Triazolopyridine Derivatives As Modulators of TNF Activity
    43.
    发明申请
    Triazolopyridine Derivatives As Modulators of TNF Activity 有权
    作为TNF活性调节剂的三唑并吡啶衍生物

    公开(公告)号:US20160304512A1

    公开(公告)日:2016-10-20

    申请号:US15101044

    申请日:2014-12-08

    CPC classification number: C07D471/04 A61K31/437 A61K31/506 A61K31/5377

    Abstract: A series of substituted [1,2,4]triazolo[4,3-a]pyridine derivatives, being potent modulators of human TNF activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

    Abstract translation: 因此,作为人类TNF活性的有效调节剂的一系列取代的[1,2,4]三唑并[4,3-a]吡啶衍生物在治疗和/或预防各种人类疾病中是有益的,包括自身免疫和炎症 疾病; 神经和神经退行性疾病; 疼痛和伤害性疾病; 心血管疾病; 代谢紊乱 眼部疾病; 和肿瘤疾病。

    METHOD FOR THE TREATMENT OF FIBROTIC DISEASE
    47.
    发明申请
    METHOD FOR THE TREATMENT OF FIBROTIC DISEASE 审中-公开
    治疗纤维性疾病的方法

    公开(公告)号:US20160200820A1

    公开(公告)日:2016-07-14

    申请号:US14914673

    申请日:2014-08-26

    Inventor: Diane MARSHALL

    Abstract: The present invention relates generally to methods of treating fibrotic disease and more specifically to an inhibitor of CSF-1R activity for the treatment and/or prophylaxis of fibrotic disease, wherein the inhibitor comprises a small chemical entity (NCE), a nucleic acid or an antibody or functionally active fragment or derivative thereof. The present invention further pertains to the use of an inhibitor of CSF-1R activity, for the manufacture of a medicament for the treatment and/or prophylaxis of fibrotic disease.

    Abstract translation: 本发明一般涉及治疗纤维化疾病的方法,更具体地涉及用于治疗和/或预防纤维化疾病的CSF-1R活性抑制剂,其中所述抑制剂包括小化学实体(NCE),核酸或 抗体或其功能活性片段或衍生物。 本发明还涉及CSF-1R活性抑制剂在制备用于治疗和/或预防纤维化疾病的药物中的应用。

    PD-1 ANTIBODIES
    48.
    发明申请
    PD-1 ANTIBODIES 有权
    PD-1抗体

    公开(公告)号:US20160068586A1

    公开(公告)日:2016-03-10

    申请号:US14802076

    申请日:2015-07-17

    Abstract: A humanised agonistic antibody which binds human PD-1 comprising a heavy chain and a light chain wherein the variable domain of the heavy chain comprises the sequence given in SEQ ID NO:1 for CDR-H1, the sequence given in SEQ ID NO:2 for CDR-H2 and the sequence given in SEQ ID NO:3 for CDR-H3 and the variable domain of the light chain comprises the sequence given in SEQ ID NO:4 for CDR-L1, the sequence given in SEQ ID NO:5 for CDR-L2 and the sequence given in SEQ ID NO:7 for CDR-L3. The invention also extends to therapeutic uses of the antibody molecules, compositions and methods for producing said antibody molecules.

    Abstract translation: 结合包含重链和轻链的人PD-1的人源化激动抗体,其中重链的可变结构域包含SEQ ID NO:1中针对CDR-H1给出的序列,SEQ ID NO:2中给出的序列 对于CDR-H2和CDR-H3的SEQ ID NO:3中给出的序列,轻链的可变结构域包含SEQ ID NO:4中针对CDR-L1给出的序列,SEQ ID NO:5中给出的序列 对于CDR-L2和针对CDR-L3的SEQ ID NO:7中给出的序列。 本发明还延伸到抗体分子的治疗用途,用于产生所述抗体分子的组合物和方法。

    Single Linker FabFv Antibodies and Methods of Producing Same
    50.
    发明申请
    Single Linker FabFv Antibodies and Methods of Producing Same 审中-公开
    单链接FabFv抗体及其生产方法

    公开(公告)号:US20160017057A1

    公开(公告)日:2016-01-21

    申请号:US14654240

    申请日:2013-12-20

    Abstract: The present disclosure relates to a multi-specific antibody molecule comprising or consisting of three polypeptides: a) a polypeptide chain of formula (I): (Vxx)nVx-Cx-X—V1; and b) a polypeptide chain of formula (II): (Vyy)nVy-Cy c) a polypeptide of formula (III):V2 wherein Vx represents a variable domain, Vxx represents a variable domain, Cx represents a constant region, X represents a linker, V represents a variable domain, Vy represents a variable domain, Vyy represents a variable domain, Cy represents a constant region, V2 represents a variable domain, n independently represents 0 or 1, wherein the polypeptide chain of formula (I) and the polypeptide chain of formula (II) is aligned such that the constant regions Cx and Cy are paired and the variable domains Vx and Vy are paired to form a binding domain and optionally a disulphide bond is present between V and V2, in particular where a disulphide bond is present. The disclosure also extends to pharmaceutical formulation comprising the construct, DNA encoding the constructs and vectors comprising same. The disclosure further extends to a method of expressing the constructs, for example in a host cell and methods for formulating same as a pharmaceutical composition. The disclosure also relates to use of the constructs and formulations in treatment.

    Abstract translation: 本公开涉及包含三种多肽或由以下三种多肽组成的多特异性抗体分子:a)式(I)的多肽链:(Vxx)nVx-Cx-X-V1; b)式(II)的多肽链:(Vyy)nVy-Cy c)式(III)的多肽:V2其中Vx表示可变结构域,Vxx表示可变结构域,Cx表示恒定区,X表示 接头,V表示可变结构域,Vy表示可变结构域,Vyy表示可变结构域,Cy表示恒定区,V2表示可变结构域,n独立地表示0或1,其中式(I)的多肽链和 排列式(II)的多肽链使得恒定区Cx和Cy配对,并且可变结构域Vx和Vy配对形成结合结构域,并且任选地在V和V 2之间存在二硫键,特别是其中 存在二硫键。 本公开还延伸到包含构建体的药物制剂,编码构建体的DNA和包含其的载体。 本公开进一步扩展到表达构建体的方法,例如在宿主细胞中的方法以及用于配制药物组合物的方法。 本公开还涉及在治疗中使用构建体和制剂。

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