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    Growth factor-binding compounds and methods of use
    3.
    发明申请
    Growth factor-binding compounds and methods of use 有权
    生长因子结合化合物和使用方法

    公开(公告)号：US20050197401A1

    公开(公告)日：2005-09-08

    申请号：US11044980

    申请日：2005-01-27

    申请人： Said Sebti ,  Andrew Hamilton ,  Rishi Jain

    发明人： Said Sebti ,  Andrew Hamilton ,  Rishi Jain

    IPC分类号： A61K31/195 ,  A61K47/48 ,  C07C237/42

    CPC分类号： B82Y5/00 ,  A61K47/54 ,  A61K47/6949

    摘要： Growth factor binding compounds having a plurality of acyclic isophthalic acid groups attached to a non-peptide organic scaffold and pharmaceutical compositions of the same are disclosed. Methods of administering and using the growth factor binding compounds or the growth factor binding compositions are also taught. These novel growth factor binding compounds are useful for treating angiogenesis, excessive cellular proliferation, tumor growth, and a combination thereof as well as inhibiting growth factor binding to cells and phosphorylation.

    摘要翻译： 公开了具有连接到非肽有机支架上的多个无环间苯二甲酸基团和其药物组合物的生长因子结合化合物。 还教导了施用和使用生长因子结合化合物或生长因子结合组合物的方法。 这些新的生长因子结合化合物可用于治疗血管发生，过度的细胞增殖，肿瘤生长及其组合以及抑制生长因子结合细胞和磷酸化。

    Compound and Methods For the Treatment of Cancer and Malaria
    5.
    发明申请
    Compound and Methods For the Treatment of Cancer and Malaria 审中-公开
    化合物和治疗癌症和疟疾的方法

    公开(公告)号：US20080312287A1

    公开(公告)日：2008-12-18

    申请号：US11886105

    申请日：2006-03-17

    申请人： Andrew Hamilton ,  Frederick Buckner ,  Matthew Glenn ,  Wesley Van Voorhis ,  Said Sebti

    发明人： Andrew Hamilton ,  Frederick Buckner ,  Matthew Glenn ,  Wesley Van Voorhis ,  Said Sebti

    IPC分类号： A61K31/4439 ,  C07D403/02 ,  A61K31/4178 ,  A61P35/00 ,  A61P33/06 ,  C07D401/02

    CPC分类号： C07D233/24 ,  C07D233/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14

    摘要： Formula (I): Where R1 is an optionally substituted C3-C12 hydrocarbyl group (preferably a cyclic alkyl group), an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R is a C(O)yR′ group (preferably forming an optionally substituted C2-C5 acyl group), or a S(O)xR′ group, where y is 0 or 1 and x is 0, 1 or 2 and R′ is H or an optionally substituted C1-C12 alkyl group, or R′ is an optionally substituted C5-C12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R5, R6, R7, R8, R9 and R10 are each independently selected from H, an optionally substituted C1-C12 hydrocarbyl group, including a C5-C12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group, or R5 and R6, R7 and R8 or R9 and R10 together form a keto (C═O) group; RN is H, an optionally substituted C1-C12 hydrocarbyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group, or an optionally substituted heteroaromatic group; A is Formula (II): a Formula (III): group, or a Formula (IV) or Formula (V) group, where Z is N, O or S; Ra is H, a C1-C12 optionally substituted hydrocarbyl group or an optionally substituted aromatic group; n is from 0 to 3; and pharmaceutically acceptable salts thereof. Compounds according to the invention are useful in one or more aspects to inhibit farnesyl transferase, or to treat malaria, neoplasia, a hyperproliferative disease state or arthritis, including rheumaroid arthritis or osteoarthritis.

    摘要翻译： 式（I）：其中R1是任选取代的C 3 -C 12烃基（优选环状烷基），任选取代的杂环基，任选取代的芳基或任选取代的杂芳基; R是C（O）y R'基团（优选形成任选取代的C 2 -C 5酰基）或S（O）x R'基团，其中y是0或1，x是0,1或2，R' 是H或任选取代的C 1 -C 12烷基，或R'是任选取代的C 5 -C 12环烷基，任选取代的杂环基，任选取代的芳基或任选取代的杂芳基; R5，R6，R7，R8，R9和R10各自独立地选自H，任选取代的C 1 -C 12烃基，包括C 5 -C 12环烷基，任选取代的杂环基，任选取代的芳族基团或任选取代的 杂芳基或R5和R6，R7和R8或R9和R10一起形成酮（CO）基团; RN为H，任选取代的C 1 -C 12烃基，任选取代的杂环基，任选取代的芳族基团或任选取代的杂芳族基团; A是式（II）：式（III）：基团，或式（IV）或式（V）基团，其中Z是N，O或S; Ra是H，C1-C12任选取代的烃基或任选取代的芳族基团; n为0〜3; 及其药学上可接受的盐。 根据本发明的化合物在一个或多个方面可用于抑制法呢基转移酶或治疗疟疾，瘤形成，过度增生性疾病状态或关节炎，包括风湿性关节炎或骨关节炎。

    Peptidomimetic inhibitors of STAT activity and uses thereof
    7.
    发明申请
    Peptidomimetic inhibitors of STAT activity and uses thereof 有权
    STAT活性的拟肽抑制剂及其用途

    公开(公告)号：US20050004009A1

    公开(公告)日：2005-01-06

    申请号：US10784309

    申请日：2004-02-20

    申请人： James Turkson ,  Richard Jove ,  Said Sebti ,  Andrew Hamilton

    发明人： James Turkson ,  Richard Jove ,  Said Sebti ,  Andrew Hamilton

    IPC分类号： A61K38/00 ,  A61K38/04 ,  A61P35/00 ,  C07K5/04 ,  C07K5/06 ,  C07K5/08 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/06191 ,  C07K5/0827

    摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention include compounds of the formula RY*L (where Y* represents phosphotyrosine), with the R group at the Y-1 position. Peptidomimetics of the invention disrupt Stat3 activation and function. Peptidomimetics of the invention significantly inhibit tumor cell growth and induce tumor cell death.

    摘要翻译： 本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。 本发明的组合物是抑制STAT功能的肽模拟物。 本发明的肽模拟物包括式RY * L（其中Y *表示磷酸酪氨酸）的化合物，其中R基团在Y-1位。 本发明的肽模拟物破坏Stat3的活化和功能。 本发明的肽模拟物显着抑制肿瘤细胞生长并诱导肿瘤细胞死亡。

    Growth factor binding molecules
    10.
    发明申请
    Growth factor binding molecules 有权

    公开(公告)号：US20060084596A1

    公开(公告)日：2006-04-20

    申请号：US11226112

    申请日：2005-09-14

    申请人： Said Sebti ,  Andrew Hamilton

    发明人： Said Sebti ,  Andrew Hamilton

    IPC分类号： A61K38/12 ,  C07K5/12

    CPC分类号： C07K7/56 ,  A61K38/00 ,  C07K14/001

    摘要： Growth factor binding molecules having a plurality of peptide loops attached to a non-peptide organic scaffold, preferably having pseudo-six amino acid peptide loops with four amino acid sidechains. The growth factor binding molecules specifically bind various growth factors and are suitable for treating a subject having tumors or restinosis. In one embodiment a platelet-derived growth factor binding molecule is disclosed that is used to inhibit tumor growth and angiogenesis in solid tumors.