专利号:WO-2004020401-A1 优先权日:2002-09-02 标题 :Synthesis of sulfonamide derivatives 发明人:KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM 权利人:SYNGENE INTERNAT PRIVATE LTD; KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM 摘要:The novel method of synthesis of sulphonamide derivatives (I), comprising reaction of alkyl-4-halophenylsulfonate with an amine. Formula (I) wherein X is halogen and R1 and R2 are independently selected from group comprising (i) C1 to C15 alkyl, straight or branched, (ii) C3 to C15 cycloalkyl, substituted or unsubstituted, (iii) C2 to C15 alkenyl, straight or branched, (iv) C2 to C15 alkynyl, straight or branched, (v) phenyl or benzyl, substituted or unsubstituted, (vi) heterocycloalkyl, substituted or unsubstituted, (vii) hydrogen, (viii) form with the nitrogen to which they are attached a 3-7 membered heterocyclic moiety such as pyrolidine, piperidine, piperazine, imidazole, pyrazole, (ix) the alkyl in i) may be attached to a moiety selected from cycloalkyl or heterocycloalkyl, substituted or unsubstituted
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:US-8163773-B2 优先权日:2005-07-11 标题 :Organic compounds 发明人:BREITENSTEIN WERNER; ERHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; MASUYA KEIICHI; KONISHI KAZUHIDE; YOKOKAWA FUMIAKI; KANAZAWA TAKANORI; JACOBY EDGAR; MARZINZIK ANDREAS; GROSCHE PHILIPP; KAWAKAMI SHIMPEI 权利人:BREITENSTEIN WERNER; ERHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; MASUYA KEIICHI; KONISHI KAZUHIDE; YOKOKAWA FUMIAKI; KANAZAWA TAKANORI; JACOBY EDGAR; MARZINZIK ANDREAS; GROSCHE PHILIPP; KAWAKAMI SHIMPEI; NOVARTIS AG 摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1, R2, T, R3 and R4 are as defined in the specification.
专利号:WO-2010039911-A1 优先权日:2008-10-01 标题 :Calcilytic compounds 发明人:JEONG JAE U; MARQUIS ROBERT W JR 权利人:GLAXOSMITHKLINE LLC; JEONG JAE U; MARQUIS ROBERT W JR 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.