摘要:
Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.
摘要:
The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient.
摘要:
A kit comprising: a sealed container containing a ready-to-use skin bleaching composition including an emulsion containing 2 to 6% wt of a peroxide bleaching agent selected from hydrogen peroxide, organic peracids and salts thereof, hydrogen peroxide adducts, and metal peroxides, percarbonates and perborates; and instructions for the use of the composition to bleach chemically tanned skin.
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 present invention relates to the field of human and animal nutrition, and in particular to certain novel compositions of conjugated linoleic acids (CLA). In particular, the present invention relates certain isomers of conjugated linoleic acids at either the SN1 and SN3 or SN2 positions of the acylglyceride molecule and another fatty acyl residue at the other of the SN1 and SN3 or SN2 positions of the acylglyceride molecule. These novel acylglyceride compositions containing conjugated linoleic acyl residues, medium chain fatty acyl residues, long chain fatty acyl residues, and &ohgr;3, &ohgr;6, and &ohgr;9 fatty acyl residues are efficacious as pharmaceutical compositions, animal feed additives, and human dietary supplements.
摘要:
The invention provides a composition of matter of the formula (I): V—L—R, where V is a vector moiety having affinity for an angiogenesis-related endothelias cell receptor, L is a linker moiety or a bond and R is a detectable moiety, characterized in that V is a non-peptidic organic group, or V is peptidic and R is a macromolecular or particulate species providing a multiplicity of labels detectable in in vivo imaging.
摘要:
Microparticulate contrast agents comprising gas or a gas precursor encapsulated by a non-polymeric and non-polymerisable wall-forming material are readily characterisable materials exhibiting surprising structural integrity and stability.
摘要:
The invention provides a composition of matter of the formula (I): V-L-R where V is a non-peptidic organic group having binding affinity for an endothelin receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body. This composition of matter may be used to image diseases and disorders, particularly of the cardiovascular system.
摘要:
The present invention relates to polymer-based gas-containing contrast agents in which microbubbles of gas are encapsulated by non-polymerizable 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).sub.m --CO--O--C(R.sup.1 R.sup.2)--O--CO--(O).sub.n --(I)where R.sup.1 and R.sup.2 each represent a hydrogen atom or a carbon-attached monovalent organic group, or R.sup.1 and R.sup.2 together form a carbon-attached divalent organic group and m and n are each zero or 1.