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1. 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：

2. 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：

3. 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.

4. 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。

5. 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.

6. 发明授权

US08962825B2 Hydroxamates as inhibitors of histone deacetylase 有权
标题翻译：羟肟酸盐作为组蛋白脱乙酰酶的抑制剂
公开(公告)号：US08962825B2
公开(公告)日：2015-02-24
申请号：US12446267
申请日：2006-10-30
申请人： David Charles Festus Moffat , Sanjay Ratilal Patel , Francesca Ann Day , Andrew James Belfield , Alistair David Graham Donald , Alan Hornsby Davidson , Alan Hastings Drummond
发明人： David Charles Festus Moffat , Sanjay Ratilal Patel , Francesca Ann Day , Andrew James Belfield , Alistair David Graham Donald , Alan Hornsby Davidson , Alan Hastings Drummond
IPC分类号： C07D345/00 , C07D239/42
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。

7. 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，

8. 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。

9. 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。

10. 发明授权

US07973181B2 Hydroxamic acid derivatives as inhibitors of HDAC enzymatic activity 有权
公开(公告)号：US07973181B2
公开(公告)日：2011-07-05
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： C07D333/70 , C07C229/36
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(Q)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.

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