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11. 发明申请

WO2023012130A1 NEW CYCLOPENTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM 审中-公开
公开(公告)号：WO2023012130A1
公开(公告)日：2023-02-09
申请号：PCT/EP2022/071608
申请日：2022-08-02
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GOBBI, Luca , HERNANDEZ, Maria-Clemencia , KOBLET, Andreas , OLIVARES MORALES, Andres Miguel , RUNTZ-SCHMITT, Valerie , ZORN, Nicolas
IPC分类号： C07D495/14 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/28
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 (formula (I)). Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, inparticular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

12. 发明申请

WO2016016162A1 6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES AS TAAR MODULATORS 审中-公开
标题翻译： 6-氨基-5,6,7,8-四氢萘-2-炔或3-氨基喹啉-7-基衍生物作为TAAR调节剂
公开(公告)号：WO2016016162A1
公开(公告)日：2016-02-04
申请号：PCT/EP2015/067106
申请日：2015-07-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GALLEY, Guido , GOERGLER, Annick , NORCROSS, Roger , PFLIEGER, Philippe , TIRLA, Alina , SCHMID, Philipp
IPC分类号： C07D213/81 , C07D311/04 , C07D231/14 , C07D239/28 , C07D413/12 , C07D261/20 , C07C233/80 , A61K31/435 , A61K31/415 , A61K31/505 , A61K31/167 , A61P25/00
CPC分类号： C07D417/12 , C07C209/78 , C07C211/60 , C07C217/92 , C07C231/12 , C07C233/80 , C07C237/48 , C07C255/42 , C07C255/58 , C07C255/60 , C07C273/1854 , C07C275/40 , C07C275/42 , C07C303/40 , C07C311/21 , C07C2601/02 , C07C2602/10 , C07D213/40 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/20 , C07D239/28 , C07D239/42 , C07D241/20 , C07D261/18 , C07D311/58 , C07D405/04 , C07D405/12 , C07D409/14
摘要： The present invention relates to a compound of formula (I), wherein L is –C(O)NH-, -NHC(O)-, -S(O) 2 NH-, -NH- or -NHC(O)NH-; Ar is phenyl, benzyl, naphthyl or heteroaryl, selected from the group consisting of pyridinyl, pyrazolyl, pyrimidinyl, isoxazolyl or pyrazinyl, wherein Ar may be optionally substituted by one, two or three R 1 ; R 1 is hydrogen, lower alkyl, lower alkoxy, halogen, cyano, cycloalkyl, NHC(O)-lower alkyl, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, or is phenyl optionally substituted by one or two halogen atoms, CF 3 O or lower alkyl, or is furanyl, thiazolyl or thiophenyl, optionally substituted by halogen or lower alkyl; X is CH or O; R is hydrogen or halogen; or a pharmaceutically suitable acid addition salt thereof, all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中L是-C（O）NH-，-NHC（O） - ， - S（O）2 NH - ， - NH-或-NHC（O）NH- ; Ar是苯基，苄基，萘基或杂芳基，选自吡啶基，吡唑基，嘧啶基，异恶唑基或吡嗪基，其中Ar可以任选被一个，两个或三个R 1取代; R 1是氢，低级烷基，低级烷氧基，卤素，氰基，环烷基，NHC（O） - 低级烷基，被卤素取代的低级烷氧基，被卤素取代的低级烷基，或被一个或两个卤素原子任选取代的苯基，CF 3 O或低级烷基，或是任选被卤素或低级烷基取代的呋喃基，噻唑基或噻吩基; X是CH或O; R是氢或卤素; 或其药学上合适的酸加成盐，所有外消旋混合物，其所有相应的对映体和/或光学异构体，其可用于治疗抑郁症，焦虑症，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经变性疾病，阿尔茨海默病，癫痫，偏头痛，高血压，物质滥用，代谢障碍，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失眠，睡眠障碍和昼夜节律，以及心血管疾病。

13. 发明申请

WO2021213952A1 BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM 审中-公开
公开(公告)号：WO2021213952A1
公开(公告)日：2021-10-28
申请号：PCT/EP2021/060021
申请日：2021-04-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GOBBI, Luca , HERNANDEZ, Maria-Clemencia , KNOFLACH, Frédéric , KOBLET, Andreas , O`CONNOR, Eoin Cornelius , OLIVARES MORALES, Andres Miguel , RUNTZ-SCHMITT, Valerie , WAMSTEEKER CUSULIN, Jaclyn , ZORN, Nicolas
IPC分类号： C07D487/04 , A61K31/5517 , A61P25/00 , A61P43/00
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.

14. 发明申请

WO2021198124A1 BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAMS 审中-公开
公开(公告)号：WO2021198124A1
公开(公告)日：2021-10-07
申请号：PCT/EP2021/058063
申请日：2021-03-29
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GOBBI, Luca , HERNANDEZ, Maria-Clemencia , KNOFLACH, Frédéric , KOBLET, Andreas , O`CONNOR, Eoin Cornelius , OLIVARES MORALES, Andres Miguel , REUTLINGER, Michael , RUNTZ-SCHMITT, Valerie , WAMSTEEKER CUSULIN, Jaclyn Ivy , ZORN, Nicolas
IPC分类号： C07D487/04 , A61K31/5517 , A61P25/00
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.

15. 发明申请

WO2016030306A1 SUBSTITUTED PYRAZINO[2,1-A]ISOQUINOLINE DERIVATIVES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的替代吡咯并[2,1-A]异喹啉衍生物
公开(公告)号：WO2016030306A1
公开(公告)日：2016-03-03
申请号：PCT/EP2015/069309
申请日：2015-08-24
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GALLEY, Guido , NORCROSS, Roger , PATINY-ADAM, Angélique , PFLIEGER, Philippe
IPC分类号： C07D471/04 , A61K31/436 , A61P3/00 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to a compound of formula (I) wherein R 1 /R 2 are independently from each other hydrogen or halogen; L is a bond, -NH-, -C(O)NH-, -NHC(O)- or NHC(O)NH-; R is hydrogen, lower alkyl, cycloalkyl, benzyl, phenyl or a five or six membered heteroaryl group, wherein phenyl and the heteroaryl groups are optionally substituted by one or two substituents, selected from halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl or di-lower alkyl amino or R is halogen if L is a bond. or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers. The compounds of formulas (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及其中R 1 / R 2彼此独立地为氢或卤素的式（I）化合物; L是键，-NH-，-C（O）NH-，-NHC（O） - 或NHC（O）NH-; R为氢，低级烷基，环烷基，苄基，苯基或五或六元杂芳基，其中苯基和杂芳基任选被一个或两个选自卤素，低级烷基，低级烷氧基，被卤素，被卤素，环烷基或二低级烷基氨基取代的低级烷氧基，或者如果L是一个键，则R是卤素。或其药学上合适的酸加成盐，与所有外消旋混合物，其所有相应的对映异构体和/或光学异构体。式（I）化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1，可用于治疗抑郁症，焦虑症，双相情感障碍，注意力缺陷多动障碍（ADHD）神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢性疾病如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，疾病能量消耗和同化，失调和体温平衡失调，睡眠障碍和昼夜节律以及心血管疾病。

16. 发明申请

WO2015165835A1 MORPHOLIN-PYRIDINE DERIVATIVES 审中-公开
标题翻译：吗啉 - 吡啶衍生物
公开(公告)号：WO2015165835A1
公开(公告)日：2015-11-05
申请号：PCT/EP2015/059002
申请日：2015-04-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GALLEY, Guido , PFLIEGER, Philippe , NORCROSS, Roger , CECERE, Giuseppe , SHEN, Hong , HU, Yimin
IPC分类号： C07D413/12 , A61K31/4245 , A61P25/00
CPC分类号： C07D413/04 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds of formula (I) wherein X is CR or N; R is hydrogen, halogen or lower alkyl; L is a bond, -C(O)- or -C(O)NH-; Ar is phenyl or a five or six membered heteroaryl group, containing one or two N atoms; R 1 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or cycloalkyl; n is 0, 1, 2 or 3; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及其中X为CR或N的式（I）化合物; R是氢，卤素或低级烷基; L是键，-C（O） - 或-C（O）NH-; Ar是苯基或含有一个或两个N原子的五或六元杂芳基; R1是卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素或环烷基取代的低级烷氧基; n为0,1,2或3; 或其药学上合适的酸加成盐，可用于所有外消旋混合物，其所有相应的对映异构体和/或光学异构体，其可用于治疗抑郁症，焦虑症，双相情感障碍，注意缺陷多动障碍（ADHD），应激相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经变性疾病，阿尔茨海默病，癫痫，偏头痛，高血压，物质滥用，代谢紊乱，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量障碍，同化，紊乱和体温平衡失调，睡眠障碍和昼夜节律，以及心血管疾病。

17. 发明公开

EP3174853A1 6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES AS TAAR MODULATORS 有权
标题翻译： 6-氨基-5,6,7,8-四氢萘基-2-YL ODER 3-氨基甘氨酸-7-Y-衍生物ALS TAAR-MODULATOREN
公开(公告)号：EP3174853A1
公开(公告)日：2017-06-07
申请号：EP15742253.6
申请日：2015-07-27
申请人： F. Hoffmann-La Roche AG
发明人： CECERE, Giuseppe , GALLEY, Guido , GOERGLER, Annick , NORCROSS, Roger , PFLIEGER, Philippe , TIRLA, Alina , SCHMID, Philipp
IPC分类号： C07D213/81 , C07D311/04 , C07D231/14 , C07D239/28 , C07D413/12 , C07D261/20 , C07C233/80 , A61K31/435 , A61K31/415 , A61K31/505 , A61K31/167 , A61P25/00
CPC分类号： C07D417/12 , C07C209/78 , C07C211/60 , C07C217/92 , C07C231/12 , C07C233/80 , C07C237/48 , C07C255/42 , C07C255/58 , C07C255/60 , C07C273/1854 , C07C275/40 , C07C275/42 , C07C303/40 , C07C311/21 , C07C2601/02 , C07C2602/10 , C07D213/40 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/20 , C07D239/28 , C07D239/42 , C07D241/20 , C07D261/18 , C07D311/58 , C07D405/04 , C07D405/12 , C07D409/14
摘要： The present invention relates to a compound of formula (I), wherein L is –C(O)NH-, -NHC(O)-, -S(O)2NH-, -NH- or -NHC(O)NH-; Ar is phenyl, benzyl, naphthyl or heteroaryl, selected from the group consisting of pyridinyl, pyrazolyl, pyrimidinyl, isoxazolyl or pyrazinyl, wherein Ar may be optionally substituted by one, two or three R1; R1 is hydrogen, lower alkyl, lower alkoxy, halogen, cyano, cycloalkyl, NHC(O)-lower alkyl, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, or is phenyl optionally substituted by one or two halogen atoms, CF3O or lower alkyl, or is furanyl, thiazolyl or thiophenyl, optionally substituted by halogen or lower alkyl; X is CH or O; R is hydrogen or halogen; or a pharmaceutically suitable acid addition salt thereof, all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中L是-C（O）NH-，-NHC（O） - ， - S（O）2 NH - ， - NH-或-NHC（O）NH- ; Ar是苯基，苄基，萘基或杂芳基，选自吡啶基，吡唑基，嘧啶基，异恶唑基或吡嗪基，其中Ar可以任选被一个，两个或三个R 1取代; R 1是氢，低级烷基，低级烷氧基，卤素，氰基，环烷基，NHC（O） - 低级烷基，被卤素取代的低级烷氧基，被卤素取代的低级烷基，或被一个或两个卤素原子任选取代的苯基，CF 3 O或低级烷基，或是任选被卤素或低级烷基取代的呋喃基，噻唑基或噻吩基; X是CH或O; R是氢或卤素; 或其药学上合适的酸加成盐，所有外消旋混合物，其所有相应的对映体和/或光学异构体，其可用于治疗抑郁症，焦虑症，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经退行性疾病，阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用，代谢障碍，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失眠，睡眠障碍和昼夜节律，以及心血管疾病。

19. 发明公开

EP3551627A1 NEW ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM 有权
公开(公告)号：EP3551627A1
公开(公告)日：2019-10-16
申请号：EP17816630.2
申请日：2017-12-07
申请人： F. Hoffmann-La Roche AG
发明人： BUETTELMANN, Bernd , CECERE, Giuseppe , FASCHING, Bernhard , GROEBKE ZBINDEN, Katrin , HERNANDEZ, Maria-Clemencia , KNUST, Henner , KOBLET, Andreas , PINARD, Emmanuel , THOMAS, Andrew
IPC分类号： C07D413/14 , A61K31/4439 , A61K31/501 , A61P25/28

20. 发明授权

EP3137459B1 MORPHOLIN-PYRIDINE DERIVATIVES HAVING AFFINITY TO THE TAAR1 RECEPTOR 有权
公开(公告)号：EP3137459B1
公开(公告)日：2018-05-23
申请号：EP15721608.6
申请日：2015-04-27
申请人： F. Hoffmann-La Roche AG
发明人： GALLEY, Guido , PFLIEGER, Philippe , NORCROSS, Roger , CECERE, Giuseppe , SHEN, Hong , HU, Yimin
IPC分类号： C07D413/12 , A61K31/4245 , A61P25/00
CPC分类号： C07D413/04 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds of formula (I) wherein X is CR or N; R is hydrogen, halogen or lower alkyl; L is a bond, -C(O)- or -C(O)NH-; Ar is phenyl or a five or six membered heteroaryl group, containing one or two N atoms; R1 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or cycloalkyl; n is 0, 1, 2 or 3; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

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