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31. 发明授权

US6048866A Substituted 2-anilinopryimidines useful as protein kinase inhibitors 失效
标题翻译：用作蛋白激酶抑制剂的取代的2-苯胺基亚氨基嘧啶
公开(公告)号：US6048866A
公开(公告)日：2000-04-11
申请号：US42402
申请日：1998-03-13
申请人： Martin Clive Hutchings , Peter David Davis , David Festus Charles Moffat
发明人： Martin Clive Hutchings , Peter David Davis , David Festus Charles Moffat
IPC分类号： A61K31/505 , A61K31/506 , A61P35/00 , A61P37/02 , A61P43/00 , C07D239/46 , C07D401/12 , C07D403/12 , C07D403/10
CPC分类号： C07D239/47 , C07D401/12
摘要： Compounds of formula (1) are described: ##STR1## and the salts, solvates, hydrates and N-oxides thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases 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：描述式（1）的化合物及其盐，溶剂合物，水合物和N-氧化物，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7具有权利要求1中给出的含义。化合物是选择性抑制剂的蛋白激酶，特别是src家族蛋白激酶，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。

32. 发明授权

US09321718B2 Benzamide derivatives and their use as HSP90 inhibtors 有权
标题翻译：苯甲酰胺衍生物及其用作HSP90抑制剂
公开(公告)号：US09321718B2
公开(公告)日：2016-04-26
申请号：US13703387
申请日：2011-06-10
申请人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： C07D211/00 , C07D295/00 , C07D209/04 , C07D207/04 , C07D207/46 , A61K31/445 , C07C235/60 , C07D207/09 , C07D209/44 , C07D211/26 , C07D211/58 , C07D207/14
CPC分类号： A61K31/4468 , A61K31/216 , A61K31/40 , A61K31/4035 , A61K31/445 , C07C235/60 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D209/44 , C07D211/26 , C07D211/58
摘要： The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供了一种化合物，其为（a）式（I）的苯基酰胺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，前药或溶剂合物：其中R1，R2，R3， R4，R5，R6和R7如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

33. 发明申请

US20140163042A1 ENZYME INHIBITORS 有权
公开(公告)号：US20140163042A1
公开(公告)日：2014-06-12
申请号：US14179880
申请日：2014-02-13
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Charles Moffat , Kenneth William John Baker , Alastair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Charles Moffat , Kenneth William John Baker , Alastair David Graham Donald
IPC分类号： C07D471/04 , C07C237/40 , C07D333/70 , C07C317/50 , C07D295/192 , C07D217/26
CPC分类号： C07C237/40 , C07C259/06 , C07C275/24 , C07C311/46 , C07C317/50 , C07C2601/08 , C07C2601/14 , C07D207/416 , C07D209/42 , C07D213/40 , C07D217/02 , C07D217/22 , C07D217/26 , C07D295/185 , C07D295/192 , C07D333/70 , C07D471/04
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein 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; Y is a bond, —C(═O), —S(═O)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; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, Alk1 and Alk2 independently represent optionally substituted divalent C3-C7 cycloalkyl radicals, or optionally substituted straight or branched, C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals which may optionally contain or terminate in an ether (—O—), thioether (—S—) or amino (—NRA—) link wherein RA is hydrogen or optionally substituted C1-C3 alkyl; 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; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system wherein the radicals R1R2NH—Y-L1-X1-[CH2]Z— and HONHCO-[LINKER]- are attached different ring atoms; and -[Linker]- represents a divalent linker radical linking a ring atom in A with the hydroxamic acid group CONIIOII, the length of the linker radical, from the terminal atom linked to the ring atom of A to the terminal atom linked to the hydroxamic acid group, is equivalent to that of an unbranched saturated hydrocarbon chain of from 3-10 carbon atoms.

34. 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。

35. 发明申请

US20130143926A1 BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS 有权
标题翻译：苯扎林衍生物及其作为HSP90抑制剂的用途
公开(公告)号：US20130143926A1
公开(公告)日：2013-06-06
申请号：US13703387
申请日：2011-06-10
申请人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： C07C235/60 , C07D207/09 , C07D211/26 , C07D209/44 , C07D211/58 , C07D207/14
CPC分类号： A61K31/4468 , A61K31/216 , A61K31/40 , A61K31/4035 , A61K31/445 , C07C235/60 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D209/44 , C07D211/26 , C07D211/58
摘要： The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供了一种化合物，其为（a）式（I）的苯基酰胺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，前药或溶剂合物：其中R1，R2，R3， R4，R5，R6和R7如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

36. 发明申请

US20100317678A1 HYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE 有权
标题翻译：羟肟酸作为组胺脱乙酰酶的抑制剂
公开(公告)号：US20100317678A1
公开(公告)日：2010-12-16
申请号：US12446267
申请日：2006-10-30
申请人： David Festus Charles Moffat , Francesca Ann Day , Sanjay Ratilal Patel , Andrew James Belfield , Alistair David Graham Donald , Alan Hornsby Davidson , Alan Hastings Drummond
发明人： David Festus Charles Moffat , Francesca Ann Day , Sanjay Ratilal Patel , Andrew James Belfield , Alistair David Graham Donald , Alan Hornsby Davidson , Alan Hastings Drummond
IPC分类号： A61K31/506 , C07D401/04 , C07D211/58 , A61K31/451 , C07D211/34 , A61P7/00 , A61P3/10 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P25/28 , C12N9/99
CPC分类号： C07D239/42
摘要： Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from (B1), (B2), (B3), (B4), (B5) and (B6). wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical; and R is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— or (b) a radical of formula R-L1-Y1—(CH2)z—,
摘要翻译：式（I）化合物及其盐，N-氧化物，水合物和溶剂化物是组蛋白脱乙酰酶抑制剂，可用于治疗细胞增殖性疾病，包括癌症：其中Q，V和W独立地表示-N =或-C ═; B是选自（B1），（B2），（B3），（B4），（B5）和（B6）的二价基团。其中标记为*的键与包含Q，V和W通过 - [Linker1] - 的环连接，并且标记为**的键与A至 - [Linker2] - 连接。 A是任选取代的单环，二环或三环碳环或杂环系; - [Linker1] - 和 - [Linker2] - 独立地表示键或二价连接基团; 并且R是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-或（b）式R-L1-Y1-（CH2）z-的基团的基团，

37. 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。

38. 发明申请

US20090298924A1 HYDROXAMIC ACID DERIVATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY 有权
标题翻译：作为HDAC酶活性抑制剂的羟基酸衍生物
公开(公告)号：US20090298924A1
公开(公告)日：2009-12-03
申请号：US11919048
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： A61K31/381 , C07C229/36 , A61K31/235 , C07D333/70 , C12N9/99
CPC分类号： C07C259/06 , C07D333/70
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein 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)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; 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-C7cycloalkyl, 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 B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring;
摘要翻译：式（I）化合物是组蛋白脱乙酰酶活性的抑制剂，可用于治疗例如癌症：其中Y 1为键， - （CO） - ， - S（O 2） - ， - C ）-O-，-OC（-O） - ， - （CO）NR 3 - ， - NR 3（CO） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（CO）NR 5 - 其中R 3和R 5独立地是氢或任选取代的（C 1 -C 6）烷基，L 1是式 - （Alk 1）m（O）n（Alk 2）p的二价基团其中m，n，p，Alk1，Alk2和Q 如权利要求中所定义; z为0或1; A表示任选取代的单环，双环或三环碳环或杂环系; - [连接子] - 表示二价连接基团; 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; 并且B是5或6个环原子的单环杂环，其中R 1与所示的环氮相邻的环碳连接，并且环B任选地与5或6个环原子的第二碳环或杂环稠合，在这种情况下显示与波浪线相交的键可以来自所述第二环中的环原子;

39. 发明授权

US06600037B1 4,5-disubstituted-2-aminopyrimidines 失效
标题翻译： 4,5-二取代-2-氨基嘧啶
公开(公告)号：US06600037B1
公开(公告)日：2003-07-29
申请号：US09692368
申请日：2000-10-19
申请人： Jeremy Martin Davis , David Festus Charles Moffat
发明人： Jeremy Martin Davis , David Festus Charles Moffat
IPC分类号： C07D23942
CPC分类号： C07D239/42 , A61K31/505 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Pyrimidines of formla (1) are described: wherein R1 is a —XR6 group; R2 and R3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, —OH, —OR10 [where R10 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group] —SH, —NO2, —CN, —SR10, —COR10, S(O)R10, —SO2R8, —SO2N(R8)(R9), —CO2R8, —CON(R8)(R9), —CSN(R8)(R9), —NH2 or substituted amino group; R4 is a X1R11 group where X1 is a covalent bond or a —C(R12)(R13)— [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alkyl or haloalkyl group] or —C(O)— group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R5 is a halogen atom or an alkynyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis.
摘要翻译：描述了formla（1）的嘧啶：其中R1是-XR6基团; R2和R3可以相同或不同，各自为氢或卤素原子或选自任选取代的脂族，脂环族，杂脂族，杂环脂族， OH，-OR 10 [其中R 10是任选取代的脂族，脂环族，杂脂族，杂脂族，芳族或杂芳族基团] -SH，-NO 2，-CN，-SR 10，-COR 10，S（O）R 10，-SO 2 R 8，-SO 2 N （R8）（R9），-CO2R8，-CON（R8）（R9），-CSN（R8）（R9），-NH2或取代氨基; R4是X1R11基团，其中X1是共价键或-C （R 12）（R 13） - [其中R 12和R 13各自为氢或卤素原子或羟基，烷基或卤代烷基]或-C（O） - 基，R 11为任选取代的苯基，噻吩基，噻唑基或吲哚基基团; R5是卤素原子或炔基;以及它们的盐，溶剂合物，水合物和N-氧化物。化合物是选择性KDR激酶和/或FGFr激酶抑制剂，并且可用于植物治疗与血管生成相关的疾病状态。

40. 发明授权

US06552029B1 2-pyrimidineamine derivatives and processes for their preparation 失效
标题翻译： 2-嘧啶胺衍生物及其制备方法
公开(公告)号：US06552029B1
公开(公告)日：2003-04-22
申请号：US09420755
申请日：1999-10-20
申请人： Peter David Davis , David Festus Charles Moffat , Mark James Batchelor , Martin Clive Hutchings , David Mark Parry
发明人： Peter David Davis , David Festus Charles Moffat , Mark James Batchelor , Martin Clive Hutchings , David Mark Parry
IPC分类号： C07D40104
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group —X1—R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.
摘要翻译：本发明描述了通式（1）的化合物，其中：Ar为任意取代的芳基; R 2为氢或卤素原子，或-X 1 -R 2a其中X 1为直接键或连接原子或基团，R 2a为任选取代的直链或支链烷基，烯基或炔基; R3是任选取代的杂环烷基;及其盐，溶剂合物，水合物和N-氧化物。化合物是选择性蛋白酪氨酸激酶抑制剂，特别是激酶ZAP-70和并且可用于预防和治疗涉及不适当的血小板活化的免疫或过敏性疾病和疾病。

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