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1. 发明申请

US20050113361A1 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US20050113361A1
公开(公告)日：2005-05-26
申请号：US11025288
申请日：2004-12-29
申请人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/10 , A61P31/12 , A61P43/00 , C07D209/42 , C07D211/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04 , C07D498/04 , C07D43/02
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a nitrogen atom, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I）中，其中相邻的R 1，R 2，R 3， R 4和R 4各自为羟基，其余各为氢原子，R 5和R 6与它们之间的氮一起形成饱和的或被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4烷基）取代的不饱和的4-6元杂环， / C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或任选在芳环上被取代的苯甲酰基一个或多个卤素原子，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 - N是NH-，Y是氮原子，或其与酸或碱形成的药学上可接受的盐。

2. 发明申请

US20050113360A1 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US20050113360A1
公开(公告)日：2005-05-26
申请号：US11024638
申请日：2004-12-28
申请人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/10 , A61P31/12 , A61P43/00 , C07D209/42 , C07D211/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04 , C07D498/04 , A61K31/423 , C07D491/02
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4 groups form an oxo-oxazolidine ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I），其中相邻的R 1，R 2，R 3， R 4和R 4组合形成与吲哚核的苯环稠合的氧代 - 恶唑烷环，另外两个R 1，R 2， >，R 3和R 4基团是氢原子，R 5和R 6以及R 6之间的氮在它们形成饱和或不饱和的4-6元杂环，其被苯氧基，苯基 - （C 1 -C 4 -C 4烷基），苯基 - （C 1 -C 6）苯氧基 - （C 1 -C 4烷基）或苯甲酰基，任选取代的（C 1 -C 4）烷氧基），苯氧基 - （C 1 -C 4烷基）在一个或多个卤素原子的芳环上，氰基或羟基，C 1 -C 4烷基或C 1 -C 3 > 4个烷氧基，X是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

3. 发明申请

US20050113359A1 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US20050113359A1
公开(公告)日：2005-05-26
申请号：US11024637
申请日：2004-12-28
申请人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/10 , A61P31/12 , A61P43/00 , C07D209/42 , C07D211/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04 , C07D498/04 , C07D43/02
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I）中，其中相邻的R 1，R 2，R 3， R 4和R 4各自为羟基，其余各为氢原子，R 5和R 6与它们之间的氮一起形成饱和的或不饱和的4-6元杂环，其被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4烷基） / C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或任选在芳环上被取代的苯甲酰基一个或多个卤素原子，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 - N是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

4. 发明授权

US07378431B2 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US07378431B2
公开(公告)日：2008-05-27
申请号：US11025288
申请日：2004-12-29
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a nitrogen atom, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I）中，其中相邻的R 1，R 2，R 3， R 4和R 4各自为羟基，其余各为氢原子，R 5和R 6与它们之间的氮一起形成饱和的或被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4烷基）取代的不饱和的4-6元杂环， / C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或任选在芳环上被取代的苯甲酰基一个或多个卤素原子，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 - N是NH-，Y是氮原子，或其与酸或碱形成的药学上可接受的盐。

5. 发明授权

US07365083B2 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US07365083B2
公开(公告)日：2008-04-29
申请号：US11024638
申请日：2004-12-28
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4 groups form an oxo-oxazolidine ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I）中，其中相邻的R 1，R 2，R 3， R 4和R 4组合形成与吲哚核的苯环稠合的氧代 - 恶唑烷环，另外两个R 1，R 2， >，R 3和R 4基团是氢原子，R 5和R 6以及R 6之间的氮在它们形成饱和或不饱和的4-6元杂环，其被苯氧基，苯基 - （C 1 -C 4 -C 4烷基），苯基 - （C 1 -C 6）苯氧基 - （C 1 -C 4烷基）或苯甲酰基，任选取代的（C 1 -C 4）烷氧基），苯氧基 - （C 1 -C 4烷基）在一个或多个卤素原子的芳环上，氰基或羟基，C 1 -C 4烷基或C 1 -C 3 > 4个烷氧基，X是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

6. 发明授权

US06919355B2 Amide derivatives as NMDA receptor antagonists 失效
公开(公告)号：US06919355B2
公开(公告)日：2005-07-19
申请号：US10412977
申请日：2003-04-11
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/10 , A61P31/12 , A61P43/00 , C07D209/42 , C07D211/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04 , C07D498/04
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： New Formula (I) compounds are disclosed having NR2B selective NMDA receptor antagonist activity: wherein one of the neighboring R1, R2, R3 and R4 groups is OH or NH2 and the others are each hydrogen , or two of the neighboring R1, R2 R3 and R4 groups in given case together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups forms a 5-6 membered homo- or heterocyclic ring, preferably pyrrole, pyrazole, imidazole, oxazole, oxo-oxazolidine, or 3-oxo-1,4-oxazine ring, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by hydroxy group, and/or in given case phenyl or phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), anilino, phenyl-(C1-C4 alkylamino), [phenyl-(C1-C4 alkyl)]-amino, benzoyl, hydroxy-diphenylmethyl, C1-C4 alkoxycarbonyl-phenoxymethyl or benzhydrylidene group, optionally substituted on the aromatic ring by one or more halogen atom, cyano or hydroxy group, C1-C4 alkyl or C1-C4 alkoxy group, X is independently oxygen, —NH— or a CH2 group, Y is independently a nitrogen atom or a —CH— group, and the salts thereof formed with acids and bases.

7. 发明授权

US07375116B2 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US07375116B2
公开(公告)日：2008-05-20
申请号：US11025287
申请日：2004-12-29
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：公开了具有NR2B选择性NMDA受体拮抗剂活性的化合物，其中相邻的R 1，R 2，R 3， R 4和R 4组合形成与吲哚核的苯环稠合的咪唑环，另外两个R 1，R 2， R 3和R 4基团是氢原子，R 5和R 6和它们之间的氮原子一起形成被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4）烷基取代的饱和或不饱和的4-6元杂环， C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或苯甲酰基，任选在一个或多个卤素原子的芳香环，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 烷氧基，X是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

8. 发明授权

US07361670B2 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US07361670B2
公开(公告)日：2008-04-22
申请号：US11024637
申请日：2004-12-28
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I）中，其中相邻的R 1，R 2，R 3， R 4和R 4各自为羟基，其余各为氢原子，R 5和R 6与它们之间的氮一起形成饱和的或被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4烷基）取代的不饱和的4-6元杂环， / C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或任选在芳环上被取代的苯甲酰基一个或多个卤素原子，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 - N是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

9. 发明申请

US20050159451A1 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US20050159451A1
公开(公告)日：2005-07-21
申请号：US11025287
申请日：2004-12-29
申请人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , Gyorgy Domany , Istvan Borza , Gizella Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/10 , A61P31/12 , A61P43/00 , C07D209/42 , C07D211/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04 , C07D498/04
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：公开了具有NR2B选择性NMDA受体拮抗剂活性的化合物，其中相邻的R 1，R 2，R 3， R 4和R 4组合形成与吲哚核的苯环稠合的咪唑环，另外两个R 1，R 2， R 3和R 4基团是氢原子，R 5和R 6和它们之间的氮原子一起形成被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4）烷基取代的饱和或不饱和的4-6元杂环， C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或苯甲酰基，任选在一个或多个卤素原子的芳香环，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 烷氧基，X是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

10. 发明申请

US20090170901A1 Benzoyl Urea Derivatives 审中-公开
公开(公告)号：US20090170901A1
公开(公告)日：2009-07-02
申请号：US11658788
申请日：2005-07-21
申请人： Istvan Borza , Gizella Bartané Szalai , Eva Bozo , Csilla Acsné Kiss , Csilla Horvath , Sandor Farkas , Jozsef Nagy , Sandor Kolok
发明人： Istvan Borza , Gizella Bartané Szalai , Eva Bozo , Csilla Acsné Kiss , Csilla Horvath , Sandor Farkas , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D211/60 , A61P25/00
CPC分类号： C07D295/215 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D401/12 , C07D413/12
摘要： The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C1-C4 alkylene, C2-C4 alkenylene, aminocarbonyl, —NH—, —N(alkyl)-, —CH2O—, —CH2S—, —CH(OH)—, —OCH2— group, wherein the meaning of alkyl is a C1-C4 alkyl group—, when the dotted bonds () represent simple C—C bonds then U is hydroxy group or hydrogen atom or when W is C1-C4 alkylene or C2-C4 alkenylene group, then one of the dotted bonds () can represent a further double C—C bond and in this case U means an electron pair, which participate in the double bond and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. Furthermore objects of the present invention are the pharmaceutical compositions containing new benzoyl urea derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.

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