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11. 发明申请

US20060189670A1 Process for the preparation of anastrozole and intermediates thereof 审中-公开
标题翻译：制备阿那曲唑及其中间体的方法
公开(公告)号：US20060189670A1
公开(公告)日：2006-08-24
申请号：US11359248
申请日：2006-02-22
申请人： Anil Khile , Narendra Joshi , Shekhar Bhirud
发明人： Anil Khile , Narendra Joshi , Shekhar Bhirud
IPC分类号： C07D249/08 , A61K31/4196
CPC分类号： C07D249/08 , Y02P20/55
摘要： A process for the preparation of anastrozole is provided, the process comprising: (a) reacting 3,5-bis(1-cyano-1-methylethyl)benzyl halide with a 4-Z-1,2,4-triazole compound of the formula wherein Z is a protecting group to produce 2,2′-[5-(4-Z-1,2,4-triazolium-1-ylmethyl)-1,3-phenylene]di(2-methylpropionitrile) halide; and (b) deprotecting the 2,2′-[5-(4-Z-1,2,4-triazolium-1-ylmethyl)-1,3-phenylene]di(2-methylpropionitrile)halide to produce anastrozole. Also provided is anastrozole substantially free of its isomers.
摘要翻译：提供了一种制备阿那曲唑的方法，该方法包括：（a）使3,5-双（1-氰基-1-甲基乙基）苄基卤与4-Z-1,2,4-三唑化合物其中Z是产生2,2' - [5-（4-Z-1,2,4-三唑鎓-1-基甲基）-1,3-亚苯基]二（2-甲基丙腈）卤化物的保护基; 和（b）使2,2' - [5-（4-Z-1,2,4-三唑鎓-1-基甲基）-1,3-亚苯基]二（2-甲基丙腈）卤化物脱保护而制备阿那曲唑。还提供了基本上不含其异构体的阿那曲唑。

12. 发明申请

US20050250706A1 Processes for the preparation of alpha polymorph of perindopril erbumine 审中-公开
标题翻译：培哚普林卵白素α多晶型物的制备方法
公开(公告)号：US20050250706A1
公开(公告)日：2005-11-10
申请号：US11122731
申请日：2005-05-05
申请人： Narendra Joshi , Shekhar Bhirud , Kodali Rao
发明人： Narendra Joshi , Shekhar Bhirud , Kodali Rao
IPC分类号： A61K31/405 , A61K38/04 , C07D209/42 , C07K5/02
CPC分类号： C07K5/022 , C07D209/42
摘要： Processes for the preparation of an alpha polymorph of perindopril erbumine is provided comprising (a) forming a solution comprising perindopril erbumine in one or more ketones; (b) heating the solution to reflux; and (c) cooling the solution to a temperature sufficient to form the alpha polymorph of perindopril erbumine. The alpha polymorphs of perindopril erbumine obtained herein have a high purity level.
摘要翻译：提供了用于制备培哚普利埃尔本辛的α多晶型物的方法，包括（a）在一种或多种酮中形成包含培哚普利埃尔本辛的溶液; （b）将溶液加热回流; 和（c）将溶液冷却到足以形成培哚普利埃尔本的α多晶型物的温度。本文获得的培哚普利埃尔本的α多晶型物具有高纯度水平。

13. 发明申请

US20060281800A1 Polymorphic form of olmesartan and process for its preparation 审中-公开
标题翻译：奥美沙坦的多形态及其制备方法
公开(公告)号：US20060281800A1
公开(公告)日：2006-12-14
申请号：US11402738
申请日：2006-04-12
申请人： Bobba Venkata Kumar , Girish Patel , Nitin Sharad Pradhan , Shekhar Bhirud
发明人： Bobba Venkata Kumar , Girish Patel , Nitin Sharad Pradhan , Shekhar Bhirud
IPC分类号： A61K31/4178 , C07D405/14
CPC分类号： C07D405/14
摘要： A process for the preparation of a novel crystalline polymorph of olmesartan medoxomil, designated Form G, is provided comprising the steps of (a) preparing a solution comprising olmesartan medoxomil and one or more solvents selected from the group consisting of a nitrile, alcohol and mixtures thereof at a suitable temperature to obtain a solution; and (b) recovering olmesartan medoxomil substantially in polymorph Form G from the solution. A novel polymorph Form G of olmesartan medoxomil and pharmaceutical compositions containing same are also provided herein.
摘要翻译：提供了一种制备名为G型的奥美沙坦酯的新结晶多晶型物的方法，包括以下步骤：（a）制备包含奥美沙坦酯和选自腈，醇和混合物的一种或多种溶剂的溶液得到溶液; 和（b）从溶液中基本上以多晶型G回收奥美沙坦酯。本文还提供奥美沙坦酯的新型多晶型物G和含有它们的药物组合物。

14. 发明申请

US20060084806A1 Processes for the preparation of imidazo[1,2-a] pyridine derivatives 审中-公开
标题翻译：咪唑并[1,2-a]吡啶衍生物的制备方法
公开(公告)号：US20060084806A1
公开(公告)日：2006-04-20
申请号：US11186662
申请日：2005-07-21
申请人： Ramasubramanian Sridharan , Shekhar Bhirud , Vandanapu Purushotham
发明人： Ramasubramanian Sridharan , Shekhar Bhirud , Vandanapu Purushotham
IPC分类号： C07D471/02
CPC分类号： C07D471/04
摘要： A process for the preparation of imidazo[1,2-a]pyridine derivatives of the formula I: wherein R is hydrogen, halogen or a C1-C4 alkyl group; R1 and R2 are independently hydrogen, a straight or branched C1-C6 alkyl group which is unsubstituted or substituted by one or more halogen atoms, hydroxyl, N(C1-C4 alkyl)2, carbamoyl or C1-C4 alkoxy radicals, a C1-C6 alkyl hydroxy group, a C3-C6 cycloalkyl radical, a benzyl radical, a phenyl radical or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a substituted or unsubstituted heterocyclic group optionally containing one or more additional heterocyclic atoms; and R3 and R4 are independently hydrogen, halogen or a C1-C4 alkyl group, or a pharmaceutically acceptable salt thereof, the process comprising (a) reacting an imidazo[1,2-a]pyridine carboxylic acid of the formula II wherein R, R3 and R4 have the aforestated meanings with a halogenating agent in the absence of a solvent to form an acid halide intermediate and (b) reacting the acid halide intermediate with an amine of the formula HNR1R2 wherein R1 and R2 have the aforestated meanings to form the compound of formula I.
摘要翻译：制备式I的咪唑并[1,2-a]吡啶衍生物的方法：其中R是氢，卤素或C 1 -C 4烷基 ; R 1和R 2独立地是氢，直链或支链C 1 -C 6烷基，其是未被取代或被一个或多个卤素原子取代，羟基，N（C 1 -C 4烷基）亚烷基，氨基甲酰基或C 1 -C 6烷基， C 1 -C 4烷氧基，C 1 -C 6烷基羟基，C 3 -C 6烷基羟基，C 1 -C 6烷基羟基， C 1 -C 6环烷基，苄基，苯基或R 1和R 2与它们的氮原子一起被结合在一起形成任选含有一个或多个另外的杂环原子的取代或未取代的杂环基; 和R 3和R 4独立地是氢，卤素或C 1 -C 4烷基，或该方法包括（a）使式II的咪唑并[1,2-a]吡啶羧酸反应，其中R 3，R 3和R 4， >在没有溶剂的情况下具有卤化剂的上述含义，以形成酰卤中间体，和（b）使酰卤中间体与式HNR 1 R 2的胺反应其中R 1和R 2具有上述含义以形成式I化合物。

15. 发明申请

US20060211867A1 Process for the preparation of perindopril 失效
标题翻译：培哚普利的制备方法
公开(公告)号：US20060211867A1
公开(公告)日：2006-09-21
申请号：US11386011
申请日：2006-03-21
申请人： Narendra Joshi , Shekhar Bhirud , Kodali Rao , Buddhavarapu Ramam , Vijay Soni
发明人： Narendra Joshi , Shekhar Bhirud , Kodali Rao , Buddhavarapu Ramam , Vijay Soni
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , Y02P20/55
摘要： A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.
摘要翻译：提供了一种制备培哚普利的方法，包括将式II的N - [（S）-1-乙酯基） - （S） - 丙氨酰卤进行缩合：其中X是卤素与（2S，3aS，7aS）-2-羧基全氢吲哚其中R是氢或保护基。

16. 发明申请

US20060211866A1 Process for the preparation of angiotensin receptor blockers and intermediates thereof 审中-公开
标题翻译：制备血管紧张素受体阻滞剂及其中间体的方法
公开(公告)号：US20060211866A1
公开(公告)日：2006-09-21
申请号：US11386010
申请日：2006-03-21
申请人： Narendra Joshi , Kodali Rao , Buddhavarapu Ramam , Shekhar Bhirud
发明人： Narendra Joshi , Kodali Rao , Buddhavarapu Ramam , Shekhar Bhirud
IPC分类号： C07D403/02 , C07D235/04
CPC分类号： C07D257/04 , C07D235/20 , C07D403/10
摘要： A process for the preparation of a biphenyl-containing compound of general formula I: wherein R1 is a C3-6 carbonyl containing compound; R2 is a substituted or unsubstituted, straight or branched C3-6 alkyl group, or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a substituted heterocyclic group selected from the group consisting of substituted or unsubstituted imidazoles, substituted or unsubstituted benzimidazoles and substituted or unsubstituted 1,3-diazaspiro[4,4]non-1-en-4-one; and R3 is a carboxylic acid ester, cyano, a substituted or unsubstituted 1H-tetrazolyl group or a substituted or unsubstituted group which may be converted in vivo into a carboxy group is provided, the process comprising reacting a compound of general formula II: wherein R1 and R2 have the aforestated meanings with a compound of general formula III: wherein Z is a leaving group and R3 has the aforestated meaning in a biphasic solvent system in the presence of a phase transfer catalyst.
摘要翻译：一种制备含联苯的通式I化合物的方法：其中R 1是含3-6个碳原子的化合物; R 2是取代或未取代的直链或支链C 3-6 - 烷基，或R 1和R 2， SUP与它们所键合的氮原子一起连接在一起形成选自取代或未取代的咪唑，取代或未取代的苯并咪唑和取代或未取代的1,3-二氮杂螺[4,4] 非1-烯-4-酮; R 3是可以在体内转化为羧基的羧酸酯，氰基，取代或未取代的1H-四唑基或取代或未取代的基团，该方法包括使通式II的化合物：其中R 1和R 2具有通式III的化合物的前述含义：其中Z是离去基团，R 3 在相转移催化剂存在下，在双相溶剂体系中具有上述含义。

17. 发明申请

US20060111560A1 Process for the preparation of crystalline form II of clarithromycin 审中-公开
标题翻译：制备克拉霉素晶型II的方法
公开(公告)号：US20060111560A1
公开(公告)日：2006-05-25
申请号：US11264835
申请日：2005-11-01
申请人： Bobba Kumar , Changdev Raut , Shekhar Bhirud
发明人： Bobba Kumar , Changdev Raut , Shekhar Bhirud
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： A process for preparing Form II crystals of clarithromycin is provided comprising (a) treating clarithromycin with a carboxylic acid in an organic solvent to provide a clarithromycin acid salt; and, (b) heating the clarithromycin acid salt at a temperature capable of providing Form II crystals of clarithromycin.
摘要翻译：提供了一种制备克拉霉素II型晶体的方法，包括（a）在有机溶剂中用羧酸处理克拉霉素以提供克拉霉素酸盐; 和（b）在能够提供克拉霉素II型晶体的温度下加热克拉霉素酸盐。

18. 发明申请

US20050203297A1 Process for the preparation of carboxamide compounds 失效
标题翻译：制备羧酰胺化合物的方法
公开(公告)号：US20050203297A1
公开(公告)日：2005-09-15
申请号：US11077723
申请日：2005-03-11
申请人： Bobba Sivakumar , Shekhar Bhirud , Chandrasekhar Batchu , Sanjay Kale
发明人： Bobba Sivakumar , Shekhar Bhirud , Chandrasekhar Batchu , Sanjay Kale
IPC分类号： C07D223/18
CPC分类号： C07D223/28 , C07D223/26
摘要： A process for preparing 5H-dibenz[b,f]azepine-5-carboxamide of the general formula: wherein R1, R2, R3 and R4 are the same or different and can be hydrogen, halogen, nitro, cyano, carboxyl, R, —CO(R), —OCO(R), —O(R), —N(R)2, —CON(R)2, and —COO(R), wherein R is selected from the group consisting of C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C5-C10 cycloalkenyl, C2-C10 alkynyl, and C6-C20 aryl, wherein the two A groups of —N(A)2 and —CON(A)2 can be the same or different, and wherein R2 and R3 can together form a bond is provided; the process comprising reacting 5H-dibenz[b,f]azepine of the general formula wherein R1, R2, R3 and R4 have the aforementioned meanings, with one or more alkali or alkaline-earth cyanates and in the presence of one or more unsaturated dicarboxylic acids.
摘要翻译：制备通式如下的5H-二苯并[b，f]吖庚因-5-甲酰胺的方法：其中R 1，R 2，R 3，（R），-O（R）， - OCO（R），-O（R）， -N（R）2，-CON（R）2，和-COO（R），其中R选自C 1〜 C 1 -C 10烷基，C 3 -C 10环烷基，C 2 -C 10烷基，C 1 -C 10烷基， 10个亚烷基，C 5 -C 10环烯基，C 2 -C 10炔基，以及 C 6 -C 20芳基，其中-N（A）2和-CON（A）2的两个A基团可以相同或不同，并且其中R 2和R 3可以一起形成键; 该方法包括使通式为的5H-二苯并[b，f]吖庚因其中R 1，R 2，R 3，R 3和R 3，具有上述含义，具有一种或多种碱金属或碱土氰酸盐，并且在一种或多种不饱和二羧酸存在下。

19. 发明申请

US20050203287A1 Process for the preparation of sulfamate derivatives 审中-公开
标题翻译：制备氨基磺酸酯衍生物的方法
公开(公告)号：US20050203287A1
公开(公告)日：2005-09-15
申请号：US11077722
申请日：2005-03-11
申请人： Chandrasekhar Batchu , Biju Kumar Pillai , Shekhar Bhirud
发明人： Chandrasekhar Batchu , Biju Kumar Pillai , Shekhar Bhirud
IPC分类号： C07D317/44 , C07H5/06
CPC分类号： C07H9/04 , C07D317/44 , C07H11/00
摘要： An improved process for the preparation of sulfamate derivatives such as topiramate is provided comprising (a) reacting an alcohol with sulfuryl chloride in the presence of an amine base and in a first halogenated hydrocarbon solvent selected from the group consisting of aliphatic halogenated hydrocarbon solvents having 1 to 12 carbon atoms and at least three halogen atoms, aliphatic halogenated hydrocarbon solvents having 2 to 12 carbon atoms and less than three halogen atoms, aromatic halogenated hydrocarbon solvents having 6 to 18 carbon atoms and mixtures thereof to produce a chlorosulfate intermediate and (b) reacting the chlorosulfate intermediate with an amine of the formula R1NH2, wherein R1 is hydrogen or an alkyl from 1 to 4 carbon atoms, in a second halogenated hydrocarbon solvent selected from the group consisting of aliphatic halogenated hydrocarbon solvents having 1 to 12 carbon atoms and at least three halogen atoms, aliphatic halogenated hydrocarbon solvents having 2 to 12 carbon atoms and less than three halogen atoms, aromatic halogenated hydrocarbon solvents having 6 to 18 carbon atoms and mixtures thereof.
摘要翻译：提供了一种制备氨基磺酸酯衍生物如托吡酯的改进方法，其包括（a）在胺碱存在下使醇与磺酰氯反应，并且在选自脂族卤代烃溶剂的第一卤代烃溶剂中具有1 至12个碳原子和至少三个卤素原子，具有2至12个碳原子和少于3个卤素原子的脂族卤代烃溶剂，具有6至18个碳原子的芳族卤代烃溶剂及其混合物，以产生氯代硫酸盐中间体和（b）使氯代硫酸盐中间体与式R 1 NH 2的胺反应，其中R 1是氢或1至4个碳原子的烷基在选自具有1至12个碳原子和至少3个卤素原子的脂族卤代烃溶剂的第二卤代烃溶剂中，脂族卤代具有2至12个碳原子和少于3个卤素原子的烃溶剂，具有6至18个碳原子的芳族卤代烃溶剂及其混合物。

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