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1. 发明申请

WO2009053452A1 4,4-DISUBSTITUTED PIPERIDINES 审中-公开
标题翻译： 4,4-取代的哌啶
公开(公告)号：WO2009053452A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064417
申请日：2008-10-24
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JELAKOVIC, Stjepan , JOTTERAND, Nathalie , STUTZ, Stefan , LYOTHIER, Isabelle
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JELAKOVIC, Stjepan , JOTTERAND, Nathalie , STUTZ, Stefan , LYOTHIER, Isabelle
IPC分类号： C07D413/14 , C07D413/12 , A61K31/538 , A61P9/12
CPC分类号： C07D413/12 , C07D413/14
摘要： The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R 2 , has the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式（I）的4,4-二取代哌啶及其盐，优选其药学上可接受的盐，其中R2具有说明书中所述的含义，其制备方法和这些化合物的用途作为药物，特别是作为肾素抑制剂。

2. 发明申请

WO2008031811A1 NITRATE ESTERS OF AMINOALCOHOLS 审中-公开
标题翻译：硝酸酯的硝酸酯
公开(公告)号：WO2008031811A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059504
申请日：2007-09-11
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , MARTI, Christiane , JOTTERAND, Nathalie
发明人： HEROLD, Peter , MAH, Robert , MARTI, Christiane , JOTTERAND, Nathalie
IPC分类号： C07C233/13 , C07D209/08 , C07D213/64 , C07D231/56 , C07D265/36 , C07D307/80 , A61K31/404 , A61K31/343 , A61K31/44 , A61K31/416 , A61P9/10 , A61P9/12
CPC分类号： C07C237/20 , C07C2601/14 , C07D209/12 , C07D211/16 , C07D211/30 , C07D213/56 , C07D213/64 , C07D215/54 , C07D231/56 , C07D265/36 , C07D307/80 , C07D401/12 , C07D405/12 , C07D413/12
摘要： The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R 1 , R 2 , R 3 , V, X, Y and Z 0 have the meanings explained in more detail in the description, to a process for their preparation and to the use of these compounds as therapeutics in cardiovascular diseases, in particular in high blood pressure and vascular and organ damage accompanying high blood pressure.
摘要翻译：本申请涉及通式（I）的取代氨基醇的新型硝酸酯衍生物，其中R 1，R 2，R 3， V，X，Y和Z 0具有在描述中更详细解释的含义，其制备方法和这些化合物作为心血管疾病，特别是高血液中的治疗剂压力和血管和器官损伤伴随高血压。

3. 发明申请

WO2007113235A1 PROCESS FOR PREPARING 6,7-DIHYDRO-5H-IMIDAZO[1,5-A]PYRIDIN-8-ONE 审中-公开
标题翻译：制备6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮的方法
公开(公告)号：WO2007113235A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053078
申请日：2007-03-30
申请人： Speedel Experimenta AG , MARTIN, Pierre , BOUDIER, Andreas , QUIRMBACH, Michael , MAH, Robert , JOTTERAND, Nathalie
发明人： MARTIN, Pierre , BOUDIER, Andreas , QUIRMBACH, Michael , MAH, Robert , JOTTERAND, Nathalie
IPC分类号： C07D213/65 , C07D233/22 , C07D471/04 , C07F7/08 , C07F7/18
CPC分类号： C07D233/22 , C07D213/65 , C07D471/04 , C07F7/0814
摘要： 6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5- a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced deprotection of the imidazole and deprotection of the alcohol functionality; 3) a process which proceeds from 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine [38666-30-7], which is oxidized.
摘要翻译： 6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮（I）可以通过以下方式获得：1）从适当保护的C-（3-羟基吡啶-2 - 基）甲胺，其胺转化为甲酰胺，然后将其环化为咪唑并[1,5-a]吡啶，并氢化成6,7-二氢-5H-咪唑并[1,5-a] 一种适当保护的C-（3-羟基吡啶-2-基）甲胺可以从市售的3-羟基-2-氰基吡啶[932-35-4]或以商业上可获得的3个步骤 2-羟甲基吡啶-3-醇[14173-30-9]; 2）制备4-羟基-1-（1H-咪唑-4-基）丁-1-酮的方法，由6,7-二氢-5H-咪唑并[1,5-a]吡啶 -8-（咪唑-1-基）磺酰胺的N，N-二甲基-2-（三烷基硅烷基）咪唑-1-磺酰胺进行的步骤（WO 2002/040484中所述），然后与适当保护的4-羟基丁醛反应，随后与仲醇的氧化，酸诱导的咪唑脱保护和醇官能团的脱保护; 3）从被氧化的5,6,7,8-四氢咪唑并[1,5-a]吡啶[38666-30-7]进行的方法。

4. 发明申请

WO2006061426A1 ω-PHENYLOCTANAMIDES 审中-公开
标题翻译：？-PHENYLOCTANAMIDES
公开(公告)号：WO2006061426A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056622
申请日：2005-12-09
申请人： Speedel Experimenta AG , HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , MARTI, Christiane
发明人： HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , MARTI, Christiane
IPC分类号： C07C237/20 , A61K31/165
CPC分类号： C07C255/59 , C07C237/20 , C07D317/58 , C07D319/18
摘要： Compounds of the general formula (I) in which the substituents R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each as defined in Claim 1 have renin-inhibiting properties and can be used as medicaments.
摘要翻译：通式（I）的化合物，其中取代基R 1，R 1，R 2，R 3，R 4， R 5，R 6和R 6各自如权利要求1中所定义，具有肾素抑制性质，可用作药物。

5. 发明申请

WO2005118541A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2005118541A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005/052418
申请日：2005-05-27
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , SCHUMACHER, Christoph , BEHNKE, Dirk , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , SCHUMACHER, Christoph , BEHNKE, Dirk , QUIRMBACH, Michael
IPC分类号： C07D213/00
CPC分类号： C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译：本申请涉及通式（I）的新型杂环化合物，其中R 1，R 2，R 2，X，Y，Z和n具有本说明书中定义的含义，其制备方法和使用这些化合物作为药物，特别是作为醛固酮合酶抑制剂。

6. 发明申请

WO2005070870A3 AMINO ALCOHOL DERIVATIVES AND THEIR USE AS RENIN INHIBITORS 审中-公开
公开(公告)号：WO2005070870A3
公开(公告)日：2005-08-04
申请号：PCT/EP2005/050273
申请日：2005-01-21
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , STUTZ, Stefan , STOJANOVIC, Aleksandar , TSCHINKE, Vincenzo , MARTI, Christiane , QUIRMBACH, Michael
发明人： HEROLD, Peter , STUTZ, Stefan , STOJANOVIC, Aleksandar , TSCHINKE, Vincenzo , MARTI, Christiane , QUIRMBACH, Michael
IPC分类号： C07C213/08
摘要： The application relates to novel amino alcohols of the general formula (I) where R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 each have the definitions illustrated in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.

7. 发明申请

WO2007085651A1 PROCESS FOR THE PREPARATION OF ORGANIC COMPOUNDS 审中-公开
标题翻译：制备有机化合物的方法
公开(公告)号：WO2007085651A1
公开(公告)日：2007-08-02
申请号：PCT/EP2007/050816
申请日：2007-01-29
申请人： Speedel Experimenta AG , HEROLD, Peter , STUTZ, Stefan , MAH, Robert , STOJANOVIC, Aleksandar , LYOTHIER, Isabelle , BEHNKE, Dirk , SPINDLER, Felix , BAPPERT, Erhard
发明人： HEROLD, Peter , STUTZ, Stefan , MAH, Robert , STOJANOVIC, Aleksandar , LYOTHIER, Isabelle , BEHNKE, Dirk , SPINDLER, Felix , BAPPERT, Erhard
IPC分类号： C07D231/56 , C07D471/04
CPC分类号： C07D471/04 , C07D231/56
摘要： Compounds of the formula I, in which R' 1 and R' 2 represent, independently of one another, H, C 1 -C 8 -alkyl, halogen, polyhalo-C 1 -C 8 -alkoxy, polyhalo-C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C 1 -C 8 -alkyl or C 1 -C 8 -alkoxy-C 1 -C 8 -alkoxy, R' 1 and R' 2 not simultaneously representing H, and R' 3 represents C 1 -C 8 -alkyl and in which the carbon atom to which the R' 3 radical is bonded exhibits either the (R) or (S) configuration, the (R) configuration being preferred, can be obtained in high yields by a stereoselective addition of R' 3 -substituted propionates to RV and R' 2 -substituted unsaturated bicyclic heterocyclyl aldehydes of the formula R-CHO to give corresponding 3-R-3-hydroxy-2-R' 3 -propionates. Conversion of the OH group to a leaving group, subsequently a regioselective elimination to give 3-R-2-R' 3 -propenoates, followed by 1 ) the saponification to give the corresponding 3-R-2-R' 3 -propenoic acids, the enantioselective hydrogenation thereof to give corresponding chiral 3-R-2-R' 3 -propanoic acids and the reduction thereof, or 2) the saponification to give the corresponding 3-R-2-R' 3 -propenoic acids, the reduction thereof to give corresponding 3-R-2-R' 3 -allyl alcohols and the enantioselective hydrogenation thereof, or 3) the reduction to give corresponding 3-R-2-R' 3 -allyl alcohols and the enantioselective hydrogenation thereof, R being
摘要翻译：其中R 1'和R“2'的式I化合物彼此独立地表示H，C 1 -C 3烷基，烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 1 - C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基-C R 1'和R“2不同时表示H，R' N 3表示C 1 -C 8 - 烷基，并且其中R'3个基团的碳原子是（R）或（S）构型可以以高收率通过立体选择性添加R'3 - 取代丙酸酯至RV和R' 式R-CHO的2-取代的不饱和双环杂环基醛，得到相应的3-R-3-羟基-2R'3 - 丙酸酯。将OH基转化为离去基团，随后进行区域选择性消除，得到3-R-2-R“3 - 丙烯酸酯，然后1）皂化，得到相应的3-R-2 -R'3'-丙烯酸，其对映选择性氢化反应，得到相应的手性3-R-2-R'3'-丙酸及其还原剂，或2）皂化，得到相应的3-R-2-R“3 - 丙烯酸，将其还原，得到相应的3-R-2-R”3 - 烯丙基醇和其对映体选择性氢化，或3）还原反应得到相应的3-R-2-R“3 - 烯丙醇及其对映选择性氢化，R为

8. 发明申请

WO2006128852A3 HETEROCYCLIC SPIRO-COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
标题翻译：作为醛固酮合成酶抑制剂的杂环螺旋化合物
公开(公告)号：WO2006128852A3
公开(公告)日：2007-02-22
申请号：PCT/EP2006062695
申请日：2006-05-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , STOJANOVIC ALEKSANDAR , MARTI CHRISTIANE , JOTTERAND NATHALIE , SCHUMACHER CHRISTOPH , QUIRMBACH MICHAEL
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , STOJANOVIC ALEKSANDAR , MARTI CHRISTIANE , JOTTERAND NATHALIE , SCHUMACHER CHRISTOPH , QUIRMBACH MICHAEL
IPC分类号： C07D491/20 , A61P5/00 , C07D471/10 , C07D471/20 , C07D491/10
CPC分类号： C07D471/04 , C07D471/10 , C07D491/10
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R 1 , R 2 , U, V, W, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及通式（I）的新的杂环化合物，其中A，R，R 1，R 2，U，V，W，X，Y Z，n和p具有在描述中更详细地阐述的定义，其制备方法和这些化合物作为药物的用途，特别是作为醛固酮合酶抑制剂。

9. 发明申请

WO2006095020A1 HETEROCYCLIC-SUBSTITUTED ALKANAMIDES USEFUL AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂有用的杂环取代的烷烃
公开(公告)号：WO2006095020A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060625
申请日：2006-03-10
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , BEHNKE, Dirk , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , BEHNKE, Dirk , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
IPC分类号： C07C237/20 , C07D307/14 , C07D321/08 , C07D211/58 , C07D307/52 , C07D307/93 , C07D207/14 , C07D205/04 , C07D319/12 , C07D493/08 , C07D309/04 , C07D311/96 , C07D309/14 , C07D303/36 , C07D311/94
CPC分类号： C07D309/06 , C07C237/20 , C07D207/14 , C07D211/58 , C07D303/36 , C07D307/00 , C07D307/14 , C07D307/20 , C07D307/52 , C07D307/93 , C07D309/08 , C07D309/10 , C07D311/00 , C07D311/94 , C07D311/96 , C07D313/14 , C07D319/12 , C07D319/14 , C07D321/08 , C07D493/08
摘要： Compounds of the general formula (I) in which the meanings of the substituents R 1 and R 2 are as stated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译：其中取代基R 1和R 2的含义如权利要求1所述的通式（I）的化合物具有肾素抑制性质并且可以使用作为药物

10. 发明申请

WO2005118541A3 HETEROCYCLIC COMPOUNDS AND THEIR USE AS ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
标题翻译：杂环化合物及其作为醛固酮合成酶抑制剂的用途
公开(公告)号：WO2005118541A3
公开(公告)日：2006-02-02
申请号：PCT/EP2005052418
申请日：2005-05-27
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , SCHUMACHER CHRISTOPH , BEHNKE DIRK , QUIRMBACH MICHAEL
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , SCHUMACHER CHRISTOPH , BEHNKE DIRK , QUIRMBACH MICHAEL
IPC分类号： C07D471/04 , A61K31/415 , C07D213/00
CPC分类号： C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) in which R, R
摘要翻译：本申请涉及通式（I）的新型杂环化合物，其中R，R

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