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1. 发明申请

WO2007073934A1 PYRIDINYL AMINE DERIVATIVES AS INHIBITORS OF CHOLESTERYL ESTER TRANSFER PROTEIN (CETP) 审中-公开
标题翻译：作为胆固醇转运蛋白（CETP）的抑制剂的吡啶胺衍生物
公开(公告)号：WO2007073934A1
公开(公告)日：2007-07-05
申请号：PCT/EP2006/012540
申请日：2006-12-27
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SAKAKI, Junichi , KISHIDA, Masashi , MATSUURA, Naoko , UMEMURA, Ichiro , KAWAHARA, Eiji , YAMADA, Ken , KONISHI, Kazuhide , IWAKI, Yuki , IMASE, Hidetomo , MIYAKE, Takahiro
发明人： SAKAKI, Junichi , KISHIDA, Masashi , MATSUURA, Naoko , UMEMURA, Ichiro , KAWAHARA, Eiji , YAMADA, Ken , KONISHI, Kazuhide , IWAKI, Yuki , IMASE, Hidetomo , MIYAKE, Takahiro
IPC分类号： C07D213/38 , C07D213/40 , C07D401/12 , A61K31/44 , A61K31/4439 , A61P3/00 , A61P9/00
CPC分类号： C07D401/12 , C07D213/74 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables are as defined, useful as inhibitors of chlosteryl ester transfer protein.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中变量如上所定义，可用作chlosteryl ester transfer protein的抑制剂。

2. 发明申请

WO2007128568A1 BICYCLIC DERIVATIVES AS CETP INHIBITORS 审中-公开
标题翻译：双酚衍生物作为CETP抑制剂
公开(公告)号：WO2007128568A1
公开(公告)日：2007-11-15
申请号：PCT/EP2007/004058
申请日：2007-05-08
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , KISHIDA, Masashi , MATSUURA, Naoko , IMASE, Hidetomo , IWAKI, Yuki , UMEMURA, Ichiro , OHMORI, Osamu , KAWAHARA, Eiji
发明人： KISHIDA, Masashi , MATSUURA, Naoko , IMASE, Hidetomo , IWAKI, Yuki , UMEMURA, Ichiro , OHMORI, Osamu , KAWAHARA, Eiji
IPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , A61K31/4427 , A61P9/00
CPC分类号： C07D471/04 , C07D401/12 , C07D401/14
摘要： The present invention relates to novel compounds of formula (I): or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.
摘要翻译：本发明涉及新的式（I）化合物：或其药物组合物，其全部变量在本文中定义。本发明还涉及本文中的化合物用于治疗或延缓进展到涉及CETP的疾病的公开。

3. 发明申请

WO2008009435A1 AMINO-PIPERIDINE DERIVATIVES AS CETP INHIBITORS 审中-公开
标题翻译：氨基哌啶衍生物作为CETP抑制剂
公开(公告)号：WO2008009435A1
公开(公告)日：2008-01-24
申请号：PCT/EP2007/006384
申请日：2007-07-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , IMASE, Hidetomo , IWAKI, Yuki , KAWANAMI, Toshio , MIYAKE, Takahiro , MOGI, Muneto , OHMORI, Osamu , QIN, Hongbo , UMEMURA, Ichiro , YAMADA, Ken , YASOSHIMA, Kayo
发明人： IMASE, Hidetomo , IWAKI, Yuki , KAWANAMI, Toshio , MIYAKE, Takahiro , MOGI, Muneto , OHMORI, Osamu , QIN, Hongbo , UMEMURA, Ichiro , YAMADA, Ken , YASOSHIMA, Kayo
IPC分类号： C07D401/12 , C07D311/30 , A61K31/455 , A61P9/00 , C07D211/58 , C07D401/14 , C07D413/14 , C07D417/14
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of formula (I), wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
摘要翻译：本发明提供式（I）化合物，其中变体R1，R2，R3，R4，R5，R6，R7如本文所定义，并且其中所述化合物是CETP的抑制剂，因此可用于治疗由CETP介导的或对CETP的抑制作用的疾病或疾病。

4. 发明申请

WO2009059943A1 4-BENZYLAMINO-1-CARBOXYACYL-PIPERIDINE DERIVATIVES AS CETP INHIBITORS USEFUL FOR THE TREATMENT OF DISEASES SUCH AS HYPERLIPIDEMIA OR ARTERIOSCLEROSIS 审中-公开
标题翻译： 4-苄氧基-1-羧氧基 - 哌啶衍生物作为CETP抑制剂用于治疗疾病如高脂血症或类风湿性心脏病
公开(公告)号：WO2009059943A1
公开(公告)日：2009-05-14
申请号：PCT/EP2008/064859
申请日：2008-11-03
申请人： NOVARTIS AG , MOGI, Muneto , YAMADA, Ken , YASOSHIMA, Kayo , KAWANAMI, Toshio , UMEMURA, Ichiro , IWAKI, Yuki , QIN, Hongbo , IMASE, Hidetomo
发明人： MOGI, Muneto , YAMADA, Ken , YASOSHIMA, Kayo , KAWANAMI, Toshio , UMEMURA, Ichiro , IWAKI, Yuki , QIN, Hongbo , IMASE, Hidetomo
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/5377 , A61P3/06
CPC分类号： C07D401/14 , C07D413/14
摘要： The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
摘要翻译：本发明提供式（I）化合物：其中变体R1，R2，R3，R4，R5，R6，R7如本文所定义，并且其中所述化合物是CETP的抑制剂，因此可用于治疗由CETP介导的或对CETP的抑制作用的疾病或疾病。

5. 发明申请

WO2007077005A1 3 , 5-SUBSTITΓUED PIPERIDINE COMPOUNDS AS RENIN INHIBITORS 审中-公开
标题翻译： 3,5-取代的哌啶化合物作为RININ抑制剂
公开(公告)号：WO2007077005A1
公开(公告)日：2007-07-12
申请号：PCT/EP2006/012581
申请日：2006-12-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , EHARA, Takeru , GROSCHE, Philipp , IRIE, Osamu , IWAKI, Yuki , KANAZAWA, Takanori , KAWAKAMI, Shimpei , KONISHI, Kazuhide , MOGI, Muneto , SUZUKI, Masaki , YOKOKAWA, Fumiaki
发明人： EHARA, Takeru , GROSCHE, Philipp , IRIE, Osamu , IWAKI, Yuki , KANAZAWA, Takanori , KAWAKAMI, Shimpei , KONISHI, Kazuhide , MOGI, Muneto , SUZUKI, Masaki , YOKOKAWA, Fumiaki
IPC分类号： C07D211/60 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545
CPC分类号： C07D401/12 , C07D211/60 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3, 5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula (I'), wherein R1 , R2, T, R3 and R4 are as defined in the specification.
摘要翻译：本发明涉及3,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,5-取代的哌啶化合物，制备3,5-取代的哌啶化合物的方法和新的中间体和部分其合成步骤。优选的化合物（其也可以盐形式存在）具有式（I'），其中R 1，R 2，T，R 3和R 4如说明书中所定义。

6. 发明申请

WO2006069788A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006069788A1
公开(公告)日：2006-07-06
申请号：PCT/EP2005/014102
申请日：2005-12-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BREITENSTEIN, Werner , EHARA, Takeru , EHRHARDT, Claus , GROSCHE, Philipp , HITOMI, Yuko , IWAKI, Yuki , KANAZAWA, Takanori , KONISHI, Kazuhide , MAIBAUM, Juergen, Klaus , MASUYA, Keiichi , NIHONYANAGI, Atsuko , OSTERMANN, Nils , SUZUKI, Masaki , TOYAO, Atsushi , YOKOKAWA, Fumiaki
发明人： BREITENSTEIN, Werner , EHARA, Takeru , EHRHARDT, Claus , GROSCHE, Philipp , HITOMI, Yuko , IWAKI, Yuki , KANAZAWA, Takanori , KONISHI, Kazuhide , MAIBAUM, Juergen, Klaus , MASUYA, Keiichi , NIHONYANAGI, Atsuko , OSTERMANN, Nils , SUZUKI, Masaki , TOYAO, Atsushi , YOKOKAWA, Fumiaki
IPC分类号： C07D401/10 , C07D401/12 , C07D413/12 , C07D413/04 , C07D409/12 , C07D405/12 , C07D409/10 , C07D401/14 , C07D417/12 , C07D413/14 , C07D471/04 , A61K31/4545 , A61P9/00
CPC分类号： C07D471/04 , C07D211/60 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要： 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
摘要翻译： 3,4-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,4-取代的哌啶化合物的药物制剂和/或包括给药3,4代哌啶化合物的方法，制备3,4-取代的哌啶化合物的方法和新的中间体和部分步骤因为它们的合成被公开。 3,4-二取代的哌啶化合物具有式（I），其中符号具有说明书中定义的含义。

7. 发明申请

WO2007132906A1 BENZYLAMINE DERIVATIVES AS CETP INHIBITORS 审中-公开
标题翻译：苯甲酰胺衍生物作为CETP抑制剂
公开(公告)号：WO2007132906A1
公开(公告)日：2007-11-22
申请号：PCT/JP2007/060086
申请日：2007-05-10
申请人： NOVARTIS AG , KONISHI, Kazuhide , IWAKI, Yuki
发明人： KONISHI, Kazuhide , IWAKI, Yuki
IPC分类号： C07D401/12 , C07D401/14 , C07D409/14 , A61K31/435 , C07F7/00 , A61P3/00 , A61P9/00
CPC分类号： C07D409/14 , C07D401/12 , C07D401/14
摘要： The present invention provides a compound of formula (I): said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
摘要翻译：本发明提供式（I）化合物：所述化合物是CETP的抑制剂，因此可用于治疗由CETP介导的病症或疾病或对CETP的抑制作用。

8. 发明申请

WO2006128659A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006128659A2
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005107
申请日：2006-05-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , NIHONYANAGI, Atsuko , TOYAO, Atsushi , IWAKI, Yuki , MASUYA, Keiichi
发明人： NIHONYANAGI, Atsuko , TOYAO, Atsushi , IWAKI, Yuki , MASUYA, Keiichi
CPC分类号： C07D417/14 , C07D403/12
摘要： The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula (I), wherein R1 , R2, R11 , C, E and D are as defined in the specification.
摘要翻译：本发明涉及取代的3,4-或更高级取代的哌嗪化合物，其用于制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 药物制剂或包含所述化合物的产品，和/或包括施用所述化合物的方法，所述化合物的制备方法，以及新型中间体，起始材料和/或其合成的部分步骤。化合物特别是式（I），其中R 1，R 2，R 11，C，E和D如说明书中所定义。

9. 发明申请

WO2010136493A1 SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS 审中-公开
标题翻译：取代的氨基酸衍生物作为NEPRILYSIN抑制剂
公开(公告)号：WO2010136493A1
公开(公告)日：2010-12-02
申请号：PCT/EP2010/057247
申请日：2010-05-26
申请人： NOVARTIS AG , COPPOLA, Gary Mark , IWAKI, Yuki , KARKI, Rajeshri Ganesh , KAWANAMI, Toshio , KSANDER, Gary Michael , MOGI, Muneto , SUN, Robert
发明人： COPPOLA, Gary Mark , IWAKI, Yuki , KARKI, Rajeshri Ganesh , KAWANAMI, Toshio , KSANDER, Gary Michael , MOGI, Muneto
IPC分类号： C07D213/82 , C07D239/36 , C07D261/18 , C07D271/06 , C07C233/47 , A61K31/21 , A61K31/435
CPC分类号： C07D317/34 , A61K31/197 , A61K31/216 , A61K31/325 , A61K31/351 , A61K31/357 , A61K31/41 , A61K31/421 , A61K31/44 , A61K31/505 , A61K31/5375 , A61K45/00 , A61K45/06 , C07B2200/05 , C07C233/47 , C07C233/49 , C07C233/51 , C07C233/56 , C07C233/63 , C07C235/12 , C07C235/78 , C07C237/16 , C07C237/22 , C07C255/60 , C07C271/22 , C07C275/24 , C07C311/08 , C07C311/51 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D213/82 , C07D239/28 , C07D239/34 , C07D239/36 , C07D257/04 , C07D261/18 , C07D263/32 , C07D265/30 , C07D271/06 , C07D295/15 , C07D309/32
摘要： The present invention provides a compound of formula I' or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 5 , B 1 , X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式I'化合物或其药学上可接受的盐，其中R1，R2，R3，R5，B1，X和n如本文所定义。本发明还涉及制备本发明化合物及其治疗用途的方法。本发明还提供药理活性剂和药物组合物的组合。

10. 发明申请

WO2010136474A3 SUBSTITUTED AMINOBUTYRIC DERIVATIVES AS NEPRILYSIN INHIBITORS 审中-公开
公开(公告)号：WO2010136474A3
公开(公告)日：2010-12-02
申请号：PCT/EP2010/057213
申请日：2010-05-26
申请人： NOVARTIS AG , COPPOLA, Gary Mark , IWAKI, Yuki , KARKI, Rajeshri Ganesh , KAWANAMI, Toshio , KSANDER, Gary Michael , MOGI, Muneto , SUN, Robert
发明人： COPPOLA, Gary Mark , IWAKI, Yuki , KARKI, Rajeshri Ganesh , KAWANAMI, Toshio , KSANDER, Gary Michael , MOGI, Muneto , SUN, Robert
IPC分类号： C07C233/45 , C07C233/57 , C07C233/64 , A61K31/166 , A61K31/165
摘要： The present invention provides a compound of formula (I') or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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