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41 条记录 (耗时 0.044 秒)

    Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
    22.
    发明授权
    Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties 失效
    具有抗高血压，心脏保护作用，抗缺血性和抗脂解性的化合物

    公开(公告)号：US06376472B1

    公开(公告)日：2002-04-23

    申请号：US09174191

    申请日：1998-10-16

    申请人： Michael R. Myers ,  Martin P. Maguire ,  Alfred P. Spada ,  William R. Ewing ,  Henry W. Pauls ,  Yong Mi Choi-Sledeski

    发明人： Michael R. Myers ,  Martin P. Maguire ,  Alfred P. Spada ,  William R. Ewing ,  Henry W. Pauls ,  Yong Mi Choi-Sledeski

    IPC分类号： C07D47334

    CPC分类号： C07H19/16 ,  C07D401/04 ,  C07D471/04 ,  C07D473/34

    摘要： A compound of the formula wherein K is N; Q is CH2 or O; R6 is hydrogen, alkyl, allyl, 2-methylallyl, 2-butenyl, or cycloalkyl where the nitrogen of the ring of X is substituted by Y; E is O or S; Y is hydrogen, alkyl, aralkyl, substituted aralkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl, or substituted heterocyclylalkyl; and n and p are independently 0, 1, 2, or 3, provided that n+p is at least 1; T is hydrogen, alkyl, alkylcarbonyl, alkylthiocarbonyl, halo, carboxyl, A and B are independently hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, or OR′; or a pharmaceutically acceptable salt thereof, a pharmaceutic-ally acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof.

    摘要翻译： 化合物K为N; Q是CH 2或O; R6是氢，烷基，烯丙基，2-甲基烯丙基，2-丁烯基或环烷基，X的环的氮被Y取代; E为O或S; Y是氢，烷基，芳烷基，取代的芳烷基，芳基，取代的芳基，杂环基，取代的杂环基，杂环基烷基或取代的杂环基烷基; n和p独立地为0,1,2或3，条件是n + p为至少1; T为氢，烷基，烷基羰基，烷硫基羰基，卤素，羧基，A和B独立地为氢，烷基，羟基烷基， 烷氧基烷基或OR';或其药学上可接受的盐，其药学上可接受的前药，其N-氧化物，其水合物或其溶剂化物。

    Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
    27.
    发明授权
    Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties 失效
    具有抗高血压，心脏保护作用，抗缺血性和抗脂解性的化合物

    公开(公告)号：US5561134A

    公开(公告)日：1996-10-01

    申请号：US316761

    申请日：1994-10-03

    申请人： Alfred P. Spada ,  Cynthia A. Fink ,  Michael R. Myers

    发明人： Alfred P. Spada ,  Cynthia A. Fink ,  Michael R. Myers

    IPC分类号： C07D473/34 ,  A61K31/435 ,  A61K31/52 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P3/06 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D471/04 ,  C07D473/00 ,  C07H19/04 ,  C07H19/052 ,  C07H19/16

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

    摘要： Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.b are independently H, OH, alkyl, hydroxyalkyl, alkyl mercaptyl, thioalkyl, alkoxy, alkyoxyalkyl, amino, alkyl amino, carboxyl, acyl, halogen, carbamoyl, alkyl carbamoyl, aryl or heterocyclyl; and R' and R" are independently hydrogen, alkyl, aralkyl, carbamoyl, alkyl carbamoyl, dialkylcarbamoyl, acyl, alkoxycarbonyl aralkoxycarbonyl, aryloxycarbonyl, or R' and R" together may form ##STR4## where R.sub.c is hydrogen or alkyl, ##STR5## where R.sub.d and R.sub.e are independently hydrogen, alkyl, or together with the carbon atom to which they are attached may form a 1,1-cycloalkyl group; provided that when X is straight chain alkylene and Q is oxygen, then Z represents a heterocyclyl including at least two heteroatoms, which are adenosine agonists useful as antihypertensive, cardioprotective, antiischemic, and antilipolytic agents, pharmaceutical compositions including such compounds, and their use in treating hypertension, myocardial ischemia, ameliorating ischemic injury and myocardial infarct size consequent to myocardial ischemia, hyperlipidemia and hypercholesterolemia are claimed.

    摘要翻译： 式的化合物其中：K为N或N-> O; Q是CH 2或O; T为或R3O-CH2; X是直链或支链亚烷基，亚环烷基或环亚烯基，其各自任选被至少一个CH 3，CH 3 CH 2，Cl，F，CF 3或CH 3 O取代; Y为NR4，O或S; a = 0或1; Z为式（Ⅰ）Z1为N，CR5，（CH）m-CR5或（CH）m-N，m为1或2; Z2为N，NR6，O或S，n为0或1; R1，R2，R3，R4，R5和R6独立地为H，烷基，芳基或杂环基; R a和R b独立地是H，OH，烷基，羟基烷基，烷基硫醇基，硫代烷基，烷氧基，烷氧基烷基，氨基，烷基氨基，羧基，酰基，卤素，氨基甲酰基，烷基氨基甲酰基，芳基或杂环基。 并且R'和R“独立地是氢，烷基，芳烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，酰基，烷氧基羰基芳烷氧基羰基，芳氧基羰基或R'和R”可一起形成其中R c是氢或烷基， 其中Rd和Re独立地是氢，烷基或与它们所连接的碳原子一起形成1,1-环烷基; 条件是当X是直链亚烷基并且Q是氧时，Z代表包括至少两个杂原子的杂环基，它们是可用作抗高血压，心脏保护，抗缺血和抗脂肪分解剂的腺苷激动剂，包括这些化合物的药物组合物，以及它们在 要求治疗高血压，心肌缺血，改善缺血性损伤和心肌缺血，高脂血症和高胆固醇血症引起的心肌梗死面积。

    Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
    29.
    发明授权
    Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties 失效
    具有抗高血压，心脏保护作用，抗缺血性和抗脂解性的化合物

    公开(公告)号：US5736554A

    公开(公告)日：1998-04-07

    申请号：US455361

    申请日：1995-05-31

    申请人： Alfred P. Spada ,  Cynthia A. Fink ,  Michael R. Myers

    发明人： Alfred P. Spada ,  Cynthia A. Fink ,  Michael R. Myers

    IPC分类号： C07D473/34 ,  A61K31/435 ,  A61K31/52 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P3/06 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D471/04 ,  C07D473/00 ,  C07H19/04 ,  C07H19/052 ,  C07H19/16 ,  A61K31/44

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

    摘要： Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.b are independently H, OH, alkyl, hydroxyalkyl, alkyl mercaptyl, thioalkyl, alkoxy, alkyoxyalkyl, amino, alkyl amino, carboxyl, acyl, halogen, carbamoyl, alkyl carbamoyl, aryl or heterocyclyl; and R' and R" are independently hydrogen, alkyl, aralkyl, carbamoyl, alkyl carbamoyl, dialkylcarbamoyl, acyl, alkoxycarbonyl, aralkoxycarbonyl, aryloxycarbonyl, or R' and R" together may form ##STR4## where R.sub.c is hydrogen or alkyl, ##STR5## where R.sub.d and R.sub.e are independently hydrogen, alkyl, or together with the carbon atom to which they are attached may form a 1,1-cycloalkyl group; provided that when X is straight chain alkylene and Q is oxygen, then Z represents a heterocyclyl including at least two heteroatoms, which are adenosine agonists useful as antihypertensive, cardioprotective, antiischemic, and antilipolytic agents, pharmaceutical compositions including such compounds, and their use in treating hypertension, myocardial ischemia, ameliorating ischemic injury and myocardial infarct size consequent to myocardial ischemia, hyperlipidemia and hypercholesterolemia are claimed.

    摘要翻译： 式的化合物其中：K为N或N-> O; Q是CH 2或O; T为或R3O-CH2; X是直链或支链亚烷基，亚环烷基或环亚烯基，其各自任选被至少一个CH 3，CH 3 CH 2，Cl，F，CF 3或CH 3 O取代; Y为NR4，O或S; a = 0或1; Z为式（Ⅰ）Z1为N，CR5，（CH）m-CR5或（CH）m-N，m为1或2; Z2为N，NR6，O或S，n为0或1; R1，R2，R3，R4，R5和R6独立地为H，烷基，芳基或杂环基; R a和R b独立地是H，OH，烷基，羟基烷基，烷基硫醇基，硫代烷基，烷氧基，烷氧基烷基，氨基，烷基氨基，羧基，酰基，卤素，氨基甲酰基，烷基氨基甲酰基，芳基或杂环基。 并且R'和R“独立地为氢，烷基，芳烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，酰基，烷氧基羰基，芳烷氧基羰基，芳氧基羰基或R'和R”一起可以形成E>，其中Rd和Re独立地为氢， 烷基或与它们所连接的碳原子一起可以形成1,1-环烷基; 条件是当X是直链亚烷基并且Q是氧时，Z代表包括至少两个杂原子的杂环基，它们是可用作抗高血压，心脏保护，抗缺血和抗脂肪分解剂的腺苷激动剂，包括这些化合物的药物组合物，以及它们在 要求治疗高血压，心肌缺血，改善缺血性损伤和心肌缺血，高脂血症和高胆固醇血症引起的心肌梗死面积。

    DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
    30.
    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。