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    • 23. 发明申请
    • BICYCLIC AMINES AS INSECTICIDES
    • 双酚A作为杀虫剂
    • WO1997043286A1
    • 1997-11-20
    • PCT/GB1997001259
    • 1997-05-09
    • ZENECA LIMITEDSALMON, RogerHOTSON, Matthew, Brian
    • ZENECA LIMITED
    • C07D451/02
    • C07D451/02A01N43/90
    • The invention provides novel compounds of formula (I) and formula (II) wherein R represents a group of formula (A) where each of W, X, Y and Z represents either a group CR or the nitrogen atom, provided that not more than two of W, X, Y, and Z represent the nitrogen atom, and where each R present is independently selected from hydrogen and halogen atoms and cyano, amino, hydrazino, acylamino, hydroxy, alkyl, hydroxyalkyl, alkoxy, haloalkyl, haloalkoxy, alkenyl, alkenyloxy, alkoxyalkenyl, alkynyl, carboxylic acyl, alkoxycarbonyl, aryl and heterocyclyl groups, said groups comprising up to 6 carbon atoms, and wherein R represents a group XR where X represents oxygen or a group NR where R and R are individually selected from hydrogen or a group selected from alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, heterocyclylalkyl, alkoxycarbonyl, and carboxylic acyl groups, said groups comprising from 1 to 15 carbon atoms, said groups being optionally substituted with one or more substituents selected from, halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, haloalkyl and alkyl groups; and acid addition salts and quaternary ammonium salts and N-oxides derived therefrom. The compounds have useful insecticidal properties.
    • 本发明提供新的式(I)和式(II)化合物,其中R 1表示式(A)中的基团,其中W,X,Y和Z各自表示基团CR或氮原子,条件是 不多于两个W,X,Y和Z表示氮原子,并且其中每个R独立地选自氢和卤素原子和氰基,氨基,肼基,酰氨基,羟基,烷基,羟基烷基,烷氧基,卤代烷基, 卤代烷氧基,烯基,烯氧基,烷氧基烯基,炔基,羧基酰基,烷氧基羰基,芳基和杂环基,所述基团包含至多6个碳原子,并且其中R 2表示XR 3基团,其中X表示氧或NR 其中R 3和R 4分别选自氢或选自烷基,芳基,杂芳基,芳烷基,杂芳基烷基,烯基,芳烯基,炔基,杂环基烷基,烷氧基羰基和羧酰基的基团,所述基团 包含1至15个碳原子,所述基团是选择性的 被一个或多个选自卤素,氰基,羧基,羧基酰基,氨基甲酰基,烷氧基羰基,烷氧基,亚烷基二氧基,羟基,硝基,卤代烷基和烷基的取代基取代。 和酸加成盐和季铵盐和由其衍生的N-氧化物。 该化合物具有有用的杀虫性质。
    • 25. 发明申请
    • FUNGICIDAL OXAZOLIDINEDIONE DERIVATIVES
    • 杀真菌毒素衍生物
    • WO1997038995A1
    • 1997-10-23
    • PCT/GB1997000822
    • 1997-03-24
    • ZENECA LIMITEDHUGGETT, Margaret, JeanWHITTINGHAM, William, GuyBUCHANAN, Kirsteen, Isobel
    • ZENECA LIMITED
    • C07D413/12
    • C07D413/12A01N43/76
    • A fungicidal oxazolidinedione compound having general formula (I) wherein R is a C-linked 6-membered heteroaromatic ring containing 2 or 3 nitrogen atoms and which is optionally N- or C-substituted with one or more of halo, hydroxy, oxo, C1-6 alkyl, C3-6 cycloalkyl, halo(C1-6)alkyl, C1-4 alkoxy(C1-6)alkyl, aryl(C1-6)alkyl, C1-6 alkoxy, halo(C1-6)alkoxy, C2-4 alkenyloxy, C1-6 alkylthio, C1-6 alkylcarbonyl, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonyl, arylcarbonyl, aryl, aryloxy, or heteroaryl, the aryl and heteroaryl substituents themselves being optionally substituted with one or more of halo, C1-6 alkyl, halo(C1-6)alkyl, C1-6 alkoxy, halo(C1-6)alkoxy, C1-4 alkoxy (C1-6) alkyl, nitro, amino, mono- or di(C1-4)alkylamino, cyano, C1-6 alkoxycarbonyl or C1-6 alkylcarbonyl, and R is phenyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, pyrrolyl, furyl, thienyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, thiadiazolyl, oxadiazolyl or tetrazolyl, any of which is optionally substituted with one or more of halo, C1-6 alkyl, halo(C1-6)alkyl, C1-6 alkoxy, halo(C1-6)alkoxy, C1-6 alkylthio, nitro, cyano, thiocyanato, C1-4 alkylsulphonyl, halo(C1-4)alkylsulphonyl, aminosulphonyl or C1-6 alkoxycarbonyl, or two adjacent substituents join to form with the carbon atoms to which they are attached a fused benzene ring optionally substituted with halo, C1-4 alkyl or C1-4 alkoxy.
    • 具有通式(I)的杀真菌恶唑烷二酮化合物,其中R 1是含有2或3个氮原子的C连接的6元杂芳族环,并且其任选被一个或多个卤素,羟基, 氧代C 1-6烷基,C 3-6环烷基,卤代(C 1-6)烷基,C 1-4烷氧基(C 1-6)烷基,芳基(C 1-6)烷基,C 1-6烷氧基,卤代(C 1-6) 烷氧基,C 2-4烷氧基,C 1-6烷硫基,C 1-6烷基羰基,C 1-6烷基羰基氨基,C 1-6烷氧基羰基,芳基羰基,芳基,芳氧基或杂芳基,芳基和杂芳基取代基本身任选被一个或多个 卤代(C 1-6)烷基,C 1-6烷氧基,卤代(C 1-6)烷氧基,C 1-4烷氧基(C 1-6)烷基,硝基,氨基,单或二(C1- 4)烷基氨基,氰基,C 1-6烷氧基羰基或C 1-6烷基羰基,R 2是苯基,吡啶基,嘧啶基,哒嗪基,吡嗪基,三嗪基,吡咯基,呋喃基,噻吩基,吡唑基,咪唑基,恶唑基,异恶唑基,噻唑基, 异噻唑基,三唑基,噻二唑基,恶二唑基或四氢呋喃基 卤代(C 1-6)烷基,C 1-6烷氧基,卤代(C 1-6)烷氧基,C 1-6烷硫基,硝基,氰基, 硫氰酸酯,C 1-4烷基磺酰基,卤代(C 1-4)烷基磺酰基,氨基磺酰基或C 1-6烷氧基羰基,或两个相邻的取代基与它们所连接的碳原子一起形成,稠合苯环任选被卤素取代,C 1-4 烷基或C 1-4烷氧基。
    • 30. 发明申请
    • SUBSTITUTED PHENYLOXAZOLIDINONES AND THEIR USE AS ANTIBIOTICS
    • 取代的苯并噻唑啉酮及其作为抗生素的用途
    • WO1997031917A1
    • 1997-09-04
    • PCT/GB1997000511
    • 1997-02-24
    • ZENECA LIMITEDBETTS, Michael, JohnMILLS, Stuart, DennettROBERTS, David, AnthonySWAIN, Michael, Lingard
    • ZENECA LIMITED
    • C07D413/10
    • C07D233/64C07D231/12C07D233/56C07D233/90C07D249/08
    • The invention concerns a compound of formula (I) wherein, for example: R is hydroxy, chloro, fluoro, amino, azido, of the for mula -NHC(=O)R wherein R is hydrogen or (1-4C)alkyl, of the formula -N(Me)C(=O)R wherein R is hydrogen, methyl or methoxy or of the formula -NHS(O)n(1-4C)alkyl wherein n is 0, 1 or 2; R and R are independently hydrogen or fluoro; R , R and R are independently selected from hydrogen, (1-4C)alkyl (optionally substituted), halo, trifluoromethyl, carboxy, (1-4C)alkoxycarbonyl, carbamoyl, N -(1-4C)alkylcarbamoyl, di-( N -(1-4C)alkyl)carbamoyl, cyano or nitro; and pharmaceutically acceptable salts thereof; and in particular the compounds N-[(5S)-(3-(4-(4-bromoimidazol-1-yl)-3-fluorophenyl)-2-oxooxazolidin-5-ylmethyl]acetamide and N-[(5S)-(3-(4-(4-cyanoimidazol-1-yl)-3-fluorophenyl)-2-oxooxazolidin-5-ylmethyl]acetamide and pharmaceutically acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
    • 本发明涉及式(I)化合物,其中例如:R 1是羟基,氯,氟,氨基,氨基,其中R a是(= O)R a,其中R a是 氢或式-N(Me)C(= O)R b的(1-4C)烷基,其中R b是氢,甲基或甲氧基或式-NHS(O)n(1- 4C)烷基,其中n为0,1或2; R 2和R 3独立地是氢或氟; R 4,R 5和R 6独立地选自氢,(1-4C)烷基(任选取代的),卤素,三氟甲基,羧基,(1-4C)烷氧基羰基,氨基甲酰基,N - (1-4C)烷基氨基甲酰基,二 - (N - (1-4C)烷基)氨基甲酰基,氰基或硝基; 及其药学上可接受的盐; 特别是N - [(5S) - (3-(4-(4-溴咪唑-1-基)-3-氟苯基)-2-氧代恶唑烷-5-基甲基]乙酰胺和N - [(5S) - (3-(4-(4-氰基咪唑-1-基)-3-氟苯基)-2-氧代恶唑烷-5-基甲基]乙酰胺及其药学上可接受的盐;其制备方法;含有它们的药物组合物及其作为抗菌剂的用途 代理商。