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522 条记录 (耗时 0.022 秒)

    Benzodiazepine analogs
    41.
    发明授权
    Benzodiazepine analogs 失效
    苯二氮卓类似物

    公开(公告)号：US4957915A

    公开(公告)日：1990-09-18

    申请号：US316463

    申请日：1989-02-27

    申请人： Sun H. Kim ,  John E. Taylor

    发明人： Sun H. Kim ,  John E. Taylor

    IPC分类号： C07D243/14 ,  A61K31/55 ,  A61K31/551 ,  A61P25/28 ,  A61P25/30 ,  C07D243/16 ,  C07D243/18 ,  C07D243/20 ,  C07D243/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

    CPC分类号： C07D405/12 ,  C07D243/24

    摘要： BZDs of the general formula 1: ##STR1## where: R represents H, alkyl, alkenyl, cycloalkyl or cycloalkenyl each with up to 8 carbon atoms, phenylalkyl with an alkylene chain of 1 to 3 carbon atoms and optionally substituted on the phenyl radical with one or two substituents selected from the group consisting of Cl, Br, F, CN, CF.sub.3, NO.sub.2, lower alkyl, and OCH.sub.3, or represents a phenyl radical which is optionally substituted with one or two substituents selected from the group consisting of Cl, F, Br, CN, I, CF.sub.3 NO.sub.2, lower alkyl and OCH.sub.3, or represents a 5-membered or 6-membered heterocyclic radical with 1 or 2 heteroatoms from the group consisting of O, N and S; R.sub.1 represents H or, together with R.sub.2, forms a bond; R.sub.2 and R.sub.4 independently of one another represent H, or an alkyl radical with 1 to 6 carbon atoms, or represent a phenylalkyl radical with an alkyl chain of 1 to 3 carbon atoms and optionally substituted on the phenyl radical with one or two substituents selected from the group consisting of Cl, Br, F, CN, CF.sub.3, NO.sub.2, CH.sub.3, C.sub.2 H.sub.5 and OCH.sub.3, or R.sub.2 together with R.sub.1, forms a bond; R.sub.3 is (CH.sub.2).sub.n CH or (CH.sub.2).sub.n --CR.sub.14 .dbd.CR.sub.14, where n is between 0 and 5 inclusive and R.sub.14 .dbd.HOL a bond; R.sub.5 and R.sub.6 independently of one another represent H, Cl, F, Br, NO.sub.2, CN, CF.sub.3, lower alkyl, or OCH.sub.3 ; R.sub.7 and R.sub.9 are independently CH.sub.2 or C.dbd.0; R.sub.8 is ##STR2## where p and q are independently between 0 and 4 and the sum of p and q is 4 or less; and R.sub.11 and R.sub.12 are independently H or a lower alkyl of between 1 and 5 carbon atoms.

    5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them
    45.
    发明授权
    5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them 失效
    5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-和含有它们的药物组合物

    公开(公告)号：US4329341A

    公开(公告)日：1982-05-11

    申请号：US178679

    申请日：1980-11-26

    申请人： Julianna Rochricht ,  Lajos Kisfaludy ,  Marton Kajtar ,  Eva Palosi ,  Laszlo Szporny

    发明人： Julianna Rochricht ,  Lajos Kisfaludy ,  Marton Kajtar ,  Eva Palosi ,  Laszlo Szporny

    IPC分类号： C07D243/24 ,  A61K31/55

    CPC分类号： C07D243/24

    摘要： The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;R.sup.2 stands for hydrogen or alkyl having 1 to 6 carbon atoms;R.sup.3 represents a group conventionally attached to the --CH(NH.sub.2)--COOH group of the known optically active or racemic .alpha.-amino-acids, preferably an optionally substituted lower alkyl group;R.sup.4 is hydrogen, chlorocarbonyl or carbamoyl; andX is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R.sup.4 stands for hydrogen R.sup.3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation. The new compounds show valuable enzyme inducing activity and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.

    摘要翻译： 本发明涉及通式（I）的新的光学活性或外消旋的5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-酮衍生物，其中R 1 代表氢，卤素，三氟甲基或硝基; R2代表氢或具有1至6个碳原子的烷基; R3表示通常与已知光学活性或外消旋的α-氨基酸的-CH（NH 2）-COOH基团连接的基团，优选任选取代的低级烷基; R4是氢，氯代羰基或氨基甲酰基; 并且X是氢，卤素或三氟甲基，条件是如果在外消旋化合物中R4代表氢，R3不是具有1至6个碳原子的烷基，其中3-和5-位的不对称中心具有 相同的绝对构型及其药学上可接受的酸加成盐及其制备方法。 新化合物显示有价值的酶诱导活性，因此可用作药物组合物的活性成分，其也在本发明的范围内。

    Benzodiazepine derivatives
    46.
    发明授权
    Benzodiazepine derivatives 失效
    苯并二氮杂衍生物

    公开(公告)号：US4327026A

    公开(公告)日：1982-04-27

    申请号：US283711

    申请日：1981-07-16

    申请人： Quirico Branca ,  Albert E. Fischli ,  Andre' Szente

    发明人： Quirico Branca ,  Albert E. Fischli ,  Andre' Szente

    IPC分类号： A61K31/55 ,  A61K31/551 ,  A61P5/38 ,  C07D243/16 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  C07D243/28

    CPC分类号： C07D243/24

    摘要： There is presented benzodiazepine derivatives of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is lower alkyl, R.sup.2 and R.sup.3 each are hydrogen or lower alkyl, R.sup.4 is the group ##STR3## R.sup.5 is hydrogen or halogen, R.sup.8 is hydrogen or lower alkyl, R.sup.9 is lower alkyl or lower alkoxyalkyl, R.sup.10 is lower alkyl, R.sup.11 is hydrogen, lower alkyl or lower hydroxyalkyl, R.sup.12 is hydrogen or lower alkyl and R.sup.14 is lower alkyl or aryl, and either R.sup.6 is hydrogen or lower alkyl and R.sup.7 is lower alkyl or lower hydroxyalkyl or R.sup.6 and R.sup.7 together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N-R.sup.13, in which R.sup.13 is hydrogen or lower alkyl, and either R.sup.6 ' is hydrogen or lower alkyl and R.sup.7 ' is lower alkyl or R.sup.6 ' and R.sup.7 ' together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula > N-R.sup.13 ', in which R.sup.13 ' is lower alkyl, with the proviso that R.sup.4 is the group R.sup.6 ' R.sup.7 ' N--CO--NH--CH(R.sup.8)-- when A is the group (c),and pharmaceutically acceptable acid addition salts thereof.The compounds exhibit aldosterone-antagonistic properties and are suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.

    摘要翻译： 呈现下式的苯并二氮杂衍生物其中A是下列基团：R 1是低级烷基，R 2和R 3各自是氢或低级烷基，R 4是基团 + TR R5是氢或卤素，R8是氢或低级烷基，R9是低级烷基或低级烷氧基烷基，R10是低级烷基，R11是氢，低级烷基或低级羟烷基，R12是氢或低级烷基，R14是低级烷基或芳基， 并且R 6是氢或低级烷基，且R 7是低级烷基或低级羟基烷基，或者R 6和R 7与氮原子一起是3-至7-元杂环，当它至少为5元时，它可以含有一个环 成员为氧或硫原子或式> N-R13的基团，其中R13为氢或低级烷基，R6'为氢或低级烷基，R7'为低级烷基或R6'和R7'以及 氮原子是3-至7-元杂环，当其为至少5元时，其可以含有作为环成员的氧 或硫原子或式“N-R13”的基团，其中R13'为低级烷基，条件是R4为R6'R7'N-CO-NH-CH（R8） - 当A为 （c）组及其药学上可接受的酸加成盐。 该化合物显示醛固酮拮抗性质，适用于控制或预防心力衰竭，肝腹水，原发性醛固酮增多症和特发性高血压。

    7-Isocyanato-1,4-benzodiazepin-2-ones
    47.
    发明授权
    7-Isocyanato-1,4-benzodiazepin-2-ones 失效
    7-异氰酸基-1,4-苯并二氮杂-2-酮

    公开(公告)号：US4294758A

    公开(公告)日：1981-10-13

    申请号：US186094

    申请日：1980-09-11

    申请人： Albert E. Fischli ,  Andre Szente

    发明人： Albert E. Fischli ,  Andre Szente

    IPC分类号： C07D243/24 ,  C07D243/26 ,  C07D243/28

    CPC分类号： C07D243/24

    摘要： This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula ##STR2## in which R.sup.7 represents a hydrogen atom or a lower alkyl group, and pharmaceutically acceptable acid addition salts thereof, which possess aldosterone-antagonistic properties and are accordingly suitable for the control or prevention of heart failure, of hepatic ascites, of primary aldosteronism and of idiopathic hypertension. Some of these compounds and salts also inhibit the intestinal resorption of cholesterol and are according suitable for the prevention or control of atherosclerosis. Also provided are a process for the manufacture of the above end products and novel intermediates therefor.

    摘要翻译： 本发明提供通式为“IMAGE”的苯并二氮杂衍生物，其中R 1表示低级烷基，R 2表示氢原子或低级烷基，R 3表示卤素原子，R 4表示氢或卤原子，R 5表示氢 原子或低级烷基，R6表示低级烷基，低级羟烷基或低级酰氧基烷基或R5表示氢原子，R6表示芳基或低级芳烷基或R5和R6与它们所连接的氮原子一起代表 3元至7元杂环，当其为至少5元时，可以含有作为环成员的氧或硫原子或其中R 7表示氢原子或式 基团和其药学上可接受的酸加成盐，其具有醛固酮拮抗性质，因此适合于控制或预防肝脏腹水的心力衰竭，o 原发性醛固酮增多症和特发性高血压。 这些化合物和盐中的一些还抑制胆固醇的肠内吸收，并且适合于预防或控制动脉粥样硬化。 还提供了制造上述最终产品的方法及其新颖的中间体。