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1. 发明申请

WO2021259815A1 AMIDOPYRIMIDONE DERIVATIVES 审中-公开
公开(公告)号：WO2021259815A1
公开(公告)日：2021-12-30
申请号：PCT/EP2021/066725
申请日：2021-06-21
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BELL, Andrew Simon , BESNARD, Jérémy , BRADLEY, Anthony Richard , GREEN, Luke , HAAP, Wolfgang , KOCER, Buelent , KUGLSTATTER, Andreas , LUCAS, Xavier , MATTEI, Patrizio , MAZUNIN, Dmitry , RATNI, Hasane , RIEMER, Claus , VAN HOORN, Willem Paul
IPC分类号： C07D239/95 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04 , C07D473/04 , A61P35/00 , A61K31/00
摘要： The present invention provides compounds of formula I or II: wherein X1, X3, R1, R2, R3, R4 and R5 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.

2. 发明申请

WO2014202493A1 INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES 审中-公开
标题翻译：吲哚-2-酮或吡咯并吡啶/吡啶-2-酮衍生物
公开(公告)号：WO2014202493A1
公开(公告)日：2014-12-24
申请号：PCT/EP2014/062491
申请日：2014-06-16
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
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.
摘要翻译：本发明涉及通式（I）的2-氧代-2,3-二氢 - 吲哚，其中Ar是含有一个，两个或三个选自N，S或O的杂原子的杂芳基; R 1是氢，低级烷基，卤素，氨基，二甲基氨基，氰基，被卤素取代的低级烷基，被羟基取代的低级烷基，CH（OH）CF 3，（CH 2）O-低级烷氧基，任选被CF 3取代的环烷基或任选地被低级烷基取代; R2是氢，低级烷基，（CH2）O-环烷基，（CH2）O-环烷基，（CH2）O-低级烷氧基，CH2）被卤素取代的-O-低级烷氧基，任选被低级烷基取代的（CH 2），（CH 2）oS（O）2-环烷基，被一个或两个羟基取代的低级烷基，被一个或两个低级烷氧基取代的低级烷基，（CH 2）o S（O）2-低级烷基，被卤素或CH 2 CH （OH）CF 3; R3是卤素或低级烷基; X是CH或N; X1是CH或N; n为1或2; o为0,1,2或3; m为0,1或2; 虚线是不是一个债券; 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/或光学异构体和/或立体异构体。该化合物可用于治疗某些中性神经系统疾病，其为阳性（精神病）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，边界线人格障碍，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。

3. 发明申请

WO2021259831A1 SULFONE DERIVATIVES 审中-公开
公开(公告)号：WO2021259831A1
公开(公告)日：2021-12-30
申请号：PCT/EP2021/066767
申请日：2021-06-21
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BELL, Andrew, Simon , BESNARD, Jérémy , BRADLEY, Anthony, Richard , GREEN, Luke , HAAP, Wolfgang , KOCER, Buelent , KUGLSTATTER, Andreas , LUCAS, Xavier , MATTEI, Patrizio , MAZUNIN, Dmitry , RIEMER, Claus , VAN HOORN, Willem Paul
IPC分类号： C07D231/56 , C07D487/04 , A61P35/00 , A61K31/416
摘要： The present invention provides compounds of formula (I) wherein X1, X2, X3, X4, R1, R1a, R1b, R2', R2", R3', R3", R6 and R7 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.

4. 发明申请

WO2022162034A1 PYRAZOLEAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2022162034A1
公开(公告)日：2022-08-04
申请号：PCT/EP2022/051823
申请日：2022-01-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BELL, Andrew Simon , BESNARD, Jérémy , BRADLEY, Anthony Richard , GREEN, Luke , HAAP, Wolfgang , KOCER, Buelent , KUGLSTATTER, Andreas , LUCAS, Xavier , MATTEI, Patrizio , MAZUNIN, Dmitry , RIEMER, Claus , VAN HOORN, Willem Paul
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61P35/00
摘要： The present invention provides compounds of formula I or II: (I) wherein X1, R1 and R2 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.

5. 发明申请

WO2022129259A1 NEW QUINAZOLINONE DERIVATIVES 审中-公开
公开(公告)号：WO2022129259A1
公开(公告)日：2022-06-23
申请号：PCT/EP2021/086049
申请日：2021-12-16
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , HEWINGS, David Stephen , HUNZIKER, Daniel , KRUMMENACHER, Daniela , PETTAZZONI, Piergiorgio Francesco Tommaso , RICKLIN, Fabienne , RIEMER, Claus , WICHMANN, Juergen
IPC分类号： C07D401/06 , C07D401/14 , C07D403/12 , C07D239/90 , C07D239/91 , A61P35/00 , A61K31/517
摘要： The invention relates to a compound of formula (I) wherein A, L, R1, R2, R3 and R4 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

6. 发明申请

WO2022129260A1 NEW ARYL-PYRIDO-PYRIMIDIN-ONE DERIVATIVES 审中-公开
公开(公告)号：WO2022129260A1
公开(公告)日：2022-06-23
申请号：PCT/EP2021/086050
申请日：2021-12-16
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , HEWINGS, David Stephen , HUNZIKER, Daniel , JUNG, Erik , PETTAZZONI, Piergiorgio Francesco Tommaso , RICKLIN, Fabienne , RIEMER, Claus , WICHMANN, Juergen
IPC分类号： C07D471/04 , A61P35/00 , A61K31/519
摘要： The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein n, R1, R2, R3, R4 and R5 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

7. 发明申请

WO2021255213A1 HETEROBIFUNCTIONAL COMPOUNDS AS DEGRADERS OF BRAF 审中-公开
公开(公告)号：WO2021255213A1
公开(公告)日：2021-12-23
申请号：PCT/EP2021/066526
申请日：2021-06-18
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC. , C4 THERAPEUTICS, INC.
发明人： DOLENTE, Cosimo , HEWINGS, David Stephen , HUNZIKER, Daniel , KUHN, Bernd , PETTAZZONI, Piergiorgio Francesco Tommaso , RICKLIN, Fabienne , RIEMER, Claus , WICHMANN, Juergen
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437
摘要： Present invention provides compounds that cause specifically the degradation of BRAF. The present compounds are useful for the treatment of various cancers.

8. 发明申请

WO2021255212A1 BRAF DEGRADERS 审中-公开
公开(公告)号：WO2021255212A1
公开(公告)日：2021-12-23
申请号：PCT/EP2021/066524
申请日：2021-06-18
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC. , C4 THERAPEUTICS, INC.
发明人： DOLENTE, Cosimo , DUPLESSIS, Martin , FITZGERALD, Mark, E. , GARZA, Victoria , GOOD, Andrew, Charles , HEWINGS, David, Stephen , HUNZIKER, Daniel , JACKSON, Katrina, L. , KUHN, Bernd , LIANG, Yanke , MOUSTAKIM, Moses , NASVESCHUK, Christopher, G. , O'SHEA, Morgan, Welzel , PETTAZZONI, Piergiorgio, Francesco, Tommaso , RICKLIN, Fabienne , RIEMER, Claus , VEITS, Gesine, Kerstin , WICHMANN, Juergen , YAP, Jeremy, L. , YU, Robert, T.
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： Present invention provides compounds that cause specifically the degradation of BRAF. The present compounds are useful for the treatment of various cancers.

9. 发明申请

WO2014040969A1 2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的2-氧代-2,3-二氢吲哚
公开(公告)号：WO2014040969A1
公开(公告)日：2014-03-20
申请号：PCT/EP2013/068668
申请日：2013-09-10
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BRUNNER, Daniela , MALBERG, Jessica , SHANKAR, Bavani G. , KOLCZEWSKI, Sabine , LIMBERG, Anja , PRINSSEN, Eric , RIEMER, Claus , STOLL, Theodor
IPC分类号： C07D403/12 , C07D401/14 , C07D401/12 , C07D471/04 , C07D209/34 , A61K31/44 , A61K31/506 , A61K31/4178 , A61K31/404 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D209/34 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein (N 1 ) is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; (N 2 ) is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R 1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R 1 may be the same or not; R 2 /R 2' are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C 3-6 -cycloalkyl ring; R 3 is lower alkyl, C 3-6 -cycloalkyl, CH 2 -C 3-6 -cycloalkyl, C 3-6 -cycloalkyl wherein one ring-carbon atom is replaced by -O-, (CH 2 ) 3 -O-C 3-6 -cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH 2 ) 3 -S(O) 2 -C 3-6 -cycloalkyl or (CH 2 ) 2 -S(O) 2 -lower alkyl; R 4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R 4 may be the same 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.
摘要翻译：本发明涉及通式（I）的2-氧代-2,3-二氢 - 吲哚，其中（N1）是苯基或杂芳基，选自吡啶基，嘧啶基，咪唑基，异恶唑基或吡唑基; （N 2）是苯基或吡啶基，其中吡啶基中的N原子可以在所有的自由位上; R1是氢，低级烷基，被卤素取代的低级烷基，低级烷氧基或卤素; n为1或2; 如果n为2，则R1可以相同或不相同; R2 / R2'彼此独立地为低级烷基，或与它们所连接的碳原子一起形成C 3-6 - 环烷基环; R3是低级烷基，C3-6-环烷基，CH2-C3-6环烷基，C3-6-环烷基，其中一个环 - 碳原子被-O - ，（CH2）3-O-C3-6-环烷基取代，被羟基取代的低级烷基，被卤素取代的低级烷基，（CH 2）3 -S（O）2 -C 3-6 - 环烷基或（CH 2）2 -S（O） R4是氢，卤素或低级烷基; m为1或2; 如果m为2，则R4可以相同或不相同; 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。

10. 发明申请

WO2010086259A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK3受体拮抗剂的哌啶衍生物
公开(公告)号：WO2010086259A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050591
申请日：2010-01-19
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/454 , A61K31/4545 , A61P25/24 , A61P25/04 , A61P25/18 , A61P25/16 , A61P25/22
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compounds of formula (I) wherein Ar 1 is aryl or a six membered heteroaryl; Ar 2 is aryl or a six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, lower alkyl, phenyl, optionally substituted by halogen, or is a five membered heteroaryl, optionally substituted by lower alkyl, or is aryl optionally substituted by halogen; is a six membered heterocyclic group, wherein X is -N(SO 2 CH 3 ); R 6 is hydrogen; Y is -N(R 7' )- R 7' is a 6-membered heteroaryl group, optionally substituted by cyano or C(O)-cycloalkyl, wherein the cycloalkyl group is optionally substituted by lower alkyl, n is 1; m is 1; o is1; p is 1; s is 0; t is 1; u is 1; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonist for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）的化合物，其中Ar 1是芳基或6元杂芳基; Ar 2是芳基或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基; R4是氢，低级烷基，任选被卤素取代的苯基，或是任选被低级烷基取代的五元杂芳基，或者是被卤素任意取代的芳基; 是六元杂环基，其中X是-N（SO 2 CH 3）; R6是氢; Y是-N（R 7'）-R 7'是任选被氰基或C（O） - 环烷基取代的6元杂芳基，其中环烷基任选被低级烷基取代，n是1; m为1; o is1; p为1; s是0; t为1; 你是1 或其药物活性盐，外消旋混合物，对映体，旋光异构体或其互变异构形式。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

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