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1. 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。

2. 发明授权

US08101597B2 Quetiapine salts and their polymorphs 失效
标题翻译：喹硫平盐及其多晶型物
公开(公告)号：US08101597B2
公开(公告)日：2012-01-24
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： A61P25/18 , A61K31/55 , C07D281/16
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。

3. 发明申请

US20120164188A1 PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES 审中-公开
标题翻译： PALIPERIDONE或其药物接受的盐，无特殊物质
公开(公告)号：US20120164188A1
公开(公告)日：2012-06-28
申请号：US13381716
申请日：2010-09-10
申请人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan
发明人： Girish Dixit , Anil Shahaji Khile , Jayesh Laljibhai Patel , Nitin Sharadchandra Pradhan
IPC分类号： A61K31/519 , A61K9/14 , A61P25/18 , C07D471/04
CPC分类号： C07D471/04
摘要： Provided herein are impurities of paliperidone, 3-[2-[4-[1-(4-fluoro-2-hydroxyphenyl)methanoyl]piperidinyl-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (methanoyl impurity), 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidin-4,9-dione (9-keto impurity), and processes for preparing and isolating thereof. Provided further herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities, process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities. Provided also herein are improved and efficient processes for preparing paliperidone intermediates.
摘要翻译：本文提供的是普利培酮，3- [2- [4- [1-（4-氟-2-羟基苯基）甲酰基]哌啶-1-基]乙基] -2-甲基-6,7,8,9- 四氢-4H-吡啶并[1,2-a]嘧啶-4-酮（甲酰基杂质），3- [2- [4-（6-氟-1,2-苯并异恶唑-3-基）-1-哌啶基] 乙基] -2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮（脱羟基杂质）和3- [2- [4-（6-氟-1,2-苯并异恶唑-3-基） -1-哌啶基]乙基] -2-甲基-7,8-二氢-6H-吡啶并[1,2-a]嘧啶-4,9-二酮（9-酮杂质），以及其制备和分离方法。本文进一步提供了基本上不含甲酰基，脱羟基和9-酮杂质的高度纯的普利培酮或其药学上可接受的盐，其制备方法和包含高度纯的普利培酮或其药学上可接受的盐基本上不含甲酰基的药物组合物，脱羟基和9-酮杂质。本文还提供了用于制备利培酮中间体的改进和有效的方法。

4. 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

5. 发明申请

US20100260851A1 Novel Polymorph of Atorvastatin Calcium and Use Thereof for the Preparation of Amorphous Atorvastatin Calcium 审中-公开
标题翻译：阿托伐他汀钙的新型多态性及其用于制备无定形阿托伐他汀钙的方法
公开(公告)号：US20100260851A1
公开(公告)日：2010-10-14
申请号：US12668433
申请日：2008-07-11
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： A61K9/14 , A61K31/40 , C07D207/34 , A61P3/06 , A61P9/10
CPC分类号： C07D207/34
摘要： The present invention provides a novel polymorphic form of atorvastatin calcium, designated as form Al, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a process for the preparation of highly pure amorphous atorvastatin calcium using the novel atorvastatin calcium form Al. The present invention also relates to novel amorphous form of atorvastatin tert-butyl ester, chemically known as [R-(R*,R*)]-2-(4-fluorophenyl)-[β],[δ]-dihydroxy -5-(1-methylethyl)-3-phenyl-4-(phenylcarbamoyl-1H-pyrrole-1-heptanoicacid tert-butyl ester, process for the preparation, and its application for preparing highly pure atorvastatin and its pharmaceutically acceptable salts thereof. The present invention also relates to use of the novel amorphous atorvastatin tert-butyl ester and novel atorvastatin calcium form al for preparing amorphous atorvastatin calcium.
摘要翻译：本发明提供了一种新型的阿托伐他汀钙多形态，称为形式A1，制备方法，药物组合物及其处理方法。本发明还提供使用新型阿托伐他汀钙形式Al制备高纯度无定形阿托伐他汀钙的方法。本发明还涉及化学上称为[R-（R *，R *）] - 2-（4-氟苯基） - [[b]]，[δ] - 二羟基 - 5-（1-甲基乙基）-3-苯基-4-（苯基氨基甲酰基-1H-吡咯-1-庚酸叔丁酯，其制备方法及其制备高纯度阿托伐他汀及其药学上可接受的盐的应用）本发明还涉及新型无定形阿托伐他汀叔丁酯和新型阿托伐他汀钙形式用于制备无定形阿托伐他汀钙的用途。

6. 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。

7. 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。

8. 发明申请

US20110014246A1 AMORPHOUS ARFORMOTEROL L-(+)-TARTRATE 审中-公开
标题翻译： AMORPHOUS ARFORMOTEROL L - （+） - TARTRATE
公开(公告)号：US20110014246A1
公开(公告)日：2011-01-20
申请号：US12919028
申请日：2009-02-27
申请人： Girish Dixit , Nandkumar Gaikwad , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Nandkumar Gaikwad , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K31/194 , C07C59/255 , A61K9/00 , A61P11/08
CPC分类号： A61K9/14 , A61K9/1688 , A61K31/167 , Y10T428/2982
摘要： Disclosed herein is a novel and stable amorphous form of arformoterol L-(+)-tartrate, a process for its preparation, pharmaceutical compositions comprising amorphous arformoterol L-(+)-tartrate, and methods of treating with amorphous arformoterol L-(+)-tartrade.
摘要翻译：本文公开了一种新型和稳定的无定形形式的阿莫曲醇L - （+） - 酒石酸盐，其制备方法，包含无定形阿霉醇L - （+） - 酒石酸盐的药物组合物，以及用无定形阿霉醇L - （+） - -tartrade

9. 发明申请

US20100104649A1 Lercanidipine Hydrochloride Polymorphs and an Improved Process for Preparation of 1,1,N-Trimethyl-N-(3,3-Diphenylpropyl)-2-Aminoethyl Acetoacetate 审中-公开
标题翻译：氯卡地平盐酸多巴胺和制备1,1,1-三甲基-N-（3,3-二苯基丙基）-2-氨基乙基乙酰乙酸酯的改进方法
公开(公告)号：US20100104649A1
公开(公告)日：2010-04-29
申请号：US12530101
申请日：2008-03-05
申请人： Girish Dixit , Krishnadatt Baldevprasad Sharma , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Girish Dixit , Krishnadatt Baldevprasad Sharma , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： A61K9/14 , C07D213/80 , C07C69/66 , A61K31/44 , A61P9/12
CPC分类号： C07C219/06 , C07C213/06 , C07D213/803
摘要： Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of substantially pure Lercanidipine intermediate, 1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl acetoacetate. The intermediate is useful for preparing Lercanidipine, or a pharmaceutically acceptable salt thereof, in high yield and purity. The present invention further provides a novel crystalline form of Lercanidipine hydrochloride and a process for its preparation. The present invention also provides a process for the preparation of amorphous form of Lercanidipine hydrochloride.
摘要翻译：本文公开了改进的，商业上可行的和工业上有利的制备基本上纯的氯卡地平中间体1,1,1-三甲基-N-（3,3-二苯基丙基）-2-氨乙基乙酰乙酸酯的方法。该中间体可用于以高产率和纯度制备乐卡尼地平或其药学上可接受的盐。本发明还提供了一种新的盐酸乐卡尼平的结晶形式及其制备方法。本发明还提供了制备盐酸乐卡地平的无定形形式的方法。

10. 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.

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