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1. 发明申请

WO2018087018A1 PHENOXYTRIAZOLES 审中-公开
公开(公告)号：WO2018087018A1
公开(公告)日：2018-05-17
申请号：PCT/EP2017/078260
申请日：2017-11-06
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , BERCHTOLD, Stefan , GALLEY, Guido , GOERGLER, Annick , JAKOB-ROETNE, Roland , KRUMMENACHER, Daniela , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , REUTLINGER, Michael , RODRIGUEZ SARMIENTO, Rosa Maria , SCHNIDER, Christian
IPC分类号： C07D401/14 , C07D413/14 , C07D403/14 , C07D417/14 , A61K31/433 , A61K31/431 , A61K31/4245 , A61K31/435 , A61K31/44 , A61K31/497 , A61P25/00
摘要： The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two R 1 occur; R 2 is lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH 2 -cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH 2 -heterocycloalkyl unsubstituted or substituted by lower alkyl; R 3 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(0) 2 -lower alkyl; n is 1, 2 or 3; if n is >1, then R 3 may be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式I化合物，HetAr是五元或六元杂芳基，选自：其中R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基，并且如果两个R 1出现则可以相同或不同; R 2是低级烷基或其单或多缩合衍生物，被卤素或低级烷氧基取代的低级烷基，未被取代或被卤素，环烷基或CH 2 2 - 取代的低级链烯基，未被取代或被低级烷基取代的卤素，杂环烷基或CH 2 - 杂环烷基取代的环烷基; R 3为卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或S（O）2 - 低级烷基; n是1,2或3; 如果n> 1，则R 3可以相同或不同; 或其药学活性酸加成盐与外消旋混合物或其相应的对映体和/或其旋光异构体和/或立体异构体反应。这些化合物可用于治疗阿尔茨海默氏病，脑淀粉样血管病，具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发梗塞性痴呆，拳击员痴呆或唐氏综合症。

2. 发明申请

WO2018001918A1 TRIAZOLOPYRIDINES AS GAMMA-SECRETASE MODULATORS 审中-公开
标题翻译： TRIAZOLOPRIDINES作为GAMMA-SECRETASE调节剂
公开(公告)号：WO2018001918A1
公开(公告)日：2018-01-04
申请号：PCT/EP2017/065617
申请日：2017-06-26
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , RODRIGUEZ SARMIENTO, Rosa Maria
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28
摘要： The present invention relates to compounds of formula (I) HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R 1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R 2 is lower alkyl substituted by halogen; R 3 is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkyl substituted by hydroxy; Y is formula (A) or (B); R 4 is lower alkoxy, lower alkoxy substituted by halogen or CN; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式（I）的化合物，HetAr为含有1,2或3个选自N，O或S的杂原子的五元或六元杂芳基; R 1是氢，低级烷基，被卤素，卤素或低级烷氧基取代的低级烷基; R 2是被卤素取代的低级烷基; R 3是氢，被卤素取代的低级烷基，低级烷基或被羟基取代的低级烷基; Y是式（A）或（B）; R 4是低级烷氧基，被卤素或CN取代的低级烷氧基; 或其药学活性酸加成盐，外消旋混合物或其相应的对映异构体和/或光学异构体和/或立体异构体。这些化合物可用于治疗阿尔茨海默氏病，脑淀粉样血管病，具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发梗塞性痴呆，拳击员痴呆或唐氏综合症。

3. 发明申请

WO2017042114A1 BRIDGED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：桥连哌啶衍生物
公开(公告)号：WO2017042114A1
公开(公告)日：2017-03-16
申请号：PCT/EP2016/070800
申请日：2016-09-05
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BAUMANN, Karlheinz , GALLEY, Guido , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RODRIGUEZ SARMIENTO, Rosa Maria , BARTELS, Bjoern , RATNI, Hasane
IPC分类号： C07D519/00 , A61K31/4375 , A61P25/28
CPC分类号： C07D519/00
摘要： The present invention relates to compounds of formula (I); hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing -O-CH 2 -O-; n is 1 to 5; R 2 is hydrogen or lower alkyl substituted by halogen; R 3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式（I）化合物; 杂芳基是含有1至3个选自O，S或N的杂原子的五元杂芳基; R 1为氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的S-低级烷基或被卤素取代的低级烷氧基或两个相邻的碳原子，可在苯基上形成另外的含有-O-CH 2 - O-; n为1至5; R2是氢或被卤素取代的低级烷基; R3是氢或被卤素取代的低级烷基; 或其药学活性的酸加成盐，外消旋混合物或其相应的对映异构体或其旋光异构体或立体异构体。这些化合物可用于治疗阿尔茨海默病，脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆症或唐氏综合症。

4. 发明申请

WO2012117001A1 NOVEL BENZODIOXOLE PIPERIDINE COMPOUNDS 审中-公开
标题翻译：新型苯并咪唑化合物
公开(公告)号：WO2012117001A1
公开(公告)日：2012-09-07
申请号：PCT/EP2012/053387
申请日：2012-02-29
申请人： F. HOFFMANN-LA ROCHE AG , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
发明人： RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
IPC分类号： A61K31/36 , A61P25/18 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D405/04 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention is concerned with novel dual modulators of the 5-HT 2A and D 3 receptors of formula (I) wherein n, Y, R 1 , R 2 , R 3 , and R 4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
摘要翻译：本发明涉及式（I）的5-HT2A和D3受体的新型双重调节剂，其中n，Y，R 1，R 2，R 3和R 4如本文所述，以及其药学上可接受的盐和酯。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为药物的用途。

5. 发明申请

WO2012004206A1 ANELLATED PYRIDINE COMPOUNDS 审中-公开
标题翻译：陈化吡啶化合物
公开(公告)号：WO2012004206A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061167
申请日：2011-07-04
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
发明人： GOBBI, Luca , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
IPC分类号： C07D491/048 , C07D495/04 , A61K31/496 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30
CPC分类号： C07D495/04 , C07D491/048
摘要： The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R 1, R 2 , and R 3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
摘要翻译：本发明涉及式（I）的5-HT2A和D3受体的新型双重调节剂，其中X，Y，A，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为药物的用途。

6. 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。

7. 发明申请

WO2010034646A1 BENZO[D]ISOXAZOL-3-YL-PIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：苯并[D] ISOXAZOL-3-YL-PIPERAZIN衍生物作为DOPAMINE D3受体的调节剂有用
公开(公告)号：WO2010034646A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/061906
申请日：2009-09-15
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , JAESCHKE, Georg , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
发明人： GOBBI, Luca , JAESCHKE, Georg , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
IPC分类号： C07D413/04 , A61K31/496 , A61P25/00
CPC分类号： C07D413/04
摘要： The present invention relates to compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful for the therapeutic and/or prophylactic treatment of cognitive disorders.
摘要翻译：本发明涉及对多巴胺D3受体具有亲和性和选择性的通式（I）化合物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于认知障碍的治疗和/或预防性治疗。

8. 发明申请

WO2011161009A1 ANELLATED PYRIDINE COMPOUNDS AS DUAL MODULATORS OF THE 5-HT2A AND D3 RECEPTORS 审中-公开
标题翻译：作为5-HT2A和D3受体的双调节剂的胡萝卜素化合物
公开(公告)号：WO2011161009A1
公开(公告)日：2011-12-29
申请号：PCT/EP2011/060080
申请日：2011-06-17
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
发明人： GOBBI, Luca , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
IPC分类号： C07D491/048 , C07D495/04 , A61K31/496 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30
CPC分类号： C07D491/048 , C07D495/04
摘要： The present invention is concerned with novel dual modulators of the 5-HT 2A and D 3 receptors of formula (I) wherein X, Y, A, R 1 , R 2 , and R 3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
摘要翻译：本发明涉及式（I）的5-HT2A和D3受体的新型双重调节剂，其中X，Y，A，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为药物的用途。

9. 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。

10. 发明申请

WO2010034648A1 PYRIDINYLPIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：作为DOPAMINE D3受体的调节剂有用的吡啶并吡啶衍生物
公开(公告)号：WO2010034648A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/061911
申请日：2009-09-15
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , JAESCHKE, Georg , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
发明人： GOBBI, Luca , JAESCHKE, Georg , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
IPC分类号： C07D213/74 , A61K31/444 , A61P25/30
CPC分类号： C07D213/74
摘要： The present invention relates to compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful for the therapeutic and/or prophylactic treatment of cognitive disorders.
摘要翻译：本发明涉及对多巴胺D3受体具有亲和性和选择性的通式（I）化合物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于认知障碍的治疗和/或预防性治疗。

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