专利号:US-2012130699-A1 优先权日:2010-11-22 标 题 :Method of molecular design and synthesis of therapeutic and preventive drugs 发明人:MARTYNOV ARTUR; FARBER BORIS S; FARBER SONYA SOPHYA 权利人:MARTYNOV ARTUR; FARBER BORIS S; FARBER SONYA SOPHYA 摘要:Industrial Application: This invention may be used in human and veterinary medicine for the design (creation and synthesis) of therapeutic and preventive drugs that are effective for the treatment of oncological and viral human and animal illnesses and for the design of new medicines. n Summary of the Invention: A new method of design and synthesis of therapeutic and preventive drugs in which a biopolymer target (protein, DNA, RNA, or a mixture of these) is used, and in the capacity of a ligand, the same biopolymer target is used, which is cut into oligomer fragments (nucleases, synthetic nucleases, and proteases); the fragments are modified through changing their charges to the opposite charge (acylation of anhydrides of dicarbonate acids or alkylation with halogen-carbonic acids). Also in the capacity of a ligand, the same biopolymer target is used, which is modified by partially changing the molecules' charges to the opposite with the creation of supramolecular biopolymer assemblies. We used supramolecule assemblies made from oligomers that were products of the hydrolysis of biopolymers, but with a change of the charge of the molecules to the opposite charge, as well as the partial change of the charges of the target biopolymers. n Technical Result: A method of molecular design and synthesis of new, unique therapeutic and preventive drugs based on self-organizing systems. The application of the method will allow a significant cut to expenditures on the design and synthesis of new drugs, expand the activity spectra of existing protein gene-engineered drugs, and create new classes of dynamic therapeutic and preventive drugs that self-adapt to the organism and target.
专利号:US-2013040990-A1 优先权日:2010-02-02 标题 :SYNTHESIS OF DGJNAc FROM D-GLUCURONOLACTONE AND USE TO INHIBIT ALPHA-N-ACETYLGALACTOSAMINIDASES 发明人:FLEET GEORGE WILLIAM JOHN; BUTTERS TERRY DOUGLAS 权利人:UNIV OXFORD; FLEET GEORGE WILLIAM JOHN; BUTTERS TERRY DOUGLAS 摘要:A convenient and scalable synthesis of DGJNAc ID from D-glucuronolactone in an overall yield of 20% is provided. DGJNAc is the first highly potent and specific competitive inhibitor of GalNAcases. DGJNAc ID is also a competitive inhibitor of -hexosaminidases. Synthesis and activity of L-DGJNAc IL is also shown. The use of DGJNAc as a potent and specific inhibitor of GalNAcases will allow useful investigation and treatment of a number of diseases, including Schindler Disease.
专利号:US-2008146656-A1 优先权日:2005-06-01 标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone 发明人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.
专利号:US-8450456-B2 优先权日:2007-12-21 标题:Activating peptide of the synthesis of aquaporins and cosmetic and/or pharmaceutical composition containing it 发明人:DAL FARRA CLAUDE; DOMLOGE NOUHA; BOTTO JEAN-MARIE 权利人:DAL FARRA CLAUDE; DOMLOGE NOUHA; BOTTO JEAN-MARIE; ISP INVESTMENTS INC 摘要:The present invention concerns a peptide of the general formula (I): n R 1 -(AA) n -X 1 —X 2 —X 3 -Pro-X 4 —X 5 —X 7 -(AA) p -R 2 , capable of activating the synthesis of proteins of the family of aquaporins. n The present invention also concerns a cosmetic, nutraceutical or pharmaceutical composition, comprising a peptide of general formula (I) as active principle. The invention also relates to the use of this new active principle in a cosmetic or nutraceutical composition, intended to improve the moisturizing and the barrier function of the epidermis and intended to stimulate cutaneous regeneration. The invention also relates to the use of this new active principle to realize a pharmaceutical composition, and in particular a dermatological composition, intended to regulate and/or stimulate the activity of the aquaporins and to thus treat the pathological dryness of the skin or mucosa. The invention also relates to a method of cosmetic treatment intended to prevent or combat against dryness of the skin and mucosa, and the manifestations of cutaneous ageing.
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-8647848-B2 优先权日:2008-06-13 标题:Enzymatic synthesis of sphingolipids 发明人:HOLLMANN FRANK; THUM OLIVER; TOELLE CHRISTOPH; PROVINZANO ANGELO; KOREVAAR CORNELIS GERRIT NIJS 权利人:HOLLMANN FRANK; THUM OLIVER; TOELLE CHRISTOPH; PROVINZANO ANGELO; KOREVAAR CORNELIS GERRIT NIJS; EVONIK GOLDSCHMIDT GMBH 摘要:The invention relates to the enzymatic synthesis of sphingolipids and compositions that contain sphingolipids from lysosphingolipids and carbonic esters, and to cosmetic, dermatological or pharmaceutical formulations containing said sphingolipids or compositions.
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