摘要:
The invention provides compounds of general Formula (I)
wherein,
A is a cyclic group being an optionally substituted aryl group or an aromatic heterocyclic group; or A is a cyclic group R A1 R A2 C-CR A3 R A4 wherein R A2 and R A3 , together with the carbon atoms to which they are attached form an optionally substituted saturated or unsaturated carbocyclic or heterocyclic group and R A1 and R A4 are as defined below or together form a bond; or A is a non-cyclic group R A1 R A2 C-CR A3 R A4 wherein R A1 - R A4 are as defined below and R A2 and R A3 may optionally together form a bond; Z is a carbon or a heteroatom; n is selected from 0, 1, 2 or 3; and R A1-A4 , W, X and Y may be the same or different and each are selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally protected hydroxy, optionally substituted amino, optionally substituted alkoxy, optionally substituted alkenoxy, optionally substituted alkynoxy, optionally substituted aryl, optionally substituted heterocyclyl, carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, optionally substituted alkylthio, halogen, nitro, sulfate, phosphate and cyano, or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group; or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof; provided that the compound is not one selected from Lamellarin A-N, S-X; D, L, K, M, N-triacetate; I-acetate; G-trimethyl ether; or T, U, V, Y-20-sulphate. Such compounds are useful as chemotherapeutic agents.
摘要:
A method of preventing or treating infection by a range of fungal pathogens in an animal or plant or stored plant product comprising administering an effective amount of a sugar acid, in particular mannonic acid, gluconic acid or galacturonic. The sugar acid can be delivered by a biocontrol that can manufacture the sugar acid. An exemplified biocontrol is Pseudomonas strain AN5, which is characterized by the capacity to convert aldose to sugar acid. Also disclosed are nucleotide sequences from enzymes in the Pseudomonas PQQ enzyme pathway which may be used to transform microorganisms and plants so that they produce sugar acids at levels sufficient to control the growth or viability of pathogens.
摘要:
Therapeutic compositions including a species of Coxiella or one or more antigenic components therefrom or analogous or homologous components thereof are disclosed. These compositions are useful in preventing, inhibiting, delaying onset of or otherwise ameliorating the effects of an autoimmune disease in a mammal, particularly insulin-dependent diabetes mellitus (IDDM). They are also useful in prolonging survival of islet tissue transplanted into a mammal.
摘要:
The invention relates to compounds of the following formula (I). In these compounds, R1, R2, R3 and R4 are each independently a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms, or hydrogen, substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, alkyloxycarbonyl, or alkylaminocarbonyl. At least two of R1, R2, R3 and R4 comprise the substituted or unsubstituted cyclitol. The linker can be any one of the following: -(CH2)w-, -(CH2)x-C6H4-(CH2)x-, -(CH2)y-NR5- (CH2)y-, and -(CH2)z-HCR6-(CH2)z-; wherein: w, x, y and z are independently an integer having a value of 0-10; R5 is a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms; and, R6 is -OH, -OSO3Na, -OSO3Na substituted with alkyl, cycloalkyl or aryl, or substituted or unsubstituted alkyl, cycloalkyl or aryl. The compounds can also include substituted or unsubstituted cyclitol carbamides with the linker bond at the carbamide nitrogen. In other embodiments, the invention provides pharmaceutical compositions which include the compounds, and use of the compounds in the prevention or treatment in a mammalian subject of a disorder resulting from angiogenesis, metastasis, inflammation and/or coagulation/thrombosis.
摘要:
The present invention relates to methods for the synthesis of chemical compounds for screening as potential tubulin polymerization inhibitors. The invention also provides chemical compounds with tubulin polymerization inhibitor activity.
摘要:
Antibodies, including monoclonal antibodies, specific for proliferating/angiogenic human endothelial cells such as human umbilical vein endothelial cells and human umbilical artery endothelial cells, and conjugates of these antibodies with a toxin material or label, are useful for inhibition of angiogenesis or for treatment of angiogenesis-dependent disease.
摘要:
A method and an apparatus are described for simultaneously assessing the functional status of component parts of the nervous system by presenting sparse stimuli to one or more parts of the sensory nervous system. Sparse stimuli consist of temporal sequences of stimulus conditions presented against a baseline null stimulus condition, where the non-null stimulus condition, or conditions, are presented relatively infrequently. The low probability of encountering a stimulus differing from a baseline or null stimulus condition in sparse stimulus sequences insures that gain control mechanisms within the nervous system will increase the neural response magnitude and also bias the measured responses to those neurone populations having such gain controls. The consequently increased response amplitudes ensure more reliably recorded responses than are obtained with non-sparse stimuli.
摘要:
Novel magnesiosilicate compounds for use in detergent compositions and as water softeners have a calcium binding capacity of at least 10 mg CaO per gram, a magnesium binding capacity of at least 10 mg MgO per gram and a calcium binding rate of no more than 300 seconds, all at room temperature. The compounds have a stuffed silica polymorph-related structure or a layered structure with a broad X-ray powder diffraction peak at a d-spacing of between 11 and 17 ANGSTROM . The compounds have an anhydrous composition MaMgbAlcSi1-(b+c)Od, where M = alkali, 0.0
摘要:
A cell for forming a composite hard material and hard materials and methods of forming composite hard materials are disclosed. A cell (10) in which the article is formed includes a talc outer sleeve (12), a glass sleeve (14) and a reflecting foil (22). A heater (18) is arranged inwardly of the foil (22) and a barrier layer (16) is arranged inwardly of the glass sleeve (14). A central column (20) is defined for receiving the charge of material (50) from which the hard composite material is to be formed. The charge material is located in a mould (76, 100) which can define the final shape of the article thereby avoiding the need for additional machining, and the mould and charge material are subject to high temperature and pressure to form the composite material whilst maintaining the charge subject to hydrostatic pressure during the application of pressure and high temperature and maintaining a low temperature gradient across the charge during formation of the composite hard material to reduce uneven pressurisation of the composite hard material. The article may also be formed by forming first and second mixtures (120, 130) of composite hard material so as to form an outer surface on the article which has a higher hard particle content than an interior core portion of the article.
摘要:
A method and apparatus for forming a coating on a substrate. The system (1) comprises an electron-beam evaporator (5) to produce an evaporant (6) from a source material, a plasma generation chamber (3), within which a magnetoplasma is generated, and a magnetic field supply means (10) to apply a magnetic field (11) to the apparatus (1), to transport the magnetoplasma (60) to the substrate (12).