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    • 41. 发明授权
    • Vinyl tricarbonyl compounds and methods of making the same
    • 乙烯基三羰基化合物及其制备方法
    • US4929751A
    • 1990-05-29
    • US109804
    • 1987-10-19
    • Harry H. WassermanNatesan MurugesanJohn H. Van Duzer
    • Harry H. WassermanNatesan MurugesanJohn H. Van Duzer
    • C07C69/738C07D231/12C07D263/32C07D401/06C07D403/06C07D405/06
    • C07D401/06C07C69/738C07D263/32C07D403/06C07D405/06
    • A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.
    • 其中R1是氢,卤素,未取代或取代的C1至C30烷基,未取代或取代的芳基,芳基烷基和具有3至7个碳原子的环烷基的式IMAMA的乙烯基三羰基化合物或其一水合物 R 2为氢,卤素,未取代或取代的C 1 -C 30烷基,未取代或取代的芳基,芳基烷基,具有3至7个碳原子的环烷基,氰基,硝基或杂环基,R 3为氢,卤素,未取代或取代的C 1至C 30 烷基,未取代或取代的芳基,芳基烷基,具有3至7个碳原子的环烷基,氰基,硝基或杂环,并且R 4是未取代或取代的C 1至C 30烷基,未取代或取代的芳基,芳烷基,环烷基具有3至7个碳原子 。 这种乙烯基三羰基化合物对肿瘤细胞有效。
    • 43. 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。