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    • 21. 发明专利
    • 17beta-hydroxysteroid dehydrogenase inhibitors
    • AU2004224061B2
    • 2011-06-16
    • AU2004224061
    • 2004-03-22
    • STERIX LTD
    • BUBERT CHRISTIANLAWRENCE HARSHANI RITHMA RUCHIRANANIPUROHIT ATULPOTTER BARRY VICTOR LLOYDFISCHER DELPHINE SOPHIE MARIONALLAN GILLIAN MARGARETVICKER NIGELREED MICHAEL JOHN
    • C07J71/00A61K31/56A61K31/566C07J20060101C07J41/00
    • There is provided a compound of Formula I wherein (I) R 1 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R 2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) =N-O-alkyl or =N-O-H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is - CH 2 - or -CH 2 CH 2 -, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO so that R 1 together with R 3 provide the enol tautomer OR R 1 together with R 3 form (xii) a pyrazole wherein (a) R 4 is =N-O-alkyl or =N-O-H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2 position is substituted with a group selected from -OH and -O-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula (II) R 2 is selected from groups capable of forming a hydrogen bond , a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III)R 3 is selected from -OH, =O, or a -C(=O)- mimetic
    • 27. 发明专利
    • COMPOUND
    • CA2519956C
    • 2012-12-18
    • CA2519956
    • 2004-03-22
    • STERIX LTD
    • VICKER NIGELLAWRENCE HARSHANIALLAN GILLIANBUBERT CHRISTIANFISCHER DELPHINEPUROHIT ATULREED MICHAELPOTTER BARRY
    • C07J71/00A61K31/56A61K31/566C07J20060101C07J41/00
    • There is provided a compound of Formula (I) wherein (I) R1 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkyiheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) =N-O-alkyl or =N-O-H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is - CH2- or -CH2CH2-, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of a I kyl heterocycle group, al ke nyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO so that R, together with R3 provide the enol tautomer (a); OR R1 together with R3 form (xii) a pyrazole wherein (a) R4 is =N-0-alkyl or =N-0-H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl. group, branched alkyl group, and an amide and/or (c) the 2 position is substituted with a group selected from -OH and -0-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula (b); (II) R2is selected from groups capable of forming a hydrogen bond, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III) R3 is selected from -OH, =O, or a -C(=O)-mimetic.
    • 29. 发明专利
    • COMPOUND
    • CA2703893A1
    • 2009-05-28
    • CA2703893
    • 2008-11-19
    • STERIX LTD
    • VICKER NIGELBAILEY HELEN VICTORIAHEATON WESLEYDAY JOANNA MARYPUROHIT ATULPOTTER BARRY VICTOR LLOYD
    • C07C209/14A61K31/167A61K31/36A61K31/4409A61P5/24A61P35/00C07C211/50C07C233/43C07C237/42C07D207/26C07D211/58C07D211/62C07D317/66
    • There is provided a compound having Formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, -OC(R13)3, -OCH(R13)2, -OCH2R13, -C(R13)3, -CH(R13)2, or -CH2R13 wherein R13 is a halogen; (c) -CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (I) aryloxy; (m) -SO2-alkyl; and (n) -N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (T) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=O, S(=O)2, C=O, S(=O)2NR16, C=ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C=O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.