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1. 发明授权

US08552194B2 Process for preparing quinoline-3-carboxamide derivatives 有权
公开(公告)号：US08552194B2
公开(公告)日：2013-10-08
申请号：US12989796
申请日：2009-04-27
申请人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： C07D215/38
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/22
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.

2. 发明申请

US20110105756A1 Process for Preparing Quinoline-3-Carboxamide Derivatives 有权
标题翻译：喹啉-3-甲酰胺衍生物的制备方法
公开(公告)号：US20110105756A1
公开(公告)日：2011-05-05
申请号：US12989796
申请日：2009-04-27
申请人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： C07D215/56
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/22
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要翻译：本文公开了以高产率和纯度制备喹啉-3-甲酰胺衍生物如拉喹莫德或其药学上可接受的盐的改进的，商业上可行的和工业上有利的方法。

3. 发明授权

US08314235B2 Process for preparing varenicline, varenicline intermediates, pharmaceutically acceptable salts thereof 失效
标题翻译：伐伦碱，伐伦碱中间体及其药学上可接受的盐的制备方法
公开(公告)号：US08314235B2
公开(公告)日：2012-11-20
申请号：US13060755
申请日：2009-08-31
申请人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan
发明人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan
IPC分类号： C07D241/40
CPC分类号： C07D471/08
摘要： Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.
摘要翻译：本文提供了一种改进的，方便的，商业上可行的和环境友好的伐伦碱或其药学上可接受的盐的制备方法，其包括使1-（4,5-二氨基-10-氮杂 - 三环[6.3.1.02 7]十二碳-2 （7），3,5-三烯-10-基）-2,2,2-三氟乙酮与氯乙醛在氧源的存在下反应。本文进一步提供了一种改进和工业上有利的制备1-（4,5-二氨基-10-氮杂 - 三环[6.3.1.02 7]十二-2（7），3,5-三烯-10-基）-2,2,2-三氟乙酮。

4. 发明申请

US20110224437A1 PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 失效
标题翻译：制备VARENICLINE，VARENICLINE中间体及其药学上可接受的药物的方法
公开(公告)号：US20110224437A1
公开(公告)日：2011-09-15
申请号：US13060755
申请日：2009-08-31
申请人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan
发明人： Girish Dixit , Krishnadatt Sharma , Kundan Singh Shekhawat , Nitin Sharadchandra Pradhan
IPC分类号： C07D471/08 , C07D221/22
CPC分类号： C07D471/08
摘要： Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.
摘要翻译：本文提供了一种用于制备伐伦尼克林或其药学上可接受的盐的改进的，方便的，商业可行的和环境友好的方法，其包括使1-（4,5-二氨基-10-氮杂 - 三环[6.3.1.02.7] 2（7），3,5-三烯-10-基）-2,2,2-三氟乙酮与氯乙醛在氧源的存在下反应。本文进一步提供了一种改进的和工业上有利的制备1-（4,5-二氨基-10-氮杂 - 三环[6.3.1.02.7]十二碳-2（7），3,5-三烯-10- 吡啶-2-基）-2,2,2-三氟乙酮。

5. 发明申请

US20110171270A1 NOVEL SOLID STATE FORMS OF LAQUINIMOD AND ITS SODIUM SALT 有权
标题翻译： LAQUINIMOD及其SODIUM盐的新型固体状态
公开(公告)号：US20110171270A1
公开(公告)日：2011-07-14
申请号：US13001715
申请日：2009-06-30
申请人： Girish Dixit , Krishnadatt Sharma , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Krishnadatt Sharma , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K31/4704 , C07D215/56 , A61K9/00 , A61P1/00 , A61P19/02 , A61P17/06 , A61P11/06 , A61P9/10 , A61P25/28 , A61P3/10
CPC分类号： C07D215/56 , A61K31/4704
摘要： Provided herein is a novel crystalline form of laquinimod, process for the preparation, pharmaceutical compositions, and method of treating thereof. Provided also herein are novel amorphous and polymorphic forms of laquinimod sodium, process for the preparation, pharmaceutical compositions, and method of treating thereof.
摘要翻译：本文提供了一种新的结晶形式的拉喹莫德，其制备方法，药物组合物及其处理方法。本文还提供了新的无定形和多晶型的拉喹莫德钠，制备方法，药物组合物及其处理方法。

6. 发明授权

US08354428B2 Solid state forms of laquinimod and its sodium salt 有权
标题翻译：固态形式的拉喹莫德及其钠盐
公开(公告)号：US08354428B2
公开(公告)日：2013-01-15
申请号：US13001715
申请日：2009-06-30
申请人： Girish Dixit , Krishnadatt Sharma , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Krishnadatt Sharma , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D215/56 , A61K31/4704
摘要： Provided herein is a novel crystalline form of laquinimod, process for the preparation, pharmaceutical compositions, and method of treating thereof. Provided also herein are novel amorphous and polymorphic forms of laquinimod sodium, process for the preparation, pharmaceutical compositions, and method of treating thereof.
摘要翻译：本文提供了一种新的结晶形式的拉喹莫德，其制备方法，药物组合物及其处理方法。本文还提供了新的无定形和多晶型的拉喹莫德钠，制备方法，药物组合物及其处理方法。

7. 发明申请

US20110021547A1 Substantially Pure and a Stable Crystalline Form of Bosentan 审中-公开
标题翻译：波斯坦的基本纯度和稳定的结晶形式
公开(公告)号：US20110021547A1
公开(公告)日：2011-01-27
申请号：US12864571
申请日：2009-01-22
申请人： Girish Dixit , Nandkumar Gaikwad , Hima Prasad Naidu , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Nandkumar Gaikwad , Hima Prasad Naidu , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K31/513 , C07D403/04
CPC分类号： C07D403/04
摘要： Described is a highly stable crystalline form of bosentan having a water content in the range of about 3-4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A5. Provided also herein is a bosentan impurity, p-tert-butyl-N[6-hydroxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide (deshydroxyethyl bosentan impurity), and process for preparing and isolating thereof. Further provided are highly pure bosentan or a pharmaceutically acceptable salt thereof substantially free of deshydroxyethyl bosentan and bosentan dimer impurities, process for the preparation thereof, and pharmaceutical compositions comprising solid particles of highly pure bosentan or a pharmaceutically acceptable salt thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 300 microns.
摘要翻译：描述了基于波生坦总重量（波生坦结晶形式A5），其制备方法和药物组合物的水含量在约3-4重量％范围内的波生坦的高度稳定的结晶形式包括波生坦晶体A5。本文还提供了一种波生坦杂质，对叔丁基-N [6-羟基-5-（2-甲氧基苯氧基）-2-（2-嘧啶基）-4-嘧啶基]苯磺酰胺（脱羟乙基波生坦杂质），和制备和分离。还提供了高纯度的波生坦或其药学上可接受的盐，其基本上不含脱羟基乙基波生坦和波生坦二聚体杂质，其制备方法以及包含高纯度波生坦固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％的颗粒（D90）具有小于约300微米的尺寸。

8. 发明申请

US20120009226A1 HIGHLY PURE LAQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：高纯度液体或其药学上可接受的盐
公开(公告)号：US20120009226A1
公开(公告)日：2012-01-12
申请号：US13133994
申请日：2009-12-15
申请人： Girish Dixit , Krishnadatt Sharma , Nitin Sharadchandra Pradhan
发明人： Girish Dixit , Krishnadatt Sharma , Nitin Sharadchandra Pradhan
IPC分类号： A61K31/4704 , A61K9/14 , A61P25/00 , A61P3/10 , A61P25/28 , A61P29/00 , A61P1/00 , A61P17/06 , A61P11/06 , A61P9/10 , C07D215/56 , A61P19/04
CPC分类号： C07D215/56
摘要： Provided herein is an impurity of laquinimod, N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide (deschloro laquinimod impurity), and process for preparation and isolation thereof. Provided further herein is a highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity.
摘要翻译：本文提供了拉喹莫德，N-乙基-N-苯基-1,2-二氢-4-羟基-1-甲基-2-氧代喹啉-3-甲酰胺（脱氯洛喹莫德杂质）的杂质及其制备和分离方法。本文进一步提供了基本上不含脱氯洛喹莫德杂质的高纯度的拉喹莫德或其药学上可接受的盐，其制备方法和包含高纯度的拉喹莫德或其药学上可接受的盐基本上不含脱氯罗喹莫德杂质的药物组合物。

9. 发明申请

US20110142883A1 Amorphous Coprecipitates of Atorvastatin Pharmaceutically Acceptable Salts 审中-公开
标题翻译：阿托伐他汀药物可接受盐的无定形共沉淀物
公开(公告)号：US20110142883A1
公开(公告)日：2011-06-16
申请号：US12669543
申请日：2008-07-21
申请人： Girish Dixit , Anil Shahaji Khile , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Anil Shahaji Khile , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K31/40 , A61K9/14 , A61P9/00 , A61P9/10
CPC分类号： C07D207/416 , A61K9/146 , A61K9/1635 , A61K31/40
摘要： The present invention relates to stable amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts with pharmaceutically acceptable excipients, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advantageously, the amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts of the present invention have improved physiochemical characteristics that assist in the effective bioavailability
摘要翻译：本发明涉及阿托伐他汀药学上可接受的盐与药学上可接受的赋形剂的稳定无定形共沉淀物，制备方法，药物组合物及其治疗方法。有利地，本发明的阿托伐他汀药物可接受的盐的无定形共沉淀物具有改善的生理化学特征，其有助于有效的生物利用度

10. 发明申请

US20100278878A1 QUETIAPINE SALTS AND THEIR POLYMORPHS 失效
标题翻译： QUETIAPINE SALTS及其POLYMORPHS
公开(公告)号：US20100278878A1
公开(公告)日：2010-11-04
申请号：US12599085
申请日：2008-05-07
申请人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K31/554 , C07D417/04 , A61K9/14 , A61P25/00
CPC分类号： C07D281/14
摘要： The present invention relates to novel and stable salt forms of quetiapine, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides novel acid addition salts of quetiapine wherein the acid counter ion is provided by an acid selected from the group consisting of benzene sulfonic acid, dibenzoyl-L-(+)-tartaric acid and di-p-toluoyl-L-(+)-tartaric acid. The present invention also provides novel polymorphic forms of quetiapine salts selected from the group consisting of quetiapine hydrobromide, quetiapine sulfate, quetiapine nitrate and quetiapine citrate.
摘要翻译：本发明涉及喹硫平的新颖稳定的盐形式，制备方法，药物组合物及其处理方法。更具体地说，本发明提供了喹硫平的新型酸加成盐，其中酸抗衡离子由选自苯磺酸，二苯甲酰基-L-（+） - 酒石酸和二对甲苯酰基 - L - （+） - 酒石酸。本发明还提供了选自喹硫平氢溴酸盐，硫酸喹硫平，硝酸喹硫平和柠檬酸喹硫平的新型多晶型盐酸喹硫平盐。

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