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1. 发明申请

WO2005023772A1 MALONAMIDE DERIVATIVES BLOCKING THE ACTIVITY OF GAMA-SECRETASE 审中-公开
标题翻译：马洛酮衍生物阻断游离氨基酸酶的活性
公开(公告)号：WO2005023772A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009700
申请日：2004-08-31
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18
CPC分类号： C07D223/16 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
摘要： The invention relates to malonamide derivatives of formula (I), wherein: R 1 is one of the following groups (Formulae a), b), c), d)); R 2 is lower alkyl, lower alkinyl, -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -S-lower alkyl, -(CH 2 ) n -CN, -(CR'R") n -CF 3 , -(CR'R") n -CHF 2 , -(CR'R") n -CH 2 F, -(CH 2 ) n -C(O)O-lower alkyl, -(CH 2 ) n -halogen, or is -(CH 2 ) n -cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF 3 ; R',R" are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R 3 , R 4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R 5 is hydrogen, lower alkyl, -(CH 2 ) n -CF 3 or -(CH 2 ) n -cycloalkyl; R 6 is hydrogen or halogen; R 7 is hydrogen or lower alkyl; R 8 is hydrogen, lower alkyl, lower alkinyl, -(CH 2 ) n -CF 3 ,-(CH 2 ) n -cycloalkyl or -(CH 2 ) n -phenyl, optionally substituted by halogen; R 9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF 3 ,-C(O)-CH 2 F,-C(O)-CHF 2 ,-C(O)-cycloalkyl,-C(O)-(CH 2 ) n -O-lower alkyl,-C(O)O-(CH 2 ) n -cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O) 2 -lower alkyl, -S(O) 2 -CF 3 ,-(CH 2 ) n -cycloalkyl or is -(CH 2 ) n -phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer’s disease.
摘要翻译：本发明涉及式（I）的丙二酰胺衍生物，其中：R 1是以下基团之一（式a），b），c），d））; R 2是低级烷基，低级炔基， - （CH 2）n O-低级烷基， - （CH 2）n S-低级烷基， - （CH 2）n -CN， - （CR'R“ CR'R“）n-CHF 2， - （CR'R”）n -CH 2 F， - （CH 2）n C（O）O-低级烷基， - （CH 2）n-卤素，或是 - （CH 2）任选被一个或多个选自苯基，卤素或CF 3的取代基取代; R'，R“独立地为n和彼此独立地为氢，低级烷基，低级烷氧基，卤素或羟基; R 3，R 4彼此独立地为氢，低级烷基，低级烷氧基，苯基或卤素; R 5是氢，低级烷基， - （CH 2）n -CF 3或 - （CH 2）n - 环烷基; R 6是氢或卤素; R 7是氢或低级烷基; R 8是任选被卤素取代的氢，低级烷基，低级炔基， - （CH 2）n -CF 3， - （CH 2）n - 环烷基或 - （CH 2） R 9是氢，低级烷基，-C（O）H，-C（O） - 低级烷基，-C（O）-CF 3，-C（O）-CH 2 F，-C（O） -C（O） - 环烷基，-C（O） - （CH 2）n O-低级烷基，-C（O）O-（CH 2）n - 环烷基，-C（O） - 苯基，任选被一个或多个或选自卤素或-C（O）O-低级烷基，或者是-S（O）2 - 低级烷基，-S（O）2-CF 3， - （CH 2）n - （CH 2）n - 苯基，任选被卤素取代; n为0,1,2,3或4; 和药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。这些化合物可用于治疗阿尔茨海默病。

2. 发明申请

WO2005040126A1 SUBSTITUTED DIBENZO-AZEPINE AND BENZO-DIAZEPINE DERIVATIVES USEFUL AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：用作GAMMA-分泌酶抑制剂的替代二苯并嗪和苯并二氮吡啶衍生物
公开(公告)号：WO2005040126A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/010821
申请日：2004-09-27
申请人： F. HOFFMAN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18
CPC分类号： C07D409/12 , C07D223/16 , C07D223/18 , C07D243/12 , C07D243/24
摘要： The present invention relates to compounds of the general formula (I) Wherein R 1 is -(CHR’) q -aryl or -(CHR') q -heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, lower alkoxy, CF 3 or halogen, or is lower alkyl, lower alkenyl, -(CH 2 ) n -Si(CH 3 ) 3 , -(CH 2 ) n -O-lower alkyl, -(CH 2 )n-S-lower alkyl, -(CH 2 ) q -cycloalkyl, -(CH 2 ) n -[CH(OH)] m -(CF 2 )p-CH q F( 3-q) , or is -(CH 2 )n-CR 2 -CF 3 , wherein the two R radicals form together with the carbon atom a cycloalkyl ring; R' is hydrogen or lower alkyl; n is 1, 2 or 3; in is 0 or 1; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl, -CH 2 CF 2 CF 3 , CH 2 CF 3 , (CH 2 ) 2 CF 3 , CF 3 , CHF 2 , CF 3 , CHF 2 , CH 2 F, or is aryl, optionally mono, di or tri-substituted by halogen, or is (CH 2 ) n NR 5 R 6 , wherein R 5 and R 6 are independently from each other hydrogen or lower alkyl; R 4 is one of the following groups wherein R 7 is hydrogen, lower akl, -(CH 2 ) n -CF 3 or -(CH 2 ) n -cycloalkyl; R 8 is hydrogen, lower alkyl, -C(O)-phenyl, -C(O)-lower alkyl, -C(O)O-(CH 2 ) n - cycloalkyl, -C(O)O-(CH 2 ) n -lower alkyl, -C(O)NH-(CH 2 ) n -lower alkyl or -C(O)NH(CH 2 ).-CyClOalkYl; R 9 is hydrogen, lower alkyl, -(CH 2 ) n -cycloalkyl or -(CH 2 ) n -CF 3 ; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racernates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease..
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是 - （CHR'）q-芳基或 - （CHR'）q-杂芳基，它们是未被取代的或被一个或二个或三个被低级烷基，低级烷氧基，CF 3或卤素，或低级烷基，低级烯基， - （CH 2）n -Si（CH 3）3 - ，（CH 2）n O-低级烷基， - （CH 2） CH 2）q - 环烷基， - （CH 2）n - [CH（OH）] m - （CF 2）p-CHFF（3-q）或 - 是（CH 2）n CR 2 CF 3，与碳原子一起为环烷基环; R'是氢或低级烷基; n为1,2或3; in是0或1; p是0，1，2，3，4，5或6; q为0,1,2或3; R 2是氢或低级烷基; R 3是氢，低级烷基，-CH 2 CF 2 CF 3，CH 2 CF 3，（CH 2）2 CF 3，CF 3，CHF 2，CF 3，CHF 2，CH 2 F，或者是芳基，任选地单，二或被卤素三取代，或是（CH 2）n NR 5 R 6，其中R 5和R 6彼此独立地是氢或低级烷基; R 4是下列基团之一，其中R 7是氢，低级ak， - （CH 2）n -CF 3或 - （CH 2）n - 环烷基; R8是氢，低级烷基，-C（O） - 苯基，-C（O） - 低级烷基，-C（O）O-（CH2）n-环烷基，-C（O）O-（CH2）低级烷基，-C（O）NH-（CH 2）n - 低级烷基或-C（O）NH（CH 2） R 9是氢，低级烷基， - （CH 2）n - 环烷基或 - （CH 2）n -CF 3; 以及用于治疗阿尔茨海默氏病的药学上合适的酸加成盐，光学纯对映异构体，ernernate或非对映体混合物。

3. 发明申请

WO2011036127A1 IMIDAZOPYRIDINE OR IMIDAZOPYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10A INHIBITORS 审中-公开
标题翻译：作为磷酸二酯酶10A抑制剂的咪唑并吡啶或咪唑并嘧啶衍生物
公开(公告)号：WO2011036127A1
公开(公告)日：2011-03-31
申请号：PCT/EP2010/063830
申请日：2010-09-21
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI, Daniela , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： ALBERATI, Daniela , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5025 , A61K31/5377 , A61K31/553 , C07D487/04
摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新咪唑并吡啶衍生物，其中R 1，R 2，R 3，R 4，R 5和A如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。

4. 发明申请

WO2012076430A1 TRIAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译：三唑啉化合物
公开(公告)号：WO2012076430A1
公开(公告)日：2012-06-14
申请号：PCT/EP2011/071685
申请日：2011-12-05
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , PETERS, Jens-Uwe
发明人： FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , PETERS, Jens-Uwe
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P25/00 , A61P35/00 , A61P3/10
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention is concerned with triazolopyridine compounds of formula (I), wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDEIOA and can be used as medicaments.
摘要翻译：本发明涉及式（I）的三唑并吡啶化合物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制PDEIOA并可用作药物。

5. 发明申请

WO2011117264A1 N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDE DERIVATIVES AND THEIR USE AS PDE10A INHIBITORS 审中-公开
标题翻译： N-（咪唑并吡啶-7-YL）-HETEROARYLAMIDE衍生物及其作为PDE10A抑制剂的用途
公开(公告)号：WO2011117264A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054385
申请日：2011-03-23
申请人： F. HOFFMANN-LA ROCHE AG , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P25/00 , A61P25/18
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R 1 , R 2 and R 8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDEIOA and used as medicaments.
摘要翻译：本发明涉及式（I）的新型咪唑并嘧啶衍生物，其中R 1，R 2和R 8如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDEIOA并用作药物。

6. 发明申请

WO2013034506A1 PDE10 MODULATORS 审中-公开
标题翻译： PDE10调制器
公开(公告)号：WO2013034506A1
公开(公告)日：2013-03-14
申请号：PCT/EP2012/067047
申请日：2012-09-03
申请人： F. HOFFMANN-LA ROCHE AG , BACHMANN, Stephan , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： BACHMANN, Stephan , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D231/14 , C07D233/90 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , A61P25/00 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422
CPC分类号： C07D471/04 , C07D231/14 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 5 , W, X, X 1 , Y, Y 1 , Z and Z 1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 5，W，X，X 1，Y，Y 1，Z和Z 1如说明书和权利要求书中所定义，以及生理上可接受的盐它们。这些化合物抑制PDE10A，可用作药物。

7. 发明申请

WO2011154327A1 NITROGEN CONTAINING HETEROARYL COMPOUNDS 审中-公开
标题翻译：含氮异氰酸酯化合物
公开(公告)号：WO2011154327A1
公开(公告)日：2011-12-15
申请号：PCT/EP2011/059234
申请日：2011-06-06
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , GRUBER, Felix , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria
发明人： BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , GRUBER, Felix , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61P25/00 , A61P35/00
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A 1 , A 2 , (a), R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基化合物，其中A1，A2，（a），R1，R2，R3，R4，R5和R6如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。

8. 发明申请

WO2011089132A1 NITROGEN-CONTAINING HETEROARYL DERIVATIVES 审中-公开
标题翻译：含氮含量衍生物
公开(公告)号：WO2011089132A1
公开(公告)日：2011-07-28
申请号：PCT/EP2011/050640
申请日：2011-01-19
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , VIEIRA, Eric
发明人： BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , VIEIRA, Eric
IPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , A 1 , A 2 , and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基衍生物，其中R1，R2，R3，R4，R5，A1，A2和Y如说明书和权利要求书中所定义，以及生理上可接受的盐及其酯。这些化合物抑制PDE10A，可用作药物。

9. 发明申请

WO2010094762A1 HETEROARYL SUBSTITUTED PYRIDAZINONE DERIVATIVES 审中-公开
标题翻译：异氟醚取代的吡咯烷酮衍生物
公开(公告)号：WO2010094762A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/052116
申请日：2010-02-19
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI, Daniela , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , ROGERS-EVANS, Mark , RUDOLPH, Markus
发明人： ALBERATI, Daniela , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , ROGERS-EVANS, Mark , RUDOLPH, Markus
IPC分类号： C07D403/14 , A61K31/501 , A61P25/00 , A61P25/18
CPC分类号： C07D403/14
摘要： The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的哒嗪酮衍生物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。

10. 发明申请

WO2009040288A1 1,1,1-TRIFLUORO-2-HYDROXY-3-PHENYLPROPANE DERIVATIVES 审中-公开
标题翻译： 1,1,1-三氟-2-羟基-3-苯基丙酸衍生物
公开(公告)号：WO2009040288A1
公开(公告)日：2009-04-02
申请号：PCT/EP2008/062412
申请日：2008-09-18
申请人： F. HOFFMANN-LA ROCHE AG , BAILLY, Jacques , HERTEL, Cornelia , HUNZIKER, Daniel , LERNER, Christian , OBST SANDER, Ulrike , PETERS, Jens-Uwe , PFLIEGER, Philippe , SCHULZ-GASCH, Tanja
发明人： BAILLY, Jacques , HERTEL, Cornelia , HUNZIKER, Daniel , LERNER, Christian , OBST SANDER, Ulrike , PETERS, Jens-Uwe , PFLIEGER, Philippe , SCHULZ-GASCH, Tanja
IPC分类号： C07D213/30 , C07D215/14 , C07D217/16 , C07D231/12 , A61K31/44 , A61P3/00 , C07D239/26 , C07D241/12 , C07D277/24 , C07D277/62 , C07D401/06 , C07D471/04 , C07D233/64 , C07D237/08 , A61P9/00
CPC分类号： C07D241/12 , C07D213/30 , C07D213/61 , C07D213/64 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D249/18 , C07D277/24 , C07D277/62 , C07D401/04 , C07D401/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds of formula (1), wherein A, n, R 1a to R 1e and R 2 to R 5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
摘要翻译：本发明涉及式（1）的化合物，其中A，n，R 1a至R 1d和R 2至R 5如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物是可用于治疗和/或预防糖尿病，血脂异常，肥胖，高血压，心血管疾病，肾上腺不平衡或抑郁症等疾病的糖皮质激素受体拮抗剂。

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