专利号:US-4271172-A 优先权日:1979-06-25 标 题 :6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acids, antibacterial compositions thereof and method of use thereof 发明人:RODRIGUEZ LUDOVIC; LECLERCQ JACQUES; YKMAN PIERRE; COSSEMENT ERIC 权利人:UCB SA 摘要:6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acids, salts and esters thereof of the formula ##STR1## wherein R 1 is hydrogen, benzyl or an alkali metal or ammonium ion and R 2 is methyl, phenyl or benzyl and process for preparing the same. n These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to penicillins, besides own antibiotic activity with a broad antibacterial spectrum. Therefore, they are useful as antibacterials agents and as therapeutic agents for humans and for animals in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.
专利号:US-9822116-B2 优先权日:2008-09-05 标 题:Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds 发明人:WU GEORGE G; WERNE GERALD; FU XIAOYONG; ORR ROBERT K; CHEN FRANK XING; CUI JIAN; SPRAGUE VICTORIA M; ZHANG FUCHENG; XIE JI; ZENG LIANSHENG; CASTELLANOS LOUIS PETER; CHEN YUYIN; POIRIER MARC; MERGELSBERG INGRID 权利人:OPKO HEALTH INC 摘要:This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
专利号:US-6534627-B1 优先权日:1989-10-23 标题:Synthesis and use of amino acid fluorides as peptide coupling reagents 发明人:CARPINO LOUIS A; EL-FAHAM AYMAN AHMED 权利人:RES CORP TECHNOLOGIES INC 摘要:The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: n or the acid fluoride salts thereof wherein n BLK is an N-amino protecting group; n AA is an amino acid residue; and n X is absent or a protecting group. n The amino acid fluoride is useful as a coupling agent in peptide synthesis.
专利号:US-6486350-B1 优先权日:1998-09-30 标 题:Biological reagents and methods for determining the mechanism in the generation of β-amyloid peptide 发明人:AUDIA JAMES E; HYSLOP PAUL A; NISSEN JEFFREY S; THOMPSON RICHARD C; TUNG JAY S; TANNER LAURA I 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are biological reagents which comprise compounds that inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of beta-amyloid peptide.
专利号:US-2014031549-A1 优先权日:2008-09-05 标题:Process and Intermediates for the Synthesis of 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one Compounds
专利号:US-2016145256-A1 优先权日:2008-09-05 标题:Process and intermediates for the synthesis of 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds