利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

29 条记录 (耗时 0.016 秒)

    Preparation of difficol
    1.
    发明公开
    Preparation of difficol 失效
    生产Difficol的。

    公开(公告)号：EP0190658A1

    公开(公告)日：1986-08-13

    申请号：EP86101175.7

    申请日：1986-01-29

    申请人： Merck & Co., Inc.

    发明人： Thorsett, Eugene D. ,  Williamson, Joanne M. ,  Wilson, Kenneth E.

    IPC分类号： C07D313/00 ,  C12P17/08 ,  C12P1/04

    CPC分类号： C12R1/125 ,  C07D313/00 ,  C07F9/65525 ,  C12P17/08

    摘要： The subject disclosure discloses a chemical intermediate in antibiotic synthesis of the structure:
    wherein

    R, is H or OH and the asterisks indicate asymmetric carbon atoms. Compounds of this type may be obtained by fermentation with a strain of B. subtilis under aerobic conditions. Compounds of the above structure are biologically inactive but are converted by phosphorylation of the hydroxyl group to produce compounds of the structure: wherein
    R 1 is H or OH, which are useful antibacterial substances having a broad spectrum of antibacterial activity.

    Bicyclic lactams as antihypertensives
    2.
    发明公开
    Bicyclic lactams as antihypertensives 失效
    双环内酰胺作为抗高血压药。

    公开(公告)号：EP0061187A1

    公开(公告)日：1982-09-29

    申请号：EP82102330.6

    申请日：1982-03-22

    申请人： Merck & Co., Inc.

    发明人： Harris, Elbert E. ,  Patchett, Arthur A. ,  Tristram, Edward W. ,  Thorsett, Eugene D. ,  Wyvratt, Matthew J., Jr.

    IPC分类号： C07D513/04 ,  A61K31/425

    CPC分类号： C07D209/48 ,  A61K38/00 ,  C07D513/04 ,  C07K5/0222

    摘要： The invention relates to bicyclic lactams and related compounds of the formula:
    wherein:

    R and R 2 are hydrogen, loweralkyl, aryl, and aralkyl;
    R, is hydrogen, alkyl; substituted lower alkyl; substituted lower alkyl having the formula R A (CH 2 )-Q-I(CH 2 ) m wherein n is 0-2, m is 1-3, R A is optionally substituted aryl or optionally substi tuted heteroaryl and 0 is 0, S, N R B , CONR C . NR C CO, CH=CH wherein R B is hydrogen, lower alkyl, aryl, aralkyl, lower alkanoyl, or aroyl, and R C is hydrogen or lower alkyl; aryl; substituted aryl; substituted aralkyl; or substituted heteroaralkyl; and the pharmaceutically acceptable salts thereof, and to a process for preparing those compounds. The compounds are useful as antihypertensives.

    Substituted caprolactam derivatives, a process for preparing and a pharmaceutical composition containing the same, and intermediates
    3.
    发明公开
    Substituted caprolactam derivatives, a process for preparing and a pharmaceutical composition containing the same, and intermediates 失效
    取代的捕获剂衍生物，制备方法和含有其的药物组合物和中间体

    公开(公告)号：EP0049505A3

    公开(公告)日：1982-08-04

    申请号：EP81107933

    申请日：1981-10-05

    申请人： MERCK & CO. INC.

    发明人： Harris, Elbert E. ,  Thorsett, Eugene D.

    IPC分类号： C07D223/10 ,  A61K31/55

    CPC分类号： C07D223/10

    摘要： Substituted caprolactam derivatives are disclosed which are useful as converting enzyme inhibitors and as antihypertensives, and a process for preparing them. Those compounds are represented by the formula
    wherein
    R 1 is hydrogen, loweralkyl, cyclic loweralkyl, amino loweralkyl, alkylamino loweralkyl, hydroxyalkyl, acylamino loweralkyl, dialkylamino loweralkyl including cyclic polyethyleneamino loweralkyl, arloweralkyl, aryl, substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy; heteroaryl, heteroarloweralkyl; R 2 is hydrogen or loweralkyl; R 3 is hydroxyl, loweralkoxy, or aralkyloxy; R 4 is hydrogen or loweralkanoyl.

    Substituted caprolactam derivatives as antihypertensives, process for preparing them, pharmaceutical composition containing them, and intermediates
    4.
    发明公开
    Substituted caprolactam derivatives as antihypertensives, process for preparing them, pharmaceutical composition containing them, and intermediates 失效
    取代的己内酰胺衍生物作为抗高血压剂，它们的制备方法，含有所述化合物和中间体的药物组合物。

    公开(公告)号：EP0046291A2

    公开(公告)日：1982-02-24

    申请号：EP81106372.6

    申请日：1981-08-17

    申请人： Merck & Co., Inc.

    发明人： Harris, Elbert E. ,  Patchett, Arthur A. ,  Thorsett, Eugene D.

    IPC分类号： C07K5/06 ,  A61K37/02

    CPC分类号： C07K5/06139 ,  A61K38/00 ,  C07K5/0222

    摘要： The invention retates to caprolactam derivatives of the formula
    wherein

    R and R are hydroxy, lower alkoxy, lower alkenoxy. aryloxy, difoweralkylamino lower alkoxy, acylamino lower alkoxy, acyloxy lower alkoxy arloweralkoxy. hydroxy lower all oxy. dihydroxy lower alkoxy, amino, hydroxyamino;
    R is hydrogen. alkyl of from 1 to 12 carbon atoms substituted loweralkyl, arloweralkyl, arloweralkenyl, heteroarlower alkyl or heteroarlower alkenyl, substituted arloweralkyl or substituted heteroarlower alkyl;
    R 2 is hydrogen, lower alkyl, cyclic lower alkyl, amino, aminolower alkyl, alkylaminoloweralkyl, hydroxyalkyl, acylaminoloweralkyl, dialkylaminoloweralkyl, arlower alkyl, aryl, substituted aryl, heteroaryl, heteroarlower alkyl;
    R 3 is hydrogen, lower alkyl, phenyl, phenyl lower alkyl, hydroxyphenyl lower alkyl, hydroxy lower alkyl, amino lower alkyl, acylamino lower aikyl, guanidino lower alkyl, imidazolyl lower alkyl, indolyl lower alkyl, mercapto lower alkyl or lower alkyl thio lower alkyl; and
    R 3 is hydrogen or lower alkyl.

    These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives. The invention relates also to a process for preparing these compounds.

    摘要翻译： 本发明涉及下式的己内酰胺衍生物： worin R 7和R <4>是羟基，低级烷氧基，低级链烯氧基，芳氧基，二低级烷氨基低级烷氧基，酰基氨基低级烷氧基，酰氧基低级烷氧基，arloweralkoxy，羟基低级烷氧基， 二羟基低级烷氧基，氨基，羟氨基; R 2是氢，具有1至12个碳原子substituiertem低级烷基，arloweralkyl，arloweralkenyl，heteroarlower烷基或链烯基heteroarlower的烷基，取代或arloweralkyl substituiertem heteroarlower烷基; [R <2>是氢，低级烷基，环状低级烷基，氨基，烷基aminolower，alkylaminoloweralkyl，羟烷基，acylaminoloweralkyl，dialkylaminoloweralkyl，arlower烷基，芳基，芳基substituiertem，杂芳基，heteroarlower烷基; ř氢<3>是，低级烷基，苯基，苯基低级烷基，羟基苯基低级烷基，羟基低级烷基，氨基低级烷基，酰氨基低级烷基，胍基的低级烷基，咪唑基低级烷基，吲哚基的低级烷基，巯基低级烷基或低级烷基 硫代低级烷基; 和R是氢或低级烷基。 这些化合物可用作血管紧张素转换酶抑制剂和用作抗高血压药是有用的。 因此，本发明涉及用于制备化合物论文的方法。

    Substituted phosphonamides, a process for preparing the same and a pharmaceutical composition which is useful in the treatment of hypertension
    6.
    发明公开
    Substituted phosphonamides, a process for preparing the same and a pharmaceutical composition which is useful in the treatment of hypertension 失效
    取代的磷酸酯，其制备方法和可用于治疗高血压的药物组合物

    公开(公告)号：EP0058427A3

    公开(公告)日：1983-10-05

    申请号：EP82101134

    申请日：1982-02-16

    申请人： MERCK & CO. INC.

    发明人： Greenlee, William J. ,  Patchett, Arthur A. ,  Harris, Elbert E. ,  Thorsett, Eugene D.

    IPC分类号： C07F09/65 ,  A61K31/675

    CPC分类号： C07K5/06191 ,  A61K38/00 ,  C07F9/5721 ,  C07F9/6539

    摘要： There are disclosed substituted phosphonamides and related compounds of the general formula
    wherein:
    R, is alkyl or substituted alkyl of C 1 -C 6 wherein the substituent is halo, amino, acylamino; aralkyl wherein the alkyl is C 1 -C 4 optionally substituted by amino or acylamino and wherein the aryl function is phenyl or naphthyl optionally substituted by halo or hydroxyl; or, heteroaralkyl wherein the alkyl is C 1 -C 4 optionally substituted by amino or acylamino and wherein the heteroaryl group can be indolyl or thienyl; R 2 is H, lower alkyl of C 1 -C 4 , aralkyl. R 3 is lower alkyl of C 1 -C 6 optionally substituted by an amino group; R 4 is H, lower alkyl of C 1 -C 6 , aralkyl. X is (CH 2 ) n wherein n is 1 or 2, CH-OCH 3 , CH-OH, or S; and,
    the pharmaceutically acceptable salts thereof. THese compounds are useful as converting enzyme inhibitors and as antihypertensives.

    摘要翻译： 公开了可用作转化酶抑制剂和抗高血压药物的取代膦酰胺和相关化合物。

    Substituted enantholactam derivatives, a process for the preparation and a pharmaceutical composition useful in the treatment of hypertension comprising the same, and intermediates
    7.
    发明公开
    Substituted enantholactam derivatives, a process for the preparation and a pharmaceutical composition useful in the treatment of hypertension comprising the same, and intermediates 失效
    庚取代的衍生物，它们的制备方法和药物组合物的方法含有它们，用于对抗高血压和中间体的用途。

    公开(公告)号：EP0049842A2

    公开(公告)日：1982-04-21

    申请号：EP81107932.6

    申请日：1981-10-05

    申请人： Merck & Co., Inc.

    发明人： Harris, Elbert E. ,  Taub, David ,  Thorsett, Eugene D.

    IPC分类号： C07D225/02 ,  A61K31/395

    CPC分类号： C07D225/02

    摘要： Substituted enantholactam dipeptides and derivatives thereof and a process for preparing them are disclosed. Those comnounds have the formula
    in which

    R' ishydrogen, lower alkyl, cycloalkyl, aminoalkyl, hydroxyalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, heterocycloalkyl, or substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy;
    R 2 ishydrogen, lower alkyl, aminolower alkyl, indolyl lower alkyl or phenyl lower alkyl;
    R 3 ishydroxy, lower alkoxy or aralkoxy;
    R 4 ishydrogen or lower alkanoyl;
    R 5 is hydrogen or lower alkyl.

    The compounds are useful as derivating enzyme inhibitors and as antihypertensives.

    摘要翻译： 取代的二肽庚及其衍生物和用于制备它们的方法是游离缺失盘。 这些化合物具有下式其中R <1>是氢，低级烷基，环烷基，氨基烷基，羟基烷基，芳基，杂芳基，芳烷基，杂芳烷基，杂环烷基，或substituiertem芳worin的取代基是卤素，烷基，氨基烷基，或 烷氧基; [R <2>是氢，低级烷基，烷基aminolower，吲哚基低级烷基或苯基低级烷基; [R <3>是羟基，低级烷氧基或芳烷氧基; [R <4>是氢或低级烷酰基; [R <5>是氢或低级烷基。 所述化合物可用作求导酶抑制剂和作为抗高血压