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1. 发明申请

WO2011141923A3 IMPROVED SYNTHESIS OF OPTICALLY PURE (S) - 3-CYANO-5-METHYL-HEXANOIC ACID ALKYL ESTER, AN INTERMEDIATE OF (S)- PREGABALIN 审中-公开
标题翻译：改进的光学纯（S）-3-氰基-5-甲基 - 十六烷酸酸式酯，中间体（S） - 孕酮
公开(公告)号：WO2011141923A3
公开(公告)日：2012-01-19
申请号：PCT/IN2010000440
申请日：2010-06-28
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , PISE VIJAY SADASHIV
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , PISE VIJAY SADASHIV
IPC分类号： C07C253/30 , C07C51/363 , C07C67/08 , C07C67/343 , C07C231/02 , C07C253/20
CPC分类号： C07C51/363 , C07B2200/07 , C07C67/08 , C07C67/303 , C07C67/343 , C07C253/20 , C07C253/30 , C07C253/34 , C07C255/22 , C07C53/19 , C07C69/40 , C07C69/593 , C07C69/34 , C07C255/19
摘要： The present invention is directed towards synthesis of (S) - 3-cyano-5-methyl-hexanoic acid ethyl ester. A cost effective, eco-friendly process for preparation of enantiomerically pure (S)-3-cyano-5-methyl-hexanoic acid alkyl ester, intermediate of ?-amino acids, particularly (S)-pregabalin.
摘要翻译：本发明涉及（S）-3-氰基-5-甲基 - 己酸乙酯的合成。用于制备对映异构体纯（S）-3-氰基-5-甲基 - 己酸烷基酯的成本有效，环保的方法，α-氨基酸，特别是（S） - 普瑞巴林的中间体。

2. 发明申请

WO2012059798A3 NOVEL METHOD FOR RACEMIZATION OF OPTICALLY PURE ß-CYANO ESTER TO CORRESPONDING RACEMIC ß-CYANO ACID 审中-公开
标题翻译：光学纯β-氰基酯相应的反应性β-氰基酸的新方法
公开(公告)号：WO2012059798A3
公开(公告)日：2012-07-19
申请号：PCT/IB2011000485
申请日：2011-03-07
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , MITRA RANGAN , RUPNAWAR MANOJ DATTATRAYA
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , MITRA RANGAN , RUPNAWAR MANOJ DATTATRAYA
IPC分类号： C07C253/30 , C07C255/18
CPC分类号： C07C253/30 , C07C255/19
摘要： A novel process for racemization of (R)-3-cyano-5 -methyl hexanoic acid ethyl ester directly to (RS)-3-cyano-5 -methyl hexanoic acid has been developed through a base catalyzed mechanism in a specific solvent system.
摘要翻译：（R）-3-氰基-5-甲基己酸乙酯直接向（RS）-3-氰基-5-甲基己酸外消旋的新方法已经通过在特定溶剂体系中的碱催化机理开发出来。

3. 发明申请

WO2012007814A3 THREE COMPONENT CO-CRYSTAL FORMATION BETWEEN DIASTEREOMERIC MIXTURES OF 3-ALKYL-4-((S)-1'PHENYLETHYLAMINO) BUTANOIC ACID AND OPTICALLY PURE 1, 1'-BI-2-NAPHTHOL 审中-公开
标题翻译： 3-ALKYL-4 - （（S）-1'-苯基氨基甲酸）二油酸和光学纯度1'-BI-2-NAPHTHOL的二元醇混合物之间的三种组分共晶形成
公开(公告)号：WO2012007814A3
公开(公告)日：2012-03-08
申请号：PCT/IB2011001605
申请日：2011-07-11
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
IPC分类号： C07C37/84 , C07C39/14 , C07C229/14
CPC分类号： C07C229/14 , C07B2200/07 , C07B2200/13 , C07C37/84 , C07C39/14
摘要： A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3(S)-propyl-4-[(S)1 '-phenyl-ethylamino]-butanoic acid and 3(R)-propyl-4-[(S)1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2T values of 8.41, 9.38, 10.32, 12.16, 15.52, 15.51, 17.84, 17.95, 19.16, 20.37, 21.74, 22.55, 24.44, 25.65, 28.40, 29.15, 29.69, 31.31, 33.54, 34.40, 35.43 (±0.2) and having differential scanning calorimetric peak at about 189.23 ° C when analyzed at the rate of heating of 10°C per minute and process for preparing the same. A process for resolution of (S)-1,1'-bi-2-naphthol from RS-1,1'-bi-2-naphthol.
摘要翻译：由（S）-1,1'-双-2-萘酚，3（S） - 丙基-4 - [（S）-1'-苯基 - 乙基氨基] - 丁酸和具有特征性粉末X射线衍射图的3（R） - 丙基-4 - [（S）1'-苯基 - 乙基氨基] - 丁酸，其中2T值为8.41,9.38,10.32,12.16,15.52,15.51 ，17.84,17.95,19.16,20.37,21.74,22.55,24.44,25.65,2840,29.15,29.69,31.31,33.54,34.40,35.43（±0.2），并且当以速率分析时在约189.23℃下具有差示扫描量热峰每分钟加热10℃，其制备方法。从RS-1,1'-双-2-萘酚中分离出（S）-1,1'-双-2-萘酚的方法。

4. 发明申请

WO2011141805A3 PROCESS FOR THE MANUFACTURE OF LAMIVUDINE 审中-公开
标题翻译：制造拉米夫定的方法
公开(公告)号：WO2011141805A3
公开(公告)日：2012-03-22
申请号：PCT/IB2011001013
申请日：2011-05-12
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , JADHAV HARISHCHANDRA SAMBHAJI , AHER UMESH PARASHRAM , DEOKAR SHARAD CHANDRABHAN
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , JADHAV HARISHCHANDRA SAMBHAJI , AHER UMESH PARASHRAM , DEOKAR SHARAD CHANDRABHAN
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： The present invention relates to an improved process for the Manufacture of Lamivudine. A process for the preparation of essentially enantiomerically pure (-)-[2R, 5S]-4-amino-1-[2- (hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (I), from L-menthyl glyoxylate is described. Also provided is a process for preparation of (+)-1- (2R/S-Cis)-4-amino-1-[(2-hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (XII), from L-menthyl glyoxylate.
摘要翻译：本发明涉及拉米夫定的制造方法。制备基本上对映体纯的（ - ） - [2R，5S] -4-氨基-1- [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H） - 嘧啶-2-基 - 描述了式（I）的2-酮，乙醛酸L-薄荷酯。还提供了制备（+） - 1-（2R / S-顺式）-4-氨基-1 - [（2-羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H）（XII）的嘧啶-2-酮，由乙醛酸L-薄荷酯。

5. 发明专利

AU2015294840A1 A process for the preparation of nucleoside phosphoramidate 未知
公开(公告)号：AU2015294840A1
公开(公告)日：2017-02-23
申请号：AU2015294840
申请日：2015-07-31
申请人： LUPIN LTD
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , MEHARE KISHOR GULABRAO , MALIK VINEET , DEOKAR SHARAD CHANDRABHAN , DANGE ABHIJEET AVINASH
IPC分类号： C07F9/24 , A61K31/7072 , A61K31/716 , C07F9/58 , C07F9/6506 , C07F9/6518 , C07F9/6521 , C07F9/653 , C07F9/6558 , C07H19/10
摘要： The present invention pertains to process for preparing nucleoside phosphoramidate and its intermediate. The present invention provides novel intermediate, its process for preparation and its use for the preparation of Sofosbuvir.

6. 发明专利

IN2956MU2013A A NOVEL PROCESS FOR SYNTHESIS OF DEFERASIROX 未知
公开(公告)号：IN2956MU2013A
公开(公告)日：2015-07-03
申请号：IN2956MU2013
申请日：2013-09-12
申请人： LUPIN LTD
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJBIHARI
IPC分类号： C07D249/08
摘要： The invention relates to metal mediated synthesis of Deferasirox 4-[3,5-bis(2-hydroxyphenyl)-lH-l,2,4-traizol-lyl] benzoic acid, [I], an iron chelating agent, synthesized from 1, 2, 4-triazole. The process involves Preparation of 3,5-dibromo-lH-l,2,4-traizole (II) from 1,2,4 triazole; reaction of compound (II) with benzyl bromide to form l-benzyl-3,5-dibromo-lH-l,2,4-traizoIe (III); reaction of compound (III) and (2-methoxyphenyl)boronic acid to give l-benzyl-3,5-bis[2-methoxyphenyl)-lH-l,2,4-traizole (IV); compound (IV) being reacted with suitable reactants to give compound (V); reacting compound (V) with (4-(methoxycarbonyl)phenyl)boronic acid to give compound (VI); and deprotection of compound (VI) to give compound [I]. A further process involves preparation of 3,5-dibromo lH-l,2,4triazole (II) from 1,2,4-traizoIe; reacting 3,5-dibromo lH-l,2,4triazole (II) and (4-(methoxycarbonyl)phenyI)boronic acid to form methyl 4-(3,5-dibromo-lH-l,2,4-triazol-l-yI)benzoate (VII) ; reaction of methyl 4-(3,5-dibromo-lH-l,2,4-triazol-l-yl)benzoate (VII) and (2-methoxyphenyl)boronic acid to form Synthesis of 4-(3,5-bis(2-methoxyphenyI)-lH-l,2,4-triazol-l-yl)benzoate (VI); deprotection of methyl 4-(3,5-bis(2-methoxyphenyl)-lH-l,2,4-triazol-l-yl)benzoate (VI) to form deferasirox (I). The invention also includes intermediates formed in the process of preparation of Deferasirox.

7. 发明专利

GB2486113A An improved process for the synthesis of alkyl/aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof 未知
公开(公告)号：GB2486113A
公开(公告)日：2012-06-06
申请号：GB201204081
申请日：2010-04-28
申请人： LUPIN LTD
发明人： ROY BHAIRAB NATH , KAMBOJ RAJENDER KUMAR , GEORGE SHAJI K , VENUGOPAL SPINVIN C , SHANMUGVADIVELU MUTHU KUMARAN , SINHA NEELIMA
IPC分类号： C07D451/02
摘要： An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DPPIV) inhibitors.

8. 发明专利

AU2002347586A1 MONOCLONAL ANTIBODY DERIVED PEPTIDE INHIBITORS FOR MYCOBACTERIAL DNA GYRASE 未知
公开(公告)号：AU2002347586A1
公开(公告)日：2004-04-08
申请号：AU2002347586
申请日：2002-09-20
申请人： LUPIN LTD
发明人： MANJUNATHA UJJINI HAVALDAR , ROY BHAIRAB NATH , NAGARAJA VALAKUNJA
IPC分类号： C07K16/12 , C07K16/40 , C07K7/08
摘要： The present invention relates to the development of monoclonal antibodies that specifically inhibit DNA gyrase from M. tuberculosis. M. smegmaris and possibly from other related bacterial species. More particularly, it has been shown that the inhibition of the enzyme is by a hitherto unknown and novel mechanism. The present invention also relates to a DNA sequence of single chain antibody consisting of complementarity determining regions of mAb. The monoclonal antibody, single chain antibody and peptides derived thereof could be useful for developing lead molecules for tuberculosis therapy. The antibodies and derived materials could be useful for a variety of purposes, including diagnosis of mycobacterial infections. The present invention also relates to the modification of antibodies and derived materials for use against diverse microbial infections and other potential applications derived thereof.

9. 发明专利

IN1097MU2014A A NOVEL PROCESS FOR THE PREPARATION OF PROSTAGLANDIN INTERMEDIATE 未知
公开(公告)号：IN1097MU2014A
公开(公告)日：2015-10-02
申请号：IN1097MU2014
申请日：2014-03-27
申请人： LUPIN LTD
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
IPC分类号： C07C405/00 , C07F7/18
摘要： The present invention relates to a novel, “green”, cost effective industrial process for the preparation of prostaglandin intermediate [D] wherein P is protecting group and R is residual side chain, using reverse micellar solution as well as water in oil micro emulsion.

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