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1. 发明授权

US08003695B2 IKK-beta serine-threonine protein kinase inhibitors 失效
标题翻译： IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂
公开(公告)号：US08003695B2
公开(公告)日：2011-08-23
申请号：US12513206
申请日：2007-10-29
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
IPC分类号： A61K31/381 , C07D333/38
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O)—, —S(═P)2-, —C(═O)O—, —C(═O)NR3-, —C(═S)—NR3, —C(═NH)—NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：式（A）和（B）其中R 7为氢或任选取代的（C1- C6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-的基团，其中：z为0或1; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR 3 - ， - C（= NH）-NR 3或-S（= O）2 NR 3 - ，其中R 3是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价连接基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

2. 发明申请

US20100087515A1 IKK-BETA SERINE-THREONINE PROTEIN KINASE INHIBITORS 失效
标题翻译： IKK-BETA丝氨酸蛋白激酶激酶抑制剂
公开(公告)号：US20100087515A1
公开(公告)日：2010-04-08
申请号：US12513206
申请日：2007-10-29
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
IPC分类号： A61K31/381 , C07D333/38 , C12N9/99 , A61P35/00 , A61P37/00 , A61P29/00 , A61P1/00 , A61P11/00
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O)—, —S(═P)2-, —C(═O)O—, —C(═O)NR3-, —C(═S)—NR3, —C(═NH)—NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：式（A）和（B）其中R 7为氢或任选取代的（C1- C6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-的基团，其中：z为0或1; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR 3 - ， - C（= NH）-NR 3或-S（= O）2 NR 3 - ，其中R 3是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价连接基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

3. 发明申请

US20110039920A1 INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE 审中-公开
标题翻译： IKK-BETA丝氨酸蛋白激酶激酶的抑制剂
公开(公告)号：US20110039920A1
公开(公告)日：2011-02-17
申请号：US12989022
申请日：2008-04-23
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
IPC分类号： A61K31/381 , C07D333/38 , C12N9/99 , A61P35/00 , A61P37/06 , A61P29/00 , A61P19/02 , A61P3/10 , A61P11/06 , A61P1/04 , A61P25/28
CPC分类号： C07D333/38
摘要： Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
摘要翻译：（2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5（氨基甲酰基氨基）-2-噻吩基]苯基}戊-4-烯酸酯; 5- {3- [4-氨甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-降冰片烯环戊酯; （2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -5-甲基苯基}戊-4-烯酸酯; 环戊基（25,4E）-2-氨基-5- {5- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -2-甲基苯基}戊-4-烯酸酯; 环戊基O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; 环戊基O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸酯的环戊基酯; 和N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸叔丁酯通过细胞内羧酸酯酶水解成相应的羧酸，并且可用于抑制IKK和bgr; 活动。

4. 发明申请

US20100069473A1 Inhibitors Of IKK-Beta Serine-Threonine Protein Kinase 失效
标题翻译： IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂
公开(公告)号：US20100069473A1
公开(公告)日：2010-03-18
申请号：US12447271
申请日：2007-10-29
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathon Gareth Williams
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathon Gareth Williams
IPC分类号： A61K31/381 , C07D333/36 , C12N9/99 , A61P35/00 , A61P37/00 , A61P29/00 , A61P11/00 , A61P17/00 , A61P3/10
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：其中R 7为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式R-L1-Y1-（CH2）z-的基团，其中：z是0或1; R是式（X）或（Y）的基团，R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R 6是氢或任选取代的C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂芳基或 - （C = O）R 3， - （C = O）OR 3或 - （C = O）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基; Y1是一个键， - （C = O） - ， - S（O 2） - ， - C（= O）O-，-OC（= O） - ， - （C = O）NR 3 - ， - NR 3 （O） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（C = O）NR 4 - ，其中R 3和R 4独立地是氢或任选取代的（C 1 -C 6）式 - （Alk1）m（Q）n（Alk2）p的二价连接基团其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

5. 发明申请

US20100035901A1 ADENINE DERIVATIVE AS INHIBITORS OF HSP90 FOR THE TREATMENT OF CANCER 失效
标题翻译：作为HSP90抑制剂的ADENINE DERIVATIVE作为治疗癌症的药物
公开(公告)号：US20100035901A1
公开(公告)日：2010-02-11
申请号：US12513658
申请日：2007-11-05
申请人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
IPC分类号： A61K31/52 , C07D473/00
CPC分类号： C07D473/34
摘要： The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供一种化合物，其为（a）式（I）的氨基酸衍生物或其互变异构体，或（b）其药学上可接受的盐，N-氧化物，水合物或溶剂合物：其中R1，R2，L1，Het A，x，y和W如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

6. 发明授权

US08217050B2 Adenine derivative as inhibitors of HSP90 for the treatment of cancer 失效
标题翻译：腺嘌呤衍生物作为HSP90抑制剂治疗癌症
公开(公告)号：US08217050B2
公开(公告)日：2012-07-10
申请号：US12513658
申请日：2007-11-05
申请人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
IPC分类号： C07D473/34 , A61K31/52 , A61P11/06 , A61P37/06 , A61P19/02 , A61P3/10 , A61P17/06 , C07F7/18 , C07F7/10
CPC分类号： C07D473/34
摘要： The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供一种化合物，其为（a）式（I）的氨基酸衍生物或其互变异构体，或（b）其药学上可接受的盐，N-氧化物，水合物或溶剂合物：其中R1，R2，L1，Het A，x，y和W如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

7. 发明申请

US20110046210A1 SUBSTITUTED THIOPENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为IKK-BETA SERINE-，THREONIN-PROTEIN激酶抑制剂的替代噻托溴铵
公开(公告)号：US20110046210A1
公开(公告)日：2011-02-24
申请号：US12989271
申请日：2009-04-23
申请人： David Festus Charles Moffat , Stephen John Davies
发明人： David Festus Charles Moffat , Stephen John Davies
IPC分类号： A61K31/381 , C07D333/38 , A61P37/00 , A61P29/00 , A61P35/00 , A61P19/02 , A61P17/06 , A61P1/00 , A61P1/04 , A61P3/10 , A61P25/28 , C12N9/99
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R1C(R2)(R3)NH—Y-L1-X1-(CH2)z— wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R2 and R3 is hydrogen, or R2 and R3 taken together with the carbon atom to which they are attached form a C3-C7 cycloalkyl ring, and z, Y, L1 and X1 are as defined in the claims.
摘要翻译：式（IA）或（IB）化合物是可用于治疗自身免疫性和炎性疾病的IKK抑制剂：其中R 7是氢或任选取代的（C 1 -C 6）烷基; A是任选取代的5-13个环原子的芳基或杂芳基; Z是式R1C（R2）（R3）NH-Y-L1-X1-（CH2）z-的基团，其中R1是羧酸基（-COOH）或可被一个或多个细胞内可水解的酯基酯酶到羧酸基团; 并且R 2和R 3独立地表示天然或非天然α氨基酸的侧链，但R 2和R 3都不是氢，或者R 2和R 3与它们所连接的碳原子一起形成C 3 -C 7环烷基环，z，Y，L1和X1如权利要求中所定义。

8. 发明授权

US08148531B2 Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity 失效
标题翻译：喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂
公开(公告)号：US08148531B2
公开(公告)日：2012-04-03
申请号：US11918898
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
IPC分类号： C07D215/00
CPC分类号： C07D215/42 , C07D215/233 , C07D215/36 , C07D215/44 , C07D239/90 , C07D239/94 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or —NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.
摘要翻译：式（IA）或（IB）的化合物是极光激酶活性的抑制剂：式（IA），（IB）其中-L1Y1- [CH2] z-是连接基，其中Y1，L1和z如索赔; R6是C1-C4烷氧基，氢或卤素; W表示键，-CH 2 - ， - O - ， - S - ， - S（= O）2 - 或-NR 5 - ，其中R 5是氢或C 1 -C 4烷基; Q为≡N-，═CH-或≡C（X1） - 其中X1为氰基，环丙基或卤素; 连接基团L2如权利要求中所定义; R是式（X）或（Y）的基团：其中R 1是羧酸基团（-COOH）或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; R4是氢; 或C 1 -C 6烷基，C 3 -C 7环烷基，芳基，芳基（C 1 -C 6烷基） - ，杂芳基，杂芳基（C 1 -C 6烷基） - ，（C = O）R 3， - （C = O）OR 3 ，或 - （C = O）NR 3，其中R3是氢或任选取代的（C1-C6）烷基，C3-C7环烷基，芳基，芳基（C1-C6烷基） - ，杂芳基或杂芳基（C1-C6烷基） ; R 41是氢或任选取代的C 1 -C 6烷基; 且D为5或6个环原子的单环杂环。

9. 发明申请

US20100216802A1 PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译：作为类似于激素治疗癌症的类激酶抑制剂的哌替啶衍生物
公开(公告)号：US20100216802A1
公开(公告)日：2010-08-26
申请号：US12446008
申请日：2007-10-19
申请人： David Festus Charles Moffat , Sanjay Ratilal Patel , Stephen John Davies , Kenneth William John Baker , Oliver James Philps
发明人： David Festus Charles Moffat , Sanjay Ratilal Patel , Stephen John Davies , Kenneth William John Baker , Oliver James Philps
IPC分类号： A61K31/519 , C07D475/00 , A61P35/00
CPC分类号： C07D475/00
摘要： Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases: wherein R1 and R2 are hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 and R3′ are independently selected from hydrogen, —CN, hydroxyl, halogen, optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, —NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1-Y1— wherein R is an alpha amino acid or alpha amino acid ester motif, linked to ring A by linker R-L1-Y1— as defined in the claims.
摘要翻译：式（I）化合物是Polo样激酶（PLK）的抑制剂，可用于治疗细胞增殖性疾病：其中R 1和R 2为氢，或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基; R3和R3'独立地选自氢，-CN，羟基，卤素，任选取代的（C1-C6）烷基，（C2-C6）烯基，（C2-C6）炔基或（C3-C6）环烷基，-NR5R6或 C 1 -C 4烷氧基，其中R 5和R 6独立地是氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的具有至多12个环原子的单环或双环碳环或杂环或环系; T是式R-L1-Y1-的基团，其中R是通过如权利要求中所定义的连接体R-L1-Y1-连接到环A的α氨基酸或α氨基酸酯基序。

10. 发明申请

US20090131461A1 Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity 失效
标题翻译：喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂
公开(公告)号：US20090131461A1
公开(公告)日：2009-05-21
申请号：US11918898
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
IPC分类号： A61K31/517 , C07D215/20 , A61K31/47 , C07D401/02 , A61P35/00 , A61P37/00 , A61K31/506 , C07D239/72
CPC分类号： C07D215/42 , C07D215/233 , C07D215/36 , C07D215/44 , C07D239/90 , C07D239/94 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X is cyano, cyclopropyl or halo; linker radicals L are as defined in the claims; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.
摘要翻译：式（IA）或（IB）的化合物是极光激酶活性的抑制剂：式（IA），（IB）其中-L1Y1- [CH2] z-是连接基，其中Y1，L1和z如索赔; R6是C1-C4烷氧基，氢或卤素; W表示键，-CH 2 - ， - O - ， - S - ， - S（-O）2 - 或-NR 5 - ，其中R 5是氢或C 1 -C 4烷基; Q是-N-，-CH-或-C（X1） - ，其中X是氰基，环丙基或卤素; 连接基自由基L如权利要求中所定义; R是式（X）或（Y）的基团：其中R 1是羧酸基团（-COOH）或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; R4是氢; 或（C 1 -C 6烷基） - ， - （CO）R 3， - （CO）OR 3或 - （ CO）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基，C 3 -C 7环烷基，芳基，芳基（C 1 -C 6烷基） - ，杂芳基或杂芳基（C 1 -C 6烷基） R 41是氢或任选取代的C 1 -C 6烷基; 且D为5或6个环原子的单环杂环。

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