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1. 发明授权

US07342004B2 Thioether sulphamate steroids as steroid inhibitors and anti-cancer compounds 失效
标题翻译：硫代硫代氨基甲酸酯类固醇作为类固醇抑制剂和抗癌化合物
公开(公告)号：US07342004B2
公开(公告)日：2008-03-11
申请号：US10367623
申请日：2003-02-14
申请人： Barry Victor Lloyd Potter , Michael John Reed , Graham Keith Packham , Matthew Paul Leese
发明人： Barry Victor Lloyd Potter , Michael John Reed , Graham Keith Packham , Matthew Paul Leese
IPC分类号： A61K31/56 , C07J31/00
CPC分类号： A61K31/37 , A61K31/565
摘要： There is provided use of a compound of Formula XI: wherein R3 is a sulphamate group and at least of R1 or R2 is a thioether group as disclosed by the present specification, capable of inhibiting steroid sulphatase.
摘要翻译：提供式XI化合物的用途：其中R 3是氨基磺酸酯基团，并且至少R 1或R 2是如本说明书所公开的能够抑制类固醇硫酸酯酶的硫醚基团。

2. 发明授权

US08865655B2 Depsipeptides and their therapeutic use 有权
标题翻译： Depsipeptides及其治疗用途
公开(公告)号：US08865655B2
公开(公告)日：2014-10-21
申请号：US12516110
申请日：2007-11-22
申请人： Arasu Ganesan , Graham Keith Packham , Alexander Richard Liam Cecil
发明人： Arasu Ganesan , Graham Keith Packham , Alexander Richard Liam Cecil
IPC分类号： C07K7/54 , A61K38/12 , A61P17/02 , C07K5/103 , C07K5/02
CPC分类号： C07K5/0205 , C07K5/1008 , C07K5/101 , G01N2333/98 , G01N2410/10 , G01N2500/00 , Y02P20/55
摘要： A compound of the general Structure (VII) or (VIII) including isoteres and pharmaceutically acceptable salts thereof, wherein R1, R2 (where X=—CONR6—), R3 and R7 are the same or different and each represents an amino-acid side chain moiety; R2 (where X=—CHZ—), R4 and R6 are the same or different and each represents hydrogen, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl; K represents a linear or branched chain of carbon atoms and containing 1-10 atoms; L represents a moiety capable of chelating zinc in the active site of a histone deacetylase (HDAC) or of conversion to such a moiety in vivo (by hydrolysis or reduction, for example); M is a linear or branched chain of carbon or other atoms and containing 1-10 atoms, and capable of undergoing in vivo cleavage to give Structure (VII); and Z is a heteroatom bonded to the macrocycle by a single or double bond, and any other group bonded to Z is H or a protecting group.
摘要翻译：一般结构（VII）或（VIII）的化合物，包括其他的异头物及其药学上可接受的盐，其中R 1，R 2（其中X = -CONR 6 - ），R 3和R 7相同或不同，并且各自表示氨基酸侧链部分; R2（其中X = -CHZ-），R4和R6相同或不同，各自表示氢，C1-C6烷基，C2-C6烯基或C2-C6炔基; K表示碳原子的直链或支链，含有1-10个原子; L表示能够在组蛋白脱乙酰酶（HDAC）的活性位点螯合锌或在体内转化成这种部分（通过水解或还原）的部分; M是碳或其它原子的直链或支链，含有1-10个原子，并且能够进行体内裂解以得到结构（Ⅶ）; 并且Z是通过单键或双键与大环结合的杂原子，并且与Z键合的任何其它基团是H或保护基团。

3. 发明授权

US07977304B2 FK 228 derivates as HDAC inhibitors 有权
标题翻译： FK 228衍生物作为HDAC抑制剂
公开(公告)号：US07977304B2
公开(公告)日：2011-07-12
申请号：US11916200
申请日：2006-06-02
申请人： Arasu Ganesan , Graham Keith Packham , Alexander Yurek-George , Alexander Richard Liam Cecil
发明人： Arasu Ganesan , Graham Keith Packham , Alexander Yurek-George , Alexander Richard Liam Cecil
IPC分类号： A61K38/12 , A61K31/542 , C07K11/00 , C07K11/02 , C07K7/54
CPC分类号： A61K38/15
摘要： Compounds which are FK228 analogues of the general formula (I) or (I′), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.
摘要翻译：发现具有通式（I）或（I'）的FK228类似物及其药学上可接受的盐的化合物抑制HDAC，其中R1，R2，R3和R4相同或不同，代表氨基酸侧链部分，每个R 6相同或不同，表示氢或C 1 -C 4烷基。

4. 发明申请

US20100056435A1 Depsipeptides and Their Therapeutic Use 有权
标题翻译：多肽及其治疗用途
公开(公告)号：US20100056435A1
公开(公告)日：2010-03-04
申请号：US12516110
申请日：2007-11-22
申请人： Arasu Ganesan , Graham Keith Packham , Alexander Richard Liam Cecil
发明人： Arasu Ganesan , Graham Keith Packham , Alexander Richard Liam Cecil
IPC分类号： A61K38/12 , C07K5/12 , C12Q1/34 , A61P35/00 , A61P9/00 , A61P37/06 , A61P3/10 , A61P31/00
CPC分类号： C07K5/0205 , C07K5/1008 , C07K5/101 , G01N2333/98 , G01N2410/10 , G01N2500/00 , Y02P20/55
摘要： A compound of the general Structure (VII) or (VIII) including isoteres and pharmaceutically acceptable salts thereof, wherein R1, R2 (where X=—CONR6—), R3 and R7 are the same or different and each represents an amino-acid side chain moiety; R2 (where X=—CHZ—), R4 and R6 are the same or different and each represents hydrogen, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl; K represents a linear or branched chain of carbon atoms and containing 1-10 atoms; L represents a moiety capable of chelating zinc in the active site of a histone deacetylase (HDAC) or of conversion to such a moiety in vivo (by hydrolysis or reduction, for example); M is a linear or branched chain of carbon or other atoms and containing 1-10 atoms, and capable of undergoing in vivo cleavage to give Structure (VII); and Z is a heteroatom bonded to the macrocycle by a single or double bond, and any other group bonded to Z is H or a protecting group.
摘要翻译：一般结构（VII）或（VIII）的化合物，包括其他的异头物及其药学上可接受的盐，其中R 1，R 2（其中X = -CONR 6 - ），R 3和R 7相同或不同，并且各自表示氨基酸侧链部分; R2（其中X = -CHZ-），R4和R6相同或不同，各自表示氢，C1-C6烷基，C2-C6烯基或C2-C6炔基; K表示碳原子的直链或支链，含有1-10个原子; L表示能够在组蛋白脱乙酰酶（HDAC）的活性位点螯合锌或在体内转化为这种部分（通过水解或还原）的部分; M是碳或其它原子的直链或支链，含有1-10个原子，并且能够进行体内裂解以得到结构（Ⅶ）; 并且Z是通过单键或双键与大环结合的杂原子，并且与Z键合的任何其它基团是H或保护基团。

5. 发明授权

US08247372B2 Depsipeptides and their therapeutic use 失效
标题翻译： Depsipeptides及其治疗用途
公开(公告)号：US08247372B2
公开(公告)日：2012-08-21
申请号：US12515880
申请日：2007-11-23
申请人： Graham Keith Packham , Arasu Ganesan , Alexander Richard Liam Cecil
发明人： Graham Keith Packham , Arasu Ganesan , Alexander Richard Liam Cecil
IPC分类号： A61K38/12 , A61P37/00
CPC分类号： C07K5/0205
摘要： Compounds which are Spiruchostatin analogues of the general formula (I) or (I′), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.
摘要翻译：发现作为通式（I）或（I'）的螺旋菌抑制蛋白类似物及其药学上可接受的盐的化合物抑制HDAC，其中R1，R2，R3和R4相同或不同，代表氨基酸侧链部分，每个R 6相同或不同，表示氢或C 1 -C 4烷基。

6. 发明申请

US20100056434A1 Depsipeptides and Their Therapeutic Use 失效
标题翻译：多肽及其治疗用途
公开(公告)号：US20100056434A1
公开(公告)日：2010-03-04
申请号：US12515880
申请日：2007-11-23
申请人： Graham Keith Packham , Arasu Ganesan , Alexander Richard Liam Cecil
发明人： Graham Keith Packham , Arasu Ganesan , Alexander Richard Liam Cecil
IPC分类号： A61K38/12 , C07K11/02 , G01N33/53 , G01N33/574 , A61P3/10 , A61P37/02 , A61P37/06 , A61P35/00
CPC分类号： C07K5/0205
摘要： Compounds which are Spiruchostatin analogues of the general formula (I) or (I′), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.
摘要翻译：发现作为通式（I）或（I'）的螺旋菌抑制蛋白类似物及其药学上可接受的盐的化合物抑制HDAC，其中R1，R2，R3和R4相同或不同，代表氨基酸侧链部分，每个R 6相同或不同，表示氢或C 1 -C 4烷基。

7. 发明申请

US20090131390A1 FK 228 derivates as HDAC inhibitors 有权
标题翻译： FK 228衍生物作为HDAC抑制剂
公开(公告)号：US20090131390A1
公开(公告)日：2009-05-21
申请号：US11916200
申请日：2006-06-02
申请人： Arasu Ganesan , Graham Keith Packham , Alexander Yurek-George , Alexander Richard Liam Cecil
发明人： Arasu Ganesan , Graham Keith Packham , Alexander Yurek-George , Alexander Richard Liam Cecil
IPC分类号： A61K31/542 , G01N33/53 , A61P35/00
CPC分类号： A61K38/15
摘要： Compounds which are FK228 analogues of the general formula (I) or (I′), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.
摘要翻译：发现具有通式（I）或（I'）的FK228类似物及其药学上可接受的盐的化合物抑制HDAC，其中R1，R2，R3和R4相同或不同，代表氨基酸侧链部分，每个R 6相同或不同，表示氢或C 1 -C 4烷基。

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