Iodinated esters
    132.
    发明授权
    Iodinated esters 失效
    碘化酯

    公开(公告)号:US5416223A

    公开(公告)日:1995-05-16

    申请号:US315502

    申请日:1994-09-30

    摘要: Water insoluble iodinated esters of formula (I), in which R.sup.1 is a substituted or unsubstituted C.sub.1-20 aliphatic, C.sub.7-20 araliphatic or C.sub.6-20 aryl group or a C.sub.1-20 heterocyclic group having one or more hereto atoms selected from O, S and N; R.sup.2 is hydrogen or a substituted or unsubstituted C.sub.1-6 aliphatic, C.sub.6-10 aryl or C.sub.7-20 araliphatic group; and R.sup.3 is a group as defined above for R.sup.1, which may be the same as or different from R.sup.1, or R.sup.2 and R.sup.3 together represent a substituted or unsubstituted C.sub.1-4 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C 7-20芳脂肪族或C 6-20芳基或具有一个或多个选自O, S和N; R2是氢或取代或未取代的C1-6脂族,C6-10芳基或C7-20芳脂肪基; 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 3一起表示取代或未取代的C 1-4亚烷基,该分子含有至少一个碘原子并且可代谢至 可溶于体液且具有生理学上可接受的产品。 这些酯可用于X射线和超声成像,特别是肝脏和脾脏成像。

    Iodinated esters
    133.
    发明授权
    Iodinated esters 失效
    碘化酯

    公开(公告)号:US5354549A

    公开(公告)日:1994-10-11

    申请号:US802529

    申请日:1991-12-05

    CPC分类号: C07D333/38

    摘要: The invention relates to metabolically labile water-insoluble esters of formula (I), wherein R.sup.1 is an aliphatic, araliphatic, aryl or heterocyclic group; R.sup.2 is hydrogen or an aliphatic, aryl or araliphatic group; R.sup.3 is as defined for R.sup.1, or R.sup.3 and R.sup.2 together form an alkylene chain; the molecule containing at least one iodine atom and being metabolised to form products which are soluble in body fluids. The esters are used in X-ray and ultrasound image enhancement.

    摘要翻译: 本发明涉及式(I)代谢不稳定的水不溶性酯,其中R1是脂族,芳脂族,芳基或杂环基; R2是氢或脂族,芳基或芳脂族基团; R3如R1所定义,或R3和R2一起形成亚烷基链; 该分子含有至少一个碘原子并被代谢以形成可溶于体液的产物。 酯用于X射线和超声图像增强。

    Chelating compounds
    134.
    发明授权
    Chelating compounds 失效
    螯合化合物

    公开(公告)号:US5322681A

    公开(公告)日:1994-06-21

    申请号:US910318

    申请日:1992-07-17

    申请人: Jo Klaveness

    发明人: Jo Klaveness

    CPC分类号: C07D471/08 A61K49/06

    摘要: The invention provides novel condensed macrocyclic chelants of formula [X(CR.sup.2 R.sup.3).sub.n ].sub.m, (wherein each X independently represents an oxygen or sulphur atom or a group of formula NH, N(CR.sup.2 R.sup.3).sub.p R.sup.4, N(CR.sup.2 R.sup.3).sub.p Y, or N(CR.sup.2 R.sup.3).sub.n- N((CR.sup.2 R.sup.3).sub.p Y).sub.2 ; each Y independently represents a group COZ, SO.sub.2 Z, POZ.sub.2, CON(OH)R.sup.2, CH.sub.2 SR.sup.2, CS.sub.2 R.sup.2 or CSZ; each Z independently represents a group OR.sup.2 or NR.sup.2 R.sup.2 ; n is an integer of 1 to 4; m is an integer of 3 to 8; p is an integer of 1 to 3; each R.sup.2 independently represents a hydrogen atom or a C.sub.1-8 alkyl group optionally mono- or poly-substituted by hydroxyl or C.sub.1-8 alkoxy groups and at least one pair of R.sup.2 groups, in each pair one being from a (CR.sup.2 R.sup.3).sub. n moiety and the other being from a (CR.sup.2 R.sup.3).sub.n or (CR.sup.2 R.sup.3).sub.p moiety, together with the intervening atoms represents a 5 to 8 membered, saturated fused ring optionally containing one or more ring heteroatoms selected from nitrogen, oxygen and sulphur, said fused ring optionally being substituted by a group R.sup.1 ; each R.sup.1 independently represents a group R.sup.4 or a nitrogen-attached group (CR.sup.2 R.sup.3).sub.p Y; each R.sup.3 independently represents a hydrogen atom or a C.sub.1-8 alkyl or C.sub.1-8 alkoxy group optionally mono or poly substituted by hydroxy or C.sub.1-8 alkoxy groups; and each R.sup.4 independently represents a hydrogen atom, a halogen atom or a hydroxyl group or an optionally mono- or poly-hydroxylated C.sub.1-8 alkyl, C.sub.1-8 alkoxy, (C.sub.1-8 alkoxy)-C.sub.1-8 alkyl or poly-(C.sub.1-8 alkoxy)-C.sub.1-8 alkyl group, a sulphonate group or a group (CR.sup.2 R.sup.3).sub.p Y; with the proviso that at least 2 Y groups are present). These chelants are useful in the preparation of diagnostic and therapeutic agents, in particular chelate complexes suitable for use as contrast agents for diagnostic imaging techniques, e.g. MRI.

    摘要翻译: 本发明提供式[X(CR 2 R 3)n] m(其中每个X独立地表示氧或硫原子)或式NH,N(CR 2 R 3)p R 4,N(CR 2 R 3)p Y或N的基团的新型稠合大环螯合剂 (CR2R3)n-N((CR2R3)pY)2;每个Y独立地表示基团COZ,SO2Z,POZ2,CON(OH)R2,CH2SR2,CS2R2或CSZ;每个Z独立地表示基团OR2或NR2R2; n是 1〜4的整数; m为3〜8的整数,p为1〜3的整数,各自独立地表示氢原子或任选被羟基或C1取代的C1-8烷基 -8个烷氧基和至少一对R2基团,每一对一个来自(CR 2 R 3)n部分,另一个来自(CR 2 R 3)n或(CR 2 R 3)p部分,连同原子代表5 至8元饱和稠环,任选地含有一个或多个选自氮,氧和硫的环杂原子,所述稠环任选被基团R 1取代;每个R 1独立地为 y表示基团R 4或氮连接基团(CR 2 R 3)p Y; 每个R 3独立地表示氢原子或任选被羟基或C 1-8烷氧基取代的C 1-8烷基或C 1-8烷氧基; 并且每个R 4独立地表示氢原子,卤素原子或羟基或任选的单 - 或多羟基化C 1-8烷基,C 1-8烷氧基,(C 1-8烷氧基)-C 1-8烷基或聚 - ( C 1-8烷氧基)-C 1-8烷基,磺酸酯基或基团(CR 2 R 3)p Y; 条件是存在至少2个Y基团)。 这些螯合剂可用于制备诊断和治疗剂,特别是适于用作诊断成像技术的造影剂的螯合配合物,例如, MRI。

    Photosensitizing compositions
    135.
    发明授权
    Photosensitizing compositions 有权
    光敏组合物

    公开(公告)号:US09026203B2

    公开(公告)日:2015-05-05

    申请号:US13390404

    申请日:2010-08-16

    CPC分类号: A61K41/0071

    摘要: The invention relates to pharmaceutically acceptable salts of amphiphilic photosensitizing agents which have a water solubility of at least 0.5 mg/ml and to their use in methods of photochemical internalization. Such salts may be formed from a pharmaceutically acceptable base, for example an organic amine such as an amino alcohol, or from a pharmaceutically acceptable acid, for example a sulphonic acid or a sulphonic acid derivative. Due to their increased water solubility, such salts are particularly suitable for use in the preparation of parenteral pharmaceutical preparations, e.g. for use as solutions for injection or infusion.

    摘要翻译: 本发明涉及两亲性光敏剂的药学上可接受的盐,它们的水溶解度至少为0.5mg / ml,并且它们在光化学内化方法中的用途。 这样的盐可以由药学上可接受的碱形成,例如有机胺如氨基醇,或由药学上可接受的酸,例如磺酸或磺酸衍生物形成。 由于其水溶性增加,这些盐特别适合用于制备肠胃外药物制剂,例如, 用作注射或输注的溶液。

    Optical Imaging Contrast Agents For Imaging Lung Cancer
    140.
    发明申请
    Optical Imaging Contrast Agents For Imaging Lung Cancer 审中-公开
    用于成像肺癌的光学成像对比剂

    公开(公告)号:US20070212305A1

    公开(公告)日:2007-09-13

    申请号:US10582893

    申请日:2004-12-17

    IPC分类号: A61K49/04

    摘要: The invention provides contrast agents for optical imaging of lung cancer in patients. The contrast agents may be used in diagnosis of lung cancer, for follow up of progress in disease development, for follow up of treatment of lung cancer and for surgical guidance. Further, the invention provides methods for optical imaging of lung cancer in patients.

    摘要翻译: 本发明提供了用于患者肺癌光学成像的造影剂。 造影剂可用于诊断肺癌,用于跟踪疾病发展进展,随访肺癌治疗和手术指导。 此外,本发明提供了患者中肺癌的光学成像方法。