中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

27 records (took 0.011 seconds)

    Ara-cytidine derivatives and process of preparation
    11.
    发明授权
    Ara-cytidine derivatives and process of preparation 失效
    Ara-cytidine衍生物及其制备方法

    公开(公告)号：US3894000A

    公开(公告)日：1975-07-08

    申请号：US38085073

    申请日：1973-07-19

    Applicant: UPJOHN CO

    Inventor： WECHTER WILLIAM J ,  WARNER DONALD T

    IPC: C07H19/06 ,  C07D51/52

    CPC classification number: C07H19/06

    Abstract: Novel 2''-0-, 3''-0-, 2'',3''-di-0-, 2'',5''-di-0- and 3'',5''-di-0esters of ara-cytidine and novel processes for their preparation are claimed. The novel 2''-0-esters (1) and 2'',5''-di-0-esters (11) are embraced by the formula

    WHEREIN Y is selected from the group consisting of 1.

    wherein R is a radical selected from the group consisting of aliphatic of from 1 through 20 carbon atoms, aromatic of from 6 through 10 carbon atoms, cage-type hydrocarbon of from 7 through 20 carbon atoms, monocyclic aliphatic of from 4 through 10 carbon atoms, araliphatic of from 7 through 12 carbon atoms and monocyclic heterocyclic of from 4 through 10 carbon atoms, including such radicals substituted by halogen, hydroxyl, carboxyl, nitro, alkoxyl or mercapto groups; 2.

    wherein R'' is a radical selected from the group consisting of aliphatic of from 1 through 20 carbon atoms, aromatic of from 6 through 10 carbon atoms, araliphatic of from 7 through 12 carbon atoms, AND Z is selected from the group consisting of Y and hydrogen; and pharmaceutically acceptable acid addition salts thereof. The novel 3''-0-esters (III) and 3'',5''-di-0-esters (IV) are embraced by the formula

    WHEREIN Z and Y are as given above, and pharmaceutically acceptable acid addition salts thereof. The novel 2'',3''-di-0-esters (V) are embraced by the formula

    WHEREIN Y is as given above, and pharmaceutically acceptable acid addition salts thereof. The compounds of the above formulae are orally active sustainedrelease immunosuppressant and anti-neoplastic agents having the characteristics of the anti-leukemic compound ara-cytidine.

    Abstract translation: ara-cytidine的新的2'-0-，3'-0-，2'，3'-二-O-，2'，5'-二-O-和3'，5'-二-O- 并要求其制备新颖的方法。 新的2'-O-酯（1）和2'，5'-二-O-酯（11）包括式WHEREIN Y选自由以下组成的组：O PARALLEL RC-，其中R为 选自1至20个碳原子的脂族基团，6至10个碳原子的芳族基团，7至20个碳原子的笼型烃基，4至10个碳原子的单环脂肪族基团， 7至12个碳原子和4至10个碳原子的单环杂环，包括被卤素，羟基，羧基，硝基，烷氧基或巯基取代的基团; 2.其中R'为选自1至20个碳原子的脂族基团，6至10个碳原子的芳族基团，7至12个碳原子的芳脂族基团，Z Z为 选自Y和氢; 及其药学上可接受的酸加成盐。

    2,2{40 -Anhydro-ara-cytidine compounds and process of preparation
    18.
    发明授权
    2,2{40 -Anhydro-ara-cytidine compounds and process of preparation 失效
    2,2 {40-非氢 - 胞苷化合物及其制备方法

    公开(公告)号：US3920630A

    公开(公告)日：1975-11-18

    申请号：US28617072

    申请日：1972-09-05

    Applicant: UPJOHN CO

    Inventor： WECHTER WILLIAM J ,  GISH DUANE T

    IPC: C07H19/06

    CPC classification number: C07H19/06 ,  Y10S514/825 ,  Y10S514/903 ,  Y10S514/908

    Abstract: wherein X is the conjugate base of a strong acid and R is a radical selected from the group consisting of straight or branched chain aliphatic or alicylic radicals containing from 1 through 20 carbon atoms; monocyclic or bicyclic aromatic radicals of from 6 through 20 carbon atoms; monocyclic heterocyclic radicals of from 4 through 10 carbon atoms; araliphatic radicals of from 7 through 12 carbon atoms; or cage-type hydrocarbon radicals containing from 7 through 20 carbon atoms; and including such radicals substituted by halogen, hydroxyl, carboxyl, nitro, alkoxyl or mercapto substituent groups. It also pertains to the preparation from compounds of formulas I and II of 5''-O-acylates of ara-cytidine. Further, it pertains to pharmaceutical compositions of compounds of formulas I and II and a process for treatment of pathological conditions therewith. Compounds of formulas I and II have immunosuppressive activities.

    and the acid addition salts thereof. It also pertains to the preparation of novel 5''-O-acyl-2,2''-anhydro-ara-cytidines of the formula II

    This invention relates to a novel process for preparing the known useful compound 2,2''-anhydro-ara-cytidine (also known as O2, 2''-anhydro-ara-cytidine and O2O2 -anhydro-1- Beta -Darabinofuranosylcytosine) having the formula I

    Abstract translation: 本发明涉及一种制备已知有用化合物2,2'-脱水 - 阿糖胞苷（也称为O 2，2'-脱水 - 阿糖胞苷和O 2 O 2 - 脱氢-β-D- - 阿拉伯呋喃糖基胞嘧啶）和其酸加成盐。 它还涉及制备式II的新的5'-O-酰基-2,2'-脱水阿糖胞苷，其中X 1是强酸的共轭碱，R是选自 由含有1至20个碳原子的直链或支链脂族或脂环基团组成的基团; 6至20个碳原子的单环或双环芳族基团; 4至10个碳原子的单环杂环基; 7至12个碳原子的芳脂族基团; 或含有7至20个碳原子的笼型烃基; 并且包括被卤素，羟基，羧基，硝基，烷氧基或巯基取代基取代的这些基团。 它还涉及由芳基胞苷的5'-O-酰化物的式I和II化合物的制备。 此外，它涉及式I和II化合物的药物组合物及其治疗病理状况的方法。 式I和II的化合物具有免疫抑制活性。

Patent Agency Ranking