会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明授权
    • Inhibitors of farnesyl protein transferase
    • US06455523B1
    • 2002-09-24
    • US09374210
    • 1999-08-13
    • Charles Z. DingSoong-Hoon KimJohn T. HuntToomas MittRajeev BhideKaterina Leftheris
    • Charles Z. DingSoong-Hoon KimJohn T. HuntToomas MittRajeev BhideKaterina Leftheris
    • A61K3155
    • C07D243/14C07D401/14C07D403/06C07D403/14C07D405/14C07D409/14C07D413/14C07D417/14C07D471/04C07D473/00C07D487/04C07D495/04
    • Inhibition of farnesyl transferase, which is an enzyme involved in ras ocogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof inhibit farnesyl protein transferase which is an enzyme involved in ras oncogene expression. In formulas I-IV and throughout their specification, the above symbols are defined as follows: m, n, r, s and t are 0 or 1; p is 0, 1 or 2; V, W and X are selected from the group consisting of oxygen, hydrogen, R1, R2 or R3; Z and Y are selected from the group consisting of CHR9, SO2, SO3, CO, CO2, O, NR10, So2NR11, CONR12, or Z may be absent; R6, R7, R9, R10, R11, R12 R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R24, R25, R26, R27, R28, R29, R30, R31, R32,R33, R34, R35, R36, R37, and R38 are selected from the group consisting of hydrogen, lower alkyl, substituted alkyl, aryl or substituted aryl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R23; U is selected from the group consisting of sulfur, oxygen, NR24, CO, SO, SO2, CO2, NR25CO2, NR26CONR27, NR28SO2, NR29SO2NR30, SO2NR31, NR32CO, CONR33, PO2R34 and PO3R35 or U is absent; R1, R2, and R3 are selected from the group consisting of hydrogen, alkyl, alkoxycarbonyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo, cyano, carboxy, carbamyl (e.g. CONH2) or substituted carbamyl further selected from CONH alkyl, CONH aryl, CONH aralkyl or cases where there are two substituents on the nitrogen selected from alkyl, aryl or aralkyl; R8 and R23 are selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo; Any two of R1, R2, and R3 can be joined to form a cycloalkyl group; R, S and T are selected from the group consisting of CH2, CO and CH(CH2)pQ wherein Q is NR36R37, OR38, or CN; and A, B, C and D are carbon, oxygen, sulfur or nitrogen. with the provisos that 1. When m is zero then V and W are not both oxygen or 2 W and X together can be oxygen only if Z is either absent, O, NR10, in formulas I and II, and V and X together can be oxygen only if Y is O, NR10, in formulas III and IV or 3. R23 may be hydrogen except when U is SO, SO2, NR25CO2 or NR28SO2, or 4. R8 may be hydrogen except when Z is SO2, CO2, or
    • 10. 发明授权
    • Phenyl sulfonamide endothelin antagonists
    • 苯磺酰胺内皮素拮抗剂
    • US6107320A
    • 2000-08-22
    • US584767
    • 1996-01-11
    • Natesan MurugesanJohn T. Hunt
    • Natesan MurugesanJohn T. Hunt
    • A61K31/42A61K31/422A61K31/423C07D261/12C07D261/16C07D261/18C07D261/20
    • C07D261/16C07D261/18C07D261/20
    • Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently(a) hydrogen, except that R.sup.1 is other than hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.
    • 该化合物可抑制内皮素的活性。 符号定义如下:R1,R2和R3各自独立地为(a)氢,除了R1不是氢; (b)烷基,烯基,炔基,烷氧基,环烷基,环烷基烷基,环烯基,环烯基烷基,芳基,芳氧基,芳烷基或芳烷氧基,其中任一个可以被Z1,Z2和Z3取代; (c)卤素; (d)羟基; (e)氰基; (f)硝基; (g)-C(O)H或-C(O)R 6; (h)-CO 2 H或-CO 2 R 6; (ⅰ)-SH,-S(O)nR 6,-S(O)m -OH,-S(O)m -OR 6,-OS(O)m -R 6,-OS(O)mOH或-OS O)m-OR6; (j)-Z4-NR7R8; 或(k)-Z4-N(R11)-Z5-NR9R10; 其余符号如说明书中所定义。