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89 条记录 (耗时 0.033 秒)

    Cyclopeptide derivatives with anti-integrin activity
    16.
    发明申请
    Cyclopeptide derivatives with anti-integrin activity 审中-公开
    具有抗整联蛋白活性的环肽衍生物

    公开(公告)号：US20070178045A1

    公开(公告)日：2007-08-02

    申请号：US11596190

    申请日：2005-05-04

    申请人： Claudio Pisano ,  Giuseppe Giannini ,  Maria Omelia Tinti ,  Loredana Vesci ,  Sergio Penco ,  Alma Dal Pozzo ,  Ni Minghong

    发明人： Claudio Pisano ,  Giuseppe Giannini ,  Maria Omelia Tinti ,  Loredana Vesci ,  Sergio Penco ,  Alma Dal Pozzo ,  Ni Minghong

    IPC分类号： A61K38/12 ,  A61K103/32 ,  A61K51/08

    CPC分类号： C07K5/12 ,  A61K38/00 ,  C07K7/64

    摘要： Formula (I) compounds are described c(R1-Arg-Gly-Asp-R2) where the meanings of the various groups are as described here below, which are integrin inhibitors, and particularly inhibitors of integrins of the α,β3 and α,β5 family, and therefore are useful as medicaments, particularly for the treatment of the diseases underlying abnormal angiogenesis, such as retinopathy, acute renal failure, osteoporosis and metastases. The compounds described herein, when suitably labelled, are also useful as diagnostic agents, especially for the detection of small tumour masses and arterial occlusion events, and as targeted drug vectors.

    摘要翻译： 式（I）化合物描述为其中各种基团的含义如下所述的c（R 1 -Arg-Gly-Asp-R 2） 整合素抑制剂，特别是α，β3和α，β5家族的整联蛋白的抑制剂，因此可用作药物，特别是用于治疗潜在的疾病 异常血管发生，如视网膜病变，急性肾衰竭，骨质疏松症和转移。 本文所述的化合物在适当标记时也可用作诊断剂，特别是用于检测小肿瘤块和动脉闭塞事件以及作为靶向药物载体。

    Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives
    17.
    发明授权
    Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives 失效
    用7-取代的喜树碱衍生物抑制肿瘤生长的方法

    公开(公告)号：US06306868B1

    公开(公告)日：2001-10-23

    申请号：US09643256

    申请日：2000-08-22

    申请人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

    发明人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

    IPC分类号： A61K31436

    CPC分类号： C07D491/22

    摘要： Compounds of formula (I), wherein: R1 is —CN, —CH(CN)—R4, —CH═C(CN)—R4, —CH2—CH(CN)—R4, —C(═NOH)—NH2, —C(═NH)—NH2, —CH═C(NO2)—R4, —CH(CN)—R5, —CH(CH2NO2)—R5; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R2 is hydrogen; R3 is hydrogen, OR6; R4 is hydrogen, C1-C6 linear or branched alkyl, CN, COOR7; R5 is hydrogen, OR8; R6 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl, (C6-C12) aryl (C2-C4) acyl, (C2-C4) acyl, amino (C1-C4) alkyl, amino (C2-C4) acyl, glycosyl; R7 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl; R8 has the same meanings of R6, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

    摘要翻译： 式（I）化合物，其中：R1是-CN，-CH（CN）-R4，-CH = C（CN）-R4，-CH2-CH（CN）-R4，-C（= NOH） ，-C（= NH）-NH 2，-CH = C（NO 2）-R 4，-CH（CN）-R 5，-CH（CH 2 NO 2） 5-四唑基，2-（4,5-二氢恶唑基），1,2,4-恶二唑啉-3-基-5-酮; R2是氢; R3是氢，OR6; R4是氢，C1-C6直链或支链烷基，CN，COOR7; R5是氢，OR8; R6是氢，C1-C6直链或支链烷基，（C6-C12）芳基（C1-C4）烷基，（C1-C4）烷氧基（C1-C4）烷基，（C1-C4） ，（C 6 -C 12）芳基（C 2 -C 4）酰基，（C 2 -C 4）酰基，氨基（C 1 -C 4）烷基，氨基（C 2 -C 4）酰基，糖基; R7是氢，C1-C6直链或支链烷基，（C6-C12）芳基（C1-C4）烷基，（C1-C4）烷氧基（C1-C4）烷基，（C1-C4） ; R8与R6具有相同的含义，独立于后者。 这些化合物作为拓扑异构酶I抑制剂是有活性的，可用作抗肿瘤药物。

    3-aryl-glycidic ester derivatives
    19.
    发明授权
    3-aryl-glycidic ester derivatives 失效
    3-芳基 - 缩水甘油酯衍生物

    公开(公告)号：US5436235A

    公开(公告)日：1995-07-25

    申请号：US16980

    申请日：1993-02-12

    申请人： Franco Buzzetti ,  Maria G. Brasca ,  Silvia Fustinoni ,  Sergio Penco

    发明人： Franco Buzzetti ,  Maria G. Brasca ,  Silvia Fustinoni ,  Sergio Penco

    IPC分类号： A61K31/335 ,  A61K31/336 ,  A61K31/40 ,  A61K31/47 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  C07D303/48 ,  C07D405/04 ,  C07D27/56

    CPC分类号： C07D405/04 ,  C07D303/48

    摘要： The present invention relates to 3-aryl-oxirane derivatives of the formula ##STR1## wherein Ar is 4'-quinoline or 5'-quinoline; each of R and R.sub.1 independently is hydrogen or C.sub.1 -C.sub.6 alkoxy; one of X and Y is hydrogen, cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, and the other of X and Y is cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, wherein R.sub.2 is C.sub.1 -C.sub.6 alkyl and each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors, in particular as anti-proliferative agents, typically as anti-cancer agents, in the treatment of psoriasis and in inhibiting the development of atheromatous plaque.

    摘要翻译： 本发明涉及式为“IMAGE”的3-芳基 - 环氧乙烷衍生物，其中Ar为4'-喹啉或5'-喹啉; R和R 1各自独立地是氢或C 1 -C 6烷氧基; X和Y中的一个是氢，氰基，-COOR 2或-CONR 3 R 4，X和Y中的另一个是氰基，-COOR 2或-CONR 3 R 4，其中R 2是C 1 -C 6烷基，R 3和R 4各自独立地是氢或C 1 -C6烷基和其药学上可接受的盐，其可用于治疗作为酪氨酸激酶抑制剂，特别是作为抗增殖剂（通常作为抗癌剂）用于治疗牛皮癣和抑制动脉粥样硬化斑块发展。