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1. 发明授权

US6140336A Spiro[2H-1-benzopyran-2,4'-piperidine]-4(3H)-one derivatives, acid addition salts thereof and pharmaceutical compositions containing them 失效
标题翻译：螺[2H-1-苯并吡喃-2,4'-哌啶] -4（3H） - 酮衍生物，其酸加成盐和含有它们的药物组合物
公开(公告)号：US6140336A
公开(公告)日：2000-10-31
申请号：US973612
申请日：1998-02-12
申请人： Kalman Harsanyi , Istvan Szabadkai , Istvan Borza , Egon Karpati , Bela Kiss , Margit Pellionisz , Sandor Farkas , Csilla Horvath , Katalin Csomor , Erzsebet Lapis , Istvan Laszlowsky , Sandor Szabo , Agnes Kis-Varga , Judit Laszy , Aniko Gere
发明人： Kalman Harsanyi , Istvan Szabadkai , Istvan Borza , Egon Karpati , Bela Kiss , Margit Pellionisz , Sandor Farkas , Csilla Horvath , Katalin Csomor , Erzsebet Lapis , Istvan Laszlowsky , Sandor Szabo , Agnes Kis-Varga , Judit Laszy , Aniko Gere
IPC分类号： C07D491/107 , A61K31/438 , A61K31/445 , A61P25/28 , C07D491/10 , C07D487/10 , A61K31/44
CPC分类号： C07D491/10
摘要： The invention relates to novel spiro[2H-1-benzopyran-2,4'-piperidine]-4(3H)-one derivatives of formula (I), ##STR1## wherein R stands for halogen, nitro group or a straight or branched chain C.sub.1-6 alkyl group, and their acid addition salts, as well as their quaternary salts of formula (Ia) ##STR2## wherein R and R' are the same or different and are identical to the meaning of said (above) R or can mean also hydrogen; and Z represents one equivalent of an anion. The compounds of formulas (I) and (Ia) exert an improving effect on dementias of various pathological origin and accompanying symptoms thereof. Furthermore, the invention relates to a process for the preparation of compounds of formulas (I) and (Ia); to pharmaceutical compositions containing as active gents the above compounds of formulas (I) and (Ia); and to a method of treatment.
摘要翻译： PCT No.PCT / HU97 / 00012 Sec。 371日期1998年2月12日 102（e）日期1998年2月12日PCT 1997年4月3日PCT公布。公开号WO97 / 37630 日期：1997年10月16日本发明涉及式（I）的新的螺[2H-1-苯并吡喃-2,4'-哌啶] -4（3H） - 酮衍生物，其中R代表卤素，硝基或直链或支链C 1-6烷基，以及它们的酸加成盐，以及它们的式（Ia）的季盐，其中R和R'相同或不同并且与所述（上）R或C 也是氢; Z表示1当量的阴离子。式（I）和（Ia）的化合物对各种病理来源及其伴随症状的痴呆发挥改善作用。此外，本发明涉及制备式（I）和（Ia）化合物的方法; 包含上述式（I）和（Ia）化合物作为活性成分的药物组合物; 以及一种治疗方法。

2. 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.

3. 发明申请

US20090048303A1 Indole-2-carboxamidine derivatives as nmda receptor antago 审中-公开
标题翻译：吲哚-2-甲脒衍生物作为nmda受体拮抗剂
公开(公告)号：US20090048303A1
公开(公告)日：2009-02-19
申请号：US11658787
申请日：2005-07-21
申请人： Istvan Borza , Csilla Horvath , Sandor Farkas , Jozsef Nagy , Sandor Kolok
发明人： Istvan Borza , Csilla Horvath , Sandor Farkas , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/4439 , C07D209/14 , A61K31/404 , C07D401/02
CPC分类号： C07D401/12 , C07D209/42 , C07D405/12
摘要： The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof. Further objects of the invention are the processes for producing indole-2-carboxamidine derivatives of formula (I), and the pharmaceutical manufacture of medicaments containing these compounds, as well as the process of treatments with these compounds, which means administering to a mammal to be treated—including human—effective amount/amounts of indole-2-carboxamidine derivatives of formula (I) of the present invention as such or as medicament. The new indole-2-carboxamidine derivatives of formula (I) of the present invention are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.
摘要翻译：因此，本发明首先涉及式（I）的新的吲哚-2-甲脒衍生物，其中X的含义是氢或卤素原子，C1-C4烷基，C1-C4烷氧基，三氟甲基，Y，V和Z独立地任选被卤素原子或卤原子取代的C 1 -C 4烷酰基氨基酰胺，任选被卤素原子或卤原子取代的C 1 -C 4烷酰胺基，三氟甲基，三氟甲氧基，C 1 -C 4烷基，C 1 -C 4 烷氧基或相邻的V和Z基团与一个或多个相同或不同的另外的杂原子和-CH-和/或-CH 2 - 基团可以形成任选取代的4-7元均 - 或杂环，优选苯，二氧戊环，A，B和C独立地是取代的碳原子或其中一个是氮原子，及其盐。本发明的另外的目的是制备式（I）的吲哚-2-甲脒衍生物和含有这些化合物的药物的药物制备方法以及用这些化合物处理的方法，这意味着给哺乳动物施用包括人的有效量/本发明式（I）的吲哚-2-甲脒衍生物的量或作为药物。本发明式（I）的新的吲哚-2-甲脒衍生物是NMDA受体的高效和选择性拮抗剂，而且大多数化合物是NMDA受体NR2B亚型的选择性拮抗剂。

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

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。

6. 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。

7. 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。

8. 发明申请

US20080312222A1 4-Benzyledene-Piperidin Derivatives 失效
标题翻译： 4-苄基 - 哌啶衍生物
公开(公告)号：US20080312222A1
公开(公告)日：2008-12-18
申请号：US11658789
申请日：2005-07-21
申请人： Istvan Borza , Csilla Horvath , Sandor Farkas , Istvan Gyertyan , Jozsef Nagy , Sandor Kolok , Kornel Galgoczy , Katalin Saghy
发明人： Istvan Borza , Csilla Horvath , Sandor Farkas , Istvan Gyertyan , Jozsef Nagy , Sandor Kolok , Kornel Galgoczy , Katalin Saghy
IPC分类号： A61K31/538 , A61K31/454 , C07D401/02 , A61P25/28 , A61P31/18 , C07D413/02
CPC分类号： C07D417/12 , C07D401/12 , C07D413/12
摘要： The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.
摘要翻译：本发明涉及用作NMDA的式（I）的新的4-亚苄基 - 哌啶衍生物，其在含有受体拮抗剂和镇痛药的特定NR2B亚单位中。

9. 发明申请

US20080300276A1 Heterocyclic Carboxylic Acide Amide Derivatives 审中-公开
标题翻译：杂环羧酸酰胺衍生物
公开(公告)号：US20080300276A1
公开(公告)日：2008-12-04
申请号：US11658486
申请日：2005-07-21
申请人： Istvan Borza , Csilla Horvath , Sandor Farkas , Istvan Gyertyan , Jozsef Nagy , Sandor Kolok , Kornel Galgoczy , Katalin Saghy
发明人： Istvan Borza , Csilla Horvath , Sandor Farkas , Istvan Gyertyan , Jozsef Nagy , Sandor Kolok , Kornel Galgoczy , Katalin Saghy
IPC分类号： A61K31/454 , C07D401/06 , A61P25/32 , A61P25/36 , A61P25/28
CPC分类号： C07D401/06
摘要： The invention relates to new heterocyclic carboxylic acid amide derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, arylsulfonamido groups, is —CH═ group or —N═ atom, Z is one or more hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluromethyl, trifluoromethoxy group and to the salts thereof, which are antagonists of NMDA receptor or are intermediates for preparing thereof.
摘要翻译：本发明涉及式（I）的新的杂环羧酸酰胺衍生物，其中X的含义是氢或卤素原子，羟基，氰基，任选被卤素原子或卤素原子取代的C 1 -C 4烷基磺酰氨基，任选地被C 1 -C 4烷酰胺基被卤素原子或卤原子取代的芳基磺酰胺基是-CH-基或-N-原子，Z是一个或多个氢或卤原子，C 1 -C 4烷基，C 1 -C 4烷氧基，氰基，三氟甲基，三氟甲氧基和其盐，它们是NMDA受体的拮抗剂或其制备的中间体。

10. 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。

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