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1. 发明申请

WO2012153154A1 OXETANE SUBSTITUTED THIENO PYRIMIDINONES 审中-公开
标题翻译： OXETANE取代三硝基吡啶酮
公开(公告)号：WO2012153154A1
公开(公告)日：2012-11-15
申请号：PCT/HU2012/000032
申请日：2012-05-04
申请人： RICHTER GEDEON NYRT. , ÉLES, János , BORZA, István , BEKE, Gyula , BOROS, András , SZALAI, Krisztina
发明人： ÉLES, János , BORZA, István , BEKE, Gyula , BOROS, András , SZALAI, Krisztina
IPC分类号： C07D495/04 , A61K31/519 , A61P3/00
CPC分类号： C07D495/04
摘要： The present invention provides a compound of Formula (I) or pharmaceutically acceptable salt thereof wherein is selected from the group consisting of unsubstituted aryl and heteroaryl groups and aryl and heteroaryl groups substituted with Q; Q represents fluoro, chloro, bromo, C 1-6 straight or branched alkyl, alkylthio, cyano, trihaloalkyl, trihaloalkoxy; Y represents CH or N; R is selected from a group consisting of hydrogen, C 1-6 straight or branched alkyl, C 1-6 alkoxy, trihaloalkyl, trihaloalkoxy, amino, alkylamino, dialkylamino, hydroxy cyano, acetyl, alkylthio and halo; k is independently an integer 2 or 3; n is an integer from 0 to 2 and m is an integer from 1 to 4 provided that sum of the integers m and n is equal to an integer from 2 to 4. The invention also relates to pharmaceutical compositions containing them, to processes for their preparation, new intermediate compounds thereof and to their use in the treatment and/or prophylaxis of a melanin concentrating hormone receptor 1 and optionally H3 receptor related disease or condition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中选自未取代的芳基和杂芳基，被Q取代的芳基和杂芳基; Q表示氟，氯，溴，C 1-6直链或支链烷基，烷硫基，氰基，三卤代烷基，三卤代烷氧基; Y表示CH或N; R选自氢，C 1-6直链或支链烷基，C 1-6烷氧基，三卤代烷基，三卤代烷氧基，氨基，烷基氨基，二烷基氨基，羟基氰基，乙酰基，烷硫基和卤素; k独立地为2或3的整数; n是0至2的整数，m是1至4的整数，条件是整数m和n的总和等于2至4的整数。本发明还涉及含有它们的药物组合物，用于其制备，其新的中间体化合物及其在治疗和/或预防黑色素浓缩激素受体1和任选的H3受体相关疾病或病症中的用途。

2. 发明申请

WO2012059776A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO2012059776A1
公开(公告)日：2012-05-10
申请号：PCT/HU2011/000104
申请日：2011-11-04
申请人： RICHTER GEDEON NYRT. , BEKE, Gyula , BÉNYEI, Gyula Attila , BORZA, István , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , PAPP, Andrea , VÁGÓ, István , VASTAG, Mónika
发明人： BEKE, Gyula , BÉNYEI, Gyula Attila , BORZA, István , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , PAPP, Andrea , VÁGÓ, István , VASTAG, Mónika
IPC分类号： C07D403/04 , C07D403/14 , C07D413/12 , A61K31/404 , A61P29/00
CPC分类号： C07D413/14 , C07D209/42 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12
摘要： The present invention relates to the indole derivatives of formula (I), wherein R 1 - R 6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及式（I）的吲哚衍生物，其中R 1 -R 6和X在权利要求书中定义，光学对映体或外消旋体和/或其盐是缓激肽B1的选择性拮抗剂以制备这些化合物，药理学含有它们的组合物及其在治疗中的用途或预防疼痛和炎症状况。

3. 发明申请

WO2018167630A1 PHARMACOLOGICALLY ACTIVE ALICYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2018167630A1
公开(公告)日：2018-09-20
申请号：PCT/IB2018/051599
申请日：2018-03-12
申请人： RICHTER GEDEON NYRT.
发明人： BORZA, István , ROMÁN, Viktor , ÉLES, János , HADADY, Zsuzsa
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00 , A61P25/00
摘要： The present invention relates to new pyrazolo[l,5-a]pyrimidine derivatives of formula (I) or pharmaceutical ly acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.

4. 发明申请

WO2022029666A1 PHARMACOLOGICALLY ACTIVE HETEROCYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2022029666A1
公开(公告)日：2022-02-10
申请号：PCT/IB2021/057180
申请日：2021-08-05
申请人： RICHTER GEDEON NYRT.
发明人： BORZA, István , ÉLES, János , ROMÁN, Viktor , PETRÓ, József Levente , GEGÖ, Csaba Lehel , BÉNYEI, Gyula Attila
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P19/00
摘要： The invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds and key intermediates used in the process. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.

5. 发明申请

WO2018167629A1 PHARMACOLOGICALLY ACTIVE ARYL-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2018167629A1
公开(公告)日：2018-09-20
申请号：PCT/IB2018/051598
申请日：2018-03-12
申请人： RICHTER GEDEON NYRT.
发明人： BORZA, István , ROMÁN, Viktor , ÉLES, János , HADADY, Zsuzsa , HUSZÁR, József
IPC分类号： C07D487/04 , A61P25/00 , A61P19/00 , A61K31/519
摘要： The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABA B receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABA B receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.

6. 发明申请

WO2013076646A1 A NEW DIAZA-BENZOFLUORANTHENE DERIVATIVE AS DRUG 审中-公开
标题翻译：新的DIAZA-BENZOFLUORANTHENE衍生物作为药物
公开(公告)号：WO2013076646A1
公开(公告)日：2013-05-30
申请号：PCT/IB2012/056561
申请日：2012-11-20
申请人： RICHTER GEDEON NYRT.
发明人： ÉLES, János , BORZA, István , TIHANYI, Károly , HORVÁTH, Csilla Mária , BALÁZS, Ottília , VASTAG, Mónika , LASZY, Judit , GYERTYÁN, István , KOCSIS, Pál
IPC分类号： C07D461/00 , A61K31/4375 , A61P25/00
CPC分类号： C07D461/00
摘要： The present invention relates to a new 16-tetrazolyl-eburnamenine of formula (I) or pharmaceutically acceptable salt thereof and/or hydrates and/or solvates thereof. The invention also relates to the pharmaceutical compositions containing the compound of formula (I) or hydrates or solvates thereof as active ingredient. The invention also relates to the synthesis of compounds of formula (I), and the chemical and pharmaceutical manufacture of medicaments containing these compounds, as well as the methods of treatment of mammals - including human - with these compounds. There is still further provided methods for the treatment of neurological, neurodegenerative and psychiatric diseases or conditions as well as comprising the step of administering to human, in need of such treatment and/or prophylaxis a pharmaceutical composition comprising a therapeutically effective amount of compound of formula (I) or pharmaceutically acceptable salts thereof alone or together with at least one and a pharmaceutically acceptable carrier and/or diluent.
摘要翻译：本发明涉及式（I）的新的16-四唑基 - 本白他宁或其药学上可接受的盐和/或其水合物和/或溶剂合物。本发明还涉及含有式（I）化合物或其水合物或溶剂合物作为活性成分的药物组合物。本发明还涉及式（I）化合物的合成，以及包含这些化合物的药物的化学和药物制备以及用这些化合物治疗哺乳动物（包括人）的方法。还有进一步提供治疗神经系统疾病，神经退行性疾病和精神病学疾病或病症的方法，并且还包括向人类施用需要这种治疗和/或预防药物组合物的步骤，所述药物组合物包含治疗有效量的式（I）或其药学上可接受的盐单独或与至少一种和药学上可接受的载体和/或稀释剂一起。

7. 发明申请

WO2022029704A1 REMDESIVIR INTERMEDIATES 审中-公开
公开(公告)号：WO2022029704A1
公开(公告)日：2022-02-10
申请号：PCT/IB2021/057242
申请日：2021-08-06
申请人： RICHTER GEDEON NYRT.
发明人： BORZA, István , UJVÁRI, Viktor , BANA, Péter , PETRO, József Levente , ÉLES, János , BÓDI, József , VARRÓ, Gábor , KLADNI, László János , SPRÁNITZ, Péter , KRÁMOS, Balázs
IPC分类号： C07H1/00 , C07D487/04 , C07D519/00 , C07H15/18 , A61P31/12 , A61P31/14
摘要： The present invention relates to a process for the preparation of a compound of formula (I) and to novel intermediates of the synthesis, wherein X is hydrogen, bromine or iodine; R1 is a protecting group, R2 is hydrogen or a protecting group, and PG is a protecting group.

8. 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。

9. 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

10. 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

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