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1. 发明授权

EP2990399B1 IMPROVED PROCESS FOR THE PREPARATION OF LACOSAMIDE 有权
标题翻译： VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON LACOSAMID
公开(公告)号：EP2990399B1
公开(公告)日：2017-03-15
申请号：EP15160898.1
申请日：2015-03-25
申请人： Rao, Davuluri Ramamohan
发明人： Ravi, Ponnaiah , Rajput, Vishal , Dhanunjaya, Mailapalli , Anilkumar, Bondada
IPC分类号： C07C231/02 , C07C231/12 , C07C235/06 , C07C247/12 , C07C51/27 , C07C237/22
CPC分类号： C07C231/08 , C07C51/27 , C07C51/29 , C07C231/02 , C07C231/12 , C07C235/06 , C07C247/12 , C07C59/115 , C07C237/06 , C07C237/22

2. 发明公开

EP2315802A4 AZIDE COMPOSITIONS AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译：维多利亚ZIDI
公开(公告)号：EP2315802A4
公开(公告)日：2012-04-18
申请号：EP09803298
申请日：2009-04-20
申请人： 3M INNOVATIVE PROPERTIES CO
发明人： JOHANNESSEN BIRGER , MANZARA ANTHONY P , GOODNER ARON Y
IPC分类号： C08K5/28 , C07C247/04 , C07C247/12
CPC分类号： C07C247/04 , C07C271/12 , C08K5/28 , C08K2201/014
摘要： Azide compositions selected from i) UOCR2CR2N3 wherein U is D, or a urethane (—CO—NR2) and R is independently H, D, or an organic group; ii) R′2NCR2CR2N3 or A-R′3NCR2CR2N3 wherein R′ is an organic group and A is an anion; or iii) G(N3)m wherein m is an integer from 2 to about 10 and G is a m-valent organic group wherein at least two of the azido groups are connected via aliphatic carbon atoms wherein G may contain organic groups, and uses thereof are described. Specifically, the azide compositions selected from the group consisting of: N3CH2CH2OCH2CHOHCH2N3, CH3OCH2CHOHCH2N3, CH3OCH2CH(OCONHC4H9)CH2N3, N3CH2CH2O[CH2CH(CH2N3)O]6H, CH3CH2C[CH2(OCH2CH(CH2N3))2OCOCH3]3N3CH2CH2OCONH(CH2)6NHCOOCH2CH2N3, (CH3)3CNHCOOCH2CH2N3, n-C4H9NDCOOCH2CH2N3, C6H5N—HCOOCH2CH2N3, C4F9OCFCF3NDCOOCH2CH2N3, DOCH2CH2N3, and [(CH3)3NCH2CH2N3]+I are described.
摘要翻译：选自i）UOCR2CR2N3，其中U是D的叠氮化物组合物或氨基甲酸酯（-CO-NR 2），R独立地是H，D或有机基团; ii）R'2NCR2CR2N3或A-R'3NCR2CR2N3，其中R'是有机基团，A是阴离子; 或iii）G（N 3）m，其中m为2至约10的整数，G为m价有机基团，其中至少两个叠氮基通过脂族碳原子连接，其中G可以含有有机基团，并且使用描述。具体地，选自N 3 CH 2 CH 2 OCH 2 CHOHCH 2 N 3，CH 3 OCH 2 CHOHCH 2 N 3，CH 3 OCH 2 CH（OCONHC 4 H 9）CH 2 N 3，N 3 CH 2 CH 2 O [CH 2 CH（CH 2 N 3）O] 6H，CH 3 CH 2 C [CH 2（OCH 2 CH（CH 2 N 3））2 OCO 3] 3 N 3 CH 2 CH 2 OCONH（CH 2）6 NHCOOCH 2 CH 2 N 3， CH3）3CNHCOOCH2CH2N3，n-C4H9NDCOOCH2CH2N3，C6H5N-HCOOCH2CH2N3，C4F9OCFCF3NDCOOCH2CH2N3，DOCH2CH2N3和[（CH3）3NCH2CH2N3] + I。

3. 发明公开

EP2289887A3 Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them 审中-公开
标题翻译：环氧羧酸酰胺，叠氮化物和氨基醇以及通过使用它们制备α-酮酰胺的方法
公开(公告)号：EP2289887A3
公开(公告)日：2011-07-06
申请号：EP10011260.6
申请日：2001-06-29
申请人： SEIKAGAKU CORPORATION
发明人： Kobayashi, Nubuo , Koji, Tsuneo , Fujita, Takashi , Nishimura, Tomofumi , Hosoda, Akihiko
IPC分类号： C07D303/48 , C07D295/20 , C07D317/66 , C07D207/16 , C07C247/12 , C07C237/22 , C07C271/22 , C07C231/12 , C07C231/16
CPC分类号： C07D295/215 , C07C231/12 , C07C231/16 , C07C237/22 , C07C247/12 , C07C271/22 , C07C2601/14 , C07D207/16 , C07D295/18 , C07D303/46 , C07D303/48 , C07D317/66 , C07D405/12 , C07D407/12 , C07D413/12
摘要： The present invention is to provide manufacturing intermediates which can be led to useful α-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide azide compounds represented by the following formula:

wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; and processes for preparing α-keto amide compound using the same.
摘要翻译：本发明的目的在于提供能够非常经济且立体地选择性地得到具有蛋白酶抑制活性的有用的α-酮酰胺化合物的制造中间体，并且提供下式所示的叠氮化合物：其中R1和R2各自表示烷基，烯基，芳族烃基或杂环基团; 以及使用其制备α-酮酰胺化合物的方法。

4. 发明公开

EP2315802A1 AZIDE COMPOSITIONS AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译： AZIDZUSAMMENSETZUNGEN和方法的生产和使用
公开(公告)号：EP2315802A1
公开(公告)日：2011-05-04
申请号：EP09803298.0
申请日：2009-04-20
申请人： 3M Innovative Properties Company
发明人： MANZARA, Anthony, P. , GOODNER, Aron, Y. , JOHANNESSEN, Judith, A.
IPC分类号： C08K5/28 , C07C247/12 , C07C247/04
CPC分类号： C07C247/04 , C07C271/12 , C08K5/28 , C08K2201/014
摘要： Azide compositions selected from i) UOCR
2 CR
2 N
3 wherein U is D, or a urethane (-CO-NR
2 ) and R is independently H, D, or an organic group; ii) R'
2 NCR
2 CR
2 N3 or A-R'
3 N CR
2 CR
2 N
3 wherein R' is an organic group and A is an anion; or iii) G(N
3) m wherein m is an integer from 2 to about 10 and G is a m-valent organic group wherein at least two of the azido groups are connected via aliphatic carbon atoms wherein G may contain organic groups, and uses thereof are described. Specifically, the azide compositions selected from the group consisting of: N
3 CH
2 CH
2 OCH
2 CHOHCH
2 N
3 , CH
3 OCH
2 CHOHCH
2 N
3 , CH
3 OCH
2 CH(OCONHC
4 H
9 )CH
2 N
3 , N
3 CH
2 CH
2 O[CH
2 CH(CH
2 N
3 )O]
6 H, CH
3 CH
2 C[CH
2 (OCH
2 CH(CH
2 N
3 ))
2 OCOCH
3 ]3 N
3 CH
2 CH
2 OCONH(CH
2 )
6 NHCOOCH
2 CH
2 N
3 , (CH
3 )
3 CNHCOOCH
2 CH
2 N
3 , n-C
4 H
9 NDCOOCH
2 CH
2 N
3 , C
6 H
5 NHCOOCH
2 CH
2 N
3 , C
4 F
9 OCFCF
3 NDCOOCH
2 CH
2 N
3 , DOCH
2 CH
2 N
3 , and [(CH
3 )
3 NCH
2 CH
2 N
3 ]
+ I are described.

5. 发明授权

EP1296935B1 PROCESS FOR THE PREPARATION OF SUBSTITUTED OCTANOYL AMIDES 有权
标题翻译：用于生产取代的酰胺辛
公开(公告)号：EP1296935B1
公开(公告)日：2009-03-25
申请号：EP01940047.2
申请日：2001-06-26
申请人： Speedel Pharma AG
发明人： HEROLD, Peter , STUTZ, Stefan , SPINDLER, Felix
IPC分类号： C07C231/02 , C07C247/12 , C07D207/32 , C07D303/40
CPC分类号： C07D207/33 , C07C57/42 , C07C59/64 , C07C69/734 , C07C231/02 , C07C247/12 , C07D303/38 , C07D307/33 , C07C237/20
摘要： Compounds of formula (II) are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted into a hydroxylactone and then the hydroxy group into a leaving group, the leaving group is replaced with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I).

6. 发明公开

EP1357110A1 Synthesis for the preparation of porphobilinogen, the compound as such as stabilized salt and intermediates thereof 审中-公开
标题翻译：一种制备胆色素原的，该化合物本身为稳定的盐和它们的中间体的方法
公开(公告)号：EP1357110A1
公开(公告)日：2003-10-29
申请号：EP02009121.1
申请日：2002-04-24
申请人： Neier, Reinhard
发明人： Neier, Reinhard , Soldermann-Pissot, Carole
IPC分类号： C07D207/32 , C12P17/10 , C07F7/18 , C07C247/12
CPC分类号： C07D207/337 , C07F7/1852 , C07F7/188 , C12P17/10 , Y02P20/55
摘要： The invention relates to a new inventive process sequence of steps a) to e) as claimed in Claim 1 for the preparation of porphobilinogen and intermediates per se as important precursors such as 3-[4-methoxycarbonylmethyl-5-(protected amino-methyl)-1 H-pyrrol-3-yl]-propionic acid methyl ester of formula 7
wherein R is a protective group,
and 3-[4-Carboxymethyl-5-(protected amino-methyl)-1 H-pyrrol-3-yl]-propionic acid di-alkali metal salt of formula 8
and especially 3-[4-carboxymethyl-5-(phenylacetyl-amino-methyl)- 1H-pyrrol-3-yl]-propionic acid di-lithium salt of formula 8a
and of carboxylate 4-(2-carboxy-ethyl)-3-carboxymethyl-1H-pyrrrol-2-yl-methyl-ammonium of formula 9
and of phenylacetate 4-(2-carboxy-ethyl)-3carboxymethyl-1 H-pyrrol-2-ylmethyl-ammonium of formula 9a
and the use thereof for the preparation of porphobilinogen.
摘要翻译：本发明涉及到的步骤a）至e）的新发明的工艺顺序，如权利要求1要求保护的用于胆色素原和中间体本身的制备作为重要的前体：例如3- AE4甲氧羰基甲基-5-（保护的氨基 - 甲基） - 式7 worin的R 1个H-吡咯-3-ylÜ - 丙酸甲酯为保护基，和3- AE4羧甲基-5-（保护的氨基 - 甲基）-1H-吡咯-3-ylÜ - 丙酸二碱式的金属盐8 和爱尤其是3- AE4羧甲基-5-（苯基乙酰基氨基 - 甲基） - 式8a的1H-吡咯-3-丙酸ylÜ二锂盐< CHEM>和的羧酸酯4-（2-羧基 - 乙基）式9 和苯乙酸4- -3羧甲基-1H-pyrrrol -2-基甲基 - 铵（2-羧基 - 乙基）-3carboxymethyl -1H-吡咯-2-基甲基 - 铵式9a中及其用于胆色素原的制备中的用途的。

7. 发明公开

EP0867431A1 Process for the preparation of azide derivatives 失效
标题翻译： Verfahren zur Herstellung von Azid-Derivaten
公开(公告)号：EP0867431A1
公开(公告)日：1998-09-30
申请号：EP98104327.6
申请日：1998-03-11
申请人： Eisai Chemical Co., Ltd.
发明人： Mizuno, Masanori , Shioiri, Takayuki
IPC分类号： C07C247/04 , C07C247/12 , C07C247/08 , C07C247/14 , C07C247/10 , C07D277/28 , C07H5/04
CPC分类号： C07C247/10 , C07C247/04 , C07C247/08 , C07C247/12 , C07C247/14 , C07D277/28 , C07H5/04
摘要： To provide a novel and industrially advantageous process for the preparation of azide derivatives useful as drugs, perfumes or intermediates of dyes.
A process for the preparation of aside derivatives by reacting an alcohol derivative with di-p-nitrophenyl phosphorazidate in the presence of 1,8-diazabicyclo[5.4.0]-7-undecene.
摘要翻译：提供用于制备用作染料的药物，香料或中间体的叠氮衍生物的新颖和工业上有利的方法。一种通过醇衍生物与二对硝基苯基氨基磷酸酯在1,8-二氮杂双环[5.4.0-7-十一碳烯]存在下反应制备衍生物的方法。

8. 发明公开

EP0480901A1 Azido-substituted fatty acid analog enzyme substrates 失效
标题翻译： Azido-substitutionierteFettsäurenals Enzymsubstratanaloge。
公开(公告)号：EP0480901A1
公开(公告)日：1992-04-15
申请号：EP91870159.0
申请日：1991-10-09
申请人： WASHINGTON UNIVERSITY
发明人： Adams, Steven Paul , Devadas, Balekudru , Gordon, Jeffrey Ivan
IPC分类号： C07C247/04 , C07C247/12 , C07C323/52 , C07D249/04 , C07D257/04 , C07D249/08 , C12P21/00 , C07K1/00 , A61K31/41 , A61K31/19 , A61K31/20
CPC分类号： C07D257/04 , C07C247/12 , C07C323/52 , C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08 , C07K1/1077 , C12N9/1029
摘要： Azido-substituted fatty acid analogs which are useful in the fatty acid acylation of peptides and proteins and as antiviral agents are disclosed having the following chemical structure:

Z - (CH₂)xCOOR

wherein
Z = azido, tetrazolyl or triazolyl
R = H or C₁-C₈ alkyl, and
x = 8-12
or structure (I) as defined above and wherein a methylene group from carbon position 3 to within 2 carbons of Z is replaced with oxygen or sulfur.
摘要翻译：公开了可用于肽和蛋白质和抗病毒剂的脂肪酸酰化的叠氮取代的脂肪酸类似物，其具有以下化学结构：Z-（CH 2）x COOR其中Z =叠氮基，四唑基或三唑基R = H或C1- C8烷基和x = 8-12或如上定义的结构（I），并且其中Z的碳位置3至2碳原子的亚甲基被氧或硫替代。

9. 发明公开

EP2990399A1 Improved process for the preparation of lacosamide and its novel intermediate 有权
标题翻译：改进方法，拉科胺PRODUCING
公开(公告)号：EP2990399A1
公开(公告)日：2016-03-02
申请号：EP15160898.1
申请日：2015-03-25
申请人： Rao, Davuluri Ramamohan
发明人： Ravi, Ponnaiah , Rajput, Vishal , Dhanunjaya, Mailapalli , Anilkumar, Bondada
IPC分类号： C07C231/02 , C07C231/12 , C07C235/06 , C07C247/12 , C07C51/27 , C07C237/22
CPC分类号： C07C231/08 , C07C51/27 , C07C51/29 , C07C231/02 , C07C231/12 , C07C235/06 , C07C247/12 , C07C59/115 , C07C237/06 , C07C237/22
摘要： An improved, cost effective process for the preparation of Lacosanide is disclosed. A novel intermediate of formula (IV) and a process for preparation of the novel intermediate is also disclosed.

wherein, X is halogen.

10. 发明授权

EP2630118B1 SYNTHESIS OF ALISKIREN 有权
标题翻译：阿利吉仑的合成
公开(公告)号：EP2630118B1
公开(公告)日：2014-11-05
申请号：EP11811559.1
申请日：2011-10-19
申请人： MYLAN LABORATORIES LIMITED
发明人： RAMA, Shankar , VADALI, Lakshmana Rao , PALLA, Vijay Kumar , SAIDUGARI, Swamy , MITTAPELLY, Nagaraju , JALDU, Ravikanth , VIJAYA, Krishna Ravi , SESHADRI, Rao Manukonda , DASARL, Srinivasa Rao , SRINIVASA, Rao Potla , DANDALA, Ramesh
IPC分类号： C07C247/12 , C07C209/42 , C07C233/48 , C07C253/30 , C07C255/29
CPC分类号： C07C231/14 , C07C43/215 , C07C231/12 , C07C241/00 , C07C247/10 , C07C255/29 , C07D307/33 , C07C237/22

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