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
    • 2. 发明申请
    • Steroid sulphatase inhibitors
    • 类固醇硫酸酶抑制剂
    • US20010018435A1
    • 2001-08-30
    • US09794853
    • 2001-02-27
    • STERIX LIMITED
    • Michael John ReedBarry Victor Lloyd Potter
    • A61K031/565A61K031/18
    • A61K31/37C07D311/16C07D311/30C07D311/32C07D311/36C07J41/0072
    • A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula 1 wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent allylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid suiphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37null C. it would provide a Km value of less tha 50 nullM.
    • 描述了在需要相同的受试者中抑制类固醇硫酸酯酶活性的方法。 所述方法包括向所述受试者施用抑制甾族硫酸酯酶的量的环系化合物; 该环系化合物包含连接下式的氨基磺酸酯基的环,其中R 1和R 2各自独立地选自H,烷基,烯基,环烷基和芳基,或一起表示任选含有一个或多个杂原子或基团的烯丙基 在亚烷基链中; 并且其中所述化合物是具有类固醇脂肪酶活性的酶的抑制剂(E.C.3.1.6.2); 并且如果所述化合物的氨基磺酸酯基团被硫酸根基团取代以形成硫酸盐化合物,并在pH 7.4和37℃下与类固醇硫酸酶(EC3.1.6.2)一起温育,则其将提供小于50的Km值 muM
    • 3. 发明申请
    • COMPOUND
    • 复合
    • WO2007096647A2
    • 2007-08-30
    • PCT/GB2007/000655
    • 2007-02-26
    • STERIX LIMITEDVICKER, NigelALLAN, Gillian, MargaretLAWRENCE, Harshani, Rithma, RuchirananiDAY, Joanna, MaryPUROHIT, AtulREED, Michael, JohnPOTTER, Barry, Victor, Lloyd
    • VICKER, NigelALLAN, Gillian, MargaretLAWRENCE, Harshani, Rithma, RuchirananiDAY, Joanna, MaryPUROHIT, AtulREED, Michael, JohnPOTTER, Barry, Victor, Lloyd
    • C07D213/75C07C49/757C07D231/54C07D213/40C07D231/12C07D261/08C07D277/40C07D307/52C07C255/40C07D231/14C07D231/38C07D307/60C07C43/205C07C43/275C07D317/54
    • C07C323/22C07C37/62C07C45/00C07C45/46C07C45/673C07C45/68C07C45/71C07C49/747C07C49/753C07C49/755C07C49/757C07C49/83C07C49/84C07C49/86C07C59/90C07C69/712C07C69/738C07C235/74C07C235/78C07C235/84C07C255/40C07C2602/08C07C2602/10C07D213/40C07D213/75C07D231/12C07D231/38C07D241/12C07D261/08C07D277/40C07D317/54C07D401/12C07C39/367
    • There is provided a compound of Formula (I): wherein R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , and R 10 , are independently selected from -H, -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO 2 ), and halogens; wherein ring A is optionally further substituted wherein X is a bond or a linker group wherein (A) (i) R 9 is selected from alkyl and halogen groups; and (ii) R10 is selected from -OH, oxyhydrocarbyl and -OSO 2 NR 1 R 2 ; wherein R 1 and R 2 are independently selected from H and hydrocarbyl or (B) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is the group -C(=0)-CR 11 R 12 -R 8 wherein R 8 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, (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 or alkenyl-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, or together with another of R 3 , R 4 , R 5 , R 6 and R 7 the enol tautomer thereof wherein R 11 and R 12 are independently selected from H and hydrocarbyl; or (C) at least one of R 3 , R 4 , R 5 , R 6 and R 7 together with another of R 3 , R 4 , R 5 , R 6 and R 7 forms a ring containing -C(=O)-; or (D) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is selected from alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, and heteroaryl groups or (E) at least one of R 3 , R 4 , R 5 , R 6 and R 7 is selected from -CN, -C(R 13 )=N-O-alkyl group, - C(R 14 )=N-O-H group, optionally substituted pyrazole, optionally substituted thiazole, optionally substituted oxazole, optionally substituted isoxazole, optionally substituted pyridine, and optionally substituted pyrimidine, or together with another of R 3 , R 4 , R 5 , R 6 and R 7 forms a nitrogen containing ring; wherein R 13 and R 14 are independently selected from H and hydrocarbyl.
    • 提供式(I)的化合物:其中R 3,R 4,R 5,R 6,/ R 7,R 9和R 10独立地选自-H,-OH,烃基,羟基烃基,氰基 (-CN),硝基(-NO 2 N 2)和卤素; 其中环A任选进一步被取代,其中X是键或连接基团,其中(A)(i)R 9选自烷基和卤素基团; 和(ii)R 10选自-OH,羟基烃基和-OSO 2 NR 1 R 2 R 2。 其中R 1和R 2独立地选自H和烃基或(B)R 3,R 4中的至少一个 R 5,R 6和R 7是基团-C(= O)-CR 11, 其中R 8选自(ⅰ)烷氧基烷基(ⅱ)腈基,(ⅰ) iii)烷基芳基,其中芳基被除了其中芳基被取代的(C 1 -C 6)烯基芳基以外的其它取代基取代(v)烷基杂芳基,其中当杂芳基仅在环中仅包含C和N时, 芳基被甲基除外(vi)烯基杂芳基(vii)= NO-烷基或= NOH基(viii)支链烯基(ix)烷基醇基或链烯基(x)酰胺或烷基酰胺,其中 (a)烷基酰胺的烷基是-CH 2 - 或 - CH 2 CH 2 - ,(b)酰胺是二 - 取代和/或(c)酰胺被至少一个烷基取代 烯基杂环基,烷基杂芳基,烯基杂芳基,杂芳基,烷基胺基,烷氧基烷基,烷基芳基,直链或支链烷基,(xi)-CHO,或与另一个R 3 R 4,R 5,R 6和R 7其烯醇互变异构体,其中R 11 R 12和R 12独立地选自H和烃基; 或(C)R 3,R 4,R 5,R 6和R 6中的至少一个, 与R 3,R 4,R 5,R 6,R 6,R 5,R 5, 和R 7形成含有-C(= O) - 的环; 或(D)R 3,R 4,R 5,R 6和R 6中的至少一个, 选自烷基杂环基,烯基杂环基,烷基杂芳基,烯基杂芳基和杂芳基,或(E)R 3,R 4中的至少一个, R 5,R 6,R 7和R 7选自-CN,-C(R 13) )= NO-烷基,-C(R 14)= NOH基,任选取代的吡唑,任选取代的噻唑,任选取代的恶唑,任选取代的异恶唑,任选取代的吡啶和任选取代的嘧啶,或 与R 3,R 4,R 5,R 6和R 7中的另一个一起, / SUB>形成含氮环; 其中R 13和R 14独立地选自H和烃基。
    • 4. 发明申请
    • 1,2,4-TRIAZOL-l-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMOURS
    • 用于治疗依靠内肿瘤的肿瘤的1,2,4-三唑-1-基联苯衍生物
    • WO2007068905A1
    • 2007-06-21
    • PCT/GB2006/004630
    • 2006-12-12
    • STERIX LIMITEDWOO, Lok, Wai, LawrenceJACKSON, TobyPUROHIT, AtulREED, Michael, JohnPOTTER, Barry, Victor, Lloyd
    • WOO, Lok, Wai, LawrenceJACKSON, TobyPUROHIT, AtulREED, Michael, JohnPOTTER, Barry, Victor, Lloyd
    • C07D249/08C07D405/10A61K31/4196A61P35/00
    • C07D249/08C07D405/10
    • There is provided a compound of Formula I wherein R 3 , R 4 , R 5 , R 6 and R 7 are independently selected from H and -Y-R 6 ; wherein each R 8 is independently selected from -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO 2 ), H-bond acceptors, and halogens; wherein at Jeast one of R 3 , R 4 , R 5 , R 6 and R 7 is -Y-R 8 wherein R 8 is selected from substituted and unsubstituted • heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further , substituted; wherein R 9 is selected from H, -OH and -OSO 2 NR 1 R 2 ; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R 3 , R 4 , R 5 , R 6 and R 7 is -Y-R 8 ; OR (b) R 9 is -OSO 2 NR 1 R 2 or - OH and four of R 3 , R 4 , R 5 , R 6 and R 7 are H and one of R 3 , R 4 , R 5 , R 6 and R 7 is -Y-R 8 . These compounds inhibit steroid sulphatase and aronatase activity and are useful in the treatment of endocrine-dependent tumours.
    • 提供式I的化合物,其中R 3,R 4,R 5,R 6和R 3 7个独立地选自H和-YR 6; 其中每个R 8独立地选自-OH,烃基,羟基烃基,氰基(-CN),硝基(-NO 2 H 2),H键受体和 卤素; 其中在R 3 R 3,R 4,R 5,R 6和R 7的每一个 其中R 8选自取代和未取代的杂环和氨基取代的苯基,其中X是键或连接基团;其中R 8选自取代和未取代的杂环和氨基取代的苯基。 其中Y是任选的连接基团; 并且其中环A任选进一步被取代; 其中R 9选自H,-OH和-OSO 2 NR 1 R 2; 其中R1和R2独立地选自H和烃基; 其中(a)X是一个键,R 3,R 4,R 5,R 6, R 3和R 7是-YR 8; OR(b)R 9是-OSO 2 NR 1 R 2 R 2或 - OH,R 4中的四个 R 3,R 4,R 5,R 6和R 7均为H和 R 3,R 4,R 5,R 6和R 7中的一个, 是-YR <8> 。 这些化合物抑制类固醇硫酸酯酶和aronatase活性,并且可用于治疗内分泌依赖性肿瘤。
    • 10. 发明申请
    • COMPOUND
    • 复合
    • WO2006032885A2
    • 2006-03-30
    • PCT/GB2005/003641
    • 2005-09-21
    • STERIX LIMITEDLEESE, MathewPUROHIT, AlanREED, Michael, JohnJOURDAN, FabricePOTTER, Barry, Victor, LloydBURBERT, Christian
    • LEESE, MathewPUROHIT, AlanREED, Michael, JohnJOURDAN, FabricePOTTER, Barry, Victor, LloydBURBERT, Christian
    • C07J41/00C07J43/00C07J31/00C07J3/00C07J7/00A61K31/565A61K31/566A61K31/57A61K31/58A61P5/32
    • C07J43/003C07J3/00C07J7/0005C07J31/006C07J41/0005C07J41/0072
    • The present invention provides a compound comprising a steroidal ring system and an optional group R 1 selected from any one of -OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the A ring of the steroidal ring system is optionally substituted at position 2 or 4 with a group R 4 which may be a suitable subtituent wherein the D ring of the steroidal ring system is substituted by a group R 2 of the formula -L-R 3 , wherein L is an optional linker group and R 3 is selected from groups which are or which comprise one of (i) -S0 2 R 5 , wherein R 5 is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) -NO 2 ; (iii) -SOR 6 , wherein R 6 is H or a hydrocarbyl group; (iv) -R 7 , wherein R 7 is a halogen; (v) - alkyl; (vi) -C(=O)R 8 , wherein R 8 is H or hydrocarbyl; (vii) -C≡CR 9 , wherein R 9 is H or hydrocarbyl; (viii) -OC(=O)NR 10 R 11 wherein R 10 and R 11 are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R 3 is -alkyl, R 4 is present as a hydrocarbon group, when R 3 is -NO 2 R 4 is present and/or R 1 is present as a sulphamate group, and when R 3 is -C(=O)R 8 R 4 is present and R 1 is present as a sulphamate group.
    • 本发明提供了包含选自-OH,氨基磺酸酯基,膦酸酯基,硫代膦酸酯基,磺酸酯基或磺酰胺中的任何一种的甾体环系和任选的基团R 1的化合物 组; 其中所述甾族环系统的A环任选在位置2或4处被基团R 4取代,所述基团R 4可以是合适的取代基,其中所述甾族环系统的D环被基团R 其中L是任选的连接基团,R 3选自以下基团:其中R 1,R 2,R 3, (i)-S 0 2 R 5,其中R 5是H,连接到D环的烃基或键或基团; (ii)-NO 2 2; (iii)-SOR 6,其中R 6是H或烃基; (iv)-R 7,其中R 7为卤素; (ⅴ) - 烷基; (vi)-C(= O)R 8,其中R 8为H或烃基; (vii)-C = CR 9,其中R 9是H或烃基; (viii)-OC(= O)NR 10 R 11,其中R 10和R 11独立地选自 由H和烃基组成; (ix),(x),(xi),(xii)和(xiii)是其中当R 3为 - 烷基时,R 4为烃, 当R 3为-NO 2 R 4存在时,和/或R 1存在作为 并且当R 3为-C(= O)时,存在R 8 R 4和R 4,并且R 1〜 >以氨基磺酸盐基团存在。