Benzodiazepine derivatives
    1.
    发明授权
    Benzodiazepine derivatives 失效
    苯并二氮杂衍生物

    公开(公告)号:US5763437A

    公开(公告)日:1998-06-09

    申请号:US776196

    申请日:1997-01-29

    CPC分类号: C07D243/24

    摘要: Benzodiazepine derivatives of formula (I) wherein R.sup.1 is aryl which may have one or more suitable substituent(s), R.sup.2 is C.sub.3 -C.sub.8 cycloalkyl which may have one or more suitable substituent(s), A is lower alkylene, R.sup.3 is a heterocyclic group selected from the group consisting of tetrahydrofuryl, dioxolanyl, filryl, thienyl, isoxazolyl, pyridyl, benzimidazolyl, benzotiazolyl, benzoxazolyl, benzopyrany, quinolyl, isoquinolyl, tetrahydroisoquinolyl, benzothienyl and benzofuryl, each of which may have one or more suitable substituent(s), or a pharmaceutically acceptable salt thereof, which are useful as a medicament.

    摘要翻译: PCT No.PCT / JP95 / 01497 Sec。 371日期1997年1月29日 102(e)1997年1月29日PCT PCT 1995年7月27日PCT公布。 公开号WO96 / 04254 日期:1996年2月15日,式(I)的苯并二氮杂衍生物,其中R 1为可具有一个或多个合适取代基的芳基,R 2为可具有一个或多个合适取代基的C 3 -C 8环烷基,A为低级亚烷基 R3是选自四氢呋喃基,二氧戊环基,二烯丙基,噻吩基,异恶唑基,吡啶基,苯并咪唑基,苯并噻唑基,苯并恶唑基,苯并吡喃基,喹啉基,异喹啉基,四氢异喹啉基,苯并噻吩基和苯并呋喃基的杂环基,其各自可以具有一个或多个 合适的取代基或其药学上可接受的盐,其可用作药物。

    Triazine derivatives, and pharmaceutical compositions comprising the same
    3.
    发明授权
    Triazine derivatives, and pharmaceutical compositions comprising the same 失效
    三嗪衍生物和包含其的药物组合物

    公开(公告)号:US4618610A

    公开(公告)日:1986-10-21

    申请号:US603173

    申请日:1984-04-23

    CPC分类号: C07D253/06

    摘要: New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or halogen;R.sup.2 is a hydroxy, protected hydroxy, amino, cyano, mercapto, lower alkylthio, arylthio, sulfamoyl, lower alkylsulfonylamino, lower alkylureido, arylureido, lower alkyl-thioureido, aryl-thioureido, lower alkenoylamino, lower alkoxycarbonylamino, lower alkoxy(thiocarbonyl)thio, or cyclic or acyclic alkanoylamino in which the cyclic and acyclic alkanoylamino group may have a substituent selected from lower alkoxy, aryl, hydroxyaryl and protected hydroxyaryl; andX is O or S;and pharmaceutically acceptable salt thereof, which are useful in the treatment of hypertension, thrombosis and ulcer in human beings and animals.

    摘要翻译: 由下式表示的新的三嗪衍生物:其中R 1是氢或卤素; R2是羟基,保护的羟基,氨基,氰基,巯基,低级烷硫基,芳硫基,氨磺酰基,低级烷基磺酰基氨基,低级烷基脲基,芳基脲基,低级烷基 - 硫脲基,芳基 - 硫脲基,低级烯酰基氨基,低级烷氧基羰基氨基,低级烷氧基(硫代羰基) 或环状或无环烷酰氨基,其中环状和非环状烷酰基氨基可以具有选自低级烷氧基,芳基,羟基芳基和被保护的羟基芳基的取代基; X为O或S; 和其药学上可接受的盐,其可用于治疗人和动物中的高血压,血栓形成和溃疡。

    Chromone compounds and preparation thereof
    8.
    发明授权
    Chromone compounds and preparation thereof 失效
    色酮化合物及其制备方法

    公开(公告)号:US4105781A

    公开(公告)日:1978-08-08

    申请号:US788735

    申请日:1977-04-19

    CPC分类号: C07D407/12 Y02P20/55

    摘要: Chromone compounds having the structure ##STR1## wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy (lower) alkylene, R.sub.1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R.sub.2 is hydrogen or lower alkoxy, Y.sub.1 is lower alkylene or hydroxyl (lower) alkylene, Z is oxygen or sulfur and R.sub.3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar (lower) alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting ##STR2## wherein Y' is hydroxy (lower) alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R--COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I'] are prepared by reacting the compound ##STR3## with the compound X--Y.sub.1 '--Z--R.sub.3 ' wherein X is an acid residue, Y' is lower alkylene or hydroxy (lower) alkylene whose hydroxy group is optionally protected by a protective group, R.sub.3 ' is hydrogen, lower alkyl, aryl, substituted aryl, or ar (lower) alkyl and Z is as defined above. When R.sub.3 ' is hydrogen, --Z--R.sub.3 ' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when --Z--R.sub.3 ' is protected to split off the protective group.

    摘要翻译: 具有结构(I)或者其中R是芳基,取代的芳基,噻吩基,呋喃基或吡啶基的结构的色酮化合物,Y是羟基(低级)亚烷基,R 1是氢,低级烷基,芳基, 取代的芳基或杂环基,R2是氢或低级烷氧基,Y1是低级亚烷基或羟基(低级)亚烷基,Z是氧或硫,R3是氢,低级烷基,芳基,取代芳基或芳(低级) 抗过敏活性,可用于治疗哮喘。 结构[I]的化合物通过其中Y'是羟基被最佳保护的羟基(低级)亚烷基或其[II]的反应性衍生物与式R-COOH的羧酸反应制备 在碱性催化剂的存在下。 然后将所得化合物与酸反应。 通过使化合物< IMAGE>与化合物X-Y1'-Z-R3'反应其中X是酸残基,Y'是低级亚烷基或羟基(低级)亚烷基 其羟基任选被保护基保护,R 3'是氢,低级烷基,芳基,取代的芳基或芳(低级)烷基,Z如上所定义。 当R3'为氢时,-Z-R3'任选被保护基保护。 当Y'为受保护基团时或当-Z-R3'被保护以分离保护基团时,所得化合物进行消除反应。

    Chromone compounds
    9.
    发明授权
    Chromone compounds 失效
    色酮化合物

    公开(公告)号:US4049664A

    公开(公告)日:1977-09-20

    申请号:US679140

    申请日:1976-04-22

    IPC分类号: C07D407/12 C07D311/22

    摘要: Chromone compounds having the structure ##STR1## wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy (lower) alkylene, R.sub.1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R.sub.2 is hydrogen or lower alkoxy, Y.sub.1 is lower alkylene or hydroxyl (lower) alkylene, Z is oxygen or sulfur and R.sub.3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting ##STR2## wherein Y' is hydroxy (lower) alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R--COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I] are prepared by reacting the compound ##STR3## with the compound X--Y.sub.1 '--Z--R.sub.3 ' wherein X is an acid residue, Y' is lower alkylene or hydroxy (lower) alkylene whose hydroxy group is optionally protected by a protective group, R.sub.3 ' is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl and Z is defined above. When R.sub.3 ' is hydrogen, --Z--R.sub.3 ' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when --Z--R.sub.3 ' is protected to split off the protective group.

    摘要翻译: 具有结构(I)的色酮化合物其中R是芳基,取代的芳基,噻吩基,呋喃基或吡啶基,Y是羟基(低级)亚烷基,R1是氢,低级烷基,芳基,取代的 芳基或杂环基,R2是氢或低级烷氧基,Y1是低级亚烷基或羟基(低级)亚烷基,Z是氧或硫,R3是氢,低级烷基,芳基,取代芳基或芳(低级)烷基具有抗 - 过敏活性,可用于治疗哮喘。 结构[I]的化合物通过使(II)其中Y'是羟基被最佳保护的羟基(低级)亚烷基或[II]的反应性衍生物与式R-COOH的羧酸反应制备 在碱性催化剂的存在下。 然后将所得化合物与酸反应。 结构[I]化合物通过使化合物(Ⅳ)与化合物X-Y1'-Z-R3'反应而制备,其中X为酸残基,Y'为低级亚烷基或羟基(低级)亚烷基 羟基任选被保护基保护,R 3'是氢,低级烷基,芳基,取代的芳基或芳(低级)烷基,Z如上所定义。 当R3'为氢时,-Z-R3'任选被保护基保护。 当Y'为受保护基团时或当-Z-R3'被保护以分离保护基团时,所得化合物进行消除反应。