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    3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors
    31.
    发明授权
    3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors 有权
    3-烷基-5-（4-烷基-5-氧代 - 四氢呋喃-2-基）吡咯烷-2-酮衍生物作为肾素抑制剂合成中的中间体

    公开(公告)号：US08198465B2

    公开(公告)日：2012-06-12

    申请号：US12823699

    申请日：2010-06-25

    申请人： Gottfried Sedelmeier ,  Dominique Grimler ,  Murat Acemoglu

    发明人： Gottfried Sedelmeier ,  Dominique Grimler ,  Murat Acemoglu

    IPC分类号： C07D307/02

    CPC分类号： C07D405/04 ,  C07C271/22 ,  C07D207/26 ,  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 II, or a salt thereof, and a compound of formula VI or a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these. Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.

    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II化合物或其盐，式VI化合物或其盐的方法，其中R3和R4以及Act如本说明书中所定义 ，以及制造这些的方法。 化合物（VI）与金属有机化合物（VII）的另外转化产生作为制备阿利吉仑的直接前体的新化合物（VIII）。

    Process for the preparation of tetrazole derivatives from organo aluminium azides
    33.
    发明授权
    Process for the preparation of tetrazole derivatives from organo aluminium azides 失效
    从有机铝叠氮化物制备四唑衍生物的方法

    公开(公告)号：US07943647B2

    公开(公告)日：2011-05-17

    申请号：US10564337

    申请日：2004-07-15

    申请人： Gottfried Sedelmeier

    发明人： Gottfried Sedelmeier

    IPC分类号： A61K31/41

    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 of the formula or a tautomer or salt thereof, wherein R represents an organic residue. Also provided are compounds obtained according to this method, new reactants and new tetrazole derivatives, useful as pharmaceuticals or agricultural compositions, foaming agents, automotive inflators, and the like.

    摘要翻译： 本发明涉及制备下式的取代的四唑或其互变异构体或其盐的方法，其中R表示有机残基。 还提供了根据该方法获得的化合物，可用作药物或农业组合物的新反应物和新的四唑衍生物，发泡剂，汽车充气机等。

    Alternative synthesis of renin inhibitors and intermediates thereof
    34.
    发明授权
    Alternative synthesis of renin inhibitors and intermediates thereof 失效
    肾素抑制剂及其中间体的替代合成

    公开(公告)号：US07910774B2

    公开(公告)日：2011-03-22

    申请号：US11573790

    申请日：2005-08-30

    申请人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    发明人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    IPC分类号： C07C233/65

    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。

    PREPARATION OF TERAZOLE DERIVATIVES
    35.
    发明申请
    PREPARATION OF TERAZOLE DERIVATIVES 审中-公开
    苯并噻唑衍生物的制备

    公开(公告)号：US20100184991A1

    公开(公告)日：2010-07-22

    申请号：US12749025

    申请日：2010-03-29

    申请人： Gottfried Sedelmeier ,  Valentina Aureggi

    发明人： Gottfried Sedelmeier ,  Valentina Aureggi

    IPC分类号： C07F15/00 ,  C07D403/04

    CPC分类号： C07D403/04

    摘要： The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula wherein R1, R2 and R3, independently of one another, represent hydrogen, halogen or an organic radical, in racemic form or as an enantiomer, a tautomer, an analog thereof or a salt thereof.

    摘要翻译： 本发明涉及一种制备下式的（S） - 吡咯烷-1H-四唑衍生物的方法，其中R 1，R 2和R 3彼此独立地代表外消旋形式的氢，卤素或有机基团，或作为对映异构体 ，互变异构体，其类似物或其盐。

    Preparation of Terazole Derivatives
    37.
    发明申请
    Preparation of Terazole Derivatives 审中-公开
    特拉唑衍生物的制备

    公开(公告)号：US20080200687A1

    公开(公告)日：2008-08-21

    申请号：US11995862

    申请日：2006-07-17

    申请人： Gottfried Sedelmeier ,  Valentina Aureggi

    发明人： Gottfried Sedelmeier ,  Valentina Aureggi

    IPC分类号： C07D257/04

    CPC分类号： C07D403/04

    摘要： The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula wherein R1, R2 and R3, independently of one another, represent hydrogen, halogen or an organic radical, in racemic form or as an enantiomer, a tautomer, an analog thereof or a salt thereof.

    摘要翻译： 本发明涉及一种制备下式的（S） - 吡咯烷-1H-四唑衍生物的方法，其中R 1，R 2，R 3， SUB>彼此独立地表示氢，卤素或有机基团，外消旋形式或作为对映体，互变异构体，其类似物或其盐。

    Process for the preparation of n-substituted 2-cyanopyrrolidines
    38.
    发明申请
    Process for the preparation of n-substituted 2-cyanopyrrolidines 失效
    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

    Enantioselective process for the preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide and new crystal forms thereof
    39.
    发明申请
    Enantioselective process for the preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide and new crystal forms thereof 审中-公开
    用于制备10,11-二氢-10-羟基-5h-二苯并[b，f]吖庚因-5-甲酰胺及其新的晶体形式的两种对映体的对映选择性方法

    公开(公告)号：US20060142566A1

    公开(公告)日：2006-06-29

    申请号：US10530617

    申请日：2003-10-06

    申请人： Christian Mathes ,  Gottfried Sedelmeier ,  Fritz Blatter ,  Sabine Pfeffer ,  Dominique Grimler

    发明人： Christian Mathes ,  Gottfried Sedelmeier ,  Fritz Blatter ,  Sabine Pfeffer ,  Dominique Grimler

    IPC分类号： C07D223/18

    CPC分类号： C07D223/24 ,  C07F15/0053

    摘要： The invention relates to a novel process for the manufacture of substituted enantiopure 10hydroxy-dihydrodibenz[b,f]azepines (Ia), (Ib) wherein each of R1 and R2, independently, are hydrogen, halogen, amino or nitro; and each of R3 and R4, independently, are hydrogen or C1-C6alkyl; by transfer hydrogenation of 10-oxo-dihydrodibenz[b,f]azepines; and to novel catalysts of formula (III′a) and (III′b) wherein M is Ru, Rh, Ir, Fe, Co or Ni; L1 is hydrogen; L2 represents an aryl or aryl-aliphatic residue; and the further radicals have the meanings as defined herein; and to new crystal forms of both enantiomers of 10,11-dihydro-10 hydroxy-5Hdibenz[b,f]azepine-5-carboxamide, obtainable by the new processes, their usage in the production of pharmaceutical preparations, new pharmaceutical preparations comprising these new crystal forms and/or the use of these new crystal forms in the treatment of disorders such as epilepsy, or in the production of pharmaceutical formulations which are suitable for this treatment.

    摘要翻译： 本发明涉及用于制备取代的对映体纯的10-羟基 - 二氢二苯并[b，f]吖庚因（Ia），（Ib）的新方法，其中R 1和R 2中的每一个 独立地是氢，卤素，氨基或硝基; R 3和R 4中的每一个独立地是氢或C 1 -C 6烷基; 通过10-氧代 - 二氢二苯并[b，f]吖庚因的转移氢化; 和式（III'a）和（III'b）的新型催化剂，其中M是Ru，Rh，Ir，Fe，Co或Ni; L 1是氢; L 2代表芳基或芳基脂族残基; 并且其它基团具有如本文所定义的含义; 以及可通过新方法获得的10,11-二氢-10羟基-5H-二苯并[b，f]吖庚因-5-甲酰胺的两种对映异构体的新结晶形式，它们在制备药物制剂中的用途，包含这些的新药物制剂 新的晶体形式和/或这些新的晶体形式用于治疗疾病如癫痫或使用适于该治疗的药物制剂。

    Substituted hydroquinone derivatives
    40.
    发明授权
    Substituted hydroquinone derivatives 失效
    取代氢醌衍生物

    公开(公告)号：US5693807A

    公开(公告)日：1997-12-02

    申请号：US465628

    申请日：1995-06-05

    申请人： Gottfried Sedelmeier ,  Gerhard Fischer

    发明人： Gottfried Sedelmeier ,  Gerhard Fischer

    IPC分类号： C07D211/62 ,  C07D405/04 ,  C07F9/59 ,  C07D211/32

    CPC分类号： C07D405/04 ,  C07D211/62 ,  C07F9/592

    摘要： The invention relates to substituted hydroquinone derivatives of the general formula I ##STR1## wherein R.sub.4 is lower alkyl and either R.sub.1 is hydroxy, halogen, a group of the formula --P(=O)(R.sub.5)R.sub.6 (Ia), a group of the formula --P.sup.+ (R.sub.7)(R.sub.8)R.sub.9 X.sup.- (Ib) or a group of the formula --Si(R.sub.7)(R.sub.8)R.sub.9 (Ic), M is methylene, R.sub.2 is hydrogen or a group of the formula ##STR2## and R.sub.3 is hydrogen or halogen, or .sub.1 is hydroxy or lower alkoxy, M is carbonyl, R.sub.2 is hydrogen and R.sub.3 is halogen, each of R.sub.5 and R.sub.6, independently of the other, is lower alkyl, lower alkoxy Or N,N-di-lower alkylamino, or is benzyl, benzyloxy, phenyl or phenoxy, each of which is unsubstituted or mono- or di-substituted at the phenyl ring, to a process for the preparation of those compounds and to the use of those compounds, and to a process in which those compounds are used.

    摘要翻译： 本发明涉及通式Ⅰ（I）的取代氢醌衍生物，其中R 4是低级烷基，R 1是羟基，卤素，式-P（= O）（R 5）R 6（Ia）的基团， 式 - +（R7）（R8）R9X-（Ib）或式-Si（R7）（R8）R9（Ic）的基团，M是亚甲基，R2是氢或式 （Id），R 3为氢或卤素，或1为羟基或低级烷氧基，M为羰基，R 2为氢，R 3为卤素，R 5和R 6各自独立地为低级烷基，低级烷氧基 或N，N-二低级烷基氨基，或苄基，苄氧基，苯基或苯氧基，其中每个在苯环上未被取代或单取代或二取代，制备这些化合物的方法和使用 的那些化合物，以及使用这些化合物的方法。