Certain aurones and their use in the treatment of allergies
    1.
    发明授权
    Certain aurones and their use in the treatment of allergies 失效
    某些ones ones及其用于治疗过敏症

    公开(公告)号:US4532257A

    公开(公告)日:1985-07-30

    申请号:US556473

    申请日:1983-11-30

    IPC分类号: C07D307/83 A61K31/34

    CPC分类号: C07D307/83

    摘要: There are described compounds of the formula ##STR1## in which either R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 is carboxyl and R.sup.2 is hydrogen, C.sub.3-4 alkenyl or C.sub.1-4 alkyl, and R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, nitro, hydroxyl, carboxyl, carboxyC.sub.1-2 alkoxy, C.sub.3-4 alkenyl, C.sub.1-4 alkyl, C.sub.3-4 alkenyloxy, C.sub.1-4 alkoxy or the group ##STR2## where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl; and salts and esters thereof. The compounds are indicated for use in the treatment of immediate sensitivity reactions and inflammatory diseases.

    摘要翻译: 描述了式“IMAGE”的化合物,其中R1和R2都是氢或R1是羧基,R2是氢,C3-4链烯基或C1-4烷基,R3,R4和R5各自是氢,硝基,羟基, 羧基,羧基C 1-2烷氧基,C 3-4烯基,C 1-4烷基,C 3-4烯氧基,C 1-4烷氧基或基团,其中R 6和R 7各自为氢或C 1-4烷基; 及其盐和酯。 该化合物用于治疗立即敏感反应和炎性疾病。

    Aurone derivatives
    2.
    再颁专利
    Aurone derivatives 失效
    Aurone衍生物

    公开(公告)号:USRE32196E

    公开(公告)日:1986-07-01

    申请号:US379793

    申请日:1982-05-19

    摘要: Substituted aurones of formula (I): ##STR1## wherein R.sup.1, R.sup.2 R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and can each represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkyl, optionally substituted phenyl, C.sub.1-6 haloalkyl, amido, amino, cyano, hydroxy, nitro, C.sub.2-4 alkenyl, carboxyl, tetrazol-5-yl and --CH.dbd.CHCOOH; orwherein R.sup.1 and R.sup.2 taken together can represent a group of formula --CH.dbd.CH--CH.dbd.CH-- provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is carboxyl, tetrazol-5-yl or --CH.dbd.CHCOOH;or a pharmaceutically-acceptable salt or ester thereof, are effective in the prophylactic chemotherapy of allergic conditions such as bronchial asthma.

    摘要翻译: AURONE DERIVAT IVES式(I)的取代的噢:其中R 1,R 2,R 3,R 4,R 5和R 6相同或不同并且各自表示氢,卤素,C 1-6烷基,C 1-6 烷氧基,C 3-8环烷基,任选取代的苯基,C 1-6卤代烷基,酰氨基,氨基,氰基,羟基,硝基,C 2-4烯基,羧基,四唑-5-基和-CH_CHCOOH; 或者其中R 1和R 2一起可以表示式-CH-CH-CH-CH-基团,条件是R 17,R 3,R 4,R 5和R 6中的至少一个是羧基,四唑-5-基或-CH = CICOOH; 或其药学上可接受的盐或酯在过敏性疾病例如支气管哮喘的预防性化学疗法中是有效的。

    SRS-A antagonists
    3.
    发明授权
    SRS-A antagonists 失效
    SRS-A拮抗剂

    公开(公告)号:US4513005A

    公开(公告)日:1985-04-23

    申请号:US386570

    申请日:1982-06-09

    摘要: There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.2 is(i) alkyl, cycloalkyl or alkenyl of up to 10 carbon atoms, unsubstituted or substituted by one or more substituents selected from aryl, cycloalkyl, halogen, hydroxy, NHR.sub.3 and COX, where R.sub.3 is H, C.sub.1-4 alkyl, aryl or an amino acid residue or COX, and X is OH, C.sub.1-4 alkyl, NH.sub.2 or an amino acid residue, or(ii) aryl or heteroaryl, unsubstituted or substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 acyl, halogen, hydroxy, carboxy, nitro, trihalomethyl, phenyl, C.sub.1-4 acylamino and NHR.sub.4, where R.sub.4 is hydrogen or C.sub.1-4 alkyl; and Y is --S--, --SO-- or --SO.sub.2 --,with the proviso that when --YR.sub.2 is glutathionyl, cysteinyl or cysteinylglycinyl, then R.sub.1 is other than an unsubstituted alkatetraenyl or alkapentaenyl radical of 12 to 16 carbon atoms.

    摘要翻译: 描述了用于治疗涉及SRS-A作为因果介质的过敏性/炎症性疾病,其游离酸形式为式I的化学活性化合物,其中R 1是(i)脂族, 至少20个碳原子的饱和或不饱和烃基,未被取代或被至少一个选自卤素,羟基,C 3-6烷氧基,C 3-6环烷基,芳基或杂芳基的取代基取代,环烷基,芳基或杂芳基是未取代或取代的 至少一个选自羟基,卤素和至多10个碳原子的烷基,烯基或炔基的取代基,(ii)未被取代或被至多16个碳原子的烷基,烯基或炔基取代的3至8个碳原子的环烷基,或 (iii)未被取代或被羟基,C 1-4烷氧基,卤素或至多16个碳原子的烷基,链烯基或炔基取代的芳基或杂芳基; 并且R 2是(i)至少10个碳原子的烷基,环烷基或链烯基,未被取代或被一个或多个选自芳基,环烷基,卤素,羟基,NHR 3和COX的取代基取代,其中R 3是H,C 1-4烷基, 芳基或氨基酸残基或COX,X为OH,C 1-4烷基,NH 2或氨基酸残基,或(ii)未被取代或被一个或多个选自C 1-4烷基,C 1 -4-烷氧基,C 2-5酰基,卤素,羟基,羧基,硝基,三卤甲基,苯基,C 1-4酰基氨基和NHR 4,其中R 4是氢或C 1-4烷基; 并且Y是-S-,-SO-或-SO 2 - ,条件是当-YR 2是谷胱甘肽基,半胱氨酰基或半胱氨酰甘氨酰基时,则R 1不同于未被取代的具有12至16个碳原子的烷基四烯基或烷基五烯基。

    Aurone derivatives
    4.
    发明授权
    Aurone derivatives 失效
    Aurone衍生物

    公开(公告)号:US4259340A

    公开(公告)日:1981-03-31

    申请号:US71515

    申请日:1979-08-31

    摘要: Substituted aurones of formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and can each represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkyl, optionally substituted phenyl, C.sub.1-6 haloalkyl, amido, amino, cyano, hydroxy, nitro, C.sub.2-4 alkenyl, carboxyl, tetrazol-5-yl and --CH.dbd.CHCOOH; orwherein R.sup.1 and R.sup.2 taken together can represent a group of formula --CH.dbd.CH--CH.dbd.CH-- provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is carboxyl, tetrazol-5-yl or --CH.dbd.CHCOOH;or a pharmaceutically-acceptable salt or ester thereof, are effective in the prophylactic chemotherapy of allergic conditions such as bronchial asthma.

    摘要翻译: 取代的式(I)的噢:其中R 1,R 2,R 3,R 4,R 5和R 6相同或不同,各自表示氢,卤素,C 1-6烷基,C 1-6烷氧基,C 3 -8环烷基,任选取代的苯基,C 1-6卤代烷基,酰氨基,氨基,氰基,羟基,硝基,C 2-4烯基,羧基,四唑-5-基和-CH = CHCOOH; 或者其中R 1和R 2一起可以表示式-CH = CH-CH = CH-的基团,条件是R 1,R 2,R 3,R 4,R 5和R 6中的至少一个是羧基,四唑-5-基或-CH = CHCOOH; 或其药学上可接受的盐或酯在过敏性疾病例如支气管哮喘的预防性化学疗法中是有效的。

    Sulfur containing alkenylenyl substituted benzoic acids and phenyl
tetrazoles and their use as anti-allergic agents
    8.
    发明授权
    Sulfur containing alkenylenyl substituted benzoic acids and phenyl tetrazoles and their use as anti-allergic agents 失效
    含硫烯基取代的苯甲酸和苯基四唑及其作为抗过敏剂的用途

    公开(公告)号:US4675335A

    公开(公告)日:1987-06-23

    申请号:US822703

    申请日:1986-01-27

    CPC分类号: C07D257/04 Y02P20/55

    摘要: Pharmaceutical compounds are described of the formula ##STR1## in which R.sup.1 is (i) R.sup.4 O(CH.sub.2 CH.sub.2 O).sub.n (CH.sub.2).sub.m --, where R.sup.4 is hydrogen or C.sub.1-5 alkyl, n is 0 or 1 to 5 and m is 1 to 7, or (ii) R.sup.5 --X-- where R.sup.5 is a polar group and X is a C.sub.6-20 alkylene or a C.sub.6-20 alkenylene radical containing from 1 to 3 double bonds, R.sup.2 is a group of the formula A--B-- where A is --COOH or ##STR2## where R.sup.6 is hydrogen or a protecting group, and B is C.sub.1-6 alkylene, and R.sup.3 is --COOH or ##STR3## where R.sup.7 is hydrogen or a protecting group; or a salt or ester thereof.

    摘要翻译: 药物化合物描述于其中R 1为(ⅰ)R 4 O(CH 2 CH 2 O)n(CH 2)m - ,其中R 4为氢或C 1-5烷基,n为0或1至5并且m为1至 7,或(ii)R 5 -X-,其中R 5是极性基团,X是含有1至3个双键的C 6-20亚烷基或C 6-20亚烯基,R 2是式AB-的基团,其中A 是-COOH或,其中R 6是氢或保护基,B是C 1-6亚烷基,R 3是-COOH或者R 7是氢或保护基; 或其盐或酯。