专利号:US-6252082-B1 优先权日:1997-01-16 标 题 :Pyridone derivatives, their preparation and their use as synthesis intermediates 发明人:LASSALLE GILBERT; BELLEVERGUE PATRICE; BOURBIER JEAN-CLAUDE; GALTIER DANIEL; MARTIN VALERIE 权利人:SANOFI SYNTHELABO 摘要:The invention concerns compounds of formula (I)in which: R is -NO2 or -NHR3, R3 being hydrogen, -COR4 (R4 selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, -COOR5 (R5 selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), -CONHR6 or SO2R6 (R6 selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), -SO2NR7R8 (R7 and R8 independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1 is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2 is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a -CH2-, -SO2 or -NR1- group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.
专利号:US-2009099367-A1 优先权日:2006-03-06 标题 :Process for preparing a leukotriene antagonist 发明人:BESSA BELLMUNT JORDI; RAFECAS JANE LLORENC; PASTO AGUILA MIREIA; VERDAGUER ESPAULELLA XAVIER; GORDO CAMPON ESTHER 权利人:FARMAPROJECTS S A 摘要:Process for preparing montelukast or a pharmaceutically acceptable salt thereof, especially its sodium salt, that comprises the condensation of an aldehyde and 7-chloro-2-methylquinoline. Moreover, novel intermediates useful for the synthesis of montelukast are described as well as their preparation.
专利号:US-9156840-B2 优先权日:2010-06-18 标题:D2 antagonists, methods of synthesis and methods of use 发明人:LUEHR GARY W; SUNDARAM ARATHI; JAISHANKAR PRIYADARSHINI; PAYNE PHILIP W; DRUZGALA PASCAL 权利人:ALTOS THERAPEUTICS LLC 摘要:Provided are D 2 or D 3 antagonist compounds and pharmaceutical compositions of formula I n nand pharmaceutically acceptable salts thereof, or isomers thereof, wherein R 1 , R 2 and R 3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D 2 or D 3 receptor from the compounds of the invention.
专利号:US-5532408-A 优先权日:1992-10-05 标 题 :α-chain-modified isocarbacyclins and process for the production thereof 发明人:KOGA MASAHIRO; TANAKA TOSHIO; FUJII TAKAO; MASEGI TSUKIO 权利人:TEIJIN LTD 摘要:PCT No. pct/jp93/01407 Sec. 371 Date Apr. 5, 1995 Sec. 102(e) Date Apr. 5, 1995 PCT Filed Oct. 1, 1993 PCT Pub. No. wo94/07838 PCT Pub. Date Apr. 14, 1995.Provided are alpha -chain-modified isocarbacyclins of which the alpha -chain is modified with a phenylene group, a cycloalkylene group or a thiophendiyl group, and these alpha -chain-modified isocarbacyclins show the activity for inhibiting the DNA synthesis of human smooth muscle cell and are expected to be capable of inhibiting the hypertrophy of a blood vessel.
专利号:US-11180523-B2 优先权日:2016-01-04 标 题 :Design, synthesis and use of synthetic nucleotides comprising charge mass tags 发明人:O'HALLORAN JONATHAN J; HEDLEY JOSEPH H 权利人:QUANTUMDX GROUP LTD 摘要:Embodiments of the present disclosure relate generally to reporter compositions which are synthetic nucleotides that comprise nucleotides with a high charge mass moiety attached thereto via a linker molecule. The linker molecules can vary in length in part to enable the high charge mass moiety to extend out from a DNA polymerase complex so that polymerization may not be influenced.
专利号:US-6025177-A 优先权日:1998-03-30 标题 :Asymmetric grignard synthesis with cyclic 1,2 aminoalcohols 发明人:SENANAYAKE CHRIS HUGH; BAKALE ROGER P; FANG QUN KEVIN; GROVER PAUL TIMOTHY; HEEFNER DONALD L; ROSSI RICHARD F; WALD STEPHEN ALAN 权利人:SEPRACOR INC 摘要:Processes for preparing a single enantiomer of an alpha , alpha -disubstituted- alpha -hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. Intermediates useful in the process are also disclosed.