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1. 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。

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

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。

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. 发明授权

US08445471B2 Process for obtaining steroidal phosphate compounds 有权
标题翻译：获得类固醇磷酸盐化合物的方法
公开(公告)号：US08445471B2
公开(公告)日：2013-05-21
申请号：US12600311
申请日：2008-05-16
申请人： Luis Sobral , Filipe Gaspar , William Heggie , Emilia Leitao , Jose Rafael Antunes
发明人： Luis Sobral , Filipe Gaspar , William Heggie , Emilia Leitao , Jose Rafael Antunes
IPC分类号： A61K31/573 , C07J1/00
CPC分类号： A61K31/573 , A61K9/1688
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-CH3 or X═F and R=β-CH3: comprises spray drying a solution comprising compound of formula (I).
摘要翻译：一种获得式（I）的21-二磷酸孕烷衍生物化合物的方法，其中X = R = H或X = F，R =α-CH 3或X = F，R =β-CH 3：包括喷雾干燥包含式（I）化合物。

6. 发明申请

US20100240916A1 PROCESS FOR OBTAINING STEROIDAL PHOSPHATE COMPOUNDS 有权
标题翻译：获得磷酸三辛酯化合物的方法
公开(公告)号：US20100240916A1
公开(公告)日：2010-09-23
申请号：US12600311
申请日：2008-05-16
申请人： Luis Sobral , Filipe Gaspar , William Heggie , Emilia Leitao , Jose Rafael Antunes
发明人： Luis Sobral , Filipe Gaspar , William Heggie , Emilia Leitao , Jose Rafael Antunes
IPC分类号： C07J51/00
CPC分类号： A61K31/573 , A61K9/1688
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-CH3 or X═F and R=β-CH3 comprises spray drying a solution comprising compound of formula (I).
摘要翻译：一种获得式（I）的21-磷酸二钠孕烷衍生物化合物的方法，其中X = R = H或X = F，R =α-CH 3或X = F，R =＆bgr; -CH 3包括喷雾干燥包含式（I）化合物。

7. 发明授权

US07541494B2 Process for the manufacture of iohexol 有权
标题翻译：制备碘海醇的方法
公开(公告)号：US07541494B2
公开(公告)日：2009-06-02
申请号：US12094589
申请日：2006-03-03
申请人： José Galindro , Susana Marto , João Bandarra , William Heggie
发明人： José Galindro , Susana Marto , João Bandarra , William Heggie
IPC分类号： C07C233/65
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）-2,4,6-三碘间苯二酰胺烷基化，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。

8. 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。

9. 发明申请

US20100145035A1 METHOD OF SYNTHESIZING MACROLIDE COMPOUNDS 有权
标题翻译：合成MACROLIDE化合物的方法
公开(公告)号：US20100145035A1
公开(公告)日：2010-06-10
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： C07H17/08
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，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。

10. 发明申请

US20090048463A1 Process for the manufacture of iohexol 有权
公开(公告)号：US20090048463A1
公开(公告)日：2009-02-19
申请号：US12094589
申请日：2006-03-03
申请人： Jose Galindro , Susana Marto , Joao Bandarra , William Heggie
发明人： Jose Galindro , Susana Marto , Joao Bandarra , William Heggie
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.

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