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1. 发明申请

WO2005085243A2 NOVEL PROCESS FOR PRODUCTION OF CABERGOLINE 审中-公开
标题翻译：生产咖啡因的新工艺
公开(公告)号：WO2005085243A2
公开(公告)日：2005-09-15
申请号：PCT/HU2005000022
申请日：2005-03-02
申请人： RICHTER GEDEON VEGYESZET , GALAMBOS JANOS , CZIBULA LASZLO , SEBOK FERENC , BALINT SANDORNE , KASSAI FERENCNE , IGNACZNE SZENDREI GYOERGYI , DEMETER ADAM
发明人： GALAMBOS JANOS , CZIBULA LASZLO , SEBOK FERENC , BALINT SANDORNE , KASSAI FERENCNE , IGNACZNE SZENDREI GYOERGYI , DEMETER ADAM
IPC分类号： C07D457/06 , C07D457/00
CPC分类号： C07D457/06
摘要： A process for preparing cabergoline (I) from ergoline-8beta-carboxylic acid ester (XIII) comprising the following steps. (a) reacting an ergoline-8beta-carboxylic acid ester of formula (XIII), wherein R1 represents a C1-4 alkyl group, in the presence of a catalyst (i) with a compound of formula (XIV), X-COOR2 (XIV) wherein R2 is an optionally substituted straight or branched C1-6 alkyl group, X represents a bromine or chlorine atom, or (ii) with a compound of formula (XV), O(COOR2)2 (XV) wherein R2 is a group as defined above; (b) reacting the obtained carbamate derivative of formula (XVI) with 3-(dimethylamino)-propylamine (DMAPA) in the presence of a catalyst; (c) reacting the obtained ergoline-8beta-carboxamide derivative of formula (XVII) with ethyl isocyanate (EtNCO) in the presence of ligand(s) and Ib and IIb metal group salt catalysts; (d) reacting the obtained protected N-acylurea derivative of formula (XVIII) with a strong aqueous inorganic acid (aq./acid); (e) reacting the obtained secondary amine (XIX) with an electrophyl allyl alcohol derivative in the presence of a palladium or nickel containing catalyst and optionally in the presence of ligand(s) to form cabergoline (I). The intermediates of (XVI), (XVII), (XVIII) and (XIX) are novel. The polymorphic amorphous form of Cabergoline (I) and the production thereof.
摘要翻译：一种从麦角灵八羧酸酯（XIII）制备卡麦角林（I）的方法，包括以下步骤。（ⅰ）在催化剂（ⅰ）与式（ⅩⅣ）的化合物，X-COOR2（ⅩⅣ）的存在下，使式（ⅩⅩⅢ）的麦角灵-8-羧酸酯，其中R 1表示C 1-4烷基， XIV）其中R2是任选取代的直链或支链C 1-6烷基，X代表溴或氯原子，或（ii）与式（ⅩⅤ）化合物，O（COOR 2）2（ⅩⅤ）化合物，其中R 2是组如上所述; （b）在催化剂存在下使所得得到的式（ⅩⅥ）的氨基甲酸酯衍生物与3-（二甲氨基） - 丙胺（DMAPA）反应; （c）在配体和Ib和IIb金属盐盐催化剂存在下，使得到的式（XVII）的麦角灵八乙酰胺衍生物与异氰酸乙酯（EtNCO）反应; （d）使得到的式（XVIII）的保护的N-酰基脲衍生物与强无机酸水溶液（水溶液）反应; （e）在含钯或镍的催化剂存在下，任选地在配体存在下，使得到的仲胺（XIX）与电子烯丙基醇衍生物反应形成卡麦角林（I）。（XVI），（XVII），（XVIII）和（XIX）的中间体是新的。卡麦角林（I）的多晶型无定形形式及其生产。

2. 发明申请

WO2010070371A8 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：WO2010070371A8
公开(公告)日：2011-04-28
申请号：PCT/HU2009000110
申请日：2009-12-18
申请人： RICHTER GEDEON NYRT , AGAINE CSONGOR EVA , CZIBULA LASZLO , SEBOK FERENC , JUHASZ BALINT , GALAMBOS JANOS , NOGRADI KATALIN
发明人： AGAINE CSONGOR EVA , CZIBULA LASZLO , SEBOK FERENC , JUHASZ BALINT , GALAMBOS JANOS , NOGRADI 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。

3. 发明申请

WO2010070369A8 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：WO2010070369A8
公开(公告)日：2011-04-28
申请号：PCT/HU2009000108
申请日：2009-12-17
申请人： RICHTER GEDEON NYRT , CZIBULA LASZLO , AGAINE CSONGOR EVA , NOGRADI KATALIN , JUHASZ BALINT , SEBOK FERENC , GALAMBOS JANOS , VAGO ISTVAN
发明人： CZIBULA LASZLO , AGAINE CSONGOR EVA , NOGRADI KATALIN , JUHASZ BALINT , SEBOK FERENC , GALAMBOS JANOS , VAGO ISTVAN
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-叔丁氧基羰基） - 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。

4. 发明申请

WO03028728A8 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：WO03028728A8
公开(公告)日：2005-04-07
申请号：PCT/HU0200095
申请日：2002-09-25
申请人： RICHTER GEDEON VEGYESZET , NOGRADI KATALIN , GALAMBOS JANOS , ACS TIBOR , BORZA ISTVAN , BIELIK ATTILA , DOMANY GYOERGY , KISS BELA , GYERTYAN ISTVAN , LASZLOVSZKY ISTVAN , HORVATH ATTILA
发明人： NOGRADI KATALIN , GALAMBOS JANOS , ACS TIBOR , BORZA ISTVAN , BIELIK ATTILA , DOMANY GYOERGY , KISS BELA , GYERTYAN ISTVAN , LASZLOVSZKY ISTVAN , HORVATH ATTILA
IPC分类号： A61K31/47 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/542 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/48 , C07D213/56 , C07D215/50 , C07D215/54 , C07D233/54 , C07D233/90 , C07D239/26 , C07D295/073 , C07D295/096 , C07D295/13 , C07D471/04 , C07D487/04 , C07D513/04 , C07D209/42 , C07D295/12
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 D3 dopamine receptor subtype selective ligands of Formula (I), wherein R1, R2 and R3 independently represent substituents selected from hydrogen, halogen, C1-6alkyl, C1-6alkoxy, cyano, hydroxy, trifluoromethyl, C1-6alkylsulfonyloxy, trifluoromethanesulfonyloxy, optionally substituted C1-6alkanoyloxy, 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 R1, R2 and R3 may combine to form an optionally substituted fused mono or bicyclic heterocyclic group, with the exception of compounds wherein a) R1= R2 = R3 = H, b) R1 = R2= H and R3 = C1-6alkoxy in the position 2 or R3 is in the position 4 of the piperazinylphenyl moiety, c) R1 = H and R2 = R3 = C1-6alkoxy; Q represents an optionally substituted C1-6alkyl, C1-6alkenyl, 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。

5. 发明专利

JP2002255939A 5-AMINONICOTINIC ACID DERIVATIVE 失效
公开(公告)号：JP2002255939A
公开(公告)日：2002-09-11
申请号：JP2001050385
申请日：2001-02-26
申请人： KOWA CO , RICHTER GEDEON VEGYESZET
发明人： NYEKI OLGA , NOOGURAADEI KATALIN , AGAINE CSONGOR EVA , BAARUTAANEE SARAI GISELA , DOMANY GYOERGY , ADAM DEMETER , GALAMBOS JANOS , GIZUR TIBOR , KASSAI FERENCNE , KIS CHIRRA , RILL ATTILA , SCHON ISTVAN , TRISCHLER FERENC , TOERLEY JOZSEF , KYOTANI YOSHINORI , YOKOYAMA TORU
IPC分类号： C07D487/04 , A61K31/4406 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/455 , A61K31/4985 , A61K31/5517 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D213/82 , C07D401/06 , C07D401/12 , C07D401/14
摘要： PROBLEM TO BE SOLVED: To provide a new 5-aminonicotinic acid derivative having both fibrinogen receptor antagonism and vasodilator action, and to provide a medical composition containing the same. SOLUTION: The 5-aminonicotinic acid derivative represented by the general formula (I) (wherein, Q denotes any group of five kinds e.g. formula (a); X denotes O or NCN group; Z denotes 2-nitroxyethyl, 2-methylpropyl, 1,1- dimethylpropyl, benzyl, 2-phenylethyl or 2-(2-chlorophenyl)ethyl group; R denotes H, an alkali metal atom, an alkaline earth metal atom or 1-4C alkyl group; the aspartic acid residue is racemic or optically active) and having both fibrinogen receptor antagonism and vasodilator action and, its pharmaceutically acceptable salt, solvate or hydrate, and a medical composition containing the compounds. The compound is especially useful as an inhibitor against platelet agglutination, platelet adhesiveness, and restenosis, a medicine for antiatheroselerotic arteriosclerosis, and a vasodilator for treating unstable stenocardia, cerebral apoplexy, cardiac infarction, and the like.

6. 发明申请

WO2008155588A8 SULFONYL-QUINOLINE DERIVATIVES 审中-公开
标题翻译：磺酰喹啉衍生物
公开(公告)号：WO2008155588A8
公开(公告)日：2009-12-30
申请号：PCT/HU2008000068
申请日：2008-06-17
申请人： RICHTER GEDEON NYRT , GALAMBOS JANOS , KESERUE GYOERGY , GAL KRISZTINA , VASTAG MONIKA , BOBOK AMRITA AGNES , WEBER CSABA , PRAUDA LBOLYA , WAGNER GABOR ANDRAS
发明人： GALAMBOS JANOS , KESERUE GYOERGY , GAL KRISZTINA , VASTAG MONIKA , BOBOK AMRITA AGNES , WEBER CSABA , PRAUDA LBOLYA , WAGNER GABOR ANDRAS
IPC分类号： C07D215/36 , A61K31/4706 , A61K31/4709 , A61P25/00 , C07D409/12
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 Ar1 represents an optionally substituted phenyl or heteroaryl group; Ar2 represents a substituted phenyl or an optionally substituted heteroaryl group; R1, R2, R3 and R4 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

7. 发明申请

WO2010070370A1 PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
标题翻译：哌嗪化合物的制备方法及其盐酸盐的制备方法
公开(公告)号：WO2010070370A1
公开(公告)日：2010-06-24
申请号：PCT/HU2009000109
申请日：2009-12-18
申请人： RICHTER GEDEON NYRT , CZIBULA LASZL , JUHASZ BALINT , AGAINE CSONGOR EVA , SEBOEK FERENC , GALAMBOS JANOS , N GRADI KATALIN
发明人： CZIBULA LASZL , JUHASZ BALINT , AGAINE CSONGOR EVA , SEBOEK FERENC , GALAMBOS JANOS , N GRADI 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) 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 C1-6 straight or branched chain or C1-2 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 R1 and R2 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：本发明涉及一种通过将反式4- [2- [4-（2,3-二氯苯基）） - 哌嗪-1-基] - 环己胺或其盐或其水合物或溶剂化物，然后在惰性溶剂中在存在碱存在下加入通式（VI）的碳酸衍生物，其中R是烷基， 6个直链或支链或C1-2完全卤代烷基，Z是-OR或-X，其中R如上所述，X是卤素，并使得到的通式（Ⅳ）化合物（其中R如上所述）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/或水合物和/或溶剂合物它们。

8. 发明专利

RS20060041A DERIVATI (TIO)KARBAMOIL-CIKLOHEKSANA KAO ANTAGONISTI D3/D2 RECEPTORA 未知
公开(公告)号：RS20060041A
公开(公告)日：2009-11-10
申请号：RSP20060041
申请日：2004-05-21
申请人： RICHTER GEDEON VEGYESZET
发明人： KISS BELA , VAGO ISTVAN , AGAINE CSONGOR EVA , GALAMBOS JANOS , NOGRADI KATALIN , GYERTYAN ISTVAN , LASZLOVSKY ISTVAN , LASZU JUDIT , SAGHY KATALIN
IPC分类号： C07D243/08 , A61K31/495 , A61P25/00 , C07D223/04 , C07D295/12 , C07D295/135 , C07D295/14 , C07D295/215 , C07D401/12
摘要： Predstavljeni pronalazak se odnosi na nove ligande za podgrupu D2 i D3 dopaminskih receptora formule (I): gde R1 i R2 nezavisno predstavljaju supstituent izabran iz grupe koju čine vodonik, alkil, aril, cikloalkil, aroil, ili R1 i R2 mogu da formiraju heterocikličan prsten sa susednim atomom azota; X predstavlja atom kiseonika ili sumpora; n je ceo broj od 1 do 2; i/ili njihove geometrijske izomere i/ili stereoizomere i/ili diastereomere i/ili soli i/ili hidrate i/ili solvate, na postupak za njihovu proizvodnju, farmaceutske kompozicije koje ih sadrže i na njihovu primenu u lečenju i/ili prevenciji stanja koje zahteva modulaciju dopaminskih receptora.

10. 发明专利

HK1093494A1 (THIO) CARBAMOYL-CYCLOHEXANE DERIVATIVES AS D3/D2 RECEPTOR ANTAGONISTS 未知
公开(公告)号：HK1093494A1
公开(公告)日：2007-03-02
申请号：HK07100087
申请日：2007-01-04
申请人： RICHTER GEDEON VEGYESZET
发明人： CSONGOR EVA AGAINE , GALAMBOS JANOS , NOGRADI KATALIN , VAGO ISTVAN , GYERTYAN ISTVAN , KISS BELA , LASZLOVSZKY ISTVAN , LASZY JUDIT , SAGHY KATALIN
IPC分类号： A61K20060101 , A61P20060101 , A61P25/00 , C07D20060101 , C07D223/04 , C07D243/08 , C07D295/135 , C07D295/215
摘要： The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 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.

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