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    Degradation fragments
    11.
    发明授权
    Degradation fragments 失效
    降解片段

    公开(公告)号：US07498421B2

    公开(公告)日：2009-03-03

    申请号：US11479024

    申请日：2006-06-30

    申请人： Joseph Floyd Clark ,  Thomas Andrew Daniel Cadoux-Hudson ,  Christopher Joseph Schofield

    发明人： Joseph Floyd Clark ,  Thomas Andrew Daniel Cadoux-Hudson ,  Christopher Joseph Schofield

    IPC分类号： C07D207/00 ,  C07D295/00 ,  C07D207/18 ,  C12P21/08 ,  C07K16/00 ,  G01N33/53

    CPC分类号： C07D207/44 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K41/0019 ,  C07D207/448 ,  C07D413/06 ,  G01N33/728 ,  Y10S436/822

    摘要： A pharmaceutical composition comprising a compound of formula (I) wherein X is an electron withdrawing group, Y1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R4, —CO2R4, —CONHR4 or —COR4, and each of R1, R2 and R4, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, or a compound of formula (II) wherein each of Y2 and Y3, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R9, —CO2R9, —CONHR9 or —COR9, Z is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclyl, —CH═C(NHR10)CH((CH2)m CO2R11)(C═O)CH3 or —CH2(C═O)CH((CH2)mCO2R11)(C═O)CH3, R8 is —(CH2)nCO2R12, each of R5 to R7 and R9 to R12, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and each of m and n, which may be the same or different, is 1 to 6 or a compound of formula (III) wherein each of Y4 to Y6, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R19, —CO2R19, —CONHR19 or —COR19, each of R16 and R17, which may be the same or different, is —(CH2)p CO2R20, each of R13 to R15 and R18 to R20, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and p is 1 to 6, or other photolabile degradation product of bilirubin or biliverdin or derivative of a photolabile degradation fragment of bilirubin or biliverdin, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier or diluent.

    摘要翻译： 一种药物组合物，其包含式（I）化合物，其中X为吸电子基团，Y 1为氢，烷基，烯基，炔基，芳基，杂环基，-SO 2 R 4，-CO 2 R 4，-CONHR 4或-COR 4， R 2和R 4可以相同或不同，是氢，烷基，环烷基，烯基，环烯基，炔基，芳基或杂环基，或式（II）化合物，其中Y2和Y3各自可以相同或 不同的是氢，烷基，烯基，炔基，芳基，杂环基，-SO 2 R 9，-CO 2 R 9，-CONHR 9或-COR 9，Z是氢，烷基，环烷基，链烯基，环烯基，炔基，芳基，杂环基，-CH-C NHR 10）CH（（CH 2）m CO 2 R 11）（CO）CH 3或-CH 2（CO）CH（（CH 2）m CO 2 R 11）（CO）CH 3，R 8是 - （CH 2）n CO 2 R 12，R 5至R 7和R 9至R 12， 可以相同或不同的是氢，烷基，环烷基，烯基，环烯基，炔基，芳基或杂环基，并且m和n可以相同或不同，m为1至6的化合物或式 III）其中Y4至Y6， 氢，烷基，烯基，炔基，芳基，杂环基，-SO 2 R 19，-CO 2 R 19，-CONHR 19或-COR 19可以相同或不同，R 16和R 17可以相同或不同，为 - （ CH2）pCO2R20，R13至R15和R18至R20各自可以相同或不同，为氢，烷基，环烷基，烯基，环烯基，炔基，芳基或杂环基，p为1-6，或其他光不稳定性 胆红素或胆红素的降解产物或胆红素或胆红素或其药学上可接受的盐的光不稳定降解片段的衍生物以及药学上可接受的载体或稀释剂。

    Pyrrolopyrimidine derivatives having pharmacological activity
    14.
    发明授权
    Pyrrolopyrimidine derivatives having pharmacological activity 失效
    具有药理活性的吡咯并嘧啶衍生物

    公开(公告)号：US6096749A

    公开(公告)日：2000-08-01

    申请号：US53266

    申请日：1998-04-01

    申请人： Peter Traxler ,  Pascal Furet ,  Wolfgang K.-D. Brill

    发明人： Peter Traxler ,  Pascal Furet ,  Wolfgang K.-D. Brill

    IPC分类号： C07D498/02 ,  A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  A61P17/06 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D20060101 ,  C07D207/18 ,  C07D239/42 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumor diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; andR.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R.sub.1 and R.sub.2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl;or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.

    摘要翻译： 本发明涉及下述化合物在肿瘤疾病和其它增殖性疾病如牛皮癣的治疗性治疗中的用途，以及该类型的新型化合物。 化合物是其中n为0至5的式I化合物，当n不为0时，R为一个或多个选自卤素，烷基，三氟甲基和烷氧基的取代基; 并且R 1和R 2各自独立地为未被取代或被卤素，三氟甲基，烷基或烷氧基取代的苯基，也可以是两个基团R 1和R 2中的一个为氢，或者R 1和R 2 一起形成未被取代或被烷基取代的具有2至5个碳原子的亚烷基链; 或其盐。 式I的化合物抑制蛋白激酶，例如表皮生长因子受体的酪氨酸蛋白激酶EGF。