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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

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。

3. 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。

4. 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。

5. 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。

6. 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.

7. 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。

8. 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。

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