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    ALPHA HELIX MIMETICS AND METHODS RELATING THERETO
    64.
    发明申请
    ALPHA HELIX MIMETICS AND METHODS RELATING THERETO 有权
    ALPHA HELIX的MIME类型和方法相关

    公开(公告)号：US20150368262A1

    公开(公告)日：2015-12-24

    申请号：US14720690

    申请日：2015-05-22

    Applicant: PRISM BioLab Co., Ltd.

    Inventor： Takenao Odagami ,  Yuji Kogami ,  Hiroyuki Kouji

    IPC: C07D495/14 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14

    CPC classification number: C07D495/14 ,  C07D401/14 ,  C07D403/14 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07D498/04

    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.

    Abstract translation: 公开了通式（I）表示的α-螺旋模拟结构和化合物，其中通式和各符号的定义如说明书中所定义，与之有关的化学文献及其相关方法。 还公开了这些化合物在治疗医学病症例如癌症疾病，纤维化疾病和包含模拟物的药物组合物中的应用。

    Thienopyrimidine Compounds
    66.
    发明申请
    Thienopyrimidine Compounds 有权
    噻吩并嘧啶化合物

    公开(公告)号：US20150342953A1

    公开(公告)日：2015-12-03

    申请号：US14803214

    申请日：2015-07-20

    Applicant: Vernalis (R&D) Ltd.

    Inventor： Allan Jordan ,  Simon Bedford ,  Klenke Burkhard ,  Ian Yule ,  Karine Poullennec

    IPC: A61K31/519

    CPC classification number: C07D495/04 ,  A61K31/519 ,  C07D495/14

    Abstract: Compounds of formula (I) are A2B receptor antagonists: Wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.

    Abstract translation: 式（I）化合物是A2B受体拮抗剂：其中R1是任选取代的芳基或任选取代的5或6元杂芳基环; R2和R3独立地选自氢，C1-C6烷基，C3-C8环烷基，C3-C8环烷基 - （C1-C6） - 烷基，在其环部分任意取代的芳基 - （C 1 -C 6） - 烷基， 任选通过C1-C6亚烷基链连接并任选在其环部分取代的5-或6-元单环杂环基，苯并咪唑-2-基 - 甲基，吡啶-3-基 - 羰基或（1-甲基 - 哌啶 -4-基） - 羰基 - 甲基; 或者R 2和R 3与它们所连接的氮原子一起形成任选取代的5-或6-元环; R 4是C 1 -C 3烷基，C 2 -C 3烯基， - （ - R 5）-R 6或任选取代的杂芳基甲基氨基; 并且R 5和R 6独立地选自氢或C 1 -C 3烷基; 或者R 5和R 6与它们所连接的氮原子一起形成任选取代的4至6元饱和环。

    Tricyclic fused thiophene derivatives as JAK inhibitors
    68.
    发明授权
    Tricyclic fused thiophene derivatives as JAK inhibitors 有权
    三环稠合噻吩衍生物作为JAK抑制剂

    公开(公告)号：US09181271B2

    公开(公告)日：2015-11-10

    申请号：US14068796

    申请日：2013-10-31

    Applicant: Incyte Corporation ,  Incyte Holdings Corporation

    Inventor： Yun-Long Li ,  Wenyu Zhu ,  Song Mei

    IPC: C07D495/12 ,  C07D495/14

    CPC classification number: C07D495/14 ,  A61K31/437 ,  C07D495/12

    Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

    Abstract translation: 本发明提供三环稠合噻吩衍生物及其组合物和使用方法，其调节Janus激酶（JAK）的活性，并且可用于治疗与JAK的活性相关的疾病，包括例如炎症性疾病 ，自身免疫性疾病，癌症等疾病。

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