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1. 发明专利

IL192983D0 NOVEL 11 BETA-HYDROXYANDROSTA-4-ENE-3-ONES 未知
公开(公告)号：IL192983D0
公开(公告)日：2009-02-11
申请号：IL19298308
申请日：2008-07-22
申请人： SUN PHARMA ADVANCED RES CO , PATEL JITEN RANCHHODBHAI , PATEL GOPALKUMAR CHIMANLAL , SHAH SAMIR RAMESHCHANDRA , MANDHANE SANJAY NANDLAL , CHITTURI TRINADHA RAO , THENNATI RAJAMANNAR , SHETH GAURAV SANJIVKUMAR , SUN PHARMACEUTICAL IND LTD
IPC分类号： C07J20100101
摘要： The invention provides 11&bgr;-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:

2. 发明专利

IL277483D0 Novel glp-1 analogues 未知
公开(公告)号：IL277483D0
公开(公告)日：2020-11-30
申请号：IL27748320
申请日：2020-09-21
申请人： SUN PHARMACEUTICAL IND LTD , THENNATI RAJAMANNAR , CHATURVEDI NISHITH , BURADE VINOD SAMPATRAO , SHAHI PRADEEP DINESH , NATARAJAN MUTHUKUMARAN , NAGARAJA RAVISHANKARA MADAVATI , ZALAWADIA RISHIT MANSUKHLAL , PANDYA KUNAL , PATEL BRIJESHKUMAR , JOSHI DHIREN RAMESHCHANDRA , SONI KRUNAL HARISHBHAI , TIWARI ABHISHEK , PATEL VIPULKUMAR SHANKARBHAI
发明人： THENNATI RAJAMANNAR , CHATURVEDI NISHITH , BURADE VINOD SAMPATRAO , SHAHI PRADEEP DINESH , NATARAJAN MUTHUKUMARAN , NAGARAJA RAVISHANKARA MADAVATI , ZALAWADIA RISHIT MANSUKHLAL , PANDYA KUNAL , PATEL BRIJESHKUMAR , JOSHI DHIREN RAMESHCHANDRA , SONI KRUNAL HARISHBHAI , TIWARI ABHISHEK , PATEL VIPULKUMAR SHANKARBHAI
IPC分类号： A61K9/00 , A61K38/00 , A61P3/04 , A61P3/10 , C07K14/605
摘要： The present disclosure pertains to novel Glucagon like Peptide-1 (GLP-1) (7-37) analogs having an amino acid sequence with Leu or Ile at the C-terminal. The new analogs are potent GLP-1 agonists with reduced adverse effect and improved duration of action. The present disclosure further relates to acylated derivatives of the new analogs which have further improved potency and duration of action and are suitable for oral administration. The analogs of present disclosure may be useful in treatment of diabetes and obesity.

3. 发明专利

IL192983A Derivatives of 17α-acyloxy,11&bgr;-hydroxyandrost-4-ene-3-one 17&bgr;-esters 未知
公开(公告)号：IL192983A
公开(公告)日：2014-06-30
申请号：IL19298308
申请日：2008-07-22
申请人： SUN PHARMA ADVANCED RES CO LTD , PATEL JITEN RANCHHODBHAI , PATEL GOPALKUMAR CHIMANLAL , SHAH SAMIR RAMESHCHANDRA , MANDHANE SANJAY NANDLAL , CHITTURI TRINADHA RAO , THENNATI RAJAMANNAR , SHETH GAURAV SANJIVKUMAR , SUN PHARMACEUTICAL IND LTD
发明人： PATEL JITEN RANCHHODBHAI , PATEL GOPALKUMAR CHIMANLAL , SHAH SAMIR RAMESHCHANDRA , MANDHANE SANJAY NANDLAL , CHITTURI TRINADHA RAO , THENNATI RAJAMANNAR , SHETH GAURAV SANJIVKUMAR
IPC分类号： C07J20060101
摘要： The invention provides 11&bgr;-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:

4. 发明专利

IL293908A A stable parenteral dosage form of cetrorelix acetate 未知
公开(公告)号：IL293908A
公开(公告)日：2022-08-01
申请号：IL29390822
申请日：2022-06-13
申请人： SUN PHARMACEUTICAL IND LTD , JOSHI JAYDIP , THUMMAR RAKESH , AGRAWAL SUDEEP , BHOWMICK SUBHAS BALARAM , YADAV ARUNKUMAR , THENNATI RAJAMANNAR
发明人： JOSHI JAYDIP , THUMMAR RAKESH , AGRAWAL SUDEEP , BHOWMICK SUBHAS BALARAM , YADAV ARUNKUMAR , THENNATI RAJAMANNAR
IPC分类号： A61K38/00 , A61K38/08 , A61K38/09 , A61K47/12 , A61P15/00 , C07K14/59 , G01N30/02 , G01N30/16
摘要： The present invention relates to a stable parenteral dosage form with a ready-to-inject sterile stable aqueous solution of Cetrorelix acetate. The invention also relates to an injection device prefilled with the ready-to-inject sterile stable aqueous solution of Cetrorelix acetate. The present invention relates to a use of a parenteral dosage form comprising a ready-to-inject sterile, stable aqueous solution of Cetrorelix acetate for inhibiting premature luteinizing hormone surges in women undergoing controlled ovarian stimulation.

5. 发明授权

US07790935B2 Process for preparation of citalopram and enantiomers 有权
标题翻译：西酞普兰和对映异构体的制备方法
公开(公告)号：US07790935B2
公开(公告)日：2010-09-07
申请号：US11660742
申请日：2005-08-12
申请人： Periyandi Nagarajan , Kilaru Srinivasu , Thennati Rajamannar
发明人： Periyandi Nagarajan , Kilaru Srinivasu , Thennati Rajamannar
IPC分类号： C07C41/09
CPC分类号： C07C255/59 , C07D307/87
摘要： The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile. The present invention also provides novel ether compound, a compound of formula Va and a process for preparation thereof.
摘要翻译：本发明提供了制备1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的方法，包括使式Ⅳa化合物在具有式RX化合物的碱，其中R选自烷基，烯基，芳基和杂芳基，其可任选被吸电子基团取代，X选自F，Cl，Br，I，CN，OTf和OR1，其中 Tf表示三氟甲磺酰基，R 1是任选取代的烷基，Z是氰基或可以转化成氰基的基团; 进一步地，其中选择RX，使得中间体醚衍生物，由所述反应形成的式Va的化合物与式VI的化合物环化，并且其中Z不是氰基，其中式VI化合物中的基团Z的转化为形成1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的氰基。本发明还提供了新颖的醚化合物，式Va的化合物及其制备方法。

6. 发明授权

US07132444B2 Process for the preparation of trans-3-ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl) amino]carbonyl]amino]sulfonyl] phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide 失效
标题翻译：制备反式-3-乙基-2,5-二氢-4-甲基-N-〔2-〔4 - 〔〔〔〔（4-甲基环己基）氨基〕羰基〕氨基〕磺酰基〕苯基〕乙基 ] -2-氧代-1H-吡咯-1-甲酰胺
公开(公告)号：US07132444B2
公开(公告)日：2006-11-07
申请号：US10501743
申请日：2003-01-06
申请人： Rohit Ravikant Soni , Thennati Rajamannar , Rajeev Budhdev Rehani
发明人： Rohit Ravikant Soni , Thennati Rajamannar , Rajeev Budhdev Rehani
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/38
摘要： The present invention provides a novel process for preparation of trans-3-ethyl 2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide via the novel intermediate compounds of formula 3.
摘要翻译：本发明提供了制备反式-3-乙基2,5-二氢-4-甲基-N- [2- [4 - [[[（4-甲基环己基）氨基]羰基]氨基]磺酰基的新方法。 ]苯基]乙基] -2-氧代-1H-吡咯-1-甲酰胺，通过式3的新型中间体化合物。

7. 发明申请

US20050070593A1 Novel process for the preparation of trans-3-ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl) amino]carbonyl] amino]sulfonyl] phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide 失效
标题翻译：制备反式-3-乙基-2,5-二氢-4-甲基-N- [2- [4 - [[[[（4-甲基环己基）氨基]羰基]氨基]磺酰基]苯基] 乙基] -2-氧代-1H-吡咯-1-甲酰胺
公开(公告)号：US20050070593A1
公开(公告)日：2005-03-31
申请号：US10501743
申请日：2003-01-06
申请人： Rohit Soni , Thennati Rajamannar , Rajeev Rehani
发明人： Rohit Soni , Thennati Rajamannar , Rajeev Rehani
IPC分类号： C07D207/38 , A61K31/4015 , C07D207/28
CPC分类号： C07D207/38
摘要： The present invention provides a novel process for preparation of trans-3-ethyl 2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide via the novel intermediate compounds of formula 3.
摘要翻译：本发明提供了制备反式-3-乙基2,5-二氢-4-甲基-N- [2- [4 - [[[（4-甲基环己基）氨基]羰基]氨基]磺酰基的新方法。 ]苯基]乙基] -2-氧代-1H-吡咯-1-甲酰胺，通过式3的新型中间体化合物。

8. 发明申请

US20050043550A1 Process for the preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile 失效
标题翻译：制备1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的方法
公开(公告)号：US20050043550A1
公开(公告)日：2005-02-24
申请号：US10500532
申请日：2003-01-07
申请人： Thennati Rajamannar , Kilaru Srinivasu , Nileshkumar Patel , Chinnapillai Rajendran
发明人： Thennati Rajamannar , Kilaru Srinivasu , Nileshkumar Patel , Chinnapillai Rajendran
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： The present invention provides an improved cyanide exchange process for preparation of 1-[3-(dimethy-lamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile, followed by the treatment of crude 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile with a cyanide reversal agent and its purification from a solvent system.
摘要翻译：本发明提供了用于制备1- [3-（二甲基 - 氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的改进的氰化物交换方法，然后处理粗品具有氰化物反转剂的1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈并从溶剂系统中纯化。

9. 发明授权

US07989645B2 Process for preparation of citalopram and enantiomers 失效
标题翻译：西酞普兰和对映异构体的制备方法
公开(公告)号：US07989645B2
公开(公告)日：2011-08-02
申请号：US12024492
申请日：2008-02-01
申请人： Periyandi Nagarajan , Kilaru Srinivasu , Thennati Rajamannar
发明人： Periyandi Nagarajan , Kilaru Srinivasu , Thennati Rajamannar
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran car-bonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile. The present invention also provides novel ether compound, a compound of formula Va and a process for preparation thereof.
摘要翻译：本发明提供了制备1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃羧腈的方法，包括使式Ⅳa化合物在存在碱与式RX化合物反应，其中R选自烷基，烯基，芳基和杂芳基，其可任选被吸电子基团取代，X选自F，Cl，Br，I，CN，OTf和OR1 其中Tf表示三氟甲磺酰基，R 1为任选取代的烷基，Z为氰基或可转化为氰基的基团; 进一步地，其中选择RX，使得中间体醚衍生物，由所述反应形成的式Va的化合物与式VI的化合物环化，并且其中Z不是氰基，其中式VI化合物中的基团Z的转化为形成1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的氰基。本发明还提供了新颖的醚化合物，式Va的化合物及其制备方法。

10. 发明授权

US07964742B2 Process for preparation of citalopram and enantiomers 失效
标题翻译：西酞普兰和对映异构体的制备方法
公开(公告)号：US07964742B2
公开(公告)日：2011-06-21
申请号：US12813256
申请日：2010-06-10
申请人： Periyandi Nagarajan , Kilaru Srinivasu , Thennati Rajamannar
发明人： Periyandi Nagarajan , Kilaru Srinivasu , Thennati Rajamannar
IPC分类号： C07D307/84
CPC分类号： C07C255/59 , C07D307/87
摘要： The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile. The present invention also provides novel ether compound, a compound of formula Va and a process for preparation thereof.
摘要翻译：本发明提供了制备1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的方法，包括使式Ⅳa化合物在具有式RX化合物的碱，其中R选自烷基，烯基，芳基和杂芳基，其可任选被吸电子基团取代，X选自F，Cl，Br，I，CN，OTf和OR1，其中 Tf表示三氟甲磺酰基，R 1是任选取代的烷基，Z是氰基或可以转化成氰基的基团; 进一步地，其中选择RX，使得中间体醚衍生物，由所述反应形成的式Va的化合物与式VI的化合物环化，并且其中Z不是氰基，其中式VI化合物中的基团Z的转化为形成1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的氰基。本发明还提供了新颖的醚化合物，式Va的化合物及其制备方法。

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