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1. 发明公开

EP3609904A1 ANTI-BACTERIAL PEPTIDE MACROCYCLES AND USE THEREOF 有权
公开(公告)号：EP3609904A1
公开(公告)日：2020-02-19
申请号：EP18717558.3
申请日：2018-04-09
申请人： F. Hoffmann-La Roche AG
发明人： ALANINE, Alexander , AMREIN, Kurt , BLEICHER, Konrad , FASCHING, Bernhard , HILPERT, Hans , KOLCZEWSKI, Sabine , KROLL, Carsten , SCHAEUBLIN, Adrian , ZAMPALONI, Claudia
IPC分类号： C07K5/02 , A61K38/00 , A61P31/04

2. 发明公开

EP1572203A1 SUBSTITUTED 4-ALKOXYOXAZOL DERIVATIVES AS PPAR AGONISTS 有权
标题翻译：取代的4- ALKOXYOXAZOL衍生物作为PPAR激动剂
公开(公告)号：EP1572203A1
公开(公告)日：2005-09-14
申请号：EP03810427.9
申请日：2003-10-31
申请人： F. HOFFMANN-LA ROCHE AG
发明人： BINGGELI, Alfred , GRETHER, Uwe , HILPERT, Hans , HIRTH, Georges , MAERKI, Hans-Peter , MEYER, Markus , MOHR, Peter
IPC分类号： A61K31/421 , C07D263/22 , C07D413/12 , A61K31/422 , A61P3/10
CPC分类号： C07D413/12 , C07D263/32 , C07D263/38
摘要： The present invention relates to compounds of formula (I) wherein R1 to R8 and n are as defined in the description and claims, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of diseases such as diabetes.

3. 发明授权

EP0975601B1 PROCESS FOR MAKING A BUTYLTHIO-ISOQUINOLINE AND INTERMEDIATES THEREFOR 失效
标题翻译：用于生产BUTHYLTHUIO-ISOCHINOLINDERIVATES及其中间体
公开(公告)号：EP0975601B1
公开(公告)日：2003-03-12
申请号：EP98919219.0
申请日：1998-04-03
申请人： F. HOFFMANN-LA ROCHE AG
发明人： HILPERT, Hans
IPC分类号： C07D217/26 , C07C321/28 , C07C319/14 , C07D303/36
CPC分类号： C07D303/36 , C07B2200/07 , C07C319/14 , C07C319/20 , C07C323/43 , C07C323/59 , C07D217/26 , C07F7/10 , C07F7/1852
摘要： A process for the manufacture of a phenylthiobutyl-isoquinoline of formula (II) and novel intermediates therefor.

4. 发明授权

EP0778823B1 VERFAHREN ZUR REDUKTION VON AMINOSÄUREN UND DEREN DERIVATEN 失效
标题翻译：一种用于减少氨基及其衍生物
公开(公告)号：EP0778823B1
公开(公告)日：1999-06-02
申请号：EP95930490.8
申请日：1995-08-17
申请人： Degussa Aktiengesellschaft , F. HOFFMANN-LA ROCHE AG
发明人： KOTTENHAHN, Matthias , DRAUZ, Karlheinz , HILPERT, Hans
IPC分类号： C07C213/00 , C07D263/24
CPC分类号： C07D263/20 , C07C213/00 , C07C215/08 , C07C215/10 , C07C215/28
摘要： A process is disclosed for reducing amino acids and derivatives thereof. Compounds of formula (I), in which n = 0 or 1 and R?1, R2, R3, R4, R5 and R6¿ have the meanings given in the description, are reduced to the corresponding amino alcohols of formula (II): the formula (I) compounds are converted in a first step, in at least one alcohol and with the addition of acid and heat, to an ester, this process producing a reaction mixture containing the ester; the ester is converted in a second reaction step with alkali or alkaline earth borohydride to compounds of formula II. By specifying that the second step be carried out without isolating the ester from the reaction mixture and by using alkali or alkaline earth borohydrides which are not activated, the invention facilitates the production from amino acids and their derivatives of the corresponding alcohols in a simple 'single vessel' process, with high yields and in such a way as to preserve a given centre of chirality. Applications: synthesis components, preparation of optically active compounds, splitting of racemic compounds.

5. 发明公开

EP0778823A1 VERFAHREN ZUR REDUKTION VON AMINOSÄUREN UND DEREN DERIVATEN 失效
标题翻译：一种用于减少氨基及其衍生物
公开(公告)号：EP0778823A1
公开(公告)日：1997-06-18
申请号：EP95930490.0
申请日：1995-08-17
申请人： Degussa Aktiengesellschaft , F. HOFFMANN-LA ROCHE AG
发明人： KOTTENHAHN, Matthias , DRAUZ, Karlheinz , HILPERT, Hans
IPC分类号： C07D263 , C07C213 , C07C215
CPC分类号： C07D263/20 , C07C213/00 , C07C215/08 , C07C215/10 , C07C215/28
摘要： A process is disclosed for reducing amino acids and derivatives thereof. Compounds of formula (I), in which n = 0 or 1 and R?1, R2, R3, R4, R5 and R6¿ have the meanings given in the description, are reduced to the corresponding amino alcohols of formula (II): the formula (I) compounds are converted in a first step, in at least one alcohol and with the addition of acid and heat, to an ester, this process producing a reaction mixture containing the ester; the ester is converted in a second reaction step with alkali or alkaline earth borohydride to compounds of formula II. By specifying that the second step be carried out without isolating the ester from the reaction mixture and by using alkali or alkaline earth borohydrides which are not activated, the invention facilitates the production from amino acids and their derivatives of the corresponding alcohols in a simple 'single vessel' process, with high yields and in such a way as to preserve a given centre of chirality. Applications: synthesis components, preparation of optically active compounds, splitting of racemic compounds.

6. 发明授权

EP3145923B1 INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-C]PYRIDIN-2-ONE DERIVATIVES 有权
公开(公告)号：EP3145923B1
公开(公告)日：2019-01-30
申请号：EP15723917.9
申请日：2015-05-19
申请人： F. Hoffmann-La Roche AG
发明人： HILPERT, Hans , KOLCZEWSKI, Sabine , LIMBERG, Anja , STOLL, Theodor
IPC分类号： C07D401/14 , C07D413/14 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/506 , C07D403/04 , C07D403/14 , C07D411/12 , C07D417/14 , C07D471/04 , A61P25/32 , A61P25/34 , A61P25/24 , A61P25/36

7. 发明公开

EP3368544A1 PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII 有权
公开(公告)号：EP3368544A1
公开(公告)日：2018-09-05
申请号：EP16785469.4
申请日：2016-10-24
申请人： F. Hoffmann-La Roche AG
发明人： ALANINE, Alexander , BEIGNET, Julien , BLEICHER, Konrad , FASCHING, Bernhard , HILPERT, Hans , HU, Taishan , MACDONALD, Dwight , JACKSON, Stephen , KOLCZEWSKI, Sabine , KROLL, Carsten , SCHAEUBLIN, Adrian , SHEN, Hong , STOLL, Theodor , THOMAS, Helmut , WAHHAB, Amal , ZAMPALONI, Claudia
IPC分类号： C07K5/02 , A61P31/04 , A61K38/00
CPC分类号： C07K5/0827 , A61K38/00 , C07K5/02 , C07K5/06086 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K5/0821
摘要： The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

8. 发明授权

EP2864324B1 DIFLUORO-HEXAHYDRO-CYCLOPENTAOXAZINYLS AND DIFLUORO-HEXAHYDRO-BENZOOXAZINYLS AS BACE1 INHIBITORS 有权
标题翻译：二氟 - 六氢 - 环戊并恶嗪和二氟 -
公开(公告)号：EP2864324B1
公开(公告)日：2018-03-28
申请号：EP13730887.0
申请日：2013-06-24
申请人： F. Hoffmann-La Roche AG
发明人： HILPERT, Hans
IPC分类号： C07D413/12 , C07D265/12 , A61K31/536 , A61P25/00
CPC分类号： C07D413/12
摘要： Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatment of, for example, Alzheimer's Disease.

9. 发明公开

EP3145923A1 INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES 有权
标题翻译：茚满-2-酮在1,3-二羟基吡咯并[3,2-C]吡啶-2-酮衍生物
公开(公告)号：EP3145923A1
公开(公告)日：2017-03-29
申请号：EP15723917.9
申请日：2015-05-19
申请人： F. Hoffmann-La Roche AG
发明人： HILPERT, Hans , KOLCZEWSKI, Sabine , LIMBERG, Anja , STOLL, Theodor
IPC分类号： C07D401/14 , C07D413/14 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/506 , C07D403/04 , C07D403/14 , C07D411/12 , C07D417/14 , C07D471/04 , A61P25/32 , A61P25/34 , A61P25/24 , A61P25/36
CPC分类号： C07D471/04 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D411/12 , C07D413/14 , C07D417/14
摘要： The present invention is concerned with indolin-2-one and l,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula (I) wherein Ar1 is phenyl, pyridinyl or pyrimidinyl; Ar2 is a 5 or 6 membered heteroaryl group, containing 2 or 3 heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, halogen or lower alkoxy; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, lower alkyl substituted by hydroxy, cycloalkyl, oxetan-3-yl, pyridinyl, imidazolyl, pyrazolyl, pyrimidinyl, which rings may optionally substituted by lower alkyl, or is -(CH2)3-S(O)2-cyclopropyl; X is CH or N; n is 1 or 2; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof, for use in the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.
摘要翻译：本发明涉及通式（I）的二氢吲哚-2-酮和1,3-二氢 - 吡咯并[3,2-c]吡啶-2-酮衍生物，其中Ar 1是苯基，吡啶基或嘧啶基; Ar 2是5或6元杂芳基，含有2或3个选自N，O或S的杂原子; R1是氢，低级烷基，卤素或低级烷氧基; R2是氢或低级烷基; 或R 3为氢，低级烷基，被羟基取代的低级烷基，环烷基，氧杂环丁烷-3-基，吡啶基，咪唑基，吡唑基，嘧啶基，该环可任选被低级烷基取代，或为 - （CH 2）3 -S（O） 2-环丙基; X是CH或N; n为1或2; 以及其药学上可接受的盐与外消旋混合物或其相应的对映异构体和/或其光学异构体和/或立体异构体一起用于治疗某些中性神经系统疾病，其为正（精神病）和阴性精神分裂症，药物滥用，酒精和药物成瘾，强迫症，认知障碍，双相情感障碍，情绪障碍，重症抑郁症，耐药性抑郁症，焦虑症，阿尔茨海默病，孤独症，帕金森病，慢性疼痛，边缘人格障碍，睡眠障碍，慢性疲劳综合征，僵硬，关节炎中的抗炎作用和平衡问题。

10. 发明公开

EP3010914A1 INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES 有权
标题翻译：二氢吲哚-2-酮或吡咯并吡啶/嘧啶-2-酮衍生物
公开(公告)号：EP3010914A1
公开(公告)日：2016-04-27
申请号：EP14729920.0
申请日：2014-06-16
申请人： F. Hoffmann-La Roche AG
发明人： BRUNNER, Daniela , HILPERT, Hans , KOLCZEWSKI, Sabine , LIMBERG, Anja , MALBERG, Jessica , PRINSSEN, Eric , RIEMER, Claus , SHANKAR, Bavani G. , STOLL, Theodor
IPC分类号： C07D405/14 , C07D413/14 , C07D401/04 , C07D403/04 , C07D413/04 , C07H19/044 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , A61P25/00 , A61K31/44 , A61K31/4409 , A61K31/4406 , A61K31/4402
CPC分类号： A61K31/4439 , A61K31/19 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/437 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61K31/7064 , A61K45/06 , C07C53/06 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04 , C07H19/044
摘要： The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R
1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF
3 , (CH
2 )
o -lower alkoxy, cycloalkyl optionally substituted by CF
3 , or heterocycloalkyl optionally substituted by lower alkyl; R
2 is hydrogen, lower alkyl, (CH
2 )
o -cycloalkyl, (CH
2 )
o -O-cycloalkyl, (CH
2 )
o -lower alkoxy, CH
2 )
o -lower alkoxy substituted by halogen, (CH
2 )
o -heterocycloalkyl optionally substituted by lower alkyl, (CH
2 )
o -S(O)
2 -cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH
2 )
o -S(O)
2 -lower alkyl, lower alkyl substituted by halogen or CH
2 CH(OH)CF
3 ; R
3 is halogen or lower alkyl; X is CH or N; X
1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

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