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1. 发明申请

US20070066835A1 Process for the synthesis of amorphous atorvastain calcium 审中-公开
标题翻译：合成无定形阿托伐他汀钙的方法
公开(公告)号：US20070066835A1
公开(公告)日：2007-03-22
申请号：US10550415
申请日：2004-03-23
申请人： Laszlo Czibula , Laszlo Dobay , Eva Papp , Ida Juhasz , Sandorne Balint
发明人： Laszlo Czibula , Laszlo Dobay , Eva Papp , Ida Juhasz , Sandorne Balint
IPC分类号： C07D207/337
CPC分类号： C07D207/34
摘要： The invention relates to a new process for the synthesis of amorphous atorvastatin calcium, which consists of dissolving the salt of the formula (I) of atorvastatin acid formed with a basic amino acid (I); in a mixture of water and a water miscible organic solvent, adding an aqueous solution of a water soluble calcium salt to the solution and isolating the so obtained entirely amorphous atorvastatin calcium of high purity by filtration.
摘要翻译：本发明涉及一种合成无定形阿托伐他汀钙的新方法，其由将碱性氨基酸（I）形成的阿托伐他汀酸的式（I）的盐溶解而成。在水和水混溶性有机溶剂的混合物中，向溶液中加入水溶性钙盐水溶液，并通过过滤分离所得到的完全无定形的阿托伐他汀钙。

2. 发明授权

US4762944A Butenoic acid derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：丁烯酸衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US4762944A
公开(公告)日：1988-08-09
申请号：US25339
申请日：1987-03-13
申请人： Janos Fischer , Laszlo Dobay , Elemer Ezer , Judit Matuz , Laszlo Szporny , Tibor Wagner
发明人： Janos Fischer , Laszlo Dobay , Elemer Ezer , Judit Matuz , Laszlo Szporny , Tibor Wagner
IPC分类号： A61K31/215 , A61P1/04 , A61P43/00 , C07C69/00 , C07C69/738 , C07C69/76
CPC分类号： A61K31/215 , C07C69/00 , C07C69/738
摘要： The invention relates to novel butenoic acid derivatives of the general formula (Ia) having E-configuration ##STR1## as well as to their Z-izomers of the general formula ##STR2## wherein R stands for a (-)-menthyl or a (+)-menthyl group. as well as pharmaceutical compositions containing these compounds.The novel butenoic acid derivatives of the general formulae (Ia) and (Ib) possess valuable pharmacological properties, mainly gastric cytoprotective effect.

3. 发明申请

US20090270630A1 PROCESS FOR THE SYNTHESIS OF BENZYLIDENE ROSIGLITAZONE BASE 审中-公开
标题翻译：苯并噻唑基合成方法
公开(公告)号：US20090270630A1
公开(公告)日：2009-10-29
申请号：US12302127
申请日：2007-06-21
申请人： Laszlo Czibula , Ferenc Sebok , Laszlo Dobay , Eva Werkne Papp , Ida Deutschne Juhasz , Judit Nagyne Bagdy , Tamasne Uberhardt
发明人： Laszlo Czibula , Ferenc Sebok , Laszlo Dobay , Eva Werkne Papp , Ida Deutschne Juhasz , Judit Nagyne Bagdy , Tamasne Uberhardt
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Process for the synthesis of 5-{4-[N-methyl-N-(2-pyridyl)-amino-ethoxy]-benzylidene}-thiazolidine-2,4-dione (INN name: benzylidene-rosiglitazone) of formula (I), which consist of the following steps: Step a) reaction of 2-chloro-pyridine and 2-(N-methylamino)-ethanol Step b) reaction of the obtained compound of formula (III) with 4-fluorobenzaldehyde Step c) reaction of the obtained compound of formula (IV) with thiazolidine-2,4-dione characterized by dissolving 4-{2-[N-methyl-N-(2-pyridyl)amino]-ethanol of formula (III) obtained in Step a) in toluene and using it in Step b) without isolation; reacting the solution of compound of formula (III) in toluene in Step b) with 4-fluorobenzaldehyde in the presence of aqueous alkali hydroxide solution and phase transfer catalyst at 25-50° C.; reacting the solution of the benzaldehyde derivative of formula (IV) obtained in Step b) in toluene in Step c) and isolating the desired product.
摘要翻译：合成式（I）的5- {4- [N-甲基-N-（2-吡啶基） - 氨基 - 乙氧基] - 亚苄基} - 噻唑烷-2,4-二酮（INN名称：亚苄基 - 罗格列酮）），其步骤如下：步骤a）2-氯 - 吡啶和2-（N-甲基氨基） - 乙醇的反应步骤b）将所得到的式（III）化合物与4-氟苯甲醛反应步骤c）反应所得到的式（Ⅳ）化合物与噻唑烷-2,4-二酮的特征在于将步骤a中获得的式（Ⅳ）的4- {2- [N-甲基-N-（2-吡啶基）氨基] - 乙醇）并在步骤b）中使用它而不分离; 使步骤b）中式（III）化合物在甲苯中的溶液与4-氟苯甲醛在碱金属氢氧化物水溶液和相转移催化剂存在下，在25-50℃下反应。使步骤b）中获得的式（IV）的苯甲醛衍生物在步骤c）中的甲苯中的溶液反应，并分离所需产物。

4. 发明授权

US4725617A Alkylamino-furanon-derivatives 失效
标题翻译：烷基氨基 - 呋喃酮衍生物
公开(公告)号：US4725617A
公开(公告)日：1988-02-16
申请号：US828011
申请日：1986-02-10
申请人： Tamas Fodor , Laszlo Dobay , Janos Fischer , Bela Stefko , Bela Kiss , Zsolt Szombathelyi , Egon Karpati , Istvan Laszlovszky , Laszlo Szporny
发明人： Tamas Fodor , Laszlo Dobay , Janos Fischer , Bela Stefko , Bela Kiss , Zsolt Szombathelyi , Egon Karpati , Istvan Laszlovszky , Laszlo Szporny
IPC分类号： C07K14/81 , A61K38/00 , A61P9/12 , A61P27/02 , A61P27/06 , C07K1/113 , C07K5/02 , C07K5/06 , A61K31/395 , C07D207/09
CPC分类号： C07K5/0222 , A61K38/00 , Y02P20/55
摘要： The present invention relates to a compound of the formula (I) ##STR1## wherein R.sup.1 stands for methyl or a group of the formula R.sup.3 --NH--(CH.sub.2).sub.4 --wherein R.sup.3 is hydrogen or a protective group being compatible with the peptide bond,R.sup.2 represents hydrogen, a protective group being compatible with the peptide bond or a cation derived from an organic or inorganic basethe pharmaceutically acceptable salts and diastereomers thereof.The compounds of the invention are useful for inhibiting the effect of the angiotensin converting ensime and they can be used in the therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.
摘要翻译：本发明涉及式（I）化合物（I）其中R1代表甲基或式R3-NH-（CH2）4-基团，其中R3是氢或保护基与肽键，R2表示氢，与肽键相容的保护基或衍生自有机或无机碱的阳离子，其药学上可接受的盐和非对映异构体。本发明的化合物可用于抑制血管紧张素转化酶的作用，可用于作为降血压剂的治疗和用于治疗心脏衰竭和青光眼。

5. 发明授权

US06596874B1 Process for preparing amlodipine benzenesulphonate 有权
标题翻译：苯磺酸氨氯地平的制备方法
公开(公告)号：US06596874B1
公开(公告)日：2003-07-22
申请号：US10019424
申请日：2001-12-20
申请人： Janos Fischer , Katalin Szöke , Laszlo Dobay , Sandor Leval
发明人： Janos Fischer , Katalin Szöke , Laszlo Dobay , Sandor Leval
IPC分类号： C07D21344
CPC分类号： C07D211/90
摘要： The invention relates to a novel process of amalodipine benzenesulphonate of formula (I) by reacting a new 2-[/2-carboxy-benzoyl)-aminoethoxy/methyl/]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-di-hydropyridine derivative of general formula (II) wherein X represents hydrogen or alkali metal or alkali earth metal or quaternary ammonium—with benzenesulphonic acid.
摘要翻译：本发明涉及通过使新的2 - [（2-羧基 - 苯甲酰基） - 氨基乙氧基/甲基] -4-（2-氯苯基）-3-乙氧基羰基-5- 其中X表示氢或碱金属或碱土金属或季铵与苯磺酸的通式（II）的甲氧基羰基-6-甲基-1,4-二氢吡啶衍生物。

6. 发明授权

US5214045A Amino acid containing acrylamide derivatives for ulcer prevention or treatment 失效
标题翻译：用于防止或治疗尿酸的含有丙烯酰胺衍生物的氨基酸
公开(公告)号：US5214045A
公开(公告)日：1993-05-25
申请号：US551518
申请日：1990-07-11
申请人： Tamas Fodor , Janos Fischer , Laszlo Dobay , Elemer Ezer , Judit Matuz , Laszlo Szporny , Gyorgy Hajos
发明人： Tamas Fodor , Janos Fischer , Laszlo Dobay , Elemer Ezer , Judit Matuz , Laszlo Szporny , Gyorgy Hajos
IPC分类号： A61K31/16 , A61K31/10 , A61K31/195 , A61K31/255 , A61K31/425 , A61K31/426 , A61P1/04 , C07C317/32 , C07C317/44 , C07C323/32 , C07C323/54 , C07C323/60 , C07D207/16 , C07D277/06 , C07D295/16 , C07D295/18 , C07D295/185 , C07D295/20
CPC分类号： C07D295/185 , C07C317/44 , C07C323/54 , C07D207/16
摘要： Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.

7. 发明授权

US4879404A Novel salicylates, their salts, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：新型水杨酸盐，其盐，含有它们的药物组合物及其制备方法
公开(公告)号：US4879404A
公开(公告)日：1989-11-07
申请号：US248970
申请日：1988-09-26
申请人： Janos Fischer , Laszlo Dobay , Mihaly Major , Elemer Ezer , Judit Matuz , Katalin Saghy , Gyorgy Hajos , Laszlo Szporny
发明人： Janos Fischer , Laszlo Dobay , Mihaly Major , Elemer Ezer , Judit Matuz , Katalin Saghy , Gyorgy Hajos , Laszlo Szporny
IPC分类号： C07C69/738 , C07C59/84 , C07C67/08 , C07C69/86 , C07C69/90
CPC分类号： C07C69/738 , Y02P20/55
摘要： The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or a C.sub.1-4 acylamino group; andR.sup.1 is hydrogen or a carboxyl-protective group or E and/or Z configuration as well as their salts.The compounds according to the invention show a cytoprotecive effect and in addition, a valuable anti-inflammatory action. Their toxicity is low.

8. 发明授权

US07625935B2 High purity butoconazole nitrate with specified particle size and a process for the preparation thereof 有权
标题翻译：具有规定粒径的高纯度布康康硝酸盐及其制备方法
公开(公告)号：US07625935B2
公开(公告)日：2009-12-01
申请号：US10584662
申请日：2005-01-25
申请人： Laszlo Czibula , Laszlo Dobay , Eva Werkne Papp , Judit Nagyne Bagdy , Ferenc Sebok
发明人： Laszlo Czibula , Laszlo Dobay , Eva Werkne Papp , Judit Nagyne Bagdy , Ferenc Sebok
IPC分类号： A61K31/4174 , C07D233/56
CPC分类号： C07D233/60
摘要： One object of the invention is high purity butoconazole nitrate of the formula (I) (I) containing maximum 0.1 wt % of chemical impurities, wherein at least 95% of the particles of the substance are below 75 μm by diameter, whereas at least 99% of the particles are below 250 μm by diameter, and process for its preparation. A pharmaceutical composition comprising as active ingredient, high purity butoconazole nitrate of specified particle size in admixture with known auxiliaries is also within the scope of the invention.
摘要翻译：本发明的一个目的是含有最多0.1重量％化学杂质的式（I）（I）的高纯度布康唑硝酸盐，其中物质的至少95％的颗粒直径小于75μm，而至少99 颗粒的百分比直径小于250毫米，其制备方法。包含与已知助剂混合的具有特定粒度的高纯度丁苯康唑硝酸盐作为活性成分的药物组合物也在本发明的范围内。

9. 发明申请

US20080221190A1 High Purity Butoconazole Nitrate with Specified Particle Size and a Process for the Preparation Thereof 有权
标题翻译：具有指定粒径的高纯度Butoconazole硝酸盐及其制备方法
公开(公告)号：US20080221190A1
公开(公告)日：2008-09-11
申请号：US10584662
申请日：2005-01-25
申请人： Laszlo Czibula , Laszlo Dobay , Eva Werkne Papp , Judit Nagyne Bagdy , Ferenc Sebok
发明人： Laszlo Czibula , Laszlo Dobay , Eva Werkne Papp , Judit Nagyne Bagdy , Ferenc Sebok
IPC分类号： C07D233/60 , A61K31/4174 , A61P31/00
CPC分类号： C07D233/60
摘要： One object of the invention is high purity butoconazole nitrate of the formula (I) (I) containing maximum 0.1 wt % of chemical impurities, wherein at least 95% of the particles of the substance are below 75pm by diameter, whereas at least 99% of the particles are below 250 μm by diameter, and process for its preparation. A pharmaceutical composition comprising as active ingredient, high purity butoconazole nitrate of specified particle size in admixture with known auxiliaries is also within the scope of
摘要翻译：本发明的一个目的是含有最多0.1重量％化学杂质的式（I）（I）的高纯度布康唑硝酸盐，其中该物质的至少95％的颗粒直径低于75μm，而至少99％的颗粒直径小于250毫米，其制备方法。含有与已知助剂混合的具有规定粒度的高纯度布康唑硝酸盐作为活性成分的药物组合物也在

10. 发明授权

US06657062B1 N-benzylpiperidine and tetrahydropyridine derivatives 有权
标题翻译： N-苄基哌啶和四氢吡啶衍生物
公开(公告)号：US06657062B1
公开(公告)日：2003-12-02
申请号：US09214099
申请日：1998-12-28
申请人： Janos Kreidl , Laszlo Czibula , Andras Nemes , Ida Deutschne Juhasz , Eva Werkne Papp , Juidit Nagyne Bagdy , Laszlo Dobay , Istvan Hegedus , Kalman Harsanyi , Istvan Borza
发明人： Janos Kreidl , Laszlo Czibula , Andras Nemes , Ida Deutschne Juhasz , Eva Werkne Papp , Juidit Nagyne Bagdy , Laszlo Dobay , Istvan Hegedus , Kalman Harsanyi , Istvan Borza
IPC分类号： C07D21118
CPC分类号： C07D405/12 , C07D211/22 , C07D211/70
摘要： A process is disclosed for the preparation of compounds of the formula (I), which compounds are useful as intermediates for the preparation of paroxetine of formula(V).
摘要翻译：公开了制备式（I）化合物的方法，该化合物可用作制备式（V）的帕罗西汀的中间体。

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