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    • 45. 发明公开
    • Milbemycin ether derivatives, their preparation and their therapeutic and agrochemical uses
    • 米尔倍霉素醚衍生物,其制备及其治疗和农用化学用途
    • EP0552817A2
    • 1993-07-28
    • EP93105233.6
    • 1991-03-01
    • Sankyo Company Limited
    • Morisawa, YasuhiroSaito, Akio,c/o Sankyo Company Ltd.Toyama, Toshimitsu, c/o Sankyo Company Ltd.Kaneko, Susumu, c/o Sankyo Company Ltd.
    • C07D493/22A61K31/365A01N43/90
    • C07D493/22A01N43/90C07H19/01
    • Compounds of formula (I):


      in which: R 1 is a variety of organic groups; R 2 is hydrogen, halogen, cyano, nitro, optionally substituted alkyl, alkoxy, alkoxyalkoxy, or a group of formula:













      or

      (in which m is 1 or 2; n is 0, 1 or 2; R 6 is a variety of organic groups; R 7 is alkyl, cycloalkyl, or aralkyl; R 9 is hydrogen or alkyl; R 10 is any of R 6 , or cyano, nitro, -COOR 7 , or -COR 6 ; Y is oxygen or sulphur; Z is -COOR 7 , -COR 6 or -S0 2 R 6 ); Q is methylene, ethylene or -OCH 2 -; P is methylene, ethylene, oxygen or a single bond; V and W each represents methylene, carbonyl or thiocarbonyl; R 3 and R 4 are hydrogen, alkyl or alkoxy; R 11 is alkyl, alkoxy, alkylthio, alkanoyloxy, alkoxycarbonyl, halogen, cyano, nitro, amino, mono- or di- alkylamino, carbamoyl, mono- or di- alkylcarbamoyl, or alkanoylamino; R 12 is hydrogen or alkyl; R 13 is alkyl; R 5 is methyl, ethyl, isopropyl or sec-butyl; and X is hydroxy, alkanoyloxy or hydroxyimino] and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.
    • 式(I)化合物:其中:R1是多种有机基团; R 2是氢,卤素,氰基,硝基,任选取代的烷基,烷氧基,烷氧基烷氧基或下式的基团:或(其中m是1或2; n是0,1或2; R 6是各种有机基团; R 7是烷基,环烷基或芳烷基; R 9是氢或烷基; R 10是R 6或氰基,硝基,-COOR 7或-COR 6中的任一个; Y是氧或硫; Z是-COOR 7,-COR 6或-SO 2 R 6) ; Q是亚甲基,亚乙基或-OCH 2 - ; P是亚甲基,亚乙基,氧或单键; V和W各代表亚甲基,羰基或硫代羰基; R3和R4是氢,烷基或烷氧基; R11为烷基,烷氧基,烷硫基,烷酰氧基,烷氧羰基,卤素,氰基,硝基,氨基,单或二烷基氨基,氨基甲酰基,单或二烷基氨基甲酰基或烷酰基氨基; R12是氢或烷基; R13是烷基; R5是甲基,乙基,异丙基或仲丁基; 和X是羟基,烷酰氧基或肟基]并且它们的盐和酯具有有价值的驱虫,杀螨和杀昆虫活性。 还提供了制备这些化合物的方法。
    • 50. 发明公开
    • Fluoromacrolides having immunosuppressive activity
    • 氟喹诺酮类免疫抑制剂Wirkung。
    • EP0530888A1
    • 1993-03-10
    • EP92202506.9
    • 1992-08-14
    • MERCK & CO. INC.
    • Goulet, MarkBeattie, Thomas R.Wyvratt, Matthew J.
    • C07H19/01A61K31/70A61K7/06
    • C07H19/01
    • Fluoromacrolides and derivatives of the general structural Formula I:

      have been prepared from suitable precursors by oxidation and fluorination at C-20. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma. Furthermore, these macrolides are useful as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis.
    • 氟代丙烯酰胺和通式结构式I的衍生物:通过C-20的氧化和氟化由合适的前体制备。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫疾病,感染性疾病和/或预防外来器官移植排斥反应。 此外,这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。 此外,这些大环内酯可用于治疗可逆性阻塞性气道疾病,特别是哮喘。 此外,这些大环内酯可用作头发活化剂,特别是用于治疗男性脱发或脱发性秃发症。