摘要:
The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro by using carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using carbazole-based fluorophores.
摘要:
The present invention relates to conjugates for differentiating between healthy and unhealthy tissue, methods of producing such conjugates as well as their use.
摘要:
The present invention provides an anticancer compound having the structure: ##STR1## wherein R is --H, --CH.sub.3, or --C.sub.2 H.sub.5 ; R1 and R2 are independently --H, --OH, --NH.sub.2, --OCH.sub.3, --C(CH.sub.3).sub.3, or a halogen atom; n is 2 to 6; X and X' are independently --N or --NO.sub.2 ; Y and Y' are independently --N, --CH, or --H; and the double-slash represents a double bond or no bond; such that when X or X' is --N, Y or Y' is --CH or --N, and the double-slash is a double bond, and when X or X' is --NO.sub.2, Y or Y' is --H, and the double-slash is no bond. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier.
摘要翻译:本发明提供具有以下结构的抗癌化合物:其中R为-H,-CH 3或-C 2 H 5; R 1和R 2独立地是-H,-OH,-NH 2,-OCH 3,-C(CH 3)3或卤素原子; n为2〜6; X和X'独立地是-N或-NO 2; Y和Y'独立地是-N,-CH或-H; 双斜杠代表双键或无键; 使得当X或X'为-N时,Y或Y'为-CH或-N,双斜线为双键,当X或X'为-NO 2时,Y或Y'为-H, 而双斜杠是没有纽带的。 本发明还提供包含上述化合物和药学上可接受的载体的药物组合物。
摘要:
The present invention is in the field of pharmaceuticals and chemical industries. In particular, one aspect of the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro and in vivo via magnetic resonance and florescence imaging by using modified carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using the modified carbazole-based fluorophore. The modified carbazole-based fluorophore according to an embodiment of the present invention is prepared by conjugating a carbazole-based fluorophore with magnetic nanoparticles to form a conjugate which is permeable to blood brain barrier of a subject being introduced therewith.
摘要:
Novel azo compounds and their bioconjugates for phototherapy and/or photodiagnosis of tumors and other lesions. The azo derivatives of the present invention are designed to absorb at the low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photoexcitation of the azo compound, with the tissue of interest.
摘要:
Compounds, compositions, their methods of preparation and use in binding bio-affecting substances to the surface membrane of bioparticles, such as enkaryotic cells, without producing appreciable detrimental effect on morphology or physiological function of cells.
摘要:
The present invention pertains to a preparation for diagnosing the transport function of the fallopian tube and to a method for making such a preparation.The diagnostic preparation for investigation of the transport function of female fallopian tube, comprises a suspension of a biocompatible, biodegradable, and, if desired, labelled particles, in a vehicle commonly used for parenteral applications wherein the particles have a spherical shape with diameters in the region 10 to 600 um, which are formed from a soft hydrophilic gel based on a polymer selected from the group comprising additionally crosslinked water-soluble nontoxic and biodegradable inert polysaccharides and physiologically inert water-soluble and biodegradable poly(amino acids), polypeptides, and their derivatives, which may contain physiologically active substances. The particles retain their shape and size in the environment of peritoneal cavity and uterotubal tract for at least 80 hours with the subsequent degradation to nontoxic product within 5 to 60 days.A method for preparation of the diagnostic preparation comprises dispersing an aqueous solution of physilogically inert, biodegradable polymer selected from the group of polysaccharides, poly(amino acids), polypeptides, and their derivatives, in a medium of nonpolar water-immiscible solvent, to 10 wt. % of the polymer having a degree of polymerization of 50 to 500, said suspension containing of 80 to 100 mol. % of .gamma.-alkyl-L-glutamate units and 0 to 20 mol. % units of L-glutamic acid, units as a suspension stabilizer, with mixing sufficient to form polymeric spherical particles with diameter 100 to 600 um, which are transferred into the gel state with bifunctional crosslinking agents. The particles are washed and then dispersed in an aqueous solution. The resulting suspension is then sterilized by heat.
摘要:
The present invention provides compounds useful as novel near-infrared labels, compositions containing these compounds, and methods of using the near-infrared labels to identify targets in vitro, in situ and in vivo. The invention also provides small or large molecule conjugates between targeting agents and NIR labels, as well as methods and kits thereof, that can be used in diagnostics and treatment of diseases related to microbes in mammalian animals.
摘要:
The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro by using carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using carbazole-based fluorophores.