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1. 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.

2. 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。

3. 发明专利

HUT56362A PROCESS FOR PRODUCING 1,8-SUBSTITUTED 2-HALOGENATED ERGOLENE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS 未知
公开(公告)号：HUT56362A
公开(公告)日：1991-08-28
申请号：HU65190
申请日：1990-02-02
申请人： RICHTER GEDEON VEGYESZET
发明人： KEVE TIBOR , MEGYERI GABOR , STEFKO BELA , KASSAI FERENCNE , NEUMAYER KATALIN , KISS BELA , LASZLOVSZKY ISTVAN , LAPIS ERZSEBET , PALOS EVA , GOOR DORA , SZPORNY LASZLO , SARKADI ADAM , AUTH FERENC , AMBRUS ANDRAS , SZABO SANDOR
IPC分类号： A61K31/48 , C07D457/02
摘要： 1,8 substd., 2 halogenated ergolene derivs. of formula (I) and acid adduct salts, - where R and R1 represent aroyl as hetero-aroyl gps.; x:chlorine as bromine atoms; and the dotted line represents a double bond in 8-9 or 9-10 position, - are prepd. from 2 halogenated ergolene derivs. of formula (II) -where x is as before - and an acid anhydride as acid-halide and by opt. formation of an acid adduct (I). - Medicinal prepn. contg. (I) have a pronounced anti-psychotic effect.

4. 发明专利

HU905743D0 PROCESS FOR PRODUCING BIS-INDOLE COMPOUND 未知
公开(公告)号：HU905743D0
公开(公告)日：1991-03-28
申请号：HU574390
申请日：1990-09-03
申请人： RICHTER GEDEON VEGYESZET
发明人： KEVE TIBOR , ACS TIBOR , ARANYI ANTAL , VEZEKENYI FERENC , STEFKO BELA , KASSAI FERENCNE , NEUMAYER KATALIN , LOERINCZ CSABA , KOVACS LAJOS , SZARVADY BELA , IVANYI GEZA , DEZSERI ESZTER , SZEN TAMAS , FEKETE GYOERGY
IPC分类号： C07D519/04

6. 发明专利

HU192932B PROCESS FOR PRODUCING APOVINCAMINOL DERIVATIVE 未知
公开(公告)号：HU192932B
公开(公告)日：1987-08-28
申请号：HU175885
申请日：1985-05-10
申请人： RICHTER GEDEON VEGYESZET
发明人： GALAMBOS JANOS , STEFKO BELA , ZSADON BELA , HORVATH KAROLYNE , KEVE TIBOR , FEKETE GYOERGY , KASSAI FERENCNE , OTTA KLARA
IPC分类号： C07D461/00
摘要： The invention relates to a new process for the preparation of 17,18-dehydro-apovincaminol-trimethoxy-benzoate of the formula (I) (I) and acid addition salts thereof. According to the invention compound of the formula (I) is prepared starting from 17,18-dehydrovincamine of the formula (IIa) (IIa) and/or 17,18-dehydro-epivincamine of formula (IIb) (IIb) by reducing with a complex metal hydride, acylating the new hydroxy-vincaminol derivative obtained selectively with 3,4,5-trimethoxy-benzoic acid or a derivative thereof capable of acylation, optionally in the presence of a catalyst and/or an acid binding agent, and treating the corresponding acylated hydroxylderivative obtained with formic acid, in the presence of an acid chloride, and, if desired, converting the compound of formula (I) obtained into an acid addition salt thereof.

7. 发明专利

HUT41024A PROCESS FOR PREPARING 2-HALOGEN-NICERGOLIN DERIVATIVES AND ACID ADDITIONAL SALTS THEREOF 未知
公开(公告)号：HUT41024A
公开(公告)日：1987-03-30
申请号：HU244785
申请日：1985-06-21
申请人： RICHTER GEDEON VEGYESZET
发明人： MEGYERI GABOR , KEVE TIBOR , STEFKO BELA , GALAMBOS JANOS , BOGSCH ERIK , KASSAI FERENCNE , TRISCHLER FERENC , SZPORNY LASZLO , KARPATI EGON , PALOSI EVA , GROO DORA , SZOMBATHELYI ZSOLT , KISS BELA , LASZLOVSZKY ISTVAN , LAPIS ERZSEBET
IPC分类号： A61K31/48 , A61P3/00 , A61P3/14 , A61P9/00 , A61P25/02 , A61P25/28 , C07D457/02
摘要： The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), (I) wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts. The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), (II) wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt. The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong alpha -adrenerg blocking and calcium-antagonistic action.

8. 发明专利

HU183062B NEW PROCESS FOR PREPARING ERGOCRISTINE 未知
公开(公告)号：HU183062B
公开(公告)日：1984-04-28
申请号：HU48879
申请日：1979-02-21
申请人： RICHTER GEDEON VEGYESZET
发明人： TERDY LASZLO , KISS JANOS , TROMPLER ARPAD , ZAMBO ISTVAN , FOELDESI JOZSEFNE , DANCSI LAJOS , KASSAI FERENCNE , GAZDAG MARIA
IPC分类号： C07D519/02

9. 发明专利

HU197006B PROCESS FOR PRODUCING ERGOLENE DERIVATIVES BY ISOMERIZATION 未知
公开(公告)号：HU197006B
公开(公告)日：1989-02-28
申请号：HU384886
申请日：1986-09-05
申请人： RICHTER GEDEON VEGYESZET
发明人： KEVE TIBOR , STEFKO BELA , KASSAI FERENCNE , MEGYERI GABOR , GALAMBOS JANOS
IPC分类号： C07D457/02

10. 发明专利

HUT44541A PROCESS FOR PREPARING 2-HALOGENATED ERGOLINE DERIVATIVES 未知
公开(公告)号：HUT44541A
公开(公告)日：1988-03-28
申请号：HU269086
申请日：1986-06-27
申请人： RICHTER GEDEON VEGYESZET
发明人： MEGYERI GABOR , IFJ KOVACS LAJOS , BOGSCH ERIK , SZEPESI GABOR , KEVE TIBOR , STEFKO BELA , KASSAI FERENCNE , TRISCHLER FERENC , GAZDAG MARIA
IPC分类号： C07B39/00 , A61K31/48 , C07B31/00 , C07C67/00 , C07D457/00 , C07D457/02 , C07D457/04 , C07D519/00 , C07D519/02 , C07D417/06
摘要： The invention relates to a novel process for the halogenation in 2-position of ergot alkaloids. The process is characterized by that as a halogenating agent a system consisting of dimethylsulfoxide, a trialkylhalosilane or triarylhalosilane and optionally a hydrogen halide is used.

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