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    • 3. 发明授权
    • Imidazole lipoxygenase inhibitors
    • 咪唑脂氧合酶抑制剂
    • US5753682A
    • 1998-05-19
    • US553546
    • 1996-05-06
    • Rodney W. StevensTakashi ManoKazuo Ando
    • Rodney W. StevensTakashi ManoKazuo Ando
    • A61K31/415A61K31/4178A61P9/00A61P11/00A61P17/00A61P19/02A61P25/00A61P29/00A61P37/08A61P43/00C07D233/54C07D233/60C07D305/04C07D309/02C07D405/10C07D405/12C07D405/14C07D521/00
    • C07D233/64C07D231/12C07D233/56C07D249/08C07D405/12C07D405/14
    • Certain novel imidazole derivatives having the ability to inhibit the lipoxygenase enzyme and having formula (I), wherein Y is hydrogen, C.sub.1 -C.sub.8 alkyl, halosubstituted C.sub.1 -C.sub.4 alkyl, phenyl, substituted phenyl, C.sub.7 -C.sub.14 phenylalkyl, C.sub.7 -C.sub.14 (substituted phenyl)alkyl, pyridyl, substituted pyridyl, C.sub.6 -C.sub.13 pyridylalkyl or C.sub.6 -C.sub.13 (substituted pyridyl)alkyl, wherein each substituent is independently halo, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halosubstituted C.sub.1 -C.sub.4 alkyl, halosubstituted C.sub.1 -C.sub.4 alkoxy, NR.sup.4 R.sup.5, CO.sub.2 R.sup.4 or CONR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 are each, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; Ar.sup.1 and Ar.sup.2 are each, independently, phenylene, mono-substituted phenylene or di-substituted phenylene, wherein the substituents are, independently, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo-substituted C.sub.1 -C.sub.4 alkyl or halo-substituted C.sub.1 -C.sub.4 alkoxy; X and X.sup.1 are each, independently, O, S, SO or SO.sub.2 ; R' is hydrogen or C.sub.1 -C.sub.4 alkyl; and R.sup.2 and R.sup.3 are each, independently, methylene, ethylene or propylene. These compounds are useful for the treatment of disease states such as bronchial asthma, skin disorders and arthritis in mammals, and as the active ingredient in pharmaceutical compositions for treating such conditions.
    • PCT No.PCT / JP94 / 00836 Sec。 371日期:1996年5月6日 102(e)日期1996年5月6日PCT 1994年5月25日PCT公布。 第WO94 / 29299号公报 日期:1994年12月22日具有抑制脂氧合酶和具有式(I)的能力的新型咪唑衍生物,其中Y为氢,C1-C8烷基,卤代C1-C4烷基,苯基,取代苯基,C7-C14苯基烷基, C7-C14(取代苯基)烷基,吡啶基,取代的吡啶基,C6-C13吡啶基烷基或C6-C13(取代的吡啶基)烷基,其中各取代基独立地为卤素,硝基,氰基,C 1 -C 4烷基,C 1 -C 4烷氧基, C 1 -C 4烷基,卤代C 1 -C 4烷氧基,NR 4 R 5,CO 2 R 4或CONR 4 R 5,其中R 4和R 5各自独立地为氢或C 1 -C 6烷基; Ar 1和Ar 2各自独立地为亚苯基,单取代亚苯基或二取代亚苯基,其中取代基独立地为卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,卤素取代的C 1 -C 4烷基或卤素取代的 C1-C4烷氧基; X和X1各自独立地为O,S,SO或SO 2; R'是氢或C 1 -C 4烷基; 并且R 2和R 3各自独立地为亚甲基,亚乙基或亚丙基。 这些化合物可用于治疗疾病状态,例如哺乳动物中的支气管哮喘,皮肤病和关节炎,以及用作治疗这些病症的药物组合物中的活性成分。
    • 5. 发明授权
    • Insecticidal and acaricidal oxetane and thietane derivatives,
compositions, and method of use therefor
    • 杀虫和杀螨的氧杂环丁烷和硫杂环丁烷衍生物,组合物及其用途的方法
    • US4714710A
    • 1987-12-22
    • US905275
    • 1986-09-09
    • Heinrich FrankeHartmut JoppienHelga Franke
    • Heinrich FrankeHartmut JoppienHelga Franke
    • C07D317/00A01N43/20A01N43/30C07D305/04C07D305/06C07D331/04C07D407/04A61K31/335A61K31/38
    • A01N43/20C07D305/06C07D331/04
    • There are described new compounds of general formula I ##STR1## in which R.sub.1 is aryl or aryl substituted by C.sub.1-4 -alkyl, halo-C.sub.1-4 -alkyl, phenyl-C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.2-4 -alkynyl, halo-C.sub.2-4 -alkynyl, phenyl-C.sub.2-4 -alkynyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, phenyl-C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyloxy, alkylsulphonyloxy, haloalkylsulphonyloxy, arylsulphonyloxy, halo-C.sub.2-4 -alkenyloxy, phenyl-C.sub.2-4 -alkenyloxy, halo, cyano, nitro, aryloxy, haloaryloxy, C.sub.1-4 -alkylaryloxy, or nitro-C.sub.1-4 -alkylaryloxy,R.sub.2 and R.sub.3 are the same or different and are hydrogen, fluorine, cyano or ethynyl,R.sub.4 is phenyl or pyridyl or these groups substituted by one or more of C.sub.1-6 -alkyl, halo-C.sub.1-6 -alkyl, phenyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkyl interrupted by an O--, N-- or S-- atom, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, phenyl-C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyloxy, halo-C.sub.2-4 -alkenyloxy, phenyl-C.sub.2-4 -alkenyloxy, aryloxy, haloaryloxy, C.sub.1-4 -alkylaryloxy, arylamino, haloarylamino, C.sub.1-4 -alkylarylamino, aryl-N--C.sub.1-4 -alkylamino, aryl-N--C.sub.1-4 acylamino, aroyl, haloaroyl, C.sub.1-4 -alkylaroyl, aryl, haloaryl, C.sub.1-4 -alkylaryl or halo,A is O or S andB is CH.sub.2 or O,processes for their preparation and their use as insecticides and acaricides.
    • 描述了通式I(I)的新化合物,其中R 1是被C 1-4 - 烷基,卤代C 1-4 - 烷基,苯基-C 1-4 - 烷基,C 2-4 - 烷基取代的芳基或芳基, 烯基,卤代C 2-4链烯基,苯基-C 2-4链烯基,C 2-4炔基,卤代C 2-4炔基,苯基-C 2-4亚烷基,C 1-4 - 烷氧基, 4-烷氧基,苯基-C 1-4 - 烷氧基,C 2-4 - 烯氧基,烷基磺酰氧基,卤代烷基磺酰氧基,芳基磺酰氧基,卤代C 2-4 - 烯氧基,苯基-C 2-4-烯氧基,卤素,氰基,硝基,芳氧基, C 1-4 - 烷基氧基或硝基-C 1-4 - 烷基芳氧基,R 2和R 3相同或不同,为氢,氟,氰基或乙炔基,R 4为苯基或吡啶基,或这些基团被一个或多个C 1-6 - 烷基,卤代C 1-6 - 烷基,苯基-C 1-6 - 烷基,被O-,N-或S-原子间隔的C 1-6 - 烷基,C 2-4链烯基,卤代C 2-4 - 烯基 苯基-C 2-4 4-烯基,C 1-4 - 烷氧基,卤代-C 1-4 - 烷氧基,苯基-C 1-4 - 烷氧基,C 2-4 - 烯氧基,卤代-C 2-4 4-烯基氧基,苯基-C 2-4 - 烯氧基,芳氧基,卤代芳氧基,C 1-4 - 烷基芳氧基,芳基氨基,卤素 芳基-N-C 1-4烷基氨基,芳基-N-C 1-4酰基氨基,芳酰基,卤代酰基,C 1-4 - 烷酰基,芳基,卤代芳基,C 1-4 - 烷基芳基或卤素,A 是O或S且B是CH 2或O,其制备方法及其作为杀虫剂和杀螨剂的用途。