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1. 发明申请

WO1988002254A1 NEW PSYCHOSTIMULANT AGENT 审中-公开
标题翻译：新的PSYCHOSTIMULANT代理
公开(公告)号：WO1988002254A1
公开(公告)日：1988-04-07
申请号：PCT/HU1987000040
申请日：1987-09-25
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , KNOLL, József , SIMAY, Antal , SZINNYEI, Éva , SOMFAI, Éva , TÖRÖK, Zoltán , MOZSOLITS, Károly , BERGMANN, János
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： A61K31/135
CPC分类号： A61K31/135
摘要： Pharmaceutical composition comprising as active ingredient a compound of general Formula (I), wherein R stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms; R stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms, alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms, with the proviso that groups R and R together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the general Formula (I) by methods known per se. The compounds of the general Formula (I) are psychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficites of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.
摘要翻译：药物组合物，其包含作为活性成分的通式（I）的化合物，其中R 1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R 2代表包含1至8个碳原子的直链或支链烷基，由卤素，羟基，具有1至4个碳原子的烷氧基或1或2个苯基取代的1至8个碳原子的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少三个碳原子。本发明还涉及通过本身已知的方法制备通式（I）的化合物的方法。通式（I）的化合物是具有新的效应谱系的精神兴奋剂，其可用于治疗增加心理活动（学习和保留）和用于治疗抑郁症的学习和保留的临床模式，如阿尔茨海默病，并且没有已知的兴奋剂的副作用（例如由于儿茶酚胺释放）。

2. 发明申请

WO1997022581A1 PROCESS FOR THE PREPARATION OF PROSTAGLANDIN E1 审中-公开
标题翻译： PROSTAGLANDIN E1的制备方法
公开(公告)号：WO1997022581A1
公开(公告)日：1997-06-26
申请号：PCT/HU1996000078
申请日：1996-12-18
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , DALMADI, Gyula , HAJDU, Félix , HERMECZ, István , MOZSOLITS, Károly , SZABO, Tibor , SZEVERÉNYI, Zoltán , VAJDA, Ervin
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： New process for the preparation of prostaglandin E1 of formula (I) starting from the compound of formula (II).
摘要翻译：从式（II）化合物制备式（I）前列腺素E1的新方法。

3. 发明申请

WO1990008131A1 IMPROVED PROCESS FOR THE PREPARATION OF AMIDOXIME DERIVATIVES 审中-公开
标题翻译：改进酰胺衍生物的制备方法
公开(公告)号：WO1990008131A1
公开(公告)日：1990-07-26
申请号：PCT/HU1990000003
申请日：1990-01-10
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , BERTOK, Béla , SZÉKELY, István , THURNER, Angelika , SOMFAI, Éva , BOTAR, Sándor , GAJARY, Antal , TAKACS, Kálmán , NAGY, Lajos
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： C07C251/58
CPC分类号： C07D213/78 , C07C259/12 , C07D295/088
摘要： The invention relates to an improved process for preparing amidoxime derivatives of general formula (I), wherein R means a C2-15 group, which may be unsaturated and/or cyclic alkyl, aralkyl group or optionally substituted and/or condensed aromatic and/or heteroaromatic group; R stands for hydrogen or an optionally substituted straight or branched chain or cyclic and/or unsaturated C1-7 alkyl or aromatic group; R represents an optionally substituted straight or branched chain or cylic and/or unsaturated C1-7 alkyl or aromatic group; or R and R together with the adjacent nitrogen atom may form a 5- to 8-membered ring optionally containing other heteroatom(s); and X stands for halogen and their salts by reacting an amidoxime of general formula (II), wherein R is as defined above, in the presence of an alkaline substance, transforming the product to a salt with an acid or transforming the salt to the base, which comprises reacting the amidoxime with an alkaline metal hydroxide or alkaline metal alkoxide and dimethylformamide or 1,3-dimethyl-2-imidazolidinone, preferably in the presence of a proton source, reacting the amidoxime complex thus obtained preferably without isolation with an amine of general formula (III). The invention relates further to pure O-(2-hydroxy-piperidino-1-propil)nicotinic acid amidoxime hydrochloride and hydrobromide and O-(2-hydroxy-3-piperidino-1-propyl)nicotinic acid amidoxime base.
摘要翻译：本发明涉及一种制备通式（I）的偕胺肟衍生物的改进方法，其中R 1表示C2-15基团，其可以是不饱和和/或环状烷基，芳烷基或任选取代的和/或稠合的芳族和/或杂芳族基团; R 2代表氢或任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; R 3表示任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; 或R 2和R 3与相邻的氮原子一起可以形成任选含有其它杂原子的5-至8-元环; X代表卤素及其盐，通过在碱存在下使通式（II）的偕胺肟（其中R 1如上述定义）在酸存在下反应，将产物转化为酸或转化盐包括使偕胺肟与碱金属氢氧化物或碱金属醇盐和二甲基甲酰胺或1,3-二甲基-2-咪唑啉酮反应，优选在质子源存在下，使得到的偕胺肟配合物优选不与其分离而与通式（III）的胺。本发明还涉及纯O-（2-羟基 - 哌啶子基-1-丙基）烟酸偕胺肟盐酸盐和氢溴酸盐和O-（2-羟基-3-哌啶子基-1-丙基）烟酸偕胺肟碱。

4. 发明申请

WO1988002748A1 PROCESS FOR THE PREPARATION OF QUINOLINE-CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：制备喹喔啉羧酸衍生物的方法
公开(公告)号：WO1988002748A1
公开(公告)日：1988-04-21
申请号：PCT/HU1987000044
申请日：1987-10-14
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , FRANK, Judit , BÉRES, József, Károlyné , KULCSAR, Gábor
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： C07D215/56
CPC分类号： C07D215/56
摘要： New and simple process for the preparation of quinoline-carboxylic acid derivatives of general formula (I) as well as hydrates and therapeutically acceptable salts thereof. In the formula the meaning of the substituents is as follows: R is a hydrogen atom or a formyl group, R is a hydrogen atom or a straight or branched chain alkyl group having 1 to 4 carbon atoms, which may be substituted by a hydroxyl group, a halogen atom or an amino group; or a CH3-NH-group, R is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. According to the invention the compound of general formula (II) or an acid addition salt thereof is reacted with piperazine in dimethylformamide and - if desired - the compound of general formula (III) thus obtained is subjected to an acidic or alkaline treatment, or is reacted advantageously with hydrazine or preferably with hydrazine-hydrate.
摘要翻译：用于制备通式（I）的喹啉羧酸衍生物的新的和简单的方法以及其水合物及其治疗上可接受的盐。在该式中，取代基的含义如下：R是氢原子或甲酰基，R 1是氢原子或具有1至4个碳原子的直链或支链烷基，其可以被羟基，卤素原子或氨基; 或CH 3 -NH基，R 2是氢原子或具有1至4个碳原子的烷基。根据本发明，将通式（II）的化合物或其酸加成盐与二甲基甲酰胺中的哌嗪反应，如果需要，将所得通式（III）的化合物进行酸或碱处理，或有利地与肼反应或优选与肼水合物反应。

5. 发明申请

WO1986003939A1 PROCESS FOR ENHANCING THE ACTIVITY OF PLANT PROTECTING AGENTS BY USING CYCLODEXTRIN 审中-公开
标题翻译：通过使用环糊精提高植物保护剂活性的方法
公开(公告)号：WO1986003939A1
公开(公告)日：1986-07-17
申请号：PCT/HU1986000001
申请日：1986-01-07
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , SZEJTLI, József , KINICZKY, Márta , TÉTÉNYI, Péter , DOBOS, Éva , TÉTÉNYINÉ ERDOSI, Magda , BERNATH, Jeno , BANKYNÉ ELOD, Erzsébet
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： A01N43/16
CPC分类号： A01N47/18 , A01N25/10 , A01N43/90 , A01N47/38 , A01N43/54 , A01N43/36 , A01N2300/00
摘要： Fungicidal plant protecting composition comprising 3-90% by weight of a fungicidal active ingredient in admixture with 1-90% by weight of cyclodextrin and optionally with usual auxiliary agents. The advantage of the synergistic composition of the present invention is that identical fungicidal effect can be achieved with a significantly lower active ingredient dosage and this decreases the costs involved with the active ingredient and reduces the risks of environmental pollution as well.
摘要翻译：杀真菌植物保护组合物，其包含3-90重量％的杀真菌活性成分与1-90重量％的环糊精和任选与常规助剂混合。本发明的协同组合物的优点是可以以显着降低的活性成分剂量实现相同的杀真菌作用，并且降低了活性成分所涉及的成本并降低了环境污染的风险。

6. 发明申请

WO1990013222A1 PLANT PROTECTING PREPARATIONS, VETERINARY AND ADDITIVE PREPARATIONS 审中-公开
标题翻译：植物保护制剂，兽医和添加剂制剂
公开(公告)号：WO1990013222A1
公开(公告)日：1990-11-15
申请号：PCT/HU1990000032
申请日：1990-05-07
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , SZÉKELY, István , NAGY, Lajos , BOHUS, Péter , SZEGO, András , PAP, László , MARMAROSI, Tamásné
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： A01N25/30
CPC分类号： A01N25/30 , A61K47/14
摘要： The invention relates to a plant protecting or veterinary or additive composition, containing beside the active ingredient and other usually applied auxiliaries, such as solid and liquid carrier(s), surface active agent(s) and further additive(s), one or more surface active agent(s) of general formulae (I) or (II), or a mixture thereof, wherein R, R , R and R are independently from each other hydrogen atom, an organic or inorganic cation or a group of the general formula -(CH2-CH2-O)nR , wherein R is a C10-20 alkyl group and n is an integer from 4 to 20, with the proviso that from among the substituents R, R and R at least one is a group of the general formula (CH2-CH2O)nR .
摘要翻译：本发明涉及植物保护或兽医或添加剂组合物，除活性成分和其它通常使用的助剂外，其还包含固体和液体载体，表面活性剂和另外的添加剂，一种或多种通式（I）或（II）的表面活性剂或其混合物，其中R，R 2，R 3和R 4彼此独立地为氢原子，有机或无机阳离子或通式为 - （CH 2 -CH 2 -O）n R 1的基团，其中R 1为C 10-20烷基，n为4至20的整数，条件是从取代基R，R 2和R 3至少一个是通式（CH 2 -CH 2 O）n R 1的基团。

7. 发明申请

WO1985003293A1 PROCESS FOR PRODUCING DIACYLDIANE HYDROHEXITES 审中-公开
标题翻译：二氯乙烷水解生产工艺
公开(公告)号：WO1985003293A1
公开(公告)日：1985-08-01
申请号：PCT/HU1985000002
申请日：1985-01-16
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , SZABO, Tibor , VIDRA, Lászlóné , DALMADI, Gyula , KACZMAREK, Edwardné , ORI, János
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： C07D303/16
CPC分类号： C07D303/16
摘要： Process for producing compounds having the general formula (I) from hexites having the general formula (II) by acylation with corresponding acid anhydrides, R et R being independent from each other and representing optionally a free carboxyl group, an alkoxycarbonyl group with 2-5 atoms of carbon or a chlorine substituted alkanyl group with 1-6 atoms of carbon, an aryl group with 7-11 atoms of carbon, a cycloalkylcarbonyl group with 7-11 atoms of carbon, a 2-furanyl group or an alkylarylcarbonyl group with 8-11 atoms of carbon, and the configuration of the hexite skeleton is similar to the configuration of dulcite, mannite or idite. The process is characterized in that the acylation is carried out in the presence of catalysts having the general formula (IV), wherein R and R represent independently from each other an alkyl group comprising each 1-6 atoms of carbon or form together an alkylene group with 1-6 atoms of carbon, and can be optionally substituted by one or two dimethylamino groups.
摘要翻译：通过用相应的酸酐进行酰化从而生成具有通式（II）的己烷的具有通式（I）的化合物的方法，R 1和R 1彼此独立地表示任选的游离羧基，烷氧基羰基与 2-5个碳原子或具有1-6个碳原子的氯取代的烷基，具有7-11个碳原子的芳基，具有7-11个碳原子的环烷基羰基，2-呋喃基或烷基芳基羰基具有8-11个碳原子的碳原子，并且六元素骨架的构型类似于dulcite，mannite或idite的构型。该方法的特征在于酰化反应在具有通式（Ⅳ）的催化剂存在下进行，其中R 2和R 3彼此独立地表示包含每个1-6个碳原子的烷基或者与1-6个碳原子一起形成亚烷基，并且可以任选被一个或两个二甲基氨基取代。

8. 发明申请

WO1996012472A1 LIPOSOME COMPOSITION CONTAINING SELEGILIN 审中-公开
标题翻译：含有塞来吉林的脂肪组合物
公开(公告)号：WO1996012472A1
公开(公告)日：1996-05-02
申请号：PCT/HU1995000052
申请日：1995-10-20
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , MEZEI, Michael , GAAL, József , SZÉKACS, Gábor , SZEBENI, Gyula , MARMAROSI, Tamásné , MAGYAR, Kálmán , LENGYEL, József , SZATMARI, István , TURI, Agnes
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
IPC分类号： A61K09/127
CPC分类号： A61K31/137 , A61K9/127
摘要： This invention provides liposomic composition, containing as active ingredient (-)-N- alpha -dimethyl-N-(2-propynylphenylethylamine) (selegilin) and/or salt thereof. This composition contains: 0.1-40 % by weight of selegilin and/or a salt thereof, 2 to 40 % by weight of lipids, preferably phospholipids, 0 to 10 % by weight of cholesterol, 0 to 20 % by weight of an alcohol, 0 to 25 % by weight of a glycol, 0 to 3 % by weight of an antioxidant, 0 to 3 % by weight of a preserving agent, 0 to 2 % by weight of a viscosity influencing agent, 0 to 50 % by weight of cyclodextrin or a cyclodextrin derivative and 30 to 90 % by weight of water. This invention relates to pharmaceutical composition, containin the liposomic composition described and if desired, usual filling and diluting agents and other auxiliaries, preferably in oral, parenteral or transdermal form. This invention provides the process for the preparation of liposomic compositions containing selegilin and/or salt thereof. Accordingly liposomic composition of this invention may be administered for the treatment of Alzheimer's disease, Parkinson's disease, depression, stroke, motion sickness or myelitis.
摘要翻译：本发明提供含有作为（ - ） - N-α-二甲基-N-（2-丙炔基苯乙胺）（selegilin）和/或其盐的活性成分的脂质体组合物。该组合物包含：0.1-40重量％的赛莱格林和/或其盐，2至40重量％的脂质，优选磷脂，0至10重量％的胆固醇，0至20重量％的醇， 0〜25重量％的二醇，0〜3重量％的抗氧化剂，0〜3重量％的防腐剂，0〜2重量％的粘度影响剂，0〜50重量％环糊精或环糊精衍生物和30〜90重量％的水。本发明涉及药物组合物，所述药物组合物包含所述的脂质体组合物，如果需要，含有通常的填充和稀释剂和其它助剂，优选口服，肠胃外或透皮形式。本发明提供了制备含有塞来林和/或其盐的脂质体组合物的方法。因此，本发明的脂质体组合物可以用于治疗阿尔茨海默氏病，帕金森病，抑郁症，中风，运动病或脊髓炎。

9. 发明申请

WO1990015795A1 NEW PROCESS FOR THE PREPARATION OF PHENYL-GUANIDINE DERIVATIVES 审中-公开
标题翻译：制备苯丙氨酸衍生物的新方法
公开(公告)号：WO1990015795A1
公开(公告)日：1990-12-27
申请号：PCT/HU1990000040
申请日：1990-06-21
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , HUSZAR, Csaba , SPERBER, Ferenc , NÉMETH, Attila , SARKÖZI, Péter , SOMFAI, Éva , PALI, Lajosné
IPC分类号： C07C323/43
CPC分类号： C07C319/20 , C07C315/04 , C07C381/14 , C07C317/42 , C07C323/44
摘要： The invention relates to a process for the preparation of guanidine-derivatives of general formula (I), wherein R means a C1-4 alkyl group, M means a hydrogenatom, sodium-, potassium-, or calcium ion, A means an -S-, -SO-, or -SO2-group; in a way, that thiocarbamide derivatives of general formula (II) are oxidized optionally in the presence of an inorganic or organic solvent and the sulfonic acid derivative of general formula (III) obtained is reacted with an aniline derivative of general formula (IV) optionally in the presence of an inorganic or organic solvent.
摘要翻译：本发明涉及制备通式（I）的胍衍生物的方法，其中R表示C 1-4烷基，M表示氢原子，钠离子，钾离子或钙离子，A表示-S - ， - SO-或-SO 2 - 基团; 在某种程度上，通式（II）的硫代氨基甲酸酯衍生物任选在无机或有机溶剂的存在下被氧化，所得通式（III）的磺酸衍生物与通式（Ⅳ）的苯胺衍生物任选地反应在无机或有机溶剂的存在下。

10. 发明申请

WO1989000380A1 PLANT-PROTECTIVE COMPOSITION 审中-公开
标题翻译：植物保护组合物
公开(公告)号：WO1989000380A1
公开(公告)日：1989-01-26
申请号：PCT/HU1988000050
申请日：1988-07-15
申请人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT
发明人： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT , DETRE, Tamás , ANGYAN, Sándor , PAPP, László , SZEGO, András , KARADI, Zoltán , BERTUSNÉ BENDE, Klára , MARMAROSINÉ KELLNER, Katalin
IPC分类号： A01N25/02
CPC分类号： A01N25/02 , A01N25/04 , Y10S514/918 , Y10S514/936 , Y10S514/937 , Y10S514/942 , Y10S514/95 , Y10S514/97 , Y10S514/973
摘要： The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s), 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules. The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 mum, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.5 % by weight of a commonly used additive such as anionic and/or nonionic surface active agents, macromolecules and water in an amount supplementing up to 100 % by weight.

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