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1. 发明授权

US06528666B1 Process of preparation of flumethasone 21-acetate, or flumethasone and its 17-carboxyl androsten analogue 有权
标题翻译：氟米松21-乙酸酯或氟米松及其17-羧基和类似物的制备方法
公开(公告)号：US06528666B1
公开(公告)日：2003-03-04
申请号：US10162862
申请日：2002-06-06
申请人： Ivan Villax , Zita Mendes
发明人： Ivan Villax , Zita Mendes
IPC分类号： C07C5022
CPC分类号： C07J5/0076 , C07J3/005 , C07J71/0015 , Y02P20/55
摘要： A process for the preparation of high purity flumethasone in high yield involves C3 protecting 9,11&bgr;-epoxy-17&agr;,21-dihydroxy-16&agr;-methylpregna-1,4-diene-3,20-dione,21-acetate, fluorinating at 6&agr;, removing the C3 protecting group, fluorinating the 9,11-epoxy group. The resulting flumethasone 21-acetate is treated with the methanolic potassium hydroxide in the presence of an oxidation agent, causing a simultaneous hydrolyzation and degradative oxidation, resulting in the formation of 6&agr;,9&agr;-difluoro-11&bgr;,17&agr;-dihydroxy-16&agr;-methyl-17&bgr;-carboxy-androsta-1,4-diene-3-one in high yield. Flumethasone 21-acetate is alternatively hydrolyzed to yield flumethasone free alcohol.
摘要翻译：以高产率制备高纯度氟米松的方法涉及C3保护9,11β-环氧-17α，21-二羟基-16α-甲基孕甾-1,4-二烯-3,20-二酮，21-乙酸酯，以6alpha氟化，除去C3保护基，氟化9,11-环氧基。得到的氟醋酸酯21-乙酸酯在氧化剂存在下用甲醇氢氧化钾处理，导致同时水解和降解氧化，导致形成6α，9α-二氟-11β，17α-二羟基-16α-甲基 - 17β-羧基 - 雄甾-1,4-二烯-3-酮。将水杨酸21-乙酸酯水解，以产生不含氟米松的酒精。

2. 发明授权

US09416097B2 Crystalline minocycline base and processes for its preparation 有权
标题翻译：结晶米诺环素碱及其制备方法
公开(公告)号：US09416097B2
公开(公告)日：2016-08-16
申请号：US13599116
申请日：2012-08-30
申请人： Zita Mendes , Jose Rafael Antunes , Susana Marto , William Heggie
发明人： Zita Mendes , Jose Rafael Antunes , Susana Marto , William Heggie
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 II and Form III, of minocycline base are provided. These are characterized 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 crystallization 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形式，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/或悬浮在选自醚中的有机溶剂中，然后从混合物中结晶来制备形式I。

3. 发明授权

US08314218B2 Method of synthesizing macrolide compounds 有权
标题翻译：大环内酯类化合物的合成方法
公开(公告)号：US08314218B2
公开(公告)日：2012-11-20
申请号：US12604618
申请日：2009-10-23
申请人： Zita Mendes , António Carlos Silva Henriques , William Heggie
发明人： Zita Mendes , António Carlos Silva Henriques , William Heggie
IPC分类号： C07H17/00 , C07G3/00
CPC分类号： C07H17/08
摘要： The present invention relates to methods for synthesizing macrolide compounds which are known to have antibacterial activity, and are useful in the therapy of bacterial infections in mammals. More specifically, the invention relates to methods for synthesizing the macrolide antibiotic, gamithromycin utilizing a novel configuration of catalysts, chemical structures, and/or methods. An embodiment of the present invention may include allowing multiple chemical reactions to proceed without the isolation of chemical intermediates. Thus, multiple reactions may occur in one reaction vessel allowing for a considerable decrease in the cycle-time. The present invention also provides a novel method for inhibiting degradation while isolating a structure of a pharmaceutical composition.
摘要翻译：本发明涉及已知具有抗菌活性的大环内酯类化合物的合成方法，并且可用于哺乳动物细菌感染的治疗。更具体地说，本发明涉及利用催化剂的新型结构，化学结构和/或方法合成大环内酯类抗生素，吡咯霉素的方法。本发明的一个实施方案可以包括允许多个化学反应进行而不隔离化学中间体。因此，在一个反应容器中可能发生多次反应，允许循环时间显着降低。本发明还提供了用于在分离药物组合物的结构的同时抑制降解的新方法。

4. 发明申请

US20130030195A1 Crystalline Minocycline Base and Processes for its Preparation 有权
标题翻译：结晶米诺环素基质及其制备方法
公开(公告)号：US20130030195A1
公开(公告)日：2013-01-31
申请号：US13599116
申请日：2012-08-30
申请人： Zita Mendes , Jose Rafael Antunes , Susana Marto , William Heggie
发明人： Zita Mendes , Jose Rafael Antunes , Susana Marto , William Heggie
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 II 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形式，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。

5. 发明申请

US20120028928A1 Process for Isolating Tigecycline and Tigecycline Made Therefrom 有权
标题翻译：用于分离替加环素和替加环素的方法
公开(公告)号：US20120028928A1
公开(公告)日：2012-02-02
申请号：US13145445
申请日：2010-01-22
申请人： Zita Mendes , Guy Villax
发明人： Zita Mendes , Guy Villax
IPC分类号： A61K31/65 , B29B9/16 , A61P31/00 , C07C237/26 , A61P17/00
CPC分类号： C07C231/24 , A61K31/65 , C07C237/26 , C07C2603/46
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.
摘要翻译：本发明提供了一种隔离替加环素的方法，该方法包括将替加环素溶液喷雾干燥在溶剂中的步骤。溶剂优选为水或有机溶剂。另一方面，提供了通过喷雾干燥，特别是无定形形式获得的替加环素。特别地，本发明提供根据本发明的方法通过喷雾干燥获得的替加环素。

6. 发明授权

US08017803B2 Process for the preparation of tamsulosin and intermediates thereof 有权
标题翻译：制备坦索罗辛及其中间体的方法
公开(公告)号：US08017803B2
公开(公告)日：2011-09-13
申请号：US11721028
申请日：2005-01-18
申请人： Zita Mendes , Joana Baptista , Dionisio Martin , William Heggie
发明人： Zita Mendes , Joana Baptista , Dionisio Martin , William Heggie
IPC分类号： C07C311/39 , C07C311/40
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 with chlorosulfonic acid with or without an organic solvent, to obtain compound R,R-2-methoxy-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 Cl; 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） - 胺或其盐与有机溶剂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] - 苯磺酸式III的酸b）在存在下在醇中进行的式III化合物R，R-2-甲氧基-5- [2-（1-苯基 - 乙基氨基） - 丙基] - 苯磺酸或其盐的氢解使用氢或氢源的钯催化剂，得到式IV化合物R - （ - ） - 5-（2-氨基 - 丙基）-2-甲氧基 - 苯磺酸c）将伯胺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表示选自Cl的卤素原子; Br和I得到式VI的5 - {（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的磺酰氯。 e）将化合物VII与氨反应得到化合物I.

7. 发明申请

US20090234154A1 Process for the preparation of tamsulosin and intermediates thereof 有权
标题翻译：制备坦索罗辛及其中间体的方法
公开(公告)号：US20090234154A1
公开(公告)日：2009-09-17
申请号：US11721028
申请日：2005-01-18
申请人： Zita Mendes , Joana Baptista , Dionisio Martin , William Heggie
发明人： Zita Mendes , Joana Baptista , Dionisio Martin , William Heggie
IPC分类号： C07C309/30 , C07C303/38
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 with chlorosulfonic acid with or without an organic solvent, to obtain compound R,R-2-methoxy-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 Cl; 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） - 胺或其盐与有机溶剂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] - 苯磺酸式III的酸b）在存在下在醇中进行的式III化合物R，R-2-甲氧基-5- [2-（1-苯基 - 乙基氨基） - 丙基] - 苯磺酸或其盐的氢解使用氢或氢源的钯催化剂，得到式IV化合物R - （ - ） - 5-（2-氨基 - 丙基）-2-甲氧基 - 苯磺酸c）将伯胺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表示选自Cl的卤素原子; Br和I得到式VI的5 - {（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的磺酰氯。 e）将化合物VII与氨反应得到化合物I.

8. 发明授权

US09187410B2 Process for isolating tigecycline and tigecycline made therefrom 有权
标题翻译：用于分离替加环素和替加环素制备的方法
公开(公告)号：US09187410B2
公开(公告)日：2015-11-17
申请号：US13145445
申请日：2010-01-22
申请人： Zita Mendes , Guy Villax
发明人： Zita Mendes , Guy Villax
IPC分类号： A61K31/65 , A61P31/00 , B29B9/16 , C07C231/24 , C07C237/26
CPC分类号： C07C231/24 , A61K31/65 , C07C237/26 , C07C2603/46
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.
摘要翻译：本发明提供了一种隔离替加环素的方法，该方法包括将替加环素溶液喷雾干燥在溶剂中的步骤。溶剂优选为水或有机溶剂。另一方面，提供了通过喷雾干燥，特别是无定形形式获得的替加环素。特别地，本发明提供根据本发明的方法通过喷雾干燥获得的替加环素。

9. 发明授权

US08258327B2 Crystalline minocycline base and processes for its preparation 有权
标题翻译：结晶米诺环素碱及其制备方法
公开(公告)号：US08258327B2
公开(公告)日：2012-09-04
申请号：US12528209
申请日：2008-02-22
申请人： Susana Marto , William Heggie , Zita Mendes , Jose Rafael Antunes
发明人： Susana Marto , William Heggie , Zita Mendes , Jose Rafael Antunes
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 II and Form III, of minocycline base are provided. These are characterized 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 crystallization 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形式，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/或悬浮在选自醚中的有机溶剂中，然后从混合物中结晶来制备形式I。

10. 发明申请

US20100286417A1 Crystalline Minocycline Base and Processes for its Preparation 有权
标题翻译：结晶米诺环素基质及其制备方法
公开(公告)号：US20100286417A1
公开(公告)日：2010-11-11
申请号：US12528209
申请日：2008-02-22
申请人： Zita Mendes , Jose Rafael Antunes , Susana Marto , William Heggie
发明人： Zita Mendes , Jose Rafael Antunes , Susana Marto , William Heggie
IPC分类号： C07C215/88 , C07C213/10
CPC分类号： C07C237/26
摘要： The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form II 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形式，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。

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