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    Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
    1.
    发明授权
    Substituted pyrido[2,3-B]pyrazines as IP receptor agonists 有权
    取代的吡啶并[2,3-B]吡嗪作为IP受体激动剂

    公开(公告)号：US09132127B2

    公开(公告)日：2015-09-15

    申请号：US14265943

    申请日：2014-04-30

    申请人： Steven John Charlton ,  Catherine LeBlanc ,  Stephen Carl McKeown

    发明人： Steven John Charlton ,  Catherine LeBlanc ,  Stephen Carl McKeown

    IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/4375 ,  C07D471/04

    CPC分类号： A61K31/4985 ,  A61K31/4375 ,  C07D471/04

    摘要： The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.

    摘要翻译： 本发明提供活化IP受体的杂环衍生物。 激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。 还包括包含这些衍生物的药物组合物。 本发明化合物的实例包括根据式Ia的化合物或其药学上可接受的盐，以及实施例的化合物。

    Pyrido[2,3-b]pyrazine compounds useful as IP receptor agonist
    2.
    发明授权
    Pyrido[2,3-b]pyrazine compounds useful as IP receptor agonist 有权
    可用作IP受体激动剂的吡啶并[2,3-b]吡嗪化合物

    公开(公告)号：US08754085B2

    公开(公告)日：2014-06-17

    申请号：US13388819

    申请日：2011-07-14

    申请人： Steven John Charlton ,  Catherine Leblanc ,  Stephen Carl McKeown

    发明人： Steven John Charlton ,  Catherine Leblanc ,  Stephen Carl McKeown

    IPC分类号： A61K31/495

    CPC分类号： A61K31/4985 ,  A61K31/4375 ,  C07D471/04

    摘要： The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.

    摘要翻译： 本发明提供活化IP受体的杂环衍生物。 激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。 还包括包含这些衍生物的药物组合物。 本发明化合物的实例包括根据式Ia的化合物或其药学上可接受的盐，以及实施例的化合物。

    Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
    3.
    发明授权
    Substituted pyrido[2,3-B]pyrazines as IP receptor agonists 有权
    取代的吡啶并[2,3-B]吡嗪作为IP受体激动剂

    公开(公告)号：US09115129B2

    公开(公告)日：2015-08-25

    申请号：US14371585

    申请日：2013-01-11

    申请人： Steven John Charlton ,  Catherine Leblanc ,  Stephen Carl McKeown

    发明人： Steven John Charlton ,  Catherine Leblanc ,  Stephen Carl McKeown

    IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/4985

    摘要： The present invention provides substituted pyrido[2,3-b]pyrazines which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such substituted pyride[2,3-b]pyrazines are also encompassed.

    摘要翻译： 本发明提供活化IP受体的取代的吡啶并[2,3-b]吡嗪。 激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。 还包括包含这种取代的吡啶并[2,3-b]吡嗪的药物组合物。

    IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS
    4.
    发明申请
    IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS 有权
    IP受体激动剂杂环化合物

    公开(公告)号：US20130102611A1

    公开(公告)日：2013-04-25

    申请号：US13388819

    申请日：2011-07-14

    申请人： Steven John Charlton ,  Catherine Leblanc ,  Stephen Carl McKeown

    发明人： Steven John Charlton ,  Catherine Leblanc ,  Stephen Carl McKeown

    IPC分类号： C07D471/04

    CPC分类号： A61K31/4985 ,  A61K31/4375 ,  C07D471/04

    摘要： The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.

    摘要翻译： 本发明提供活化IP受体的杂环衍生物。 激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。 还包括包含这些衍生物的药物组合物。 本发明化合物的实例包括根据式Ia的化合物或其药学上可接受的盐，以及实施例的化合物。

    Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
    10.
    发明授权
    Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 失效
    双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂

    公开(公告)号：US06169091A

    公开(公告)日：2001-01-02

    申请号：US09051324

    申请日：1998-08-26

    申请人： George Stuart Cockerill ,  Stephen Barry Guntrip ,  Stephen Carl McKeown ,  Martin John Page ,  Kathryn Jane Smith ,  Sadie Vile ,  Alan Thomas Hudson ,  Paul Barraclough ,  Karl Witold Franzmann

    发明人： George Stuart Cockerill ,  Stephen Barry Guntrip ,  Stephen Carl McKeown ,  Martin John Page ,  Kathryn Jane Smith ,  Sadie Vile ,  Alan Thomas Hudson ,  Paul Barraclough ,  Karl Witold Franzmann

    IPC分类号： C07D48704

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R3 is a group ZR4 wherein Z is joined to R4 through a (CH2)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR′), V(CHR) or V where R and R′ are each C1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O)m or NRb where Rb is hydrogen or Rb is C1-4 alkyl; and R4 is an optionally substituted C3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R3 is a group ZR4 in which Z is NRb, and NRb and R4 together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors. The compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.

    摘要翻译： 取代的式（A）的杂芳族化合物，其中X是N或CH; 其中（a）表示稠合的5,6或7-元杂环，R3是基团ZR4，其中Z通过其中p为0,1或2的（CH 2）p基团连接到R 4，Z表示 组V（CH 2），V（CF 2），（CH 2）V，（CF 2）V，V（CRR'），V（CHR）或V其中R和R'各自是C 1-4烷基，其中V是 羰基，二羰基，CH（OH），CH（CN），磺酰胺，酰胺，O，S（O）m或NR b，其中R b是氢或R b是C 1-4烷基; 并且R 4是任选取代的C 3-6环烷基或任选取代的5,6,7,8,9或10元碳环或杂环部分; 或R3是Z Z4，其中Z是NRb，NRb和R4一起形成任选取代的5,6,7,8,9或10元碳环或杂环部分是蛋白质酪氨酸激酶抑制剂。 描述了这些化合物，以及其制备方法，包括这些化合物的药物组合物及其在医学中的用途，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，变态反应，哮喘，移植排斥，炎症 ，血栓形成，神经系统疾病和癌症。