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    • 1. 发明申请
    • ANTITUMORAL ANALOGS OF LAMELLARINS
    • 层状蛋白的抗肿瘤类似物
    • WO2004014917A3
    • 2004-05-13
    • PCT/GB0303541
    • 2003-08-13
    • PHARMA MAR SAUBAILLY CHRISTIANFRANCESCH SOLLOSO ANDRESMATEO URBANO MARIA CRISTINAJIMENEZ GUERRERO JOSE ANTONIOPASTOR DEL CASTILLO ALFREDOCUEVAS MARCHANTE CARMENRUFFLES GRAHAM KEITH
    • BAILLY CHRISTIANFRANCESCH SOLLOSO ANDRESMATEO URBANO MARIA CRISTINAJIMENEZ GUERRERO JOSE ANTONIOPASTOR DEL CASTILLO ALFREDOCUEVAS MARCHANTE CARMEN
    • C07D491/147A61K31/437A61K31/4745A61P35/00A61P43/00C07D471/14C07D491/00C07D491/14A61K31/435C07D471/04
    • C07D471/14C07D491/14
    • New lamellarins are provided of the general formula III wherein X is selected from the group consisting of N, O and S; wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR', SH, SR', SO2R', NHR', N(R')2, N=R', NHCOR', N(COR')2, NHS02R', N02, PO(R'2, P02R', C(=0)H, C(=0)R', C02H, C02R', OPO(R')2, OP02R', OC(=0)H, OC(=0)R', N=C(R')2, substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted C1-C12 haloalkyl, substituted or unsubstituted C2-C12 alkenyl, substituted or unsubstituted C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R' groups is independently selected from the group consisting of H, OH, N02, NH2, SH, CN, halogen, =0, C(=0)H, C(=O)CH3, C02H, C(=0)R', substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-C18 alkoxyl, substituted or unsubstituted C1-C18 aminoalkyl, substituted or unsubstituted C1-C18 aminoacid, substituted or unsubstituted C1-C18 thioalkyl, substituted or unsubstituted C1-C18 alkylsulfinyl, substituted or unsubstituted C1-C18 alkylsulfonyl; wherein the pairs of groups R1 and R2, R2 and R3, R3 and R4, R3 and R9, R4 and R9, R9 and R5, R9 and R6, or R6 and R7, R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and the dotted line represents an single or double bond; or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof.
    • 提供了通式III的新片晶蛋白,其中X选自N,O和S; 其中R1,R2,R3,R4,R5,R6,R7,R8和R9各自独立地选自H,OH,OR',SH,SR',SO2R',NHR',N 2,N = R',NHCOR',N(COR')2,NHSO 2 R',NO 2,PO(R'2,PO 2 R',C(= O)H,C(= O)R',CO 2 H, (= O)H,OC(= O)R',N = C(R')2,取代或未取代的C 1 -C 12烷基,取代或未取代的C 1 -C 12卤代烷基 取代或未取代的C 2 -C 12烯基,取代或未取代的C 2 -C 12炔基,取代或未取代的芳基,取代或未取代的芳烷基和取代或未取代的杂芳族基团;其中每个R'基团独立地选自H,OH (= O)CH 3,CO 2 H,C(= O)R',取代或未取代的C 1 -C 18烷基,取代或未取代的C 2 -C 6烷基,取代或未取代的C 1 -C 18烷基, -C 18烯基,取代或未取代的C 2 -C 18炔基,取代或未取代的芳基,取代或未取代的C 1 -C 18烷氧基,取代或未取代的C 1 -C 18氨基烷基, 取代或未取代的C 1 -C 18硫代烷基,取代或未取代的C 1 -C 18烷基亚磺酰基,取代或未取代的C 1 -C 18烷基磺酰基; 其中基团对R1和R2,R2和R3,R3和R4,R3和R9,R4和R9,R9和R5,R9和R6或R6和R7,R7和R8可以连接成碳环或杂环 系统; 虚线表示单键或双键; 或其药学上可接受的盐,衍生物,前药或立体异构体。