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11. 发明授权

US11034687B2 BACE1 inhibitors 有权
公开(公告)号：US11034687B2
公开(公告)日：2021-06-15
申请号：US16903616
申请日：2020-06-17
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Cosimo Dolente , Wolfgang Guba , Wolfgang Haap , Ulrike Obst Sander , Jens-Uwe Peters , Thomas Woltering
IPC分类号： C07D417/14
摘要： The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

12. 发明申请

US20200308166A1 BACE1 INHIBITORS 审中-公开
公开(公告)号：US20200308166A1
公开(公告)日：2020-10-01
申请号：US16903616
申请日：2020-06-17
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Cosimo Dolente , Wolfgang Guba , Wolfgang Haap , Ulrike Obst Sander , Jens-Uwe Peters , Thomas Woltering
IPC分类号： C07D417/14
摘要： The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

13. 发明授权

US10723729B2 BACE1 inhibitors 有权
公开(公告)号：US10723729B2
公开(公告)日：2020-07-28
申请号：US16512905
申请日：2019-07-16
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Cosimo Dolente , Wolfgang Guba , Wolfgang Haap , Ulrike Obst Sander , Jens-Uwe Peters , Thomas Woltering
IPC分类号： C07D417/14
摘要： The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

14. 发明授权

US10479796B2 Spiro-oxazolones 有权
公开(公告)号：US10479796B2
公开(公告)日：2019-11-19
申请号：US15174674
申请日：2016-06-06
申请人： Hoffmann-La Roche Inc.
发明人： Valerie Runtz-Schmitt , Patrick Schnider , Cosimo Dolente , Bernhard Fasching
IPC分类号： C07D491/107 , C07D491/10 , C07D491/12 , C07D498/10 , C07D491/20 , C07D519/00
摘要： The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

15. 发明申请

US20180057485A1 BACE1 INHIBITORS 审中-公开
公开(公告)号：US20180057485A1
公开(公告)日：2018-03-01
申请号：US15558273
申请日：2016-03-16
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Cosimo Dolente , Wolfgang Guba , Wolfgang Haap , Ulrike Obst Sander , Jens-Uwe Peters , Thomas Woltering
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

16. 发明授权

US09346824B2 Cyclohexyl-4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes as V1a antagonists 有权
标题翻译：环己基-4H，6H-5-氧杂-2,3,10b-三氮杂 - 苯并[e]薁作为V1a拮抗剂
公开(公告)号：US09346824B2
公开(公告)日：2016-05-24
申请号：US14245126
申请日：2014-04-04
申请人： Hoffmann-La Roche Inc.
发明人： Cosimo Dolente , Patrick Schnider
IPC分类号： A61K31/553 , C07D498/04
CPC分类号： C07D498/04
摘要： The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明提供作为V1a受体调节剂的4H，6H-5-氧杂-2,3,10b-三氮杂 - 苯并[e]薁，特别是作为V1a受体拮抗剂，它们的制备，含有它们的药物组合物及其用作药物。本发明的活性化合物可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑，抑郁障碍，强迫症强迫症，自闭症谱系障碍，精神分裂症和侵略行为。

17. 发明授权

US12116349B2 Methylquinazolinone derivatives 有权
公开(公告)号：US12116349B2
公开(公告)日：2024-10-15
申请号：US17835245
申请日：2022-06-08
申请人： Hoffmann-La Roche Inc.
发明人： Cosimo Dolente , David Stephen Hewings , Daniel Hunziker , Daniela Krummenacher , Piergiorgio Francesco Tommaso Pettazzoni , Juergen Wichmann
IPC分类号： C07D239/88 , A61P35/00
CPC分类号： C07D239/88 , A61P35/00
摘要： The invention provides a novel compound having the general formula (I)

or a pharmaceutically acceptable salt thereof. The compound of formula (I) can be used as a medicament.

18. 发明授权

US10829500B2 Pyridyl-triazabicycles 有权
公开(公告)号：US10829500B2
公开(公告)日：2020-11-10
申请号：US16527307
申请日：2019-07-31
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Cosimo Dolente , Wolfgang Guba , Wolfgang Haap , Andreas Kuglstatter , Ulrike Obst Sander , Jens-Uwe Peters , Mark Rogers-Evans , Thomas Woltering , Christian Schnider , Roger Wermuth
IPC分类号： C07D513/04 , A61K31/549 , C07D417/04 , A61P25/28
摘要： The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

19. 发明申请

US20200039997A1 SPIRO-OXAZOLONES 审中-公开
公开(公告)号：US20200039997A1
公开(公告)日：2020-02-06
申请号：US16596293
申请日：2019-10-08
申请人： Hoffmann-La Roche Inc.
发明人： Valerie Runtz-Schmitt , Patrick Schnider , Cosimo Dolente , Bernhard Fasching
IPC分类号： C07D491/107 , C07D491/12 , C07D498/10 , C07D491/10 , C07D491/20 , C07D519/00
摘要： The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

20. 发明申请

US20190337936A1 BACE1 INHIBITORS 审中-公开
公开(公告)号：US20190337936A1
公开(公告)日：2019-11-07
申请号：US16512905
申请日：2019-07-16
申请人： Hoffmann-La Roche Inc.
发明人： Bjoern Bartels , Cosimo Dolente , Wolfgang Guba , Wolfgang Haap , Ulrike Obst Sander , Jens-Uwe Peters , Thomas Woltering
IPC分类号： C07D417/14
摘要： The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

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