METHODS OF IDENTIFYING MODULATORS OF BROMODOMAINS
    36.
    发明申请
    METHODS OF IDENTIFYING MODULATORS OF BROMODOMAINS 审中-公开
    鉴定BROMODOMAIN的调节剂的方法

    公开(公告)号:WO2006083692A2

    公开(公告)日:2006-08-10

    申请号:PCT/US2006/002840

    申请日:2006-01-27

    Abstract: The present invention features compounds of the following general formula (I) wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, aryl, aralkyl; substituted aralkyl, heteroaryl; substituted heteroaryl, phenyl, SO 2 , NH 2 , NO 2 , SO 2 , CH 2 , CH 2 CH 3 , OCH 3 , OCOCH 3 , CH 2 COCH 3 , and OH, CN and halogen; R 2 is selected from the group consisting of hydrogen; lower alkyl, aryl, phenyl, aralkyl; substituted aralkyl, heteroaryl; substituted heteroaryl, SO 2 NH 2 NH 3 + NO 2 , SO 2 , CH 3 , CH 2 CH 3 , OCH 3 , OCOCH 3 , CH 2 COCH 3, and OH, halogen, carboxy, and alkoxy; X is selected from the group consisting of lower alkyl, SO 2 , NH, NO 2 , , CH 3 , CH 2 CH 3 , OCH 3 , OCOCH 3 , CH 2 COCH 3 , and OH, carboxy, and alkoxy; and n is an integer from O to 10 and their pharmaceutically acceptable salts of acids or bases as well as pharmaceutical compositions comprising these compounds. The invention further provides methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HW related disease. The present invention also features compounds of the following general formula (II) wherein: R 1 R 2 and R 3 are independently selected from the group consisting of hydrogen; lower alkyl, aryl, phenyl, aralkyl; substituted aralkyl, heteroaryl; substituted heteroaryl, SO 2 , NH 2 , NH 3 + NO 2, SO 2 , CH 3 , CH 2 CH 3 , OCH 3 , OCOCH 3 , CH 2 COCH 3 , OH, SH, halogen, carboxy; and R 4 is selected from the group consisting of lower alkyl, aryl, SO 2 , NH, NO 2 , CH 3 , CH 2 CH 3 , OCH 3 , OCOCH 3 , CH 2 COCH 3 , OH, carboxy, and alkoxy as well as pharmaceutical compositions comprising these compounds. The invention further provides methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods f treating HW infection and HIY related disease. The present invention also features compounds of formula (III) wherein R 1 , R 2 , R 3 , R 4 R 5 , and R 6 are independently selected from the group consisting of hydrogen; lower alkyl, aryl, phenyl, aralkyl; substituted aralkyl, heteroaryl, substituted heteroaryl, SO 2 NH 2 , NH 3 + , NO 2 , SO 2 , CH 3 , CH 2 CH 3 , OCH 3 , OCOCH 3 , CH 2 COCH 3 , OCH 2 CH 3 , OCH(CH 3 ) 2 , OCH 2 COOH, OCHCH 3 COOH, OCH 2 COCH 3 , OCH 2 CONH 2 , OCOCH(CH 3 ) 2 , OCH 2 CH 2 OH, OCH 2 CH 2 CH 3 , O(CH 2 ) 3 CH 3 , OCHCH 3 COOCH 3 , OCH 2 CON(CH 3 ) 2 ,NH(CH 2 ) 3 N(CH 3 ) 2 , NH(CH 2 ) 2 N(CH 3 ) 2 , NH(CH 2 ) 2 OH, NH(CH 2 ) 3 CH 3 , NHCH 3 , SH, halogen, carboxy, and alkoxy as well as pharmaceutical compositions comprising these compounds. The invention further provides methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HIV related disease.

    Abstract translation: 本发明的特征在于以下通式(I)的化合物,其中R 1选自氢,低级烷基,芳基,芳烷基; 取代的芳烷基,杂芳基; 取代的杂芳基,苯基,SO 2,NH 2,NO 2,SO 2,CH 2 CH 2,CH 3,OCH 3,OCOCH 3,CH 2, CO,SO 3,OH,CN和卤素; R 2选自氢; 低级烷基,芳基,苯基,芳烷基; 取代的芳烷基,杂芳基; 取代的杂芳基,SO 2 NH 2 NH 3,

    METHODS OF IDENTIFYING MODULATORS OF THE FGF RECEPTOR
    37.
    发明申请
    METHODS OF IDENTIFYING MODULATORS OF THE FGF RECEPTOR 审中-公开
    鉴定FGF受体调节剂的方法

    公开(公告)号:WO0151521A3

    公开(公告)日:2001-12-20

    申请号:PCT/US0100821

    申请日:2001-01-10

    Inventor: ZHOU MING-MING

    CPC classification number: C07K14/71 C07K14/475 C07K2319/00 G06F19/16

    Abstract: The present invention provides fragments of SNT and FGFR which can form a binding complex that is amenable to structural determinations by NMR spectroscopy. The three-dimensional structural data is also included as part of the invention. In addition, the present invention provides methodology for related structure based rational drug design using the three-dimensional data. Nucleotide and amino acid sequences of the fragments are also provided.

    Abstract translation: 本发明提供SNT和FGFR的片段,其可以形成可通过NMR光谱法进行结构测定的结合复合物。 作为本发明的一部分,还包括三维结构数据。 此外,本发明提供了使用三维数据的基于相关结构的合理药物设计的方法。 还提供了片段的核苷酸和氨基酸序列。

    FLAME-RETARDANT COMPOUND, CONTINUOUS MATERIALS AND PRODUCTS CONSTRUCTED THEREFROM AND METHODS OF MANUFACTURE THEREOF
    40.
    发明申请
    FLAME-RETARDANT COMPOUND, CONTINUOUS MATERIALS AND PRODUCTS CONSTRUCTED THEREFROM AND METHODS OF MANUFACTURE THEREOF 审中-公开
    阻燃化合物,连续材料及其制造的产品及其制造方法

    公开(公告)号:WO2011159897A1

    公开(公告)日:2011-12-22

    申请号:PCT/US2011/040702

    申请日:2011-06-16

    Inventor: CHEN, Ming-ming

    Abstract: A zero-halogen flame-retardant compound and continuous materials extruded therefrom comprise poly(ethylene terephthalate) (PET), fire-retardant ingredients melamine cyanurate (MC) and melamine polyphosphate (MPP), and an organo titanate coupling agent. The coupling agent acts as a dispersion agent to the fine powders of PET, MC and MPP and also allows the resin of the fine powders to be compounded at a reduced temperature which prevents degradation of the PET. The compound can be extruded as a thin film, sheet or tubing, and also as a filament or yarn, including monofi laments and multifi laments, which can ultimately be used to construct a protective sleeve.

    Abstract translation: 零卤素阻燃化合物和从其挤出的连续材料包括聚对苯二甲酸乙二醇酯(PET),阻燃成分三聚氰胺氰尿酸酯(MC)和聚磷酸三聚氰胺(MPP),以及有机钛酸酯偶联剂。 偶联剂用作PET,MC和MPP的细粉末的分散剂,并且还可以在降低温度的情况下将细粉末的树脂混合,以防止PET的劣化。 化合物可以作为薄膜,片材或管材挤出,也可以作为长丝或纱线挤出,包括单丝和多丝,最终可用于构建保护套。

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