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9 条记录 (耗时 0.027 秒)

    Process for the preparation of azacycloalkylakanoyl pseudotetrapeptides
    3.
    发明授权
    Process for the preparation of azacycloalkylakanoyl pseudotetrapeptides 失效
    制备氮杂环烷基烷酰基假四肽的方法

    公开(公告)号：US06180759B2

    公开(公告)日：2001-01-30

    申请号：US09544680

    申请日：2000-04-07

    申请人： James J. Mencel ,  Robert Stammler ,  Christophe Daubie ,  Michel Lavigne ,  Benoit J. Vanasse ,  Robert C. Liu ,  Patrick Leon ,  Geoffrey A. D'Netto ,  Adam W. Sledeski

    发明人： James J. Mencel ,  Robert Stammler ,  Christophe Daubie ,  Michel Lavigne ,  Benoit J. Vanasse ,  Robert C. Liu ,  Patrick Leon ,  Geoffrey A. D'Netto ,  Adam W. Sledeski

    IPC分类号： C07C22718

    CPC分类号： C07D211/34 ,  C07K5/021 ,  C07K5/06113 ,  Y02P20/55

    摘要： This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.

    摘要翻译： 本发明涉及制备式I的假四肽或其盐或前药的方法，其中任选地氮保护氮杂环基;是单键或双键; q为1-5; B是烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，芳烷基，烷基芳基或烷基烷基; Q2是H或羧酸保护基; J是-H，烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，取代的芳基，芳烷基，取代的芳烷基; L是OR 1或NR 1 R 2，其中R 1和R 2独立地是-H，烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，芳烷基，烷基芳基或烷基烷基; 并且p是1或2，其包括两个二肽或伪多肽的偶联。

    Process for preparing 2,4- dihydroxypyridine and 2,4- dihydroxy-3-nitropyridine
    5.
    发明授权
    Process for preparing 2,4- dihydroxypyridine and 2,4- dihydroxy-3-nitropyridine 失效
    制备2,4-二羟基吡啶和2,4-二羟基-3-硝基吡啶的方法

    公开(公告)号：US06307054B1

    公开(公告)日：2001-10-23

    申请号：US09108622

    申请日：1998-07-01

    申请人： Larry K. Truesdale ,  James P. Sherbine ,  Benoit J. Vanasse

    发明人： Larry K. Truesdale ,  James P. Sherbine ,  Benoit J. Vanasse

    IPC分类号： C07D21369

    CPC分类号： C07D213/80 ,  C07D213/61 ,  C07D473/00

    摘要： The present invention is directed to a process for preparing 2,4-dihydroxy-pyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroxy-3-nitropyridine comprising reacting 2,4-dihydroxypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischemia, ameliorating ischenic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.

    摘要翻译： 本发明涉及一种制备2,4-二羟基 - 吡啶的方法，包括加热式A的化合物，其中R是H，烷基或芳烷基和磷酸，其中磷酸与水的比例不小于约27至 1重量％。 本发明还涉及制备2,4-二羟基-3-硝基吡啶的方法，其包括使2,4-二羟基吡啶与硝酸反应。本发明的方法制备可用于制备可用于治疗心血管的化合物的中间体 由高血压或心肌缺血引起的疾病，改善严重性损伤或心肌梗死面积，或治疗高脂血症或高胆固醇血症。

    Process for preparing 2,4-dihydroxypyridine and 2,4-dihydroxy-3-nitropyridine
    6.
    发明授权
    Process for preparing 2,4-dihydroxypyridine and 2,4-dihydroxy-3-nitropyridine 失效
    制备2,4-二羟基吡啶和2,4-二羟基-3-硝基吡啶的方法

    公开(公告)号：US06392049B1

    公开(公告)日：2002-05-21

    申请号：US09861023

    申请日：2001-05-18

    申请人： Larry K. Truesdale ,  James P. Sherbine ,  Benoit J. Vanasse

    发明人： Larry K. Truesdale ,  James P. Sherbine ,  Benoit J. Vanasse

    IPC分类号： C07D21373

    CPC分类号： C07D213/80 ,  C07D213/61 ,  C07D473/00

    摘要： The present invention is directed to a process for preparing 2,4-dihydroypyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroy-3-nitropyridine comprising reacting 2,4-dihydroypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischeria, ameliorating ischemic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.

    摘要翻译： 本发明涉及一种制备2,4-二氢吡啶的方法，包括加热式A的化合物，其中R是H，烷基或芳烷基和磷酸，其中磷酸与水的比例不小于约27至1重量％ ％。 本发明还涉及制备2,4-二氢-3-硝基吡啶的方法，其包括使2,4-二氢吡啶与硝酸反应。本发明的方法制备可用于制备可用于治疗心血管的化合物的中间体 由高血压或心肌胰岛素标记的疾病，改善缺血性损伤或心肌梗死面积，或治疗高脂血症或高胆固醇血症。

    DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
    9.
    发明授权
    DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof 失效
    DI（1R） - （ - ）樟脑磺酸）盐，其制备及其用途

    公开(公告)号：US5652366A

    公开(公告)日：1997-07-29

    申请号：US484811

    申请日：1995-06-07

    申请人： Alfred P. Spada ,  Cynthia A. Fink ,  Michael R. Myers ,  Laurence W. Reilly ,  Benoit J. Vanasse

    发明人： Alfred P. Spada ,  Cynthia A. Fink ,  Michael R. Myers ,  Laurence W. Reilly ,  Benoit J. Vanasse

    IPC分类号： C07D471/04 ,  C07D473/00 ,  C07H19/052 ,  C07H19/16

    CPC分类号： C07D471/04 ,  C07D473/00 ,  C07H19/052 ,  C07H19/16

    摘要： This invention relates to di[(1 R)-(-)-camphosulfonic acid) salt of [1S-[1.alpha.,2.beta.,3.beta.,4.alpha.,(S*)]]-4-[7-[[2-(3-chloro-2-thienyl)-1-ethylethyl]amino]3 H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide, and a process for preparing the compound, comprising reacting a reaction mixture of (-)-1.beta.-N-ethyl-2.alpha.,3.alpha.-isopropylidenedioxy-4.beta.-[3-amino-4-[2-(5-chloro-2-thienyl)-(1R)-1-ethylethyl]amino-2-pyridyl]aminocyclopentanecarboxamide and formamidine acetate, and then treating the reaction mixture with (1 R)-(-)-10-camphorsulfonic acid.The salt is useful in purifying [1 S-[1.alpha.,2.beta.,3.beta.,4.alpha.,(S*)]]-4-[7-[[2-(3-chloro-2-thienyl)-1-ethylethyl]amino]-3 H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide which possesses adenosine agonist activity and is useful as an anti-hypertensive, cardioprotective, anti-ischemic, and antilipolytic agent.

    摘要翻译： 本发明涉及[1S- [1α，2β，3β，4α，（S *）]] - 4- [7 - [[ 2-（3-氯-2-噻吩基）-1-乙基乙基]氨基] 3 H-咪唑并[4,5-b]吡啶-3-基] -N-乙基-2,3-二羟基环戊烷甲酰胺，以及 制备该化合物，包括使（ - ） - 1β-N-乙基-2α，αα-异亚丙基二氧基-4β-[3-氨基-4- [2-（5-氯-2-噻吩基） ） - （1R）-1-乙基乙基]氨基-2-吡啶基]氨基环戊烷甲酰胺和甲脒乙酸盐，然后用（1R） - （ - ） - 10-樟脑磺酸处理反应混合物。 该盐可用于纯化[1 S- [1α，2β，3β，4α，（S *）]] -4- [7 - [[2-（3-氯-2-噻吩基） - 乙基]氨基] -3H-咪唑并[4,5-b]吡啶-3-基] -N-乙基-2,3-二羟基环戊烷甲酰胺，其具有腺苷激动剂活性，可用作抗高血压，心脏保护，抗 - 抗血清剂和抗脂肪分解剂。