Composition containing fluorescence-generating substrate
    11.
    发明授权
    Composition containing fluorescence-generating substrate 失效
    含荧光发生基质的组合物

    公开(公告)号:US06180844B2

    公开(公告)日:2001-01-30

    申请号:US09264678

    申请日:1999-03-09

    IPC分类号: C07C1300

    CPC分类号: C12Q1/28

    摘要: A fluorescent dye-forming composition is provided that contains a fluorescence-generating substrate of formula (I): where R1 and R2 are each independently a hydrogen atom, or an electron-donating group selected from a lower alkyl group, a lower alkoxy group, a hydroxyl group, an alkylcarbonyloxy group, an amino group di-substituted with a lower alkyl group, and an aryl group; L is selected from —NHCO— or —CONH—; Y is selected from -alkylene-COOH or formula (II):  where R3, R4 and R5 each independently represent a hydrogen atom, carboxyl group, or an electron-donating group selected from a lower alkyl group, a lower alkoxy group, a hydroxyl group, an alkylcarbonyloxy group, an amino group di-substituted with a lower alkyl group, and an aryl group. Alternatively, two of R3, R4 and R5 form, together with the adjacent carbon atoms to which they bond, a fused 5-membered or 6-membered hydrocarbon ring. Alkylene represents a linear or branched C1-6 alkylene group; and a represents an integer of 0 or 1. The substrate forms a fluorescent dye having good binding to biological samples.

    摘要翻译: 提供荧光染料形成组合物,其含有式(I)的荧光发生底物:其中R 1和R 2各自独立地为氢原子,或者是供体基团,其选自低级烷基,低级烷氧基, 羟基,烷基羰基氧基,被低级烷基二取代的氨基和芳基; L选自-NHCO-或-CONH-; Y选自 - 亚烷基-COOH或式(II) :其中R3,R4和R5各自独立地表示氢原子,羧基或供体基团,其选自低级烷基,低级烷氧基,羟基,烷基羰基氧基,二取代的氨基 低级烷基和芳基。 或者,R 3,R 4和R 5中的两个与它们键合的相邻碳原子一起形成稠合的5元或6元烃环。 亚烷基表示直链或支链C 1-6亚烷基; a表示0或1的整数。底物形成与生物样品具有良好结合性的荧光染料。

    1-Fluoro-1,1-Bis-(Phenylsulfonyl)Methane and Production Method Thereof
    12.
    发明申请
    1-Fluoro-1,1-Bis-(Phenylsulfonyl)Methane and Production Method Thereof 失效
    1-氟-1,1-二 - (苯基磺酰基)甲烷及其制备方法

    公开(公告)号:US20090131723A1

    公开(公告)日:2009-05-21

    申请号:US12224664

    申请日:2007-03-02

    IPC分类号: C07C317/14 C07C315/04

    CPC分类号: C07C317/14

    摘要: A novel 1-fluoro-1,1-bis(arylsulfonyl)methane is provided which is useful in monofluoromethylation. Also provided is a production method thereof.A method for producing a fluorobis(arylsulfonyl)methane, the method including the steps of: treating a bis(arylsulfonyl)methane represented by the following formula (1), (ArSO2)2CH2  (1) (wherein Ar represents a substituted or unsubstituted phenyl group or naphthyl group) with a base; and then adding a fluorination reagent thereto, to produce fluorobis(arylsulfonyl)methane represented by the following formula (2) (ArSO2)2CHF  (2) (wherein Ar is defined as above), and a fluorobis(arylsulfonyl)methane (2) represented by the above formula (2), which is a novel compound that is very useful in producing a monofluoromethyl.

    摘要翻译: 提供了一种新颖的1-氟-1,1-双(芳基磺酰基)甲烷,其可用于单氟甲基化。 还提供了其制备方法。 一种制备氟双(芳基磺酰基)甲烷的方法,所述方法包括以下步骤:处理由下式(1)表示的双(芳基磺酰基)甲烷,<?在线式描述=“在线式”末端 (“Ar”)2CH2(1)<?in-line-formula description =“In-line formula”end =“tail”?>(其中Ar表示取代或未取代的苯基或萘基) 一个基地 然后向其中加入氟化试剂以产生由下式(2)表示的氟双(芳基磺酰基)甲烷<?in-line-formula description =“In-line Formulas”end =“lead”→(ArSO 2)2CHF (式中,Ar如上所定义),上述式(2)表示的氟双(芳基磺酰基)甲烷(2) ),它是一种在生产单氟甲基中非常有用的新型化合物。

    Trihalomethionine derivative and pharmaceutical product containing the same
    13.
    发明授权
    Trihalomethionine derivative and pharmaceutical product containing the same 失效
    三卤代甲硫氨酸衍生物和含有它们的药物产品

    公开(公告)号:US07868206B2

    公开(公告)日:2011-01-11

    申请号:US12159459

    申请日:2006-12-27

    IPC分类号: C07C233/05 A61K31/16

    CPC分类号: C07C323/60 C07C2602/08

    摘要: A compound represented by the formula (I) is used as an active ingredient in a medicament for treatment or prevention of infectious diseases caused by protozoa or bacterium. X represents halogen, Z represents —(CH2)m— wherein m is an integer of 1-5, and R represents one of the following (i)-(v): (i) hydrogen n represents an integer of 0-5, R1's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. R2's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. (iv) alkyl having 1-5 carbon atoms, (v) hydroxyalkyl having 1-5 carbon atoms.

    摘要翻译: 在由用于治疗或预防由原生动物或细菌引起的感染性疾病的药物中使用由式(I)表示的化合物作为活性成分。 X表示卤素,Z表示 - (CH 2)m - ,其中m为1-5的整数,R表示以下(i) - (v)中的一个:(i)氢n表示0-5的整数, R 1独立地表示氢,卤素,具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 R 2独立地表示氢,卤素,具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 (iv)具有1-5个碳原子的烷基,(v)具有1-5个碳原子的羟烷基。

    NOVEL TRIHALOMETHIONINE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING THE SAME
    14.
    发明申请
    NOVEL TRIHALOMETHIONINE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING THE SAME 失效
    新型三缩水甘油衍生物和含有它们的药物产品

    公开(公告)号:US20100076224A1

    公开(公告)日:2010-03-25

    申请号:US12159459

    申请日:2006-12-27

    IPC分类号: C07C237/06

    CPC分类号: C07C323/60 C07C2602/08

    摘要: A compound represented by the formula (I) is used as an active ingredient in a medicament for treatment or prevention of infectious diseases caused by protozoa or bacterium. X represents halogen, Z represents —(CH2)m— wherein m is an integer of 1-5, and R represents one of the following (i)-(v): (i) hydrogen n represents an integer of 0-5, R1's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. R2's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. (iv) alkyl having 1-5 carbon atoms, (v) hydroxyalkyl having 1-5 carbon atoms.

    摘要翻译: 在由用于治疗或预防由原生动物或细菌引起的感染性疾病的药物中使用由式(I)表示的化合物作为活性成分。 X表示卤素,Z表示 - (CH 2)m - ,其中m为1-5的整数,R表示以下(i) - (v)中的一个:(i)氢n表示0-5的整数, R 1独立地表示氢,卤素,具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 R 2独立地表示氢,卤素,具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 (iv)具有1-5个碳原子的烷基,(v)具有1-5个碳原子的羟烷基。

    1-fluoro-1, 1-bis-(phenylsulfonyl)methane and production method thereof
    15.
    发明授权
    1-fluoro-1, 1-bis-(phenylsulfonyl)methane and production method thereof 失效
    1-氟-1,1-双 - (苯基磺酰基)甲烷及其制备方法

    公开(公告)号:US07638654B2

    公开(公告)日:2009-12-29

    申请号:US12224664

    申请日:2007-03-02

    IPC分类号: C07C315/04 C07C317/14

    CPC分类号: C07C317/14

    摘要: A novel 1-fluoro-1,1-bis(arylsulfonyl)methane is provided which is useful in monofluoromethylation. Also provided is a production method thereof.A method for producing a fluorobis(arylsulfonyl)methane, the method including the steps of: treating a bis(arylsulfonyl)methane represented by the following formula (1), (ArSO2)2CH2  (1) (wherein Ar represents a substituted or unsubstituted phenyl group or naphthyl group) with a base; and then adding a fluorination reagent thereto, to produce fluorobis(arylsulfonyl)methane represented by the following formula (2) (ArSO2)2CHF  (2) (wherein Ar is defined as above), and a fluorobis(arylsulfonyl)methane (2) represented by the above formula (2), which is a novel compound that is very useful in producing a monofluoromethyl.

    摘要翻译: 提供了一种新颖的1-氟-1,1-双(芳基磺酰基)甲烷,其可用于单氟甲基化。 还提供了其制备方法。 一种制备氟双(芳基磺酰基)甲烷的方法,所述方法包括以下步骤:处理由下式(1)表示的双(芳基磺酰基)甲烷,(ArSO 2)2 CH 2(1)(其中Ar表示取代或未取代的苯基 基团或萘基); 然后向其中加入氟化试剂,得到由下式(2)(ArSO 2)2 CHF(2)(其中Ar如上定义)表示的氟双(芳基磺酰基)甲烷和表示为氟代双(芳基磺酰基)甲烷(2) 通过上述式(2),其是在制备单氟甲基中非常有用的新型化合物。

    Efficient method for the synthesis of N-cyclic maleamic acids and
N-cyclic maleimides
    17.
    发明授权
    Efficient method for the synthesis of N-cyclic maleamic acids and N-cyclic maleimides 失效
    用于合成N-环状马来酰胺酸和N-环状马来酰亚胺的高效方法

    公开(公告)号:US5965746A

    公开(公告)日:1999-10-12

    申请号:US89235

    申请日:1998-06-02

    CPC分类号: C07D207/448 C07D405/04

    摘要: Provided are methods for the synthesis of N-cyclic maleamic acids and N-cyclic maleimide derivatives, as well as N-cyclic maleamic acids and N-cyclic maleimides synthesized thereby. The method for synthesis of an N-cyclic maleamic acid involves reacting an amino group-containing N-cyclic compound with maleic anhydride in acetic acid to obtain an N-cyclic maleamic acid. An N-cyclic maleimide can be formed by adding hexamethyldisilazane to an N-cyclic maleamic acid prepared according to the above-described method, thereby cyclizing a maleamic acid site of the N-cyclic maleamic acid. The described methods allow for the products to be obtained at high yields.

    摘要翻译: 提供了合成N-环状马来酰胺酸和N-环状马来酰亚胺衍生物的方法,以及由此合成的N-环状马来酰胺酸和N-环状马来酰亚胺。 合成N-环状马来酰胺酸的方法包括在乙酸中使含氨基的N-环状化合物与马来酸酐反应,得到N-环状马来酰胺酸。 通过将六甲基二硅氮烷加入到根据上述方法制备的N-环状马来酰胺酸中,可以形成N-环状马来酰亚胺,由此环化N-环状马来酰胺酸的马来酰胺酸位点。 所描述的方法允许以高产率获得产物。