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-11912654-B2 优先权日:2021-09-03 标 题:Process for stereospecific synthesis of vitamin K2 and its novel intermediates 发明人:MEHTA DILIP; SHASHTRI MAYANK; RAJU BNS; SHAH ASHWIN; VORA PARIN; MAHALE UMAKANT 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to a novel process for the synthesis of stereospecific compounds of Vitamin K2 group in general and Vitamin K2-7. The present disclosure further discloses novel intermediates useful in the synthesis of stereospecific Vitamin K2-7. Compounds of the Vitamin K2 group obtained are crystalline and exhibit well defined melting points.
专利号:US-7273933-B1 优先权日:1998-02-26 标 题 :Methods for synthesis of oligonucleotides 发明人:KROTZ ACHIM H; RAVIKUMAR VASULINGA T 权利人:ISIS PHARMACEUTICALS INC 摘要:Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether solvents to achieve deprotection of protected hydroxyl groups.
专利号:US-5665598-A 优先权日:1994-04-13 标题:Synthesis of chiral N-protected-α-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent 发明人:ABOOD NORMAN A; NOSAL ROGER A 权利人:SEARLE & CO 摘要:A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with alpha -chymotrypsin provides N-Boc-L-propargylglycine in high yield.
专利号:WO-2017175233-A1 优先权日:2016-04-04 标 题:Process for large scale liquid phase synthesis of carbetocin and its novel intermediates 发明人:Mohammed Khalid Anwer; Mohammed Mohosin Layek 权利人:DAVULURI RAMAMOHAN RAO 摘要:A process for large scale liquid phase synthesis of Carbetocin is disclosed. Novel intermediates of formula (A), formula (B), and processes for their preparation are also disclosed.
专利号:US-2014220556-A1 优先权日:2013-02-06 标题 :Method of Design and Synthesis of a New Drug 发明人:MARTYNOV ARTUR; FARBER BORIS S; FARBER SONYA SOPHYA 权利人:MARTYNOV ARTUR; FARBER BORIS S; FARBER SONYA SOPHYA 摘要:A method of design and synthesis of a new drug. This invention may be used in human and veterinary medicine for the design of new drugs that are effective in the treatment of oncological and viral human and animal illnesses and for the design of new medicines. In the method a biopolymer target for the drug action is selected; then the quantity of nitrogen-containing positively charged groups available for modification is calculated. Biopolymer target may be cut into oligomer fragments. Some of calculated nitrogen-containing positively charged groups are substituted with negatively charged groups by combinatorial modification. The obtained supramolecular assemblies are used as drug for the biopolymer target.
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