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    4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION
    5.
    发明公开
    4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 有权
    4-氨基-4-氧代哌嗪代谢物ALS HEMMER VIRALER REPLIKATION

    公开(公告)号：EP2041156A1

    公开(公告)日：2009-04-01

    申请号：EP07810457.7

    申请日：2007-07-13

    申请人： Achillion Pharmaceuticals, Inc.

    发明人： PHADKE, Avinash ,  WANG, Xiangzhu ,  ZHANG, Suoming ,  AGARWAL, Atul

    IPC分类号： C07K5/02 ,  C07K5/06 ,  A61K38/00 ,  C07K5/08

    CPC分类号： A61K38/05 ,  A61K38/00 ,  A61K38/12 ,  A61K45/06 ,  C07K5/02 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191 ,  C07K5/0808 ,  C07K5/12

    摘要： The invention rovides 4-amino-4-oxobutanoyl peptide compounds of Formula I (I) and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18 R19, n, M,, n, M,, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.

    摘要翻译： 本发明提供式I的4-氨基-4-氧代丁酰基肽化合物及其药用盐和水合物。 变量R 1 -R 9，R 16，R 18，R 19，n，M，，n，M，和Z在本文中定义。 某些式I的化合物可用作抗病毒剂。 本文公开的某些4-氨基-4-氧代丁酰肽化合物是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。 本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽化合物和一种或多种药学上可接受的载体的药物组合物。 这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽化合物作为唯一的活性剂，或者可以含有含有肽化合物的4-氨基-4-氧代丁酰肽与一种或多种其它药物活性剂的组合。 本发明还提供了用于治疗哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

    COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS
    6.
    发明公开
    COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS 有权
    VERBINDUNGEN ZUR BEHANDLUNG VON KOMPLEMENTVERMITTELTEN ERKRANKUNGEN

    公开(公告)号：EP3110805A1

    公开(公告)日：2017-01-04

    申请号：EP15755573.1

    申请日：2015-02-25

    申请人： Achillion Pharmaceuticals, Inc.

    发明人： PHADKE, Avinash, S. ,  WANG, Xiangzhu ,  CHEN, Dawei ,  HASHIMOTO, Akihiro ,  GADHACHANDA, Venkat, Rao ,  PAIS, Godwin ,  WANG, Qiuping ,  AGARWAL, Atul ,  DESHPANDE, Milind ,  WILES, Jason, Allan

    IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D471/04

    摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

    摘要翻译： 提供化合物，使用方法以及制备包含式I的补体因子D的抑制剂的方法或其药学上可接受的盐或组合物。 本文描述的抑制剂靶向因子D并且在替代补体途径的早期和必需点抑制或调节补体级联，并降低D因子调节经典和凝集素补体途径的能力。 本文所述的因子D的抑制剂能够减少与某些自身免疫性，炎性和神经变性疾病以及缺血 - 再灌注损伤和癌症相关的补体的过度活化。