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1. 发明申请

WO1985002842A1 PROCESS FOR THE PREPARATION OF 1,2,4-TRIAZOLE 审中-公开
标题翻译：制备1,2,4-三唑的方法
公开(公告)号：WO1985002842A1
公开(公告)日：1985-07-04
申请号：PCT/HU1984000066
申请日：1984-12-21
申请人： ALKALOIDA VEGYÉSZETI GYAR
发明人： ALKALOIDA VEGYÉSZETI GYAR , KORODI, Ferenc , LITKEI, László
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： Process for the preparation of 1,2,4-triazole by the ring closure of diformyl hydrazine prepared by the formylation of hydrazine and ammonia which comprises reacting ammonium formiate with hydrazine hydrate by feeding continuously hydrazine or hydrazine hydrate at 120-160 C to the aqueous solution of ammonium formiate and removing continuously the formed water ammonia from the mixture and isolating, if desired, the cold precipitated triazole from the mixture.
摘要翻译：通过肼和氨甲酰化制备的二甲酰肼的闭环制备1,2,4-三唑的方法，其包括通过在120-160℃下连续供入肼或水合肼将甲酸铵与水合肼反应至甲酸铵水溶液，并从混合物中连续除去形成的水氨，如果需要，从混合物中分离出冷沉淀的三唑。

2. 发明申请

WO1994022413A2 TRIAZOLE SUBSTITUTED QUINOLINE DERIVATIVES 审中-公开
标题翻译：三唑取代的喹啉衍生物
公开(公告)号：WO1994022413A2
公开(公告)日：1994-10-13
申请号：PCT/HU1994000008
申请日：1994-03-31
申请人： ALKALOIDA VEGYÉSZETI GYAR RT. , FRANK, László , KORODI, Ferenc , GYIRES, Klára , GALAMB, Vilmos , BILKEI-GORZO, András
发明人： ALKALOIDA VEGYÉSZETI GYAR RT.
IPC分类号： A61K00/00
CPC分类号： C07D231/12 , A61K31/47 , C07D233/56 , C07D249/08 , C07D401/12
摘要： The invention relates to pharmaceutical compositions for the treatment or prevention of lesions of gastrointestinal mucous membranes and having secretion inhibiting, cytoprotective activities. The compositions contain in a biologically effective quantity a triazole-group-substituted quinoline derivative of general formula (I), R stands for a 1-triazolyl-group in position 2 or 4 or a 3-triazolyl-thio or a 5-/C1-4-alkyl/-3-triazolyl-thio-group, R stands for a hydrogen atom in position 3 or optionally in position 2, or for a C1-4-alkyl-group, R stands for a hydrogen atom or for a C1-4-alkyl-group, X stands for a hydrogen or halogen-atom or for a C1-4-alkyl-group or its salts. The invention includes processes for the preparation of the above compositions, and methods for treatment of patients in need of such treatment by administering the substance or the composition. The preferred substance of formula (IV) is also subject of the invention.
摘要翻译：本发明涉及用于治疗或预防胃肠粘膜病变并具有分泌抑制，细胞保护活性的药物组合物。组合物含有生物有效量的通式（I）的三唑基取代喹啉衍生物，R 1表示位置2或4或3-三唑基硫基或5位上的1-三唑基 - / C 1-4 - 烷基-3-三唑基 - 硫基，R 2表示3位或任选位置2的氢原子或C1-4 - 烷基，R 3表示氢原子，代表氢原子或C1-4烷基，X代表氢或卤素原子或C1-4烷基或其盐。本发明包括制备上述组合物的方法，以及通过施用该物质或组合物来治疗需要这种治疗的患者的方法。式（IV）的优选物质也是本发明的主题。

3. 发明申请

WO1994014799A1 BENZOPYRAN DERIVATIVES 审中-公开
标题翻译： BENZOPYRAN衍生物
公开(公告)号：WO1994014799A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000079
申请日：1993-12-20
申请人： ALKALOIDA VEGYÉSZETI GYAR RT. , ESZENYI, Tibor , SEBÖK, Péter , FRANK, László , PAPP, Gyula , TIMAR, Tibor , BARTIK, Tamás
发明人： ALKALOIDA VEGYÉSZETI GYAR RT.
IPC分类号： C07D405/04
CPC分类号： C07D405/04 , C07D311/22
摘要： The invention relates to novel benzopyran derivatives of general formula (I) possessing pharmacological activity, as well as to pharmaceutical compositions containing the compounds of general formula (I) and process for the preparation thereof. In general formula (I) R1 stands for a C1-6alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, aryloxy, aralkyloxy, hydroxy, nitro, cyano, formyl, C1-6acyl or C1-6alkylcyano group or a halo atom, R2 stands for a C1-6alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, aryloxy, aralkyloxy or hydroxyl group, R1 and R2 together stand for alkylenedioxy, and R3 and R4 stand for a C1-6alkyl group.
摘要翻译：本发明涉及具有药理活性的通式（I）的新型苯并吡喃衍生物，以及含有通式（I）化合物的药物组合物及其制备方法。在通式（I）中，R 1表示C 1-6烷氧基，烯氧基，炔氧基，环烷氧基，芳氧基，芳烷氧基，羟基，硝基，氰基，甲酰基，C 1-6酰基或C 1-6烷基氰基或卤素原子，烷氧基，链烯氧基，炔氧基，环烷氧基，芳氧基，芳烷氧基或羟基，R1和R2一起代表亚烷基二氧基，R3和R4代表C1-6烷基。

4. 发明申请

WO1986006721A1 TRIAZOLYL QUINOLINE DERIVATIVES 审中-公开
标题翻译：三唑衍生物衍生物
公开(公告)号：WO1986006721A1
公开(公告)日：1986-11-20
申请号：PCT/HU1986000026
申请日：1986-05-07
申请人： ALKALOIDA VEGYÉSZETI GYAR , KORODI, Ferenc , FRANK, László , SALAMON, Zoltán , SANDOR, József , POCSAI, Emma , TEREBES, Erzsébet
发明人： ALKALOIDA VEGYÉSZETI GYAR
IPC分类号： C07D401/04
CPC分类号： C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08 , C07D401/12
摘要： New triazolyl quinoline derivatives and acid addition salts thereof (wherein R stands for hydrogen, methyl, trihalogenomethyl or carboxy; R is hydrogen, halogen, C1-4 alkyl, hydroxy, C1-4 alkoxy, phenoxy, amino, acetamino, C1-4 dialkylamino, acetyl, benzoyl, methylthio, carboxy, cyano, ethoxycarbonyl, nitro or trihalogenomethyl; R represents hydrogen, C1-4 alkyl or C1-4 alkoxy; R stands for hydrogen, methyl or ethyl and X stands for a valency bond or -S-). The new compounds of general formula (I) possess valuable analgesic, antiphlogistic and fungicidal effect and can be used both in therapy and agriculture.
摘要翻译：新的三唑基喹啉衍生物及其酸加成盐（其中R 1代表氢，甲基，三卤代甲基或羧基; R 2是氢，卤素，C 1-4烷基，羟基，C 1-4烷氧基，苯氧基，氨基，乙酰氨基，C 1-4二烷基氨基，乙酰基，苯甲酰基，甲硫基，羧基，氰基，乙氧基羰基，硝基或三卤代甲基; R 3表示氢，C 1-4烷基或C 1-4烷氧基; R 4表示氢，甲基或乙基，X表示价键或-S-）。通式（I）的新化合物具有有价值的止痛，消炎和杀菌作用，可用于治疗和农业。

5. 发明申请

WO1985003932A1 NOVEL DIASTEREOMER SALTS OF PHENYLALANINE AND N-ACYL DERIVATIVES THEREOF AND PROCESS FOR THE SEPARATION OF OPTICALLY ACTIVE PHENYLALANINE AND N-ACYL DERIVATIVES THEREOF 审中-公开
标题翻译：苯乙烯胺和N-乙酸衍生物的新型二异氰酸酯盐及其分离光学活性苯丙氨酸及其N-取代基衍生物的方法
公开(公告)号：WO1985003932A1
公开(公告)日：1985-09-12
申请号：PCT/HU1985000012
申请日：1985-03-01
申请人： ALKALOIDA VEGYÉSZETI GYAR , ACS, Mária , FAIGL, Ferenc , FOGASSY, Elemér
发明人： ALKALOIDA VEGYÉSZETI GYAR
IPC分类号： C07C101/08
CPC分类号： C07C227/34 , C07C229/36
摘要： The separation of optically active phenylalanine and N-acyl derivatives thereof and novel diastereomer salts of the said compounds. According to the invention a racemic compound of formula (I), is reacted with an optically active resolving agent of formula (II), in a polar solvent and/or a mixture of solvents comprising at least one apolar solvent and optionally an achiral acid or base, thereafter a) when using the D-isomer of the resolving agent of formula (II), the crystalline diastereomer salt formed with the L-isomer of the compound of formula (I) is separated, or b) when using the L-isomer of the resolving agent of formula (II), the crystalline diastereomer salt formed with the D-isomer of the compound of formula (I) is separated, and the enantiomers of the compound of formula (I) from the diastereomer salt or the mother liquor are liberated by the aid of an achiral acid or base and the optically active product is separated in crystalline form.
摘要翻译：光学活性苯丙氨酸及其N-酰基衍生物的分离和所述化合物的新型非对映异构体盐。根据本发明，将式（I）的外消旋化合物与式（II）的光学活性拆分剂在极性溶剂和/或包含至少一种非极性溶剂和任选的非手性酸的溶剂混合物中反应或碱，然后a）当使用式（II）的拆分剂的D-异构体时，与式（I）化合物的L-异构体形成的结晶非对映体盐分离，或b）当使用L- 分离式（II）的拆分剂的异构体，与式（I）化合物的D-异构体形成的结晶非对映异构体盐，并且来自非对映异构体盐或母体的式（I）化合物的对映异构体液体通过非手性酸或碱解除，光学活性产物以结晶形式分离。

6. 发明申请

WO1984002906A1 NEW AMINO DERIVATIVES OF 2-ADN-(2,2,5,5-TETRAMETHYL-3-PYRROLIN-3-CARBONYL)BD 审中-公开
标题翻译： 2- [N-（2,2,5,5-四甲基-3-吡咯烷-3-基羰基）]的新氨基衍生物]
公开(公告)号：WO1984002906A1
公开(公告)日：1984-08-02
申请号：PCT/HU1984000004
申请日：1984-01-20
申请人： ALKALOIDA VEGYÉSZETI GYAR , HIDEG, Kálmán , HANKOVSZKY, Olga, H. , FRANK, László , BODI, Ilona , CSAK, József
发明人： ALKALOIDA VEGYÉSZETI GYAR
IPC分类号： C07D207/16
CPC分类号： C07D207/22 , C07D207/16
摘要： The 2- ADN-(2,2,5,5-tetramethyl-3-pyrrolin-3-carbonyl) BD amino derivatives are substituted on the nitrogen of the carboxamide with different aromatic heteroaromatic or aryloxy groups (which may be substituted with one or a plurality of alkyl or alkoxy groups containing from 1 to 4 atoms of carbon or with halogen atoms), with an amino group, with a diphenyl-methyl group or with a group R4-NH-CO-, wherein R4 is an aromatic group optionally substitueted with an alkyl group, preferably a substituted phenyl group. The substituents on the nitrogen atom of the carboxamide may be bound to the nitrogen atom by alkyl groups containing from 1 to 5 atoms of carbon, which may be straight or branched and which may be substituted with hydroxyl or aminocarbonyl groups. The present invention relates to the production of the overmentioned compounds by the transformation of 2,2,6,6-tetramethyl-3,5-dibromine-piperidone-4 or the salts thereof with the corresponding amines and optionally the saturation of the pyrrole cycle with hydrogen. The present invention also relates to pharmaceutical preparations usable as antiarrhythmics.

7. 发明申请

WO1992018513A1 NEW NON-HYGROSCOPIC MONO-AMMONIUM SALTS 审中-公开
标题翻译：新型非聚合单胺盐
公开(公告)号：WO1992018513A1
公开(公告)日：1992-10-29
申请号：PCT/HU1992000016
申请日：1992-04-15
申请人： ALKALOIDA VEGYÉSZETI GYAR RT.
发明人： ALKALOIDA VEGYÉSZETI GYAR RT. , POWELL, Fulgencio , LITKEI, László , GALAMB, Vilmos , GULYAS, Imre , RÉPASI, János , RÉPASINÉ VERES, Agota , VIGH, József , KOCZKA, Istvánné , FEHÉRVARI, Edit , ROKA, Lászlóné , PETHE, Lászlóné , NEU, József
IPC分类号： C07F09/38
CPC分类号： C07K14/65 , A01N57/20 , A61K38/00 , C07F9/301 , C07F9/3813
摘要： New, non-hygroscopic, crystalline mono-ammonium salts of general formula (I), where, R stands for hydroxy or alkyl; -A stands for 1-4 alkyl-amino- or amino-alkyl-groups containing primary or secondary amino-groups, preferably -CH2-NH- or -CH(NH2)-CH2-groups; B stands for ammonium, -ion, or alkyl-substituted ammonium-ion- as well as processes to obtain the same by preparing the mono-ammonium salt of general formula (I), according to any method known generally for the preparation of salts, whereby, along with avoiding other contaminations, on the course of or after salt-formation the di-ammonium salt of general formula (V), where, -R , A and B stand for the above, is eliminated or its formation is repressed. Herbicidal or plant-growth-regulating compositions containing the non-hygroscopic salts, processes for their preparation and methods of treatment of unwanted plants and weed as well as a composition consisting of a bag, which is solid and preferably flexible in its dry state, which is made of a water-soluble polymer and which contains the new substances or compositions.
摘要翻译：新的非吸湿性的通式（I）的结晶单铵盐，其中R 1代表羟基或烷基; -A代表含有伯或仲氨基，优选-CH 2 -NH-或-CH（NH 2）-CH 2 - 基团的1-4个烷基 - 氨基 - 或氨基 - 烷基 - 基团; B代表铵，-ion或烷基取代的铵离子，以及通过制备通式（I）的单铵盐，根据通常用于制备盐的任何方法获得相同的铵盐，由此，除了避免其他污染物之外，在盐形成过程中或之后，通式（V）的二铵盐（其中-R 1，A和B代表上述）被除去或形成被压制含有非吸湿盐的除草剂或植物生长调节组合物，其制备方法和治疗不想要的植物和杂草的方法以及由干燥状态下为固体并且优选柔性的袋组成的组合物，其中由水溶性聚合物制成，并含有新物质或组合物。

8. 发明申请

WO1988000197A1 BENZOPYRAN AND BENZOTHIOPYRAN DERIVATIVES AND COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：苯并噻吩和苯并噻吩衍生物及其组合物
公开(公告)号：WO1988000197A1
公开(公告)日：1988-01-14
申请号：PCT/HU1987000027
申请日：1987-06-24
申请人： ALKALOIDA VEGYÉSZETI GYAR , BOGNAR, Rezso , JASZBERÉNYI, Csaba , MAKLEIT, Sándor , FODOR, András , DEAK, Péter , TIMAR, Tibor
发明人： ALKALOIDA VEGYÉSZETI GYAR
IPC分类号： C07D517/04
CPC分类号： C07D513/04 , A01N43/90 , A01N55/00 , C07D517/04 , C07D517/14 , C07F9/6596
摘要： The compounds of general formula (I), wherein R , R , R , n, Q and Q are as defined in claim 1 as well as their biologically active salts. The invention also relates to fungicide, nematocide, acaricide, bactericide and insecticide compositions containing the compounds of general formula (I) as active ingredients as well as to the process for the preparation of these compounds and compositions.
摘要翻译：通式（I）的化合物，其中R 1，R 2，R 3，n，Q 1和Q 2如权利要求1所定义，以及它们的生物活性盐。本发明还涉及含有通式（I）的化合物作为活性成分的杀真菌剂，杀线虫剂，杀螨剂，杀菌剂和杀虫剂组合物以及制备这些化合物和组合物的方法。

9. 发明申请

WO1985003636A1 PROCESS FOR PRODUCING PHARMACEUTICAL PREPARATIONS WITH DEPOSITION EFFECT 审中-公开
标题翻译：生产具有沉积效应的药物制剂的方法
公开(公告)号：WO1985003636A1
公开(公告)日：1985-08-29
申请号：PCT/HU1985000008
申请日：1985-02-14
申请人： ALKALOIDA VEGYÉSZETI GYAR
发明人： ALKALOIDA VEGYÉSZETI GYAR , KUBALA, Ferencné , DANICSKA, István
IPC分类号： A61K09/20
CPC分类号： A61K9/2027 , A61K9/2095 , A61K9/284
摘要： Process for producing pharmaceutical preparations with deposition effect from inert polymers, characterized in that the active substance and the auxiliary materials are regularly granulated and wetted with a solution of inert polymers in organic solvents, and in that (a) the granulate is pressed into structured tablets and is heat treated, and/or in that (b) the granulate is pressed into structured tablets and surface coated with a permeable inert polymer film, the permeability of the coating being controlled with water-soluble substances.
摘要翻译：由惰性聚合物制备具有沉积效果的药物制剂的方法，其特征在于活性物质和辅助材料用有机溶剂中的惰性聚合物溶液定期造粒和润湿，并且（a）将颗粒压制成结构化片剂并且（或）（b）将颗粒压制成结构化片剂并用可渗透的惰性聚合物膜表面涂覆，涂层的渗透性被水溶性物质控制。

10. 发明申请

WO1991001315A1 NEW QUINOLINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：新的喹啉衍生物及其制备方法
公开(公告)号：WO1991001315A1
公开(公告)日：1991-02-07
申请号：PCT/HU1990000050
申请日：1990-07-20
申请人： ALKALOIDA VEGYÉSZETI GYAR , SALAMON, Zoltán , JEKO, József , IMRE, Ilona , CZELLÉR, Magdolna
发明人： ALKALOIDA VEGYÉSZETI GYAR
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The invention relates to a process for the preparation of quinoline derivatives of general formula (I), wherein R stands for hydrogen or a group of formula (II). The invention is carried out by (a) reacting a halogene-quinoline-derivative of general formula (III), wherein X stands for chlorine or bromine in the presence of alkali-t-alkylate with alpha -picoline-N-oxide of formula (IV), or (b) oxidizing a compound of formula (V).
摘要翻译：本发明涉及制备通式（I）的喹啉衍生物的方法，其中R 1代表氢或式（II）基团。本发明通过以下步骤进行：（a）使碱式烷基化物与α-甲基-3-氧化物反应，其中X 2代表氯或溴，通式（III）的卤素 - 喹啉衍生物的式（Ⅳ）化合物，或（b）氧化式（Ⅴ）化合物。

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