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1. 发明申请

WO2006077024A2 5-AMINOINDOLE DERIVATIVES 审中-公开
标题翻译： 5-氨基吲哚衍生物
公开(公告)号：WO2006077024A2
公开(公告)日：2006-07-27
申请号：PCT/EP2006/000125
申请日：2006-01-10
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias Heinrich , PLANCHER, Jean-Marc , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria
发明人： NETTEKOVEN, Matthias Heinrich , PLANCHER, Jean-Marc , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria
IPC分类号： C07D209/40 , A61K31/404 , A61P3/04
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 5， R 4和m如说明书和权利要求书中所定义，及其药学上可接受的盐以及包含这些化合物的药物组合物及其制备方法。该化合物可用于治疗和/或预防与H3受体调节有关的疾病。

2. 发明申请

WO2005117865A1 NAPHTHALINE DERIVATIVES USEFUL AS HISTAMINE-3-RECEPTOR LIGANDS 审中-公开
标题翻译：作为组胺-3受体配体有用的萘衍生物
公开(公告)号：WO2005117865A1
公开(公告)日：2005-12-15
申请号：PCT/EP2005/005594
申请日：2005-05-24
申请人： F. HOFFMANN-LA ROCHE AG , GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , PLANCHER, Jean-Marc , RAAB, Susanne , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
发明人： GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , PLANCHER, Jean-Marc , RAAB, Susanne , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
IPC分类号： A61K31/435
CPC分类号： C07D401/10 , C07D205/04 , C07D207/06 , C07D207/12 , C07D207/14 , C07D209/44 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D217/06 , C07D295/088 , C07D295/192
摘要： The present invention relates to compounds of formula (I) wherein A, R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）化合物，其中A，R 1和R 2如说明书和权利要求及其药学上可接受的盐所定义，用于制备这些化合物和含有它们的药物组合物。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

3. 发明申请

WO2006045416A1 QUINOLINE DERIVATIVES 审中-公开
标题翻译：喹啉衍生物
公开(公告)号：WO2006045416A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/010814
申请日：2005-10-07
申请人： F. HOFFMANN-LA ROCHE AG , GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , RAAB, Susanne , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
发明人： GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , RAAB, Susanne , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
IPC分类号： C07D401/06 , C07D215/20 , A61K31/47
CPC分类号： C07D401/14 , C07D215/48 , C07D401/12 , C07D405/14 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein R', R 2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2和A如说明书和权利要求中所定义，及其药学上可接受的盐以及包含这些化合物和给他们准备的方法。该化合物可用于治疗和/或预防与H3受体调节相关的疾病。

4. 发明申请

WO2006063718A1 PIPERAZINYL PYRIDINE DERIVATIVES AS ANTI-OBESITY AGENTS 审中-公开
标题翻译：哌嗪衍生物作为抗生素代谢物
公开(公告)号：WO2006063718A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/013072
申请日：2005-12-07
申请人： F.HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias, Heinrich , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria
发明人： NETTEKOVEN, Matthias, Heinrich , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria
IPC分类号： C07D213/74 , C07D213/75 , C07D213/76 , A61K31/496 , A61P3/04
CPC分类号： C07D213/74 , C07D213/75 , C07D213/76
摘要： The present invention relates to compounds of formula (I), wherein R 1 , R 2 , X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment an /or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，X，Y，Z和m如说明书和权利要求中所定义，和其药学上可接受的盐以及包含这些化合物的药物组合物及其制备方法。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

5. 发明申请

WO2017097728A1 BRIDGED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：桥联的哌啶衍生物
公开(公告)号：WO2017097728A1
公开(公告)日：2017-06-15
申请号：PCT/EP2016/079816
申请日：2016-12-06
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , BAUMANN, Karlheinz , GALLEY, Guido , JAESCHKE, Georg , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , RODRIGUEZ-SARMIENTO, Rosa Maria
IPC分类号： C07D471/04 , C07D487/04 , A61P25/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to a compound of formula (I), wherein Het Ar 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, -CH 2 -C 3-6 -cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R 3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C 3-6 -cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n = 2, R 1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or 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，其中Het Ar是含有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为氢，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，-CH 2 -C 3 -C 6 - 环烷基取代的低级烷基，其被一个或两个取代基取代，所述取代基选自被卤素或卤素取代的低级烷基，或被卤素取代的低级烯基; R 3是氢，被卤素，低级烷基，卤素，C 3-6 - 环烷基或被羟基取代的低级烷基取代的低级烷基; n是1或2; 对于n = 2，R 1可以彼此独立; Y是CH或N; 或其药学活性酸加成盐与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。

6. 发明公开

EP3386978A1 BRIDGED PIPERIDINE DERIVATIVES 有权
公开(公告)号：EP3386978A1
公开(公告)日：2018-10-17
申请号：EP16805853.5
申请日：2016-12-06
申请人： F. Hoffmann-La Roche AG
发明人： BARTELS, Bjoern , BAUMANN, Karlheinz , GALLEY, Guido , JAESCHKE, Georg , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , RODRIGUEZ-SARMIENTO, Rosa Maria
IPC分类号： C07D471/04 , C07D487/04 , A61P25/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to a compound of formula (I), wherein Het Ar is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, -CH2-C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n = 2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or 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.

7. 发明授权

EP1841734B1 5-AMINOINDOLE DERIVATIVES 有权
标题翻译： 5-氨基吲哚衍生物
公开(公告)号：EP1841734B1
公开(公告)日：2009-07-29
申请号：EP06706180.4
申请日：2006-01-10
申请人： F. Hoffmann-La Roche AG
发明人： NETTEKOVEN, Matthias Heinrich , PLANCHER, Jean-Marc , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria
IPC分类号： C07D209/40 , A61K31/404 , A61P3/04
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4 and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

8. 发明授权

EP1805166B1 QUINOLINE DERIVATIVES 有权
标题翻译：喹啉
公开(公告)号：EP1805166B1
公开(公告)日：2011-07-27
申请号：EP05798160.7
申请日：2005-10-07
申请人： F. Hoffmann-La Roche AG
发明人： GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , RAAB, Susanne , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
IPC分类号： C07D401/06 , C07D215/20 , A61K31/47
CPC分类号： C07D401/14 , C07D215/48 , C07D401/12 , C07D405/14 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein R', R2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

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