专利号:WO-2012101648-A1 优先权日:2011-01-24 标题:Novel process for the synthesis of enantiomerically pure 2-methoxy-5-[(2r)-2-(4-alkylpiperazin-l-yl)propyl]-benzenesulfonamide 发明人:HAVALDAR FREDDY H; DABHOLKAR BHUSHAN VASANT; MULE GANESH BABAN 权利人:HAVALDAR FREDDY H 摘要:Where R is C1-C3 alkyl, alkenyl A novel process for synthesis of compound of Formula 1 comprising steroselective catalytic reduction of compound of Formula IV under hydrogen gas pressure to obtain an intermediate compound of Formula II, which on coupling in presence of coupling agent and base in presence of organic solvent to obtain compound of Formula X, Formula X on reacting with deprotecting agent in presence of organic solvent results in formation of compound of Formula XI, condensation of Formula XI with alkyl halide results in formation of compound of Formula I.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:RU-2118320-C1 优先权日:1993-03-15 标 题:Enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]- -piperazine, method of their synthesis, method of synthesis of enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-piperazine, enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-piperazine, enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-piperazine derivatives
专利号:US-7179794-B2 优先权日:1998-06-08 标题 :Multivalent macrolide antibiotics 发明人:GRIFFIN JOHN H; PACE JOHN L 权利人:THERAVANCE INC 摘要:Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
专利号:RU-2128659-C1 优先权日:1993-02-19 标题:Substituted derivatives of azolone, method of their synthesis, pharmaceutical composition and method of its preparing
专利号:US-9115102-B2 优先权日:2009-09-17 标题 :N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors 发明人:CHAMBON SANDRINE; CLARY LAURENCE; SCHUPPLI MARLENE 权利人:CHAMBON SANDRINE; CLARY LAURENCE; SCHUPPLI MARLENE; GALDERMA RES & DEV 摘要:The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.