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    Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof
    53.
    发明申请
    Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof 有权
    包含二核苷多磷酸盐及其盐的药物制剂

    公开(公告)号：US20050085439A1

    公开(公告)日：2005-04-21

    申请号：US10962016

    申请日：2004-10-07

    申请人： Benjamin Yerxa ,  Ward Peterson ,  Janet Rideout ,  William Pendergast

    发明人： Benjamin Yerxa ,  Ward Peterson ,  Janet Rideout ,  William Pendergast

    IPC分类号： A61K31/7084 ,  C07H19/04 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  A61K31/7072

    CPC分类号： C07H19/10 ,  A61K31/7072 ,  A61K31/7084 ,  C07H19/04 ,  C07H19/20 ,  C07H21/00 ,  Y10S514/851

    摘要： The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphate salts. The present invention also provides P1-(2′-deoxycytidine 5′-)P4-(uridine 5′-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts. The present further provides a pharmaceutical formulation comprising a P1-(2′-deoxycytidine 5′-)P4-(uridine 5′-)tetraphosphate, tetra-(alkali metal) salt, in a pharmaceutically acceptable carrier.

    摘要翻译： 本发明提供治疗水肿性视网膜病变的方法。 该方法包括施用包含水解抗性P2Y受体激动剂的药物制剂，以刺激从视网膜下和视网膜空间中除去病理性外来流体，从而减少与视网膜脱离和视网膜水肿相关的所述流体的积聚。 P2Y受体激动剂可以与通常用于治疗水肿性视网膜疾病的治疗剂和辅助剂一起施用。 可用于本发明的药物制剂包含具有增强的细胞外水解抗性的P2Y受体激动剂，例如二核苷多磷酸酯化合物或耐水解的单核苷三磷酸盐。 本发明还提供了P 1 - （2'-脱氧胞苷5' - ）P 4 - （尿苷5'-）四磷酸盐，四（碱金属盐）盐 作为四钠，四锂，四钾和混合（四碱金属）盐。 本发明还提供一种药物制剂，其包含P 1 - （2'-脱氧胞苷5' - ）P 4 - （尿苷5' - ）四磷酸酯，四 - （碱 金属）盐，在药学上可接受的载体中。

    Pharmaceutically active benzoquinazoline compounds
    54.
    发明授权
    Pharmaceutically active benzoquinazoline compounds 失效
    药用活性苯并喹唑啉化合物

    公开(公告)号：US06762188B1

    公开(公告)日：2004-07-13

    申请号：US09952394

    申请日：2001-09-12

    申请人： William Pendergast ,  Scott Howard Dickerson ,  Julius Vass Johnson ,  Robert Ferone

    发明人： William Pendergast ,  Scott Howard Dickerson ,  Julius Vass Johnson ,  Robert Ferone

    IPC分类号： A61K31502

    CPC分类号： C07D403/12 ,  C07D239/70

    摘要： Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —CH═CH— or N═N—, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.

    摘要翻译： 式（I）化合物或其盐，其中虚线表示单键或双键，R 1是任选被烷基，烷酰基或苄基取代的烷基或氨基; R 2，R 3，R 4和R 5相同或不同，各自选自氢，苯基，卤素，硝基，基团S（O）n R 8，其中n为 整数0,1或2和R 8是卤素或烷基或基团NR 9 R 10，其中R 9和R 10均为氢，NR 11 R 12 其中R 11和R 12相同或不同，各自为氢或烷基，OR 13，其中R 13为氢或任选被卤素取代的烷基的C 1-4; 任选被OR 14或NR 14 R 15基团取代的C 1-4脂族基团，其中R 14和R 15相同或不同，各自为氢或烷基; 或R 2至R 5中的两个连接在一起形成苯并基团，或R 2至R 5之一为XYR 16基团，其中X为CH 2，NR 17， CO或S（O）m，Y是CH 2，NR 17，O或S（O）m，或XY是O，NR 17，-CH = CH-或N = N- 可用于治疗肿瘤的药物。 还描述了制备式（I）化合物的药物组合物和方法。