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1. 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。

2. 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.

3. 发明申请

US20100317865A1 ENZYME AND RECEPTOR MODULATION 审中-公开
标题翻译：酶和受体调节
公开(公告)号：US20100317865A1
公开(公告)日：2010-12-16
申请号：US12867455
申请日：2009-02-27
申请人： Alan Hornsby Davidson , Alan Hastings Drummond , David Festus Charles Moffat , Alistair David Graham Donald , Stephen John Davies
发明人： Alan Hornsby Davidson , Alan Hastings Drummond , David Festus Charles Moffat , Alistair David Graham Donald , Stephen John Davies
IPC分类号： C07D213/56 , C07D213/79 , C07C229/48 , C07C229/34 , A61K31/4418 , A61K31/216 , A61K31/196 , A61K31/197 , A61K31/44 , G01N33/566 , A61P35/00 , A61P37/02 , A61P29/00
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。

4. 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。

5. 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。

6. 发明授权

US07939666B2 Enzyme inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US07939666B2
公开(公告)日：2011-05-10
申请号：US11918139
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： C07D471/02 , C07D217/00 , C07D213/72 , C07D209/04 , C07D333/50 , C07C229/28
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.
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。

7. 发明授权

US08686032B2 Enzyme inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US08686032B2
公开(公告)日：2014-04-01
申请号：US12957829
申请日：2010-12-01
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： A61K31/381 , A61K31/27 , C07C271/02 , C07C271/06
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:
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：

8. 发明申请

US20090291978A1 Enzyme Inhibitors 有权
公开(公告)号：US20090291978A1
公开(公告)日：2009-11-26
申请号：US11918139
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： A61K31/437 , C07D471/02 , C07C229/28 , A61K31/216 , A61K31/192 , C07D217/00 , A61K31/472 , C07D213/72 , A61K31/44 , C07D209/04 , A61K31/404 , C07D333/50 , A61K31/381 , A61P35/00 , A61P25/00 , A61P29/00 , A61P3/10 , A61P37/06
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; L is a divalent radical of formula -(Alk1)m(O)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 hetero-cyclic radical having 5-13 ring members, AIk1 and AIk2 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; X 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 CONHOH, 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.

9. 发明申请

US20130116318A1 Enzyme Inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US20130116318A1
公开(公告)日：2013-05-09
申请号：US12957829
申请日：2010-12-01
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： A61K31/381 , A61K31/27
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:
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：

10. 发明授权

US08778953B2 Inhibitors of P38 map kinase 有权
标题翻译： P38地图激酶抑制剂
公开(公告)号：US08778953B2
公开(公告)日：2014-07-15
申请号：US12867774
申请日：2009-02-27
申请人： David Festus Charles Moffat , Stephen John Davies , Stephane Pintat
发明人： David Festus Charles Moffat , Stephen John Davies , Stephane Pintat
IPC分类号： A01N43/54 , A61K31/505 , A01N43/40 , A61K31/44 , C07D239/02 , C07D213/72
CPC分类号： C07D213/73
摘要： Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; 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 are as defined in the claims.
摘要翻译：式（I）化合物是可用于治疗自身免疫性和炎性疾病的p38 MAP激酶抑制剂：其中：G为-N =或-CH =; D是任选取代的具有5-13个环成员的二价单环或双环芳基或杂芳基; R6是氢或任选取代的C 1 -C 3烷基; P表示氢，U表示式（IA）的基团; 或U表示氢，P表示式（IA）的基团; 其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z为0或1; -X1-L1-Y-是连接基或键; 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; 并且R 2和R 3如权利要求中所定义。

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