BIOMARKER DISCOVERY IN COMPLEX BIOLOGICAL FLUID USING BEAD OR PARTICLE BASED LIBRARIES AND DIAGNOSTIC KITS AND THERAPEUTICS
    2.
    发明申请
    BIOMARKER DISCOVERY IN COMPLEX BIOLOGICAL FLUID USING BEAD OR PARTICLE BASED LIBRARIES AND DIAGNOSTIC KITS AND THERAPEUTICS 审中-公开
    生物识别在复杂生物流体中的应用基于珠粒或基于颗粒的图书馆和诊断套件及治疗方法

    公开(公告)号:WO2012129423A2

    公开(公告)日:2012-09-27

    申请号:PCT/US2012/030161

    申请日:2012-03-22

    摘要: The present invention is useful in screening for biomarkers associated with any other disease or condition. Such diseases and conditions range from the neurological diseases, autoimmune diseases and cancers identified above as well as any other disease or condition that has a biomarker such as an antibody or other characterizing protein or biomolecule associated with the disease or progression of the disease. The large ligand libraries of the invention can be used directly in biological fluid, under the appropriate experimental conditions and according to the processes recited herein, to screen for such markers and without the need to use fewer support members (e.g. about 100,000 or less) or without the need to transfer such peptoids or ligands to a microarray before screening the biological fluid. In addition, the ligand libraries may also be used to screen for cell based receptors that specifically relate to a particular cell surface marker.

    摘要翻译: 本发明可用于筛选与任何其它疾病或病症相关的生物标志物。 这些疾病和病症范围从神经系统疾病,自身免疫性疾病和上述癌症以及具有生物标志物如抗体或其它特征性蛋白质或与该疾病或疾病进展相关的生物分子的任何其它疾病或病症。 本发明的大配体文库可以在适当的实验条件下,并根据本文所述的方法直接用于生物流体,以筛选这些标记物,而不需要使用较少的支持成员(例如约100,000或更少)或 而不需要在筛选生物流体之前将这些类似物或配体转移到微阵列。 此外,配体文库也可用于筛选特异性涉及特定细胞表面标志物的基于细胞的受体。

    BIOMOLECULE BINDING LIGANDS
    4.
    发明申请
    BIOMOLECULE BINDING LIGANDS 审中-公开
    生物分子绑定配偶

    公开(公告)号:WO2009007676A2

    公开(公告)日:2009-01-15

    申请号:PCT/GB2008/002222

    申请日:2008-06-27

    摘要: The invention provides biomolecule binding ligands, collections of biomolecule binding ligands, and their use in the purification of biological mixtures and in the identification of ligands having an affinity for a substance. The ligand is a compound of formula (III) or a compound of formula (IV): wherein for compounds of formula (I) one of R 1a , R 1b ,R 2 , R 3 and R 4 is a group comprising a linker attached to a support, and the others of R 1a , R 1b , R 2 , R 3 and R 4 are independently selected from optionally substituted C 1-20 alkyl, optionally substituted C 3-20 heterocyclyl or optionally substituted C 5-20 aryl, and R 1a , R 1b and R 2 are additionally selected from hydrogen, and R 2 is additionally further selected from -S(=O)R 5 and -C(=S)NR 6 R 7 , wherein R 5 , R 6 and R 7 are independently optionally substituted C 1-20 alkyl, optionally substituted C 3-20 heterocyclyl or optionally substituted C 5-20 aryl, or, optionally, two or more of the others of R 1a , R 1b , R 2 , R 3 and R 4 , together with the atoms to which they are bound, may form a ring; and for compounds of formula (II) one of R 1a , R 1b , R 3 and R 4 isa group comprising a linker attached to a support, and the others of R 1a , R 1b , R 3 and R 4 are independently selected optionally substituted C 1-20 alkyl, optionally substituted C 3-20 heterocyclyl or optionally substituted C 5-20 aryl, and R 1a , and R 1b are additionally selected from hydrogen, or, optionally, two or more of the others of R 1a , R 1b , R 3 and R 4 , together with the atomsto which they are bound, may form a ring.

    摘要翻译: 本发明提供了生物分子结合配体,生物分子结合配体的集合,以及它们在纯化生物混合物中的用途以及鉴定对物质具有亲和力的配体。 配体是式(III)化合物或式(Ⅳ)化合物:其中对于式(I)化合物,R 1a,R 1b,R 2,R 3和R 4中的一个是包含连接于载体上的连接基团, 其中R1a,R1b,R2,R3和R4独立地选自任选取代的C 1-20烷基,任选取代的C 3-20杂环基或任选取代的C 5-20芳基,并且R 1a,R 1b和R 2另外选自氢,并且R 2是 另外还选自-S(= O)R 5和-C(= S)NR 6 R 7,其中R 5,R 6和R 7独立地是任选取代的C 1-20烷基,任选取代的C 3-20杂环基或任选取代的C 5-20芳基,或 任选地,R 1a,R 1b,R 2,R 3和R 4中的两个或更多个与它们所结合的原子一起形成环; 并且对于式(II)化合物,R 1a,R 1b,R 3和R 4中的一个是包含连接于载体的连接体的基团,R 1a,R 1b,R 3和R 4中的其它基团独立地选自任选被取代的C 1-20烷基, C 3-20杂环基或任选取代的C 5-20芳基,并且R 1a和R 1b另外选自氢,或任选地,R 1a,R 1b,R 3和R 4中的两个或多个,以及它们所结合的原子团 ,可能会形成一个戒指。

    DISSOLUTION AND PRECIPITATION OF COCRYSTALS WITH IONIZABLE COMPONENTS
    5.
    发明申请
    DISSOLUTION AND PRECIPITATION OF COCRYSTALS WITH IONIZABLE COMPONENTS 审中-公开
    具有离子化成分的石墨的分解和降解

    公开(公告)号:WO2008054609A2

    公开(公告)日:2008-05-08

    申请号:PCT/US2007021308

    申请日:2007-10-04

    IPC分类号: C07D223/16 C40B30/00

    CPC分类号: C40B30/00 C40B20/08 C40B40/04

    摘要: An approach to designing families of cocrystals with desired (tunable) pH dependent dissolution is developed. The solubility and dissolution rate of a family of cocrystals with the same API and a series of ligands that are weak acids or weak bases has been found to be determined and controlled by the acid or base dissociation constant of the ligand and the pH of the dissolution medium. In various aspects, pH dependent dissolution is imparted to a non-ionizable API or the dissolution of ionizable API's is modulated.

    摘要翻译: 开发了设计具有期望(可调谐)pH依赖性溶解的共晶体家族的方法。 已经发现具有相同API的一系列共晶体和弱酸或弱碱的一系列配体的溶解度和溶解速率由配体的酸或碱解离常数和溶解的pH来确定和控制 中。 在各个方面,将pH依赖性溶解赋予不可离子化的API,或者调节可离子化的API的溶解。

    METHODOLOGY FOR PREPARING COMBINATORIAL LIBRARIES BASED UPON A BICYCLIC SCAFFOLD
    10.
    发明申请
    METHODOLOGY FOR PREPARING COMBINATORIAL LIBRARIES BASED UPON A BICYCLIC SCAFFOLD 审中-公开
    用于制作基于双相线的组合图书馆的方法

    公开(公告)号:WO2005056523A3

    公开(公告)日:2006-12-07

    申请号:PCT/US2004040620

    申请日:2004-12-06

    摘要: The present invention relates to tetrahydro-pyrrolo[1,2-a]imidazole-2,5-dione derivative compounds, hexahydropyrrolo[1,2-a]pyrimidine-2,6-dione derivative compounds, and combinatorial libraries comprising such compounds. The present invention also relates to methods of preparing such compounds. The present invention also relates to methods of preparing such compounds. The methods first involve providing a functionalized resin solid support. Next, the functionalized resin solid support is reacted with amino acids under conditions effective to produce a resin bound dipeptide or tripeptide alcohol intermediate compound. Then, the resin bound dipeptide or tripeptide alcohol intermediate compound is oxidized under conditions effective to convert the resin bound dipeptide or tripeptide alcohol intermediate compound to a resin bound dipeptide or tripeptide aldehyde intermediate compound, Finally, the resin bound dipeptide or tripeptide aldehyde intermediate compound is cyclized under conditions effective to produce the tetrahydro-pyrrolo[1,2-a]imidazole-2,5-dione derivative or hexahydro-pyrrolo[1,2-a]pyrimidine-2,6-dione derivative compound. The methods can be performed in solid phase solid/solution phase, or solution phase.

    摘要翻译: 本发明涉及四氢 - 吡咯并[1,2-a]咪唑-2,5-二酮衍生物化合物,六氢吡咯并[1,2-a]嘧啶-2,6-二酮衍生物化合物,以及包含这些化合物的组合文库。 本发明还涉及制备这些化合物的方法。 本发明还涉及制备这些化合物的方法。 该方法首先涉及提供官能化的树脂固体支持物。 接下来,官能化树脂固体支持物在有效产生树脂结合二肽或三肽醇中间体化合物的条件下与氨基酸反应。 然后,树脂结合的二肽或三肽醇中间体化合物在有效将树脂结合的二肽或三肽醇中间体化合物转化为树脂结合的二肽或三肽醛中间体化合物的条件下被氧化。最后,树脂结合的二肽或三肽醛中间体化合物是 在有效产生四氢 - 吡咯并[1,2-a]咪唑-2,5-二酮衍生物或六氢 - 吡咯并[1,2-a]嘧啶-2,6-二酮衍生物化合物的条件下环化。 该方法可以在固相/溶液相或溶液相中进行。