Disubstituted 4-hydroxyphenylthio anilides
    1.
    发明授权
    Disubstituted 4-hydroxyphenylthio anilides 失效
    二取代的4-羟基苯基硫代酰苯胺

    公开(公告)号:US5225444A

    公开(公告)日:1993-07-06

    申请号:US750810

    申请日:1991-08-27

    IPC分类号: C07C317/44

    CPC分类号: C07C317/44

    摘要: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.

    摘要翻译: 本发明的化合物是由下式表示的酰苯胺:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基和基团组成的组中相同或不同的成员,其中n,m和p是 独立地为1〜8的整数,条件是n + m + p等于或小于10; X是硫基,亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R3是氢或低级烷基; 并且R 4是苯基或取代的苯基。 本发明的化合物可用于治疗炎症,过敏和超敏反应以及免疫系统的其它病症。

    Novel disubstituted 4-hydroxyphenylthio anilides
    2.
    发明授权
    Novel disubstituted 4-hydroxyphenylthio anilides 失效
    新型二取代的4-羟基苯基硫代酰苯胺

    公开(公告)号:US5071876A

    公开(公告)日:1991-12-10

    申请号:US558965

    申请日:1990-07-27

    IPC分类号: C07C317/44

    摘要: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.

    摘要翻译: 本发明的化合物是由下式表示的酰苯胺:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基和基团组成的组中相同或不同的成员,其中n,m和p是 独立地为1〜8的整数,条件是n + m + p等于或小于10; X是硫基,亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R3是氢或低级烷基; 并且R 4是苯基或取代的苯基。 本发明的化合物可用于治疗炎症,过敏和超敏反应以及免疫系统的其它病症。

    Azabicycloalkyl and azatricycloalkyl amides
    3.
    发明授权
    Azabicycloalkyl and azatricycloalkyl amides 失效
    偶氮二环烷基和氮杂环烷基酰胺

    公开(公告)号:US5198435A

    公开(公告)日:1993-03-30

    申请号:US669543

    申请日:1991-03-14

    IPC分类号: C07D295/185 C07D453/02

    CPC分类号: C07D295/185 C07D453/02

    摘要: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided than n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.

    摘要翻译: 本发明的化合物是由下式表示的双环,三环,氮杂双环和氮杂三环酰胺:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基组成的组中相同或不同的成员 其中n,m和p独立地为n + m + p等于或小于10提供的1至8的整数; x是硫代,亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R 3选自二环烷基氨基,三环烷基氨基,氮杂双环烷基,氮杂环烷基,氮杂双环烷基氨基,氮杂三环烷基氨基或二环烷基氨基。 该化合物可用作抗炎和抗过敏剂。

    Bicycloalky, tricycloalkyl, azabicycloalkyl, and azatricycloalkyl thio
amides used to treat inflammation, allergy, asthma and skin disorders
    4.
    发明授权
    Bicycloalky, tricycloalkyl, azabicycloalkyl, and azatricycloalkyl thio amides used to treat inflammation, allergy, asthma and skin disorders 失效
    用于治疗炎症,过敏,哮喘和皮肤疾病的双环烷基,三环烷基,氮杂双环烷基和氮杂三环烷基硫代酰胺

    公开(公告)号:US5157053A

    公开(公告)日:1992-10-20

    申请号:US600342

    申请日:1990-10-19

    IPC分类号: C07D295/185 C07D453/02

    摘要: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group-consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, aszabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino, The compounds are useful as anti-inflammatory and anti-allergy agents.

    摘要翻译: 本发明的化合物是由下式表示的双环,三环,氮杂双环和氮杂三环酰胺:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基组成的组中相同或不同的成员 其中n,m和p独立地为1至8的整数,条件是n + m + p等于或小于10; x是硫代,亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R3选自二环烷基氨基,三环烷基氨基,氮杂双环烷基,氮杂环烷基,二氮杂环烷基氨基,氮杂环烷基氨基或二环烷基氨基。该化合物可用作抗炎和抗过敏剂。

    Azabicycloalkyl and azatricycloalkyl amides used to treat inflammation,
allergy, asthma and skin disorders
    6.
    发明授权
    Azabicycloalkyl and azatricycloalkyl amides used to treat inflammation, allergy, asthma and skin disorders 失效
    用于治疗炎症,过敏,哮喘和皮肤疾病的氮杂双环烷基和氮杂三环烷基酰胺

    公开(公告)号:US5244899A

    公开(公告)日:1993-09-14

    申请号:US921876

    申请日:1992-07-29

    IPC分类号: C07D295/185 C07D453/02

    摘要: The compounds of this invention are azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.

    摘要翻译: 本发明的化合物是由下式表示的氮杂双环和氮杂三环酰胺:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基组成的组中相同或不同的成员,其中n,m 并且p独立地为1〜8的整数,条件是n + m + p等于或小于10; X是硫基,亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R3选自氮杂双环烷基氨基,氮杂环烷基氨基或二环烷基氨基。 该化合物可用作抗炎和抗过敏剂。

    Phenolic thioethers as inhibitors of 5-lipoxygenase
    7.
    发明授权
    Phenolic thioethers as inhibitors of 5-lipoxygenase 失效
    酚硫醚作为5-脂氧合酶的抑制剂

    公开(公告)号:US4711903A

    公开(公告)日:1987-12-08

    申请号:US824984

    申请日:1986-01-31

    摘要: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R.sub.3 represents CO.sub.2 H, CO.sub.2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; amd the pharmaceutically acceptable salts thereof. The compounds of the present invention are specific inhibitors of 5-lipoxygenase and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.

    摘要翻译: 本发明的化合物包括由下式表示的取代的酚类硫醚:其中:R 1和R 2相同或不同并且独立地代表叔烷基或苯基; A表示亚烷基或被烷基,二烷基或羟基取代的亚甲基,条件是当A包括羟基亚甲基时,羟基亚甲基不与杂原子相邻; 苯基,苄基,取代的苯基或取代的苄基取代的硫,亚砜,砜,氧,-NH-或氮。 C表示亚烷基或被烷基取代的亚甲基; R3表示CO 2 H,CO 2 - 烷基或四唑基; m为0或1,n为2,3或4,p为1,2或3; 其药学上可接受的盐。 本发明的化合物是5-脂氧合酶的特异性抑制剂,因此可用于治疗局部和全身炎症,变态反应和过敏反应以及涉及5-脂氧合酶代谢途径中形成的药物的其它病症。

    Bicycloalkyl tricycloalkyl, azabicycloalkyl and azatricycoalkyl amides
    8.
    发明授权
    Bicycloalkyl tricycloalkyl, azabicycloalkyl and azatricycoalkyl amides 失效
    双环烷基三环烷基,氮杂双环烷基和吖嗪基烷基酰胺

    公开(公告)号:US5019597A

    公开(公告)日:1991-05-28

    申请号:US79731

    申请日:1987-07-30

    CPC分类号: C07D295/185 C07D453/02

    摘要: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.

    摘要翻译: 本发明的化合物是由下式表示的双环,三环,氮杂双环和氮杂三环酰胺:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基组成的组中相同或不同的成员 其中n,m和p独立地为1至8的整数,条件是n + m + p等于或小于10; X是硫基,亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R 3选自二环烷基氨基,三环烷基氨基,氮杂双环烷基,氮杂环烷基,氮杂双环烷基氨基,氮杂三环烷基氨基或二环烷基氨基。 该化合物可用作抗炎和抗过敏剂。

    Acylaminoalkylpyridines ad use in treatment of inflammation and allergy
reactions
    9.
    发明授权
    Acylaminoalkylpyridines ad use in treatment of inflammation and allergy reactions 失效
    酰氨基烷基吡啶广泛用于治疗炎症和过敏反应

    公开(公告)号:US4663333A

    公开(公告)日:1987-05-05

    申请号:US809955

    申请日:1985-12-20

    CPC分类号: C07D213/40

    摘要: The compounds of this invention are acylaminoalkylpyridines representd by the formula ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk.sub.1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R.sub.3 is lower alkyl, Alk.sub.2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R.sub.4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; and the pharmaceutically acceptable salts thereof. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.

    摘要翻译: 本发明的化合物是由下式表示的酰基氨基烷基吡啶:其中:R 1和R 2是由卤素,苯基,取代的苯基和取代的苯基组成的组中相同或不同的成员,其中n,m和p独立地为 n + m + p的1〜8的整数等于或小于10; X是硫基,亚磺酰基或磺酰基; Alk1是1至6个碳原子的直链或支链低级亚烷基,R3是低级烷基,Alk2是1至4个碳原子的直链或支链亚烷基; R 4选自氢,卤素,羟基,低级烷基和低级烷氧基; 及其药学上可接受的盐。 本发明的化合物可用于治疗炎症,过敏和超敏反应以及免疫系统的其它病症。

    Cyclic phenolic thioethers
    10.
    发明授权
    Cyclic phenolic thioethers 失效
    环状酚类硫醚

    公开(公告)号:US5393764A

    公开(公告)日:1995-02-28

    申请号:US107821

    申请日:1993-08-25

    摘要: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof. The compounds of the present invention are inhibitors of 5-lipoxygenase.

    摘要翻译: PCT No.PCT / US92 / 03569。 371日期:1993年8月25日 102(e)日期1993年8月25日PCT提交1992年5月5日PCT公布。 WO92 / 19608 PCT出版物 本发明的化合物包括由式(I)表示的取代的酚类硫醚,其中:R 1和R 2相同或不同并且独立地代表叔烷基或苯基; R3表示氢或烷基; X表示 - (CH 2)w B-(CH 2)y - ,其中B表示O,S或CH 2,w和y各自独立地为0至3的整数,条件是w + y的和等于或 小于3; A表示O或S(O)n,其中n为0,1或2; p是1至4的整数; 和R表示烷基; 哦; OR4,其中R4是1-4个碳原子的烷基; NR5R6其中R5是氢或烷基,R6是氢,烷基,杂环烷基,其中杂环可以被任选取代; 环烷基 取代的环烷基; 苯基; 取代的苯基; 苯基烷基; 或取代的苯基烷基; 或NR5R6一起形成可任选被取代的杂环; 或R为(CH 2)t COOR 7,其中t为1至4的整数,且R 7为氢或1至4个碳原子的烷基; 及其药学上可接受的盐和立体异构体或几何异构体。 本发明的化合物是5-脂氧合酶的抑制剂。