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    Connective Tissue Growth Factor Signaling
    6.
    发明申请
    Connective Tissue Growth Factor Signaling 审中-公开
    结缔组织生长因子信号传导

    公开(公告)号：US20080254487A1

    公开(公告)日：2008-10-16

    申请号：US10586318

    申请日：2005-01-14

    申请人： Stephen J. Klaus ,  David Y. Liu ,  Irina Aizman

    发明人： Stephen J. Klaus ,  David Y. Liu ,  Irina Aizman

    IPC分类号： G01N33/566 ,  C07H3/00 ,  C12Q1/02

    CPC分类号： G01N33/74 ,  A61K31/737 ,  G01N2500/02

    摘要： The present invention provides compounds and agents that modulate CTGF-mediated cell adhesion and/or binding of CTGF to cells. The invention further provides assays that may be used to identify additional modulators of CTGF-mediated cell adhesion and CTGF binding to cells, and assays that may be used to identify compounds or agents that modulate interaction of CTGF with HSPGs.

    摘要翻译： 本发明提供调节CTGF​​介导的细胞粘附和/或CTGF与细胞结合的化合物和试剂。 本发明进一步提供可用于鉴定CTGF介导的细胞粘附和CTGF与细胞结合的其它调节剂的测定法，以及可用于鉴定调节CTGF​​与HSPG相互作用的化合物或试剂的测定法。

    Compounds and methods for treatment of cancer-related anemia
    8.
    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：US20070293575A1

    公开(公告)日：2007-12-20

    申请号：US11455202

    申请日：2006-06-15

    申请人： Todd W. Seeley ,  David Y. Liu ,  Stephen J. Klaus

    发明人： Todd W. Seeley ,  David Y. Liu ,  Stephen J. Klaus

    IPC分类号： A61K31/198

    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。

    Compounds and methods to treat cardiac failure and other disorders
    9.
    发明授权
    Compounds and methods to treat cardiac failure and other disorders 有权
    治疗心力衰竭和其他疾病的化合物和方法

    公开(公告)号：US07189739B2

    公开(公告)日：2007-03-13

    申请号：US10076131

    申请日：2002-02-13

    申请人： Babu J. Mavunkel ,  David Y. Liu ,  George F. Schreiner ,  John A. Lewicki ,  John J. Perumattam

    发明人： Babu J. Mavunkel ,  David Y. Liu ,  George F. Schreiner ,  John A. Lewicki ,  John J. Perumattam

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D209/08 ,  C07D209/24 ,  C07D235/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04

    摘要： The invention is directed to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Ar1 is indole, benzimidazole, or benzotriazole, optionally substituted with lower alkyl (1–4C), halo, or lower alkoxy (1–4C); X1 is CO or an isostere thereof; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl; n is 0 or 1; Z is CH or N; X2 is CH, CH2 or an isostere thereof; and Ar2 consists of one or two phenyl moieties directly coupled to X2 and optionally substituted by halo, nitro, alkyl (1–6C), CN or CF3, or by RCO, COOR, CONR2, NR2, OR or SR, wherein R is H or alkyl (1–6C) or by phenyl, itself optionally substituted by the foregoing substituents; with the proviso that if Z is N, X1 is CO, and Ar1 is indole, Ar1 must be coupled to X1 through the 2-, 5-, 6- or 7-position. These compounds are useful in the treatment of conditions associated with inflammation. In addition, the above compounds and other compounds described herein are useful in treating conditions associated with cardiac failure.

    摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中Ar 1是吲哚，苯并咪唑或苯并三唑，任选被低级烷基（1-4C），卤素或低级烷氧基（ 1-4C）; X 1是CO或其等同体; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基; n为0或1; Z是CH或N; X 2是CH，CH 2或它们的等离子体; 和Ar 2由一个或两个直接与X 2连接的苯基部分组成，并且任选被卤素，硝基，烷基（1-6C），CN或CF 3或RCO，COOR，CONR 2，NR 2，OR或SR，其中R是H或烷基（1-6C）或苯基 本身任选被上述取代基取代; 条件是如果Z为N，则X 1为CO，Ar 1为吲哚，则Ar 1必须与X 1 通过2-，5-，6-或7-位。 这些化合物可用于治疗与炎症相关的病症。 此外，本文所述的上述化合物和其它化合物可用于治疗与心力衰竭相关的病症。

    Compounds and methods to treat cardiac failure and other disorders
    10.
    发明授权
    Compounds and methods to treat cardiac failure and other disorders 有权
    治疗心力衰竭和其他疾病的化合物和方法

    公开(公告)号：US06340685B1

    公开(公告)日：2002-01-22

    申请号：US09275176

    申请日：1999-03-24

    申请人： Babu J. Mavunkel ,  John A. Lewicki ,  David Y. Liu ,  George F. Schreiner ,  John J. Perumattam

    发明人： Babu J. Mavunkel ,  John A. Lewicki ,  David Y. Liu ,  George F. Schreiner ,  John J. Perumattam

    IPC分类号： A61K31496

    CPC分类号： C07D235/06 ,  C07D209/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

    摘要： A compound of the formula: and the pharmaceutically acceptable salts thereof, wherein each of Z1 and Z2 is independently CR4 or N; where each R4 is independently H or is alkyl (1-6C) optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by CN or ═O, or by an aliphatic or aromatic 5 or 6 membered ring optionally containing 1-2 N heteroatoms; or two R4 taken together form a bridge optionally containing a heteroatom; R1 is  wherein X1 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two 6 taken together may form an alkyene (2-3C) bridge; n is 0 or 2; Z3 is CH or N; X2 is CH, CH2 or an isostere thereof; and Ar consists of one or two phenyl moieties directly coupled to X2 optionally substituted by halo, nitro, alkyl (1-6C), alkenyl (1-6C), CN or CF3, or by RCO, COOR, CONR2, NR2, OR, SR, OOCR or NROCR wherein R is H or alkyl (1-6C) or by phenyl, itself optionally substituted by the foregoing substituents; R2 is H, or alkyl (1-6C) optionally including one heteroatom which is O, S or N, and optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by CN or ═O, or by an aliphatic or aromatic 5 or 6 membered ring optionally containing 1-2 N heteroatoms; R3 is H, halo, NO2, alkyl (1-6C), alkenyl (1-6C), CN, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C).

    摘要翻译： 下式化合物及其药学上可接受的盐，其中Z 1和Z 2各自独立地为CR 4或N;其中每个R 4独立地为H或烷基（1-6C），任选地包括一个或多个选自O，S 其中R是H或烷基（1-6C），或CN或= O，或被一个或多个选自下列基团取代：卤素，OR，SR，NR2，RCO，COOR，CONR2，OOCR或NROCR， 任选含有1-2个N杂原子的脂族或芳族5或6元环; R 2一起形成任选含有杂原子的桥; R 1是其中X 1是CO或其等同体; m是0或1; Y是任选取代的烷基，任选取代的芳基或任选取代的芳烷基或两个6一起形成 烷基（2-3C）桥; n为0或2; Z3为CH或N; X2为CH，CH2或其等同基团; 并且Ar由直接连接到X2上的一个或两个苯基部分，任选被卤素，硝基，烷基（1-6C），烯基（1-6C），CN或CF 3或RCO，COOR，CONR2，NR2，OR，SR ，OOCR或NROCR，其​​中R为H或烷基（1-6C）或苯基，其本身任选被前述取代基取代; R 2为H或任选包括一个为O，S或N的杂原子的烷基（1-6C） 并且任选被一个或多个卤素，OR，SR，NR 2，RCO，COOR，CONR 2，OOCR或NROCR取代，其中R是H或烷基（1-6C），或CN或= O，或被脂族或 芳香族5或6元环，任选地含有1-2个N杂原子; R3是H，卤素，NO2，烷基（1-6C），烯基（1-6C），CN，OR，SR，NR2，RCO，COOR，CONR2， OOCR或NROCR，其​​中R是H或烷基（1-6C）。