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1. 发明授权

US09688675B2 1,7-naphthyridine derivatives 有权
公开(公告)号：US09688675B2
公开(公告)日：2017-06-27
申请号：US15007631
申请日：2016-01-27
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Jens-Uwe Peters , Juergen Wichmann
IPC分类号： C07D471/02 , A61K31/44 , C07D471/04 , C07D401/04 , C07D498/04
CPC分类号： C07D471/04 , C07D401/04 , C07D498/04
摘要： The present invention relates to compounds of general formula I wherein R1, R2, R3 and R4 are as defined herein which may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.

2. 发明申请

US20160137643A1 1,7-NAPHTHYRIDINE DERIVATIVES 有权
标题翻译： 1,7-萘啶衍生物
公开(公告)号：US20160137643A1
公开(公告)日：2016-05-19
申请号：US15007631
申请日：2016-01-27
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Jens-Uwe Peters , Juergen Wichmann
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D401/04 , C07D498/04
摘要： The present invention relates to compounds of general formula I wherein R1, R2, R3 and R4 are as defined herein which maybe used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：本发明涉及通式I的化合物，其中R 1，R 2，R 3和R 4如本文所定义，其可用于治疗精神分裂症，强迫症人格障碍，主要抑郁症，双相性精神障碍，焦虑症，正常老化，癫痫，视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，恐慌症，帕金森病，痴呆，阿尔茨海默病，认知障碍，化疗诱发的认知功能障碍（“chemobrain”），唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑性共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风以及由于放射治疗引起的干扰，慢性应激，视神经病变或黄斑变性，或滥用选自酒精，阿片剂的神经活性药物，甲基苯丙胺，苯环利定和可卡因。

3. 发明申请

US20160016963A1 Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-one 有权
标题翻译：哌嗪基[1,2-a]吲哚-1-酮和[1,4]二氮杂环庚烯并[1,2-a]吲哚-1-酮
公开(公告)号：US20160016963A1
公开(公告)日：2016-01-21
申请号：US14868059
申请日：2015-09-28
申请人： Hoffmann-La Roche Inc.
发明人： Ravi Jagasia , Roland Jakob-Roetne , Juergen Wichmann
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates to compounds of general formula I wherein R1 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, CF3 or lower alkyl; R3 is hydrogen, lower alkyl, lower alkenyl, lower alkinyl, heterocycloalkyl, lower alkyl substituted by cyano, cyano, benzyl substituted by halogen, 2-oxa-6-aza-spiro[3.3]hept-6-yl or is lower alkoxy substituted by halogen; X is —CH2— or —CH2—CH2—; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：本发明涉及通式Ⅰ化合物，其中R1是卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素或氰基取代的低级烷氧基; R2是氢，CF3或低级烷基; R 3是氢，低级烷基，低级烯基，低级炔基，杂环烷基，被氰基取代的低级烷基，氰基，被卤素取代的苄基，2-氧杂-6-氮杂 - 螺[3.3]庚-6-基或是低级烷氧基取代通过卤素; X是-CH 2 - 或-CH 2 -CH 2 - ; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应。这些化合物可用于治疗精神分裂症，强迫症人格障碍，重性抑郁症，双相障碍，焦虑症，正常老化，癫痫，视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱导的认知功能障碍，唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风，放射治疗，慢性压力，滥用神经活性药物，如酒精，阿片剂，甲基苯丙胺，苯环利定和可卡因。

4. 发明申请

US20150259341A1 IMIDAZOPYRIDINE DERIVATIVES 有权
标题翻译：咪唑吡啶衍生物
公开(公告)号：US20150259341A1
公开(公告)日：2015-09-17
申请号：US14723061
申请日：2015-05-27
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Juergen Wichmann
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(0)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：本发明涉及通式的化合物，其中Ar是苯基或吡啶基; X1是N或CH，X2是N或CH，条件是X1或X2中只有一个是N，另一个是CH; R 1是氢，卤素，低级烷基，低级烷氧基，被卤素，氰基或S（O）2-低级烷基取代的低级烷基; R2是氢，卤素，低级烷基，低级烷氧基，被卤素或氰基取代的低级烷基; n为1或2; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应。这些化合物可用于治疗精神分裂症，强迫症人格障碍，重性抑郁症，双相障碍，焦虑症，正常老化，癫痫，视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱导的认知功能障碍，唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风，放射治疗，慢性压力，滥用神经活性药物，如酒精，阿片剂，甲基苯丙胺，苯环利定和可卡因。

5. 发明申请

US20150252049A1 MGLU2/3 ANTAGONISTS FOR THE TREATMENT OF AUTISTIC DISORDERS 审中-公开
标题翻译： MGLU2 / 3治疗传染性疾病的拮抗剂
公开(公告)号：US20150252049A1
公开(公告)日：2015-09-10
申请号：US14694625
申请日：2015-04-23
申请人： Hoffmann-La Roche Inc.
发明人： Silvia Gatti McArthur , Michael Saxe , Juergen Wichmann , Thomas Woltering
IPC分类号： C07D487/04 , C07D401/04
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/0031 , A61K9/0095 , A61K9/02 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/4825 , A61K9/4858 , A61K9/4866 , A61K31/00 , A61K31/444 , A61K47/10 , A61K2121/00 , C07D401/04 , C07D487/04
摘要： This invention relates to a new medical use for certain chemical compounds and pharmaceutical compositions containing them. The invention relates to compounds which are mGlu2/3 negative allosteric modulators for use in the treatment of Autistic Spectrum Disorder (ASD), in particular, autism. In another aspect, the invention relates to a pharmaceutical composition for use in the treatment of ASD comprising a compound according to the invention and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及某些化学化合物的新医疗用途和含有它们的药物组合物。本发明涉及用于治疗自闭症谱系（ASD），特别是自闭症的mGlu2 / 3负变构调节剂的化合物。另一方面，本发明涉及用于治疗ASD的药物组合物，其包含根据本发明的化合物和药学上可接受的载体。

6. 发明申请

US20150252044A1 SUBSTITUTED 1,6-NAPHTHYRIDINES 有权
公开(公告)号：US20150252044A1
公开(公告)日：2015-09-10
申请号：US14717109
申请日：2015-05-20
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Rainer E. Martin , Jens-Uwe Peters , Juergen Wichmann
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541
摘要： The present invention relates to the use of compounds of general formula wherein R′ is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)—NH-lower alkyl, CH2—C(O)—NH-lower alkyl, CH2—NH—C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, NH—S(O)2—CH3, —(CH2)m—O-lower alkyl or —(CH2)n—S(O)2—CH3; or is —(CR2)n-phenyl, optionally substituted by —S(O)2CH3 or lower alkoxy; or is —(CH2)n-heterocycloalkyl, optionally substituted by lower alkyl and ═O; or is —(CH2)n-heteroaryl, optionally substituted by one or two lower alkyl groups; or is —(CH2)n-cycloalkyl, optionally substituted by cyano; or R2 and R3 form together with the N atom to which they are attached a heterocyclic ring, selected from morpholine, piperidine, 1,1-dioxo-thiomorpholine or piperazine which may be substituted by lower alkyl or C(O)O-lower alkyl, or may form a pyrrolidine ring, optionally substituted by hydroxy; R is independently from n hydrogen or lower alkyl; n is 0, 1, 2, 3; m is 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, for the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs selected from alcohol, opiates, methamphetamine, phencyclidine or cocaine.

7. 发明申请

US20150246922A1 PIPERAZINO[1,2-A]INDOL-1-ONES AND [1,4]DIAZEPINO[1,2-A]INDOL-1-ONE 有权
标题翻译：哌嗪[1,2-A]吲哚-1-酮和[1,4]二氮杂萘并[1,2-A]吲哚-1-酮
公开(公告)号：US20150246922A1
公开(公告)日：2015-09-03
申请号：US14614232
申请日：2015-02-04
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Juergen Wichmann
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of general formula I or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, R and n are as defined herein.The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：本发明涉及通式I的化合物或其药学上可接受的盐，其中R1，R2，R3，X，R和n如本文所定义。这些化合物可用于治疗精神分裂症，强迫症人格障碍，重性抑郁症，双相障碍，焦虑症，正常老化，癫痫，视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱导的认知功能障碍，唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风，放射治疗，慢性压力，滥用神经活性药物，如酒精，阿片剂，甲基苯丙胺，苯环利定和可卡因。

8. 发明授权

US10577332B2 Tetrazole derivatives 有权
公开(公告)号：US10577332B2
公开(公告)日：2020-03-03
申请号：US15569349
申请日：2016-04-19
申请人： Hoffmann-La Roche Inc.
发明人： Marius Hoener , Juergen Wichmann
IPC分类号： C07D409/12 , A61K31/41 , C07D257/04 , C07D257/06
摘要： The present invention relates to compounds of formula I wherein R1′ is CH3 R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1′ and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tertbutyl, cyclopropyl or CF3; R3 is Cl, F, CF3, methyl, methoxy, isopropyl or cyclopropyl; R4 is hydrogen, methyl, F or Cl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof for use in the treatment of schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

9. 发明授权

US10457663B2 Pyrazol-pyridine derivatives 有权
公开(公告)号：US10457663B2
公开(公告)日：2019-10-29
申请号：US16049469
申请日：2018-07-30
申请人： Hoffmann-La Roche Inc.
发明人： Marius Hoener , Juergen Wichmann
IPC分类号： C07D401/04 , C07D409/14
摘要： The present invention relates to compounds of formula I wherein R1′ is CH3; R1 is CH3, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1′ and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, CH3, ethyl, isopropyl, tert-butyl, cyclopropyl, cyclopropyl-methyl or hydroxy-methyl; R3 is hydrogen, Cl, F, CF3, CH3, isopropyl, methoxy, cyano or cyclopropyl; R4 is hydrogen, CH3, F or Cl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

10. 发明授权

US10457644B2 Pyrazol compounds as EAAT3 inhibitors 有权
公开(公告)号：US10457644B2
公开(公告)日：2019-10-29
申请号：US16195441
申请日：2018-11-19
申请人： Hoffmann-La Roche Inc.
发明人： Marius Hoener , Juergen Wichmann
IPC分类号： C07D231/12
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R1′, R2, R3, R4 are as defined herein, compositions including the compounds and methods of using the compounds.

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