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11. 发明申请

US20140088159A1 ENZYME AND RECEPTOR MODULATION 审中-公开
标题翻译：酶和受体调节
公开(公告)号：US20140088159A1
公开(公告)日：2014-03-27
申请号：US14091522
申请日：2013-11-27
申请人： Alan Hastings Drummond , Alan Hornsby Davidson , David Festus Charles Moffat , Alastair David Graham Donald , Stephen John Davies
发明人： Alan Hastings Drummond , Alan Hornsby Davidson , David Festus Charles Moffat , Alastair David Graham Donald , Stephen John Davies
IPC分类号： C07D213/73 , C12Q1/48
CPC分类号： A61K31/4418 , A61K47/542 , C07D213/73 , C12Q1/485
摘要： Covalent conjugates of an α,α-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the α,α-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.
摘要翻译： α，α-二取代的甘氨酸酯的共价轭合物和靶细胞内酶或受体的活性的调节剂，其中缀合物的酯基可被一个或多个细胞内羧酸酯酶可水解成相应的酸和α，α 二取代的甘氨酸酯在远离抑制剂和靶酶或受体之间的结合界面的位置与调节物缀合，进入细胞，并且活性酸水解产物积聚在细胞内。

12. 发明申请

US20130303576A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：US20130303576A1
公开(公告)日：2013-11-14
申请号：US13946488
申请日：2013-07-19
申请人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
发明人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
IPC分类号： C07D213/58
CPC分类号： C07C237/20 , C07C259/06 , C07C2601/08 , C07D213/56 , C07D213/58
摘要： Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH—Or —CH2CH2—; 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; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)O—, —C(═O)NR′—, —C(═S)—NR′, —C(═NH)NR′ or —S(═O)2NR— wherein R′ is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q. Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.
摘要翻译：式（I）化合物抑制HDAC活性：其中A，B和D独立地表示= CH-或= N-; W是-CH = CH-或-CH 2 CH 2 - ; R1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; R2和R3选自天然或非天然α氨基酸的侧链，条件是R2和R3都不是氢，或者R2和R3与它们所连接的碳一起形成3-6 元环饱和环烷基或杂环基环; Y是-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR' - ， - ，-C（= NH）NR'或-S（= O）2 NH-，其中R'是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）n（Alk2）p-的二价基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义; X1表示键; -C（= O）; 或-S（= O）2 - ; -NR4C（= O） - ， - C（= O）NR4-，-NR4C（= O）NR5-，-NR4S（= O）2-或-S（= O）2NR4-，其中R4和R5独立地氢或任选取代的C 1 -C 6烷基; z为0或1。

13. 发明申请

US20120149736A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：US20120149736A1
公开(公告)日：2012-06-14
申请号：US13202105
申请日：2010-02-25
申请人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
发明人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
IPC分类号： A61K31/44 , C07C259/06 , A61K31/216 , A61K31/196 , A61P35/00 , A61P25/00 , A61P29/00 , A61P3/10 , A61P7/00 , A61P19/02 , A61P11/06 , A61P11/00 , A61P17/06 , A61P1/00 , C07D213/56
CPC分类号： C07C237/20 , C07C259/06 , C07C2601/08 , C07D213/56 , C07D213/58
摘要： Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)O—, —C(═O)NR′—, —C(═5)—NR′, —C(═NH)NR′ or —S(═O)2NR — wherein R′ is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula —(Alk1)m,(Q)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(═O)NR4—,— NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.
摘要翻译：式（I）化合物抑制HDAC活性：其中A，B和D独立地表示= CH-或= N-; W是-CH = CH-或-CH 2 CH 2 - ; R1是羧酸基团（-COOH），或可通过一个或多个细胞内羧酸酯酶可羧酸酯基的酯基; R2和R3选自天然或非天然α氨基酸的侧链，条件是R2和R3都不是氢，或者R2和R3与它们所连接的碳一起形成3 -6元饱和环烷基或杂环基环; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR' - ， - ，-C（= NH）NR'或-S（= O）2 NR - ，其中R'是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m，（Q）n（Alk2）p-的二价基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义; X1表示键; -C（= O）; 或-S（= O）2 - ; -NR 4 C（= O） - ， - C（= O）NR 4 - ， - NR 4 C（= O）NR 5 - ，-NR 4 S（= O）2 - 或-S（= O）2 NR 4 - 氢或任选取代的C 1 -C 6烷基; z为0或1。

14. 发明申请

US20100010010A1 HDAC INHIBITORS 有权
标题翻译： HDAC抑制剂
公开(公告)号：US20100010010A1
公开(公告)日：2010-01-14
申请号：US12443096
申请日：2007-09-14
申请人： Alan Hornsby Davidson , David Festus Charles Moffat , Francesca Ann Day , Alastair David Graham Donald
发明人： Alan Hornsby Davidson , David Festus Charles Moffat , Francesca Ann Day , Alastair David Graham Donald
IPC分类号： A61K31/4965 , C07C229/32 , C07D211/56 , C07D241/04 , A61K31/235 , A61K31/445 , A61P35/00
CPC分类号： C07C259/06 , C07C311/19 , C07C2601/08 , C07C2601/14 , C07D211/34 , C07D211/58 , C07D213/56 , C07D215/22 , C07D241/04 , C07D333/70 , C07D409/12 , C07D471/04
摘要： Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ═C— or ═N—; W is a divalent radical —CH═CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
摘要翻译：式（I）化合物抑制HDAC活性，其中A，B和D独立地表示-C-或-N-; W是二价基团-CH-CH-或CH 2 CH 2 - ; R1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; R2是天然或非天然α氨基酸的侧链; z为0或1; Y，L1和X1如权利要求中所定义。

15. 发明申请

US20140155439A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：US20140155439A1
公开(公告)日：2014-06-05
申请号：US14175072
申请日：2014-02-07
申请人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
发明人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
IPC分类号： C07D213/56 , C07C237/20
CPC分类号： C07C237/20 , C07C259/06 , C07C2601/08 , C07D213/56 , C07D213/58
摘要： Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH2CH2—; 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; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C═O)—, —S(═O)2—, —C(C═O)O—, —C(C═O)NR′—, —C(═S)—NR′, —C(═NH)NR′ or —S(═O)2NR— wherein R′ is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(C═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.
摘要翻译：式（I）化合物抑制HDAC活性：其中A，B和D独立地表示= CH-或= N-; W是-CH = CH-或-CH 2 CH 2 - ; R1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; R2和R3选自天然或非天然α氨基酸的侧链，条件是R2和R3都不是氢，或者R2和R3与它们所连接的碳一起形成3-6 元环饱和环烷基或杂环基环; Y是键，-C（= O） - ， - S（= O）2 - ， - C（C = O）O-，-C（C = O）NR' - ， - -NR'，-C（= NH）NR'或-S（= O）2 NR-，其中R'是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价基团，其中n，n，p，Q，Alk1和Alk2如权利要求中所定义; X1表示键; -C（= O）; 或-S（= O）2 - ; -NR 4 C（= O） - ， - C（C = O）NR 4 - ，-NR 4 C（= O）NR 5 - ，-NR 4 S（= O）2 - 或-S（= O）2 NR 4 - 独立地是氢或任选取代的C 1 -C 6烷基; z为0或1。

16. 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。

17. 发明授权

US6093716A Substituted 2-pyrimidineamines and processes for their preparation 失效
标题翻译：取代的2-嘧啶胺及其制备方法
公开(公告)号：US6093716A
公开(公告)日：2000-07-25
申请号：US931271
申请日：1997-09-15
申请人： Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
发明人： Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
IPC分类号： A61K31/506 , A61P1/04 , A61P11/06 , A61P29/00 , A61P35/00 , A61P37/00 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/505 , C07D401/12 , C07D403/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of general formula (1): ##STR1## are described wherein Het is an optionally substituted heteroaromatic group; R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group; R.sup.2 is a hydrogen or halogen atom or a group --X.sup.1 --R.sup.2a where X.sup.1 is a direct bond or a linker atom or group, and R.sup.2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.3 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
摘要翻译：描述通式（1）的化合物：其中Het是任选取代的杂芳基; R1是氢原子或直链或支链烷基; R2是氢或卤素原子或-X1-R2a，其中X1是直接键或连接原子或基团，R2a是任选取代的直链或支链烷基，烯基或炔基; R3是任选取代的芳族或杂芳族基团; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是选择性蛋白激酶抑制剂，特别是激酶p56lck，ZAP-70和蛋白激酶C，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的蛋白激酶作用具有作用的其它疾病。

18. 发明授权

US6057329A Fused polycyclic 2-aminopyrimidine derivatives 失效
标题翻译：稠合多环2-氨基嘧啶衍生物
公开(公告)号：US6057329A
公开(公告)日：2000-05-02
申请号：US997174
申请日：1997-12-22
申请人： Jeremy Martin Davis , Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
发明人： Jeremy Martin Davis , Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
IPC分类号： A61K31/517 , A61P1/04 , A61P11/06 , A61P29/00 , A61P35/00 , A61P37/06 , C07D239/70 , C07D239/84 , C07D401/12 , C07D403/12 , C07D471/04 , C07D495/04 , C07D487/04
CPC分类号： C07D401/12 , C07D239/70 , C07D471/04 , C07D495/04
摘要： Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.
摘要翻译：式（1）的稠合多环2-氨基嘧啶：其中Ar是任选取代的芳族或杂芳族基团; X是碳原子或氮原子; Y是碳或氮原子; Z是连接基团; A与X和Y一起形成任选取代的单环或双环芳族或杂芳基; 并描述了其盐，溶剂合物，水合物和N-氧化物。这些化合物是蛋白酪氨酸激酶p56lck和p59fyn的有效和选择性抑制剂，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的p56lck和/或p59fyn活性具有作用的其它疾病。

19. 发明授权

US5922741A 5-aminopyrazoles useful as tyrosine kinase inhibitors 失效
标题翻译： 5-氨基吡唑可用作酪氨酸激酶抑制剂
公开(公告)号：US5922741A
公开(公告)日：1999-07-13
申请号：US839211
申请日：1997-04-22
申请人： Peter David Davis , Jeremy Martin Davis , David Festus Charles Moffat
发明人： Peter David Davis , Jeremy Martin Davis , David Festus Charles Moffat
IPC分类号： A61K31/00 , A61K31/415 , A61K31/4155 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D231/12 , C07D231/38 , C07D401/04 , C07D405/04 , C07D409/04 , C07D401/06
CPC分类号： C07D231/38 , C07D401/04 , C07D405/04 , C07D409/04
摘要： Compounds of general formula (1) are described: ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X.sup.1 is an oxygen or sulphur atom;R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen atom or a group --Alk.sup.1 or --X.sup.2 Alk.sup.1 where Alk.sup.1 is an optionally substituted aliphatic or heteroaliphatic group and X.sup.2 is a --C(O)--, --C(S)--, or --S(O).sub.n group where n is an integer 1 or 2;R.sup.3 is a hydrogen atom or a group --Alk.sup.2, �where Alk.sup.2 is as defined for Alk.sup.1 !, --X.sup.2 Alk.sup.2, --Ar.sup.1 �where Ar.sup.1 is an optionally substituted aromatic or heteroaromatic group!, --Alk.sup.2 Ar.sup.1, or --X.sup.2 Alk.sup.2 Ar.sup.1 ;and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective inhibitors of the protein tyrosine kinase p56.sup.lck and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck activity is believed to have a role.
摘要翻译：描述通式（1）的化合物：其中Ar是任选取代的芳族或杂芳族基团; X1是氧或硫原子; R1是氢原子或甲基; R2是氢原子或基团-Alk1或-X2Alk1，其中Alk1是任选取代的脂族或杂脂族基团，X 2是-C（O） - ， - C（S） - 或-S（O）n基团，其中 n是整数1或2; R3是氢原子或基团-Alk2 [其中Alk2如Alk1所定义]，-X2Alk2，-Ar1 [其中Ar1是任选取代的芳族或杂芳族基团]，-Alk2Ar1或-X2Alk2Ar1; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是蛋白酪氨酸激酶p56lck的选择性抑制剂，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的p56lck活性具有作用的其它疾病。

20. 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。

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