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1. 发明申请

WO2020127624A1 OXOPYRIDO[1,2-A]PYRIMIDINE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION 审中-公开
公开(公告)号：WO2020127624A1
公开(公告)日：2020-06-25
申请号：PCT/EP2019/086151
申请日：2019-12-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DEY, Fabian , DING, Xiao , HU, Yimin , LIU, Yongqiang , SHEN, Hong , SHI, Houguang , TAN, Xuefei , ZHOU, Chengang , ZHOU, Mingwei
IPC分类号： C07D519/00 , A61P31/04 , A61K31/519
摘要： The present invention relates to novel compounds of formula (I), wherein R 1 to R 7 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

2. 发明申请

WO2020109190A1 TRICYCLIC COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION 审中-公开
公开(公告)号：WO2020109190A1
公开(公告)日：2020-06-04
申请号：PCT/EP2019/082335
申请日：2019-11-25
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DEY, Fabian , HU, Yimin , LIU, Yongqiang , SHEN, Hong , SHI, Houguang , TAN, Xuefei , YAN, Shixiang , ZHANG, Weixing , ZHANG, Zhiwei , ZHOU, Chengang , ZHOU, Mingwei , ZHU, Wei
IPC分类号： C07D471/04 , C07D487/04 , A61P31/04 , A61K31/437
摘要： The present invention relates to novel compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as DNA gyrase and/or topoisomerase IV inhibitors in the treatment and/or prophylaxis of bacterial infection.

3. 发明申请

WO2014037480A1 6-AMINO ACID HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION 审中-公开
标题翻译：用于治疗和预防乙型肝炎病毒感染的6-氨基酸异羟尿嘧啶
公开(公告)号：WO2014037480A1
公开(公告)日：2014-03-13
申请号：PCT/EP2013/068429
申请日：2013-09-06
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GUO, Lei , HU, Taishan , HU, Yimin , KOCER, Buelent , LIN, Xianfeng , LIU, Haixia , MAYWEG, Alexander V. , QIU, Zongxing , SHEN, Hong , TANG, Guozhi , WANG, Lisha , WU, Guolong , YAN, Shixiang , ZHANG, Weixing , ZHOU, Mingwei , ZHU, Wei
IPC分类号： C07D401/14 , C07D413/14 , C07D403/06 , C07D409/14 , C07D417/14 , A61K31/506 , A61K31/5355 , A61P31/20
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/14 , C07D403/06 , C07D409/14 , C07D413/14 , A61K2300/00
摘要： The invention provides novel compounds having the general formula:, wherein R 1 , R 2 , R 3 , R 4 and A are as described herein, compositions including the compounds and methods of using the compounds.
摘要翻译：本发明提供具有以下通式的新化合物：其中R1，R2，R3，R4和A如本文所述，包括该化合物的组合物和使用该化合物的方法。

4. 发明申请

WO2020104436A1 FREE AMINO COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION 审中-公开
公开(公告)号：WO2020104436A1
公开(公告)日：2020-05-28
申请号：PCT/EP2019/081760
申请日：2019-11-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： SHEN, Hong , TAN, Xuefei , ZHOU, Chengang , ZHOU, Mingwei , HU, Yimin , SHI, Houguang , DEY, Fabian , LIU, Yongqiang , DING, Xiao
IPC分类号： C07D519/00 , A61P31/04 , A61K31/4375
摘要： -84- ABSTRACT The present invention relates to novel compounds of formula (I), (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein, and their pharmaceutically 5 acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

5. 发明申请

WO2016016292A1 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：WO2016016292A1
公开(公告)日：2016-02-04
申请号：PCT/EP2015/067353
申请日：2015-07-29
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GALLEY, Guido , HU, Yimin , NORCROSS, Roger , PFLIEGER, Philippe , SHEN, Hong
IPC分类号： C07D491/06 , A61K31/35 , A61K31/407 , A61P25/28
CPC分类号： C07D491/08 , C07D491/06
摘要： The present invention relates to compounds of formula (I), wherein L is a bond, -C(O)NH-, -NHC(O)-, -CH 2 NHC(O)-, CH 2 C(O)NH-, -CH 2 NH-, -NH- or -NHC(O)NH-; R1 is hydrogen, lower alkyl, halogen, lower alkoxy-alkyl, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is phenyl or heteroaryl selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl or pyrazolyl, and wherein phenyl and heteroaryl are optionally substituted by one, two or three substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl or O-CH 2 -cycloalkyl; 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L是一个键，-C（O）NH-，-NHC（O） - ， - CH 2 NHC（O） - ，CH 2 C（O）NH-， - CH 2 NH- ，-NH-或-NHC（O）NH-; R 1是氢，低级烷基，卤素，低级烷氧基 - 烷基，被卤素取代的低级烷氧基，被卤素取代的低级烷基或是选自吡啶基，嘧啶基，吡嗪基或吡唑基的苯基或杂芳基，其中苯基和杂芳基是任选地被一个，两个或三个选自卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，环烷基或O-CH 2 - 环烷基取代的取代基取代; 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。

6. 发明申请

WO2015181061A1 5-OXA-2-AZABICYCLO[2.2.2]OCTAN-4-YL AND 5-OXA-2-AZABICYCLO[2.2.1]HEPTAN-4-YL DERIVATIVES AS TAAR1 MODULATORS 审中-公开
标题翻译： 5-OXA-2-甲氨喋呤[2.2.2] OCT-4-YL和5-OXA-2-氮杂双环[2.2.1] HEPTAN-4-YL衍生物作为TAAR1调节剂
公开(公告)号：WO2015181061A1
公开(公告)日：2015-12-03
申请号：PCT/EP2015/061348
申请日：2015-05-22
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： CECERE, Giuseppe , GALLEY, Guido , HU, Yimin , NORCROSS, Roger , PFLIEGER, Philippe , SHEN, Hong
IPC分类号： C07D491/08 , A61K31/5386 , A61P25/00
CPC分类号： C07D491/08
摘要： The invention relates to compounds of formula (I) wherein.....C.....is -CH 2 - or -CH 2 -CH 2 -; X is -NH-, -C(0)NH- or -NHC(0)NH-; Ar is phenyl or a 5 or 6-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 cycloalkyl, lower alkoxy substituted by halogen or is cycloalkyl; -( )- is -CH 2 -; n is 0 or 1; m is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which compounds 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）的化合物，其中..... C .....是-CH 2 - 或-CH 2 -CH 2 - ; X是-NH-，-C（O）NH-或-NHC（O）NH-; Ar是苯基或含有一个或两个N原子的5或6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，被环烷基取代的低级烷氧基，被卤素取代的低级烷氧基或是环烷基; - （） - 是-CH 2 - ; n为0或1; m为0,1或2; 或其药学上合适的酸加成盐，适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，该化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD）压力相关疾病，精神障碍，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，药物滥用，代谢紊乱，进食障碍，糖尿病，糖尿病并发症，肥胖，血脂异常，能量消耗障碍和体温平衡的同化，紊乱和功能障碍，睡眠和昼夜节律紊乱以及心血管疾病。

7. 发明申请

WO2014184328A1 6-BRIDGED HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION 审中-公开
标题翻译：用于治疗和预防乙型肝炎病毒感染的6-桥联异噻唑啉酮
公开(公告)号：WO2014184328A1
公开(公告)日：2014-11-20
申请号：PCT/EP2014/060034
申请日：2014-05-16
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GUO, Lei , HU, Taishan , HU, Yimin , KOCER, Buelent , KOU, Buyu , LI, Gangqin , LIN, Xianfeng , LIU, Haixia , SHEN, Hong , SHI, Houguang , WU, Guolong , ZHANG, Zhisen , ZHOU, Mingwei , ZHU, Wei
IPC分类号： C07D491/08 , C07D453/06 , C07D471/08 , C07D487/08 , C07D491/18 , A61K31/506 , A61P31/12
CPC分类号： C07D498/18 , A61K31/506 , C07D417/14 , C07D453/06 , C07D471/08 , C07D487/08 , C07D491/08 , C07D491/18 , C07D498/08 , C07D498/20 , C07D513/08
摘要： The invention provides novel compounds having the general formula: wherein R 1 , R2, R3 and R 4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds for the treatment or prophylaxis of hepatitis B virus infection.
摘要翻译：本发明提供具有以下通式的新化合物：其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其药学上可接受的盐或互变异构体异构体或其对映异构体或非对映异构体。本发明还包含包含化合物的组合物和使用该化合物治疗或预防乙型肝炎病毒感染的方法。

8. 发明申请

WO2020109191A1 ARYL COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION 审中-公开
公开(公告)号：WO2020109191A1
公开(公告)日：2020-06-04
申请号：PCT/EP2019/082336
申请日：2019-11-25
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DEY, Fabian , HU, Yimin , LIU, Yongqiang , SHEN, Hong , SHI, Houguang , TAN, Xuefei , YAN, Shixiang , ZHANG, Weixing , ZHANG, Zhiwei , ZHOU, Chengang , ZHOU, Mingwei , ZHU, Wei
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61P31/04
摘要： The present invention relates to novel compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as DNA gyrase and/or topoisomerase IV inhibitors in the treatment and/or prophylaxis of bacterial infection.

9. 发明申请

WO2019228940A1 NOVEL OXOQUINOLIZINE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION 审中-公开
公开(公告)号：WO2019228940A1
公开(公告)日：2019-12-05
申请号：PCT/EP2019/063562
申请日：2019-05-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DEY, Fabian , DING, Xiao , HU, Yimin , LIU, Yongqiang , SHEN, Hong , SHI, Houguang , TAN, Xuefei , ZHOU, Chengang , ZHOU, Mingwei
IPC分类号： C07D519/00 , A61P31/04 , A61K31/437 , A61K31/4375
摘要： The present invention relates to novel compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as described herein, and their pharmaceutically 5 acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

10. 发明申请

WO2018178041A1 Novel pyrido[2,3-b]indole compounds for the treatment and prophylaxis of bacterial infection 审中-公开
公开(公告)号：WO2018178041A1
公开(公告)日：2018-10-04
申请号：PCT/EP2018/057709
申请日：2018-03-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DEY, Fabian , HU, Yimin , LIU, Yongqiang , LIN, Xianfeng , SHEN, Hong , SHI, Houguang , TAN, Xuefei , VERCRUYSSE, Maarten , YAN, Shixiang , ZHOU, Chengang , ZHOU, Mingwei
IPC分类号： C07D471/04 , A61K31/4375 , A61P31/04
摘要： The present invention relates to novel compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

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