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1. 发明授权

US07019137B2 Process for making chiral 1,4-disubstituted piperazines 失效
公开(公告)号：US07019137B2
公开(公告)日：2006-03-28
申请号：US10384837
申请日：2003-03-10
申请人： Ivo Jirkovsky , Joseph Zeldis , Gregg Brian Feigelson
发明人： Ivo Jirkovsky , Joseph Zeldis , Gregg Brian Feigelson
IPC分类号： C07D295/15
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.

2. 发明授权

US06713626B2 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：US06713626B2
公开(公告)日：2004-03-30
申请号：US10384845
申请日：2003-03-10
申请人： Gregg Brian Feigelson , Joseph Zeldis , Ivo Jirkovsky
发明人： Gregg Brian Feigelson , Joseph Zeldis , Ivo Jirkovsky
IPC分类号： C07D40112
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，并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，通过置换引入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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

US20050070709A1 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：US20050070709A1
公开(公告)日：2005-03-31
申请号：US10919099
申请日：2004-08-16
申请人： Anita Chan , Gregg Feigelson , Joseph Zeldis , Ivo Jirkovsky
发明人： Anita Chan , Gregg Feigelson , Joseph Zeldis , Ivo Jirkovsky
IPC分类号： A61P25/00 , C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12 , C07D319/14 , C07D413/02
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，其中R和R'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。

8. 发明授权

US4997948A 5-[(1- and 2-naphthalenyl) sulfonyl]-2,4-thiazolidinediones and derivatives thereof 失效
标题翻译： 5 - [（1-和2-萘基）磺酰基] -2,4-噻唑烷二酮及其衍生物
公开(公告)号：US4997948A
公开(公告)日：1991-03-05
申请号：US428817
申请日：1989-10-27
申请人： Arie Zask , Ivo Jirkovsky
发明人： Arie Zask , Ivo Jirkovsky
IPC分类号： C07D277/36
CPC分类号： C07D277/36
摘要： Disclosed herein are 1- or 2-thio, thiomethylene, and sulfonylnaphthalene derivatives of formulas I and II ##STR1## or a pharmaceutically acceptable catonic salt thereof, wherein n is 0 or 1R.sub.5 is hydrogen, bromo, chloro, trifluoromethyl or difluoroethyl;R.sub.6 is hydrogen, hydroxy, methoxy or ethoxy; andR.sub.7 is hydrogen or R.sub.7 and R.sub.6 are both methyl or ethyl carbonate,provided that, when S(O).sub.2 is in the 2 position of the naphthalene ring, R.sub.5, R.sub.6 and R.sub.7 are each hydrogen. The disclosed compounds possess blood-glucose lowering actions and are useful in the treatment of diabetes mellitus.
摘要翻译：本文公开了式I和II的1-或2-硫代，亚甲基亚甲基和磺酰基萘衍生物或其药学上可接受的盐，其中n为0或1个R 5为氢，溴，氯，三氟甲基或二氟乙基; R6是氢，羟基，甲氧基或乙氧基; 并且R 7是氢或R 7和R 6都是甲基或碳酸乙酯，条件是当S（O）2在萘环的2位时，R 5，R 6和R 7各自为氢。所公开的化合物具有降血糖作用，可用于治疗糖尿病。

9. 发明授权

US4066780A Pyranoindole derivatives as antiulcer agents 失效
标题翻译：吡咯并吲哚衍生物作为抗溃疡剂
公开(公告)号：US4066780A
公开(公告)日：1978-01-03
申请号：US736606
申请日：1976-10-28
申请人： Christopher A. Demerson , Leslie G. Humber , Andre A. Asselin , Ivo Jirkovsky , Thomas A. Dobson
发明人： Christopher A. Demerson , Leslie G. Humber , Andre A. Asselin , Ivo Jirkovsky , Thomas A. Dobson
IPC分类号： C07D209/08 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535
CPC分类号： C07D209/08 , Y10S514/925
摘要： Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[3,4-b]indole or thiopyrano[3,4-b]indole nucleus or having said radical attached to the 1 position of a pyrano[4,3-b]indole or thiopyrano[4,3-b]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3,4,5,6,7,8, and 9. The pyrano[3,4-b]indole or thiopyrano[3,4-b]indole derivatives having the amino(lower)alkyl radical only at position 9 possess two substitutents at position 1 and may be optionally substituted at position 3,4,5,6,7, and 8; the derivatives having an amino(lower)alkyl radical at both positions 1 and 9 are further substituted at position 1 and may be optionally substituted at positions 3,4,5,6,7 and 8. The pyrano-and thiopyranoindole derivatives of this invention are useful antidepressant and antiulcer agents. Methods for the preparation and use of these derivatives are also disclosed.
摘要翻译：吡喃并吲哚和噻喃并吲哚衍生物，其特征在于具有连接于吡喃并[3,4-b]吲哚或噻喃并[3,4-b]吲哚核的1位和9位的氨基（低级）烷基，或具有所述基团公开了连接于吡喃并[4,3-b]吲哚或噻喃并[4,3-b]吲哚核的1位的化合物。氨基（低级）烷基的氨基部分可进一步被一个或两个低级烷基取代或并入杂环胺基中。仅在位置1具有氨基（低级）烷基的衍生物在位置1处进一步被取代，并且可以在3,4,5,6,7,8和9位任意被取代。吡喃并[3,4-b ]吲哚或噻喃并[3,4-b]吲哚衍生物，其仅在位置9具有氨基（低级）烷基，在位置1具有两个取代基，并且可以在3,4,5,6,7和8位上任选被取代 ; 具有位置1和9位置上的氨基（低级）烷基的衍生物在位置1处进一步被取代，并且可以在3,4,5,6,7和8位任意被取代。本发明的吡喃和噻喃并吲哚衍生物是有用的抗抑郁药和抗溃疡剂。还公开了这些衍生物的制备和使用方法。

10. 发明授权

US4035495A Pyrrolobenzoxazines, pyrrolobenzothiazines and process therefor 失效
标题翻译：吡咯并苯并嗪，吡咯并苯并噻嗪及其制备方法
公开(公告)号：US4035495A
公开(公告)日：1977-07-12
申请号：US548318
申请日：1975-02-10
申请人： Ivo Jirkovsky , Leslie G. Humber
发明人： Ivo Jirkovsky , Leslie G. Humber
IPC分类号： C07D498/04 , C07D513/04 , A61K31/54 , A61K31/535 , C07D265/28 , C07D279/16
CPC分类号： C07D513/04
摘要： 4H-Pyrrolo[2,1-c][1,4]benzoxazines and 4H-pyrrolo[2,1-c]-[1,4]benzothiazines characterized by having an alkylamine substituent at position 4 are disclosed. The compounds are characterized further by having an alkyl substituent on the same carbon atom bearing the alkylamine substituent. In addition the compounds may be optionally substituted at positions 1 and 6 to 9. Also disclosed are 4H-pyrrolo-[2,1-c][1,4]benzoxazines and 4H-pyrrolo[2,1-c][1,4]benzothiazines which are dialkylated at position 4 and have a methylamino substituent at position 1. The foregoing compounds possess antihypertensive and central nervous system depressant activity and methods for their preparation and use are described.
摘要翻译：公开了在4位具有烷基胺取代基的4H-吡咯并[2,1-c] [1,4]苯并恶嗪和4H-吡咯并[2,1-c] - [1,4]苯并噻嗪。化合物的特征还在于具有烷基取代基的碳原子上具有烷基取代基。此外，化合物可以在1和6位至9位任选被取代。还公开了4H-吡咯并[2,1-c] [1,4]苯并恶嗪和4H-吡咯并[2,1-c] 4]苯并噻嗪，它们在4位被二烷基化并且在1位具有甲基氨基取代基。上述化合物具有抗高血压和中枢神经系统抑制活性，并且描述了它们的制备和使用方法。

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