Blood coagulation factor inhibitors
    1.
    发明授权
    Blood coagulation factor inhibitors 有权
    凝血因子抑制剂

    公开(公告)号:US08486892B2

    公开(公告)日:2013-07-16

    申请号:US12811854

    申请日:2009-01-22

    摘要: The invention relates to novel compounds with formula (I) X1-X2-X3-X4-X5-(X6)n-(X7)m-Y useful as blood coagulation factor inhibitors. The compounds (I) may be used for treatment of thrombotic conditions or as stabilizers of liquid formulations of blood coagulation factors, in particular liquid formulations of FVIIa, Factor VII variants, or Factor VII derivatives.

    摘要翻译: 本发明涉及可用作凝血因子抑制剂的式(I)X1-X2-X3-X4-X5-(X6)n-(X7)m-Y的新型化合物。 化合物(I)可用于治疗血栓形成状况或作为血液凝固因子的液体制剂的稳定剂,特别是FVIIa,因子VII变体或因子VII衍生物的液体制剂。

    Substituted piperidines
    6.
    发明授权
    Substituted piperidines 失效
    取代的哌啶

    公开(公告)号:US07064135B2

    公开(公告)日:2006-06-20

    申请号:US10267620

    申请日:2002-10-09

    摘要: A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

    摘要翻译: 一类新的取代的哌啶,包含它们的药物组合物及其用于治疗与组胺H3受体有关的疾病和病症的用途。 更具体地说,这些化合物可用于治疗与组胺H3受体相互作用有益的疾病和病症。

    PROCESS FOR THE PREPARATION OF ENOLATE SALTS OF 4-FLUORO-2-HYDROXYMETHYLENE-3 OXO-BUTYRATES
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF ENOLATE SALTS OF 4-FLUORO-2-HYDROXYMETHYLENE-3 OXO-BUTYRATES 有权
    制备4-氟-2-羟基乙烯基-3-氧代丁酸酯的增稠盐的方法

    公开(公告)号:US20130338394A1

    公开(公告)日:2013-12-19

    申请号:US13809739

    申请日:2011-07-11

    IPC分类号: C07C67/31 C07C69/14

    摘要: Enolate salts of 4-fluoro-2-hydroxymethylene-3-oxobutyrates of formula wherein R1 is C1-10 alkyl, R2 and R3 are independently hydrogen or fluorine, M is an alkali or alkaline earth metal, and n is 1 or 2, are prepared from enolate salts of the corresponding 4-fluoro-3-oxobutyrates and carbon monoxide. The enolate salts of formula I can be alkylated or acylated to obtain the corresponding enol ethers and esters. The 4-fluoro-3-oxobutyrate starting material can be prepared from 1,1-difluoroethyl methyl ethers by SbF5-catalyzed fluoromethane elimination followed by halogen exchange with lithium chloride, reacting the thus obtained fluoroacetyl chloride with ketene and quenching with the appropriate alcohol R1—OH.

    摘要翻译: 4-氟-2-羟基亚甲基-3-氧代丁酸烯醇盐,其中R 1是C 1-10烷基,R 2和R 3独立地是氢或氟,M是碱金属或碱土金属,n是1或2是 由相应的4-氟-3-氧代丁酸乙酯和一氧化碳的烯醇盐制备。 式I的烯醇盐可以被烷基化或酰化以得到相应的烯醇醚和酯。 4-氟-3-氧代丁酸酯原料可以由1,1-二氟乙基甲基醚通过SbF 5催化的氟甲烷消除制备,随后与氯化锂进行卤素交换,使得到的氟乙酰氯与乙烯酮反应,并用适当的醇R 1 -哦。

    Stabilisation of Liquid-Formulated Factor VII(A) Polypeptides by Aldehyde-Containing Compounds
    9.
    发明申请
    Stabilisation of Liquid-Formulated Factor VII(A) Polypeptides by Aldehyde-Containing Compounds 审中-公开
    通过含醛化合物稳定液体配制因子VII(A)多肽

    公开(公告)号:US20100303786A1

    公开(公告)日:2010-12-02

    申请号:US12743612

    申请日:2008-11-21

    IPC分类号: A61K38/48 A61P7/04

    摘要: The present invention is directed to liquid, aqueous pharmaceutical compositions stabilised against chemical and/or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The main embodiment is represented by a liquid, aqueous pharmaceutical composition comprising at least 0.01 mg/mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 4.0 to about 9.0; and at least one stabilising agent (iii) comprising a R—CHO motif, e.g. Benzaldehyde, 3-hydroxybenzaldehyde, 4-hydroxybenzaldehyde, or 5-formyl-4-methylimidazole.

    摘要翻译: 本发明涉及针对含有因子VII多肽的化学和/或物理降解稳定的液体水性药物组合物,以及用于制备和使用这些组合物的方法以及含有该组合物的小瓶,以及这些组合物在治疗中的用途 的因子VII反应综合征。 主要实施方案由包含至少0.01mg / mL的因子VII多肽(i)的液体含水药物组合物表示; 适于将pH保持在约4.0至约9.0范围内的缓冲剂(ii); 和至少一种包含R-CHO基序的稳定剂(iii),例如 苯甲醛,3-羟基苯甲醛,4-羟基苯甲醛或5-甲酰基-4-甲基咪唑。