专利号:WO-0120995-A9 优先权日:1999-09-23 标题:Compounds directed against pilus biogenesis and activity in pathogenic bacteria; methods and compositions for synthesis thereof 发明人:KIHLBERG JAN; LARSSON ANDREAS; SVENSSON ANETTE; FEX TOMAS; HULTGREN SCOTT J; PINKNER JERRY 权利人:UNIV WASHINGTON; KIHLBERG JAN; LARSSON ANDREAS; SVENSSON ANETTE; FEX TOMAS; HULTGREN SCOTT J; PINKNER JERRY 摘要:Many Gram-negative pathogens assemble adhesive structures on their surfaces that allow them to colonize host tissues and cause disease. Novel compositions which inhibit or prevent the formation of a pilus chaperone-subunit complex are disclosed. Interfering with the function of the pili chaperone negatively affects the chaperone/usher pathway which is one molecular mechanism by which Gram-negative bacteria assemble adhesive pili structures and thus prevent or inhibit pilus assembly. Also provided are methods for the treatment or prevention of diseases caused by tissue-adhering pilus-forming bacteria by inhibiting the function of pilus chaperones. Also provided are pharmaceutical preparations capable of inhibiting or preventing the formation of a pilus chaperone-subunit complex. Also provided are methods of synthesizing the N-substituted amino acid compounds and compounds useful for the synthesis thereof. In particular, novel fluorinated linker compounds and methods of synthesis are provided. Methods for using the fluorinated linker compounds in methods of solid-phase synthesis of the N-substituted amino acid compounds are also disclosed.
专利号:US-8193360-B2 优先权日:2003-07-31 标 题:Radiolabelled fluorobenzamide analogues, their synthesis and use in diagnostic imaging 发明人:MACH ROBERT H; TU ZHUDE 权利人:MACH ROBERT H; TU ZHUDE; UNIV WASHINGTON 摘要:Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18 F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123 I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
专利号:CN-1835911-A 优先权日:2003-09-01 标题 :Process for the synthesis of N- [ -1-carboxybutyl ] - -alanine esters and use of the compounds in the synthesis of perindopril
专利号:US-10774043-B2 优先权日:2016-05-06 标题 :Glycolactam compounds, process for preparation and uses thereof 发明人:BHATTACHARYA ASISH KUMAR; CHAND HEMENDER RAMI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses compounds of Formula I, n nwherein each of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are independently selected from H, OBn, OH, CH 2 OBn, CH 2 OH, CH 3 ; R 9 is selected from alkyl, substituted alkyl, hydroxyl alkyl, alkenyl, benzyl; process for preparation of N-alkylated glycolactam compounds of Formula I and their use for the synthesis of piperidine alkaloids and their analogues.
专利号:US-2012172336-A2 优先权日:2009-03-19 标 题:Fosfluconazole Derivatives, Synthesis, and Use in Long Acting Formulations 发明人:GONNISSEN YVES; VOORSPOELS JODY 权利人:GONNISSEN YVES; VOORSPOELS JODY; SEPS PHARMA N V 摘要:The invention relates to a compound of formula (1) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R 1 to R 2 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.
专利号:WO-2020018581-A1 优先权日:2018-07-16 标题 :Synthesis of straight-chain lepidopteran pheromones through one- or two- carbon homologation of fatty alkenes