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1. 发明申请

US20110112090A1 Depsipeptides and Their Therapeutic Use 失效
标题翻译：多肽及其治疗用途
公开(公告)号：US20110112090A1
公开(公告)日：2011-05-12
申请号：US12991491
申请日：2009-05-22
申请人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Cyrille Davy Tomassi , Alexander Richard Liam Cecil , Thomas James Hill
发明人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Cyrille Davy Tomassi , Alexander Richard Liam Cecil , Thomas James Hill
IPC分类号： A61K31/5377 , A61K31/395 , A61K31/497 , A61K31/4427 , C07D269/00 , C07D513/08 , A61P17/14 , A61P35/00 , A61P9/00 , A61P31/00 , A61P7/00 , A61P37/00 , A61P3/10 , A61P19/10 , A61P3/00 , A61P17/00 , A61P17/02
CPC分类号： C07K5/02 , C07K5/1008 , C07K5/101 , C07K5/1016 , C07K5/1021 , C07K5/1024 , Y02P20/55
摘要： A Compound of structure (IX) or (X) or a pharmaceutically acceptable salt thereof, wherein: X is —C(═O)N(R10)— or —CH(OPr3)—; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.
摘要翻译：结构（IX）或（X）的化合物或其药学上可接受的盐，其中：X为-C（= O）N（R 10） - 或-CH（OPr 3） - ; R7，R9和R10相同或不同，代表氢或氨基酸侧链部分，来自天然或非天然氨基酸; Pr1和Pr2相同或不同，表示氢或硫醇保护基; Pr3是氢或醇保护基; R 1，R 2，R 5和R 6相同或不同，表示氢或氨基酸侧链部分，其自然或非天然氨基酸，或R 1和R 2和/或R 5和R 6与碳原子一起它们连接，形成螺环部分，条件是：R 1和R 2各自不是氢，或者R 5和R 6中的每一个不是氢。

2. 发明授权

US08614193B2 Depsipeptides and their therapeutic use 失效
标题翻译： Depsipeptides及其治疗用途
公开(公告)号：US08614193B2
公开(公告)日：2013-12-24
申请号：US12991491
申请日：2009-05-22
申请人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Cyrille Davy Tomassi , Alexander Richard Liam Cecil , Thomas James Hill
发明人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Cyrille Davy Tomassi , Alexander Richard Liam Cecil , Thomas James Hill
IPC分类号： A61K38/12 , A61K31/542 , C07K11/00 , C07K11/02 , C07K7/54
CPC分类号： C07K5/02 , C07K5/1008 , C07K5/101 , C07K5/1016 , C07K5/1021 , C07K5/1024 , Y02P20/55
摘要： The subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(═O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.
摘要翻译：本申请涉及结构IX或X的化合物或其药学上可接受的盐，其中：X为-C（= O）N（R 10） - 或-CH（OPr 3） - ; R7，R9和R10相同或不同，代表氢或氨基酸侧链部分，来自天然或非天然氨基酸; Pr1和Pr2相同或不同，表示氢或硫醇保护基; Pr3是氢或醇保护基; R 1，R 2，R 5和R 6相同或不同，表示氢或氨基酸侧链部分，与天然或非天然氨基酸或R1和R2和/或R5和R6一起与碳原子一起它们连接，形成螺环部分，条件是：R 1和R 2各自不是氢，或者R 5和R 6中的每一个不是氢。

3. 发明授权

US09200007B2 Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors 有权
标题翻译：三环杂环化合物作为磷酸肌醇3-激酶抑制剂
公开(公告)号：US09200007B2
公开(公告)日：2015-12-01
申请号：US13388164
申请日：2010-08-19
申请人： Stephen Joseph Shuttleworth , Alexander Richard Liam Cecil , Thomas James Hill , Franck Alexandre Silva
发明人： Stephen Joseph Shuttleworth , Alexander Richard Liam Cecil , Thomas James Hill , Franck Alexandre Silva
IPC分类号： C07D491/147 , C07D495/14 , C07D519/00
CPC分类号： C07D495/14 , C07D491/147 , C07D519/00
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中：W是O，N-H，N-（C 1 -C 10烷基）或S; 每个X独立地是CH或N; R1是含有至少1个选自N或O的杂原子的5至7元饱和或不饱和的，任选取代的杂环; R2为（LQ）mY; 并且每个R 3独立地是H，C 1 -C 10烷基，芳基或杂芳基，令人惊奇地发现是PI3K-p110δ的抑制剂，因此在治疗中具有效用。

4. 发明申请

US20120178737A1 Tricyclic Heterocyclic Compounds as Phosphoinositide 3-Kinase Inhibitors 有权
标题翻译：三环杂环化合物作为磷酸肌醇3-激酶抑制剂
公开(公告)号：US20120178737A1
公开(公告)日：2012-07-12
申请号：US13388164
申请日：2010-08-19
申请人： Stephen Joseph Shuttleworth , Alexander Richard Liam Cecil , Thomas James Hill , Franck Alexandre Silva
发明人： Stephen Joseph Shuttleworth , Alexander Richard Liam Cecil , Thomas James Hill , Franck Alexandre Silva
IPC分类号： A61K31/5377 , C07D491/147 , A61P35/00 , A61P29/00 , A61P37/06 , C07D495/14 , C07D519/00
CPC分类号： C07D495/14 , C07D491/147 , C07D519/00
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中：W是O，N-H，N-（C 1 -C 10烷基）或S; 每个X独立地是CH或N; R1是含有至少1个选自N或O的杂原子的5至7元饱和或不饱和的任选取代的杂环; R2为（LQ）mY; 并且每个R 3独立地是H，C 1 -C 10烷基，芳基或杂芳基，令人惊奇地发现是PI3K-p110δ的抑制剂，因此在治疗中具有效用。

5. 发明申请

US20120129848A1 Benzo [E] [1,3] Oxazin-4-One Derivatives as Phosphoinositide 3-Kinase Inhibitors 有权
标题翻译：苯并[E] [1,3]恶嗪-4-酮衍生物作为磷酸肌醇3-激酶抑制剂
公开(公告)号：US20120129848A1
公开(公告)日：2012-05-24
申请号：US13384310
申请日：2010-07-23
申请人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
发明人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
IPC分类号： C07D413/04 , A61P9/00 , A61K31/5377
CPC分类号： C07D265/24
摘要： Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)— alkyl. —C(O)—NH2, —C(O)—NH— alkyl, —SO2— alkyl, —SO2—NH2 or —SO2—NH— alkyl; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1C6 bis alkylamino, C1C6 acylamino, C1-C6 aminoalkyl, mono (C1C6 alkyl) amino C1-C6 alkyl, bis (C1C6 alkyl) amino C1C6 alkyl, C1-C6-acylamino or C1 C6 alkynyl-NR11, R11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, —C(O)—R7, —C(O)—NH2, —C(O)—NH—R7, —SO2—R7, —SO2—NH2, —SO2—NH—R7, NH-acyl, NH-sulfonyl, NR7-acyl, NR7-sulfonyl, N—C(O)—NH—R7, N—SO2—NH—R7, N—C(O)—NR7R7 or N—SO2—NR7R7; and R7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.
摘要翻译：式（I）化合物：其中：W为O，N-H，N-烷基，N-烯基，N-炔基，N-芳基，N-杂芳基或S; 每个X独立地是CH或N; R1是式（b）或R3是H，烷基，NH2，OH，= 0或卤素; 每个A和B独立地是CH或N; D是NHR4; R4是H，烷基，-C（O） - 烷基。 -C（O）-NH 2，-C（O）-NH-烷基，-SO 2 - 烷基，-SO 2 -NH 2或-SO 2 -NH-烷基; R2是被至少一个含氮基取代的芳基，或R2是含氮杂芳基，被含氮基取代的环烷基，含氮环烷基，C1-C6单烷基氨基，C1C6双烷基氨基，C1C6酰基氨基，C1- C 1 -C 6烷基，单（C 1 -C 6烷基）氨基C 1 -C 6烷基，双（C 1 -C 6烷基）氨基C 1 -C 6烷基，C 1 -C 6酰基氨基或C 1 -C 6炔基-NR 11，R 11是H，烷基，烯基，炔基，芳基，杂芳基，，O-烷基，NH-烷基，N-二烷基，-C（O）-R 7，-C（O）-NH 2，-C（O）-NH-R7，-SO 2 -R 7，-SO 2 -NH 2 - SO2-NH-R7，NH-酰基，NH-磺酰基，NR7-酰基，NR7-磺酰基，N-C（O）-NH-R7，N-SO2-NH-R7，N-C（O）-NR7R7或 N-SO2-NR7R7; 和R7是烷基，芳基或杂芳基，可用作PI3K抑制剂，并且可用于治疗。

6. 发明授权

US08981087B2 Benzo [E] [1,3] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors 有权
标题翻译：苯并[E] [1,3]恶嗪-4-酮衍生物作为磷酸肌醇3-激酶抑制剂
公开(公告)号：US08981087B2
公开(公告)日：2015-03-17
申请号：US13384310
申请日：2010-07-23
申请人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
发明人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
IPC分类号： C07D265/24 , C07D413/04 , A61K31/536 , A61K31/5365 , A61P19/02
CPC分类号： C07D265/24
摘要： Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl. —C(O)—NH2, —C(O)—NH-alkyl, —SO2-alkyl, —SO2—NH2 or —SO2—NH-alkyl; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1C6 bis alkylamino, C1C6 acylamino, C1-C6 aminoalkyl, mono (C1C6 alkyl)amino C1-C6 alkyl, bis (C1C6 alkyl)amino C1C6 alkyl, C1-C6-acylamino or C1 C6 alkynyl-NR11, R11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, —C(O)—R7, —C(O)—NH2, —C(O)—NH—R7, —SO2—R7, —SO2—NH2, —SO2—NH—R7, NH-acyl, NH-sulfonyl, NR7-acyl, NR7-sulfonyl, N—C(O)—NH—R7, N—SO2—NH—R7, N—C(O)—NR7R7 or N—SO2—NR7R7; and R7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.
摘要翻译：式（I）的化合物：其中：W是O，N-H，N-烷基，N-烯基，N-炔基，N-芳基，N-杂芳基或S; 每个X独立地是CH或N; R1是式（b）或R3是H，烷基，NH2，OH，= 0或卤素; 每个A和B独立地是CH或N; D是NHR4; R4是H，烷基，-C（O） - 烷基。 -C（O）-NH 2，-C（O）-NH-烷基，-SO 2 - 烷基，-SO 2 -NH 2或-SO 2 -NH-烷基; R2是被至少一个含氮基取代的芳基，或R2是含氮杂芳基，被含氮基取代的环烷基，含氮环烷基，C1-C6单烷基氨基，C1C6双烷基氨基，C1C6酰基氨基，C1- C 1 -C 6烷基，单（C 1 -C 6烷基）氨基C 1 -C 6烷基，双（C 1 -C 6烷基）氨基C 1 -C 6烷基，C 1 -C 6酰基氨基或C 1 -C 6炔基-NR 11，R 11是H，烷基，烯基，炔基，芳基，杂芳基，，O-烷基，NH-烷基，N-二烷基，-C（O）-R 7，-C（O）-NH 2，-C（O）-NH-R7，-SO 2 -R 7，-SO 2 -NH 2 - SO2-NH-R7，NH-酰基，NH-磺酰基，NR7-酰基，NR7-磺酰基，N-C（O）-NH-R7，N-SO2-NH-R7，N-C（O）-NR7R7或 N-SO2-NR7R7; 和R7是烷基，芳基或杂芳基，可用作PI3K抑制剂，并且可用于治疗。

7. 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。

8. 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。

9. 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。

10. 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。

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