Derivatives of benzofuran or benzodioxazole compounds
    12.
    发明授权
    Derivatives of benzofuran or benzodioxazole compounds 失效
    苯并呋喃或苯并恶唑化合物的衍生物

    公开(公告)号:US06716987B1

    公开(公告)日:2004-04-06

    申请号:US10023091

    申请日:2001-12-20

    IPC分类号: C07D41300

    摘要: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.

    摘要翻译: 由下式(I)表示的含氧杂环化合物:其中R 1和R 2独立地表示氢,低级烷基,氰基, - (CH 2)nE 1 -CO-G 1(其中 E 1表示键,O或NH;且G 1表示氢,取代或未取代的低级烷基,OR 6或NR 7 R 8; n表示0〜 4)等; R 1和R 2相互结合形成饱和碳环和与其相邻的碳原子。 或R 2,以及下述R 11或R 13组合形成单键; R 3表示氢,苯基或卤素; R 4表示羟基,低级烷氧基等; A表示-C(R 9)(R 10) - 或O; B表示O,NR 11,-C(R 12)(R 13) - 或-C(R 14)(R 15)-C(R 16)(R 16) <17>) - ; D表示(i)-C(R 18)(R 19)-X-(其中X表示-C(R 21)(R 22) - ,S或NR 23) ,(ii)-C(R 19)= Y- [Y表示-C(R 24) - Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii) 一个债券 R 5表示芳基,芳香族杂环基,环烷基,吡啶-N-氧化物,氰基或低级烷氧基羰基; 或其药学上可接受的盐。

    Condensed purine derivatives
    14.
    发明授权
    Condensed purine derivatives 失效
    凝血嘌呤衍生物

    公开(公告)号:US06306847B1

    公开(公告)日:2001-10-23

    申请号:US09090936

    申请日:1998-06-05

    IPC分类号: C07D48714

    CPC分类号: C07D487/14

    摘要: The present invention provides condensed purine derivatives or pharmacologically acceptable salts thereof exhibiting adenosine A3 acceptor antagonising activity, and having an antiasthmatic action, a bronchodilator action, an antiantiitching action, etc., and represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents hydrogen, lower alkyl, or substituted or unsubstituted aralkyl; X1 and X2 are the same or different and each represents hydrogen, lower alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted aryl; and n represents an integer of 0 to 3).

    摘要翻译: 本发明提供具有腺苷A3受体拮抗活性的缩合嘌呤衍生物或其药理学上可接受的盐,并具有抗哮喘作用,支气管扩张剂作用,抗脱除作用等,并由下式(I)表示:(其中R1表示 取代或未取代的芳基或取代或未取代的芳族杂环基; R 2表示氢,低级烷基,脂环族烷基,取代或未取代的芳烷基,取代或未取代的芳基或取代或未取代的芳族杂环基; R 3表示氢,低级烷基或 取代或未取代的芳烷基; X 1和X 2相同或不同,各自表示氢,低级烷基,取代或未取代的芳烷基或取代或未取代的芳基; n表示0〜3的整数。

    Xanthine derivatives
    16.
    发明授权
    Xanthine derivatives 失效
    黄嘌呤衍生物

    公开(公告)号:US5756735A

    公开(公告)日:1998-05-26

    申请号:US483159

    申请日:1995-06-07

    IPC分类号: C07D473/06

    CPC分类号: C07D473/06

    摘要: The present invention relates to novel xanthine derivatives of the formula (I) which are selectively antagonistic to an adenosine A.sub.2 receptor, and pharmaceutically acceptable salts thereof. Formula (I): ##STR1## In the formula, R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom, a propyl group, a butyl group or an allyl group; R.sup.3 represents a hydrogen atom or a lower alkyl group; Y.sup.1 and Y.sup.2 are the same or different and each represents a hydrogen atom or a methyl group; and Z represents a substituted or unsubstituted phenyl group, a pyridyl group, an imidazolyl group, a furyl group or a thienyl group.

    摘要翻译: 本发明涉及对腺苷A2受体选择性拮抗的式(I)的新颖黄嘌呤衍生物及其药学上可接受的盐。 式(I):(I)式中,R 1和R 2相同或不同,表示氢原子,丙基,丁基或烯丙基; R3表示氢原子或低级烷基; Y1和Y2相同或不同,各自表示氢原子或甲基; Z表示取代或未取代的苯基,吡啶基,咪唑基,呋喃基或噻吩基。

    Process for producing thermoplastic copolymer powder
    18.
    发明授权
    Process for producing thermoplastic copolymer powder 失效
    生产热塑性共聚物粉末的方法

    公开(公告)号:US5521231A

    公开(公告)日:1996-05-28

    申请号:US381888

    申请日:1995-02-24

    摘要: A process for producing a thermoplastic polymer powder which comprises adding a polymer (B) and/or an inorganic compound (C) to a coagulation slurry or a powder of a thermoplastic polymer (A) obtained from emulsion polymerization and having a glass transition temperature Tg defined by the following equation (1), in an amount of 0.1-10 parts by weight to 100 parts by weight of the thermoplastic polymer (A), compacting the thermoplastic polymer (A) at a temperature in a range of (Tg-30) to (Tg+50).degree. C., and comminuting it:Tg=W.sub.1 .times.Tg.sub.1 +W.sub.2 .times.Tg.sub.2 + . . . +W.sub.n .times.Tg.sub.n ( 1)wherein n is the number of the monomers forming the thermoplastic polymer (A); W.sub.1, W.sub.2, . . . W.sub.n each represents weight fraction of each monomer i (i=1, 2, . . . n) in the polymer (A); and Tg.sub.1, Tg.sub.2, . . . Tg.sub.n each represents the glass transition temperature of the polymer composed of each monomer i. According to the present invention, it is possible to remarkably enhance bulk specific gravity of thermoplastic polymers as compared with the case using the methods known in the art.

    摘要翻译: PCT No.PCT / JP93 / 01221 Sec。 371日期:1995年2月24日 102(e)1995年2月24日PCT PCT 1993年8月31日PCT公布。 出版物WO94 / 05722 日本特开2002-1933年所述的热塑性聚合物粉末的制造方法,其特征在于,将聚合物(B)和/或无机化合物(C)添加到由乳液聚合得到的凝固浆料或热塑性聚合物(A)的粉末中 并且具有由下式(1)定义的玻璃化转变温度Tg,相对于100重量份热塑性聚合物(A)为0.1-10重量份,在热塑性聚合物(A)的温度下压制热塑性聚合物 (Tg-30)至(Tg + 50)℃的范围,并粉碎:Tg = W1xTg1 + W2xTg2 +。 。 。 + WnxTgn(1)其中n是形成热塑性聚合物(A)的单体数目; W1,W2,。 。 。 Wn分别表示聚合物(A)中各单体i(i = 1,2,...)的重量分数。 和Tg1,Tg2。 。 。 Tgn各自表示由各单体i构成的聚合物的玻璃化转变温度。 根据本发明,与使用本领域已知方法的情况相比,可以显着提高热塑性聚合物的体积比重。