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1. 发明申请

WO2010070369A1 PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：哌嗪盐及其制备方法
公开(公告)号：WO2010070369A1
公开(公告)日：2010-06-24
申请号：PCT/HU2009/000108
申请日：2009-12-17
申请人： RICHTER GEDEON NYRT. , CZIBULA, Lászl , AGAINE CSONGOR, Eva , NOGRADI, Katalin , JUHASZ, Bálint , SEBOK, Ferenc , GALAMBOS, János , VAGO, István
发明人： CZIBULA, Lászl , AGAINE CSONGOR, Eva , NOGRADI, Katalin , JUHASZ, Bálint , SEBOK, Ferenc , GALAMBOS, János , VAGO, István
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N- {4- {2-[4-(2,3-dichlorophenyl)-piperazine-l -il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)amino]- cyclohexyl} -acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{l-[4- (N-tert-butoxycarbonyl)-amino] -cyclohexyl} -ethyl methanesulfonate; c) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert- butylester obtained to a temperature between 40-100°C in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl)piperazine-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate.
摘要翻译：本发明涉及新的反式N- {4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物，以及制备反式N- { 4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物，所述方法包括步骤a）使反式-2- {1- [4-（N- 叔丁氧基羰基）氨基] - 环己基} - 乙酸酯与硼氢化钠和三氯化铝反应，得到反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 乙醇; b）将获得的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基]环己基} - 乙醇与甲磺酰氯在酸结合剂存在下反应，得到反式-2- {1- [4- （N-叔丁氧基羰基） - 氨基] - 环己基} - 乙基甲磺酸酯; c）在酸结合剂存在下，使得到的与2,3-二氯苯基哌嗪的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 乙基甲基磺酸酯反应，得到反式-2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 氨基甲酸叔丁酯; d）将得到的反式2- {1- [4-（N-叔丁氧羰基） - 氨基] - 环己基} - 氨基甲酸叔丁酯加热至40-100℃的温度，在盐酸/甲醇水溶液得到反式N- {4- {2- [4-（2,3-二氯苯基）哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物。

2. 发明申请

WO2008155588A1 SULFONYL-QUINOLINE DERIVATIVES 审中-公开
标题翻译：磺酰喹啉衍生物
公开(公告)号：WO2008155588A1
公开(公告)日：2008-12-24
申请号：PCT/HU2008/000068
申请日：2008-06-17
申请人： RICHTER GEDEON NYRT. , VASTAG, Mónika , GALAMBOS, János , KESERÛ, György , GÁL, Krisztina , BOBOK, Amrita, Ágnes , WÉBER, Csaba , PRAUDA, lnolya , WÁGNER, Gábor, András
发明人： GALAMBOS, János , KESERÛ, György , GÁL, Krisztina , BOBOK, Amrita, Ágnes , WÉBER, Csaba , PRAUDA, lnolya , WÁGNER, Gábor, András
IPC分类号： C07D215/36 , C07D409/12 , A61K31/4706 , A61K31/4709 , A61P25/00
CPC分类号： C07D215/36 , C07D409/12
摘要： New mGluRl and mGluR5 receptor subtype preferring ligands of formula: (I) and/or salts and/or hydrates and/or solvates thereof, to the processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in therapy and/or prevention of a condition which requires modulation of mGluRl and mGluR5 receptors.FORMULE (I) wherein Ar 1 represents an optionally substituted phenyl or heteroaryl group; Ar 2 represents a substituted phenyl or an optionally substituted heteroaryl group; R 1 , R 2 , R 3 and R 4 represent independently a substituent selected from hydrogen, halogen, cyano, alkyl, alkoxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl
摘要翻译：新的mGluR1和mGluR5受体亚型优选式（I）的配体和/或其盐和/或水合物和/或溶剂化物，其制备方法和中间体，含有这些化合物的药物组合物及其在治疗和 /或预防需要调节mGluR1和mGluR5受体的病症。其中Ar 1表示任选取代的苯基或杂芳基; Ar 2表示取代的苯基或任选取代的杂芳基; R1，R2，R3和R4独立地表示选自氢，卤素，氰基，烷基，烷氧基，羟基，三氟甲基，氨基，烷基氨基，二烷基氨基，氨基甲基，烷基氨基甲基，二烷基氨基甲基

3. 发明申请

WO2010070370A8 PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
公开(公告)号：WO2010070370A8
公开(公告)日：2010-06-24
申请号：PCT/HU2009/000109
申请日：2009-12-18
申请人： RICHTER GEDEON NYRT. , CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
发明人： CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
IPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving suspending trans 4-[2-[4-(2,3-dichlorophenyl)-piperazine1-il]-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C 1-6 straight or branched chain or C 1-2 fully halogenated alkyl, Z is -O-R or -X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R 1 and R 2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.

4. 发明申请

WO2011073705A1 NOVEL PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
标题翻译：制备哌嗪化合物及其盐酸盐的新工艺
公开(公告)号：WO2011073705A1
公开(公告)日：2011-06-23
申请号：PCT/HU2010/000144
申请日：2010-12-17
申请人： RICHTER GEDEON NYRT. , CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
发明人： CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) wherein R 1 and R 2 represent independently hydrogen or C 1-6 alkyl with straight or branched chain optionally substituted with aryl group; or C 2-7 alkenyl containing 1-3 double bonds; or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifiuoro-C 1-6 alkoxy, C 1-6 -alkoxycarbonil, C 1-6 alkanoyl, aryl, C 1-6 alkylthio, halogen or cyano; or optionally substituted monocyclic, bicyclic or tricyclic C 3-14 cycloalkyl group; R 1 and R 2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid salts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence of a base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C 1-6 straight or branched chain, partially or fully halogenated C 1-2 alkyl or phenyl, Z is -O-R or -X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R 1 and R 2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.
摘要翻译：本发明涉及制备通式（I）化合物的新方法，其中R 1和R 2独立地表示氢或任选被芳基取代的直链或支链的C 1-6烷基; 或含有1-3个双键的C2-7烯基; 或任选被一个或多个C 1-6烷氧基，三氟-C 1-6烷氧基，C 1-6 - 烷氧羰基，C 1-6烷酰基，芳基，C 1-6烷硫基，卤素或氰基取代的单环，双环或三环芳基; 或任选取代的单环，双环或三环C 3-14环烷基; R1和R2与相邻的氮一起形成饱和或不饱和的任选取代的单环或双环杂环，其可以含有选自氧，氮或硫原子的其它杂原子和盐酸盐和/或其水合物和/或溶剂合物，通过溶解或将式（III）的反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺或其盐或其水合物或溶剂合物悬浮在惰性溶剂中碱的存在然后加入通式（VI）的碳酸衍生物，其中R是具有C 1-6直链或支链，部分或完全卤代的C 1-2烷基或苯基的烷基，Z是-OR或-X，其中 R是如上所述，X是卤素，并且其中R如上所述获得的通式（IV）化合物原位或任选地在分离状态下与通式（Ⅴ）的胺反应，其中R 1和R 2是如上所述，得到通式（I）的化合物），然后任选地形成盐酸盐和/或其水合物和/或溶剂合物。

5. 发明申请

WO2010070371A1 PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES 审中-公开
标题翻译：制备哌嗪衍生物的方法
公开(公告)号：WO2010070371A1
公开(公告)日：2010-06-24
申请号：PCT/HU2009/000110
申请日：2009-12-18
申请人： RICHTER GEDEON NYRT. , ÁGAINÉ CSONGOR, Éva , CZIBULE, László , SEBÖK, Ferenc , JUHÁSZ, Bálint , GALAMBOS, János , NÓGRÁDI, Katalin
发明人： ÁGAINÉ CSONGOR, Éva , CZIBULE, László , SEBÖK, Ferenc , JUHÁSZ, Bálint , GALAMBOS, János , NÓGRÁDI, Katalin
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The invention relates to a process for the preparation of the trans N-{ 4-{2-[4-(2,3- dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of formula (I) by reacting the compound of formula (III) with a carbamoylchloride of formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100 °C in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant.
摘要翻译：本发明涉及制备式（I）的反式N- {4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己基} - 氨基甲酰胺衍生物的方法）通过使式（III）的化合物与式（II）的氨基甲酰氯反应，其包括在存在下在40-100℃的温度下在溶剂和浓氢氧化碱水溶液的混合物中进行反应的相转移催化剂，分离相并洗涤有机层，然后除去溶剂并干燥获得的式（I）化合物，直到其重量恒定。

6. 发明申请

WO2020012424A1 SUBSTITUTED (AZA)INDOLE DERIVATIVES 审中-公开
公开(公告)号：WO2020012424A1
公开(公告)日：2020-01-16
申请号：PCT/IB2019/055950
申请日：2019-07-12
申请人： RICHTER GEDEON NYRT.
发明人： LEDNECZKI, István , ÉLES, János , TAPOLCSÁNYI, Pál , HORVÁTH, Anita , NÉMETHY, Zsolt , LÉVAY, György István , GALAMBOS, János
IPC分类号： C07D403/12 , C07D401/12 , C07D471/04 , C07D209/08 , C07D209/10 , C07D209/42 , A61K31/404 , A61K31/437
摘要： The invention relates to substituted (aza)indole derivatives, or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof, as well as to pharmaceutical compositions containing them and to their use as modulators of α7 nicotinic acetylcholine receptor activity in a mammalian subject. (I)

7. 发明申请

WO2005012266A1 (THIO) CARBAMOYL-CYCLOHEXANE DERIVATIVES AS D3/D2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：（THIO）碳水化合物衍生物作为D3 / D2受体拮抗剂
公开(公告)号：WO2005012266A1
公开(公告)日：2005-02-10
申请号：PCT/HU2004/000056
申请日：2004-05-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , ÁGAINÉ CSONGOR, Éva , GALAMBOS, János , NÓGRÁDI, Katalin , VÁGÓ, István , GYERTYÁN, István , KISS, Béla , LASZLOVSZKY, István , LASZY, Judit , SÁGHY, Katalin
发明人： ÁGAINÉ CSONGOR, Éva , GALAMBOS, János , NÓGRÁDI, Katalin , VÁGÓ, István , GYERTYÁN, István , KISS, Béla , LASZLOVSZKY, István , LASZY, Judit , SÁGHY, Katalin
IPC分类号： C07D243/08
CPC分类号： C07D295/215 , C07D223/04 , C07D243/08 , C07D295/135
摘要： The present invention relates to new D 3 and D 2 dopamine receptor subtype preferring ligands of formula (I): wherein R 1 and R 2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R 1 and R 2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.
摘要翻译：本发明涉及新的D3和D2多巴胺受体亚型优选式（I）的配体：其中R 1和R 2分别独立地表示选自氢，烷基，芳基，环烷基，芳酰基或R 1和R 2中的取代基，可以与相邻的氮原子; X表示氧或硫原子; n是1至2的整数，和/或几何异构体和/或立体异构体和/或非对映异构体和/或其盐和/或水合物和/或溶剂合物，其制备方法涉及含有与其在治疗和/或预防需要调节多巴胺受体的病症中的用途相同。

8. 发明申请

WO2006082456A1 CYCLOHEXYLAMIDES AS DOPAMINE D3 , D2 AND 5HT1A ANTAGONISTS 审中-公开
标题翻译：环辛基胺作为DOPAMINE D3，D2和5HT1A拮抗剂
公开(公告)号：WO2006082456A1
公开(公告)日：2006-08-10
申请号：PCT/HU2006/000012
申请日：2006-02-02
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , ÁGAINÉ CSONGOR, Éva , DOMÁNY, György , GALAMBOS, János , GYERTYÁN, István , KISS, Béla , SÁGHY, Katalin , SCHMIDT, Éva
发明人： ÁGAINÉ CSONGOR, Éva , DOMÁNY, György , GALAMBOS, János , GYERTYÁN, István , KISS, Béla , SÁGHY, Katalin , SCHMIDT, Éva
IPC分类号： C07D295/12 , A61K31/495 , A61K31/535 , A61P25/00
CPC分类号： C07D295/135
摘要： The present invention relates to new dopamine D 3 and D 2 and serotonin 5-HT 1A receptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula -NR 1 R 2 , wherein R 1 and R 2 represent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or R 1 and R 2 form with the adjacent nitrogen atom and optionally with further heteroatom(s) a heterocyclic ring; m is an integer of 0 to 1 ; n is an integer of 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine and/or 5-HT 1A receptors.
摘要翻译：本发明涉及新的多巴胺D 3和D 2和5-羟色胺5-HT 1A受体亚型优选式（I）的配体; 其中A表示烷基，烯基，芳基，杂芳基，环烷基或式-NR 1 R 2的基团，其中R 1和R 2，取代基独立地表示选自氢，烷基，链烯基，芳基，杂芳基或环烷基的取代基或R 1和R 2，以及相邻的氮原子和任选地带有杂原子的杂环; m为0〜1的整数; n是1至2的整数，和/或几何异构体和/或立体异构体和/或非对映异构体和/或其盐和/或水合物和/或溶剂化物，其制备方法，含有其相同的药物组合物以及它们在治疗和/或预防需要调节多巴胺和/或5-HT 1A受体的病症中的用途。

9. 发明申请

WO2003029233A1 NEW SULFONAMIDE DERIVATIVES AS D3-RECEPTOR AGONISTS 审中-公开
标题翻译：新的磺酰胺衍生物作为D3受体激动剂
公开(公告)号：WO2003029233A1
公开(公告)日：2003-04-10
申请号：PCT/HU2002/000093
申请日：2002-09-25
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , GALAMBOS, János , NÓGRÁDI, Katalin , ÁGAINÉ CSONGOR, Éva , KESERÚ, György, Miklós , VÁGÓ, István , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , LASZY, Judit
发明人： GALAMBOS, János , NÓGRÁDI, Katalin , ÁGAINÉ CSONGOR, Éva , KESERÚ, György, Miklós , VÁGÓ, István , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , LASZY, Judit
IPC分类号： C07D295/12
CPC分类号： C07D295/135 , C07D211/14 , C07D211/18 , C07D211/28 , C07D211/44 , C07D211/46 , C07D211/58 , C07D213/71 , C07D295/04 , C07D295/12
摘要： The present invention relates to new D 3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their us in therapy and/or prevention of psychoses ( e.g. schizophrenia, schizo-affective disorders, etc ), drug ( e.g. alcohol, cocaine and nicotine, opioids etc. ) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders ( e.g. bulimia nervosa, etc. ), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's desases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases ( e.g. glaucoma etc. ).
摘要翻译：本发明涉及式（I）的新的D3多巴胺受体亚型选择配体，其含有与其相同的药物组合物，以及用于治疗和/或预防精神病（例如精神分裂症，分裂症情感障碍等），药物（例如，酒精，可卡因和尼古丁，阿片样物质等）滥用，伴随精神分裂症的认知障碍，轻度至中度认知缺陷，遗忘症，进食障碍（例如神经性贪食症等），注意力缺陷障碍，儿童多动症，精神抑郁症，焦虑症，性功能障碍，睡眠障碍，呕吐，侵略，自闭症，眼部疼痛眼疾病（如青光眼等），躁狂症，偏执狂和妄想障碍，运动障碍（如帕金森病，精神安定药诱发的帕金森病，迟发性运动障碍）。

10. 发明申请

WO2003028728A1 4-(4-SUBSTITUTED PIPERAZINYL-1YL)-BUTYLCARBOXAMIDES AS D3 DOPAMINE SUBTYPE SELECTIVE LIGANDS 审中-公开
标题翻译： 4-（4-取代的哌嗪-1-基） - 丁醛作为D3多巴胺亚型选择性配体
公开(公告)号：WO2003028728A1
公开(公告)日：2003-04-10
申请号：PCT/HU2002/000095
申请日：2002-09-25
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , GALAMBOS, János , ÁCS, Tibor , BORZA, István , BIELIK, Attila , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , HORVÁTH, Attila
发明人： NÓGRÁDI, Katalin , GALAMBOS, János , ÁCS, Tibor , BORZA, István , BIELIK, Attila , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , HORVÁTH, Attila
IPC分类号： A61K31/496
CPC分类号： C07D209/48 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/542 , C07D207/34 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/50 , C07D215/54 , C07D233/64 , C07D239/26 , C07D295/073 , C07D295/096 , C07D295/13 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to new D 3 dopamine receptor subtype selective ligands of Formula (I), wherein R 1 , R 2 and R 3 independently represent substituents selected from hydrogen, halogen, C 1-6 alkyl, C 1-6 alkoxy, cyano, hydroxy, trifluoromethyl, C 1-6 alkylsulfonyloxy, trifluoromethanesulfonyloxy, optionally substituted C 1-6 alkanoyloxy, amino, aminoalkyl, carboxy, aminocarbonyl, N-hydroxycarbamimidoyl, carbamimidoyl, hydroxycarbamoyl, thiocarbamoyl, sulfamoyl, optionally substituted phenyl or naphthyl, optionally substituted mono or bicyclic heterocyclic group, two adjacent groups of R 1 , R 2 and R 3 may combine to form an optionally substituted fused mono or bicyclic heterocyclic group, with the exception of compounds wherein a) R 1 = R 2 = R 3 = H, b) R 1 = R 2 = H and R 3 = C 1-6 alkoxy in the position 2 or R 3 is in the position 4 of the piperazinylphenyl moiety, c) R¿1 ?= H and R 2 = R 3 = C 1-6 alkoxy; Q represents an optionally substituted C 1-6 alkyl, C 1-6 alkenyl, phenyl or heteroaryl group.
摘要翻译：本发明涉及式（I）的新的D3多巴胺受体亚型选择性配体，其中R 1，R 2和R 3独立地表示选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，羟基，三氟甲基，C 1-6烷基磺酰氧基，三氟甲磺酰氧基，任选取代的C 1-6烷酰氧基，氨基，氨基烷基，羧基，氨基羰基，N-羟基甲脒基，氨基甲酰基，氨基甲酰基，硫代氨基甲酰基，氨磺酰基，任选取代的苯基或萘基，任选取代的单或双环杂环基，并且R 3可以结合形成任选取代的稠合单或双环杂环基，除了其中a）R 1 = R 2 = R 3 = H，b）R 1 = R 2 = H和R 3 = C 1-6烷氧基在位置2或 R3在哌嗪基苯基部分的位置4，c）R1 = H，R2 = R3 = C1-6烷氧基; Q表示任选取代的C 1-6烷基，C 1-6烯基，苯基或杂芳基。

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