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    • 2. 发明授权
    • Fungicides
    • 杀菌剂
    • US06432964B1
    • 2002-08-13
    • US09423135
    • 1999-11-05
    • John Frederick AtherallThomas Lawley HoughStephen David LindellMary Josephine O'MahonyJohn Henry ParsonsElizabeth Anne Saville-Stones
    • John Frederick AtherallThomas Lawley HoughStephen David LindellMary Josephine O'MahonyJohn Henry ParsonsElizabeth Anne Saville-Stones
    • A01N4390
    • C07D495/04A01N43/90
    • The invention provides the use in combating fungi of compounds of general formula (I) wherein R1 is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, Ra, Ra3Si, RaS or RaO, where Ra is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; R2 has the same meaning as Ra or can be hydrogen; Z is oxygen or sulfur, M is a thiophene ring, and R3 and R4, which may be the same or different, have the same meaning as Ra or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group ORc or S(O)mRc, where Rc has the same meaning as Ra or is hydrogen or acyl and m is 0, 1 or 2; or R3 and R4 together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R1 is hydrogen.
    • 本发明提供了用于对抗通式(I)的化合物的用途,其中R 1是氢,羟基,酰基,酰氧基,任选取代的氨基,Ra,Ra 3 Si,RaS或RaO,其中R a是任选取代的烷基,任选取代的链烯基, 任选取代的炔基,任选取代的环烷基,任选取代的环烯基,任选取代的芳基或任选取代的杂环基; R2具有与Ra相同的含义,也可以是氢; Z是氧或硫,M是噻吩环,并且可以相同或不同的R 3和R 4具有与R a相同的含义或可以是任选取代的氨基,氢,卤素,氰基,硝基或基团OR c或 S(O)m R c,其中R c具有与R a相同的含义或氢或酰基,m为0,1或2; 或R 3和R 4与它们所连接的原子一起形成任选取代的碳环或杂环; 以及R1为氢的化合物的互变异构体。
    • 5. 发明授权
    • Thieno[2,3-B] pyridines as potassium channel inhibitors
    • 噻吩并[2,3-B]吡啶作为钾通道抑制剂
    • US07576212B2
    • 2009-08-18
    • US11297330
    • 2005-12-09
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John MadgeDerek John
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John MadgeDerek John
    • C07D513/02
    • C07D495/04C07D333/36C07D333/38C07D409/12
    • The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.
    • 本发明提供下式的化合物:其中R1是芳基,杂芳基,环烷基或烷基; R2是H,烷基,硝基,CO 2 R 7,CONR 5 R 6或卤素; R3和R4是H,NR5R6,NC(O)R7,卤素,三氟甲基,烷基,CONR5R6,CO2R7,腈或烷氧基; R5和R6可以相同或不同,可以是H,烷基,芳基,杂芳基或环烷基; 或R 5和R 6可以一起形成饱和的,不饱和的或部分饱和的4至7元环,其中所述环可任选地包含一个或多个选自N,O或S的其它杂原子; R7是H或烷基; A是H,卤素或式X-L-Y基团; X是O,S或NR8; R8是H或烷基; L是(CH 2)n,其中n是0,1,2,3或4; Y为芳基,杂环基,烷基,链烯基或环烷基; 式I化合物中硫的单和二氧化和/或氮部分的单氧化的产物; 或其药学上可接受的盐。 这些化合物可用作钾离子通道的抑制剂,因此可用于治疗各种病症,包括心律失常和2型糖尿病。
    • 9. 发明授权
    • Furanopyrimidine compounds as potassium ion channel inhibitors
    • 呋喃并嘧啶化合物作为钾离子通道抑制剂
    • US07456187B2
    • 2008-11-25
    • US11148991
    • 2005-06-10
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John Madge
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John Madge
    • C07D491/048A61K31/519A61P9/06
    • C07D491/04
    • A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, —CO2R7, CONR4R5 or halo; R3 is H, NR4R5, NC(O)R8, halo, trifluoromethyl, alkyl, nitrile or alkoxy; R4 and R5 may be the same or different, and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R4 and R5 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; X is O, S or NR6; R6 is H or alkyl; R7 is hydrogen, methyl or ethyl; R8 is methyl or ethyl; L is (CH2)n, where n is 1, 2 or 3; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; together with pharmaceutically acceptable salts thereof. The use of these compounds as potassium channel inhibitors is also described.
    • 式(I)化合物,其中R 1是芳基,杂芳基,环烷基或烷基; R 2是H,烷基,硝基,-CO 2 R 7,CONR 4 R 5 /或卤素; R 3是H,NR 4 R 5,NC(O)R 8,卤素,三氟甲基,烷基 ,腈或烷氧基; R 4和R 5可以相同或不同,并且可以是H,烷基,芳基,杂芳基或环烷基; 或R 4和R 5可以一起形成饱和的,不饱和的或部分饱和的4至7元环,其中所述环可以任选地包含一个或多个其它选自N ,O或S; X是O,S或NR 6; R 6是H或烷基; R 7是氢,甲基或乙基; R 8是甲基或乙基; L是(CH 2 CH 2)n N,其中n是1,2或3; Y为芳基,杂环基,烷基,链烯基或环烷基; 以及其药学上可接受的盐。 还描述了这些化合物作为钾通道抑制剂的用途。