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1. 发明申请

US20060199854A1 Process for the preparation of n-substituted 2-cyanopyrrolidines 失效
标题翻译： N-取代的2-氰基吡咯烷的制备方法
公开(公告)号：US20060199854A1
公开(公告)日：2006-09-07
申请号：US10552835
申请日：2004-04-15
申请人： Frank Schafer , Gottfried Sedelmeier
发明人： Frank Schafer , Gottfried Sedelmeier
IPC分类号： A61K31/401 , C07D207/277
CPC分类号： C07D207/16
摘要： The present invention relates to a process for the preparation of a N—(N′-substituted glycyl)-2-cyanopyrrolidine comprising at least (a) reacting, in the presence of dimethylformamide, a compound of formula (V) wherein, independently of each other, X1 and X3 are halogen; X2 is halogen, OH, O—C(═O)—CH2X3, —O—SO2—(C1-8)alkyl or —O—SO2-(aryl), with L-prolinamide, followed by (b) reacting the resultant compound without isolation with a dehydration agent, optionally followed by (c) reacting, in the presence of a base, the resultant compound without isolation with an appropriate amine and (d) recovering the resultant cornpound in free form or in acid addition salt form.
摘要翻译：本发明涉及一种制备N-（N'取代的甘氨酰基）-2-氰基吡咯烷的方法，该方法至少包括（a）在二甲基甲酰胺存在下使式（Ⅴ）化合物与彼此之间，X 1和X 3是卤素; X 2是卤素，OH，OC（-O）-CH 2 X 3，-O-SO 2

2. 发明申请

US20080207921A1 Organic Compounds 失效
标题翻译：有机化合物
公开(公告)号：US20080207921A1
公开(公告)日：2008-08-28
申请号：US11916875
申请日：2006-06-06
申请人： Stuart John Mickel , Gottfried Sedelmeier , Hans Hirt , Frank Schafer , Michael Foulkes , Walter Prikoszovich
发明人： Stuart John Mickel , Gottfried Sedelmeier , Hans Hirt , Frank Schafer , Michael Foulkes , Walter Prikoszovich
IPC分类号： C07D207/06
CPC分类号： C07D405/04 , C07C237/22 , C07D207/08 , C07D307/32 , C07D307/33 , Y02P20/55
摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof, said manufacture comprising (preferably consisting in) reacting a compound of the formula I,
摘要翻译：本发明涉及可用于合成药物活性化合物，特别是肾素抑制剂如阿利吉仑的新方法，新工艺步骤和新型中间体。特别地，本发明涉及制备式III化合物的方法，其中R 1，R 2，R 2，R 3， SUB>和PG如说明书中所定义，或其盐，所述制备包含（优选地）使式I化合物，

3. 发明授权

US08716495B2 Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid 有权
标题翻译：制备5-联苯-4-氨基-2-甲基戊酸的方法
公开(公告)号：US08716495B2
公开(公告)日：2014-05-06
申请号：US13333437
申请日：2011-12-21
申请人： David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
发明人： David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
IPC分类号： C07D207/26 , C07C219/18 , C07D207/12
CPC分类号： C07C231/02 , C07C219/18 , C07C227/16 , C07C227/20 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/12 , C07C231/14 , C07C233/47 , C07C269/04 , C07C271/22 , C07C2601/16 , C07D207/12 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/404 , C07D207/44 , C07D403/06 , C07F7/10 , Y02P20/55
摘要： The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
摘要翻译：本发明涉及式（1）的吡咯烷-2-酮或其盐，其中R1是氢或氮保护基，其制备方法及其在制备NEP-抑制剂中的用途，特别是在制备N-（3-羧基-1-氧代丙基） - （4S） - （对苯基苯基甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。

4. 发明授权

US08569528B2 Process for the preparation of tetrazole derivatives from organo boron and organo aluminium azides 失效
标题翻译：从有机硼和有机铝叠氮化物制备四唑衍生物的方法
公开(公告)号：US08569528B2
公开(公告)日：2013-10-29
申请号：US13603770
申请日：2012-09-05
申请人： Gottfried Sedelmeier
发明人： Gottfried Sedelmeier
IPC分类号： C07F5/02 , C07F5/06
CPC分类号： C07D257/04 , C07D403/10 , C07F5/02 , C07F5/066
摘要： The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
摘要翻译：本发明涉及一种制备取代的四唑的方法，根据该方法获得的化合物，新的反应物和新的四唑衍生物。

5. 发明申请

US20120330026A1 PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES 失效
标题翻译：从有机硼和有机铝酸钠制备四唑衍生物的方法
公开(公告)号：US20120330026A1
公开(公告)日：2012-12-27
申请号：US13603770
申请日：2012-09-05
申请人： Gottfried Sedelmeier
发明人： Gottfried Sedelmeier
IPC分类号： C07D257/04 , C07D403/10
CPC分类号： C07D257/04 , C07D403/10 , C07F5/02 , C07F5/066
摘要： The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
摘要翻译：本发明涉及一种制备取代的四唑的方法，根据该方法获得的化合物，新的反应物和新的四唑衍生物。

6. 发明授权

US08338620B2 Methods for the production of C-8 lactam lactone compounds 失效
标题翻译：生产C-8内酰胺内酯化合物的方法
公开(公告)号：US08338620B2
公开(公告)日：2012-12-25
申请号：US12594414
申请日：2008-04-01
申请人： Gottfried Sedelmeier
发明人： Gottfried Sedelmeier
IPC分类号： C07D207/26 , C07D405/04 , C07C205/44 , C07C205/16 , C07C205/29
CPC分类号： C07C271/16 , C07C45/00 , C07C45/30 , C07C45/44 , C07C47/277 , C07C201/12 , C07C205/15 , C07C205/30 , C07C205/31 , C07C205/40 , C07C205/44 , C07C205/51 , C07C205/53 , C07C231/12 , C07C231/18 , C07D207/16 , C07D207/26 , C07D307/33 , C07D405/04 , C07D407/04 , C07F7/1804 , C07C237/20 , C07C205/16
摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, the invention relates to a process for the manufacture of a compound of the formula I, or a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
摘要翻译：本发明涉及可用于合成药物活性化合物，特别是阿利吉仑的肾素抑制剂的新方法，新方法步骤和新型中间体，本发明涉及制备式I化合物或其盐，其中R1和Act如本说明书中所定义，以及制备该化合物的方法以及该方法中的中间体。

7. 发明授权

US08143416B2 Alternative synthesis of renin inhibitors and intermediates thereof 失效
标题翻译：肾素抑制剂及其中间体的替代合成
公开(公告)号：US08143416B2
公开(公告)日：2012-03-27
申请号：US13022243
申请日：2011-02-07
申请人： Gottfried Sedelmeier , Stuart John Mickel , Heinrich Rueeger
发明人： Gottfried Sedelmeier , Stuart John Mickel , Heinrich Rueeger
IPC分类号： C07D263/52
CPC分类号： C07D207/26 , C07C271/16 , C07C271/22 , C07D211/76 , C07D307/33
摘要： The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
摘要翻译：本发明涉及制备下式化合物的合成路线：其中R 1是卤素，C 1-6卤代烷基，C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素，C1-4烷基或C1-4烷氧基; R3和R4独立地是支链的C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷酰氧基-C 1-6烷基，C 1-6氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6烷基，C 1 （O）C 1-6烷基，C 1-6烷基-O-（O）C 1-6烷基，H 2 N-C（O）-C 1-6烷基，C 1-6烷基-NH- C （O）-C 1-6烷基或（C 1-6烷基）2 N -C（O）-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

8. 发明授权

US08115016B2 Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid 有权
标题翻译：制备5-联苯-4-氨基-2-甲基戊酸的方法
公开(公告)号：US08115016B2
公开(公告)日：2012-02-14
申请号：US12522767
申请日：2008-01-10
申请人： David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
发明人： David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
IPC分类号： C07D207/26 , C07D207/27 , C07D207/263 , C07D207/267 , C07F7/10
CPC分类号： C07C231/02 , C07C219/18 , C07C227/16 , C07C227/20 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/12 , C07C231/14 , C07C233/47 , C07C269/04 , C07C271/22 , C07C2601/16 , C07D207/12 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/404 , C07D207/44 , C07D403/06 , C07F7/10 , Y02P20/55
摘要： The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
摘要翻译：本发明涉及式（1）的吡咯烷-2-酮或其盐，其中R1是氢或氮保护基，其制备方法及其在制备NEP-抑制剂中的用途，特别是在制备N-（3-羧基-1-氧代丙基） - （4S） - （对苯基苯甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。

9. 发明申请

US20100274027A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：US20100274027A1
公开(公告)日：2010-10-28
申请号：US12823518
申请日：2010-06-25
申请人： Stuart John Mickel , Gottfried Sedelmeier , Hans Hirt , Frank Schäfer , Michael Foulkes , Walter Prikoszovich
发明人： Stuart John Mickel , Gottfried Sedelmeier , Hans Hirt , Frank Schäfer , Michael Foulkes , Walter Prikoszovich
IPC分类号： C07D207/00 , C07C215/04 , C07D405/04 , C07D207/08
CPC分类号： C07D405/04 , C07C237/22 , C07D207/08 , C07D307/32 , C07D307/33 , Y02P20/55
摘要： The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Allskiren. Inter alia, the invention provides a process for the manufacture of a compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof. The manufacture comprises (preferably consists of) reacting a compound of the formula I, with a reagent able to transform hydroxy into X where X is for example a leaving group.
摘要翻译：本发明提供了一种新颖的方法，新颖的方法步骤和可用于合成药物活性化合物，特别是肾素抑制剂例如Allskiren的新型中间体。特别地，本发明提供了制备式III化合物的方法，其中R，R 1，R 2，R 3和PG如说明书中所定义，或其盐。该制造方法包括（优选由式I化合物）与能够将羟基转化为X的试剂反应，其中X为例如离去基团。

10. 发明申请

US20080249318A1 Process for phenylacetic acid derivatives 审中-公开
标题翻译：苯乙酸衍生物工艺
公开(公告)号：US20080249318A1
公开(公告)日：2008-10-09
申请号：US11893481
申请日：2007-08-16
申请人： Murat Acemoglu , Thomas Allmendinger , John Vincent Calienni , Jacques Cercus , Olivier Loiseleur , Gottfried Sedelmeier , David Xu
发明人： Murat Acemoglu , Thomas Allmendinger , John Vincent Calienni , Jacques Cercus , Olivier Loiseleur , Gottfried Sedelmeier , David Xu
IPC分类号： C07D209/34 , C07C227/22 , C07C211/55 , C07C233/01
CPC分类号： C07C211/52 , C07C211/56 , C07C227/22 , C07C229/42 , C07C233/15 , C07C235/16 , C07C235/24 , C07C2601/16 , C07D209/34
摘要： A process for the production of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable prodrug ester thereof, comprising cleaving a lactam of formula II wherein the symbols are as defined, with a base; and precursors therefor and processes for the preparation of the precursors. The compounds of Formula I are pharmaceutically active compounds which are selective inhibitors of Cyclooxygenase II.
摘要翻译：制备式I化合物或其药学上可接受的盐或其药学上可接受的前药酯的方法，其包括用碱定义其中符号如本文所定义的式II的内酰胺; 及其前体和制备前体的方法。式I的化合物是作为环加氧酶II的选择性抑制剂的药物活性化合物。

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