205 results about "Functional derivative" patented technology

The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (N(t)RTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

A radiation curable ink composition comprising at least one initiator and at least one polyhedral oligomeric silsesquioxane (POSS) represented by the following empirical formula [R(SiO1.5)]n wherein n=4,6,8,10,12,14,16 and larger and each R is independently hydrogen, an inorganic group, an alkyl group, an alkylene group, an aryl group, an arylene group, or non-heterocyclic group-containing organo-functional derivatives of alkyl, alkylene, aryl or arylene groups; and a process for obtaining a colourless, monochrome or multicolour ink jet image comprising the steps of jetting one or more streams of ink droplets having the above-mentioned composition onto an ink-jet ink receiver material, and subjecting the obtained image to radiation curing.

A multi-component curable composition which is reactive upon admixing of the components and which comprises:(i) an acrylic polymer having acetoacetoxy functionality; and(ii) an acetoacetoxy functional derivative of a low molecular weight polyol; and(iii) a crosslinking component comprising at least one imine functional compound having an average of at least two imine groups per molecule which are reactive with acetoacetoxy functionality.

The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.

New chemotherapeutic medicaments and certain medical uses and methods for use of such chemotherapeutic medicaments for treatment of disease in human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. Preferably, the halogenated xanthene is Rose Bengal or a functional derivative of Rose Bengal. The halogenated xanthenes constitute a family of useful chemotherapeutic agents that afford selective, persistent accumulation in certain tissues. In preferred embodiments, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs, the mouth and digestive tract and related organs, the urinary and reproductive tracts and related organs, the respiratory tract and related organs, the circulatory system and related organs, the head and neck, the endocrine and lymphoreticular systems and related organs, various other tissues, such as connective tissues and various tissue surfaces exposed during surgery, as well as various tissues exhibiting microbial or parasitic infection. In another preferred embodiment, such medicaments are produced in various formulations useful for intracorporeal or topical administration, including in liquid, semisolid, solid or aerosol delivery vehicles.

The present invention is directed to a recombinant enzymes having alcohol and aldehyde dehydrogenase activity which comprises one or more recombinant polypeptides selected from the group consisting of polypeptides which are identified by SEQ ID NO 5, SEQ ID NO 6, SEQ ID NO 7, SEQ ID NO 8 and chimeric recombinant polypeptides that are a chimeric combination of at least two of the following amino acid sequences identified by SEQ ID NO 5, SEQ ID NO 6, SEQ ID NO 7, SEQ ID NO 8 and functional derivatives of the polypeptides identified above which contain addition, insertion, deletion and / or substitution of one or more amino acid residues, wherein said enzymatic polypeptides have said alcohol and aldehyde dehydrogenase activity. DNA molecules encoding the recombinant polypeptides, vectors comprising such DNA molecules, host cells transformed by such vectors and processes for the production of such recombinant enzymes are provided. Furthermore, the recombinant enzymes having alcohol and aldehyde dehydrogenase activity are used for obtaining aldehydes, ketones or carboxylic acids, and specifically, 2-keto-L-gulonic acid an intermediate for the production of L-ascorbic acid (vitamin C).

A pharmaceutical aerosol formulation comprising particles of (a) formoterol or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof and (b) mometasone or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative, thereof dispersed in a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and a mixture thereof, and a bulking agent having a mass median diameter of less than one micron.

The invention is directed to an improved drug delivery system that includes a micelle, comprising polyethylene glycol and a lipid component, and a pharmaceutical agent dispersed in the lipid component. The delivery system may also include a targeting ligand. The micelle delivery system of the invention is capable of stabilizing, inter alia, poorly soluble pharmaceutical agents and increasing their delivery efficacy. Appropriate pharmaceutical agents useful in the system of the invention include anti-inflammatory agents, agents for photodynamic therapy, anti-tumor agents, anti-neoplastic agents, anti-metastatic agents, and imaging agents, as well as hydrophobized derivatives thereof. Specifically, the pharmaceutical agent can be porphyrin, chlorine-6-trimethyl ester, tamoxifen, paclitaxel, 1,3-bis(2-chloroethyl)-1-nitrosourea, camptothecin, ellipticine, rhodamine, dequalinium, diphenylhexatriene, vitamin K3, diethylene triamine pentaacetic acid, or a functional derivative thereof. The micelles in the system of the invention have low critical micellar concentration and high kinetic stability, which provides great advantages in biodistribution, for example, accumulation at the site of a tumor.

The present invention relates to compositions and use of fluidized polymer suspensions containing allyloxy linkage and its functional derivatives, and water soluble polymers for use in oil field applications as fluid additives for drilling and cementing processes.

The present invention relates to therapeutic combinations of [2-(6-amino-purin-9 yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2 hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (−)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and / or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

An energy curable ink composition comprising an acrylate-functional derivative of soybean oil and one or more further acrylate-functional materials is suitable for printing on a cold-set lithographic press and is cured by exposure to an actinic radiation source located on the press.

The present invention is directed to compounds of the general formula (I) or pharmaceutical acceptable salts or physiologically functional derivatives thereof wherein: n is a non-aromatic ring system containing two to seven carbon atoms, wherein the ring system can contain one ore two double bonds; X is C, CH or CH2; Y is selected from C, CH, CH2, S, NR, CH2-CH2, H2C—CH, HC—CH2, C—CH2, H2C—C, or C—C; one or more of the hydrogen atoms can optionally be substituted by one or more substituents R′; each of the dotted lines means a single, a double or triple bond with the exclusion of a combination of a triple with triple bond and a double with a triple bond; R′ is independently H, —CN, alkyl, cycloalkyl, aminoalkyl, alkylamino, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, hydroxyalkylamino, halogene, haloalkyl, haloalkyloxy; R is H, an alkyl or cycloalkyl group; Z is CH, C, or P; p is 0 or 1.

The use is described of the long pentraxin PTX3 (PTX3) or one of its functional derivatives as an agent inhibiting the activity of growth factor FGF-8, for the preparation of a medicine for the treatment of tumour diseases associated with abnormal activation of growth factor FGF-8.

Methods for improving binding of a proteinaceous substance to cell-wall material of a Gram-positive bacterium are disclosed. The proteinaceous substance includes an AcmA cell-wall binding domain, homolog or functional derivative thereof. The method includes treating the cell-wall material with a solution capable of removing a cell-wall component such as a protein, lipoteichoic acid or carbohydrate from the cell-wall material and contacting the proteinaceous substance with the cell-wall material.

The invention belongs to the technical field of power systems and relates to an improved discrimination method of Lyapunov robust stability of a power system containing uncertain delay links, which ischaracterized by solving the Lyapunov functional of a delay system based on the Krasovskii theory, then expressing the derived function of a system trajectory from the functional by a group of linearmatrix inequalities (LMI), reducing the conservation of the criterion by introducing a few necessary loose terms in the process of deducing functional derivatives and then transforming the disturbance terms containing uncertainties by utilizing the Schur complement, thereby obtaining the stability criterion. The method of the invention has the advantages of less conservation and high operation efficiency.

A method and compositions for regulating bone density and / or circulating lipid levels in a subject based on the combined administration of at least one isoflavone or functional derivative, equivalent or analogue thereof and at least one lipid regulating drug. The method and compositions are applicable to the beneficial alteration of blood lipoprotein levels, the improvement of vascular compliance, the decrease in the propensity of thrombogenic events, the reduction in the risk of vascular disease, coronary heart disease, and arteriosclerosis, and to the treatment or prevention of osteoporosis.

The invention is based on the discovery that STM / Hop promotes proliferation of human glioblastoma-derived cells but not of normal astrocytes and that the proliferation requires the binding of STM / Hop to PrPC. The invention is directed to methods for treating cancer which rely on interfering with the Hop-PrPC interaction and to peptides, and antibodies raised against the peptides, which directly provide that interference. The invention is further based on the discovery that STI1230-245 peptide and its human homologue Hop23o-245 provide the desired interference with the STI1 / Hop-Pre interaction and inhibit the STI 1 / Hop-induced proliferation of glioma and glioblastoma cells. The invention is thus further directed to methods of treating cancer that employ these peptides and functional derivatives thereof, and antibodies directed to the peptides and derivatives. The invention is further directed to means of treating cancer which involve reducing the effective amount of Hop or reducing the expression of Hop. The invention is further directed to means of alleviating or eliminating the side effects of drug therapy and radiotherapy used in treating patients with brain cancers.

A novel method of treating and preventing viral diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of viral infections and the diseases associated with such viral infections. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made compositions comprising a substance exhibiting Tubercin and / or SSM activity or a functional derivative thereof.

Accordingly, the invention relates to a pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof, and at least one NMDA receptor antagonists or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof.

A neuroprotective composition for protecting neuronal cells against oxidative stress and methods for using and preparing the same. More particularly, the neuroprotective composition of the invention comprises a therapeutically effective amount of ceruloplasmin or a functional derivative thereof. The neuroprotective composition is characterized in that it protects neuronal cells from reactive oxygen species such as .O2- and .OH. In a preferred embodiment, the neuroprotective composition further comprises an antioxidant consisting of catalase or of an amphiphilic physiological antioxidative solution comprising a mixture of pyruvate, antioxidant, and lipid(s) such as fatty acids. The neuroprotective composition could be used for the treatment of brain trauma, brain or cerebrovascular ischemia, neurodegenerative diseases, poisoning of neuronal cells, the diminution of drugs side effects and for preservation of neuronal grafts.

A pharmaceutical composition for rectal or vaginal application, characterized in that it contains as active substance the platinum complex of general formula wherein A each independently is an —NH3 group or an amino group containing 1 to 18 carbon atoms, B each independently is a halogen atom, a hydroxy group or a —O—C(O)—R group wherein R each independently is hydrogen atom or an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group containing 1 to 10 carbon atoms or functional derivatives of these groups, and X each independently is a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X together form a dicarboxylate group containing 2 to 20 carbon atoms, and a hydrophilic gel-forming base, comprising gelatin, water and glycerol.

The novel positively charged prodrugs of acetylsalicylic acid and its analogues in the general formula(1) 'Structure 1' were designed and synthesized. The compounds of the general formula(1) 'Structure 1' indicated above can be prepared from functional derivatives of ASA or its analogues,(for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and push the pro-drug into the cytosol. The experiment results suggest that the pro-drug, diethylaminoethyl acetylsalicylate.AcOH, diffuses through human skin -400 times faster than acetylsalicylic acid itself and -100 times faster than ethyl acetylsalicylate. In plasma, 80% of these pro-drugs can change back to the drug in a few minutes. The pro-drugs can be used medicinally in treating any aspirin-treatable conditions in humans or animals and be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of aspirin, most notably GI disturbances such as dyspepsia, gastroduodenal bleeding, gastric ulcerations, and gastritis. Controlled transdermal administration systems of the prodrug enable the aspirin in the blood to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of aspirin.

The present invention belongs to the field of polymer compound material. The invention discloses an O-quaternary-N-thiourea chitosan, a preparation method and application thereof, and the chitosan is a chemical modified functional derivative of chitosan. The preparation method of the O-quaternary-N-thiourea chitosan comprises the following steps: adopting chitosan as a raw material and carrying out reaction with benzaldehyde to obtain chitosan Schiff base, then carrying out reaction with 2,3-glycidyl trimethyl ammonium chloride to obtain O-quaternary-N-chitosan Schiff base; carrying out deprotection of an amino group positioned on the second carbon atom (C2) of the O-quaternary-N-chitosan Schiff base through a methanol-hydrochloric acid solution to obtain O-quaternary chitosan, adding the O-quaternary chitosan to the mixture of ammonium thiocyanate and chloroacetyl chloride to carry out reaction, and then obtaining the O-quaternary-N-thiourea chitosan. The O-quaternary-N-thiourea chitosan provided in the invention achieves a substantial increase in antibacterial property compared with chitosan. The invention can be used in a plurality of application fields of antibacterial material, daily chemical products, industrial wastewater treatment and the like.