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51. 发明申请

US20100267965A1 3-Alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one Derivatives as Intermediates in the Synthesis of Renin Inhibitors 有权
标题翻译： 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：US20100267965A1
公开(公告)日：2010-10-21
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： C07D405/04 , C07D307/20 , C07C43/205 , C07C271/18
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）。

52. 发明授权

US07767831B2 Process for preparing renin inhibitors 失效
标题翻译：制备肾素抑制剂的方法
公开(公告)号：US07767831B2
公开(公告)日：2010-08-03
申请号：US11916875
申请日：2006-06-06
申请人： Stuart J Mickel , Gottfried Sedelmeier , Hans Hirt , Frank Schäfer , Michael Foulkes , Walter Prikoszovich
发明人： Stuart J Mickel , Gottfried Sedelmeier , Hans Hirt , Frank Schäfer , Michael Foulkes , Walter Prikoszovich
IPC分类号： C07D207/08
CPC分类号： C07D405/04 , C07C237/22 , C07D207/08 , C07D307/32 , C07D307/33 , Y02P20/55
摘要： The present invention provides 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 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。

53. 发明申请

US20080312462A1 Process for the manufacture of HMG-CoA reductase inhibitory mevalonic acid derivatives 审中-公开
标题翻译：制备HMG-CoA还原酶抑制性甲羟戊酸衍生物的方法
公开(公告)号：US20080312462A1
公开(公告)日：2008-12-18
申请号：US12220259
申请日：2008-07-23
申请人： Gottfried Sedelmeier , Christian Mathes
发明人： Gottfried Sedelmeier , Christian Mathes
IPC分类号： C07F15/00
CPC分类号： C07F9/5352 , C07C51/09 , C07C59/42 , C07D309/30 , C07F15/004 , C07F15/0053 , C07F15/008 , C07F15/025 , C07F15/045 , C07F15/065
摘要： The invention relates to a process for the manufacture of a compound of formula: (Formula I); or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element (a) represents —CH2—CH2 CH— or —CH═CH— and R represents a cyclic radical.
摘要翻译：本发明涉及制备式（I）化合物的方法：或其盐，特别是与其碱或其内酯的药学上可接受的盐，其中元素（a）表示-CH 2 -CH 2 CH-或-CH-CH-，R表示环状基团。

54. 发明授权

US07456283B2 N-phenyl-2-pyrimidine-amine derivatives 有权
标题翻译： N-苯基-2-嘧啶 - 胺衍生物
公开(公告)号：US07456283B2
公开(公告)日：2008-11-25
申请号：US10503538
申请日：2003-02-06
申请人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Michael Bürger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
发明人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Michael Bürger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07D401/04 , C07D295/155 , C07D401/14
摘要： The present invention relates to novel amides and a process for preparing these amides.
摘要翻译：本发明涉及新颖的酰胺和这些酰胺的制备方法。

55. 发明申请

US20070293673A1 N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES 有权
公开(公告)号：US20070293673A1
公开(公告)日：2007-12-20
申请号：US11845924
申请日：2007-08-28
申请人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Burger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
发明人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Burger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
IPC分类号： C07D241/04 , C07D401/02
CPC分类号： C07D401/04 , C07D295/155 , C07D401/14
摘要： The present invention relates to novel amides and a process for preparing these amides.

56. 发明申请

US20070293672A1 N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES 有权
公开(公告)号：US20070293672A1
公开(公告)日：2007-12-20
申请号：US11845914
申请日：2007-08-28
申请人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Burger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
发明人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Burger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
IPC分类号： C07D241/04 , C07D401/02
CPC分类号： C07D401/04 , C07D295/155 , C07D401/14
摘要： The present invention relates to novel amides and a process for preparing these amides.

57. 发明申请

US20070293504A1 N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES 有权
公开(公告)号：US20070293504A1
公开(公告)日：2007-12-20
申请号：US11845934
申请日：2007-08-28
申请人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Burger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
发明人： Olivier Loiseleur , Daniel Kaufmann , Stephan Abel , Hans Burger , Mark Meisenbach , Beat Schmitz , Gottfried Sedelmeier
IPC分类号： A61K31/4965 , A61K31/497 , A61P35/00 , C07D241/04 , C07D401/02
CPC分类号： C07D401/04 , C07D295/155 , C07D401/14
摘要： The present invention relates to novel amides and a process for preparing these amides.

58. 发明授权

US5312914A Process for the manufacture of 4-acetoxy-3-hydroxyethyl-azetidinone 失效
标题翻译：制备4-乙酰氧基-3-羟乙基 - 氮杂环丁酮的方法
公开(公告)号：US5312914A
公开(公告)日：1994-05-17
申请号：US937457
申请日：1992-08-27
申请人： Gottfried Sedelmeier , Jacques Bersier
发明人： Gottfried Sedelmeier , Jacques Bersier
IPC分类号： C07D205/08 , C07D307/68 , C07B53/00 , C07D307/66
CPC分类号： C07D205/08 , C07D307/68
摘要： The invention relates to a novel process for the manufacture of 4-acetoxy-3-hydroxyethyl-azetidinone of the formula ##STR1## especially 4(R)-acetoxy-3(R)-(1'(R)-hydroxyethyl)-2-azetidinone, from enantiomerically pure compounds of the formula ##STR2## in which R.sup.1 represents lower alkyl and Z.sup.1 represents amino, arylmethylamino, acylamino or azido, by reduction of the C.dbd.C double bond and optionally of the arylmethylamino or azido group with hydrogen, epimerization, opening of the lactone ring, cyclisation to the .beta.-lactam, optionally after hydrolysis of the acylamino group, and oxidative decarboxylation of the original lactone carboxy group in the presence of an acetate-yielding agent. Compounds of the formula I can be used as starting materials for the manufacture of .beta.-lactam antibiotics. The invention also relates to novel intermediates and starting materials.
摘要翻译：本发明涉及制备式（I）的4-乙酰氧基-3-羟乙基 - 氮杂环丁酮的新方法，特别是4（R） - 乙酰氧基-3（R） - （1'（R） - 羟乙基）-2-氮杂环丁酮，由对映异构体纯的式Y1和Z1表示氨基，芳基甲基氨基，酰氨基或叠氮基，通过还原C = C双键和任选的芳基甲基氨基或叠氮基与氢，差向异构化，开环内酯环，任选地在酰基氨基水解后环化成β-内酰胺，以及在产生乙酸酯的试剂存在下原始内酯羧基的氧化脱羧作用。式I化合物可用作制备β-内酰胺抗生素的起始原料。本发明还涉及新的中间体和起始材料。

59. 发明授权

US5066801A Preparation of sulfonic acid esters 失效
标题翻译：磺酸酯的制备
公开(公告)号：US5066801A
公开(公告)日：1991-11-19
申请号：US544076
申请日：1990-06-26
申请人： Hans-Ulrich Blaser , Hans-Peter Jalett , Gottfried Sedelmeier
发明人： Hans-Ulrich Blaser , Hans-Peter Jalett , Gottfried Sedelmeier
IPC分类号： C07D223/16 , A61K31/55 , A61P9/12 , A61P21/00 , A61P25/18 , A61P43/00 , B01J31/00 , B01J31/02 , B01J31/28 , C07B43/04 , C07B53/00 , C07B55/00 , C07B61/00 , C07C67/00 , C07C67/31 , C07C69/675 , C07C227/00 , C07C227/08 , C07C227/16 , C07C227/32 , C07C229/02 , C07C229/08 , C07C271/42 , C07C301/00 , C07C303/28 , C07C309/63 , C07C309/72 , C07C309/73 , C07K5/078
CPC分类号： C07C227/32 , C07C309/00 , C07K5/06139
摘要： The invention relates to novel sulfonic acid esters of formula I ##STR1## wherein R.sup.1 is C.sub.5 -C.sub.6 cycloalkyl which is unsubstituted or substituted by C.sub.1 -C.sub.7 alkyl, unsubstituted or substituted phenyl, R.sup.2 is C.sub.1 -C.sub.7 alkyl, R.sup.3 is phenyl which is substituted by halogen or nitro, and the asterisk denotes a carbon atom that is either present in the preponderant number of molecules in the S configuration or in the preponderant number of molecules in the R configuration.These compounds can be prepared by enantio-selective reduction of 4-R.sup.1 -substituted .alpha.-oxobutyric acid compounds and subsequent conversion of the resultant .alpha.-hydroxy group into the --OSO.sub.2 --R.sup.3 group. The compounds of formula I are suitable intermediates for the preparation of ACE inhibitors or precursors thereof.

60. 发明授权

US4436903A Process for the production of 7 .beta.-substituted-3-unsubstituted-3-cephem-4-carboxylic acid compounds 失效
标题翻译：用于制备7β-取代-3-未取代的3-头孢烯-4-羧酸化合物的方法
公开(公告)号：US4436903A
公开(公告)日：1984-03-13
申请号：US329916
申请日：1981-12-11
申请人： Gottfried Sedelmeier , Riccardo Scartazzini
发明人： Gottfried Sedelmeier , Riccardo Scartazzini
IPC分类号： A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/18 , C07D501/20 , C07D501/59
CPC分类号： C07D501/04 , C07D501/59 , Y02P20/55
摘要： The invention relates to a novel advantageous process for the production of compounds of the formula ##STR1## wherein n is 1, R.sub.1.sup.a is hydrogen or an amino protective group R.sub.1.sup.A, R.sub.1.sup.b is hydrogen or an acyl group Ac, or R.sub.1.sup.a and R.sub.1.sup.b together are a bivalent amino protective group, R.sub.2 is hydroxyl or a radical which, together with the carbonyl grouping --C(.dbd.O)--, forms a protected carboxyl group, and the group of the formula --N(R.sub.3.sup.a) (R.sub.3.sup.b) is a secondary or tertiary amino group, or a salt thereof with salt-forming groups. The process comprises reaction of the corresponding 3-amino compounds with borohydrides in the presence of acids.
摘要翻译：本发明涉及一种制备式（I）化合物的新型有利方法，其中n为1，R 1a为氢或氨基保护基R1A，R1b为氢或酰基Ac或R1a和R1b 一起是二价氨基保护基，R2是羟基或与羰基-C（= O） - 一起形成受保护的羧基的基团，式-N（R3a）（R3b）的基团是仲或叔氨基，或其盐与成盐基团。该方法包括在酸存在下相应的3-氨基化合物与硼氢化物的反应。

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