.beta.-d-phenylthioxylosides, and their use as therapeutic agents
    6.
    发明授权
    .beta.-d-phenylthioxylosides, and their use as therapeutic agents 失效
    β-β-苯硫噻嗪类及其作为治疗剂的用途

    公开(公告)号:US5246961A

    公开(公告)日:1993-09-21

    申请号:US793649

    申请日:1991-11-18

    摘要: The present invention relates, by way of novel industrial products, to the .beta.-D-phenylthioxyloside compounds of the formula ##STR1## in which: X represents a sulfur atom or an oxygen atom;R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent a hydrogen atom, a nitro group, a cyano group, a group --CO--R (in which R represents a C.sub.1 -C.sub.4 alkyl group or a trifluoromethyl group), an amino group, an acetamido group (NHCOCH.sub.3), a C.sub.1 -C.sub.4 alkoxy group, a trifluoromethyl group or a phenyl group substituted by one or more cyano, nitro or trifluoromethyl groups, it being possible for R.sub.1 and R.sub.2, taken together, to form, with the phenyl group to which they are bonded, a .beta.-naphthalenyl group which is unsubstituted or substituted by one or more cyano, nitro or trifluoromethyl groups; andY represents the hydrogen atom or an aliphatic acyl group.

    摘要翻译: 本发明通过新工业产品涉及式(I)的β-D-苯硫噻酰氯化合物,其中:X表示硫原子或氧原子; R 1,R 2和R 3相同或不同,各自表示氢原子,硝基,氰基,-CO-R基(其中R表示C1-C4烷基或三氟甲基), 氨基,乙酰氨基(NHCOCH 3),C 1 -C 4烷氧基,三氟甲基或被一个或多个氰基,硝基或三氟甲基取代的苯基,可以将R 1和R 2一起形成, 与它们所键合的苯基,未被取代或被一个或多个氰基,硝基或三氟甲基取代的β-萘基; Y表示氢原子或脂肪族酰基。

    Benzylphenyl osides, method of preparation and use therefor
    8.
    发明授权
    Benzylphenyl osides, method of preparation and use therefor 失效
    苄基苯基膦,其制备方法及用途

    公开(公告)号:US4598068A

    公开(公告)日:1986-07-01

    申请号:US632009

    申请日:1984-07-18

    CPC分类号: C07H15/203

    摘要: The present invention relates, by way of new industrial products, to the benzylphenyl osides of the formula ##STR1## in which: X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5, which are identical or different, each represent a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkyl group substituted by one or more halogen atoms (in particular a CF.sub.3 group), an OH group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 alkoxy group substituted by one or more halogen atoms, a nitro group, a group NR'R" (in which R' and R", which are identical or different, each represent the hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an acetyl group), a methylthio group, a methylsulfinyl group or a mesyl group, andR represents an ose radical chosen from the group comprising(a) the .alpha.-L-rhamnosyl radical,(b) non-hydrolyzable monosaccharide radicals and(c) non-hydrolyzable monosaccharide radicals in which the hydroxyl group on the carbon atom in the 2-position is replaced with an amine group, the hydroxyl and amine groups of the group R being capable of acetylation, and their addition salts in cases where at least one of the groups X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5 and R comprises a basic radical.These new products are useful in therapy. They can be prepared by reducing the corresponding benzoylphenyl and .alpha.-hydroxybenzylphenyl osides.

    摘要翻译: 本发明通过新的工业产品涉及式(I)的苄基苯基酮,其中:相同或不同的X 1,X 2,X 3,X 4和X 5各自表示氢原子, 卤素原子,C1-C4烷基,被一个或多个卤素原子(特别是CF 3基团)取代的C 1 -C 4烷基,OH基,C 1 -C 4烷氧基,C 1 -C 4烷氧基取代 通过一个或多个卤素原子,硝基,NR'R“基团(其中R'和R”'相同或不同,各自表示氢原子,C 1 -C 4烷基或乙酰基 ),甲硫基,甲基亚磺酰基或甲磺酰基,R表示选自(a)α-L-鼠李糖基,(b)不可水解单糖基和(c) 2位上碳原子上的羟基被胺基取代的水解性单糖基团,其中羟基和胺基团 在基团X1,X2,X3,X4,X5和R中的至少一个包含碱性基团的情况下,p R能够进行乙酰化,以及它们的加成盐。 这些新产品在治疗中是有用的。 它们可以通过还原相应的苯甲酰基苯基和α-羟基苄基苯基膦来制备。

    Benzoyl-phenyl-piperidine derivatives
    10.
    发明授权
    Benzoyl-phenyl-piperidine derivatives 失效
    苯甲酰基 - 苯基 - 哌啶衍生物

    公开(公告)号:US4528294A

    公开(公告)日:1985-07-09

    申请号:US391915

    申请日:1982-06-24

    摘要: The present invention relates to new benzoyl-phenyl-piperidine derivatives selected from the group consisting of:(i) 2-piperidinobenzophenones of the general formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent an atom of hydrogen, a hydroxy group, CF.sub.3, a halogen, a lower alkyl group or a lower alkoxy group;R.sub.4 represents an atom of hydrogen, a halogen, an NO.sub.2 group, an NR'R" group [where R' and R", which are identical or different, represent an atom of hydrogen, a lower alkyl group or a CO.sub.2 R group (where R represents a lower alkyl group or a benzyl group)];R.sub.5 and R.sub.6, which are identical or different, each represent an atom of hydrogen, a C.sub.1 -C.sub.4 -alkyl group, an OH group, a phenyl group or a benzyl group; and(ii) acid addition salts thereof.The invention also relates to the method for preparing these new derivatives and to their use in therapeutics, particularly as immunostimulant and immunoadjuvant agents.

    摘要翻译: 本发明涉及选自以下的新的苯甲酰基 - 苯基 - 哌啶衍生物:(i)具有以下通式的2-哌啶二苯甲酮:其中:R1,R2和R3相同或不同 各自表示氢原子,羟基,CF 3,卤素,低级烷基或低级烷氧基; R 4表示氢原子,卤素,NO 2基,NR'R“基[其中R'和R”相同或不同,表示氢原子,低级烷基或CO 2 R基团 (其中R表示低级烷基或苄基)]; R5,R6相同或不同,分别表示氢原子,C1-C4烷基,OH基,苯基或苄基。 和(ii)其酸加成盐。 本发明还涉及制备这些新衍生物及其在治疗学中的用途的方法,特别是作为免疫刺激剂和免疫佐剂。