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    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS
    43.
    发明申请
    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
    一致的约束，全合成大环化合物

    公开(公告)号：US20150051183A1

    公开(公告)日：2015-02-19

    申请号：US14385689

    申请日：2013-03-15

    申请人： POLYPHOR AG

    发明人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Arnaud Piettre ,  Jean-François Gosalbes ,  Marc Thommen

    IPC分类号： C07D273/02 ,  C07D498/18 ,  C07D515/08 ,  C07D498/08 ,  C07D291/08

    CPC分类号： C07D273/02 ,  C07D291/08 ,  C07D498/04 ,  C07D498/08 ,  C07D498/18 ,  C07D515/06 ,  C07D515/08 ,  C07D515/18 ,  C07D515/22

    摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

    摘要翻译： 式（I）的构象限制的空间定义的大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.由该环系统I描述的大环通过平行合成或组合化学在溶液中容易地制备 或固相。 它们被设计为与各种特异性生物靶标类型相互作用，例如对G-蛋白偶联受体（GPCR）具有激动作用或拮抗活性，对酶或抗微生物活性的抑制活性。 特别地，这些大环化合物显示对亚型1（ECE-1）和/或半胱氨酸蛋白酶组织蛋白酶S（CatS）的内皮素转化酶的抑制活性，和/或作为催产素（OT）受体的拮抗剂，促甲状腺激素释放激素 （TRH）受体和/或白三烯B4（LTB4）受体和/或作为铃蟾肽3（BB3）受体的激动剂，和/或显示针对至少一种细菌菌株的抗微生物活性。 因此，它们作为各种疾病的药物具有巨大的潜力。

    Ecteinascidin analogs for use as antitumour agents
    45.
    发明授权
    Ecteinascidin analogs for use as antitumour agents 有权
    用作抗肿瘤剂的抗坏血酸类抗生素

    公开(公告)号：US07763615B2

    公开(公告)日：2010-07-27

    申请号：US10485536

    申请日：2002-08-06

    申请人： Pilar Gallego ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Valentin Martinez

    发明人： Pilar Gallego ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Valentin Martinez

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D487/00 ,  C07D491/00 ,  C07D513/00

    CPC分类号： C07D515/22

    摘要： Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclic; wherein X is independently selected of OR′, CN, (═O), or H; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein m is 0, 1 or 2; and wherein n is 0, 1, 2, 3, or 4, and their use as antitumoral agent.

    摘要翻译： 基团R 1，R 2，R 3，R 4和R 5各自独立地选自H，OH，OR'，SH，SR'，SOR'，SO 2 R'，C的通式（I）的抗坏血酸素736衍生物 （= O）R'，C（= O）OR'，NO 2，NH 2，NHR'，N（R'）2，NHC（O）R'，CN，卤素，= O，取代或未取代的C 1 -C 25烷基 取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基，取代或未取代的杂环基; 其中X独立地选自OR'，CN，（= O）或H; 其中每个R'基团独立地选自H，OH，NO 2，NH 2，SH，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H， 未取代的C 1 -C 25烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基; 其中m为0,1或2; 并且其中n为0,1,2,3或4，并且其用作抗肿瘤剂。

    DIFLUOROMETHYL-CONTAINING MACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
    46.
    发明申请
    DIFLUOROMETHYL-CONTAINING MACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS 有权
    含有大分子化合物作为丙型肝炎病毒抑制剂

    公开(公告)号：US20090274657A1

    公开(公告)日：2009-11-05

    申请号：US12433191

    申请日：2009-04-30

    申请人： Yonghua Gai ,  Dong Liu ,  Joel D. Moore ,  Yat Sun Or ,  Zhe Wang

    发明人： Yonghua Gai ,  Dong Liu ,  Joel D. Moore ,  Yat Sun Or ,  Zhe Wang

    IPC分类号： A61K38/21 ,  C07D241/36 ,  A61K31/4985 ,  A61K31/70 ,  A61P31/12

    CPC分类号： C07D513/22 ,  C07D498/22 ,  C07D515/22

    摘要： The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。