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1. 发明授权

US08877947B2 Process for preparation of substantially pure fosamprenavir calcium and its intermediates 有权
标题翻译：制备基本纯净的福沙那韦钙及其中间体的方法
公开(公告)号：US08877947B2
公开(公告)日：2014-11-04
申请号：US13822197
申请日：2011-09-05
申请人： Surinder Kumar Arora , Samir Shanteshwar Shabade , Gaurav Kumar , Purna Chandra Ray , Girij Pal Singh
发明人： Surinder Kumar Arora , Samir Shanteshwar Shabade , Gaurav Kumar , Purna Chandra Ray , Girij Pal Singh
IPC分类号： C07D307/20 , C07F9/06 , G01N30/16 , C07D405/12
CPC分类号： C07F9/65515 , C07D307/20 , C07D405/12 , G01N30/16
摘要： The present invention relates to fosamprenavir calcium (Ia) substantially free of isomer impurity, (3R)tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propyl carbamate (Ib), and its process for preparation thereof. The present invention also provides fosamprenavir calcium intermediate, (S)-3-tetrahydrofuranyl-N-succinimidyl carbonate (IIa) substantially free of (R)-3-tetrahydrofuranylsuccinimidyl carbonate (IIb) and its process for preparation thereof.
摘要翻译：本发明涉及基本上不含异构体杂质的福桑那韦钙（Ia），（3R）四氢-3-呋喃基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基 -2-（膦酰氧基）丙基氨基甲酸酯（Ib）及其制备方法。本发明还提供了基本上不含（R）-3-四氢呋喃基琥珀酰亚胺基碳酸酯（IIb）的扇贝纳可维酸钙中间体（S）-3-四氢呋喃基-N-琥珀酰亚胺基碳酸酯（IIa）及其制备方法。

2. 发明申请

US20130225845A1 PROCESS FOR PREPARATION OF ESTRADIOL VALERATE AND A NOVEL CRYSTALLINE FORM A OF ESTRADIOL DIVALERATE 审中-公开
标题翻译：制备新戊酰胆碱酯和新戊酰胺的新型晶体形式的方法
公开(公告)号：US20130225845A1
公开(公告)日：2013-08-29
申请号：US13883593
申请日：2011-10-28
申请人： Sachin Arun Sasane , Vijay Ashok Ahire , Rajesh Vyas , Nandu Baban Bhise , Girij Pal Singh
发明人： Sachin Arun Sasane , Vijay Ashok Ahire , Rajesh Vyas , Nandu Baban Bhise , Girij Pal Singh
IPC分类号： C07J1/00
CPC分类号： C07J1/0074
摘要： The present invention relates to the process for the preparation of estradiol valerate (I) which involves isolation of crystalline estradiol divalerate (III) by crystallization from an alcoholic solvent.
摘要翻译：本发明涉及戊酸雌二醇（I）的制备方法，其涉及通过从醇溶剂中结晶分离结晶雌二醇二戊酸酯（III）。

3. 发明申请

US20120316238A1 NOVEL POLYMOMORPH OF DESVENLAFAXINE BENZOATE 有权
标题翻译：新戊酰苯酚的新型聚合物
公开(公告)号：US20120316238A1
公开(公告)日：2012-12-13
申请号：US13238953
申请日：2011-09-21
申请人： Gurvinder Pal SINGH , Dabeer Rauf Karnalkar , Hemraj Mahadeorao Lande , Girij Pal Singh
发明人： Gurvinder Pal SINGH , Dabeer Rauf Karnalkar , Hemraj Mahadeorao Lande , Girij Pal Singh
IPC分类号： A61K31/205 , C07C213/10 , A61P25/24 , C07C215/64
CPC分类号： A61K31/205 , C07C63/08 , C07C215/64 , C07C2601/14
摘要： The present invention relates to a novel crystalline form L of (±)-desvenlafaxine benzoate and process for the preparing of the same. Further, the present invention also relates to pharmaceutical composition of novel crystalline form L of desvenlafaxine benzoate and one or more pharmaceutically acceptable excipient.
摘要翻译：本发明涉及一种新型的（±） - 去甲基安非他明盐酸盐的结晶形式L及其制备方法。此外，本发明还涉及新型结晶形式L的脱甲霜拉西坦苯甲酸酯和一种或多种药学上可接受的赋形剂的药物组合物。

4. 发明授权

US07728151B2 Process for the purification of perindopril 失效
标题翻译：培哚普利净化方法
公开(公告)号：US07728151B2
公开(公告)日：2010-06-01
申请号：US11886382
申请日：2005-06-09
申请人： Girij Pal Singh , Himanshu Madhav Godbole , Umesh Babanrao Rananaware , Vilas Nathu Dhake , Suhas Ganpat Tambe , Sagar Purushottam Nehate
发明人： Girij Pal Singh , Himanshu Madhav Godbole , Umesh Babanrao Rananaware , Vilas Nathu Dhake , Suhas Ganpat Tambe , Sagar Purushottam Nehate
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： A dicyclohexyamine salt of compound of formula I, namely perindopril, having an X-ray powder diffraction pattern with characteristic peaks (2θ): 8.462, 10.624, 18.693, 9.424, 17.272, 14.177, 19.499, 20.765, 21.409, and 14.540. A process for preparation of the said salt of perindopril and its use in the purification of an impure perindopril and a process for purification of perindropril comprising formation of its salt with dicyclohexylamine. The present invention also relates to preparation of Perindopril tert-butyl amine salt directly from Perindopril dicyclohexylamine salt without isolating the free base.
摘要翻译：具有具有特征峰的X射线粉末衍射图（2＆amp; Thetas）的式I化合物的二环氧胺盐，即培哚普利，为8.462,10.624,18.693,9.424,17.272,14.177,19.499,20.765，21.409和14.540。制备所述所述培哚普利盐的方法及其在纯化培哚普利的纯化中的用途和包括与二环己基胺形成盐的培哚普利的纯化方法。本发明还涉及直接从培哚普利二环己基胺盐制备培哚普利叔丁胺盐而不分离游离碱。

5. 发明申请

US20100105925A1 NOVEL PROCESS FOR PREPARATION OF DULOXETINE HYDROCHLORIDE 失效
标题翻译：用于制备DOROXETINE氢氯化物的新方法
公开(公告)号：US20100105925A1
公开(公告)日：2010-04-29
申请号：US12530214
申请日：2008-03-05
申请人： Rajinder Singh Siyan , Sunil Kumar Vinubhai Gohel , Girij Pal Singh
发明人： Rajinder Singh Siyan , Sunil Kumar Vinubhai Gohel , Girij Pal Singh
IPC分类号： C07D333/20 , C07C51/42
CPC分类号： C07D333/20
摘要： An improved process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following: (i) preparation of racemic condensed compound (RS)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (4) by reaction of racemic hydroxy compound (2) with 1-fluoronaphthalene (3) in presence of a base such as sodamide, potassium amide or potassium bis(trimethylsilyl)amide (KHDMS) in polar aprotic solvent, (ii) optical resolution of racemic condensed compound (5a+5b) with di-benzoyl-L-tartaric acid (7, DBTA, R═H) or di-para-anisoyl-L-tartaric acid (7, DATA, R═OCH3) to obtain crude (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine dibenzoyl tartarate salt (8a) or (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine di-p-anisoyl tartarate salt (9a) respectively, (iii) optionally purification of crude tartarate salts (8a or 9a) by crystallization, (iv) optionally purification of duloxetine hydrochloride (1) by crystallization and (v) racemization of undesired (R)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (5b) by treatment with base potassium bis(trimethylsilyl)amide (KHDMS) to obtain racemic mixture of condensed compounds (5a and 5b).
摘要翻译：具有手性纯度大于99.9％的改进的度洛西汀盐酸盐（1）的改进方法，其特征在于：（i）制备外消旋缩合化合物（RS）-N，N-二甲基-3-（1-萘氧基）3-（2-噻吩基）丙胺（4），通过外消旋羟基化合物（2）与1-氟萘（3）在碱如Sodamide，氨基化钾或双（三甲基甲硅烷基）氨基钾（KHDMS）的存在下反应，在极性非质子溶剂中，（ii）用二苯甲酰基-L-酒石酸（7，DBTA，R = H）或二对甲氧基苯甲酰基-L-酒石酸（7）的外消旋缩合化合物（5a + 5b），DATA，R = OCH 3），得到粗（S）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺二苯甲酰酒石酸盐（8a）或（S）-N，N （3-萘基氧基）-3-（2-噻吩基）丙胺二对茴香酰酒石酸盐（9a），（iii）任选地通过结晶纯化粗酒石酸盐（8a或9a），（iv ）任选地通过哭泣来纯化度洛西汀盐酸盐（1）（R）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺（5b）通过用双（三甲基甲硅烷基）氨基钾酰胺（KHDMS）处理），得到缩合化合物（5a和5b）的外消旋混合物。

6. 发明授权

US07521566B2 Process for preparation of perindopril and salts thereof 有权
标题翻译：培哚普利及其盐的制备方法
公开(公告)号：US07521566B2
公开(公告)日：2009-04-21
申请号：US10547243
申请日：2003-02-28
申请人： Debashish Datta , Girij Pal Singh , Himanshu Madhav Godbole , Rajinder Singh Siyan
发明人： Debashish Datta , Girij Pal Singh , Himanshu Madhav Godbole , Rajinder Singh Siyan
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , C07C227/32 , C07C227/34 , C07C229/12
摘要： A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe, convenient and cost-effective. The process involves reaction of compound of formula (I), wherein X is chlorine or bromine with compound of formula (VII) wherein A signifies that the six-membered ring of the bicyclic system is either saturated or unsaturated to give compound of formula (VIII), wherein A is as defined above, followed by catalytic hydrogenation of the compound of formula (VIII) thus obtained to give the perindopril of formula (II). The above process for the manufacture of perindopril would specifically avoid the use of harmful chemicals like phosgene or costly coupling agents like dicyclohexylcarbodiimide and 1-hydroxybenxotriazole usually used for such manufacture. The process would also not require any intervention of a catalyst and does not require any alkaline or acidic reaction conditions. Importantly, the process provides for manufacture of perindopril with high stereoselectively giving perindopril (II) having (S)-configuration in all the five chiral centres of the molecule, conforming to pharmacoepeial specifications. The invention also relates to a method for preparation of the compound of formula (I) and also to a method for preparation of N-[(S)-1-carbethoxybutyl]-(S)-alanine of formula (III) used in the process.
摘要翻译：一种制备式（II）培哚普利及其盐的方法，其简单，安全，方便和具有成本效益。该方法包括式（I）化合物，其中X是氯或溴与式（Ⅶ）化合物反应，其中A表示双环系统的六元环是饱和或不饱和的，得到式（Ⅷ）化合物），其中A如上所定义，然后将由此获得的式（VIII）化合物进行催化氢化，得到式（II）的培哚普利。上述制造培哚普利的方法将特别避免使用通常用于制造的有害化学物质如光气或昂贵的偶联剂如二环己基碳二亚胺和1-羟基苯并三唑。该方法也不需要任何催化剂的干预，并且不需要任何碱性或酸性反应条件。重要的是，该方法提供了高度立体选择性地给予符合药代动力学规范的在分子的所有五个手性中心具有（S） - 构型的培哚普利（II）的培哚普利的培哚普利。本发明还涉及制备式（I）化合物的方法，还涉及制备式（III）化合物的N - [（S）-1-乙酯基丁基] - （S） - 丙氨酸的方法，处理。

7. 发明申请

US20080139823A1 Process for the Purification of Perindopril 失效
标题翻译：培哚普利净化方法
公开(公告)号：US20080139823A1
公开(公告)日：2008-06-12
申请号：US11886382
申请日：2005-06-09
申请人： Girij Pal Singh , Himanshu Madhav Godbole , Umesh Babanrao Rananaware , Vilas Nathu Dhake , Suhas Ganpat Tambe , Sagar Purushottam Nehate
发明人： Girij Pal Singh , Himanshu Madhav Godbole , Umesh Babanrao Rananaware , Vilas Nathu Dhake , Suhas Ganpat Tambe , Sagar Purushottam Nehate
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： A dicyclohexyamine salt of compound of formula I, namely perindopril, having an X-ray powder diffraction pattern with characteristic peaks (2θ): 8.462, 10.624, 18.693, 9.424, 17.272, 14.177, 19.499, 20.765, 21.409, and 14.540. A process for preparation of the said salt of perindopril and its use in the purification of an impure perindopril and a process for purification of perindropril comprising formation of its salt with dicyclohexylamine. The present invention also relates to preparation of Perindopril tert-butyl amine salt directly from Perindopril dicyclohexylamine salt without isolating the free base.
摘要翻译：式I化合物的二环氧胺盐，即培哚普利，具有特征峰（2θ）的X射线粉末衍射图：8.462,10.624,18.693,9.424,17.272,14.177,19.499,20.765，21.409和14.540。制备所述所述培哚普利盐的方法及其在纯化培哚普利的纯化中的用途和包括与二环己基胺形成盐的培哚普利的纯化方法。本发明还涉及直接从培哚普利二环己基胺盐制备培哚普利叔丁胺盐而不分离游离碱。

8. 发明授权

US08981110B2 Process for the preparation of olmesartan medoxomil 有权
标题翻译：奥美沙坦酯的制备方法
公开(公告)号：US08981110B2
公开(公告)日：2015-03-17
申请号：US14237213
申请日：2012-07-31
申请人： Rajendra Vishwanath Firke , Ujjwal Komalsing Sisodiya , Chandrakant Shriram Bhangale , Radhakrishna Bhikaji Shivdavkar , Himanshu Madhav Godbole , Girij Pal Singh
发明人： Rajendra Vishwanath Firke , Ujjwal Komalsing Sisodiya , Chandrakant Shriram Bhangale , Radhakrishna Bhikaji Shivdavkar , Himanshu Madhav Godbole , Girij Pal Singh
IPC分类号： C07D403/10 , A61K31/41 , C07D405/14
CPC分类号： C07D405/14
摘要： The present invention provides novel process for preparation of olmesartan medoxomil (I) substantially free of olmesartan acid impurity (II) comprising, reacting trityl olmesartan medoxomil (III) with acid, filtering the precipitate of trityl alcohol, subjecting the filtrate to agitated thin film drying and recovering olmesartan medoxomil (I).
摘要翻译：本发明提供了制备基本上不含奥美沙坦杂质（II）的奥美沙坦酯（I）的新方法，其包括使三苯甲基奥美沙坦酯（III）与酸反应，过滤三苯甲基醇沉淀物，对滤液进行搅拌薄膜干燥并回收奥美沙坦酯（I）。

9. 发明申请

US20140179930A1 PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL 有权
标题翻译：制备奥美沙坦的方法
公开(公告)号：US20140179930A1
公开(公告)日：2014-06-26
申请号：US14237213
申请日：2012-07-31
申请人： Rajendra Vishwanath Firke , Ujjwal Komalsing Sisodia , Chandrakant Shriram Bhangale , Radhakrishna Bhikaji Shivdavkar , Himanshu Madhav Godbole , Girij Pal Singh
发明人： Rajendra Vishwanath Firke , Ujjwal Komalsing Sisodia , Chandrakant Shriram Bhangale , Radhakrishna Bhikaji Shivdavkar , Himanshu Madhav Godbole , Girij Pal Singh
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention provides novel process for preparation of olmesartan medoxomil (I) substantially free of olmesartan acid impurity (II) comprising, reacting trityl olmesartan medoxomil (III) with acid, filtering the precipitate of trityl alcohol, subjecting the filtrate to agitated thin film drying and recovering olmesartan medoxomil (I).
摘要翻译：本发明提供了制备基本上不含奥美沙坦杂质（II）的奥美沙坦酯（I）的新方法，其包括使三苯甲基奥美沙坦酯（III）与酸反应，过滤三苯甲基醇沉淀物，对滤液进行搅拌薄膜干燥并回收奥美沙坦酯（I）。

10. 发明申请

US20140155607A1 Novel Salts of Raltegravir 有权
标题翻译： Raltegravir的新型盐
公开(公告)号：US20140155607A1
公开(公告)日：2014-06-05
申请号：US14009178
申请日：2012-04-04
申请人： Purna Chandra Ray , Ashok Sopanrao Yadav , Dnyaneshwar Tukaram Singare , Surinder Kumar Arora , Girij Pal Singh
发明人： Purna Chandra Ray , Ashok Sopanrao Yadav , Dnyaneshwar Tukaram Singare , Surinder Kumar Arora , Girij Pal Singh
IPC分类号： C07D413/12
CPC分类号： C07D413/12 , A61K31/513 , C07C211/04
摘要： The present invention provides novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation.
摘要翻译：本发明提供了raltegravir的新型盐，即raltegravir的葡甲胺盐，erbumine盐，铵盐，三盐和L-精氨酸盐及其制备方法。

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