Abstract:
PROBLEM TO BE SOLVED: To obtain compositions containing phenylacetate (PAA), pharmaceutically acceptable salts thereof, derivatives thereof or analogues thereof, intended to regulate the lipid metabolism of subjects, reduce the serum triglycerides of subjects, sensitize subjects to radiotherapy, inhibit the production of IL-6 in cells, induce the production of TGFα (transforming growth factor α) in cells, inhibit the production of TGF-β2 in cells, treat the AIDS-related dysfunction of subjects' central nervous system, enhance the immunological surveillance of subjects, treat hemoglobin-unrelated morbid states, and promote curing the wounds of subjects. SOLUTION: The pharmaceutical compositions and the like for sensitizing the subjects to radiotherapy and containing a therapeutically effective amount of phenylacetate derivative of formula (1), salts thereof, stereoisomers thereof, or mixtures thereof are provided. COPYRIGHT: (C)2005,JPO&NCIPI
Abstract:
PROBLEM TO BE SOLVED: To obtain compositions containing phenylacetate (PAA), pharmaceutically acceptable salts thereof, derivatives thereof or analogues thereof, intended to regulate the lipid metabolism of subjects, reduce the serum triglycerides of subjects, sensitize subjects to radiotherapy, inhibit the production of IL-6 in cells, induce the production of TGFα (transforming growth factor α) in cells, inhibit the production of TGF-β2 in cells, treat the AIDS-related dysfunction of subjects' central nervous system, enhance the immunological surveillance of subjects, treat hemoglobin-unrelated morbid states, and promote curing the wounds of subjects. SOLUTION: A therapeutic method for modulating subjects' fat metabolism comprises a step for administering a therapeutic amount of phenylacetate derivative of formula (1), salts thereof, stereoisomers thereof, or mixtures thereof. COPYRIGHT: (C)2005,JPO&NCIPI
Abstract in simplified Chinese:本发明提供一系列hGH-RH(1-29)NH2之新颖的合成拮抗性类似物。这些类似物可在脑下垂体的GH-RH受体上抑制内源性hGH-RH之活性,因此可避免生长激素的释放。类似物也可经由对癌细胞的直接作用而抑制人类癌症的增殖。相较于先前所说明的类似物,新的类似物之较高的抑制性能系导源于各种氨基酸的取代。
Abstract:
Procedimiento de preparación de un compuesto lifolizado de la fórmula (1):**Fórmula** en la que: P es hidrógeno o un resto de protección de grupo amino; R es hidrógeno o alquilo; A es 0, 1, ó 2; R1, R2, y R3 son cada uno independientemente hidrógeno, alquilo, cicloalquilo, arilo, o -CH2-R5; R5, en cada caso, es arilo, aralquilo, alquilarilo, cicloalquilo, heterociclilo, heteroarilo, o -W-R6, en el que W es un calcógeno y R6 es alquilo; en la que la parte de anillo de cualquiera de dichos arilo, aralquilo, alquilarilo, cicloalquilo, heterociclilo o heteroarilo en R1, R2, R3 o R5 puede estar opcionalmente sustituida; y Z1 y Z2 juntos forman un resto derivado de manitol; comprendiendo el procedimiento: (a) preparar una mezcla que comprende (i) agua, (ii) un compuesto de fórmula (3)**Fórmula** en la que P, R, A, R1 y R3 son como se han definido anteriormente; y Z' y Z'' son OH; y (iii) manitol; y (iv) un disolvente miscible en agua; en la que el manitol y el compuesto de fórmula (3) están presentes en una proporción p/p de 10:1; y (b) liofilizar la mezcla; en el que: el compuesto de fórmula (1) es un éster de manitol del ácido N-(2-piracino)carbonil-L-fenilalanina-L-leucina borónico; y el compuesto de fórmula (3) es el ácido N-(2-piracino)carbonil-L-fenilalanina-L-leucina borónico.
Abstract:
This invention provides folic acid-containing pharmaceutical compositions comprising either an oral contraceptive or a hormone replacement composition. This 5 invention also provides methods of administering folic acid to a subject using the instant pharmaceutical compositions. Finally, this invention provides a drug delivery system useful for administering the instant pharmaceutical compositions.
Abstract:
The present invention provides a method of identifying novel broadly crossreactive neutralizing monoclonal anti-bodies using sequential antigen panning of phage display libraries, antibodies obtained in accordance with such a method, as well as fusion proteins and conjugates comprising same, and related isolated or purified nucleic acid molecules, vectors, host cells, compositions, and methods of use to inhibit an infection, reduce the severity of an infection, treat an infection, treat an infection, and inhibit cancer. Flow chart of sequential antigen panning (m12 and m14) pComb3H phage Preabsorption on pre-washed M-280 streptavidin beads Depletion with sCD4 1" round of panning (rp) against 50 nM biotinylated gpl40sg. 6-sCD4 1" round panned library Preabsorption on pre-washed M-280 streptavidin beads Depletion with sCD4 2 nd rp against 10 nM biotinylated gpl4089.6-sCD4 complexes 2 "d round panned library Preabsorption on pre-washed M-280 streptavidin beads 3 rd rp against 2 nM biotinylated gpl40sg.6-sCD4 complexes 3rd round panned library 4, rp against 2 nM biotinylated gpl40WHXB2-SCD4 complexes 4h round panned library screen individual clones from 4*, 5* and 6"1 round panned libraries by phage ELISA using gpl20/l4089.6/HBx2 and gpl20 Ma and their complexes with sCD4 as antigens selection of clones with highest binding activity to all antigens
Abstract:
The invention provides a microarray and methods for producing a protein microarray. The array comprises multiple nucleic acid molecules immobilized on a substrate, each comprising (i) a protein-binding domain and (ii) a nucleic acid sequence encoding a fusion protein comprising a polypeptide of interest and a DNA-binding protein that binds the protein-binding domain, and one or more fusion proteins produced from the multiple nucleic acid molecules. Each fusion protein is immobilized on the substrate via binding to a nucleic acid sequence comprising the protein-binding domain present on the nucleic acid molecule from which the fusion protein is produced or on the substrate. The invention also provides a method of analyzing protein interactions with, for example, other proteins, lipids and drugs.
Abstract:
Disclosed are compounds of the formula (I) wherein R is C-C alkyl, which may be optionally further substituted with one or more C-C cycloalkyl groups, or a C-C cycloalkyl, which may be optionally substituted with one or more C-C alkyl groups, R’ is hydrogen or lower alkyl, R” is a C-C alkyl or halo, and the bond between C14 and C15 can be a single bond or double bond. Also disclosed are pharmaceutical compositions comprising such compounds and methods of use thereof. These compounds can find use in treating a number of diseases or conditions such as hypogonadism, hypergonadism, osteoporosis, and anemia, in providing hormonal therapy and contraception, as an anabolic agent, and in suppressing the release of hormones such as the luteinizing hormone.