Optically-active diamide derivatives
    2.
    发明授权
    Optically-active diamide derivatives 失效
    光学活性二酰胺衍生物

    公开(公告)号:US4495355A

    公开(公告)日:1985-01-22

    申请号:US448505

    申请日:1982-12-09

    摘要: A novel optically active diamide derivative represented by the following general formula is provided, which is useful as a starting material for asymmetric synthesis of optically active compounds, ##STR1## wherein R.sup.1 is an acyclic or cyclic, divalent atomic group containing at least one carbon atom which will, upon substitution of one of the heterocyclic groups in the formula with a nucleophilic reagent, stand as an asymmetric center in the substitution product; R.sup.2 is a substituent which has such a configuration and a molecular size that the regioselectivity in the substitution reaction of the heterocyclic group with the nucleophilic reagent can be determined by a stereo-chemical interaction thereof with the substituent R.sup.1, the steric configuration of the two asymmetric carbon atoms to which the R.sup.2 substituents are attached being identical; X is a sulfur atom or an oxygen atom; and n is an integer which is 1 or 2. Such a diamide derivative can be prepared by subjecting the corresponding dicarboxylic acid or an anhydride thereof to a condensation reaction with the corresponding heterocyclic compound in the presence of a condensation agent. The optically-active diamide derivative can be used in the reaction with a nucleophilic reagent to obtain an optically-active compound. The resulting compound can be further modified by subjecting it to reaction with another nucleophilic reagent or to hydrolysis.

    摘要翻译: 提供了由以下通式表示的新的光学活性二酰胺衍生物,其可用作不对称合成光学活性化合物的起始原料,其中R 1是含有至少一个碳原子的无环或环状二价原子团 当用亲核试剂取代式中的一个杂环基时,它将在取代产物中作为不对称中心; R2是具有这样的构型和分子大小的取代基,即杂环基与亲核试剂的取代反应中的区域选择性可以通过其与取代基R1的立体化学相互作用来确定,两个不对称的立体构型 R2取代基所连接的碳原子是相同的; X是硫原子或氧原子; n为1或2的整数。这种二酰胺衍生物可以通过在缩合剂的存在下,使相应的二羧酸或其酸酐与相应的杂环化合物进行缩合反应来制备。 光学活性二酰胺衍生物可用于与亲核试剂的反应,得到光学活性化合物。 所得化合物可以通过使其与另一种亲核试剂反应或进行水解进一步改性。

    Inhibitors of ion channels
    3.
    发明授权
    Inhibitors of ion channels 失效
    离子通道抑制剂

    公开(公告)号:US07615569B2

    公开(公告)日:2009-11-10

    申请号:US11464057

    申请日:2006-08-11

    摘要: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

    摘要翻译: 提供了可用于通过电压门控钠通道抑制钠离子通量来治疗疾病的化合物,组合物和方法。 更具体地,本发明提供了可用于治疗中枢或周围神经系统疾病,特别是疼痛和慢性疼痛的杂环芳基磺酰胺,组合物和方法,其通过阻断与所述病症的发作或复发相关的钠通道。 本发明的化合物,组合物和方法特别用于通过电压门控钠通道抑制离子通量来治疗神经性或炎性疼痛。

    Indandione bis-azomethine pigments
    5.
    发明授权
    Indandione bis-azomethine pigments 失效
    茚二酮双偶氮甲碱颜料

    公开(公告)号:US4122117A

    公开(公告)日:1978-10-24

    申请号:US760389

    申请日:1977-01-18

    CPC分类号: C09B55/007

    摘要: An indandione pigment having high tinting strength and good weatherability and light fastness of the formula ##STR1## WHEREIN A is a phenylene or naphthylene group optionally substituted by a halogen atom, a lower alkyl group, a lower alkoxy group or a nitro group; n is 2 or 1; and B represents a direct bond or an n valont aromatic radical.The pigment mentioned above can be prepared by reacting an indandione derivative of the formula ##STR2## (E is an alkoxy group with 1 to 3 carbon atoms, or an amino group; and G is an oxygen atom, or ##STR3## in which Q is a lower alkyl group, and Q.sub.2 is a lower alkyl group or a phenyl group) with an amino compound of the formula H.sub.2 N--B--NH.sub.2 ]n-1.

    摘要翻译: 具有高着色强度和良好的耐候性和耐光性的茚满二酮颜料,其中A是任选被卤素原子,低级烷基,低级烷氧基或硝基取代的亚苯基或亚萘基; n为2或1; 并且B表示直接键或n个芳香族基团。

    Carbamate esters of 2-oxyimino-3-keto-1,4-diheterocyclics
    6.
    发明授权
    Carbamate esters of 2-oxyimino-3-keto-1,4-diheterocyclics 失效
    2-氧亚氨基-3-酮基-1,4-二杂环的氨基甲酸酯

    公开(公告)号:US3883510A

    公开(公告)日:1975-05-13

    申请号:US40966773

    申请日:1973-10-25

    申请人: DU PONT

    发明人: BELLINA RUSSELL F

    CPC分类号: C07D283/02 C07D281/00

    摘要: Chemical compounds of the class of carbamate esters of 2oxyimino-3-keto-1,4-diheterocyclics, such as 2methylcarbamoyloxyimino-4-methyl-3-thiomorpholinone useful in controlling pests such as insects and nematodes.

    摘要翻译: 2-氧亚氨基-3-酮基-1,4-二杂环类的氨基甲酸酯类化合物,例如2-甲基氨基甲酰氧基亚氨基-4-甲基-3-硫代吗啉酮,可用于防治害虫如昆虫和线虫。

    Azolyloxy-carboxylic acid n-oxy-amide compounds
    8.
    发明授权
    Azolyloxy-carboxylic acid n-oxy-amide compounds 失效
    芳氧基 - 羧酸正氧化酰胺化合物

    公开(公告)号:US4408055A

    公开(公告)日:1983-10-04

    申请号:US204147

    申请日:1980-11-05

    摘要: Azolyloxy-carboxylic acid N-oxy-amide compound of the formula ##STR1## wherein R is a five-membered hetero-aromatic monocyclic radical which contains an oxygen atom or a sulphur atom and in addition 1 to 3 nitrogen atoms and which is optionally substituted by halogen, cyano, nitro, amino, alkylamino, arylamino, dialkylamino, alkylcarbonylamino, alkylcarbonyl, carboxyl, alkoxycarbonyl, carbamoyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl (which is optionally substituted by halogen, nitro or alkyl), aryl (which is optionally substituted by halogen, cyano, nitro, alkyl or alkoxy), by a radical which is optionally substituted by halogen and is selected from aralkyl, alkoxy, alkenoxy, alkynoxy, alkoxycarbonylalkoxy, aralkoxy, aryloxy, alkylthio, alkenylthio, alkoxycarbonylalkylthio, aralkylthio, arylthio, alkylsulphinyl, alkylsulphonyl, alkyl, alkenyl, alkynyl, alkoxyalkyl, aralkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, arylthioalkyl, arylsulphinylalkyl, arylsulphonylalkyl, carboxyalkyl, and alkoxycarbonylalkyl, or by optionally substituted aminocarbonylalkyl, cyanoalkyl or cycloalkyl, or which is optionally benzo-fused, the benzo radical optionally being substituted by halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino, dialkylamino, nitro, cyano, alkoxycarbonyl or optionally halogen-substituted alkylenedioxy,R.sup.1 is hydrogen or alkyl, andR.sup.2 and R.sup.3 are individually selected from optionally substituted radicals selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl orR.sup.2 and R.sup.3 taken together represent alkyleneare effective herbicides.

    摘要翻译: 具有下式的酰氧基 - 羧酸N-氧化 - 酰胺化合物(I)其中R是含有氧原子或硫原子的5元杂芳族单环基团,另外还含有1至3个氮原子, 烷基氨基,烷基羰基,羧基,烷氧基羰基,氨基甲酰基,烷基氨基羰基,二烷基氨基羰基,芳基氨基羰基(其任选被卤素,硝基或烷基取代),芳基(其是 任选地被卤素,氰基,硝基,烷基或烷氧基取代),其任选被卤素取代的基团,并且选自芳烷基,烷氧基,烯氧基,炔氧基,烷氧基羰基烷氧基,芳烷氧基,芳氧基,烷硫基,烯硫基,烷氧基羰基烷硫基,芳烷硫基, ,烷基亚磺酰基,烷基磺酰基,烷基,烯基,炔基,烷氧基烷基,芳烷氧基烷基,芳氧基烷基,烷硫基烷基,烷基亚磺酰基烷基,烷基磺酰基烷基,芳硫基 芳基亚磺酰基烷基,芳基磺酰基烷基,羧基烷基和烷氧基羰基烷基,或任选取代的氨基羰基烷基,氰基烷基或环烷基,或任选苯并稠合,任选被卤素,烷基,卤代烷基,烷氧基,卤代烷氧基,烷硫基,卤代烷硫基, 氨基,烷基氨基,二烷基氨基,硝基,氰基,烷氧基羰基或任选卤素取代的亚烷基二氧基,R 1是氢或烷基,R 2和R 3分别选自任选取代的基团,其选自烷基,烯基,炔基,环烷基, ,芳基或R2和R3一起代表亚烷基是有效的除草剂。