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    • 7. 发明授权
    • Biologically active peptides and compositions, their use
    • 生物活性肽和组合物,其用途
    • US6153590A
    • 2000-11-28
    • US930584
    • 1998-02-02
    • Raymond AndersenJohn ColemanDilip De SilvaFangming KongEdward PiersDebra WallaceMichel RobergeTeresa Allen
    • Raymond AndersenJohn ColemanDilip De SilvaFangming KongEdward PiersDebra WallaceMichel RobergeTeresa Allen
    • A61K38/00A61P35/00C07K5/02C07K5/027C07K5/078C07K5/08C07K5/083
    • C07K5/0205C07K5/0827A61K38/00
    • Compounds of general formula I ##STR1## wherein: R.sub.1 and R.sub.70 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; R.sub.2 represents a hydrogen atom or an optionally substituted alkyl or acyl group or is absent when R.sub.6 represents a group --CH.dbd. as hereinafter described; R.sub.73 represents a hydrogen atom or an optional substituent or is absent when R.sub.6 represents a methylene group or a group --CH.dbd. as hereinafter described; Y represents an optional substituent; n represents 0, 1, 2, 3, or 4; R.sub.3 represents a hydrogen atom, or an optionally substituted alkyl group; R.sub.74 represents a hydrogen atom, a hydroxy group or an optionally substituted alkyl or acyl group; R.sub.7 represents a hydrogen atom or an alkyl group; R.sub.75 represents an optionally substituted alkyl group; and i) R.sub.6 and R.sub.71 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group; and R.sub.72 represents a hydrogen atom; or ii) R.sub.71 represents a hydrogen atom or an optionally susbtituted alkyl or acyl group and R.sub.72 represents a hydrogen atom or R.sub.71 and R.sub.72 are joined together such that a double bond is formed between the carbon atoms to which they are attached; and R.sub.6 represents an optionally substituted methylene group bonded to the indole moiety thereby forming a tricyclic moiety; or R.sub.6 represents an optionally substituted group --CH.dbd. bonded to the indole moiety thereby to form an aromatic tricyclic moiety; for use in therapy and as antimitotic reagents are described.
    • PCT No.PCT / GB96 / 00942 Sec。 371日期1998年2月2日 102(e)1998年2月2日PCT 1996年4月22日PCT PCT。 出版物WO96 / 33211 日期:1996年10月24日通式I化合物其中:R 1和R 70独立地表示氢原子或任选取代的烷基或酰基; R2表示氢原子或任选取代的烷基或酰基,或当R6表示基团-CH =时不存在,如下所述; 当R 6表示亚甲基或-CH =如下所述时,R 73表示氢原子或任选的取代基或不存在; Y表示任选的取代基; n表示0,1,2,3或4; R3表示氢原子或任选取代的烷基; R 74表示氢原子,羟基或任选取代的烷基或酰基; R7表示氢原子或烷基; R75表示任选取代的烷基; 和i)R 6和R 71独立地表示氢原子或任选取代的烷基或酰基; R 72表示氢原子; 或ii)R 71表示氢原子或任选取代的烷基或酰基,R 72表示氢原子或R 71和R 72连接在一起,使得在它们所连接的碳原子之间形成双键; 并且R 6表示与吲哚部分键合的任选取代的亚甲基,从而形成三环部分; 或R6表示与吲哚部分键合的任选取代的基团-CH =,从而形成芳族三环部分; 用于治疗和用作抗有益剂的试剂。
    • 10. 发明申请
    • Ceratamines A and B, and Analogues, Syntheses and Pharmaceutical Compositions Thereof
    • Ceratamines A和B及其类似物,合成和药物组合物
    • US20080255090A1
    • 2008-10-16
    • US10571932
    • 2004-09-15
    • Raymond J. AndersenMichel RobergeEmiliano Manzo
    • Raymond J. AndersenMichel RobergeEmiliano Manzo
    • C07D487/04A61K31/55A61P35/00
    • C07D487/04
    • Antimitotic compounds and salts are provided in which the compound has the structure (formula (I)): wherein X and Y are substituted or unsubstituted and are selected from carbon atoms and atoms of groups 15 and 16 of the periodic table; Z is selected from N—R, O and S; U is selected from CR1, N, NH, NR, S and O, R1, R2, and R3 are independently selected from H, NH2, NHR, NR2, SH, SR, SiR3, OH, OR, F, CI, Br, I, ═O, ═S and R; W is selected from O, S, and H2; R4 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NR2 and halide; R is selected from H, substituted or unsubstituted aryl, and substituted or unsubstituted 1 to 20 carbon linear, branched, or cyclic, saturated or unsaturated alkyl, in which alkyl carbon atoms are replaced by 0 to 10 oxygen, 0 to 10 sulphur, and 0 to 10 N atoms; and wherein bonds to carbon atoms or to any of X, Y, Z and U are saturated or unsaturated; and providing that when W is H2, R4 is not H, OH, or unsubstituted phenyl.
    • 提供了其中化合物具有结构(式(I))的反仿构化合物和盐:其中X和Y是取代或未取代的,并且选自周期表第15和16族的碳原子和原子; Z选自N-R,O和S; U选自CR 1,N,NH,NR,S和O,R 1,R 2和R 3 独立地选自H,NH 2,NHR,NR 2,SH,SR,SiR 3,OH,OR, F,Cl,Br,I,-O,-S和R; W选自O,S和H 2; R 4选自H,R,OH,OR,SH,SR,NH 2,NHR,NR 2和卤素; R选自H,取代或未取代的芳基和取代或未取代的1至20个直链,支链或环状饱和或不饱和的烷基,其中烷基碳原子被0至10个氧,0至10个硫代替,以及 0〜10N原子; 并且其中与碳原子或X,Y,Z和U中的任一个的键是饱和或不饱和的; 并且当W是H 2 H时,R 4不是H,OH或未被取代的苯基。