1,2,4-Triazine derivatives, and their production and use
    1.
    发明授权
    1,2,4-Triazine derivatives, and their production and use 失效
    1,2,4-三嗪衍生物及其生产和使用

    公开(公告)号:US4343801A

    公开(公告)日:1982-08-10

    申请号:US212442

    申请日:1980-12-03

    CPC分类号: C07D401/04 C07D409/14

    摘要: A compound of the formula: ##STR1## wherein Ar is a phenyl group substituted with halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, C.sub.1 -C.sub.8 alkylsulfonyl, nitro, trihalomethyl, cyano, C.sub.1 -C.sub.8 alkylamino, di(C.sub.1 -C.sub.8)-alkylamino, amino, hydroxyl, phenyl and/or phenoxy, a naphthyl group or a thienyl group optionally substituted with halogen, which is useful as an antifungal agent.

    摘要翻译: 下式的化合物,其中Ar是被卤素取代的苯基,C1-C8烷基,C1-C8烷氧基,C1-C8烷硫基,C1-C8烷基磺酰基,硝基,三卤代甲基,氰基,C1-C8烷基氨基, 二(C1-C8) - 烷基氨基,氨基,羟基,苯基和/或苯氧基,萘基或任选被卤素取代的噻吩基,其可用作抗真菌剂。

    N-Substituted imidazole derivatives, and their use
    2.
    发明授权
    N-Substituted imidazole derivatives, and their use 失效
    N-取代的咪唑衍生物及其用途

    公开(公告)号:US4288448A

    公开(公告)日:1981-09-08

    申请号:US210619

    申请日:1980-11-26

    摘要: An N-substituted imidazole compound of the formula: ##STR1## wherein R and R' are independently a phenyl group optionally substituted with one or more halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, phenyl, phenoxy, phenylthio, hydroxyl, trifluoromethyl, amino, carbamoyl, di(C.sub.1 -C.sub.8) alkylamino, C.sub.1 -C.sub.8 alkanoylamino, nitro, cyano, carboxy, C.sub.1 -C.sub.8 alkoxycarbonyl, C.sub.1 -C.sub.8 alkylsulfonyloxy or C.sub.1 -C.sub.8 alkanoylpiperazino groups; a C.sub.1 -C.sub.15 alkyl group or a phenyl (C.sub.1 -C.sub.2) alkyl group optionally bearing halogen on the benzene ring, and its acid-addition salts, which is useful as an antifungal agent.

    摘要翻译: 具有下式的N-取代的咪唑化合物:其中R和R'独立地是任选被一个或多个卤素,C 1 -C 8烷基,C 1 -C 8烷氧基,C 1 -C 8烷硫基,苯基,苯氧基, 苯基硫基,羟基,三氟甲基,氨基,氨基甲酰基,二(C1-C8)烷基氨基,C1-C8烷酰基氨基,硝基,氰基,羧基,C1-C8烷氧基羰基,C1-C8烷基磺酰氧基或C1-C8烷酰基哌嗪基; 在苯环上任选带有卤素的C 1 -C 15烷基或苯基(C 1 -C 2)烷基及其酸加成盐,其可用作抗真菌剂。

    Phenoxy carboxylic acid derivatives as anti-atheroslerosis agents
    5.
    发明授权
    Phenoxy carboxylic acid derivatives as anti-atheroslerosis agents 失效
    苯氧基羧酸衍生物作为抗动脉粥样硬化剂

    公开(公告)号:US3959484A

    公开(公告)日:1976-05-25

    申请号:US459861

    申请日:1974-04-10

    摘要: Novel anti-atheroscelersosis agents having the formula, ##SPC1##Wherein typical examples of R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.8 alkyl, phenyl, benzyl and phenethyl, or R.sup.1 and R.sup.2 may form cycloalkylidene together with a carbon atom bonded therewith; R.sup.3 and R.sup.4 each is hydrogen or C.sub.1 -C.sub.4 alkyl; Y is hydroxyl, C.sub.1 -C.sub.4 alkoxy, phenoxy or an amine residue; A is hydrogen or a group of the formula, ##EQU1## wherein R.sup.3, R.sup.4 and Y have the same meanings as defined above; and D and E each is hydrogen or halogen.These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##SPC2## with chloroform and a ketone compound of the formula,R.sup.3 --CO--R.sup.4in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##EQU2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, d, e and T have the same meanings as definend above; and X is halogen or hydroxyl.

    摘要翻译: 具有下式的新型抗动脉粥样硬化剂:其中R1和R2的典型实例是氢,C1-C8烷基,苯基,苄基和苯乙基,或R1和R2可以与其键合的碳原子一起形成亚环烷基; R3和R4各自为氢或C1-C4烷基; Y是羟基,C 1 -C 4烷氧基,苯氧基或胺残基; A是氢或下式的基团R3R4 ANGLE -C-COY,其中R3,R4和Y具有与上述相同的含义; D和E各自为氢或卤素。

    Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric
acid)-cyclohexane).alpha.-methyl substituted
    6.
    发明授权
    Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric acid)-cyclohexane).alpha.-methyl substituted 失效
    4-(1,1-双 - (苯氧基 - 丙酸) - 环己烷)(60-甲基取代的)的二杂环酯

    公开(公告)号:US4092324A

    公开(公告)日:1978-05-30

    申请号:US716666

    申请日:1976-08-23

    摘要: Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A preresents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent).

    摘要翻译: 作为具有良好吸收性和低毒性的抗动脉硬化剂的双苯氧基羧酸衍生物,它们是由通式表示的新化合物,其中R 1和R 2表示氢原子或低级烷基,并且A表示( 其中,在R 3为氢原子的情况下,R 4表示氨基 - 低级烷基,N-低级烷基氨基烷基,杂环基或杂环基取代的烷基;或者,R 3和R 4可以通过中间杂原子 原子形成杂环基,如果所述杂原子是氮原子,则该氮原子可以具有作为取代基的低级烷基)或者其中R5表示氢原子,羟烷基或其衍生物,和 R6表示羟基烷基或杂环基;或者R5和R6可以连接形成环状基团,或者可以通过另一个中间杂原子连接形成杂环基,如果所述杂原子是氮原子 ,该氮原子可以具有低级烷基作为取代基)。

    Thiazolidin-4-one derivatives and acid addition salts thereof useful for
treating PAF mediated diseases
    8.
    发明授权
    Thiazolidin-4-one derivatives and acid addition salts thereof useful for treating PAF mediated diseases 失效
    噻唑烷-4-酮衍生物及其适用于治疗PAF介导性疾病的酸添加物

    公开(公告)号:US5106860A

    公开(公告)日:1992-04-21

    申请号:US624566

    申请日:1990-12-10

    IPC分类号: C07D417/04

    CPC分类号: C07D417/04

    摘要: Thiazolidin-4-one derivative represented by the following general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl,or(ii) a residue represented by the general formula ##STR2## wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2;R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl,or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

    Thiazolidin-4-one derivatives useful for treating diseases caused by
platelet activating factor
    9.
    发明授权
    Thiazolidin-4-one derivatives useful for treating diseases caused by platelet activating factor 失效
    可用于治疗血小板活化因子引起的疾病的噻唑烷-4-酮衍生物

    公开(公告)号:US4992455A

    公开(公告)日:1991-02-12

    申请号:US196058

    申请日:1988-05-19

    IPC分类号: C07D417/04

    CPC分类号: C07D417/04

    摘要: Thiazolidin-4-one derivative represented by the folowing general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl, or(ii) a residue represented by the general formula{(CH.sub.2).sub.n O}.sub.m {(CH.sub.2).sub.n' O}B--R.sup.5 wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2; andR.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanol) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR2## (R.sup.10 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms), with the proviso that, when R.sup.1 is hydrogen and R.sup.2 is methyl, R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanoyl) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.