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1. 发明申请

WO2005023818A2 HETEROBICYCLIC COMPOUNDS AS PHARMACEUTICALLY ACTIVE AGENTS 审中-公开
标题翻译：作为药物活性剂的杂环化合物
公开(公告)号：WO2005023818A2
公开(公告)日：2005-03-17
申请号：PCT/EP2004/010161
申请日：2004-09-10
申请人： AXXIMA PHARMACEUTICALS AG , KOUL, Anil , KLEBL, Bert , MÜLLER, Gerhard , MISSIO, Andrea , SCHWAB, Wilfried , HAFENBRADL, Doris , NEUMANN, Lars , SOMMER, Marc-Nicola , MÜLLER, Stefan , HOPPE, Edmund , FREISLEBEN, Achim , BACKES, Alexander , HARTUNG, Christian , FELBER, Beatrice , ZECH, Birgit , ENGKVIST, Ola , KERI, György , ÖRFI, Laszlo , BANHEGYI, Peter , GREFF, Zoltan , HORVÁTH, Zoltán , VARGA, Zoltán , MARKO, Péter , PATÓ, Jànos , SZABADKAI, István , SZÉKELYHIDI, Zsolt , WÁCZEK, Frigyes
发明人： KOUL, Anil , KLEBL, Bert , MÜLLER, Gerhard , MISSIO, Andrea , SCHWAB, Wilfried , HAFENBRADL, Doris , NEUMANN, Lars , SOMMER, Marc-Nicola , MÜLLER, Stefan , HOPPE, Edmund , FREISLEBEN, Achim , BACKES, Alexander , HARTUNG, Christian , FELBER, Beatrice , ZECH, Birgit , ENGKVIST, Ola , KERI, György , ÖRFI, Laszlo , BANHEGYI, Peter , GREFF, Zoltan , HORVÁTH, Zoltán , VARGA, Zoltán , MARKO, Péter , PATÓ, Jànos , SZABADKAI, István , SZÉKELYHIDI, Zsolt , WÁCZEK, Frigyes
IPC分类号： C07D495/00
CPC分类号： C07D409/12 , C07D209/42 , C07D333/66 , C07D333/68 , C07D491/04 , C07D493/04 , C07D495/04 , C07D495/10
摘要： Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
摘要翻译：描述了杂双环化合物，例如4,5,6,7-四氢＆shy;苯并[b]噻吩-3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3- C]噻喃＆害羞; 3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸酰胺或苯并[b]噻吩-3-羧酸酰胺及其药学上可接受的盐，其用途这些衍生物用于预防和/或治疗各种疾病，如感染性疾病，包括分枝杆菌和害羞;诱导感染和机会性疾病，朊病毒疾病，免疫性疾病，自身免疫性疾病，双相性和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经退行性疾病和中风，以及含有至少一种杂双环化合物和/或其药学上可接受的盐的组合物。此外，公开了用于合成杂双环化合物的反应程序。

2. 发明申请

WO2002094796A3 BENZO[G]QUINOXALINE DERIVATIVES AS EFFECTIVE COMPOUNDS AGAINST INFECTIOUS DISEASES 审中-公开
公开(公告)号：WO2002094796A3
公开(公告)日：2002-11-28
申请号：PCT/EP2002/005573
申请日：2002-05-21
申请人： AXXIMA PHARMACEUTICALS AG , PATÓ, János , KÉRI, György , ÖRFI, László , WÁCZEK, Frigyes , HORVÁTH, Zoltán , BÁNHEGYI, Péter , SZABADKAI, István , MAROSFALVI, Jenö , HEGYMEGI-BARAKONYI, Bálint , SZÉKELYHIDI, Zsolt , GREFF, Zoltán , CHOIDAS, Axel , BACHER, Gerald , DAUB, Henrik , OBERT, Sabine , KURTENBACH, Alexander , HABENBERGER, Peter
发明人： PATÓ, János , KÉRI, György , ÖRFI, László , WÁCZEK, Frigyes , HORVÁTH, Zoltán , BÁNHEGYI, Péter , SZABADKAI, István , MAROSFALVI, Jenö , HEGYMEGI-BARAKONYI, Bálint , SZÉKELYHIDI, Zsolt , GREFF, Zoltán , CHOIDAS, Axel , BACHER, Gerald , DAUB, Henrik , OBERT, Sabine , KURTENBACH, Alexander , HABENBERGER, Peter
IPC分类号： C07D241/38
摘要： The present invention relates to benzo[g]quinoxaline derivatives of the general formula (I), processes for manufacturing said benzo[g]quinoxaline derivatives, the use of the benzo[g]quinoxaline derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases and opportunistic infections, diabetes, cancer, inflammation, as well as compositions containing at least one benzo[g]quinoxaline derivative and/or pharmaceutically acceptable salt thereof. Further, the present invention is directed to methods for preventing and/or treating of infectious diseases, diabetes, cancer, and inflammation using the inventive benzo[g]quinoxaline derivatives.

3. 发明申请

WO2002094796A2 BENZO[G]QUINOXALINE DERIVATIVES AS EFFECTIVE COMPOUNDS AGAINST INFECTIOUS DISEASES 审中-公开
标题翻译：苯并[G]喹啉衍生物作为有效的化合物对抗感染性疾病
公开(公告)号：WO2002094796A2
公开(公告)日：2002-11-28
申请号：PCT/EP2002/005573
申请日：2002-05-21
申请人： AXXIMA PHARMACEUTICALS AG , PATÓ, János , KÉRI, György , ÖRFI, László , WÁCZEK, Frigyes , HORVÁTH, Zoltán , BÁNHEGYI, Péter , SZABADKAI, István , MAROSFALVI, Jenö , HEGYMEGI-BARAKONYI, Bálint , SZÉKELYHIDI, Zsolt , GREFF, Zoltán , CHOIDAS, Axel , BACHER, Gerald , DAUB, Henrik , OBERT, Sabine , KURTENBACH, Alexander , HABENBERGER, Peter
发明人： PATÓ, János , KÉRI, György , ÖRFI, László , WÁCZEK, Frigyes , HORVÁTH, Zoltán , BÁNHEGYI, Péter , SZABADKAI, István , MAROSFALVI, Jenö , HEGYMEGI-BARAKONYI, Bálint , SZÉKELYHIDI, Zsolt , GREFF, Zoltán , CHOIDAS, Axel , BACHER, Gerald , DAUB, Henrik , OBERT, Sabine , KURTENBACH, Alexander , HABENBERGER, Peter
IPC分类号： C07D241/00
CPC分类号： C07D241/38 , C07D231/12 , C07D233/56 , C07D241/52 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D513/14
摘要： The present invention relates to benzo[g]quinoxaline derivatives of the general formula (I), processes for manufacturing said benzo[g]quinoxaline derivatives, the use of the benzo[g]quinoxaline derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases and opportunistic infections, diabetes, cancer, inflammation, as well as compositions containing at least one benzo[g]quinoxaline derivative and/or pharmaceutically acceptable salt thereof. Further, the present invention is directed to methods for preventing and/or treating of infectious diseases, diabetes, cancer, and inflammation using the inventive benzo[g]quinoxaline derivatives.
摘要翻译：本发明涉及通式（I）的苯并[g]喹喔啉衍生物，制备所述苯并[g]喹喔啉衍生物的方法，使用苯并[g]喹喔啉衍生物作为药物活性剂，特别是用于预防和 /或治疗感染性疾病和机会性感染，糖尿病，癌症，炎症，以及含有至少一种苯并[g]喹喔啉衍生物和/或其药学上可接受的盐的组合物。此外，本发明涉及使用本发明的苯并[g]喹喔啉衍生物预防和/或治疗感染性疾病，糖尿病，癌症和炎症的方法。

4. 发明申请

WO2005088957A1 METHOD AND ARRANGEMENT FOR IMAGING A PRIMARILY TWO-DIMENSIONAL TARGET 审中-公开
标题翻译：用于成像一个二维目标的方法和装置
公开(公告)号：WO2005088957A1
公开(公告)日：2005-09-22
申请号：PCT/IB2005/050789
申请日：2005-03-03
申请人： HORVÁTH, Zoltán , VIRÁG, Tibor
发明人： HORVÁTH, Zoltán , VIRÁG, Tibor
IPC分类号： H04N1/195
CPC分类号： H04N1/195 , H04N1/04 , H04N2201/0434
摘要： To imaging a two-dimensional target (T) and ensuring primarily scanning, photography and digitalization of the whole surface of book-pages in a way that the expensive or museum piece book needs to be opened at a relatively little angle of slightly exceeding 45°, a method is proposed comprising the steps of matching at least one optical unit adapted for influencing the direction of rays of light falling onto it with the target (T), illuminating the target (T) while directing an optical recording means to the optical unit and turning away the optical recording means and displacing in a receding manner from the plane of the target (T) at a predetermined angle α in a curved course compared to the optical axis (OA) originating from the centre of the target (T) while tilting a mirror (M) half to the extent of said displacement - i.e. with an angle α/2 - of the optical recording means, and mapping the pixels of the target (T) reaching the optical recording means through the optical unit by projecting the rays originating from the pixels of the target (T) at right angles to the target (T) through the optical unit to sensor means of the optical recording means in the whole range of the optical angle of the optical recording means.
摘要翻译：为了对二维目标（T）进行成像，并确保以书页的整个表面的主要扫描，摄影和数字化方式，使得昂贵的或博物馆的书需要以略超过45°的相对小的角度打开提出了一种方法，其包括以下步骤：将至少一个适于影响其上的光线的方向的光学单元与目标（T）匹配，同时将光学记录装置引导到光学单元并且与来自目标（T）的中心的光轴（OA）相比，在弯曲的过程中以预定角度α从目标（T）的平面以后退方式离开光学记录装置并且以后退方式移位，同时将镜子（M）倾斜一半到所述位移的程度（即，具有光学记录装置的角度α/ 2），并且通过光学u映射到达光学记录装置的目标（T）的像素在光记录装置的光学角度的整个范围内，通过光学单元将来自目标（T）的像素的射线与目标（T）成直角投影到光学记录装置的传感器装置。

5. 发明申请

WO2006117578A1 PROCESS AND APPARATUS FOR HEAT TRANSFER 审中-公开
标题翻译：加热和加热装置
公开(公告)号：WO2006117578A1
公开(公告)日：2006-11-09
申请号：PCT/HU2006/000030
申请日：2006-04-21
申请人： DR-PACK II. KFT , PELCZ, Antal , ILLÉS, Tamás , HORVÁTH, Zoltán , SIMON, László
发明人： PELCZ, Antal , ILLÉS, Tamás , HORVÁTH, Zoltán , SIMON, László
IPC分类号： B29C47/88
CPC分类号： B29C47/8825 , B29C47/0021 , B29C47/0026
摘要： Process for heat transfer between a solid object and a material layer, comprising the steps of: a) arranging a heat-discharging surface from a heat-receiving surface at a gap (R) for the flow (4); b) generating a speed difference between said surfaces by providing a relative movement thereof; c) increasing the speed (v l ) of the flow (4) in the gap (R) compared to the speed of these surfaces (v H and/or v F ) by means of said speed difference; d) maintaining a turbulent flow (4) in the gap (R) and carrying out the heat transfer by this flow (4). In the apparatus, the heat-receiving surface of the solid object (H) is formed on a structural part, e.g. rotor (2), which is relatively movably arranged in a housing (3) compared to the heat-discharging material layer (F). It is provided with a heat-removing unit and/or a heating unit.
摘要翻译：在固体物料与材料层之间进行热传递的方法，包括以下步骤：a）在所述流动（4）的间隙（R）处从受热表面设置放热表面; b）通过提供其相对运动而在所述表面之间产生速度差; c）增加间隙（R）中的流（4）的速度（v 1 L 1）与这些表面的速度（v H H H和/ SUB> F ）; d）在间隙（R）中保持湍流（4）并且通过该流（4）进行热传递。在该装置中，固体物体（H）的受热面形成在结构部件上。转子（2），其与散热材料层（F）相比可相对移动地布置在壳体（3）中。设有散热单元和/或加热单元。

6. 发明申请

WO2003093588A1 ARRANGEMENT FOR ONE-ARMED BATTERIES PROVIDED WITH ELECTROMAGNETIC SHUT-OFF VALVE 审中-公开
标题翻译：电动关闭阀提供的单臂电池的安装
公开(公告)号：WO2003093588A1
公开(公告)日：2003-11-13
申请号：PCT/HU2003/000032
申请日：2003-04-25
申请人： KEROX MULTIPOLÁR II. IPARI ÉS KERESKEDELMI KFT. , HORVÁTH, Zoltán
发明人： HORVÁTH, Zoltán
IPC分类号： E03C1/05
CPC分类号： E03C1/057
摘要： The invention relates to one-armed batteries provided with an electromagnetic shut-off valve, comprising a cartridge for controlling the amount and ratio of the cold and warm water. The inlet holes for the cold and warm water, and the outlet hole for the mixed water are on the bottom plane of the cartridge, whereas at the upper part the operating element of the battery arm is situated. The essence of the invention is that a socket (7) is fitted to the bottom of the cartridge (8), the jacket of said body has two seals (20). Three channels (13, 14, 15) are formed in the socket (7). The channel (15) connected to the outlet hole (10) enters a window (11) cut into the jacket between the seals (20), whereas the channels (13, 14) connected to the inlet holes interconnect the two front planes (12, 16) of the socket (7). The window (11) is in a water transporting connection with the outlet tube (6), whereas the channels connected to the inlet holes are connected with the network water mains transporting the cold and warm water. In the socket (7), opposite to the channel (15) opening into the window (11), there is a nest, where an electromagnetic valve unit (18) is fixed from the opposite side of the cartridge (8), which reaches through the window (11) and is fitted to the channel (15).
摘要翻译：本发明涉及具有电磁截止阀的单臂电池，其包括用于控制冷水和暖水的量和比例的盒。用于冷和暖水的入口孔和用于混合水的出口孔在盒的底部平面上，而在上部，电池臂的操作元件位于其上。本发明的实质是将插座（7）装配到盒（8）的底部，所述主体的护套具有两个密封件（20）。三个通道（13,14,15）形成在插座（7）中。连接到出口孔（10）的通道（15）进入在密封件（20）之间切入护套的窗口（11），而连接到入口孔的通道（13,14）将两个前平面（12 ，16）。窗口（11）与出口管（6）处于水输送连接中，而连接到入口孔的通道与运送冷热水的网络水管连接。在插座（7）中，与通向窗口（11）的通道（15）相对的是一个嵌套，其中电磁阀单元（18）从盒（8）的相对侧被固定，通过窗口（11）并且安装到通道（15）。

7. 发明申请

WO2011132008A2 CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：控制释放药物组合物
公开(公告)号：WO2011132008A2
公开(公告)日：2011-10-27
申请号：PCT/HU2011/000037
申请日：2011-04-21
申请人： EGIS Gyűgyszergyár Nyilvánosan Múködő Részvény társaság , KORBÉLY, Tibor , ZSIGMOND, Zsolt , UJFALUSSY, György , PÁLFI, Zoltánné , HORVÁTH, Zoltán , ORBÁN, Ádám , ÁBRAHÁM, Krisztina , BOKOR, Zsolt, Istavánné
发明人： KORBÉLY, Tibor , ZSIGMOND, Zsolt , UJFALUSSY, György , PÁLFI, Zoltánné , HORVÁTH, Zoltán , ORBÁN, Ádám , ÁBRAHÁM, Krisztina , BOKOR, Zsolt, Istavánné
IPC分类号： A61K31/554
CPC分类号： A61K31/554 , A61K9/2081 , A61K9/5026 , A61K9/5047
摘要： The present invention relates to a sustained release pharmaceutical composition. Particularly, a sustained release compressed tablet which contains coated compacted granules containing the active ingredient quetiapine and further excipients. If desired, one or more coatings are on the surface of the tablet.
摘要翻译：本发明涉及缓释药物组合物。特别地，包含含有活性成分喹硫平和其它赋形剂的包被的压实颗粒的缓释压制片剂。如果需要，片剂表面上有一层或多层涂层。

8. 发明申请

WO2009001148A2 INDUSTRIAL METHOD FOR THE SYNTHESIS OF 17-ACETOXY-11β-[4-(DIMETHYLAMINO)-PHENYL]-21-METHOXY-19-NORPREGNA-4,9-DIEN-3,20-DIONE AND THE KEY INTERMEDIATES OF THE PROCESS 审中-公开
标题翻译：合成17-乙酰基-11β-[4-（二甲基氨基）苯基] -2-甲氧基-19-壬基-4,9-二烯-3,20-二酮的工业方法及其工艺的主要中间体
公开(公告)号：WO2009001148A2
公开(公告)日：2008-12-31
申请号：PCT/HU2008/000073
申请日：2008-06-19
申请人： RICHTER GEDEON NYRT. , BÓDI, József , VISKY, György , SZÉLES, János , MAHÓ, Sándor , SÁNTA, Csaba , CSÖRGEI, János , TUBA, Zoltán , TERDY, László , MOLNÁR, Csaba , ARANYI, Antal , HORVÁTH, Zoltán , BALOGH, Gábor
发明人： BÓDI, József , VISKY, György , SZÉLES, János , MAHÓ, Sándor , SÁNTA, Csaba , CSÖRGEI, János , TUBA, Zoltán , TERDY, László , MOLNÁR, Csaba , ARANYI, Antal , HORVÁTH, Zoltán , BALOGH, Gábor
CPC分类号： C07J41/0083 , C07J21/006 , C07J41/0094 , C07J51/00 , Y02P20/55
摘要： The present invention relates to a process for the synthesis of the known 17-acetoxy-11-β-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(l l)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones. The process according to the invention is the following: i) formation of an epoxide on the double bond in position 5(10) of 3,3-[l,2-ethandiyl- bis(oxy)]-oestr-5(10),9(l l)-dien-17-one of formula (II) with hydrogen peroxide; ii) addition of hydrogen cyanide formed in situ on position 17 of the obtained 5,10α- epoxy-3,3-[l,2-ethandiyl-bis(oxy)]-5α-oestr-9(l l)-en-17-one of formula (III); iii) silylation of the hydroxyl group in position 17 of the formed 5,10α-epoxy-3,3-[l,2- ethandiyl-bis(oxy)]-17α-hydroxy-5α-oestr-9(l l)-en-17β-carbonitrile of formula (IV) with trimethyl chlorosilane; iv) reacting the obtained 5,10α-epoxy-3,3-[l,2-ethandiyl-bis(oxy)]-17-[trimethyl-silyl-oxy]-5α-oestr-9(l l)-en-17β-carbonitrile of formula (V) with 4-(dimethylamino)-phenyl magnesium bromide Grignard reagent in the presence of CuCl (Teutsch reaction); v) silylation of the hydroxyl group in position 5 of the formed l lβ-[4-(dimethyl-amino)-phenyl] -3,3 - [1,2-ethandiyl-bis(oxy)] -5 -hydroxy- 17α- [trimethylsilyl-(oxy)] -5 α-oestr-9-en-17β-carbonitrile of formula (VI) with trimethyl chlorosilane; vi) reacting the obtained llβ-[4-(dimethylamino)-phenyl]-3,3-[l,2-ethandiyl-bis(oxy)]-5,17α-bis-[trimethyl-silyl-(oxy)]-5α-oestr-9-en-17β-carbonitrile of formula (VII) with diisobutyl aluminum hydride and after addition of acid to the reaction mixture; vii) methoxy-methylation of the obtained l lβ-[4-(dimethylamino)-phenyl]-3,3-[1,2-ethandiyl-bis(oxy)]-5, 17α-bis-[trimethyl-silyl-(oxy)]-5α-oestr-9-en-17β-carbaldehide of formula (VIII) with methoxy-methyl Grignard reagent formed in situ, while hydrolyzing the trimethylsilyl protective groups; viii) oxidation of the hydroxyl group in position 20 of the obtained 17,20ξ-dihydroxy-11β-[4-(dimemylarnino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3-one of formula (IX) with dicyclohexyl carbodiimide in the presence of dimethyl sulfoxide and a strong organic acid (Swern oxidation), and in given case after purification by chromatography; ix) acetylation of the hydroxyl group in position 17 of the obtained 11β-[4-(dimethylamino)-phenyl] -17-hydroxy-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (X) with acetic anhydride in the presence of perchloric acid, and in given case the obtained 7-acetoxy-11β-[4-(dimethylamino)-phenyl)]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I) is purified by chromatography. The invention also relates to the new intermediates of formula (VII) and (VIII).
摘要翻译：本发明涉及合成已知的17-乙酰氧基-11-β-[4-（二甲基氨基） - 苯基] -2-甲氧基-19-去甲基-4,9-二烯-3,20-二酮（10），9（11） - 二酮-17-（式（I）的化合物（CDB-4124） II）。化合物CDB-4124属于抗激素类。根据本发明的方法如下：i）在3,3- [1,2-乙二基 - 双（氧基）] - 甲酯-5（10）的5（10）位的双键上形成环氧化物，，（II）的9（II） - 二烯-17-酮与过氧化氢反应; ii）在获得的5,10a-环氧-3,3- [1,2-乙二基 - 双（氧基）]-5α-异（9）-en-17的位置17上原位形成的氰化氢的加入 - 一个式（III）的化合物; iii）形成的5,10a-环氧-3,3- [1,2-乙二基 - 双（氧基）]-17α-羟基-5a-甲酯-9（11）-en的17位羟基的甲硅烷基化（IV）的-17β-腈与三甲基氯硅烷反应; iv）使得到的5,10a-环氧-3,3- [1,2-乙二基 - 双（氧基）] - 17- [三甲基 - 甲硅烷氧基] -5a-甲酯-9（II）-en-17β （V）与4-（二甲基氨基） - 苯基溴化镁Grignard试剂在CuCl存在下的反应（Teutsch反应）; v）形成的11β-[4-（二甲基 - 氨基） - 苯基] -3,3 - [1,2-乙二基 - 双（氧基）] -5-羟基-17α的位置5的羟基的甲硅烷基化 - （三甲基甲硅烷基 - （氧基）]-5α-甲基-9-烯-17β-甲腈与三氯甲硅烷; vi）使所得的11β-[4-（二甲基氨基） - 苯基] -3,3- [1,2-乙二基 - 双（氧基）] -5,17a-双 - [三甲基 - 甲硅烷基 - （氧基）（Ⅶ）的5-甲基-9-烯-17β-腈与二异丁基氢化铝反应，并向反应混合物中加入酸; vii）所得的11β-[4-（二甲基氨基） - 苯基] -3,3- [1,2-乙二基 - 双（氧基）] -5,17a-双 - [三甲基甲硅烷基 - （氧基）]-5α-甲基-9-烯-17β-al底物与甲氧基甲基格氏试剂原位形成，同时水解三甲基甲硅烷基保护基; viii）所获得的17,20β-二羟基-11β-[4-（二甲基氨基）苯基] -21-甲氧基-19-去甲基-4,9-二烯-3-酮的20位羟基氧化式（Ⅸ）与二环己基碳二亚胺在二甲基亚砜和强有机酸（Swern氧化）存在下反应，在给定的情况下通过色谱纯化; ix）得到的17β-[4-（二甲基氨基） - 苯基] -17-羟基-21-甲氧基-19-去甲基-4,9-二烯-3,20-二酮的17位羟基乙酰化为式（X）与高氯酸存在下的乙酸酐反应，在给定情况下得到的7-乙酰氧基-11β-[4-（二甲基氨基） - 苯基）] - 21-甲氧基-19-去甲基-4,9-二烯 - （I）的3,20-二酮通过色谱法纯化。本发明还涉及式（VII）和（VIII）的新中间体。

9. 发明申请

WO2006032937A1 APPARATUS AND PROCESS FOR PRODUCING EXTRUDED PLASTIC FOIL HOSE 审中-公开
标题翻译：用于生产挤出塑料薄膜软管的装置和方法
公开(公告)号：WO2006032937A1
公开(公告)日：2006-03-30
申请号：PCT/HU2005/000107
申请日：2005-09-22
申请人： DR-PACK II. KFT , PELCZ, Antal , ILLÉS, Tamás , HORVÁTH, Zoltán , SIMON, László
发明人： PELCZ, Antal , ILLÉS, Tamás , HORVÁTH, Zoltán , SIMON, László
IPC分类号： B29C47/88
CPC分类号： B29C47/883 , B29C47/0026 , B29C47/8835 , B29C47/8885 , B29C47/889
摘要： The apparatus comprises an internal and/or external multiple-stage cooling device (40, 47) arranged coaxially with a drawing orifice (H) of an axtruder die (E), and having multi-level tangential outlets for the coolant to stabilize a non-stabilized section (M) of the expanded foil hose (F) by spiral coolant streams (46, 48). The internal device (40) comprises cooling units (41-44) arranged at axial distance from each other, surrounding the foil section (M) through a gap (G1). Each cooling unit (41-44) is connected to a coolant supply (45) to supply the coolant of selectively adjustable temperature.The external cooling device (47) comprises at least two cooling units (47.1, 47.2, 47.3) arranged at axial distance from each other, surrounding the foil section (M) through a gap (G). Each cooling unit (41-44) is provided with tangential inlets (17, 18) and is connected to a coolant supply (60) to supply the coolant of selectively and individually adjustable temperature and/or volume and/or pressure.
摘要翻译：该设备包括内部和/或外部多级冷却装置（40,47），该内部和/或外部多级冷却装置（40,47）与前刀模（E）的拉制孔口（H）同轴布置，并且具有多级切向通过螺旋冷却剂流（46,48）使冷却剂出口稳定膨胀的薄膜软管（F）的非稳定区段（M）。内部装置（40）包括彼此轴向间隔布置的冷却单元（41-44），所述冷却单元（41-44）通过间隙（G1）围绕箔片部分（M）。每个冷却单元（41-44）连接到冷却剂供应（45）以供应可选择性调节温度的冷却剂。外部冷却装置（47）包括至少两个冷却单元（47.1,47.2,47.3），所述至少两个冷却单元彼此隔开，通过间隙（G）围绕箔片部分（M）。每个冷却单元（41-44）设置有切向入口（17,18）并连接到冷却剂供应器（60）以供应选择性和单独可调节的温度和/或体积和/或压力的冷却剂。

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