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1. 发明申请

WO2013024168A1 PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗诸如阿尔茨海默病的TAUOPATHIES的哌嗪衍生物
公开(公告)号：WO2013024168A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/066136
申请日：2012-08-17
申请人： REMYND NV , GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
发明人： GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
IPC分类号： C07D285/08 , C07D417/04 , C07D417/12 , A61K31/433 , A61P25/28
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G 1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is -NR 2 R 3 ; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl; tetrahydropyran-4-yl; -CH 2 -cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R 2 and R 3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is -CH 2 - or -(CH 2 ) 2 -; Ar is phenyl or pyridinyl; R 4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
摘要翻译：本发明涉及式（IA）化合物，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基; 四氢吡喃-4-基; 苯; 被一个或多个卤素取代的苯乙基; 苯氧基; 被一个或多个卤素取代的苯氧基甲基; 苄氧; 由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3是低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基; 或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。本发明还涉及式（IA）化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。

2. 发明申请

WO2016015333A1 2-OXA-5-AZABICYCLO [2.2.1] HEPTAN-3-YL DERIVATIVES 审中-公开
标题翻译： 2-OXA-5-AZABICYCLO [2.2.1] HEPTAN-3-YL衍生物
公开(公告)号：WO2016015333A1
公开(公告)日：2016-02-04
申请号：PCT/CN2014/083549
申请日：2014-08-01
申请人： F.HOFFMANN-LA ROCHE AG , NORCROSS, Roger , GALLEY, Guido , CECERE, Giuseppe , PFLIEGER, Philippe , SHEN, Hong , HU, Yimin
发明人： NORCROSS, Roger , GALLEY, Guido , CECERE, Giuseppe , PFLIEGER, Philippe , SHEN, Hong , HU, Yimin
IPC分类号： C07D498/08 , A61K31/535
CPC分类号： C07D491/08 , C07D491/06
摘要： 2-Oxa-5-azabicyclo[2.2.1]heptan-3-yl derivatives or pharmaceutically suitable acid addition salts thereof, all racemic mixtures thereof, enantiomers and/or optical isomers thereof are provided, which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.
摘要翻译：提供2-氧杂-5-氮杂双环[2.2.1]庚-3-基衍生物或其药学上合适的酸加成盐，其全部外消旋混合物，对映体和/或光学异构体，其对微量胺具有良好的亲和性相关受体（TAAR），特别是TAAR1。

3. 发明申请

WO2006103399A1 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO2006103399A1
公开(公告)日：2006-10-05
申请号：PCT/GB2006/001062
申请日：2006-03-22
申请人： ISTITUTO DE RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , CECERE, Giuseppe , FERREIRA, Maria del Rosario Rico , JONES, Philip , PACE, Paola , PETROCCHI, Alessia , SUMMA, Vincenzo
发明人： CECERE, Giuseppe , FERREIRA, Maria del Rosario Rico , JONES, Philip , PACE, Paola , PETROCCHI, Alessia , SUMMA, Vincenzo
IPC分类号： C07D487/04 , C07D513/14 , C07D493/20 , C07D513/04 , C07D487/14 , C07D498/04 , A61K31/551 , A61K31/519 , A61P31/00 , A61K31/5377 , A61K31/553 , A61K31/542
CPC分类号： C07D487/04 , C07D487/14 , C07D513/04 , C07D513/14
摘要： Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R l , R 2 , R 3 , R 4 , R 5 , R 6 R 7 ; R 8 R 9 and R 10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment , or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是FHV整合酶的抑制剂和FHV复制抑制剂（I），其中m，n，X，R 1，R 2，R 3 R 4，R 5，R 6，R 6，R 7，本文定义了R 9和R 10和R 10。该化合物可用于预防或治疗HTV感染以及预防，治疗或延迟AIDS发病。该化合物用于抗HTV感染和ADDS作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

4. 发明申请

WO2015165085A1 MORPHOLIN-PYRIDINE DERIVATIVES 审中-公开
标题翻译：吗啉 - 吡啶衍生物
公开(公告)号：WO2015165085A1
公开(公告)日：2015-11-05
申请号：PCT/CN2014/076623
申请日：2014-04-30
申请人： F.HOFFMANN-LA ROCHE AG , NORCROSS, Roger , GALLEY, Guido , CECERE, Giuseppe , PFLIEGER, Philippe , SHEN, Hong , HU, Yimin
发明人： NORCROSS, Roger , GALLEY, Guido , CECERE, Giuseppe , PFLIEGER, Philippe , SHEN, Hong , HU, Yimin
IPC分类号： C07D413/04 , C07D413/14 , A61K31/5377 , A61P25/22 , A61P25/24 , A61P25/18 , A61P25/16 , A61P25/28 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/12
CPC分类号： C07D413/04 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds of formula (I), wherein X is CH or N; 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：本发明涉及式（I）化合物，其中X为CH或N; 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; 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，其所有相应的对映体和/或光学异构体，其可用于治疗抑郁症，焦虑障碍，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，阿尔茨海默氏病，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，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。

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