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:
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:
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。
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:
The present invention provides a method of treatment of a human or non-human (e.g. mammalian, avian or reptilian) animal subject by the parenteral administration of a lipophilic pharmaceutical agent, the improvement comprising administering said pharmaceutical agent in an oil-in-water emulsion containing a conjugated linoleic acid or a physiologically tolerable derivative thereof.
摘要:
The present invention provides a method of treating or preventing a disorder typified by an immunodificiency (e.g. HIV), wherein the patient is administered a COX-2 inhibitor or derivative or pharmaceutically acceptable salt thereof, preferably diisopropylfluorophasphate. L-745337, rofecoxib, NS 398, SC 58125, etodolac, meloxicam, celecoxib or nimesulide, and compositions and products containing the same or use of the same in preparing medicaments and for treatment.
摘要:
The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.
摘要翻译:本发明涉及作为5-氨基乙酰丙酸的酯或其药学上可接受的盐的化合物,包括式(I)的化合物R 2 N 2 CH 2 其中R 1可以表示任选取代的烷基,其中R 1表示任选被取代的烷基, 羟基,烷氧基,酰氧基,烷氧基羰基氧基,氨基,芳基,氧代或氟基团,且任选被氧,氮,硫或磷原子间隔; R 2表示氢原子或基团R > 1 SUP>,并且两个R 2个基团可以相同或不同),以及它们在诊断和光化学治疗身体的外部或内部表面的障碍或异常中的用途,以及产品和 用于执行本发明的试剂盒。
摘要:
The invention provides a method of treatment of a human or non-human subject to combat sub-dermal soft tissue pain therein, said method comprising administering to a subject in need thereof an effective amount of a physiologically tolerable strontium compound.
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.