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    • 2. 再颁专利
    • Prophylactic and therapeutic composition for circulatory disorders and
method of treatment
    • 循环障碍的预防和治疗组合物及治疗方法
    • USRE35801E
    • 1998-05-19
    • US309558
    • 1994-09-20
    • Hiroyoshi NishiToshiaki WatanabeSatoshi YukiYasuhiro MorinakaKatsuhiko IsekiHiroko Nakajima (nee Sakurai)
    • Hiroyoshi NishiToshiaki WatanabeSatoshi YukiYasuhiro MorinakaKatsuhiko IsekiHiroko Nakajima (nee Sakurai)
    • C07D231/20C07D231/22C07D231/26C07D231/28C07D231/56A61K31/415
    • C07D231/56C07D231/20C07D231/22C07D231/26C07D231/28
    • A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group, or a pharmaceutically acceptable salt thereof as an active ingredient. The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor against lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.
    • 一种循环系统疾病的预防和治疗剂,其包含下式的吡唑啉酮衍生物:其中R 1表示氢原子,芳基,具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R 2表示氢原子,芳氧基,芳基巯基,碳原子数1〜5的烷基或碳原子数1〜3的羟烷基,或者R 1和R 2一起表示碳原子数3〜5的亚烷基。 R3表示氢原子,碳原子数1〜5的烷基,碳原子数5〜7的环烷基,碳原子数1〜3的羟烷基,苄基,萘基或苯基, 未取代或被1〜3个选自碳原子数1〜5的烷基,碳原子数为1〜5的烷氧基,碳原子数1〜3的烷氧基,碳原子数1〜3的烷氧基,烷氧基羰基, 总碳数为2至5,具有1至3个碳原子的烷基巯基,具有1至4个碳原子的烷基氨基,总碳数为2至8的二烷基氨基,卤素原子,三氟甲基,羧基,氰基,羟基 基团,硝基,氨基和乙酰胺基,或其药学上可接受的盐作为活性成分。 本发明的药剂可用作循环障碍的预防和治疗剂,特别是作为抗脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。
    • 4. 发明授权
    • 1-arylpyrazoles
    • 1-芳基吡唑
    • US5079370A
    • 1992-01-07
    • US681886
    • 1991-04-08
    • Themistocles D. J. D'SilvaGail S. PowellPhilip R. TimmonsRichard G. Pennicard
    • Themistocles D. J. D'SilvaGail S. PowellPhilip R. TimmonsRichard G. Pennicard
    • C07D231/28
    • C07D231/28
    • The invention describes novel 3-cyano-4-sulfenylated-5-alkoxy-1-arylpyrazoles of general formula(I) ##STR1## wherein typically preferred substituents are: R is C.sub.1 to C.sub.4 alkyl fully substituted by halogen;R.sub.1 is C.sub.1 to C.sub.4 alkyl, C.sub.3 to C.sub.6 alkenyl and alkynyl or aralkyl (each of which may be optionally substituted), dialkylaminocarbonyl or a group --P(.dbd.X)(Oalkyl)(Salkyl) wherein X is oxygen or sulfur;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are each hydrogen or halogen;R.sub.4 is CF.sub.3, OCF.sub.3, SCF.sub.3, SOCF.sub.3, SO.sub.2 CF.sub.3, OCHF.sub.2, halogen or alkyl; and n is 0, 1 or 2.The invention further relates to intermediates and processes to make the compounds and to compositions thereof and to methods of control of arthopod (especially insect) nematode, helminth, and protozoan pests.
    • 本发明描述了通式(I)的新的3-氰基-4-亚磺酰基-5-烷氧基-1-芳基吡唑,其中通常优选的取代基是:R是被卤素完全取代的C1-C4烷基; R 1为C 1至C 4烷基,C 3至C 6烯基和炔基或芳烷基(其各自可任选被取代),二烷基氨基羰基或基团-P(= X)(O烷基)(S烷基),其中X为氧或硫; R2,R3,R5和R6各自为氢或卤素; R4是CF3,OCF3,SCF3,SOCF3,SO2CF3,OCHF2,卤素或烷基; 本发明进一步涉及制备化合物及其组合物的中间体和方法以及控制蒿草(尤其是昆虫)线虫,蠕虫和原生动物害虫的方法。
    • 7. 发明授权
    • 4-Substituted pyrazoles
    • 4-取代的吡唑
    • US4112109A
    • 1978-09-05
    • US766187
    • 1977-02-07
    • Eike MollerKarl Meng, deceasedEgbert WehingerHarald HorstmannFriedel Seuter
    • Eike MollerKarl Meng, deceasedEgbert WehingerHarald HorstmannFriedel Seuter
    • C07D231/20C07D231/28A61K31/415
    • C07D231/20C07D231/28Y10S514/822Y10S514/869
    • Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.
    • 其中R为氢,烷基,芳基,芳烷基,三氟甲基或杂环的吡唑类化合物。 R 1为未取代或被卤素,三氟甲基,烷基,烷氧基或硝基取代的芳基或芳烷基; 或卤素取代的烷硫基部分; R2是低级烷基; 苯基; 或苄基; R 3为未取代的或被烷基,烯基,烷氧基,卤素,三氟甲基,三氟甲氧基,单 - 或二 - 烷基氨基,硝基,氰基,甲酰氨基,磺酰氨基或SO-烷基取代的芳基; 与5至7元环或杂环稠合的苯基,所述杂环具有1或2个氧或硫杂原子; 或吡啶基; 并且R 4是未取代的或取代的碳酰基或磺酰基; 有用于他们的DIYTIC,SALURETIC,ANTIHYPERTENSIVE和抗生素属性。