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:RU-2069658-C1 优先权日:1989-02-17 标 题 :Method of synthesis of pure enantiomers of 1,4-dihydropyridines, pure enantiomers of 1,4-dihydropyridines and isothioureides
专利号:US-2008242662-A1 优先权日:2005-05-31 标题 :Organic Compounds 发明人:NIHONYANAGI ATSUKO; TOYAO ATSUSHI; IWAKI YUKI; MASUYA KEIICHI 权利人:NIHONYANAGI ATSUKO; TOYAO ATSUSHI; IWAKI YUKI; MASUYA KEIICHI 摘要:The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof 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; 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; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, n n n n n n n n n n wherein R1, R2, R11, C, E and D are as defined in the specification.
专利号:US-2009281161-A1 优先权日:2006-06-13 标 题:Organic Compounds 发明人:MAIBAUM JUERGEN KLAUS; LORTHIOIS EDWIGE LILIANE JEANNE 权利人:MAIBAUM JUERGEN KLAUS; LORTHIOIS EDWIGE LILIANE JEANNE 摘要:Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-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-2009270417-A1 优先权日:2006-06-13 标 题:Organic Compounds 发明人:MAIBAUM JUERGEN KLAUS; LORTHIOIS EDWIGE LILIANE JEANNE; BUEHIMAYER PETER 权利人:NOVARTIS AG 摘要:Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-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-2008194629-A1 优先权日:2005-05-03 标题 :3-Mono-and 3,5-Disubstituted Piperidine Derivatives as Renin Inhibitors 发明人:BAESCHLIN DANIEL KASPAR; BREITENSTEIN WERNER; EHRHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; RUDISSER SIMON; VANGREVELINGHE ERIC; IRIE OSAMU; UMEMURA ICHIRO; SUZUKI MASAKI; MOGI MUNETO; KANAZAWA TAKANORI; YOKOKAWA FUMIAKI; NIHONYANAGI ATSUKO 权利人:BAESCHLIN DANIEL KASPAR; BREITENSTEIN WERNER; EHRHARDT CLAUS; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; ZIMMERMANN JUERG; RUDISSER SIMON; VANGREVELINGHE ERIC; IRIE OSAMU; UMEMURA ICHIRO; SUZUKI MASAKI; MOGI MUNETO; KANAZAWA TAKANORI; YOKOKAWA FUMIAKI; NIHONYANAGI ATSUKO 摘要:The invention relates to 3,5-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-piperidine compound, and/or a method of treatment comprising administering a 3,5-piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.
[参考文献]: A Rolandi, Et Al. Dithiocarbamate Pesticides: Activity Of Propineb In The Micronucleus Test In Mice. Mutat Res. 1984 Mar;135(3):193-7. [参考文献]: Aurore Bonnechère, Et Al. A Rapid And Environmental Friendly Determination Of The Dithiocarbamate Metabolites Ethylenethiourea And Propylenethiourea In Fruit And Vegetables By Ultra High Performance Liquid Chromatography Tandem Mass Spectrometry. J Chromatogr A. 2011 Jul 22;1218(29):4627-31. [参考文献]: Cristina Ripollés, Et Al. Liquid Chromatography Coupled To Tandem Mass Spectrometry For The Residue Determination Of Ethylenethiourea (Etu) And Propylenethiourea (Ptu) In Water. J Chromatogr A. 2012 Jun 22:1243:53-61. [参考文献]: Elias A Kazos, Et Al. Determination Of Dithiocarbamate Fungicide Propineb And Its Main Metabolite Propylenethiourea In Airborne Samples. Chemosphere. 2007 Aug;68(11):2104-10. [参考文献]: G Vettorazzi, Et Al. International Safety Assessment Of Pesticides: Dithiocarbamate Pesticides, Etu, And Ptu--A Review And Update. Teratog Carcinog Mutagen. 1995;15(6):313-37.
合成参考文献
参考文献:10.1107/s1600536811008002 摘要:Devarajegowda HC, Roopashree KR, Mohammed IA, Mahalakshmi, Sankolli R. 4-Hy-droxy-6-(4-meth-oxy-phen-yl)-4-phenyl-1,3-diazinane-2-thione. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o815.