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    Substituted n-[(pyridyl)alkyl]aryl-carboxamide
    1.
    发明授权
    Substituted n-[(pyridyl)alkyl]aryl-carboxamide 失效
    取代的n - [（吡啶基）烷基]芳基 - 甲酰胺

    公开(公告)号：US4916145A

    公开(公告)日：1990-04-10

    申请号：US072386

    申请日：1987-07-10

    申请人： Jefferson W. Tilley ,  Robert W. Guthrie ,  John W. Clader ,  Ronald A. LeMahieu

    发明人： Jefferson W. Tilley ,  Robert W. Guthrie ,  John W. Clader ,  Ronald A. LeMahieu

    IPC分类号： C07D213/40 ,  C07D401/06

    CPC分类号： C07D213/40 ,  C07D401/06

    摘要： The invention relates to compounds of the formula ##STR1## wherein *B is ##STR2## Y is O or S, *A is *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, provided that when m is 1, then n must be at least 1, X is O or S, R.sub.1 and R.sub.4, independently, are hydrogen, lower alkyl, hydroxy or lower alkoxy, provided that when *B is other than ##STR3## at least one of R.sub.1 and R.sub.4, and one of R.sub.6 and R.sub.7 must be hydrogen, R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl, cycloalkyl, halogen, nitro, lower alkoxy, lower alkenyl, lower alkynyl or aryl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, and pharmaceutical acceptable acid addition salts thereof.The compounds of formula I exhibit activity as Platelet Activating Factor (PAF) antagonists and are, therefore, useful as agents for the prevention and treatment of vascular diseases, pulmonary diseases, dermatological disorders, transplant rejection, immunological disorders and inflammatory conditions.

    摘要翻译： 本发明涉及下式化合物其中* B为Y或O，S为* - （CH 2）n - （X）m - （CH 2）r - ，n或r， 如果m为1，则n必须至少为1，X为O或S，R 1和R 4独立地为氢，低级烷基 ，羟基或低级烷氧基，条件是当* B不是R 1和R 4中的至少一个时，R 6和R 7中的一个必须是氢，R 2和R 3独立地是氢，低级烷基，环烷基，卤素，硝基 低级烷氧基，低级烯基，低级炔基或芳基，R5和R6独立地是氢或低级烷基，R7是氢，低级烷基，环烷基或芳基，Het是单环5-或6-元杂芳族或双环杂芳族 含有一个或两个选自氮氧和硫的杂原子的基团，该基团可以被低级烷基，卤素或芳基取代，并且星号表示连接点，当R6和R7为dif时 其对映异构体和外消旋混合物，及其药学上可接受的酸加成盐。 式I化合物表现出作为血小板活化因子（PAF）拮抗剂的活性，因此可用作预防和治疗血管疾病，肺部疾病，皮肤病学疾病，移植排斥反应，免疫学障碍和炎性病症的药剂。

    Pyridine compounds which are useful in treating a disease state characterized by an excess of platelet activating factors
    3.
    发明授权
    Pyridine compounds which are useful in treating a disease state characterized by an excess of platelet activating factors 失效
    可用于治疗以血小板活化因子过量为特征的疾病状态的吡啶化合物

    公开(公告)号：US4927838A

    公开(公告)日：1990-05-22

    申请号：US215464

    申请日：1988-07-05

    申请人： Robert W. Guthrie ,  Richard W. Kierstead ,  John G. Mullin ,  Jefferson W. Tilley

    发明人： Robert W. Guthrie ,  Richard W. Kierstead ,  John G. Mullin ,  Jefferson W. Tilley

    IPC分类号： C07D213/38 ,  C07D213/40 ,  C07D239/26 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D213/40 ,  C07D213/38 ,  C07D239/26 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： The invention relates to compounds of the formula ##STR1## wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH.sub.2).sub.n --(X).sub.s --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R.sub.1 and R.sub.2, independently, are lower alkyl, lower alkenyl or aryl, or one of R.sub.1 or R.sub.2 is hydrogen and the other is ##STR2## wherein W is ##STR3## --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, O, S, or ##STR4## and X.sub.1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X.sub.2, X.sub.3 and X.sub.4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R.sub.3 is hydrogen, lower alkyl or aryl, R.sub.4 is hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl, R.sub.5 is hydrogen or lower alkyl,R.sub.6 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 6-membered heteroaromatic radical containing one or two nitrogen atoms, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.5 and R.sub.6 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 本发明涉及下式化合物其中Y和Y'为氢或一起为O或S，* A为对亚苯基或* - （CH2）n-（X）s-（CH2）r- - ，X为O，S或-CH = CH-，n或r独立地为0至3的整数，m为0至1的整数，s为0至1的整数，条件是当s为 1，n + m必须至少为2，t为0至10的整数，R1和R2独立地为低级烷基，低级烯基或芳基，或者R1或R2中的一个为氢，另一个为氢; 其中W是-CH 2 -CH 2 - ， - CH 2 - ，O，S或者X，且X 1是低级烷基，未被取代的或被低级烷氧基，低级烷基或卤素单取代或二取代或三取代的苯基，和 X2，X3和X4独立地是氢，低级烷基，低级烷氧基或卤素，R3是氢，低级烷基或芳基，R4是氢，低级烷基，芳基，芳基 - 低级烷基或酰基，R5是氢或低级烷基 ，R6是氢，低级烷基，环烷基，低级 - 低级烷基或芳基，Het是单环6元杂芳族 含有一个或两个氮原子的基团，该基团可以被低级烷基，卤素或芳基取代，星号表示连接点，当R 5和R 6不同时，其R 1和R 2是它们的对映体和外消旋混合物 不同的，它们的几何异构体及其药学上可接受的酸加成盐。

    Cyclopropylpropenamides
    4.
    发明授权
    Cyclopropylpropenamides 失效
    环丙基丙烯酰胺

    公开(公告)号：US4786646A

    公开(公告)日：1988-11-22

    申请号：US72390

    申请日：1987-07-10

    申请人： Robert W. Guthrie ,  Richard W. Kierstead ,  Jefferson W. Tilley

    发明人： Robert W. Guthrie ,  Richard W. Kierstead ,  Jefferson W. Tilley

    IPC分类号： C07D207/32 ,  C07D207/335 ,  C07D213/40 ,  C07D233/54 ,  C07D237/08 ,  C07D239/26 ,  C07D277/28 ,  C07D307/52 ,  C07D311/58 ,  C07D333/20 ,  A61K31/44 ,  C07D413/00

    CPC分类号： C07D207/335 ,  C07D213/40 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D277/28 ,  C07D307/52 ,  C07D311/58 ,  C07D333/20

    摘要： The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and their enantiomers, diastereomers and racemic mixtures thereof, as well as when *E is ##STR3## their geometric isomers, and pharmaceutically acceptable acid addition salts thereof.The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.

    摘要翻译： 本发明涉及下式化合物：Y是O或S，* A是对亚苯基或* - （CH 2）n - （X）m - （CH 2）r - ，X是O，S或-CH = CH - ，n或r独立地为0至3的整数，s是0至1的整数，m是0至1的整数，条件是当m为1时，n + s必须至少为2，R 1 且R 2独立地为氢，低级烷基，环烷基，低级烯基，Het或芳基，* E为或（ - ）（CH 2）k - ，其中k为0至4的整数，R 3，R 4和R 8独立地为 氢或低级烷基，R5和R6独立地是氢或低级烷基，R7是氢，低级烷基，环烷基，低级 - 低级烷基或芳基，Het是单环5-或6-元杂芳族或双环杂芳族基，其含有 一个或两个选自氮，氧和硫的杂原子，该基团可以被低级烷基，卤素或芳基取代，星号表示连接点，以及它们的对映异构体，非对映异构体和外消旋混合物，以及当* E 它们的几何异构体及其药学上可接受的酸加成盐。 式I化合物表现出作为血小板活化因子（PAF）拮抗剂的活性，因此可用于以过量血小板活化因子为特征的疾病状态或用于预防和治疗心血管疾病，肺部疾病，免疫学疾病，炎性疾病，皮肤病学 疾病，休克或移植排斥。

    Pentadieneamide compounds which have useful activity of treating a disease characterized by an excess of platelet activating factor
    9.
    发明授权
    Pentadieneamide compounds which have useful activity of treating a disease characterized by an excess of platelet activating factor 失效
    具有治疗以过量血小板活化因子为特征的疾病的有用活性的戊二酰胺化合物

    公开(公告)号：US4975438A

    公开(公告)日：1990-12-04

    申请号：US241174

    申请日：1988-09-06

    申请人： Robert W. Guthrie ,  Richard W. Kierstead ,  Jefferson W. Tilley

    发明人： Robert W. Guthrie ,  Richard W. Kierstead ,  Jefferson W. Tilley

    IPC分类号： C07D213/56 ,  C07D217/02 ,  C07D217/16 ,  C07D409/12

    CPC分类号： C07D409/12 ,  C07D213/56 ,  C07D217/02 ,  C07D217/16

    摘要： Compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, Aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described.The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.

    摘要翻译： 式IY的化合物是O或S，* A是对亚苯基或* - （CH 2）n - （X）m - （CH 2）r - ，X是O，S或-CH = CH-，n或 r独立地为0至3的整数，s为0至1的整数，m为0至1的整数，条件是当m为1时，n + s必须至少为2，R1和R2独立地为 是氢，低级烷基，环烷基，低级烯基，Het，芳基，R3，R4和R8独立地是氢，低级烷基，芳基，R5和R6独立地是氢或低级烷基，R7是氢，低级烷基 ，环烷基，Het-低级烷基或芳基，Het是含有一个或两个选自氮，氧和硫的杂原子的单环5或6元杂芳族或双环杂芳族基团，该基团可被低级烷基取代， 卤素或芳基，星号表示连接点，当R 6和R 7不同时，当R 1和R 2不同时，它们的对映异构体和外消旋混合物，它们的几何异构体和药学上可接受的 其酸加成盐。 式I化合物表现出作为血小板活化因子（PAF）拮抗剂的活性，因此可用于以过量血小板活化因子为特征的疾病状态或用于预防和治疗心血管疾病，肺部疾病，免疫学疾病，炎性疾病，皮肤病学 疾病，休克或移植排斥。

    Cycloproylpropenamides useful as platelet activing factor (PAF) antagonists
    10.
    发明授权
    Cycloproylpropenamides useful as platelet activing factor (PAF) antagonists 失效
    可用作血小板激活因子（PAF）拮抗剂的环丙基丙酰胺

    公开(公告)号：US4927826A

    公开(公告)日：1990-05-22

    申请号：US238224

    申请日：1988-08-30

    申请人： Robert W. Guthrie ,  Richard W. Kierstead ,  Jefferson W. Tilley

    发明人： Robert W. Guthrie ,  Richard W. Kierstead ,  Jefferson W. Tilley

    IPC分类号： C07D207/32 ,  C07D207/335 ,  C07D213/40 ,  C07D233/54 ,  C07D237/08 ,  C07D239/26 ,  C07D277/28 ,  C07D307/52 ,  C07D311/58 ,  C07D333/20

    CPC分类号： C07D207/335 ,  C07D213/40 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D277/28 ,  C07D307/52 ,  C07D311/58 ,  C07D333/20

    摘要： The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl. Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer fro 0 to 4. R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and their enantiomers, diastereomers and racemic mixtures thereof, as well as when *E is ##STR3## their geometric isomers and pharmaceutically acceptable acid addition salts thereof.The compounds of formula 1 exhibit activity as paltelet activiating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.

    摘要翻译： 本发明涉及下式化合物：Y是O或S，* A是对亚苯基或* - （CH 2）n - （X）m - （CH 2）r - ，X是O，S或-CH = CH + 13，n或r独立地为0〜3的整数，s为0〜1的整数，m为0〜1的整数，条件是当m为1时，n + s必须至少为2， R1和R2独立地是氢，低级烷基，环烷基，低级烯基。 Het或芳基，* E为<或>（ - ）（CH 2）k - 其中k为0至4的整数.R 3，R 4和R 8独立地为氢或低级烷基，R 5和R 6独立地为氢或低级烷基， R7是氢，低级烷基，环烷基，低级 - 低级烷基或芳基，Het是含有一个或两个选自氮，氧和硫的杂原子的单环五元或六元杂芳族或双环杂芳族基，该基可以 被低级烷基，卤素或芳基取代，星号表示连接点，以及它们的对映异构体，非对映异构体和外消旋混合物，以及当* E是它们的几何异构体及其药学上可接受的酸加成盐时。 式1的化合物显示作为paletlet活化因子（PAF）拮抗剂的活性，因此可用于以过量血小板活化因子为特征的疾病状态或用于预防和治疗心血管疾病，肺部疾病，免疫学疾病，炎性疾病，皮肤病学 疾病，休克或移植排斥。