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1. 发明申请

WO2013117512A1 NOVEL AZETIDINE DERIVATIVES 审中-公开
标题翻译：新的AZETIDINE DERIVATIVES
公开(公告)号：WO2013117512A1
公开(公告)日：2013-08-15
申请号：PCT/EP2013/052139
申请日：2013-02-04
申请人： F. HOFFMANN-LA ROCHE AG , ANSELM, Lilly , BANNER, David , HAAP, Wolfgang , KUHN, Bernd , LUEBBERS, Thomas , PETERS, Jens-Uwe , SPINNLER, Beat
发明人： ANSELM, Lilly , BANNER, David , HAAP, Wolfgang , KUHN, Bernd , LUEBBERS, Thomas , PETERS, Jens-Uwe , SPINNLER, Beat
IPC分类号： C07D401/14 , A61K31/4439 , A61P3/00
CPC分类号： C07D401/14
摘要： The invention relates to a compound of formula (I) wherein A 1 , A 2 and R 1 to R 8 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）化合物，其中A1，A2和R1至R8如描述和权利要求中所定义。式（I）化合物可以用作药物。

2. 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。

3. 发明申请

WO2010063610A1 PYRIDAZINONE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO2010063610A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/065692
申请日：2009-11-24
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI, Daniela , GOBBI, Luca , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , ROGERS-EVANS, Mark , RUDOLPH, Markus
发明人： ALBERATI, Daniela , GOBBI, Luca , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , ROGERS-EVANS, Mark , RUDOLPH, Markus
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , A61P25/00 , A61K31/501
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14
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。

4. 发明申请

WO2006108773A1 (3,4-DIHYDRO-QUINAZOLIN-2-YL)-INDAN-1-YL-AMINES 审中-公开
标题翻译：（3,4-二氢 - 喹唑啉-2-基） - 茚满-1-基胺
公开(公告)号：WO2006108773A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/061279
申请日：2006-04-03
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
IPC分类号： C07D239/84 , A61K31/517 , A61P25/24
CPC分类号： C07D409/04 , C07D239/84 , C07D413/04
摘要： The present invention relates to compounds of formula (I) wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R2 is hydrogen, lower alkyl, aryl or hetaryl, wherein aryl and hetaryl may be optionally substituted by one or more substituents selected from the group consisting of lower alkyl or halogen; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I for 5-HT5Areceptor related diseases.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基，低级烷氧基，卤素或被卤素取代的低级烷基; R2是氢，低级烷基，芳基或杂芳基，其中芳基和杂芳基可以任选被一个或多个选自低级烷基或卤素的取代基取代; n为1或2; 及其药学上可接受的酸加成盐。已经发现式I化合物对5-HT5A受体具有良好的活性。因此，本发明提供式I化合物用于5-HT5受体相关疾病的用途。

5. 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。

6. 发明申请

WO2013120921A1 NOVEL PYRROLIDINE DERIVATIVES 审中-公开
标题翻译：新型吡咯烷衍生物
公开(公告)号：WO2013120921A1
公开(公告)日：2013-08-22
申请号：PCT/EP2013052914
申请日：2013-02-14
申请人： HOFFMANN LA ROCHE , BANNER DAVID , HAAP WOLFGANG , LUEBBERS THOMAS , PETERS JENS-UWE
发明人： BANNER DAVID , HAAP WOLFGANG , LUEBBERS THOMAS , PETERS JENS-UWE
IPC分类号： C07D401/14 , A61K31/401 , A61P3/00 , C07D403/06 , C07D405/14 , C07D409/14 , C07D417/08 , C07D417/14
CPC分类号： C07D417/14 , C07D207/10 , C07D401/14 , C07D403/06 , C07D403/08 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/08
摘要： The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）化合物，其中A1至A3和R1至R3如在说明书和权利要求书中所定义。式（I）化合物可以用作药物。

7. 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。

8. 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。

9. 发明申请

WO2005002577A1 DUAL NK1/NK3 ANTAGONISTS FOR TREATING SCHIZOPHRENIA 审中-公开
标题翻译：用于处理SCHIZOPHRENIA的双NK1 / NK3拮抗剂
公开(公告)号：WO2005002577A1
公开(公告)日：2005-01-13
申请号：PCT/EP2004/006929
申请日：2004-06-25
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN, Torsten , KOBLET, Andreas , PETERS, Jens-Uwe , SCHNIDER, Patrick , SLEIGHT, Andrew , STADLER, Heinz
发明人： HOFFMANN, Torsten , KOBLET, Andreas , PETERS, Jens-Uwe , SCHNIDER, Patrick , SLEIGHT, Andrew , STADLER, Heinz
IPC分类号： A61K31/44
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The use of compounds of the general formula wherein the substituents are as described in claim 1 or pharmaceutically active acid-addition salts thereof for the preparation of medicaments for the treatment of schizophrenia.
摘要翻译：使用通式的化合物，其中取代基如权利要求1所述或其药学活性的酸加成盐用于制备治疗精神分裂症的药物。

10. 发明申请

WO2013104613A1 MACROCYCLIC AMIDES AS PROTEASE INHIBITORS 审中-公开
标题翻译：大环素作为蛋白酶抑制剂
公开(公告)号：WO2013104613A1
公开(公告)日：2013-07-18
申请号：PCT/EP2013/050204
申请日：2013-01-08
申请人： F. HOFFMANN-LA ROCHE AG , ANSELM, Lilli , BANNER, David , BLANC, Jean-Baptiste , GAUFRETEAU, Delphine , HAAP, Wolfgang , HARTMANN, Guido , KUHN, Bernd , LUEBBERS, Thomas , PETERS, Jens-Uwe , SPINNLER, Beat
发明人： ANSELM, Lilli , BANNER, David , BLANC, Jean-Baptiste , GAUFRETEAU, Delphine , HAAP, Wolfgang , HARTMANN, Guido , KUHN, Bernd , LUEBBERS, Thomas , PETERS, Jens-Uwe , SPINNLER, Beat
IPC分类号： C07D498/08 , C07D498/18 , C07D498/22 , C07D515/08 , C07D515/22 , C07D273/01 , A61K31/395 , A61K31/407 , A61K31/4353 , A61K31/397 , A61P3/10
CPC分类号： C07D273/01 , C07D269/00 , C07D273/02 , C07D413/10 , C07D498/06 , C07D498/08 , C07D498/18 , C07D498/22 , C07D515/06 , C07D515/08 , C07D515/22
摘要： The invention relates to a compound of formula (I) wherein A, B, D and R 1 to R 6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）化合物，其中A，B，D和R 1至R 6如在说明书和权利要求书中所定义。式（I）化合物可以用作药物。

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