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1. 发明专利

JP2013028624A PYRIDINE AND PYRIDINE DERIVATIVE AS mGluR2 ANTAGONIST 有权
标题翻译：吡啶和吡啶衍生物作为mGluR2拮抗剂
公开(公告)号：JP2013028624A
公开(公告)日：2013-02-07
申请号：JP2012203498
申请日：2012-09-14
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： GATTI MCARTHUR SILVIA , GOETSCHI ERWIN , WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
IPC分类号： C07D213/34 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P25/18 , A61P25/20 , A61P25/28 , A61P35/00 , A61P43/00 , C07D213/53 , C07D213/57 , C07D213/71 , C07D213/73 , C07D239/26 , C07D239/42 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14
CPC分类号： C07D239/30 , C07D213/61 , C07D213/64 , C07D213/79 , C07D213/81 , C07D213/84 , C07D239/28 , C07D239/34 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F5/025
摘要： PROBLEM TO BE SOLVED: To provide compounds to be used for treatment or prevention of psychosis, schizophrenia, Alzheimer's disease, cognitive disorders, memory deficits, colon cancer, sleep disturbance, circadian rhythm disorders, and glial tumors.SOLUTION: The compounds are represented by formula (I). In the formula: one of X and Y is N while the other is CH, or both X and Y are N; A is aryl or 5 or 6 membered heteroaryl each of which is optionally substituted by 1C-6C alkyl; B is H, cyano or, is optionally substituted aryl or optionally substituted 5 or 6 membered heteroaryl.
摘要翻译：待解决的问题：提供用于治疗或预防精神病，精神分裂症，阿尔茨海默病，认知障碍，记忆缺陷，结肠癌，睡眠障碍，昼夜节律障碍和胶质瘤的化合物。化合物由式（I）表示。在下式中：X和Y之一是N，而另一个是CH，或者X和Y都是N; A是芳基或5或6元杂芳基，其各自任选被1C-6C烷基取代; B是H，氰基或是任选取代的芳基或任选取代的5或6元杂芳基。版权所有（C）2013，JPO＆INPIT

2. 发明专利

JP2000086597A 2-AMINO-BICYCLO[3.1.0]HEXANE-2,6-DICARBOXYLIC ACID DERIVATIVES AND THEIR PRODUCTION 失效
公开(公告)号：JP2000086597A
公开(公告)日：2000-03-28
申请号：JP24416799
申请日：1999-08-31
申请人： HOFFMANN LA ROCHE
发明人： ADAM GEO , HUGUENIN-VIRCHAUX PHILIPPE N , MUTEL VINCENT , STADLER HEINZ , WOLTERING THOMAS JOHANNES
IPC分类号： A61K31/00 , A61K31/196 , A61P25/00 , A61P25/18 , C07C227/16 , C07C227/32 , C07C229/50 , C07C247/14
摘要： PROBLEM TO BE SOLVED: To readily obtain the subject compound useful as a ligand for a metabotropic glutamate receptor of group II in high yield in a diastereomeric and enantiomeric purity by using a specific intermediate. SOLUTION: The carbonyl group of a compound of formula I (R" and R"' are each benzyl or a lower alkyl) is reduced to a hydroxyl group to give a compound or formula II or III. If desired, the compound of formula II is alkylated, alkenylated or benzylated, the azido group is reduced to an amino group and the ester group is hydrolysed. The double bond of the obtained compound is hydrogenated using, if desired, a tritium gas to give a compound of formula IV (R1 is hydroxyl, a lower alkoxy, a lower alkenyloxy, benzyloxy, H or the like; R11 is H, a deuterium atom, a tritium atom or the like; R2 is H or the like). As a result, a compound useful for suppression of a neurological symptom and a psychiatric disease is provided.

3. 发明专利

JPH1171380A 5H-THIAZOLO(3,2-A)PYRIMIDINE DERIVATIVE 失效
公开(公告)号：JPH1171380A
公开(公告)日：1999-03-16
申请号：JP19936398
申请日：1998-07-15
申请人： HOFFMANN LA ROCHE
发明人： ADAM GEO , KOLCZEWSKI SABINE , MUTEL VINCENT , WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
IPC分类号： C07D239/22 , A61K31/00 , A61K31/505 , A61K31/519 , A61P1/08 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P27/02 , A61P43/00 , C07D239/00 , C07D239/40 , C07D277/00 , C07D513/04
摘要： PROBLEM TO BE SOLVED: To obtain the subject novel compound that is useful as a therapeutic and preventive agent for cerebral function restriction caused by transplantation, head injury, cardiac arrest, acute and/or chronic neurological disorders as an antagonist of metabotropic glutamate receptor and/or as an agonist. SOLUTION: This compound is represented by formula I (R is H, a lower alkoxy or the like; R is a lower alkyl, a lower alkoxy or the like; R -R are each H, a halogen or the like) or its salt, typically (RS)-2-(2,6- dichlorophenyl)-5-(2-methoxyphenyl)-7-methyl-5H-thiazolo [3,2- a]pyrimidine-6-carboxylic 2-dimethylaminoethyl ester. This compound is prepared by reaction of a compound of formula II with α-bromo-acetaldehyde, when necessary, in addition, converting the compound of formula I to its salt. The intermediate compound of formula II is novel and is prepared, for example, by reaction of 4-metoxybenzaldehyde with acetylacetone and thiourea.

4. 发明申请

WO2005040171A8 PYRAZOLO AND IMIDAZO-PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡唑并咪唑并吡啶衍生物
公开(公告)号：WO2005040171A8
公开(公告)日：2006-08-03
申请号：PCT/EP2004010807
申请日：2004-09-27
申请人： HOFFMANN LA ROCHE , WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
发明人： WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula (I) wherein A, D, E, L, M, Q, R 1 , R 2 and R 3 are as defined in the description and claims and to processes for their preparation, pharmaceutical compositions containing said derivatives and their use in the prevention and treatment of diseases.
摘要翻译：本发明涉及式（I）的新型吡唑并咪唑并嘧啶衍生物，其中A，D，E，L，M，Q，R 1，R 2，和R 3如在说明书和权利要求书及其制备方法中所定义，含有所述衍生物的药物组合物及其在预防和治疗疾病中的用途。

5. 发明申请

WO0129011A3 BENZODIAZEPINE DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为代谢型谷氨酸受体拮抗剂的苯二甲酸衍生物
公开(公告)号：WO0129011A3
公开(公告)日：2001-11-08
申请号：PCT/EP0009553
申请日：2000-09-29
申请人： HOFFMANN LA ROCHE
发明人： ADAM GEO , ALANINE ALEXANDER , GOETSCHI ERWIN , MUTEL VINCENT , WOLTERING THOMAS JOHANNES
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/08 , A61P3/08 , A61P9/00 , A61P9/10 , A61P13/00 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P43/00 , C07D243/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14 , C07D491/056 , C07D491/113 , C07F7/10
CPC分类号： C07D243/12
摘要： The present invention relates to compounds of general formula (I) wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R is halogen or phenyl which is optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, or cyano; In case X is an ethynediyl group, R is phenyl, optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy or halo-lower alkoxy; R is a 5 or 6 membered aryl or heteroaryl which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.
摘要翻译：本发明涉及通式（I）的化合物，其中X为单键或亚乙二基，其中，在X为单键的情况下，R 1为卤素或任选被卤素取代的苯基，低级烷基，卤代低级烷基，低级烷氧基，卤代低级烷氧基或氰基; 在X为乙炔二基的情况下，R 1为苯基，任选被卤素，低级烷基，卤代低级烷基，低级环烷基，低级烷氧基或卤代低级烷氧基取代; R 3是任选被取代的5或6元芳基或杂芳基。根据本发明的化合物可用于治疗或预防急性和/或慢性神经障碍，例如精神病，精神分裂症，阿尔茨海默病，认知障碍和记忆缺陷。

6. 发明申请

WO0129012A3 BENZODIAZEPINE DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为代谢谷氨酸受体拮抗剂的苯二氮卓衍生物
公开(公告)号：WO0129012A3
公开(公告)日：2001-11-08
申请号：PCT/EP0009554
申请日：2000-09-29
申请人： HOFFMANN LA ROCHE
发明人： ADAM GEO , ALANINE ALEXANDER , GOETSCHI ERWIN , MUTEL VINCENT , WOLTERING THOMAS JOHANNES
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/08 , A61P3/08 , A61P9/08 , A61P13/02 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/02 , A61P43/00 , C07D243/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/10 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/08 , C07D409/14 , C07D413/10 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/14 , C07F7/10
CPC分类号： C07D401/04 , C07D243/12 , C07D403/10 , C07D405/06 , C07D413/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to compounds of general formula (I) wherein R is phenyl; pyridine; thiophenyl or thiazolyl, which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.
摘要翻译：本发明涉及通式（I）的化合物，其中R 3是苯基; 吡啶; 噻吩基或噻唑基，其任选被取代。根据本发明的化合物可用于治疗或预防急性和/或慢性神经障碍，例如精神病，精神分裂症，阿尔茨海默病，认知障碍和记忆缺陷。

7. 发明申请

WO9825930A2 USE OF BI- AND TRICYCLIC PYRIDONE DERIVATIVES AGAINST ALZHEIMER'S DISEASE 审中-公开
标题翻译：使用双嘧嘧啶衍生物对抗阿尔茨海默病
公开(公告)号：WO9825930A2
公开(公告)日：1998-06-18
申请号：PCT/EP9706865
申请日：1997-12-09
申请人： HOFFMANN LA ROCHE
发明人： HUBER TROTTMANN GERDA , JAKOB-ROETNE ROLAND , KOLCZEWSKI SABINE , NORCROSS ROGER DAVID , WOLTERING THOMAS JOHANNES
IPC分类号： C07D455/02 , C07D455/06 , C07D471/14 , C07D495/14 , C07D495/00
CPC分类号： C07D471/14 , C07D455/02 , C07D455/06 , C07D495/14
摘要： The invention is concerned with the use of bi- and tricyclic pyridone compounds of general formula (I) and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of beta -amyloid peptide activity, especially for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及使用通式（I）的二环和三环吡啶酮化合物及其药学上可接受的盐来生产用于预防或治疗与β-淀粉样蛋白肽活性的抑制相关的疾病的药物，特别是用于治疗阿尔茨海默病。

8. 发明专利

BRPI0908919A2 Derivados de 2-aminoquinolina como antagonistas do receptor 5-ht5a 未知
公开(公告)号：BRPI0908919A2
公开(公告)日：2015-07-28
申请号：BRPI0908919
申请日：2009-03-03
申请人： HOFFMANN LA ROCHE
发明人： KOLCZEWSKI SABINE , RIEMER CLAUS , ROCHE OLIVIER , STEWARD LUCINDA , WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
IPC分类号： A61K31/4709 , A61P3/06 , A61P25/00 , C07D215/38 , C07D405/12

9. 发明专利

ES2529457T3 Derivados de piridinas y pirimidinas como agonistas de mGluR2 未知
公开(公告)号：ES2529457T3
公开(公告)日：2015-02-20
申请号：ES07727038
申请日：2007-03-19
申请人： HOFFMANN LA ROCHE
发明人： GATTI MCARTHUR SILVIA , GOETSCHI ERWIN , WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
IPC分类号： C07D213/34 , A61K31/444 , A61K31/506 , A61P25/00 , C07D233/96 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/04 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要： Un compuesto de fórmula (I):**Fórmula** que es en la que el heteroarilo de 5 o 6 miembros es imidazolilo, [1,2,4]oxadiazolilo, pirrolilo, 1H-pirazolilo, piridinilo, [1,2,4] triazolilo, tiazolilo, pirimidinilo o tiofenilo, cada uno de los cuales opcionalmente sustituido con alquilo C1-6; B es un arilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido de 5 o 6 miembros, en el que los sustituyentes se seleccionan entre el grupo que consiste en: halo, nitro, alquilo C1-6 opcionalmente sustituido con hidroxi, NRaRb, en el que Ra y Rb son independientemente H, alquilo C1-6 o -(CO)-alquilo C1-6, -S-alquilo C1-6, -(SO2)-OH, -(SO2)-alquilo C1-6, -(SO2)-NRcRd, en el que Rc y Rd son independientemente: H, alquilo C1-6 opcionalmente sustituido con hidroxi, haloalquilo C1-6, alcoxi C1-6, -(CO)alquilo C1-6 opcionalmente sustituido con alcoxi C1-6, -(CH2CH2O)nCHRe, en el que Re es H o CH2OH y n es 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10, -(CH2)m-arilo, en el que m es 1 o 2 y el arilo está opcionalmente sustituido con halo o alcoxi C1-6, -(CH2)p-cicloalquilo C3-6, en el que p es 0 o 1, heteroalquilo de 5 o 6 miembros, -(SO2)-NRfRg, en el que Rf y Rg junto con el átomo de nitrógeno al que están unidos forman un anillo heterocicloalquilo de 4, 5 o 6 miembros que contiene opcionalmente un heteroátomo adicional seleccionado entre nitrógeno, oxígeno, azufre o un grupo SO2, en el que dicho anillo heterocicloalquilo de 4, 5 o 6 miembros está opcionalmente sustituido con: un sustituyente seleccionado entre el grupo que consiste en hidroxi, alquilo C1-6, alcoxi C1-6 que está opcionalmente sustituido con hidroxi, y un heteroariloxi de 5 o 6 miembros, NHSO2-alquilo C1-6, y NHSO2-NRhRi en el que Rh y Ri son independientemente H, alquilo C1-6, -(CO)O- alquilo C1-6, o Rh y Ri junto con el átomo de nitrógeno al que están unidos forman un anillo heterocicloalquilo de 4, 5 o 6 miembros que contiene opcionalmente un heteroátomo adicional seleccionado entre nitrógeno, oxígeno o azufre, en el que dicho anillo heterocicloalquilo de 4, 5 o 6 miembros está opcionalmente sustituido con alquilo C1-6; R1 es H, halógeno, alquilo C1-6 opcionalmente sustituid 5 o con hidroxi, alcoxi C1-6, haloalquilo C1-6, cicloalquilo C1-6; R2 es H, ciano, halógeno, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquilo C1-6 o cicloalquilo C3-6; R3 es halógeno, H, alcoxi C1-6, haloalquilo C1-6, alquilo C1-6, cicloalquilo C3-6, haloalcoxi C1-6, o es NRjRk en el que Rj y Rk se seleccionan independientemente entre el grupo que consiste en: H, cicloalquilo C3-8, arilo, heteroarilo que tiene de 5 a 12 átomos en el anillo y alquilo C1-6 que está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, hidroxi, cicloalquilo C3-8, arilo, heteroarilo que tiene de 5 a 12 átomos en el anillo y -NRlRm, en el que Rl y Rm se seleccionan independientemente entre el grupo que consiste en H y alquilo C1-6; o Rj y Rk pueden formar, junto con el átomo de nitrógeno al que están unidos, un grupo heterocíclico opcionalmente sustituido que comprende de 5 a 12 átomos, en el anillo que contiene opcionalmente un heteroátomo adicional seleccionado entre nitrógeno, oxígeno o azufre, en el que dicho grupo heteroarilo está opcionalmente sustituido con uno, dos, tres, cuatro o cinco sustituyentes que se seleccionan entre el grupo que consiste en halógeno, hidroxi, alquilo C1-6 y haloalquilo C1-6; o R2 y R3 juntos pueden formar un puente dioxo; R4 es H o halo; así como sales farmacéuticamente aceptables del mismo, excluyendo los siguientes compuestos de la fórmula (I): 6,6'-Dimetil-4,4'-difenil-[2,2']bipiridinilo, 6,6'-Dimetil-4,4'-di-p-tolil-[2,2']bipiridinilo, 4,4'-Difenil-[2,2']bipiridinilo, 4-Fenil-[2,2';6',2"]terpiridina, 4,4'-Di-p-tolil-[2,2']bipiridinilo, 6-Bromometil-6'-metil-4,4'-difenil-[2,2']bipiridinilo, 4,4'-Bis-(4-cloro-fenil)-6,6'-dimetil-[2,2']bipiridinilo, 4-Fenil-2-(4-piridin-2-il-tiazol-2-il)-piridina, 4,4'-Bis-(4-fluoro-fenil)-[2,2']bipiridinilo, 4,4'-Bis-(2,4-difluoro-fenil)-[2,2']bipiridinilo, 4,4'-Bis-(2,3,4-trifluoro-fenil)-[2,2']bipiridinilo, 4,4'-Bis-(4-cloro-fenil)-[2,2']bipiridinilo, 3-(4-fenil-2-piridil)-5-fenil-1,2,4-triazol, 4-p-tolil-[2,2';6',2"]terpiridina, y 4-((4-metoxifenil)-2,2':6',2"]-terpiridina.

10. 发明专利

DK2001849T3 PYRIDIN- OG PYRIMIDINDERIVATER SOM MGLUR2-ANTAGONISTER 未知
公开(公告)号：DK2001849T3
公开(公告)日：2014-12-15
申请号：DK07727038
申请日：2007-03-19
申请人： HOFFMANN LA ROCHE
发明人： GATTI MCARTHUR SILVIA , GOETSCHI ERWIN , WICHMANN JUERGEN , WOLTERING THOMAS JOHANNES
IPC分类号： C07D213/34 , A61K31/444 , A61K31/506 , A61P25/00 , C07D233/96 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/04 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14

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