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1. 发明申请

US20070281964A1 Novel Crystalline Polymorphs of Clopidogrel 有权
标题翻译：氯吡格雷的新型结晶多晶型物
公开(公告)号：US20070281964A1
公开(公告)日：2007-12-06
申请号：US10571419
申请日：2004-09-09
申请人： Ramakrishnan Arul , Ajay Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
发明人： Ramakrishnan Arul , Ajay Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
IPC分类号： A61K31/4365 , A61P7/02 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1, 2 and 3. The present invention further relates to processes for preparing such forms, pharmaceutical compositions comprising such forms, and uses for such forms and compositions. The pharmaceutical compositions may be used, in particular, for inhibiting platelet aggregation or for treating, preventing or managing thrombosis, atherothrombosis, an atherothrombotic event, ischaemic stroke, myocardial infarction, non-Q-wave myocardial infarction, atherosclerosis, peripheral arterial disease, or unstable angina. The present invention also relates to methods of treating said disorders. Formula (1).
摘要翻译：本发明涉及血小板聚集抑制剂（+） - （S） - 甲基-2-（2-氯苯基） - （6,7-二氢-4H-噻吩并[3,2-c]吡啶-3-基）（1），以溴化氢的形式，被鉴定为多晶型形式1,2和3.本发明还涉及制备这些形式的方法，包含这些形式的药物组合物和用于这种形式和组成。药物组合物可特别用于抑制血小板聚集或治疗，预防或控制血栓形成，动脉粥样硬化血栓形成，动脉粥样硬化血栓形成事件，缺血性卒中，心肌梗死，非Q波心肌梗塞，动脉粥样硬化，外周动脉疾病或不稳定型心绞痛本发明还涉及治疗所述疾病的方法。公式1）。

2. 发明授权

US07897613B2 Crystalline polymorphs of clopidogrel 有权
标题翻译：氯吡格雷的结晶多晶型物
公开(公告)号：US07897613B2
公开(公告)日：2011-03-01
申请号：US10571419
申请日：2004-09-09
申请人： Ramakrishnan Arul , Ajay Singh Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
发明人： Ramakrishnan Arul , Ajay Singh Rawat , Maheshkumar Gadakar , Rajesh Rao , Abhinay Pise , Jason Gray
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02
CPC分类号： C07D495/04
摘要： The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1, 2 and 3. The present invention further relates to processes for preparing such forms, pharmaceutical compositions comprising such forms, and uses for such forms and compositions. The pharmaceutical compositions may be used, in particular, for inhibiting platelet aggregation or for treating, preventing or managing thrombosis, atherothrombosis, an atherothrombotic event, ischaemic stroke, myocardial infarction, non-Q-wave myocardial infarction, atherosclerosis, peripheral arterial disease, or unstable angina. The present invention also relates to methods of treating said disorders. Formula (1).
摘要翻译：本发明涉及血小板聚集抑制剂（+） - （S） - 甲基-2-（2-氯苯基） - （6,7-二氢-4H-噻吩并[3,2-c]吡啶-3-基）（1），以溴化氢的形式，被鉴定为多晶型形式1,2和3.本发明还涉及制备这些形式的方法，包含这些形式的药物组合物和用于这种形式和组成。药物组合物可特别用于抑制血小板聚集或治疗，预防或控制血栓形成，动脉粥样硬化血栓形成，动脉粥样硬化血栓形成事件，缺血性中风，心肌梗塞，非Q波心肌梗塞，动脉粥样硬化，外周动脉疾病或不稳定型心绞痛本发明还涉及治疗所述疾病的方法。公式1）。

3. 发明授权

US08252783B2 Quinolone carboxylic acids, derivatives thereof, and methods of making and using same 失效
标题翻译：喹诺酮羧酸，其衍生物及其制备和使用方法
公开(公告)号：US08252783B2
公开(公告)日：2012-08-28
申请号：US12561283
申请日：2009-09-17
申请人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
发明人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
IPC分类号： A61K31/553 , C07D401/04
CPC分类号： C07D401/04 , C07D215/233 , C07D403/04 , C07D413/04 , C07D417/04
摘要： A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
摘要翻译：如本文所示，制备具有式I，Ia，Ib或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上的一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮和在整个合成过程中保留这些取代基的取向。本方法包括比现有技术方法更少的步骤。本方法还可以包括从对映异构体混合物中简单分离喹诺酮羧酸或其衍生物的所需对映异构体。包含通过本方法制备的氟喹诺酮类的药物组合物可以有效地用于各种微生物病原体。

4. 发明申请

US20100029936A1 Quinolone Carboxylic Acids, Derivatives Thereof, and Methods of Making and Using Same 失效
标题翻译：喹诺酮羧酸，其衍生物及其制备和使用方法
公开(公告)号：US20100029936A1
公开(公告)日：2010-02-04
申请号：US12561283
申请日：2009-09-17
申请人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
发明人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
IPC分类号： C07D401/10
CPC分类号： C07D401/04 , C07D215/233 , C07D403/04 , C07D413/04 , C07D417/04
摘要： A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
摘要翻译：如本文所示，制备具有式I，Ia，Ib或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上的一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮和在整个合成过程中保留这些取代基的取向。本方法包括比现有技术方法更少的步骤。本方法还可以包括从对映异构体混合物中简单分离喹诺酮羧酸或其衍生物的所需对映异构体。包含通过本方法制备的氟喹诺酮类的药物组合物可以有效地用于各种微生物病原体。

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