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31. 发明申请

WO2016055496A1 BACE1 INHIBITORS 审中-公开
标题翻译： BACE1抑制剂
公开(公告)号：WO2016055496A1
公开(公告)日：2016-04-14
申请号：PCT/EP2015/073077
申请日：2015-10-07
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , CUENI, Philipp , DOLENTE, Cosimo , GUBA, Wolfgang , HAAP, Wolfgang , KUGLSTATTER, Andreas , OBST SANDER, Ulrike , PETERS, Jens-Uwe , ROGERS-EVANS, Mark , VIFIAN, Walter , WOLTERING, Thomas
IPC分类号： C07D513/04 , A61K31/554 , A61K31/542 , A61P25/28
CPC分类号： C07D513/04 , A61P25/28 , C07D519/00
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.
摘要翻译：本发明提供具有BACE1抑制活性的式I化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默氏病。

32. 发明申请

WO2016023927A1 2,2,2-TRIFLUOROETHYL-THIADIAZINES 审中-公开
标题翻译： 2,2,2-三氟 - 噻二嗪
公开(公告)号：WO2016023927A1
公开(公告)日：2016-02-18
申请号：PCT/EP2015/068506
申请日：2015-08-12
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： ANSELM, Lilli , BARTELS, Bjoern , DOLENTE, Cosimo , GUBA, Wolfgang , HAAP, Wolfgang , PETERS, Jens-Uwe , WOLTERING, Thomas , OBST SANDER, Ulrike , ROGERS-EVANS, Mark
IPC分类号： C07D403/12 , A61K45/06 , A61K31/54
CPC分类号： C07D403/12
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.
摘要翻译：本发明提供具有BACE1抑制活性的式（I）化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默氏病。

33. 发明申请

WO2015044075A1 ETHYNYL DERIVATIVES 审中-公开
标题翻译：乙炔衍生物
公开(公告)号：WO2015044075A1
公开(公告)日：2015-04-02
申请号：PCT/EP2014/070100
申请日：2014-09-22
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BIEMANS, Barbara , GUBA, Wolfgang , JAESCHKE, Georg , RICCI, Antonio , RUEHER, Daniel , VIEIRA, Eric
IPC分类号： C07D405/14 , C07D401/04 , C07D401/10 , C07D405/04 , C07D239/91 , C07D471/04 , C07D473/04 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/517 , A61P3/10 , A61P25/10 , A61P25/22 , A61P25/24
CPC分类号： C07D239/96 , C07D239/91 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/14 , C07D471/04 , C07D473/04 , C07D475/02 , C07D475/04 , C07D487/04 , C07D487/06 , C07D495/04 , C07D513/04
摘要： The present invention relates to compounds of formula I wherein Y is N or C-R 1' ; G is a 5 or 6-membered aromatic or heteroaromatic ring containing 0, 1, 2 or 3 heteroatoms, selected from the group consisting of phenyl, pyridinyl with different N-positions, imidazolyl, pyrazinyl, pyrimidinyl, thiophenyl, thiazolyl, pyrazolyl or thiadiazolyl, which are optionally substituted by 1, 2 or 3 substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or NRR'; R and R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a five or six membered saturated heterocyclic group which may contain an additional oxygen, NH, or N-lower alkyl group; R 1 is hydrogen, halogen or lower alkyl substituted by halogen; R 1' is hydrogen, halogen or lower alkyl substituted by halogen; R 2 is hydrogen, lower alkyl, lower alkoxyalkyl, cycloalkyl or heterocycloalkyl; or R 2 may form together with the closest carbon atom in group G a group (IA) for A being -CH 2 -, -CH 2 CH 2 , or -C(CH 3 ) 2 -, R 3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; 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. It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
摘要翻译：本发明涉及式I化合物，其中Y是N或C-R 1'; G是含有0,1,2或3个杂原子的5或6元芳族或杂芳环，选自苯基，具有不同N-位的吡啶基，咪唑基，吡嗪基，嘧啶基，噻吩基，噻唑基，吡唑基或噻二唑基其任选被1,2或3个选自卤素，低级烷基，低级烷氧基，被卤素或NRR'取代的低级烷氧基的取代基取代; R和R'彼此独立地为氢或低级烷基，或者可以与它们所连接的N原子一起形成五元或六元饱和杂环基，其可以含有另外的氧，NH或N-低级烷基 ; R1是氢，卤素或被卤素取代的低级烷基; R 1'是氢，卤素或被卤素取代的低级烷基; R2是氢，低级烷基，低级烷氧基烷基，环烷基或杂环烷基; 或R 2可以与G中最接近的碳原子一起形成A的基团（IA）为-CH 2 - ， - CH 2 CH 2或-C（CH 3）2 - ，R 3为苯基或吡啶基，其中吡啶基中的N原子组可能处于不同的位置; 或其药学上可接受的盐或酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。已经令人惊奇地发现，通式I的化合物是代谢型谷氨酸受体4（mGluR4）的正变构调节剂（PAM），其可用于治疗帕金森病，焦虑，呕吐，强迫症，孤独症，神经保护，癌症，抑郁症和糖尿病2型。

34. 发明申请

WO2023088856A1 HETEROCYCLIC NLRP3 INHIBITORS 审中-公开
公开(公告)号：WO2023088856A1
公开(公告)日：2023-05-25
申请号：PCT/EP2022/081866
申请日：2022-11-15
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： AITKEN, Lewis Scott , BOUCHE, Lea Aurelie , GUBA, Wolfgang , JAESCHKE, Georg , MESCH, Stefanie Katharina , STEINER, Sandra , TOSSTORFF, Andreas Michael
IPC分类号： C07D487/04 , C07D495/04 , A61K31/5025 , A61P3/00 , A61P9/00 , A61P11/00 , A61P29/00 , A61P35/00
摘要： The invention relates to novel compounds having the general formula Ib wherein R1, R1b, R2, R3, and Z are as described herein, composition including the compounds and methods of using the compounds.

35. 发明申请

WO2022043486A1 IMIDAZOLE-PYRAZOLE DERIVATIVES AS ANTIBACTERIALS 审中-公开
公开(公告)号：WO2022043486A1
公开(公告)日：2022-03-03
申请号：PCT/EP2021/073722
申请日：2021-08-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GRALL-ULSEMER, Sandra , GUBA, Wolfgang , LERNER, Christian , LI, Mingming , LIU, Yongqiang , RUDOLPH, Markus , SCHMITT, Sébastien , URNER, Lorenz , WANG, Yongguang , WANG, Min , WANG, Jianhua , YANG, Song , ZHOU, Chengang , MATTEI, Patrizio
IPC分类号： A61P31/04 , C07D401/14 , C07D403/14 , A61K31/4439 , A61K31/496 , A61K31/501 , A61K31/505
摘要： The invention provides novel imidazole pyrazole derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein A and R1-R7 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, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

36. 发明申请

WO2021233851A1 NEW MALONITRILE DERIVATIVES 审中-公开
公开(公告)号：WO2021233851A1
公开(公告)日：2021-11-25
申请号：PCT/EP2021/063037
申请日：2021-05-18
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DÉCORET, Guillaume , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , GUBA, Wolfgang , HUNZIKER, Daniel
IPC分类号： A61P17/00 , A61K31/4192 , A61K31/42 , C07D413/12 , A61K31/425 , A61K31/47 , A61P19/02 , A61P31/00 , A61P37/00 , C07D217/22 , C07D255/02 , C07D261/08 , C07D263/32 , C07D401/12 , C07D417/12 , C07D487/04 , C07D495/04
摘要： The invention relates to a compound of formula (I) wherein R1-R2 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

37. 发明申请

WO2021209484A1 BENZIMIDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2021209484A1
公开(公告)日：2021-10-21
申请号：PCT/EP2021/059622
申请日：2021-04-14
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , HUNZIKER, Daniel , GUBA, Wolfgang , BERCHTOLD, Stefan , KRUMM, Danny , KRUMMENACHER, Daniela , HILBERT, Manuel
IPC分类号： C07D235/06 , C07D235/08 , C07D235/10 , C07D235/14 , C07D235/30 , C07D401/06 , C07D403/06 , A61P29/00 , A61K31/4184
摘要： The invention relates to a compound of formula (I) wherein R1-R4 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

38. 发明申请

WO2017220544A1 NOVEL[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES 审中-公开
标题翻译： NOVEL [1,2,3] TRIAZOLO [4,5-D]嘧啶衍生物
公开(公告)号：WO2017220544A1
公开(公告)日：2017-12-28
申请号：PCT/EP2017/065037
申请日：2017-06-20
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GOBBI, Luca , GRETHER, Uwe , GUBA, Wolfgang , KRETZ, Julian , MARTIN, Rainer E. , WESTPHAL, Matthias
IPC分类号： C07D487/04 , A61K31/519 , A61P25/02 , A61P25/18 , A61P3/10 , A61P9/10 , A61P25/28 , A61P35/00 , A61P37/00 , A61P27/02
摘要： The invention relates to a compound of formula (I) wherein R wherein R 1 to R 4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）的化合物，其中R 1其中R 1至R 4如说明书中所定义并且在式索赔。式（I）化合物可以用作药物。

39. 发明申请

WO2017009275A1 ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS 审中-公开
标题翻译：乙烯衍生物作为代谢型谷氨酸受体调节剂
公开(公告)号：WO2017009275A1
公开(公告)日：2017-01-19
申请号：PCT/EP2016/066393
申请日：2016-07-11
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BIEMANS, Barbara , GUBA, Wolfgang , JAESCHKE, Georg , LINDEMANN, Lothar , O`HARA, Fionn , RICCI, Antonio , RUEHER, Daniel , VIEIRA, Eric
IPC分类号： C07D401/10 , C07D471/10 , C07D487/10 , C07D491/107 , C07D491/20 , A61K31/527 , A61P25/00
CPC分类号： C07D487/10 , A61P1/08 , A61P3/10 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P35/00 , C07D401/10 , C07D471/10 , C07D491/107 , C07D491/20
摘要： The present invention relates to compounds of formula I wherein R 1 is lower alkyl; R 2 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; n is 0, 1 or 2; V/U are independently from each other O or CH 2 , wherein V and U cannot be simultaneously O; L is a five or six membered heteroaryl group, selected from 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 may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
摘要翻译：本发明涉及式Ⅰ化合物，其中R 1是低级烷基; R2是苯基或吡啶基，其中吡啶基中的N原子可以在不同的位置; n为0,1或2; V / U彼此独立地为O或CH2，其中V和U不能同时为O; L是选自或可药用盐或酸加成盐的五元或六元杂芳基，外消旋混合物或其相应的对映异构体和/或其旋光异构体和/或立体异构体。该化合物可用于治疗帕金森病，焦虑症，呕吐，强迫症，孤独症，神经保护，癌症，抑郁症和糖尿病2型。

40. 发明申请

WO2016071211A1 BACE1 INHIBITORS 审中-公开
标题翻译： BACE1抑制剂
公开(公告)号：WO2016071211A1
公开(公告)日：2016-05-12
申请号：PCT/EP2015/075196
申请日：2015-10-30
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , DOLENTE, Cosimo , GUBA, Wolfgang , HAAP, Wolfgang , OBST SANDER, Ulrike , PETERS, Jens-Uwe , ROGERS-EVANS, Mark , ROMBACH, Didier , WOLTERING, Thomas
IPC分类号： C07D513/04 , A61K31/542 , A61P25/28
CPC分类号： C07D513/04
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.
摘要翻译：本发明提供具有BACE1抑制活性的式（I）化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默氏病。

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