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    • 1. 发明申请
    • BENZENESULFONE COMPOUNDS AND SALTS THEREOF
    • 苯并呋喃酮化合物及其盐
    • WO1998008820A1
    • 1998-03-05
    • PCT/JP1997002934
    • 1997-08-25
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.YOKOTA, MasakiKAWAZOE, SouichirouOKAMOTO, YoshinoriKUBOTA, HirokazuNAITO, RyoARAKIDA, Yasuhito
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D215/12
    • C07D215/14
    • Benzenesulfone compounds represented by general formula (I) or pharmaceutically acceptable salts thereof, useful as pharmaceuticals having a combination of leucotriene antagonism with thromboxane A2 antagonism and good oral absorbability, especially as agents for preventing and treating diseases and which leucotriene and thromboxane A2 participate, such as bronchial asthma, wherein B represents an optionally substituted quinolyl group; D represents an optionally substituted phenyl group; E represents a group represented by formulas (a), (b), or (c); one of A and A represents an optionally substituted methylene group or an optionally substituted ethylene group with the other representing a single bond, an optionally substituted methylene group, or an optionally substituted ethylene group, provided that when 1 is 1 and Y represents an optionally substituted phenylene group, each of A and A may represent a single bond; X represents an oxygen atom or a sulfur atom; Y represents an optionally substituted phenylene group, an optionally substituted phenyleneoxy group, or an optionally substituted spirocyclopropinyl group; Z represents a group represented by the formula: -CH=CH-, -CH2-CH2-, -CH2O-, or -O-CH2-; R represents a carboxyl group or tetrazolyl group which may be optionally substituted with an ester residue; 1, n, p, and q, which may be the same or different, are each 0 or 1; and m represents 1, 2, or 3.
    • 通式(I)表示的苯磺酸盐或其药学上可接受的盐,其可用作具有白三烯拮抗作用与血栓素A2拮抗作用的组合和良好的口服吸收性的药物,特别是作为预防和治疗疾病的药物以及白内障和血栓素A2参与的药物 作为支气管哮喘,其中B表示任选取代的喹啉基; D表示任选取代的苯基; E表示由式(a),(b)或(c)表示的基团。 A 1和A 2之一表示任选取代的亚甲基或任选取代的亚乙基,另一个代表单键,任选取代的亚甲基或任选取代的亚乙基,条件是当1为1时 Y表示任意取代的亚苯基,A 1和A 2中的每一个可以表示单键; X表示氧原子或硫原子; Y表示任选取代的亚苯基,任选取代的亚苯基氧基或任选取代的螺环丙基; Z表示由下式表示的基团:-CH = CH-,-CH 2 -CH 2 - , - CH 2 O - 或-O-CH 2 - ; R表示可任选被酯残基取代的羧基或四唑基; 1,n,p和q可以相同或不同,各自为0或1; m表示1,2或3。
    • 2. 发明申请
    • AZOLE DERIVATIVE
    • 偶像衍生
    • WO1996011916A1
    • 1996-04-25
    • PCT/JP1995002085
    • 1995-10-12
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.NAGAOKA, HitoshiYOKOTA, MasakiAKANE, HiroakiARAKIDA, YasuhitoISOMURA, Yasuo
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D263/32
    • C07D263/56C07D277/24C07D277/26C07D277/30C07D277/36C07D277/64C07D413/12C07D417/12
    • An azole derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having both of a leukotriene antagonistic effect and a thromboxane A2 antagonistic effect and being useful in preventing or treating allergic diseases, ischemic heart diseases or ischemic brain diseases, and a medicinal composition containing the same as the active ingredient, wherein R and R may be the same or different and represent each hydrogen, cycloalkyl, etc., or R and R together with (a) may form a fused ring (b) or (c) which may be substituted by optionally substituted lower alkyl, amino, etc.; R , R , R and R may be the same or different and represent each hydrogen, amino, etc.; R represents cyano, tetrazolyl, -COOR , etc.; R represents hydrogen or lower alkyl; D represents optionally substituted lower alkylene; X and Z may be the same or different and represent each oxygen or sulfur; Y represents -N= or -CH=; A represents -O-B-, -B-O-, -S-B-, -B-S- or -B- (B being lower alkylene or lower alkenylene); and n is 0, 1 or 2.
    • 由通式(I)表示的唑衍生物或其药学上可接受的盐具有白细胞三烯拮抗作用和血栓素A2拮抗作用,可用于预防或治疗过敏性疾病,缺血性心脏病或缺血性脑病,以及 含有与活性成分相同的药物组合物,其中R 1和R 2可以相同或不同,表示各个氢,环烷基等,或R 1和R 2与(a )可以形成可被任选取代的低级烷基,氨基等取代的稠环(b)或(c); R 3,R 6,R 7和R 8可以相同或不同,表示各个氢,氨基等; R 4表示氰基,四唑基,-COOR 9等; R 5表示氢或低级烷基; D表示任选取代的低级亚烷基; X和Z可以相同或不同,表示每个氧或硫; Y表示-N =或-CH =; A表示-O-B-,-B-O-,-S-B-,-B-S-或-B-(B为低级亚烷基或低级亚烯基); n为0,1或2。