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1. 发明申请

WO2006010966A1 NEW BENZOYL UREA DERIVATIVES 审中-公开
标题翻译：新的苯甲酸衍生物
公开(公告)号：WO2006010966A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000079
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , BORZA, István , BARTÁNÉ SZALAI, Gizella , BOZÓ, Éva , KISS, Csilla , HORVÁTH, Csilla , FARKAS, Sándor , NAGY, József , KOLOK, Sándor
发明人： BORZA, István , BARTÁNÉ SZALAI, Gizella , BOZÓ, Éva , KISS, Csilla , HORVÁTH, Csilla , FARKAS, Sándor , NAGY, József , KOLOK, Sándor
IPC分类号： C07D295/20
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, C 1 -C 4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C 1 -C 4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C 1 -C 4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C 1 -C 4 alkyl or C 1 -C 4 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 -CH 2 - 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-l,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C 1 -C 4 alkylene, C 2 -C 4 alkenylene, aminocarbonyl, -NH-, -N(alkyl)-, -CH 2 O-, -CH 2 S-, -CH(OH)-, -OCH 2 - group, wherein the meaning of alkyl is a C 1 -C 4 alkyl group -, when the dotted bonds ( --- ) represent simple C-C bonds then U is hydroxy group or hydrogen atom or when W is C 1 -C 4 alkylene or C 2 -C 4 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.
摘要翻译：式（I）的新的苯甲酰脲衍生物，其中X和Y的含义独立地是氢原子，羟基，苄氧基，氨基，硝基，C

2. 发明申请

WO2003010159A1 PIPERIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NMDA受体拮抗剂的哌啶衍生物
公开(公告)号：WO2003010159A1
公开(公告)日：2003-02-06
申请号：PCT/HU2002/000071
申请日：2002-07-23
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , DOMÁNY, György , HORVÁTH, Csilla , FARKAS, Sándor , BARTÁNÉ SZALAI, Gisella , NAGY, József , KOLOK, Sándor , KOVÁCSNÉ BOZÓ, Éva , BORZA, István , VÁGÓ, István , BIELIK, Attila , IGNÁCZNÉ SZENDREI, Györgyi , KESERÚ, György
发明人： DOMÁNY, György , HORVÁTH, Csilla , FARKAS, Sándor , BARTÁNÉ SZALAI, Gisella , NAGY, József , KOLOK, Sándor , KOVÁCSNÉ BOZÓ, Éva , BORZA, István , VÁGÓ, István , BIELIK, Attila , IGNÁCZNÉ SZENDREI, Györgyi , KESERÚ, György
IPC分类号： C07D401/12
CPC分类号： C07D211/14 , C07D211/16 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to new carboxylic acid amide derivatives of formula (I), wherein U, V, W, X, Y, Z, n and m are as defined as in Claim 1. A further object of the invention are the processes for producing of carboxylic acid amide compounds 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 compounds of formula (I) of the present invention as such or as medicament. The new carboxylic acid amide 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：本发明涉及式（I）的新的羧酸酰胺衍生物，其中U，V，W，X，Y，Z，n和m如权利要求1所定义。本发明的另一个目的是制备式（I）的羧酸酰胺化合物，以及含有这些化合物的药物的药物制造，以及用这些化合物处理的方法，这意味着对待治疗的哺乳动物施用包括人 - 有效量/ 本发明的式（I）化合物本身或作为药物。本发明式（I）的新羧酸酰胺衍生物是NMDA受体的高效和选择性拮抗剂，而且大部分化合物是NMDA受体NR2B亚型的选择性拮抗剂。

3. 发明申请

WO2006010967A1 KYNURENIC ACID AMIDE DERIVATIVES AS NR2B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NR2B受体拮抗剂的氨基酸酰胺衍生物
公开(公告)号：WO2006010967A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000080
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , NAGY, József , KOLOK, Sándor
发明人： BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , NAGY, József , KOLOK, Sándor
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The new kynurenic acid amide derivatives of formula (I): 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.
摘要翻译：式（I）的新的犬尿酸酰胺衍生物：和光学对映体，外消旋体及其盐是NMDA受体的高效和选择性拮抗剂，此外，大多数化合物是NMDA受体NR2B亚型的选择性拮抗剂。

4. 发明申请

WO2006010968A1 NEW ARYLOXY ACETIC ACID AMIDE DERIVATIVES 审中-公开
标题翻译：新ARYLOXY乙酸酰胺衍生物
公开(公告)号：WO2006010968A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000081
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , KESERÛ, György , VÁGÓ, István , FARKAS, Sándor , HORVÁTH, Csilla , BIELIK, Attila , BORZA, István , WÉBER, Csaba , KOLOK, Sándor , NAGY, József
发明人： KESERÛ, György , VÁGÓ, István , FARKAS, Sándor , HORVÁTH, Csilla , BIELIK, Attila , BORZA, István , WÉBER, Csaba , KOLOK, Sándor , NAGY, József
IPC分类号： C07C235/34 , C07D211/08 , C07D235/06 , C07D263/56 , A61K31/16 , A61K31/18 , A61K31/445 , A61K31/4184
CPC分类号： C07D211/22 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/52 , C07D211/58 , C07D211/70 , C07D401/12 , C07D413/12
摘要： The new aryloxy acetic acid amide derivatives of formula (I) where R 1 and R 2 are the same or different and can be hydrogen atom or C 1-4 alkanoylamido group optionally substituted by halogen atom or C 1-4 alkyl-sulfonylamido group or N'-( C 1-4 alkyl)-ureido group C 1-6 alkoxy-carbonyl-amido or di-( C 1-4 alkyl)-amino group with the proviso that only one of them can be hydrogen atom, or R 1 and R 2 form together a -NH-CO-NH-, -NH-N=CH- or -NH-CO-O- chain attached to two neighbouring carbon atoms of the benzyl group, R 3 and R 4 mean the same or different C 1-4 alkyl groups which are substituted by phenyl group, or R 3 and R 4 mean together a C 4-6 alkylene chain which can be interrupted optionally by a nitrogen atom and which can contain a C-C double bound and which C 4-6 alkylene chain can substituted by one or two substituents from the following hydroxy group, phenyl or phenoxy group optionally substituted by a C 1-4 alkyl or trifluoro methyl group, =CH-phenyl group which can be substituted by halogen atom or C 1-4 alkyl group, C 1-4 alkyl group optionally substituted by hydroxy groµp and one or two phenyl groups which can be substituted by halogen atom or C 1-4 alkyl group, C 1-4 alkyl amino group which is substituted by a phenyl or naphtyl group which can be substituted optionally by a halogen atom or a C 1-4 alkyl group, as well as their salts formed with organic or inorganic acids or bases and solvates of these compounds are functional antagonists of NMDA receptors, which target the NMDA receptors primarily via binding to the ifenprodil binding site. Furthermore objects of the present invention are the pharmaceutical compositions containing new aryloxy acetic acid amide 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.
摘要翻译：式（I）的新的芳氧基乙酸酰胺衍生物，其中R

5. 发明申请

WO2006010965A1 INDOLE-2 -CARBOXAMIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚-2-羧酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：WO2006010965A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000078
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , NAGY, József , KOLOK, Sándor
发明人： BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , NAGY, József , KOLOK, Sándor
IPC分类号： C07D209/42
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, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C 1 -C 4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C 1 -C 4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C 1 -C 4 alkyl, C 1 -C 4 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 -CH 2 - 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，C

6. 发明申请

WO2006010964A1 NEW 4-BENZYLIDENE-PIPERIDIN DERIVATIVES 审中-公开
标题翻译：新的4-苯并噻吩 - 哌啶衍生物
公开(公告)号：WO2006010964A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000077
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , GYERTYÁN, István , NAGY, József , KOLOK, Sándor , GALGÓCZY, Kornél , SÁGHY, Katalin
发明人： BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , GYERTYÁN, István , NAGY, József , KOLOK, Sándor , GALGÓCZY, Kornél , SÁGHY, Katalin
IPC分类号： C07D401/12
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。

7. 发明申请

WO2006010969A1 NEW HETEROCYCLIC CARBOXYLIC ACID AMIDE DERIVATIVES 审中-公开
标题翻译：新的杂环羧酸酰胺衍生物
公开(公告)号：WO2006010969A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000082
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , GYERTYÁN, István , NAGY, József , KOLOK, Sándor , GALGÓCZY, Kornél , SÁGHY, Katalin
发明人： BORZA, István , HORVÁTH, Csilla , FARKAS, Sándor , GYERTYÁN, István , NAGY, József , KOLOK, Sándor , GALGÓCZY, Kornél , SÁGHY, Katalin
IPC分类号： C07D401/06
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, C 1 -C 4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C 1 -C 4 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, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, cyano, trifluoromethyl, 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，C

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