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1. 发明申请

WO2009106599A3 SUBSTITUTED PIPERIDINES AS THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：替代的哌啶类作为治疗化合物
公开(公告)号：WO2009106599A3
公开(公告)日：2009-12-03
申请号：PCT/EP2009052335
申请日：2009-02-27
申请人： NOVARTIS AG , HEROLD PETER , MAH ROBERT , STUTZ STEFAN , TSCHINKE VINCENZO , LYOTHIER ISABELLE , JELAKOVIC STJEPAN
发明人： HEROLD PETER , MAH ROBERT , STUTZ STEFAN , TSCHINKE VINCENZO , LYOTHIER ISABELLE , JELAKOVIC STJEPAN
IPC分类号： C07D405/12 , A61K31/445 , A61K31/4523 , A61K31/538 , A61K31/5386 , C07D405/14 , C07D413/12 , C07D413/14
CPC分类号： C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Use of compounds of the general formula (I) and pharmaceutically acceptable salt thereof, in which R, R1 and X have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin Il and/or HIV protease inhibitors.
摘要翻译：其中R，R 1和X具有描述中详细说明的定义的通式（I）化合物及其药学上可接受的盐作为β-分泌酶，组织蛋白酶D，浆细胞蛋白酶II和/或HIV蛋白酶抑制剂。

2. 发明申请

WO2009074674A3 TRISUBSTITUTED PIPERIDINES AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂的TRISUBSTITUTED PIPERIDINES
公开(公告)号：WO2009074674A3
公开(公告)日：2009-07-30
申请号：PCT/EP2008067407
申请日：2008-12-12
申请人： NOVARTIS AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , JELAKOVIC STJEPAN , STUTZ STEFAN , BEHNKE DIRK , JOTTERAND NATHALIE
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , JELAKOVIC STJEPAN , STUTZ STEFAN , BEHNKE DIRK , JOTTERAND NATHALIE
IPC分类号： C07D491/113 , A61K31/435 , A61P9/00 , A61P13/00 , C07D491/107
CPC分类号： C07D491/107 , C07D491/113
摘要： The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R1, R2', X, U, W, m and n have 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）的三取代哌啶及其盐，优选其药学上可接受的盐，其中R 1，R 2'，X，U，W，m和n具有说明书中所述的含义，它们的制备和这些化合物作为药物的使用，特别是作为肾素抑制剂。

3. 发明申请

WO2007031557A3 ALCANOIC ACID AMIDES SUBSTITUTED BY SATURATED O-HETEROCYCLES 审中-公开
标题翻译：用饱和杂环取代的无水酸酰胺
公开(公告)号：WO2007031557A3
公开(公告)日：2007-05-24
申请号：PCT/EP2006066368
申请日：2006-09-14
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , JELAKOVIC STJEPAN , MARTI CHRISTIANE
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , JELAKOVIC STJEPAN , MARTI CHRISTIANE
IPC分类号： A61K31/335 , A61P9/00
CPC分类号： A61K31/335
摘要： Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译：其中取代基R 1至R 6的含义如权利要求1中所示的通式（式I）的化合物具有肾素抑制性质并可用作药物。

4. 发明申请

WO2006103277A2 SUBSTITUTED PIPERIDINES 审中-公开
标题翻译：取代的管道
公开(公告)号：WO2006103277A2
公开(公告)日：2006-10-05
申请号：PCT/EP2006061197
申请日：2006-03-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , MARTI CHRISTIANE , STUTZ STEFAN , JELAKOVIC STJEPAN , HOLLINGER FRANK , KONTEATIS ZENON D , LUDINGTON JENNIFER L , QUIRMBACH MICHAEL , STOJANOVIC ALEKSANDAR , BEHNKE DIRK
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , MARTI CHRISTIANE , STUTZ STEFAN , JELAKOVIC STJEPAN , HOLLINGER FRANK , KONTEATIS ZENON D , LUDINGTON JENNIFER L , QUIRMBACH MICHAEL , STOJANOVIC ALEKSANDAR , BEHNKE DIRK
IPC分类号： C07D413/12 , A61K31/445 , C07D413/14
CPC分类号： C07D413/12 , C07D413/14
摘要： SP-P2140 ATE - 132 - Abstract Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：描述了通式（I）和（II）的新型取代的哌啶与具有如在说明书中详细说明的取代基定义的新颖取代的哌啶。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

5. 发明申请

WO2009056617A2 4,4-DISUBSTITUTED PIPERIDINES 审中-公开
标题翻译： 4,4-取代的哌啶
公开(公告)号：WO2009056617A2
公开(公告)日：2009-05-07
申请号：PCT/EP2008064767
申请日：2008-10-31
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , JELAKOVIC STJEPAN , STUTZ STEFAN , MARTI CHRISTIANE
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , JELAKOVIC STJEPAN , STUTZ STEFAN , MARTI CHRISTIANE
IPC分类号： C07D413/14 , A61K31/538
CPC分类号： C07D413/14
摘要： The application relates to 4,4-disubstituted piperidinesof the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R2, 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为药物，特别是作为肾素抑制剂。

6. 发明申请

WO2008113835A9 PROCESS FOR PREPARING (R OR S)-5-{1-AZIDO-3-[6-METHOXY-5-(3-METHOXY-PROPOXY)-PYRIDIN-3-YLMETHYL]-4-METHYL-PENTYL}-3-ALKYL-DIHYDRO-FURAN-2-ONE 审中-公开
标题翻译：（R OR S）-5- {1-氨基-3- [6-甲氧基-5-（3-甲氧基 - 丙氧基） - 吡啶-3-基]甲基] -4-甲基戊-3-炔酸的方法 - 二氢 - 呋喃-2-酮
公开(公告)号：WO2008113835A9
公开(公告)日：2009-02-19
申请号：PCT/EP2008053323
申请日：2008-03-19
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , LYOTHIER ISABELLE , BEHNKE DIRK
发明人： HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , LYOTHIER ISABELLE , BEHNKE DIRK
IPC分类号： C07D213/69
CPC分类号： C07D213/69 , C07D405/06
摘要： Compounds of the formula (E), in which R'3 is isopropyl and R'4 is C1-C8-alkyl, and in which the carbon atom to which the R'3 radical is bonded has either (R) or (S) configuration, preference being given to (R) configuration, are obtainable in high yields A) by a stereoselective addition of isopropyl-substitutedpropionic esters to 6- methoxy-5-(3-methoxypropoxy)pyridine-3-carbaldehyde to give corresponding 2- {hydroxy-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]methyl}-3-methylbutanoic esters, subsequent conversion of the OH group to a leaving group, and a subsequent regioselective elimination to give 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]- meth-(E)-ylidene]-3-methylbutanoic esters, followed by 1) hydrolysis to give the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)- pyridin-3-yl]meth-(E)-ylidene]-3-methylbutanoic acid, the enantioselective hydrogenation thereof to the corresponding chiral 2-[6-methoxy-5-(3-methoxy- propoxy)pyridin-3-ylmethyl]-3-methylbutanoic acid and the reduction thereof,or 2) hydrolysis to the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3- yl]meth-(E)-ylidene]-3-methylbutanoic acid, the reduction thereof to the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]meth-(E)-ylidene]-3- methylbutan-1-ol and the enantioselective hydrogenation thereof, or 3) reduction to the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]- meth-(E)-ylidene]-3-methylbutan-1-ol and the enantioselective hydrogenation thereof, or B) by a Sonogashira coupling of 5-bromo-2-methoxy-3-(3-methoxypropoxy)pyridine, SP-P2216_ATE -80- 5-iodo-2-methoxy-3-(3-methoxypropoxy)pyridine or of trifluoromethanesulphonic acid 6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl ester with 2-propyn-1-ol to give 3-[6- methoxy-5-(3-methoxypropoxy)pyridin-3-yl]prop-2-yn-1-ol, followed by addition of an R' 3-Grignard compound to give 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]- meth-(E)-ylidene]-3-methylbutan-1-ol and the enantioselective hydrogenation thereof; substitution of the chiral 2-[6-methoxy-5-(3-methoxy-propoxy)-pyridin-3-ylmethyl]-3- methyl-butan-1-ol resulting from pathways A) or B)to give 5-(2-halomethyl-3-methyl- butyl)-2-methoxy-3-(3-methoxy-propoxy)-pyridine, coupling thereof with a (E)-(R)-5- halo-2-alkyl-pent-4-enoic acid amide, followed by halogenation,hydroxylation lactonizatization and azidation.
摘要翻译：式（E）的化合物，其中R'3是异丙基，R'4是C1-C8-烷基，并且其中R'3基团键合的碳原子具有（R）或（S）通过立体选择性地向6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-甲醛中加入异丙基取代的丙酸酯，得到相应的2- { 羟基 - [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基]甲基} -3-甲基丁酸酯，随后OH基转化为离去基团，随后进行区域选择性消除，得到2- [1 - [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基] - 甲基 - （E） - 亚基] -3-甲基丁酸酯，然后1）水解，得到相应的2- [1- [6 - 甲氧基-5-（3-甲氧基丙氧基） - 吡啶-3-基]甲基 - （E） - 亚基] -3-甲基丁酸，其对映选择性氢化为相应的手性2- [6-甲氧基-5-（3 - 甲氧基 - 丙氧基）吡啶-3-基甲基] -3-甲基丁酸，或者2）水解成相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基]甲基 - （E） - 亚基] -3-甲基丁酸，还原的相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基]甲基 - （E） - 亚基] -3-甲基丁-1-醇及其对映选择性氢化，或 3）还原为相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基] - 甲基 - （E） - 亚基] -3-甲基丁-1-醇和对映选择性氢化，或B）通过5-溴-2-甲氧基-3-（3-甲氧基丙氧基）吡啶，SP-P2216_ATE -80- 5-碘-2-甲氧基-3-（3-甲氧基丙氧基）吡啶的Sonogashira偶联或的三氟甲磺酸6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基酯与2-丙炔-1-醇反应，得到3- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基] 丙-2-炔-1-醇，然后加入R'3-格氏化合物，得到2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基] - 甲基（ E） - 亚基] -3-甲基丁-1-醇和对映选择性氢其基因; 取代由途径A）或B）得到的手性2- [6-甲氧基-5-（3-甲氧基 - 丙氧基） - 吡啶-3-基甲基] -3-甲基 - 丁-1-醇，得到5-（ -2-甲氧基-3-（3-甲氧基 - 丙氧基） - 吡啶，与（E） - （R）-5-卤代-2-烷基 - 戊-4 - 烯酸酰胺，然后卤化，羟基化内酯化和叠氮化。

7. 发明申请

WO2008055941A8 PROCESS FOR PREPARING OF 2-ALKYL-3-ARYL-PROP-2 ENE-1-OLS 审中-公开
标题翻译：制备2-烷基-3-芳基-El-2环己-1-磺酸的方法
公开(公告)号：WO2008055941A8
公开(公告)日：2008-06-26
申请号：PCT/EP2007062024
申请日：2007-11-08
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , LYOTHIER ISABELLE , BEHNKE DIRK
发明人： HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , LYOTHIER ISABELLE , BEHNKE DIRK
IPC分类号： C07C29/36 , C07C29/44 , C07C41/18 , C07C41/30 , C07C43/23
CPC分类号： C07C41/20 , C07B2200/07 , C07C41/22 , C07C41/30 , C07C231/12 , C07C235/34 , C07C43/23 , C07C43/225
摘要： Process for preparing a compound of the formula (I) in which R 1 and R 2 are each independently 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, where R 1 and R 2 are not both H, and R 3 is C 1 -C 8 -alkyl, which is characterized in that a) a compound of the formula (II) in which R 1 and R 2 are each as defined above and X is Br, I, triflate, toyslate or mesylate is reacted with prop-2-yn-1-ol to give the compound of the formula (III), b) the compound of the formula (III) is reacted with an alkyl-metal compound in which "alkyl" is as defined above for R 3 to give a compound of the formula (I).
摘要翻译：制备式（I）化合物的方法，其中R 1和R 2各自独立地为H，C 1 -C 3 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 3 C 1 -C 8烷基，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 其中R 1和R 2都不是H，R 1和R 2都不是H， 3是C 1 -C 8 - 烷基，其特征在于a）式（II）的化合物，其中R 1 R 2和R 2各自如上所定义，X是Br，I，三氟甲磺酸酯，玩具和甲磺酸酯与丙-2-炔-1-醇反应，得到式（III）的化合物，b）式（III）化合物与烷基金属化合物反应，其中“烷基”如上述R 3所定义，得到式（I ）。

8. 发明申请

WO2007085651A8 PROCESS FOR THE STEREOSELECTIVE PREPARATION OF ALCOHOLS FROM ALPHA, BETA- INSATURATED COMPOUNDS 审中-公开
标题翻译：来自ALPHA，β-绝缘化合物的醇的立体选择性制备方法
公开(公告)号：WO2007085651A8
公开(公告)日：2007-10-11
申请号：PCT/EP2007050816
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： A process for the synthesis of an alcohol of formula (I), using as intermediate a compound of formula (V).
摘要翻译：用于合成式（I）的醇的方法，使用式（V）化合物作为中间体。

9. 发明申请

WO2008055939A3 PROCESS FOR PREPARING 2-ALKYL-3-HETEROCYCLYL- PROP-2-EN- 1-OL DERIVATIVES 审中-公开
标题翻译：制备2-烷基-3-环己基 - 丙-2-烯-1-醇衍生物的方法
公开(公告)号：WO2008055939A3
公开(公告)日：2008-07-31
申请号：PCT/EP2007062022
申请日：2007-11-08
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , LYOTHIER ISABELLE , BEHNKE DIRK
发明人： HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , LYOTHIER ISABELLE , BEHNKE DIRK
IPC分类号： C07D231/56
CPC分类号： C07D231/56
摘要： Process for preparing a compound of the formula (I) in which Het is a bicyclic unsaturated heterocyclyl bonded to the rest of the molecule via a carbon atom, where the ring not bonded directly to the rest of the molecule is substituted by R 1 and R 2 , R 1 and R 2 are each independently 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, where R 1 and R 2 are not both H, and R 3 is C 1 -C 8 -alkyl, which is characterized in that a) a compound of the formula ( II) in which Het, R 1 and R 2 are each as defined above and X is Br, I, triflate, tosylate or mesylate is reacted with prop-2-yn-1-ol to give a compound of the formula (III) and b) the compound of the formula (III) is reacted with an alkyl-metal compound in which "alkyl" is as defined above for R 3 to give a compound of the formula (I).
摘要翻译：制备其中Het是通过碳原子与分子的其余部分键合的双环不饱和杂环基的式（I）化合物的方法，其中不与分子的其余部分键合的环被R 1和R 2，R 1和R 2各自独立地为H，C 1〜 C 8 - 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 - C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基 -C 1 -C 8 - 烷氧基，其中R 1和R 2不都是H，R 其特征在于a）式（II）化合物，其中Het，C 1 -C 6烷基，C 1 -C 6烷基， R 1和R 2各自如上所定义，X是Br，I，三氟甲磺酸酯，甲苯磺酸酯或甲磺酸酯与丙-2-炔-1-醇反应，得到一种化合物（III）和b）使式（III）的化合物与烷基金属化合物反应，其中“烷基”如上述R 3所定义，得到式（一世）。

10. 发明申请

WO2007065942A3 BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS 审中-公开
标题翻译：双相异构体咪唑啉化合物
公开(公告)号：WO2007065942A3
公开(公告)日：2007-07-26
申请号：PCT/EP2006069462
申请日：2006-12-08
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , QUIRMBACH MICHAEL , MARTI CHRISTIANE , STOJANOVIC ALEKSANDAR , STUTZ STEFAN
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , QUIRMBACH MICHAEL , MARTI CHRISTIANE , STOJANOVIC ALEKSANDAR , STUTZ STEFAN
IPC分类号： C07D471/04 , A61K31/437 , A61P5/42
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , R 3 , R 4 and n 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R 1，R 2，R 2，R 3，R 3，R 3，并且n具有在说明书中更详细地描述的定义，其制备方法和这些化合物作为药物，特别是作为醛固酮合酶抑制剂的用途。

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