PEPTIDES
    84.
    发明申请
    PEPTIDES 审中-公开

    公开(公告)号:WO9747593A2

    公开(公告)日:1997-12-18

    申请号:PCT/EP9703077

    申请日:1997-06-12

    Inventor: SEEBACH DIETER

    CPC classification number: C07C271/22 A61K31/435 C07C237/22

    Abstract: The invention provides novel beta -peptides comprising 2 or more different beta -amino acid residues, preferably compounds of formula (I) wherein the R residues, X and n are as defined. Compounds of the invention having as few as 5 or 6 beta -amino acid residues exhibit stable structures in solution and the compounds generally exhibit good resistance to proteolytic degradation. The compounds of the invention provide a valuable new source of structural diversity for synthesis of biologically active compounds, e.g. for pharmaceutical uses.

    Abstract translation: 本发明提供了包含2个或更多个不同β-氨基酸残基的新型β-肽,优选其中R残基X和n如所定义的式(I)化合物。 具有少至5或6个β-氨基酸残基的本发明化合物在溶液中表现出稳定的结构,并且化合物通常表现出对蛋白水解降解的良好抗性。 本发明的化合物为生物活性化合物的合成提供了有价值的新的结构多样性来源,例如, 用于制药用途。

    RING FINGER PROTEIN
    85.
    发明申请
    RING FINGER PROTEIN 审中-公开
    戒指指纹蛋白

    公开(公告)号:WO9712900A3

    公开(公告)日:1997-05-15

    申请号:PCT/IB9500810

    申请日:1995-09-29

    CPC classification number: C07K14/4703

    Abstract: This invention relates to a protein which is essential for the formation of an active cyclin-dependent kinase (CDK)/cyclin complex, derivatives of said protein, antibodies specific for said protein, and to means and methods for the production thereof. The invention is also directed to nucleic acids coding for a protein of the invention, to a method of obtaining such nucleic acid molecules, and to the expression thereof. Furthermore, the invention is directed to uses of the proteins and nucleic acids of the invention.

    POLYMER-BOUND FLUOROPHORES AS OPTICAL ION SENSORS
    86.
    发明申请
    POLYMER-BOUND FLUOROPHORES AS OPTICAL ION SENSORS 审中-公开
    聚对苯二甲酸乙二醇酯作为光离子传感器

    公开(公告)号:WO1997011067A1

    公开(公告)日:1997-03-27

    申请号:PCT/EP1996003954

    申请日:1996-09-10

    Inventor: CIBA-GEIGY AG

    CPC classification number: C07D493/10 C07D219/08 C07D311/82 G01N33/533

    Abstract: The invention relates to compounds of formula (I), (IIa) or (IIb), wherein R1, R2, R5 and R6 are each independently of one another hydrogen, -SO2-(C1-C6)alkylphenyl, C1-C30alkyl, C1-C30alkyl-CO- or a radical of formula -(CnH2n-O-)m-R10; R3 is hydrogen or -SO2-(C1-C6)alkylphenyl; R4 and R7 are C1-C30 alkylene or a radical of formula -(CnH2n-O-)m-R10; Z is a functional group which is selected from the group consisting of -OH, -SH, -NH2, -COOH, -NCO, -CO-NR8YR9Y, -NH-CO-CH=CH2, -NH-CO-C(CH3)=CH2; R8 and R9 are each independently of the other C1-C30alkylene; R10 is a direct bond or C1-C12alkylene; n is a number from 2 to 6, and m is a number from 1 to 10, with the proviso that the total number of carbon atoms is at most 30; and Y is -OH or -SH. The compounds are used as comonomers for the preparation of copolymer membranes for plasticiser-free ion sensors.

    Abstract translation: 本发明涉及式(I),(IIa)或(IIb)的化合物,其中R 1,R 2,R 5和R 6各自独立地为氢,-SO 2 - (C 1 -C 6)烷基苯基,C 1 -C 30烷基, -C 30烷基-CO-或式 - (C n H 2n -O-)m -R 10的基团; R3是氢或-SO2-(C1-C6)烷基苯基; R4和R7是C1-C30亚烷基或式 - (CnH2n-O-)m -R10的基团; Z是选自-OH,-SH,-NH2,-COOH,-NCO,-CO-NR8YR9Y,-NH-CO-CH = CH2,-NH-CO-C(CH3 )= CH 2; R8和R9各自独立地为C 1 -C 30亚烷基; R10是直接键或C1-C12亚烷基; n为2〜6的数,m为1〜10的数,条件是碳原子数为30以下。 Y为-OH或-SH。 该化合物用作制备用于不含增塑剂的离子传感器的共聚物膜的共聚单体。

    ACYLATED OLIGOPEPTIDE DERIVATIVES HAVING CELL SIGNAL INHIBITING ACTIVITY
    87.
    发明申请
    ACYLATED OLIGOPEPTIDE DERIVATIVES HAVING CELL SIGNAL INHIBITING ACTIVITY 审中-公开
    具有细胞信号抑制活性的酰化寡核苷酸衍生物

    公开(公告)号:WO1997008193A1

    公开(公告)日:1997-03-06

    申请号:PCT/EP1996003473

    申请日:1996-08-06

    Inventor: CIBA-GEIGY AG

    Abstract: The invention relates to an acylated peptide, namely a compound of formula (I), wherein n is 0 to 15, X is arylcarbonyl, cycloalkylcarbonyl, tricycloalkylcarbonyl, arylsulfonyl, heterocyclylcarbonyl, heterocyclylsulfonyl, carbamoyl-lower alkanoyl, aryl-lower alkylcarbonyl, cycloalkyl-lower alkylcarbonyl, aryl-lower alkylsulfonyl, heterocyclyl-lower alkylcarbonyl, heterocyclyl-lower alkylsulfonyl with the proviso that in any of the lower alkyl radicals mentioned a methylene group may be replaced with oxa, aza or thia; heterocyclyl-lower alkenylcarbonyl or aryl-lower alkenylcarbonyl; or, if Y is a secondary or tertiary amino group, is one of the moieties X mentioned above or lower alkanoyl, halo-lower alkanoyl, lower-alkoxycarbonyl, aryl-lower alkoxycarbonyl or cycloalkyl-lower alkoxycarbonyl; PTI is the bivalent radical of tyrosine or (preferably) the bivalent radical of phosphotyrosine or a phosphotyrosine mimic, AA stands for a bivalent radical of a natural or unnatural amino acid, and Y is hydroxy, a C-terminal protecting group or a primary, secondary or tertiary amino group, or a salt thereof, said compound being useful for the treatment of diseases that respond to inhibition of the interaction of (a) protein(s) comprising (an) SH2 domain(s) and a protein tyrosine kinase or a modified version thereof.

    Abstract translation: 本发明涉及酰化肽,即式(I)化合物,其中n为0至15,X为芳基羰基,环烷基羰基,三环烷基羰基,芳基磺酰基,杂环基羰基,杂环基磺酰基,氨基甲酰基 - 低级烷酰基,芳基 - 低级烷基羰基,环烷基 - 低级烷基羰基,芳基 - 低级烷基磺酰基,杂环基 - 低级烷基羰基,杂环基 - 低级烷基磺酰基,条件是在所提及的任何低级烷基中亚甲基可以被氧杂,氮杂或硫代替代; 杂环基低级烯基羰基或芳基 - 低级烯基羰基; 或者如果Y是仲或叔氨基,则是上述部分X或低级烷酰基,卤代低级烷酰基,低级烷氧基羰基,芳基 - 低级烷氧基羰基或环烷基 - 低级烷氧基羰基之一; PTI是酪氨酸或(优选)磷酸酪氨酸或磷酸酪氨酸模拟物的二价基团的二价基团,AA代表天然或非天然氨基酸的二价基团,Y是羟基,C-末端保护基或伯, 仲或叔氨基或其盐,所述化合物可用于治疗响应于(a)包含(a)SH2结构域和蛋白质酪氨酸激酶的蛋白质的相互作用的抑制的疾病,或 其修改版本。

    PROCESS FOR THE HYDROGENATION OF IMINES
    88.
    发明申请
    PROCESS FOR THE HYDROGENATION OF IMINES 审中-公开
    加氢方法

    公开(公告)号:WO1997005095A1

    公开(公告)日:1997-02-13

    申请号:PCT/EP1996003143

    申请日:1996-07-17

    Inventor: CIBA-GEIGY AG

    Abstract: A process for the hydrogenation of imines with hydrogen under elevated pressure in the presence of iridium catalysts containing diphosphine ligands, with or without an inert solvent, the reaction mixture containing a soluble ammonium chloride, bromide or iodide or a soluble metal chloride, bromide or iodide, wherein the reaction mixture additionally contains at least one solid acid with the exception of ion exchangers. Improved optical yields and high chemical conversion rates are achieved while the catalyst is easily separable.

    Abstract translation: 在含有二膦配体的铱催化剂存在下,在升高的压力下氢化亚胺的方法,在有或者没有惰性溶剂的情况下,含有可溶性氯化铵,溴化物或碘化物的反应混合物或可溶性金属氯化物,溴化物或碘化物 ,其中所述反应混合物另外含有除离子交换剂之外的至少一种固体酸。 在催化剂容易分离的同时,获得了提高的光学收率和高化学转化率。

    FLOW CELL
    89.
    发明申请
    FLOW CELL 审中-公开
    流通池

    公开(公告)号:WO1997001087A1

    公开(公告)日:1997-01-09

    申请号:PCT/EP1996002519

    申请日:1996-06-10

    Inventor: CIBA-GEIGY AG

    CPC classification number: G01N21/05 G01N2021/0346

    Abstract: A flow cell (1) has in its interior a flow channel (2) and is provided with an inlet opening (3) for the sample and with an outlet opening (4). Also provided are means for producing a sample-free blocked volume located in the flow channel (2). Those means comprise, for example, a further inlet opening (5) for a reference fluid, that inlet opening (5) being so positioned that the reference fluid flows counter to the sample in the flow channel (2). The flow cell (1) is suitable for a sensor apparatus in which one of the boundary surfaces of the flow channel (2) comprises a detection layer that contains selectively sensitive recognition elements for an analyte. The flow cell (1) is also suitable for an optical detection device which preferably utilises luminescence excitation in the evanescent field of an optical waveguide.

    Abstract translation: 流动池(1)在其内部具有流动通道(2),并且设置有用于样品的入口开口(3)和出口开口(4)。 还提供了用于产生位于流动通道(2)中的无样品阻塞体积的装置。 这些装置包括例如用于参考流体的另一个入口开口(5),该入口开口(5)被定位成使得参考流体与流动通道(2)中的样品相反。 流动池(1)适用于传感器装置,其中流动通道(2)的边界表面之一包括检测层,该检测层包含用于分析物的选择性敏感的识别元件。 流动池(1)还适用于光学检测装置,其优选地在光波导的消逝场中利用发光激发。

    THIOAMIDES S-OXIDES FOR USE AS PESTICIDES
    90.
    发明申请
    THIOAMIDES S-OXIDES FOR USE AS PESTICIDES 审中-公开
    用作杀虫剂的硫氧化物S-氧化物

    公开(公告)号:WO1997000859A1

    公开(公告)日:1997-01-09

    申请号:PCT/EP1996002520

    申请日:1996-06-10

    Inventor: CIBA-GEIGY AG

    CPC classification number: A01N43/80 A01N41/02 C07C327/60 C07D261/20

    Abstract: Thioamide S-oxides of formula (I) are suitable as fungicidally, insecticidally and acaricidally active ingredients in crop protection, in which R1 is hydrogen or C1-C4alkyl, and R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl or C3-C6cycloalkyl, and in which R3 and R4 independently of one another are hydrogen, cyano, C1-C4alkyl, halo-C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, cyclopropylmethyl, C1-C4alkoxy, C2-C5alkoxyalkyl, C1-C4alkoxycarbonyl, C1-C4alkylthio, C2-C5alkylthioalkyl; an unsubstituted or up to trisubstituted ring which has not more than 15 ring carbon atoms, which can be polycyclic and which contains 0-3 hetero atoms N, O or S, it being possible for this ring to be bonded via an aliphatic bridge having not more than 4 carbon atoms and/or via either CO, oxygen or sulfur; or in which R3 and R4 together with the joint carbon atom form an unsubstituted or up to trisubstituted ring which has not more than 15 ring carbon atoms, which can be polycyclic and which contains 0-3 hereto atoms N, O or S. They can be used on their own or as formulated compositions, preferably for controlling or preventing infestation with microorganisms.

    Abstract translation: 式(I)的硫酰胺S-氧化物在作物保护中适合作为杀真菌,杀虫和杀螨活性成分,其中R1是氢或C1-C4烷基,R2是氢,C1-C4烷基,C2-C4链烯基,C2-C4炔基或 C 3 -C 6环烷基,其中R 3和R 4彼此独立地是氢,氰基,C 1 -C 4烷基,卤代-C 1 -C 4烷基,C 2 -C 4烯基,C 2 -C 4炔基,C 3 -C 6环烷基,环丙基甲基,C 1 -C 4烷氧基,C 2 -C 5烷氧基烷基 ,C 1 -C 4烷氧基羰基,C 1 -C 4烷硫基,C 2 -C 5烷硫基烷基; 具有不多于15个环碳原子的未被取代或最多三取代的环,其可以是多环的并且含有0-3个杂原子N,O或S,该环可能通过没有 多于4个碳原子和/或经由CO,氧或硫; 或其中R 3和R 4与连接碳原子一起形成具有不多于15个环碳原子的未取代或至多三取代的环,其可以是多环的并且含有0-3个原子N ,O或S.它们可以单独使用或作为配制的组合物使用,优选用于控制或预防用微生物侵染。

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