0476 , C07C233/54 , C07C233/88 , C07D317/28 , C07D317/36 , C07D333/32
摘要： Water insoluble iodinated esters of formula (I), in which R is a substituted or unsubstituted C1-20 aliphatic, C7-20 araliphatic or C6-20 aryl group or a C1-20 heterocyclic group having one or more hetero atoms selected from O, S and N; R is hydrogen or a substitued or unsubstituted C1-6 aliphatic, C6-10 aryl or C7-20 araliphatic group; and R is a group as defined above for R , which may be the same as or different from R , or R and R together represent a substituted or unsubstituted C1-4 alkylene group, the molecule containing at least one iodine atom and being metabolisable to products which are soluble in body fluids and are physiologically acceptable. The esters are useful in X-ray and ultrasound imaging, especially liver and spleen imaging.
摘要翻译：式（I）的水不溶性碘化酯，其中R 1是取代或未取代的C 1-20脂族基，C 3-20芳脂基或C 6-20芳基或选自具有一个或多个杂原子的C 1-20杂环基从O，S和N; R 2是氢或取代或未取代的C 1-6脂族，C 6-10芳基或C 7-20芳脂基基团; 并且R 3是如上对R 1所定义的基团，其可以与R 1相同或不同，或者R 2和R 3一起代表取代或未取代的C1-4 亚烷基，该分子含有至少一个碘原子，并且可溶于体液的生物学可接受的产物。这些酯可用于X射线和超声成像，特别是肝脏和脾脏成像。

4. 发明申请

WO1996007434A1 IMPROVEMENTS IN OR RELATING TO CONTRAST AGENTS 审中-公开
标题翻译：改进或与对比剂相关
公开(公告)号：WO1996007434A1
公开(公告)日：1996-03-14
申请号：PCT/GB1995002109
申请日：1995-09-06
申请人： MARSDEN, John, Christopher , NYCOMED IMAGING AS , KLAVENESS, Jo , RONGVED, Pål , STRANDE, Per
发明人： MARSDEN, John, Christopher , NYCOMED IMAGING AS
IPC分类号： A61K49/00
CPC分类号： A61B8/481 , A61F2210/0004 , A61K49/0002 , A61K49/22 , A61L15/62 , A61L27/58
摘要： Contrast agents comprising gas-containing polymer microparticles and/or microballoons in which the polymer is a biodegradable polymer comprising repeating units of formula (II) (where a is an integer of 9-19 and b is an integer of 1-8) may be used in diagnostic applications such as ultrasound and MR imaging. The polymers are novel and are also claimed per se.
摘要翻译：包含含气体的聚合物微粒和/或微球的造影剂可以是其中聚合物是包含式（II）的重复单元（其中a为9-19的整数，b为1-8的整数）的可生物降解的聚合物用于诊断应用，如超声和MR成像。聚合物是新颖的，并且本身也是要求的。

5. 发明申请

WO1994021301A1 IMPROVEMENTS IN OR RELATING TO CONTRAST AGENTS 审中-公开
标题翻译：改进或与对比剂相关
公开(公告)号：WO1994021301A1
公开(公告)日：1994-09-29
申请号：PCT/GB1994000521
申请日：1994-03-16
申请人： HOLMES, Michael, John , NYCOMED IMAGING A.S , BERG, Arne , DUGSTAD, Harald , FOSS, Per, Antonius , KLAVENESS, Jo , OSTENSEN, Jonny , RONGVED, Pål , STRANDE, Per
发明人： HOLMES, Michael, John , NYCOMED IMAGING A.S
IPC分类号： A61K49/00
CPC分类号： A61K49/226 , A61K49/223
摘要： Oil-in-water emulsions in which the oil phase comprises condensed or dissolved oil-soluble gas/fluid or gas precursor are useful as ultrasound contrast agents. Such products contain insignificant amounts of free gas bubbles or microbubbles in their stored form and exhibit good storage stability, but may be designed to promote rapid microbubble generation immediately before or upon administration.
摘要翻译：其中油相包含冷凝或溶解的油溶性气体/流体或气体前体的水包油乳剂可用作超声造影剂。这样的产品在其储存形式中含有不显着量的游离气泡或微泡，并表现出良好的储存稳定性，但可以设计用于在施用之前或之后促进快速产生微泡。

6. 发明申请

WO1993018070A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO1993018070A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000469
申请日：1993-03-05
申请人： NYCOMED IMAGING AS , KLAVENESS, Jo , REDFORD, Keith , SOLBERG, Jan , STRANDE, Per
发明人： NYCOMED IMAGING AS
IPC分类号： C08F08/14
CPC分类号： A61K49/1857 , A61K49/223
摘要： Non-crosslinked non-polypeptide polymers containing biodegradable lipophilic side chains incorporating methylene diester units of the formula -[-CO-O-C(R R )-O-CO-]- (where R and R each represents a hydrogen atom or a carbon-attached monovalent organic group or R and R together form a carbon-attached divalent organic group) whereby the lipophilic moieties are biodegradatively cleavable to yield a water-soluble polymer.
摘要翻译：含有具有式 - [ - CO-OC（R 1 R 2）-O-CO - ] - （其中R 1和R 2）的亚甲基二酯单元的可生物降解的亲脂侧链的非交联非多肽聚合物 <2>各自表示氢原子或连碳的一价有机基团，或者R 1和R 2一起形成碳键的二价有机基团），由此亲油部分可生物降解地切割，得到水溶性聚合物。

7. 发明申请

WO1992011232A1 CHELATING AGENTS 审中-公开
标题翻译：焊接剂
公开(公告)号：WO1992011232A1
公开(公告)日：1992-07-09
申请号：PCT/EP1991002468
申请日：1991-12-20
申请人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED AS , STRANDE, Per , KLAVENESS, Jo , RONGVED, Pål , DUGSTAD, Harald
发明人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED AS
IPC分类号： C07C237/04
CPC分类号： C07D213/40 , C07C237/10 , C07C2602/08 , C07D209/20 , C07D211/58 , C07D213/75 , C07D295/13
摘要： There are provided chelating agents of formula (I) (wherein n is 0 or 1 and at least one R group comprises a group NR R where one of R and R comprises a cyclic lipophilic group) and metal chelates and salts thereof. The chelates with paramagnetic or heavy metal ions are particularly suited for use as hepatobiliary contrast agents.
摘要翻译：提供式（I）的螯合剂（其中n为0或1，并且至少一个R 1基团包含基团NR 11 R 14，其中R 11和R 14中的一个包含环状亲油基团）和金属螯合物及其盐。具有顺磁性或重金属离子的螯合物特别适合用作肝胆造影剂。

8. 发明申请

WO1989006979A1 PARAMAGNETIC COMPOUNDS 审中-公开
标题翻译：参考化合物
公开(公告)号：WO1989006979A1
公开(公告)日：1989-08-10
申请号：PCT/EP1989000078
申请日：1989-01-26
申请人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED AS , KLAVENESS, Jo , RONGVED, Pål , STRANDE, Per
发明人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED AS
IPC分类号： A61K49/00
CPC分类号： A61K49/085 , A61K49/126 , Y10T436/24
摘要： There are provided paramagnetic compounds comprising a paramagnetic metal species chelated by a chelating moiety bound by an amide group to a linker group itself bound by an ester group to a macromolecule, wherein said linker group provides a carbon chain of at least 2 atoms between said amide group and said ester group. The novel compounds are particularly suitable as contrast agents, e.g. in magnetic resonance imaging.

9. 发明申请

WO1995007270A1 CHELANTS AS CONTRAST ENHANCING AGENTS 审中-公开
标题翻译：作为对比增强剂的CHELANTS
公开(公告)号：WO1995007270A1
公开(公告)日：1995-03-16
申请号：PCT/GB1994001931
申请日：1994-09-06
申请人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian , GARRITY, Martha , CROFTS, Shaun, Paul , CARVALHO, Joan , STRANDE, Per , DUGSTAD, Harald
发明人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian
IPC分类号： C07D257/02
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 Y) or -N(CR 2Y)-; each Z is a group R or a group CR 2Y, at least one Z being a group CR 2Y; each Y is a group CO2H, PO3H, SO3H, CONR 2, CON(OR )R , CNS or CONR NR 2; m is 0 or 1 or 2; each n is 2 or 3; q is 0 or 1 when B is (CR Y) and 2 when B is N(CR 2Y); p is an integer having a value of at least 2; each R 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 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 di- and trichelates with paramagnetic or heavy metal ions are especially useful as diagnostic imaging contrast agents.
摘要翻译：本发明提供一种式（Ⅶ）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（CR 1 Y）或-N （CR 1 2Y） - ;每个Z是基团R 1或基团CR 1Y 2，至少一个Z是基团CR 2Y;每个Y是基团CO 2 H，PO 3 H，SO 3 H ，CONR 1，CON（OR 1）R 1，CNS或CONR 1 NR 12，m为0或1或2;每个n为2或3; q为0或 1，当B为（CR 1）Y）时为2，B为N时为2（CR 1 2Y）; p为值至少为2的整数;每个R 1可以相同或不同任选被一个或多个羟基或烷氧基取代的烷基，芳基或芳烷基或环原子上或Z基团中的两个R 1一起表示连接基团L;每个L可以相同或不同的表示分子量小于1000的键或有机连接基团及其盐和螯合物，这些化合物，特别是具有顺磁或重金属离子的二 - 和三 - s作为诊断成像造影剂是特别有用的。

10. 发明申请

WO1995006518A1 POLYMERIC SURFACTANT-ENCAPSULATED MICROBUBBLES AND THEIR USE IN ULTRASOUND IMAGING 审中-公开
标题翻译：聚合物表面活性剂包封微生物及其在超声成像中的应用
公开(公告)号：WO1995006518A1
公开(公告)日：1995-03-09
申请号：PCT/GB1994001923
申请日：1994-09-05
申请人： NYCOMED IMAGING A/S , DUGSTAD, Harald , FOSS, Per, Antonius , KLAVENESS, Jo , REDFORD, Keith , RONGVED, Pål , SKURTVEIT, Roald , STRANDE, Per
发明人： NYCOMED IMAGING A/S
IPC分类号： B01F17/00
CPC分类号： B01F17/0028 , A61K49/223 , Y10T428/2985
摘要： Polymer-based gas-containing contrast agents in which microbubbles of gas are encapsulated by non-polymerisable wall-forming block or graft copolymer surfactants. The polymer surfactants are preferably biodegradable and include block and graft copolymers containing linkages of formula (I): -(O)m-CO-O-C(R R )-O-CO-(O)n- (where R and R each represent a hydrogen atom or a carbon-attached monovalent organic group or R and R together form a carbon-attached divalent organic group and m and n are each zero or 1) which are themselves novel.
摘要翻译：基于聚合物的含气体造影剂，其中气体的微泡被不可聚合的壁形成嵌段或接枝共聚物表面活性剂包封。聚合物表面活性剂优选是可生物降解的，并且包括含有式（I）的键的嵌段和接枝共聚物： - （O）m -CO-OC（R 1 R 2）-O-CO-（O）n - 其中R 1和R 2各自表示氢原子或连接碳的一价有机基团，或者R 1和R 2一起形成连接碳的二价有机基团，m和n各自为零或 1）本身就是小说。

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