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1. 发明授权

US07291745B2 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：US07291745B2
公开(公告)日：2007-11-06
申请号：US11386011
申请日：2006-03-21
申请人： Narendra Shriram Joshi , Shekhar Bhaskar Bhirud , Kodali Eswara Rao , Buddhavarapu Pattabhi Ramam , Vijay Soni
发明人： Narendra Shriram Joshi , Shekhar Bhaskar Bhirud , Kodali Eswara Rao , Buddhavarapu Pattabhi Ramam , Vijay Soni
IPC分类号： C07D209/12
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。

2. 发明授权

US09056813B2 Process for preparation of fingolimod 有权
标题翻译：芬戈莫德的制备方法
公开(公告)号：US09056813B2
公开(公告)日：2015-06-16
申请号：US14373214
申请日：2013-01-17
申请人： Milind Gharpure , Krishna Narawade , Prem Chand , Shekhar Bhaskar Bhirud
发明人： Milind Gharpure , Krishna Narawade , Prem Chand , Shekhar Bhaskar Bhirud
IPC分类号： C07C209/78 , C07C215/10 , C07C29/14 , C07C209/16 , C07C45/30 , C07C29/00 , C07C45/64 , C07C67/293 , C07C17/16 , C07C303/28 , C07C231/12 , C07C213/08 , C07C215/28
CPC分类号： C07C209/78 , C07C17/16 , C07C29/00 , C07C29/14 , C07C45/30 , C07C45/64 , C07C67/293 , C07C209/16 , C07C213/08 , C07C215/10 , C07C215/28 , C07C231/12 , C07C303/28 , C07C309/66 , C07C233/47 , C07C22/04 , C07C69/157 , C07C49/82 , C07C33/20
摘要： The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA.
摘要翻译：本发明提供了一种不含式IA的区域异构体杂质化合物的芬戈莫德，式I化合物或其药学上可接受的盐的制备方法。

3. 发明授权

US07312329B2 Process for the preparation of pyrimidine derivatives 失效
标题翻译：制备嘧啶衍生物的方法
公开(公告)号：US07312329B2
公开(公告)日：2007-12-25
申请号：US11004755
申请日：2004-12-03
申请人： Narendra Joshi , Shekhar Bhaskar Bhirud , Batchu Chandrasekhar , K. Eswara Rao , Subhash Damle
发明人： Narendra Joshi , Shekhar Bhaskar Bhirud , Batchu Chandrasekhar , K. Eswara Rao , Subhash Damle
IPC分类号： C07F9/02 , C07D239/02
CPC分类号： C07D239/42 , Y02P20/55
摘要： An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
摘要翻译：提供了制备嘧啶衍生物的改进方法，包括使通式为Wittig试剂反应其中R为1至10个碳原子的烷基，芳基或芳基烷基，R 1是被取代或未取代的烃基，R 2和R 3相同或不同，为氢或取代或未取代的烃基; Z可以被甲酰基，乙酰基，丙酰基，丁酰基，异丁酰基，戊酰基，异戊酰基，被磺酰基或烷基磺酰基取代的氨基，和被烷基，氨基或烷基氨基取代的磺酰基取代的硫，氧，磺酰基或亚氨基，X是卤素 ; 与其中R 4为氢的通式的醛，能够形成无毒的药学上可接受的盐的低级烷基或阳离子和每个R 5相同或不同的是氢或可水解保护基团，或每个R 5与每个键合的氧原子一起形成可水解的环保护基团，或每个R 5， SUP>键合到与每个氧原子键合的相同取代基以形成可水解保护基团; 在一个基地的存在。

4. 发明授权

US08552219B2 Process for preparing L-phenyl-3-dimethylaminopropane derivative 失效
标题翻译：制备L-苯基-3-二甲基氨基丙烷衍生物的方法
公开(公告)号：US08552219B2
公开(公告)日：2013-10-08
申请号：US13824210
申请日：2011-09-20
申请人： Shekhar Bhaskar Bhirud , Perminder Singh Johar , Sushanta Mishra , Danish Jamshad
发明人： Shekhar Bhaskar Bhirud , Perminder Singh Johar , Sushanta Mishra , Danish Jamshad
IPC分类号： C07C209/70 , C07C309/73
CPC分类号： C07C213/02 , C07C213/00 , C07C309/73 , C07C215/54
摘要： Provided is a process for the preparing 1-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.
摘要翻译：提供了通过新型中间体制备式I的1-苯基-3-二甲基氨基丙烷衍生物（该式应该在此插入）及其药学上可接受的盐的方法。

5. 发明申请

US20130190522A1 PROCESS FOR PREPARING L-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVE 失效
标题翻译：制备L-苯基-3-二甲氨基酚衍生物的方法
公开(公告)号：US20130190522A1
公开(公告)日：2013-07-25
申请号：US13824210
申请日：2011-09-20
申请人： Shekhar Bhaskar Bhirud , Perminder Singh Johar , Sushanta Mishra , Danish Jamshad
发明人： Shekhar Bhaskar Bhirud , Perminder Singh Johar , Sushanta Mishra , Danish Jamshad
IPC分类号： C07C213/02 , C07C309/73 , C07C213/00
CPC分类号： C07C213/02 , C07C213/00 , C07C309/73 , C07C215/54
摘要： Provided is a process for the preparing 1-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.
摘要翻译：提供了通过新型中间体制备式I的1-苯基-3-二甲基氨基丙烷衍生物（该式应该在此插入）及其药学上可接受的盐的方法。

6. 发明授权

US07459553B2 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：US07459553B2
公开(公告)日：2008-12-02
申请号：US11077723
申请日：2005-03-11
申请人： Bobba Venkata Sivakumar , Shekhar Bhaskar Bhirud , Chandrasekhar Batchu , Sanjay Anantha Kale
发明人： Bobba Venkata Sivakumar , Shekhar Bhaskar Bhirud , Chandrasekhar Batchu , Sanjay Anantha 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：制备以下通式的5H-二苯并[b，f]吖庚因-5-甲酰胺的方法：其中R 1，R 2，R 3和R 4相同或不同，并且可以是氢，卤素，硝基，氰基，羧基， -CO（R），-OCO（R），-O（R），-N（R）2，-CON（R）2和-COO（R） C10烷基，C3-C10环烷基，C2-C10烯基，C5-C10环烯基，C2-C10炔基和C6-C20芳基，其中-N（A）2和-CON（A）2的两个A基团可以是提供相同或不同的，并且其中R2和R3可以一起形成键; 该方法包括将通式为其中R 1，R 2，R 3和R 4具有上述含义的5H-二苯并[b，f]吖庚因与一种或多种碱金属或碱土氰酸酯反应，并在一种或多种不饱和二羧酸存在下酸。

7. 发明授权

US07414143B2 Process for the preparation of 4,4-dimethyl-6-ethynylthiochroman 失效
标题翻译：制备4,4-二甲基-6-乙炔基二氢苯并噻喃的方法
公开(公告)号：US07414143B2
公开(公告)日：2008-08-19
申请号：US11158856
申请日：2005-06-22
申请人： Bobba Venkata Siva Kumar , Vishvas Dattatraya Patil , Changdev Namdev Raut , Shekhar Bhaskar Bhirud , Batchu Chandrasekhar
发明人： Bobba Venkata Siva Kumar , Vishvas Dattatraya Patil , Changdev Namdev Raut , Shekhar Bhaskar Bhirud , Batchu Chandrasekhar
IPC分类号： C07D335/04
CPC分类号： C07D335/06
摘要： An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a β-chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the β-chloro vinyl carbonyl compound intermediate with an alkali metal to provide the 4,4-dimethyl-6-ethynylthiochroman.
摘要翻译：提供了一种用于制备他扎罗汀4,4-二甲基-6-乙炔基二氢苯并噻喃的关键中间体的改进方法，其包括（a）使下式的4,4-二甲基-6-乙酰基二氢苯并二氢吡喃与酰氯和酰氨基其中R是氢或1至15个碳原子的烃基，R 1和R 2可以相同或不同，并且是烃基的通式 1至15个碳原子或R 1和R 2与它们所键合的氮原子一起连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子或R 1和R 2中的一个与其键合的氮原子一起与羰基连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子以形成通式的β-氯乙烯基羰基化合物中间体其中R具有t 他提到意义和（b）使β-氯乙烯基羰基化合物中间体与碱金属反应，得到4,4-二甲基-6-乙炔基二氢苯并噻喃。

8. 发明授权

US09353114B2 Process for the preparation of dipeptidylpeptidase inhibitors 有权
标题翻译：二肽基肽酶抑制剂的制备方法
公开(公告)号：US09353114B2
公开(公告)日：2016-05-31
申请号：US14421896
申请日：2013-08-06
申请人： Sunil Kumar Singh , Sachin Srivastava , Shekhar Bhaskar Bhirud
发明人： Sunil Kumar Singh , Sachin Srivastava , Shekhar Bhaskar Bhirud
IPC分类号： C07D401/04 , C07D473/06 , C07D473/04
CPC分类号： C07D473/18 , C07C69/78 , C07D401/04 , C07D473/04 , C07D473/06
摘要： Provided is a process for the preparation of linagliptin of Formula I, comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyi, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.
摘要翻译：本发明提供制备式I的利格列汀的方法，其包括使式II化合物脱保护，其中R 1和R 2与它们所连接的氮一起形成苯二甲酰亚氨基，其中苯二酰亚氨基的芳环被一个或更多选自卤素，烷基，硝基和氨基的R3取代基; 或R 1为H且R 2选自三烷基甲硅烷基，2-三烷基硅烷基乙氧基氨基甲酸酯，乙酰基，三卤代乙酰基，9-芴基甲氧基羰基，三苯甲基，烷基磺酰基，芳基磺酰基，二苯基膦和磺酰基乙氧基羰基。

9. 发明申请

US20090298884A1 Esomeprazole Strontium Salt, Process For Its Preparation and Pharmaceutical Compositions Containing Same 审中-公开
标题翻译：埃索美拉唑锶盐，其制备方法和含有它的药物组合物
公开(公告)号：US20090298884A1
公开(公告)日：2009-12-03
申请号：US11920024
申请日：2006-05-02
申请人： Shekhar Bhaskar Bhirud , Nitin Sharad Chandra Pradhan , Bobba Venkata Siva Kumar , Pravin Bhalchandra Kulkarni
发明人： Shekhar Bhaskar Bhirud , Nitin Sharad Chandra Pradhan , Bobba Venkata Siva Kumar , Pravin Bhalchandra Kulkarni
IPC分类号： A61K31/4439 , C07D401/02 , A61P1/00
CPC分类号： C07D401/12
摘要： A strontium salt of esomeprazole is provided. A process for preparing a strontium salt of esomeprazole is also provided comprising reacting esomeprazole free base or a sodium, potassium or lithium salt of esomeprazole with a strontium source in one or more solvents.
摘要翻译：提供了艾美拉唑的锶盐。还提供了制备艾美拉唑锶盐的方法，包括使埃索美拉唑游离碱或埃索美拉唑钠盐，钾盐或锂盐与一种或多种溶剂中的锶源反应。

10. 发明申请

US20060084826A1 Process for the preparation of naphthylmethylamine derivatives 审中-公开
标题翻译：萘甲基胺衍生物的制备方法
公开(公告)号：US20060084826A1
公开(公告)日：2006-04-20
申请号：US11215448
申请日：2005-08-30
申请人： Ramasubramanian Sridharan , Shekhar Bhaskar Bhirud , Vandanapu Loka Appala Purushotham , Ravindra Ashok Janrao
发明人： Ramasubramanian Sridharan , Shekhar Bhaskar Bhirud , Vandanapu Loka Appala Purushotham , Ravindra Ashok Janrao
IPC分类号： C07C209/06
CPC分类号： C07C209/08 , C07C211/31
摘要： Disclosed is a process for the preparation of a naphthylmethylamine derivative or a pharmaceutically acceptable salt thereof of Formula I wherein R1 is a lower straight or branched alkyl group and R2 is a lower straight or branched alkyl group, aryl group or araylalkyl group, the process comprising reacting a N-alkyl-1-naphthylmethylamine HCl compound of Formula II: wherein R1 has the aforestated meaning, with a compound of Formula III wherein X is a halogen and R2 has the aforestated meaning in the presence of at least one base and in at least one solvent.
摘要翻译：公开了制备式I的萘基甲基胺衍生物或其药学上可接受的盐的方法，其中R 1是低级直链或支链烷基，R 2是低级直链或支链烷基，芳基或芳烷基，该方法包括使式II的N-烷基-1-萘甲基甲基胺HCl化合物（其中R 1具有上述含义）与式III其中X是卤素，R 2 O在至少一个碱和至少一种溶剂的存在下具有上述含义。

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