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    QUINOXALINE-CONTAINING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
    7.
    发明申请
    QUINOXALINE-CONTAINING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS 审中-公开
    含喹啉的化合物作为丙型肝炎病毒抑制剂

    公开(公告)号：WO2009064975A1

    公开(公告)日：2009-05-22

    申请号：PCT/US2008/083541

    申请日：2008-11-14

    Applicant: ENANTA PHARMACEUTICALS, INC. ,  GAI, Yonghua ,  OR, Yat, Sun ,  WANG, Zhe

    Inventor： GAI, Yonghua ,  OR, Yat, Sun ,  WANG, Zhe

    IPC: A01N43/60 ,  A61K31/495

    CPC classification number: C07K5/1027 ,  C07D498/18 ,  C07D498/22 ,  C07K5/0827 ,  C07K5/1021

    Abstract: The present invention discloses compounds of formula I and II 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.

    Abstract translation: 本发明公开了抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶活性的式I和II化合物或其药学上可接受的盐，酯或前药。 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。

    TRIAZOLYL MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS
    9.
    发明申请
    TRIAZOLYL MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
    三氮唑大环内酯类C丝氨酸蛋白酶抑制剂

    公开(公告)号：WO2008021960A3

    公开(公告)日：2008-11-06

    申请号：PCT/US2007075588

    申请日：2007-08-09

    Applicant: ENANTA PHARM INC ,  SUN YING ,  NIU DEQIANG ,  OR YAT SUN ,  WANG ZHE

    Inventor： SUN YING ,  NIU DEQIANG ,  OR YAT SUN ,  WANG ZHE

    IPC: A61K38/12

    CPC classification number: C07K5/0804 ,  A61K38/21 ,  C07K5/0827 ,  A61K2300/00

    Abstract: The present invention relates to compounds of Formula I or II, 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 to the subject a pharmaceutical composition comprising a compound of the present invention.

    Abstract translation: 本发明涉及式I或II的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，本发明化合物干扰丙型肝炎病毒的生命周期，并且也可用作抗病毒剂。 本发明进一步涉及包含前述化合物的药物组合物，用于给予患有HCV感染的受试者。 本发明还涉及通过向受试者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。

    PEPTIDES FOR ACTIVATION OF ANGIOGENESIS, PHARMACEUTICAL COMPOUNDS CONTAINING SAME AND USE OF THESE COMPOUNDS
    10.
    发明申请
    PEPTIDES FOR ACTIVATION OF ANGIOGENESIS, PHARMACEUTICAL COMPOUNDS CONTAINING SAME AND USE OF THESE COMPOUNDS 审中-公开
    用于激活血管生成的药物，含有它们的药物化合物和这些化合物的使用

    公开(公告)号：WO2008050161A2

    公开(公告)日：2008-05-02

    申请号：PCT/HU2007/000095

    申请日：2007-10-19

    Applicant: Biostatin Gyógyszerkutató-Fejlesztö Kft. ,  HORVÁTH, Anikó ,  KÉRI, György ,  TÓVÁRI, József ,  SEPRÖDI, János ,  VÁNTUS, Tibor ,  KENESSEY, István ,  IDEI, Miklós ,  TANAI, Gyula Sándorné

    Inventor： HORVÁTH, Anikó ,  KÉRI, György ,  TÓVÁRI, József ,  SEPRÖDI, János ,  VÁNTUS, Tibor ,  KENESSEY, István ,  IDEI, Miklós ,  TANAI, Gyula Sándorné

    IPC: C07K5/062 ,  C07K5/068 ,  C07K5/087 ,  C07K5/093 ,  C07K5/11 ,  C07K5/117 ,  C07K14/52 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/19

    CPC classification number: C07K14/52 ,  A61K38/00 ,  C07K5/0606 ,  C07K5/06086 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/0827 ,  C07K5/1019 ,  C07K5/1027 ,  Y02P20/55

    Abstract: The invention provides novel peptides of formula (I) and their salts or metal complexes R0- R1- Q(X) - R2- R3 (I) - wherein the main substituent meanings are as follows: Q represents Lys, Cys or Ser; X is H, Bzl, R0, R0-Tyr-Pro-Asp-Glu-Ile-Glu-Tyr-Ile-Phe, R0- Ile-Lys-Pro-His- Gln-Gly-Gln, or R0- Gly-Val-Ser-Ser-Ser-Ser, R 0 stands for H or NH2-protecting groups commonly used in peptide chemistry, R 1 is Trp, D-Trp, Phe, D-Phe, ß-Asp(a-Dopa), ß-Asp(a-Ind), Tyr-Pro-Asp- Glu-Ile-Glu-Tyr-Ile-Phe, Ile-Lys-Pro-His-Gln-Gly-Gln, Pro-Glu-Ser-Thr- Asn-Leu, Gly-Val-Ser-Ser-Ser-Ser, or a valency bond, R 2 represents Gly, Asn-Asp-Glu-Gly-Leu-Glu-(Gly) n, Asp-Asp-Gly-Gln-Ile-(Gly) n, His, Ser, Cpa, Dopa, Tyr, Thr, Pro, Trp-Ser, Phe-Ser, 2-aminophenyl-, or Cys(X2), wherein X2 is Acm, Bzl or an SH-protecting group commonly used in peptide chemistry, and R 3 is OH, OMe, NH2, or amide substituted by one or two identical or different C1-C6 alkyl group(s), Thr-NH2, or Tyr-OMe. The invention further provides pharmaceutical compositions containing these peptides with the ability of stimulating angiogenesis and vascularization. The invention further relates to the use of these compounds for preparing pharmaceutical compositions for treatment of injured tissues such as chronic wounds, heart tissues injured by ischemia or heart attack, and neural tissues injured by stroke. The invention also relates to a method for preparing tissue samples for testing angiogenesis-inhibiting agents.

    Abstract translation: 本发明提供式（I）的新型肽及其盐或金属络合物R0-R1-Q（X）-RR2-R3（Ⅰ） - 其中主要取代基含义如下：Q代表Lys，Cys或Ser; X是H，Bz1，R0，R0-Tyr-Pro-Asp-Glu-Ile-Glu-Tyr-Ile-Phe，R0-Ile-Lys-Pro-His-Gln-Gly-Gln或R0-Gly-Val -Ser-Ser-Ser-Ser，R 0代表肽化学中通常使用的H或NH 2保护基团，R 1是Trp，D-Trp，Phe， D-Phe，ß-Asp（a-Dopa），ß-Asp（a-Ind），Tyr-Pro-Asp-Glu-Ile-Glu-Tyr-Ile-Phe，Ile-Lys-Pro-His-Gln- Gly-Gln，Pro-Glu-Ser-Thr-Asn-Leu，Gly-Val-Ser-Ser-Ser-Ser或价键，R 2代表Gly，Asn-Asp-Glu -Gly-Leu-Glu-（Gly）n，Asp-Asp-Gly-Gln-Ile-（Gly）n，His，Ser，Cpa，Dopa，Tyr，Thr，Pro，Trp-Ser，Phe-Ser， - 氨基苯基 - 或Cys（X2），其中X2是肽化学中通常使用的Acm，Bzl或SH保护基，R 3是OH，OMe，NH 2或被一个 或两个相同或不同的C 1 -C 6烷基，Thr-NH 2或Tyr-OMe。 本发明进一步提供含有能刺激血管生成和血管形成的这些肽的药物组合物。 本发明还涉及这些化合物用于制备用于治疗受伤组织如慢性伤口，由缺血或心脏病发作损伤的心脏组织以及由中风损伤的神经组织的药物组合物的用途。 本发明还涉及一种用于制备用于测试血管发生抑制剂的组织样品的方法。

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