Quinazoline derivatives as medicaments
    11.
    发明授权
    Quinazoline derivatives as medicaments 有权
    喹唑啉衍生物作为药物

    公开(公告)号:US06277989B1

    公开(公告)日:2001-08-21

    申请号:US09525034

    申请日:2000-03-14

    IPC分类号: C07D23942

    摘要: The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

    摘要翻译: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法,其中R3是不干扰取代基;每个Z是CR2或N,其中环中不超过两个Z位置 A是N,并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族,环状杂脂族,芳族或杂芳族部分的残基。

    Quinazoline derivatives as inhibitors of P-38 &agr;
    12.
    发明授权
    Quinazoline derivatives as inhibitors of P-38 &agr; 有权
    喹唑啉衍生物作为P-38α的抑制剂

    公开(公告)号:US06184226B2

    公开(公告)日:2001-02-06

    申请号:US09141916

    申请日:1998-08-28

    IPC分类号: A01N5500

    摘要: The invention describes compounds of the formula and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH or N; R1 is H, alkyl (1-6C) or arylalkyl optionally substituted on the aryl group with 1-3 substituents independently selected from alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); n is 0, 1 or 2; Ar is phenyl, pyridyl, indolyl, or pyrimidyl, each optionally substituted with a group selected from the group consisting of optionally substituted alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); and R3 is a branched or cyclic alkyl group (5-7C) or is phenyl optionally substituted with 1-2 substituents which substituents are selected from the group consisting of alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C) which are useful as antiinflammatories and in treating cardiac disorders.

    摘要翻译: 本发明描述了下式的化合物及其药学上可接受的盐及其药学上可接受的盐,其中R2各自独立地为非干扰性取代基; m为0-4的整数; Z为CH或N; R 1为H,烷基(1-6C) (1-6C),卤素,OR,NR2,SR,-OOCR,-NROCR,RCO,-COOR,-CONR2,-SO2NR2,CN等的任选取代的芳基, CF 3和NO 2,其中每个R独立地为H或低级烷基(1-4C); n为0,1或2; Ar为苯基,吡啶基,吲哚基或嘧啶基,各自任选被选自以下的基团取代: 任选取代的烷基(1-6C),卤素,OR,NR2,SR,-OOCR,-NROCR,RCO,-COOR,-CONR2,SO2NR2,CN,CF3和NO2,其中每个R独立地为H或低级烷基 (1-4C); 和R 3是支链或环状烷基(5-7C),或是任选被1-2个取代基取代的苯基,所述取代基选自烷基(1-6C),卤素,OR,NR2,SR,-OOCR, -NROCR,RCO,-COOR,-CONR2,-SO2NR2,CN,CF3和NO2,其中每个R独立地为H或可用作抗炎剂和治疗心脏疾病的低级烷基(1-4C)。

    Compounds and methods for treatment of cancer-related anemia
    15.
    发明申请
    Compounds and methods for treatment of cancer-related anemia 审中-公开
    用于治疗癌症相关性贫血的化合物和方法

    公开(公告)号:US20110015223A1

    公开(公告)日:2011-01-20

    申请号:US12806589

    申请日:2010-08-16

    IPC分类号: A61K31/472 A61P7/06

    CPC分类号: A61K31/47

    摘要: The invention relates to methods and compounds for treating anemia of cancer. In particular, methods for treating anemia of cancer in a subject having cancer, and methods for increasing reticulocytes, increasing hemoglobin, increasing hematocrit, and increasing red blood cell count in subjects having anemia of cancer, wherein such subjects are refractory to treatment with recombinant human erythropoietin (EPO) are encompassed herein.

    摘要翻译: 本发明涉及治疗癌症贫血的方法和化合物。 特别地,在具有癌症的受试者中治疗癌症的贫血的方法和增加网织红细胞的方法,增加血红蛋白,增加血细胞比容,以及增加患有贫血的受试者的红细胞计数,其中这些受试者对重组人治疗是难以治疗的 红细胞生成素(EPO)包括在本文中。