专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20080009634A1 Process for synthesizing beta-lactamase inhibitor intermediates 审中-公开
标题翻译： β-内酰胺酶抑制剂中间体的合成方法
公开(公告)号：US20080009634A1
公开(公告)日：2008-01-10
申请号：US11820575
申请日：2007-06-18
申请人： Michael Winkley , Anita Chan , Ivo Jirkovsky , Kenneth Kremer , Joseph Zeldis , Antonia Nikitenko , Henry Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam Venkatesan
发明人： Michael Winkley , Anita Chan , Ivo Jirkovsky , Kenneth Kremer , Joseph Zeldis , Antonia Nikitenko , Henry Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam Venkatesan
IPC分类号： C07D277/60 , C07D487/04
CPC分类号： C07D498/04 , C07D487/04
摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
摘要翻译：提供了一种制备具有结构式I的双环杂芳基羧醛的方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

2. 发明授权

US07361773B2 Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines 失效
标题翻译： N1-（2'-吡啶基）-1,2-丙二胺氨基磺酸的制备及其在生物活性哌嗪合成中的应用
公开(公告)号：US07361773B2
公开(公告)日：2008-04-22
申请号：US10919099
申请日：2004-08-16
申请人： Anita Wai-Yin Chan , Gregg Brian Feigelson , Joseph Zeldis , Ivo Ladislav Jirkovsky
发明人： Anita Wai-Yin Chan , Gregg Brian Feigelson , Joseph Zeldis , Ivo Ladislav Jirkovsky
IPC分类号： C07D319/14
CPC分类号： C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12
摘要： A process for making a compound of the formula comprising dialkylating a benzodioxane aniline
摘要翻译：一种制备式的化合物的方法，包括使苯并二恶烷苯胺二烷基化

3. 发明授权

US07256289B2 Process for making chiral 1,4-disubstituted piperazines 失效
标题翻译：制备手性1,4-二取代哌嗪的方法
公开(公告)号：US07256289B2
公开(公告)日：2007-08-14
申请号：US11147055
申请日：2005-06-07
申请人： Ivo Ladislav Jirkovsky , Joseph Zeldis , Gregg Brian Feigelson
发明人： Ivo Ladislav Jirkovsky , Joseph Zeldis , Gregg Brian Feigelson
IPC分类号： C07D405/04
CPC分类号： C07D487/10 , C07B2200/07 , C07C229/12 , C07C309/06 , C07D319/18
摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders. The intermediate compounds of Formula II and IV as set forth herein are also included.
摘要翻译：用于立体选择性制备新型手性氮芥衍生物的方法，其用于合成下式所示的光学活性1,4-二取代哌嗪：其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。还包括本文所述的式II和IV的中间体化合物。

4. 发明申请

US20050228181A1 Process for making chiral 1,4-disubstituted piperazines 失效
标题翻译：制备手性1,4-二取代哌嗪的方法
公开(公告)号：US20050228181A1
公开(公告)日：2005-10-13
申请号：US11147055
申请日：2005-06-07
申请人： Joseph Zeldis , Gregg Feigelson , Ivo Jirkovsky
发明人： Joseph Zeldis , Gregg Feigelson , Ivo Jirkovsky
IPC分类号： C07D295/08 , C07B53/00 , C07C229/12 , C07D213/75 , C07D295/10 , C07D319/18 , C07D401/00 , C07D405/12 , C07D487/10 , A61K31/496 , C07C229/06 , C07D45/02
CPC分类号： C07D487/10 , C07B2200/07 , C07C229/12 , C07C309/06 , C07D319/18
摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.
摘要翻译：用于立体选择性制备新型手性氮芥衍生物的方法，其用于合成下式所示的光学活性1,4-二取代哌嗪：其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。

5. 发明授权

US06784294B2 Preparation of N1-(2′-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines 失效
标题翻译： N1-（2'-吡啶基）-1,2-丙二胺氨基磺酸的制备及其在生物活性哌嗪合成中的应用
公开(公告)号：US06784294B2
公开(公告)日：2004-08-31
申请号：US10385337
申请日：2003-03-10
申请人： Anita Wai-Yin Chan , Gregg Brian Feigelson , Joseph Zeldis , Ivo Jirkovsky
发明人： Anita Wai-Yin Chan , Gregg Brian Feigelson , Joseph Zeldis , Ivo Jirkovsky
IPC分类号： C07D401100
CPC分类号： C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12
摘要： A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R′ wherein R and R′ are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.
摘要翻译：通过使式I化合物与R 2和R'中的NH 2 R'反应制备式II的N1-（2'-吡啶基）-1,2-链烷二胺氨基磺酸的方法如说明书中所定义。本发明还包括式II化合物及其旋光异构体。式II化合物是可用于制备在5-HT 1A受体上有活性的手性哌嗪衍生物的中间体。

6. 发明授权

US06242605B1 Aryloxy-alkyl-dialkylamines 失效
标题翻译：芳氧基 - 烷基 - 二烷基胺
公开(公告)号：US06242605B1
公开(公告)日：2001-06-05
申请号：US09458316
申请日：1999-12-10
申请人： Panolil Raveendranath , Joseph Zeldis , Galina Vid , John R. Potoski , Jianxin Ren , Silvio Iera
发明人： Panolil Raveendranath , Joseph Zeldis , Galina Vid , John R. Potoski , Jianxin Ren , Silvio Iera
IPC分类号： C07D23702
CPC分类号： C07D295/088 , C07C217/48
摘要： The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.
摘要翻译：本发明提供了可用于合成生物活性化合物的化合物及其制备方法，具有下式的化合物：其中：R 1和R 2独立地选自H; C1-C12烷基或C1-C6全氟化烷基; X表示离去基团; A为0或S; m为1〜3的整数，优选为2; R 3，R 4，R 5和R 6独立地选自H，卤素，-NO 2，烷基，烷氧基，C 1 -C 6全氟烷基，OH或其C 1 -C 4酯或其烷基醚，-CN，-O-R 1， O-Ar，-S-R 1，-S-Ar，-SO-R 1，-SO-Ar，-SO 2 -R 1，-SO 2 -Ar，-CO-R 1，-CO-Ar，-CO 2 -R -CO 2 -Ar; 并且Y选自a）部分：其中R 7和R 8独立地选自H，C 1 -C 6烷基或苯基; 或b）任选取代的五元，六元或七元饱和的不饱和或部分不饱和的杂环或双环杂环，其含有至多两个选自-O - ， - NH - ， - N（C 1 -C 4烷基） - ， - N =和-S（O）n - 。

7. 发明申请

US20090018332A1 Processes For Preparing Bicyclic Oxazine Carboxaldehyde and Beta-Lactamase Inhibitors 审中-公开
标题翻译：制备双环恶嗪甲醛和β-内酰胺酶抑制剂的方法
公开(公告)号：US20090018332A1
公开(公告)日：2009-01-15
申请号：US12144733
申请日：2008-06-24
申请人： Kenneth Alfred Martin Kremer , Lalitha Krishnan , Aranapakam Mudumbai Venkatesan , Mellard Norman Jennings , Joseph Zeldis , Takao Abe , Tarek Suhayl Mansour , Henry Lee Strong
发明人： Kenneth Alfred Martin Kremer , Lalitha Krishnan , Aranapakam Mudumbai Venkatesan , Mellard Norman Jennings , Joseph Zeldis , Takao Abe , Tarek Suhayl Mansour , Henry Lee Strong
IPC分类号： C07D498/04
CPC分类号： C07C47/277 , C07C43/303 , C07C45/513 , C07C45/71 , C07C47/263 , C07C69/716 , C07C257/14 , C07D265/30 , C07D498/04 , C07D519/00
摘要： The invention relates to processes for the preparation of the bicyclic oxazine carboxaldehyde Compound 1: The invention also relates to the use of Compound 1 in the preparation of □-lactamase inhibitors.
摘要翻译：本发明涉及制备双环恶嗪甲醛的方法化合物1：本发明还涉及化合物1在制备β-内酰胺酶抑制剂中的用途。

8. 发明申请

US20080058543A1 Process for making chiral 1,4-disubstituted piperazines 审中-公开
标题翻译：制备手性1,4-二取代哌嗪的方法
公开(公告)号：US20080058543A1
公开(公告)日：2008-03-06
申请号：US11891062
申请日：2007-08-08
申请人： Joseph Zeldis , Gregg Feigelson , Ivo Jirkovsky
发明人： Joseph Zeldis , Gregg Feigelson , Ivo Jirkovsky
IPC分类号： C07C309/63 , C07C229/02
CPC分类号： C07D487/10 , C07B2200/07 , C07C229/12 , C07C309/06 , C07D319/18
摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.
摘要翻译：用于立体选择性制备新型手性氮芥衍生物的方法，其用于合成下式所示的光学活性1,4-二取代哌嗪：其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。

9. 发明授权

US07276611B2 Process for synthesizing beta-lactamase inhibitor intermediates 失效
标题翻译： β-内酰胺酶抑制剂中间体的合成方法
公开(公告)号：US07276611B2
公开(公告)日：2007-10-02
申请号：US10844243
申请日：2004-05-12
申请人： Michael William Winkley , Anita Wai-Yin Chan , Ivo L. Jirkovsky , Kenneth Alfred Martin Kremer , Joseph Zeldis , Antonia Aristotelevna Nikitenko , Henry Lee Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam M. Venkatesan
发明人： Michael William Winkley , Anita Wai-Yin Chan , Ivo L. Jirkovsky , Kenneth Alfred Martin Kremer , Joseph Zeldis , Antonia Aristotelevna Nikitenko , Henry Lee Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam M. Venkatesan
IPC分类号： C07D231/54
CPC分类号： C07D498/04 , C07D487/04
摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
摘要翻译：提供了一种制备具有结构式I的双环杂芳基羧醛的方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

10. 发明授权

US07091349B2 Process for synthesizing N-aryl piperazines with chiral N′-1-[benzoyl(2-pyridyl)amino]-2-propane substitution 失效
标题翻译：用手性N'-1- [苯甲酰基（2-吡啶基）氨基] -2-丙烷取代物合成N-芳基哌嗪的方法
公开(公告)号：US07091349B2
公开(公告)日：2006-08-15
申请号：US10780972
申请日：2004-02-18
申请人： Gregg Brian Feigelson , Joseph Zeldis , Ivo Ladislav Jirkovsky
发明人： Gregg Brian Feigelson , Joseph Zeldis , Ivo Ladislav Jirkovsky
IPC分类号： C07D401/12 , C07D405/14
CPC分类号： C07D405/12 , C07D319/18
摘要： A process for formation of N-aryl piperazines with chiral N′-1-[benzoyl(2-pyridyl)amino]-2-propane side-chains having the structure shown in formula below, and for making intermediate compounds therefor. In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N, N′ disubstituted piperazines act on the central nervous system at 5HT receptors.
摘要翻译：用具有下式结构的手性N'-1- [苯甲酰基（2-吡啶基）氨基] -2-丙烷侧链形成N-芳基哌嗪的方法，制备其中间体化合物。在该方法中，在哌嗪环形成步骤中引入手性，通过置换并入2-氨基吡啶基取代。所得N，N'二取代的哌嗪作用于5HT受体的中枢神经系统。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式