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1. 发明申请

WO2023057423A1 CYCLOHEPTA-THIENO-DIAZEPINE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF THE GABA A GAMMA1 RECEPTOR 审中-公开
公开(公告)号：WO2023057423A1
公开(公告)日：2023-04-13
申请号：PCT/EP2022/077524
申请日：2022-10-04
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , CECERE, Giuseppe , GALLEY, Guido , GOBBI, Luca , GOEBEL, Martin , HERNANDEZ, Maria-Clemencia , OLIVARES MORALES, Andrés Miguel , RATNI, Hasane , REUTLINGER, Michael , RUNTZ-SCHMITT, Valerie
IPC分类号： C07D495/14 , C07D495/22 , A61P25/00 , A61K31/5517
摘要： The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. (I) Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

2. 发明申请

WO2022194802A1 NEW THIADIAZOLOPYRIMIDONE DERIVATIVES 审中-公开
公开(公告)号：WO2022194802A1
公开(公告)日：2022-09-22
申请号：PCT/EP2022/056587
申请日：2022-03-15
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GRETHER, Nadine , O'HARA, Fionn Susannah , PIRAS, Matilde , RATNI, Hasane , REUTLINGER, Michael , VIFIAN, Walter , ZAMBALDO, Claudio
IPC分类号： C07D513/04 , A61K31/519 , A61P25/28
摘要： The invention relates to a compound of formula (I) wherein R1-R4 and A1 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

3. 发明申请

WO2020120521A1 7-PHENOXY-N-(3-AZABICYCLO[3.2.1]OCTAN-8-YL)-6,7-DIHYDRO-5H-PYRROLO[1,2-B][1,2,4]TRIAZOL-2-AMINE DERIVATIVES AND RELATED COMPOUNDS AS GAMMA-SECRETASE MODULATORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
公开(公告)号：WO2020120521A1
公开(公告)日：2020-06-18
申请号：PCT/EP2019/084538
申请日：2019-12-11
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： FREI, Beat , RATNI, Hasane
IPC分类号： C07D487/04 , A61K31/4196 , A61K31/501 , A61K31/506 , A61K31/46 , A61P25/28 , A61P27/16
摘要： The invention provides 7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl) -6,7-dihydro-5H-pyrrolo[l,2-b][l,2,4]triazol-2-amine derivatives and related compounds of the general formula (I) wherein R 1 , Ar, n and m are as described herein, compositions including the compounds, processes of manufacturing the compounds and the compounds for use in methods of medical treatment. The present compounds are as gamma-secretase modulators for the treatment of diseases associated with the deposition of β-amyloid in the brain, such as Alzheimer's disease, cerebral amyloid angiopathy, cochlear synaptopathy, hearing loss, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 54 to 74; examples 1 to 64; table). An exemplary compound is e.g. (R)-7-(3,5-difluorophenoxy)-N- ((lR,5S,8s)-3-(6-methoxypyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl) -6,7-dihydro-5H-pyrrolo[l,2-b][l,2,4]triazol-2-amine (example 1).

4. 发明申请

WO2018007331A1 FUSED PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：稠合的嘧啶衍生物
公开(公告)号：WO2018007331A1
公开(公告)日：2018-01-11
申请号：PCT/EP2017/066521
申请日：2017-07-03
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 , STEINER, Sandra , REUTLINGER, Michael
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
摘要： The present invention relates to compounds of formula (I), wherein R 1 is phenyl, lower alkyl, C 3-6 -cycloalkyl, -CH 2 -C 3-6 -cycloalkyl, or bridged C 3-5 -cycloalkyl, optionally substituted by one, two or three substituents, selected from halogen, lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen, halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R 3 is a five membered heteroaryl group, selected from (A), (B), (C), (D); wherein R 6 is hydrogen or lower alkyl; R 7 is halogen or lower alkyl; R 8 is hydrogen or lower alkyl; R 9 is hydrogen or lower alkyl; R 4 is lower alkyl or lower alkyl substituted by hydroxy; R 5 /R 5' is independently from each other hydrogen or lower alkyl; -( ) n - is –CH 2 - or –CH 2 CH 2 - for n being 1 or 2; X is CH or N; 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，其中R 1为苯基，低级烷基，C 3-6 - 环烷基， -CH 2 -C 3-6 - 环烷基或桥连的C 3-5 - 环烷基，其任选被一个，两个或三个取代基取代选自卤素，低级烷基或被卤素取代的低级烷基; R 2是氢，卤素，低级烷氧基，被卤素取代的低级烷基或被卤素取代的低级烷氧基; R 3是选自（A），（B），（C），（D）的五元杂芳基; 其中R 6是氢或低级烷基; R 7是卤素或低级烷基; R 8是氢或低级烷基; R 9是氢或低级烷基; R 4是低级烷基或被羟基取代的低级烷基; R 5 / R 5'彼此独立地为氢或低级烷基; - （ - ）n - 为-CH 2 - 或-CH 2 CH 2 - 时，n为1或 2; X是CH或N; 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。

5. 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。

6. 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。

7. 发明申请

WO2015197503A1 IMIDAZO[1,2-A]PYRAZIN-1YL-BENZAMIDE COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-公开
标题翻译：咪达唑[1,2-A]吡嗪-1-基 - 苯甲酰化合物治疗脊髓性肌阵挛
公开(公告)号：WO2015197503A1
公开(公告)日：2015-12-30
申请号：PCT/EP2015/063894
申请日：2015-06-22
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GREEN, Luke , PINARD, Emmanuel , RATNI, Hasane , WILLIAMSON, Patrick
IPC分类号： C07D487/04 , A61K31/519 , A61P21/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula (I) wherein A, X l , X 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as described herein, as well as pharmaceutically acceptable salts 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 for the treatment of spinal muscular atrophy.
摘要翻译：本发明提供式（I）化合物，其中A，X1，X2，R1，R2，R3，R4和R5如本文所述，以及其药学上可接受的盐。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用于治疗脊髓性肌肉萎缩的药物的用途。

8. 发明申请

WO2015173181A1 COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-公开
标题翻译：用于治疗脊柱肌瘤的化合物
公开(公告)号：WO2015173181A1
公开(公告)日：2015-11-19
申请号：PCT/EP2015/060343
申请日：2015-05-11
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC. , PTC THERAPEUTICS INC.
发明人： RATNI, Hasane , GREEN, Luke , NARYSHKIN, Nikolai A. , WEETALL, Marla L.
IPC分类号： C07D487/04 , C07D519/00 , A61K31/5025 , A61P21/00
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention provides compounds of formula (I) wherein A, R 1 , R 2 and R 3 are as described herein, as well as pharmaceutically acceptable salts 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：本发明提供式（I）化合物，其中A，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐。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

WO2021259815A1 AMIDOPYRIMIDONE DERIVATIVES 审中-公开
公开(公告)号：WO2021259815A1
公开(公告)日：2021-12-30
申请号：PCT/EP2021/066725
申请日：2021-06-21
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BELL, Andrew Simon , BESNARD, Jérémy , BRADLEY, Anthony Richard , GREEN, Luke , HAAP, Wolfgang , KOCER, Buelent , KUGLSTATTER, Andreas , LUCAS, Xavier , MATTEI, Patrizio , MAZUNIN, Dmitry , RATNI, Hasane , RIEMER, Claus , VAN HOORN, Willem Paul
IPC分类号： C07D239/95 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04 , C07D473/04 , A61P35/00 , A61K31/00
摘要： The present invention provides compounds of formula I or II: wherein X1, X3, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts 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.

10. 发明申请

WO2021249908A2 AMINO-PYRIMIDINE AMIDES 审中-公开
公开(公告)号：WO2021249908A2
公开(公告)日：2021-12-16
申请号：PCT/EP2021/065111
申请日：2021-06-07
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BEURIER, Angélica , BOGDOS, Michael , GREEN, Luke , KRAMER, Christian , MAZUNIN, Dmitry , PINARD, Emmanuel , RATNI, Hasane
IPC分类号： C07D403/06 , C07D498/10 , A61K31/397 , A61P1/10 , A61P13/00 , A61P29/00
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein, compositions including the compounds and methods of using the compounds.

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