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1. 发明申请

WO2008102161A2 CRYSTALLINE MINOCYCLINE BASE AND PROCESSES FOR ITS PREPARATION 审中-公开
标题翻译：晶体小分子碱基及其制备方法
公开(公告)号：WO2008102161A2
公开(公告)日：2008-08-28
申请号：PCT/GB2008/000625
申请日：2008-02-22
申请人： HOVIONE INTER LTD. , MENDES, Zita , ANTUNES, Jose, Rafael , MARTO, Susana , HEGGIE, William
发明人： MENDES, Zita , ANTUNES, Jose, Rafael , MARTO, Susana , HEGGIE, William
IPC分类号： C07C237/26
CPC分类号： C07C237/26
摘要： The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form Il and Form III, of minocycline base are provided. These are characterised by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallisation from the mixture.
摘要翻译：本发明提供了结晶米诺环素碱。特别地，提供了三环结构的多晶型，称为米诺环素碱的I型，II型和III型。其特征在于XRD和IR数据。还提供了制备新多晶型体的方法。例如，通过将无定形米诺环素碱溶解和/或悬浮在选自醚的有机溶剂中，然后从混合物中结晶来制备形式I。

2. 发明申请

WO2006043015A1 PROCESS FOR THE ESTERIFICATION OF A CARBOTHIOIC ACID 审中-公开
标题翻译：过氧化氢的制备方法
公开(公告)号：WO2006043015A1
公开(公告)日：2006-04-27
申请号：PCT/GB2004/005052
申请日：2004-12-02
申请人： HOVIONE INTER LTD. , TURNER, Craig, Robert , SOBRAL, Luis , MARTIN, Dionisio , HEGGIE, William , LEITÄO, Emilia
发明人： SOBRAL, Luis , MARTIN, Dionisio , HEGGIE, William , LEITÄO, Emilia
IPC分类号： C07J31/00
CPC分类号： C07J31/006
摘要： A process for preparing compounds of formula: (II) by esterification of the C-17 hydroxyl group of 6α, 9α-difluoro-11β, 17α-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carbothioic acid, the compound of formula: (I) comprises treating compound (I) with a slight excess of an acyl chloride of general formula R-COCI, where R represents -CH2CH3, -CH2CH2CH3 or -CH(CH3)2, in an inert solvent, in the presence of a tertiary amine. Preferably the process is carried out using pyridine in the presence of acetone at a temperature of from 5 °C to -20 °C. z.
摘要翻译：通过酯化6a，9a-二氟-11β，17α-二羟基-16-甲基-3-氧代雄甾-1,4-二烯-17β-硫代碳酸酯的C-17羟基来制备式（II）化合物的方法酸，式（I）化合物包括用稍微过量的通式R-COCl的酰氯处理化合物（I），其中R表示-CH 2 CH 3，-CH 2 CH 2 CH 3或-CH（CH 3）2，在惰性溶剂，在叔胺的存在下。优选地，该方法使用吡啶在丙酮存在下，在5℃至-20℃的温度下进行。 ž。

3. 发明申请

WO2010084325A3 PROCESS FOR ISOLATING TIGECYCLINE 审中-公开
公开(公告)号：WO2010084325A3
公开(公告)日：2010-07-29
申请号：PCT/GB2010/000104
申请日：2010-01-22
申请人： HOVIONE INTER LTD , MENDES, Zita , VILLAX, Guy , CRAIG, Robert, Turner
发明人： MENDES, Zita , VILLAX, Guy
IPC分类号： C07C231/24 , C07C237/26 , A61K31/65 , A61P17/00
摘要： The present invention provides a process for isolating tigecycline which process comprises the step of spray drying a solution of tigecycline in a solvent. Preferably the solvent is water or an organic solvent. In another aspect, there is provided tigecycline obtainable by spray drying, particularly in amorphous form. In particular, the invention provides tigecycline obtainable by spray drying according to the process of the invention.

4. 发明申请

WO2008102161A3 CRYSTALLINE MINOCYCLINE BASE AND PROCESSES FOR ITS PREPARATION 审中-公开
公开(公告)号：WO2008102161A3
公开(公告)日：2008-08-28
申请号：PCT/GB2008/000625
申请日：2008-02-22
申请人： HOVIONE INTER LTD. , MENDES, Zita , ANTUNES, Jose, Rafael , MARTO, Susana , HEGGIE, William
发明人： MENDES, Zita , ANTUNES, Jose, Rafael , MARTO, Susana , HEGGIE, William
IPC分类号： C07C237/26
摘要： The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form Il and Form III, of minocycline base are provided. These are characterised by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallisation from the mixture.

5. 发明申请

WO2007060380A1 PROCESS FOR THE MANUFACTURE OF IOHEXOL 审中-公开
标题翻译： IOHEXOL制造工艺
公开(公告)号：WO2007060380A1
公开(公告)日：2007-05-31
申请号：PCT/GB2006/000768
申请日：2006-03-03
申请人： HOVIONE INTER LTD , TURNER, Craig, Robert , GALINDRO, José , MARTO, Susana , BANDARRA, João, António, Moínho , HEGGIE, William
发明人： GALINDRO, José , MARTO, Susana , BANDARRA, João, António, Moínho , HEGGIE, William
IPC分类号： C07C233/69
CPC分类号： C07C231/08 , C07C237/46
摘要： A process for the production of iohexol comprises alkylating 5-Acetamido-N,N'-bis(2,3-dihydroxypropyl)-2,4,6- triiodoisophthalamide using 2(2-methoxy-ethoxy)-ethanol as solvent in the presence of a base, and optionally isolating crude iohexol from the reaction mixture. Preferably, the alkylating agent is 1-chloro-2,3 propanediol and the base is an alkali metal hydroxide such as sodium hydroxide or potassium hydroxide.
摘要翻译：制备碘海醇的方法包括使用2（2-甲氧基 - 乙氧基） - 乙醇作为溶剂使5-乙酰氨基-N，N'-双（2,3-二羟基丙基）-2,4,6-三碘邻苯二甲酰胺烷基化，的碱，并且任选地从反应混合物中分离粗己烯醇。优选地，烷基化剂是1-氯-2,3丙二醇，碱是碱金属氢氧化物如氢氧化钠或氢氧化钾。

6. 发明申请

WO2006061549A1 PROCESS FOR THE PREPARATION OF TAMSULOSIN AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备TAMSULOSIN及其中间体的方法
公开(公告)号：WO2006061549A1
公开(公告)日：2006-06-15
申请号：PCT/GB2005/000155
申请日：2005-01-18
申请人： HOVIONE INTER LTD. , TURNER, Craig, Robert , MENDES, Zita , BAPTISTA, Joana , MARTIN, Dionisio , HEGGIE, William
发明人： MENDES, Zita , BAPTISTA, Joana , MARTIN, Dionisio , HEGGIE, William
IPC分类号： C07C303/38 , C07C311/37 , C07C309/46 , A61K31/18
CPC分类号： C07C303/38 , C07B2200/07 , C07C303/08 , C07C303/22 , C07C309/49 , C07C311/37 , C07C309/88
摘要： A process for producing tamsulosin of formula (I) and pharmaceutically acceptable addition salts, thereof comprises the steps of : a) Reacting compound R,R-[2-(4-methoxy-phenyl)-1-methyl-ethyl]-(1-phenyl-ethyl)-amine of formula (II) or a salt thereof (II) with chlorosulfonic acid with or without an organic solvent, to obtain compound R,R-2methoxy-5-[2-(1-phenyl-ethylamino)-propyl]-benzenesulfonic acid of formula (III) b) Hydrogenolysis of compound R,R-2-methoxy-5-[2-(1-phenyl-ethylamino)-propyl]- benzenesulfonic acid of formula III or a salt thereof carried out in an alcohol in the presence of a palladium catalyst using hydrogen or a source of hydrogen, to obtain compound R-(-)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula (IV) c)Reacting primary amine R-(-)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula (IV), or a salt thereof, with a compound of formula (V) wherein X represents an halogen atom selected from the group consisting of C1;Br and I, to obtain 5- [(2R)-2-[2-(2-ethoxy-phenoxy)-ethylamino]-propyl]-2-methoxy-benzenesulfonic acid compound of formula (VI) d) Reacting compound of formula (VI) with an halogenating agent, to obtain the corresponding sulfonylchloride of formula (VII). e)Reacting compound VII with ammonia to obtain compound I.
摘要翻译：制备式（I）的坦索罗辛及其药学上可接受的加成盐的方法包括以下步骤：a）使化合物R，R- [2-（4-甲氧基 - 苯基）-1-甲基 - 乙基] - （1 苯基 - 乙基） - 胺或其盐（II）与具有或不含有机溶剂的氯磺酸反应，得到化合物R，R-2-甲氧基-5- [2-（1-苯基 - 乙基氨基） - 丙基] - 苯磺酸b）氢化式III化合物R，R-2-甲氧基-5- [2-（1-苯基 - 乙基氨基） - 丙基] - 苯磺酸或其载体的盐在使用氢或氢源的钯催化剂存在下在醇中进行反应，得到式（IV）的化合物R - （ - ） - 5-（2-氨基 - 丙基）-2-甲氧基 - 苯磺酸c ）将式（Ⅳ）的伯胺R - （ - ） - 5-（2-氨基丙基）-2-甲氧基 - 苯磺酸或其盐与式（Ⅴ）化合物反应其中X代表卤素选自C1; Br和I的原子，得到5 - （Ⅵ）的[（2R）-2- [2-（2-乙氧基 - 苯氧基） - 乙基氨基] - 丙基] -2-甲氧基 - 苯磺酸化合物d）将式（Ⅵ）化合物与卤化剂，得到相应的式（Ⅶ）磺酰氯。 e）将化合物VII与氨反应得到化合物I.

7. 发明专利

JPH0380149B2 失效
公开(公告)号：JPH0380149B2
公开(公告)日：1991-12-24
申请号：JP29337685
申请日：1985-12-27
申请人： HOVIONE INTER LTD
发明人： VILLAX JOAO EMERICO , PAGE PHILLIP RONALD
IPC分类号： B01J20060101 , B01J31/00 , B01J31/24 , C07B61/00 , C07C20060101 , C07C231/12 , C07C235/26 , C07C237/26 , C07F15/00

8. 发明申请

WO2011131947A2 A PROCESS FOR PARTICLE PROCESSING OF ACTIVE PHARMACEUTICAL INGREDIENTS 审中-公开
标题翻译：活性药物成分颗粒加工方法
公开(公告)号：WO2011131947A2
公开(公告)日：2011-10-27
申请号：PCT/GB2011/000631
申请日：2011-04-21
申请人： HOVIONE INTER LTD , GIL, Marco , CACELA, Constanca , MENDONCA, Ricardo , GASPAR, Filipe , TURNER, Craig Robert
发明人： GIL, Marco , CACELA, Constanca , MENDONCA, Ricardo , GASPAR, Filipe
IPC分类号： A61K9/14 , A61K31/137 , A61K31/46 , A61K31/56 , A61K31/58
CPC分类号： A61J3/02 , A61K9/0075 , A61K9/14 , A61K31/137 , A61K31/46 , A61K31/56 , A61K31/58
摘要： A process for reducing the particle size of an active pharmaceutical ingredient (API) while maintaining its polymorphic form, comprises the step of processing the active pharmaceutical ingredient by cavitation at elevated pressure. The process preferably comprises the step of isolating the processed active ingredient in the form of powder, wherein the isolation step comprises filtration or spray drying. Particles produced by the process of the invention typically have a span value of less than 2.5.
摘要翻译：在保持其多晶型形式的同时降低活性药物成分（API）的粒度的方法包括通过在升高的压力下的空化来加工活性药物成分的步骤。该方法优选包括以粉末形式分离经处理的活性成分的步骤，其中分离步骤包括过滤或喷雾干燥。通过本发明的方法生产的颗粒通常具有小于2.5的跨度值。

9. 发明申请

WO2008139210A3 PROCESS FOR OBTAINING STEROIDAL PHOSPHATE COMPOUNDS 审中-公开
公开(公告)号：WO2008139210A3
公开(公告)日：2008-11-20
申请号：PCT/GB2008/001709
申请日：2008-05-16
申请人： HOVIONE INTER LTD. , TURNER, Craig, Robert , SOBRAL, Luis , GASPAR, Filipe , HEGGIE, William , LEITAO, Emilia , ANTUNES, Jose, Refael
发明人： SOBRAL, Luis , GASPAR, Filipe , HEGGIE, William , LEITAO, Emilia , ANTUNES, Jose, Refael
IPC分类号： A61K9/16 , A61K31/573 , A61P29/00
摘要： A process for obtaining 21-disodium phosphate pregnane derivative compounds of formula (I), wherein X=R=H or X=F and R=α-CH 3 or X=F and R=β-CH 3: comprises spray drying a solution comprising compound of formula (I).

10. 发明专利

JP2014169319A Crystalline minocycline base and method for manufacturing the same 审中-公开
标题翻译：晶体小分子碱基及其制造方法
公开(公告)号：JP2014169319A
公开(公告)日：2014-09-18
申请号：JP2014104022
申请日：2014-05-20
申请人： Hovione Inter Ltd , ホビオネインテルリミテッド
发明人： MENDEZ ZITA , JOSE RAFAEL ANTUNES , SUSANA MARTO , WILLIAM HEGGIE
IPC分类号： C07C237/26 , A61K31/65 , A61P31/04
CPC分类号： C07C237/26
摘要： PROBLEM TO BE SOLVED: To provide a minocycline base having an impurity of 4-epi-minocycline controlled to an extremely low level and having a form more stable than that of a minocycline base known in only an amorphous form.SOLUTION: Provided is the method for manufacturing a minocycline base having three kinds of crystal polymorphic form named as a form I, a form II and a form III characterized by XRD and IR data, and new polymorphic forms thereof. For example, in the form I, a crystalline minocycline is manufactured by dissolving and/or suspending amorphous minocycline salt into an organic solvent selected from ether, such as methyl tert-butyl ether and forming a crystal from the mixture.
摘要翻译：要解决的问题：提供具有控制在极低水平的4-表 - 米诺环素的杂质的米诺环素碱，并且其形式比仅以无定形形式已知的二甲胺四环素的形式更稳定。解决方案：提供了该方法用于制造具有三种以XRD和IR数据表征的晶型I，II型和III型晶体多晶型的米诺环素碱基及其新型多晶型。例如，以I形式，通过将无定形米诺环素盐溶解和/或悬浮于选自醚，如甲基叔丁基醚的有机溶剂中并从混合物中形成晶体来制造结晶米诺环素。

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