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    • 42. 发明申请
    • 4-[2-(PYRIMIDIN-4-OXY- OR 4-YLAMINO)-ETHYL]-PHENYL-OXIMES
    • 4- [2-(吡啶基-4-氧代 - 或4-氯苯基) - 乙基] - 苯基氧化
    • WO1997009316A1
    • 1997-03-13
    • PCT/EP1996003864
    • 1996-09-03
    • SANDOZ LTD.SANDOZ-PATENT-GMBHSANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SCHAUB, FritzLAMBERTH, Clemens
    • SANDOZ LTD.SANDOZ-PATENT-GMBHSANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.
    • C07D239/42
    • C07D495/04A01N43/54C07C69/78C07C251/48C07C251/54C07D239/34C07D239/88C07D239/94
    • The invention discloses 4-[2-(pyrimidin-4-yloxy- or -4-ylamino)-ethyl]-phenyl-oximes of formula (I), wherein Z is NH or oxygen, R1 is hydrogen, C1-4alkyl, C1-4haloalkyl or C3-6cycloalkyl, R2 is hydrogen, C1-10alkyl, C3-8alkenyl, C3-8alkynyl, C3-8haloalkenyl, C1-8alkoxy-C1-4alkyl, C3-8alkenyloxy-C1-4alkyl, C3-8haloalkenyloxy-C1-4alkyl, C3-8alkynyloxy-C1-4alkyl, C1-8haloalkoxy-C1-4alkyl, C1-8alkylthio-C1-4alkyl, aryl, aryloxy-C1-4alkyl, aryl-C1-4alkoxy-C1-4alkyl, heteroaryloxy-C1-4alkyl, C1-4alkoxy-C1-4alkoxy-C1-4alkyl, or aryl-C1-8alkyl, R3 and R4 independently are halogen, C1-4alkyl, C1-4alkoxy, C1-4alkoxy-C1-4alkyl, C1-4alkoxycarbonyl-C1-4alkyl, C1-4alkoxycarbonyl, cyano-C1-4alkyl, cyano, or -COOH, or R3 and R4 together form a bridge member selected from 1,4-butylene, 1,4-butadienylene, or -S-CH=CH- each optionally substituted by one or two radicals selected from halogen or C1-4alkyl; the use of such compounds for the control of undesired acarinae, fungi, and insects, compositions for facilitating such use, and the preparation of the compounds of formula (I).
    • 本发明公开了式(I)的4- [2-(嘧啶-4-基氧基 - 或-4-基氨基) - 乙基] - 苯基 - 肟,其中Z是NH或氧,R 1是氢,C 1-4烷基,C 1 4-卤代烷基或C 3-6环烷基,R 2是氢,C 1-10烷基,C 3-8烯基,C 3-8炔基,C 3-8卤代烯基,C 1-8烷氧基-C 1-4烷基,C 3-8烯烃氧基-C 1-4烷基,C 3-8卤代烯氧基-C 1-4烷基 ,C 3-8炔基氧基-C 1-4烷基,C 1-8卤代烷氧基-C 1-4烷基,C 1-8烷硫基-C 1-4烷基,芳基,芳氧基-C 1-4烷基,芳基-C 1-4烷氧基-C 1-4烷基,杂芳氧基-C 1-4烷基,C 1 1-4烷氧基-C 1-4烷氧基-C 1-4烷基或芳基-C 1-8烷基,R 3和R 4独立地是卤素,C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基-C 1-4烷基,C 1-4烷氧基羰基-C 1-4烷基,C 1 -C 4烷氧基 4-烷氧基羰基,氰基-C 1-4烷基,氰基或-COOH,或R 3和R 4一起形成选自1,4-亚丁基,1,4-丁二烯基或-S-CH = CH-的桥连体,各自任选被 选自卤素或C 1-4烷基的一个或两个基团; 使用这种化合物来控制不希望的螨虫,真菌和昆虫,促进这种用途的组合物和式(I)化合物的制备。
    • 44. 发明申请
    • IMMUNOCOMPROMISED ANIMALS COMPRISING HUMAN SYNOVIAL TISSUE
    • 包含人体征服组织的免疫组织化学动物
    • WO1996039811A1
    • 1996-12-19
    • PCT/EP1996002457
    • 1996-06-06
    • SANDOZ LTD.SYSTEMIX, INC.SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SANDOZ-PATENT-GMBH
    • SANDOZ LTD.SYSTEMIX, INC.SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SANDOZ-PATENT-GMBHKNUDSEN, David, E., B.
    • A01K67/027
    • A01K67/0271
    • Immunocompromised hosts are provided, comprising a functional human synovial sac and articular cartilage. An intact human fetal patella is introduced into the xenogeneic host at a site that permits survival of the tissue, and permits experimental manipulation.Engrafted patella show early differentiation into a columnar matrix and stratification consistent with joint cartilage. The patellar articular surface is closely overlaid with a single layer of large cuboidal to attenuated cells with a central, oval to brick shaped nuclei and clear to pale eosinophilic cytoplasm consistent with synoviocytes. This layer reflects on itself at the margins of the patellar graft and closes, forming a complete envelope over the patellar articular surface. The human articular tissue is useful for investigating the effects of agents such as bacteria and bacterial peptides, cytokines and proteases on synovial function and dysfunction, growing neoplastic synovial sarcoma tissue in a natural environment, studying the hematopoietic interactions that are involved in various inflammatory arthritic diseases, and determining the role of HLA haplotypes in development of joint diseases.
    • 提供了免疫受损宿主,包括功能性人滑膜和关节软骨。 将完整的人胎儿髌骨引入到允许组织存活的位点的异种宿主中,并允许实验操作。移植的髌骨显示早期分化成柱状基质并且与关节软骨一致。 髌骨关节表面紧密地覆盖着一层大的长方体细胞,具有中心的,椭圆形到砖状的细胞核,并且与滑膜细胞一致的清澈至浅的嗜酸性细胞质。 该层在髌骨移植物的边缘自身反射并闭合,在髌骨关节面上形成完整的包膜。 人关节组织可用于研究细菌和细菌肽,细胞因子和蛋白酶等药物对滑膜功能和功能障碍的作用,在自然环境中生长的肿瘤滑膜肉瘤组织,研究各种炎症性关节炎疾病涉及的造血相互作用 ,并确定HLA单倍体在关节疾病发展中的作用。
    • 50. 发明申请
    • GLYCERIN DERIVATIVES AND USES THEREOF
    • 甘氨酸衍生物及其用途
    • WO1994010125A1
    • 1994-05-11
    • PCT/EP1993002917
    • 1993-10-21
    • SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SANDOZ-PATENT-GMBHSANDOZ LTD.NAGAHAMA, ShizuoOCHIAI, KeikoOHBA, SetsuyaTOMITA, TakakoWAKABAYASHI, Toshio
    • SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SANDOZ-PATENT-GMBHSANDOZ LTD.
    • C07C69/587
    • C07C69/587
    • A compound of formula (I) wherein R1 and R2 are acyl groups derived from different unsaturated fatty acids, both R1 groups being identical, one acyl group of R1 and R2 is an acyl group derived from eicosapentaenoic acid or docosahexaenoic acid, and theother acyl group is an acyl group derived from linoleic acid, gamma -linolenic acid, eicosapentaenoic acid or docosahexaenoic acid, and which is preferably in pure form comprising at least 90 % of the compound, has platelet aggregation inhibition activity and can be effectively used not only as a medicine for the therapy or prevention of thrombotic inflammation and platelet aggregation-induced arterial sclerosis, but also as a well-balanced nutrient clysis. Also certain compounds of formula (I), in particular the compound in which R1 is an eicosapentaenoyl residue and R2 is a gamma -linolenoyl residue, have anti-hypertriglyceridemic activity and are useful for the therapeutic treatment or prevention of diseases caused by hypertriglyceridemic such as cardiac infarction or arteriosclerosis.
    • 式(I)的化合物,其中R 1和R 2是衍生自不同不饱和脂肪酸的酰基,两个R 1基团相同,R 1和R 2的一个酰基是衍生自二十碳五烯酸或二十二碳六烯酸的酰基,以及其它酰基 是衍生自亚油酸,γ-亚麻酸,二十碳五烯酸或二十二碳六烯酸的酰基,其优选为包含至少90%的化合物的纯形式,具有血小板聚集抑制活性,并且可以有效地用作 用于治疗或预防血栓形成炎症和血小板聚集诱导的动脉硬化的药物,还可以作为平衡的营养物质溶解。 还有某些式(I)化合物,特别是其中R 1为二十碳五烯酰基残基且R 2为γ-亚苄基酰基残基的化合物具有抗高甘油三酯血症活性,并且可用于治疗或预防由高甘油三酯血症引起的疾病,例如 心肌梗塞或动脉硬化。