D-pentofuranose derivatives and process for preparing the same
    1.
    发明授权
    D-pentofuranose derivatives and process for preparing the same 失效
    D-呋喃糖衍生物及其制备方法

    公开(公告)号:US5880294A

    公开(公告)日:1999-03-09

    申请号:US981814

    申请日:1998-01-06

    CPC分类号: C07H9/04 C07H13/04 C07H19/04

    摘要: The present invention relates to D-pentofuranose derivatives represented by the following formulas (1) through (4): ##STR1## (wherein A represents a chlorobenzoyl group; R.sup.1 represents a hydrogen atom, an aliphatic lower acyl group, a substituted or unsubstituted benzoyl group; each of X and Y represents a lower alkyl group; Z represents an ethynyl group or tri-lower alkyl silylethynyl group; the sugar moiety in formula (1) represents xylose; and the sugar moiety of each of formulas (3) and (4) represents ribose). The present invention also relates to a process for preparing the compound (2) characterized by oxidizing the compound of formula (1) with a hypochlorite in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidinoxy compound, and these compounds are useful as intermediates in the synthesis of 3'-C-substituted ribonucleoside derivatives having excellent antitumor activities.

    摘要翻译: PCT No.PCT / JP97 / 01427 Sec。 371日期:1998年1月6日 102(e)日期1998年1月6日PCT 1997年4月24日PCT公布。 公开号WO97 / 43295 日期:1997年11月20日本发明涉及由下式(1)〜(4)表示的D-呋喃糖衍生物:< IMAGE>(2)< IMAGE>(3) )(其中A表示氯苯甲酰基; R1表示氢原子,脂肪族低级酰基,取代或未取代的苯甲酰基; X和Y各自表示低级烷基; Z表示乙炔基或三低级烷基甲硅烷基乙炔基 式(1)中的糖部分表示木糖;式(3)和(4)各自的糖部分表示核糖)。 本发明还涉及一种制备化合物(2)的方法,其特征在于在催化量的2,2,6,6-四甲基哌啶氧基化合物存在下,用次氯酸盐氧化式(1)化合物,这些化合物 可用作合成具有优异抗肿瘤活性的3'-取代核糖核苷衍生物的中间体。

    Condensed-Indan derivatives and pharmaceutically acceptable salts thereof
    5.
    发明授权
    Condensed-Indan derivatives and pharmaceutically acceptable salts thereof 失效
    缩合 - 茚满衍生物及其药学上可接受的盐

    公开(公告)号:US5733918A

    公开(公告)日:1998-03-31

    申请号:US578542

    申请日:1996-01-19

    摘要: A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## wherein ring A represents an optionally substituted benzene ring or naphthalene ring, or a benzene ring having a lower alkylenedioxy group, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR=N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.3 represents a lower alkyl group optionally substituted by a substituted amino group, except when R represents an optionally substituted nitrogen-containing heterocyclic group; ring A and ring B are a benzene ring having no substituent group.

    摘要翻译: PCT No.PCT / JP95 / 00944 Sec。 371日期1996年1月19日 102(e)日期1996年1月19日PCT提交1995年5月18日PCT公布。 出版物WO95 / 32187 日期:1995年11月30日由式(1)表示的缩合 - 缩水甘油衍生物及其药学上可接受的盐:其中环A表示任选取代的苯环或萘环,或具有低级亚烷基二氧基 基团,环B表示任选取代的苯环或具有较低亚烷基二氧基的苯环。 Y表示-N = CR-或-CR = N-,R表示-NR1R2基,任选取代的含氮杂环基或-OR 3基,其中R1和R2相同或不同,各自为氢原子 ; 苯基; 任选取代的含氮杂环基; 或可以被选自任选取代的氨基,低级烷氧基,苯基,含氮杂环基,被低级烷基取代的氧化胺基中的至少一种取代的低级烷基 基团或羟基; R3表示任选被取代的氨基取代的低级烷基,除了当R表示任意取代的含氮杂环基时; 环A和环B是没有取代基的苯环。

    Condensed-indan derivatives and pharmaceutically acceptable salts thereof
    6.
    发明授权
    Condensed-indan derivatives and pharmaceutically acceptable salts thereof 失效
    缩水甘油衍生物及其药学上可接受的盐

    公开(公告)号:US5710162A

    公开(公告)日:1998-01-20

    申请号:US713224

    申请日:1996-09-12

    摘要: A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## wherein ring A represents an optionally substituted naphthalene ring, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR.dbd.N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.3 represents a lower alkyl group optionally substituted by a substituted amino group.

    摘要翻译: 由式(1)表示的缩合 - 茚满衍生物及其药学上可接受的盐:其中环A表示任选取代的萘环,环B表示任选取代的苯环或具有低级亚烷基二氧基的苯环 组。 Y表示-N = CR-或-CR = N-,R表示-NR1R2基,任选取代的含氮杂环基或-OR 3基,其中R1和R2相同或不同,各自为氢原子 ; 苯基; 任选取代的含氮杂环基; 或可以被选自任选取代的氨基,低级烷氧基,苯基,含氮杂环基,被低级烷基取代的氧化胺基中的至少一种取代的低级烷基 基团或羟基; R3表示任选被取代的氨基取代的低级烷基。

    Condensed-indan derivatives and pharmaceutically acceptable salts thereof
    7.
    发明授权
    Condensed-indan derivatives and pharmaceutically acceptable salts thereof 失效
    缩水甘油衍生物及其药学上可接受的盐

    公开(公告)号:US6028079A

    公开(公告)日:2000-02-22

    申请号:US909934

    申请日:1997-08-12

    摘要: A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: wherein ring A represents an optionally substituted benzene ring or naphthalene ring, or a benzene ring having a lower alkylenedioxy group, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR.dbd.N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.3 represents a lower alkyl group optionally substituted by a substituted amino group, except when R represents an optionally substituted nitrogen-containing heterocyclic group; ring A and ring B are a benzene ring having no substituent group.

    摘要翻译: 由式(1)表示的缩合 - 茚满衍生物及其药学上可接受的盐:其中环A表示任选取代的苯环或萘环,或具有低亚烷基二氧基的苯环,环B表示任选取代的苯环或 具有低亚烷基二氧基的苯环。 Y表示-N = CR-或-CR = N-,R表示-NR1R2基,任选取代的含氮杂环基或-OR 3基,其中R1和R2相同或不同,各自为氢原子 ; 苯基; 任选取代的含氮杂环基; 或可以被选自任选取代的氨基,低级烷氧基,苯基,含氮杂环基,被低级烷基取代的氧化胺基中的至少一种取代的低级烷基 基团或羟基; R3表示任选被取代的氨基取代的低级烷基,除了当R表示任意取代的含氮杂环基时; 环A和环B是没有取代基的苯环。

    Process for preparing 1-amino-1,2,3-triazole
    8.
    发明授权
    Process for preparing 1-amino-1,2,3-triazole 失效
    1-氨基-1,2,3-三唑的制备方法

    公开(公告)号:US5728841A

    公开(公告)日:1998-03-17

    申请号:US637718

    申请日:1996-04-30

    IPC分类号: C07D249/04

    CPC分类号: C07D249/04

    摘要: This invention is to provide a process for preparing 1-amino-1,2,3-triazole represented by formula (III): ##STR1## comprising cyclizing glyoxal bishydrazone represented by formula (I): ##STR2## by reaction with an aqueous hydrogen peroxide solution in the presence of a catalytic amount of a transition metal oxide represented by formula (II): M.sub.m O.sub.n wherein M represents a transition metal atom; and m and n, which may be the same or different, each represent an integer of 1 to 5.

    摘要翻译: PCT No.PCT / JP95 / 01727 Sec。 371日期:1996年04月30日 102(e)日期1996年4月30日PCT提交1995年8月30日PCT公布。 出版物WO96 / 06835 日本特开1996年3月7日本发明提供一种制备由式(III)表示的1-氨基-1,2,3-三唑的方法:包含使由式(I)表示的乙二醛双腙环化: 在催化量的由式(II)表示的过渡金属氧化物存在下,过氧化物溶液:MmOn其中M表示过渡金属原子; m和n可相同或不同,分别表示1〜5的整数。

    Condensed indan derivatives and salts thereof
    10.
    发明授权
    Condensed indan derivatives and salts thereof 失效
    稠合茚满衍生物及其盐

    公开(公告)号:US5763453A

    公开(公告)日:1998-06-09

    申请号:US809602

    申请日:1997-04-03

    CPC分类号: C07D401/04 C07D221/18

    摘要: A condensed indan derivative represented by the formula (1) ##STR1## wherein the ring A is an optionally substituted benzene ring or a benzene ring which has lower alkylenedioxy group(s), the ring B is an optionally substituted benzene ring or a benzene ring which has lower alkylene dioxy group(s), and R is a group --NR.sub.1 R.sub.2, an optionally substituted nitrogen-containing heterocyclic group, a group --OR.sub.3 or a group --SR.sub.4 (wherein R.sub.1 and R.sub.2 are the same or different and each represent a hydrogen atom, a phenyl group, an optionally substituted nitrogen-containing heterocyclic group, or a lower alkyl group which may be substituted by optionally substituted amino group(s), lower alkoxy group(s), phenyl group(s), nitrogen-containing heterocyclic group(s) or hydroxyl group(s), and R.sub.3 and R.sub.4 each represent a lower alkyl group which may be substituted by substituted amino group(s)), provided that at least one of the rings A and B is a substituted benzene ring and R is not --NHCH.sub.3, and salts thereof, and medical use of said derivative and salts.

    摘要翻译: PCT No.PCT / JP96 / 02195 Sec。 371日期1997年4月3日 102(e)日期1997年4月3日PCT提交1996年8月2日PCT公布。 公开号WO97 / 06145 日本公报1997年2月20日由式(1)表示的缩合茚满衍生物(1)其中环A为任选取代的苯环或具有低亚烷基二氧基的苯环,环B为 任选取代的苯环或具有低级亚烷基二氧基的苯环,R为基团-NR1R2,任选取代的含氮杂环基,-OR3基或-SR4基(其中R1和R2为 相同或不同,各自表示氢原子,苯基,任选取代的含氮杂环基或可被任选取代的氨基取代的低级烷基,低级烷氧基,苯基 基团,含氮杂环基或羟基,R 3和R 4各自表示可以被取代的氨基取代的低级烷基),条件是至少一个 环A和B是取代的苯环,R不是-NHCH 3及其盐,以及所述衍生物和盐的医疗用途。