专利号:US-6495693-B2 优先权日:1996-11-22 标题:N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; PORTER WARREN J; THORSETT EUGENE D; WU JING 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:WO-0071569-A1 优先权日:1999-05-26 标题 :Minimal isolation peptide synthesis process using ion-exchange resins as scavenging agents 发明人:TOLLE JOHN C; CALIFANO JEAN-CHRISTOPHE; DHAON MADHUP K; SACHS HOWARD A; BLODGETT JAMES K 权利人:ABBOTT LAB 摘要:A process for the production of a polypeptide having a pre-determined number and sequence of amino acid residues, comprising the steps of first exposing a first substrate amino acid or peptide fragment to a stoichiometric excess of a second reactant amino acid or peptide fragment to form a condensation product; second, contacting the reaction solution from the first step with an insoluble scavenger to sequester the excess of the second reactant amino acid or peptide fragment; third, removing from the solution the sequestered excess second reactant amino acid or peptide fragment; fourth, subjecting the reaction solution to a reaction which removes the protecting group from either the N- or C-terminus of the condensation product of the first step; and fifth, if necessary, repeating the first through fourth steps. The method is capable of large-scale production of peptides in solution, is not subject to the one-terminus-only limitation of the solid-phase method, possesses the 'cleanliness' of the solid-phase method and, like the solid-phase method, is capable of automation. Most importantly, however, the method of the present invention does not require the frequent isolation of intermediates in a lengthy synthetic sequence nor, necessarily, the removal of all contaminating by-products from the reaction mixture prior to subsequent processing steps.
专利号:US-2005032187-A1 优先权日:2003-08-01 标题:Novel peptide-forming enzyme, microbe producing the enzyme and method for producing peptide using them 发明人:YOKOZEKI KENZO; SUZUKI SONOKO; HARA SEIICHI; KATAYAMA SATOSHI 权利人:AJINOMOTO KK 摘要:The present invention relates to a novel enzyme that allows peptide to be produced easily, inexpensively and at high yield without going through a complex synthesis method. More particularly, the present invention provides a novel enzyme that catalyzes a peptide-producing reaction from a carboxy component and an amine component, a microbe that produces the enzyme, and a method for inexpensive production of peptides using this enzyme or microbe. The novel enzyme that efficiently produces peptide was discovered from a newly discovered microbe belonging to the genus Empedobacter , and a method was found that allows peptides to be produced inexpensively and easily.
专利号:US-2005032154-A1 优先权日:2002-07-26 标题 :Method for producing tripeptides and/or peptides longer than tripeptides 发明人:YOKOZEKI KENZO; SUZUKI SONOKO; HARA SEIICHI; ABE ISAO 权利人:AJINOMOTO KK 摘要:It is an object of the present invention to provide a method that allows the production of peptides that are equal to or longer than tripeptides easily, inexpensively and at high yield without going through a complex synthesis method. The inventors of the present invention have found a novel enzyme that efficiently produces a peptide from bacteria belonging to the genus Empedobacter or the genus Sphingobacterium . In the present invention, this enzyme is allowed to act on a carboxy component and an amine component to produce peptides that are equal to or longer than tripeptides.
专利号:US-6096782-A 优先权日:1996-11-22 标 题:N-(aryl/heteroaryl) amino acid derivatives pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
专利号:US-9795613-B2 优先权日:2014-12-10 标题 :GLP-1 receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK 权利人:CELGENE INT II SÀRL 摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.