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    • 3. 发明申请
    • PYRAZOLE DERIVATIVES HAVING KINASE MODULATING ACTIVITY
    • 具有激酶调节活性的吡唑衍生物
    • WO2006070202A1
    • 2006-07-06
    • PCT/GB2005/005109
    • 2005-12-30
    • ASTEX THERAPEUTICS LIMITEDBERDINI, ValerioO'BRIEN, Michael, AlistairNAVARRO, Eva, FigueroaWYATT, Paul, Graham
    • BERDINI, ValerioO'BRIEN, Michael, AlistairNAVARRO, Eva, FigueroaWYATT, Paul, Graham
    • C07D413/14C07D403/04C07D407/14A01N43/56A61K31/4178A61K31/422A61P35/00
    • C07D403/04C07D405/14C07D413/14
    • The invention provides a compound of the formula (I): or a salt, tautomer, N-oxide or solvate thereof; wherein A is selected from a bond, CH 2 and CH(CN); R l is selected from: (i) a cycloalkyl group of 3 to 6 ring members optionally substituted by one or more substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino and cyano; (ii) a phenyl group optionally substituted by up to three substituents selected from methyl, ethyl, fluorine, chlorine, methoxy, ethoxy and methylsulphonyl, but excluding 2,6-difluorophenyl, 2-fluoro-6-methoxy and 5-chloro-2-methoxyphenyl; (iii) a monocyclic heterocyclic group selected from furyl and isoxazolyl, the heterocyclic group being optionally substituted by one or two groups selected from methyl, ethyl, and a group CH 2 R 2 where R 2 is a five or six membered saturated heterocyclic ring containing one or two heteroatom ring members selected from O and N, the heterocyclic ring being optionally substituted by one or two methyl groups; and (iv) a bicyclic heterocyclic group selected from 2,3-dihydrobenzofuranyl and benzo[c]isoxazolyl, the bicyclic group being optionally substituted by one or two substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino, cyano and chlorine, the bicyclic heterocyclic group being other than a 2,2-dimethyl-2,3-dihydrobenzofuran-7-yl group.
    • 本发明提供式(I)化合物或其盐,互变异构体,N-氧化物或其溶剂合物; 其中A选自键,CH 2和CH(CN); R 1选自:(i)任选被一个或多个选自甲基,乙基,羟基,甲氧基,乙氧基,氟,氨基和氰基的取代基取代的3至6个环成员的环烷基; (ii)任选被至多三个选自甲基,乙基,氟,氯,甲氧基,乙氧基和甲基磺酰基的取代基取代的苯基,但不包括2,6-二氟苯基,2-氟-6-甲氧基和5-氯-2 - 甲氧基; (iii)选自呋喃基和异恶唑基的单环杂环基,杂环基团任选被一个或两个选自甲基,乙基和CH 2 R 2 R 2 O 2基团取代 其中R 2是含有一个或两个选自O和N的杂原子环成员的五或六元饱和杂环,杂环任选被一个或两个甲基取代; 和(iv)选自2,3-二氢苯并呋喃基和苯并[c]异恶唑基的双环杂环基,双环基团任选被一个或两个选自甲基,乙基,羟基,甲氧基,乙氧基,氟,氨基,氰基 和氯,双环杂环基不同于2,2-二甲基-2,3-二氢苯并呋喃-7-基。
    • 4. 发明申请
    • PHARMACEUTICAL COMPOUNDS
    • 药物化合物
    • WO2006051290A2
    • 2006-05-18
    • PCT/GB2005/004323
    • 2005-11-09
    • ASTEX THERAPEUTICS LIMITEDTHE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITALCANCER RESEARCH TECHNOLOGY LIMITEDBERDINI, ValerioBOYLE, Robert, GeorgeSAXTY, GordonVERDONK, Marinus, LeendertWOODHEAD, Steven, JohnWYATT, Paul, GrahamSORE, Hannah, FionaWALKER, David, WinterCALDWELL, JohnCOLLINS, Ian
    • BERDINI, ValerioBOYLE, Robert, GeorgeSAXTY, GordonVERDONK, Marinus, LeendertWOODHEAD, Steven, JohnWYATT, Paul, GrahamSORE, Hannah, FionaWALKER, David, WinterCALDWELL, JohnCOLLINS, Ian
    • A61K31/505A61P35/00C07D239/88C07D401/12C07D401/04C07D401/06C07D403/12
    • C07D403/12A61K31/505C07D239/88C07D239/91C07D239/96C07D401/04C07D401/06C07D401/12C07D403/04
    • The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a are absent, or A is a saturated optionally substituted C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R 1 , R la , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ;or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.
    • 本发明提供式(I)化合物或其盐,溶剂化物,互变异构体或N-氧化物,用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症,其中 环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7,NR 7 CO,C(R 8)= C(R 8)或(R 8) 其中X是O,S或NR 7(其中X是O,S或NR 7)其中X是O,S或NR 7 ; 条件是当J 2是-J 1,R 1是N-CO时,E不是NR 7 CO ; m和n各自为0或1,其中m + n = 1或2; A是键,R 4和R 4a不存在,或A是饱和的任选取代的C 1-7烃连接基团,其具有 在E和G之间延伸的5个原子的最大链长度,连接基团A中的一个碳原子任选地被O或N取代; R 1,R 2,R 2,R 3和R 3各自为H; 卤素; 任选被卤素,OH或C 1-12烷氧基取代的C 1-6烷基; CN; CONHR 8 ; NH 2 ; NHCOR 10或NHCONHR 10; R 4是H或C 1-4烷基; R 4a是H,C 1-4烷基或基团R 9; R 5和R 6各自选自H,R 9和C 1-4烃基,任选被 卤素,C 1-2烷氧基或R 9或NR 5 R 6形成饱和的4-7 元环杂环基; R 7是H或C 1-4烷基; 每个H或任选被氟取代的饱和C 1-4烃基的R 8和R 8 8a; R 9是含有至多3个选自N,O和S的环杂原子的单环或双环碳环或杂环基; 或R 4,R 4a和A一起形成饱和单环4-7元杂环; 或NR 5 R 6,R 4和A形成饱和的4-7元单环杂环; 或R 4,...,以及R 7或R 8,A和E形成4-7元饱和单环杂环; 或NR 5 R 6和R 7或R 8与A和E一起形成4-7元环 饱和单环杂环; R 10是任选取代的苯基或苄基。