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    • 4. 发明授权
    • Thiazolidin-4-one derivatives useful for treating diseases caused by
platelet activating factor
    • 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
    • US4992455A
    • 1991-02-12
    • US196058
    • 1988-05-19
    • Masao EnomotoAtsuyuki KojimaYoshihiro KomuroShigeaki MorookaShunji AonoYuzuru SanemitsuMasato MizutaniYou Tanabe
    • Masao EnomotoAtsuyuki KojimaYoshihiro KomuroShigeaki MorookaShunji AonoYuzuru SanemitsuMasato MizutaniYou Tanabe
    • C07D417/04
    • C07D417/04
    • 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.
    • 6. 发明授权
    • Phenoxy carboxylic acid derivative
    • 苯氧基羧酸衍生物
    • US4031134A
    • 1977-06-21
    • US292110
    • 1972-09-25
    • Yasushi NakamuraKunio AgatsumaYoshihiro TanakaShunji Aono
    • Yasushi NakamuraKunio AgatsumaYoshihiro TanakaShunji Aono
    • C07C51/367C07C51/41C07C59/68C07C59/72C07C65/14C07C69/76
    • C07C59/72C07C51/367C07C51/412C07C59/68
    • Novel anti-atherosolerosis agents having the formula, ##STR1## 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, ##STR2## wherein R.sup.3, and 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, ##STR3## 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, ##STR4## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, D, E and Y have the same meanings as defined above; and X is halogen or hydroxyl.
    • 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,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。
    • 8. 发明授权
    • Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric
acid)-cyclohexane).alpha.-methyl substituted
    • 4-(1,1-双 - (苯氧基 - 丙酸) - 环己烷)(60-甲基取代的)的二杂环酯
    • US4092324A
    • 1978-05-30
    • US716666
    • 1976-08-23
    • Yoshio SuzukiMasayoshi MinaiNoritaka HammaEiichi MurayamaShunji Aono
    • Yoshio SuzukiMasayoshi MinaiNoritaka HammaEiichi MurayamaShunji Aono
    • C07D211/46C07D213/30C07D213/75C07D213/55
    • C07D213/30C07D211/46C07D213/75
    • 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).
    • 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)。