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1. 发明申请

WO2011021038A1 TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS 审中-公开
标题翻译：三聚异氰酸酯化合物作为磷酸三辛酯抑制剂
公开(公告)号：WO2011021038A1
公开(公告)日：2011-02-24
申请号：PCT/GB2010/051370
申请日：2010-08-19
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen Joseph , CECIL, Alexander Richard Liam , HILL, Thomas James , SILVA, Franck Alexandre
发明人： SHUTTLEWORTH, Stephen Joseph , CECIL, Alexander Richard Liam , HILL, Thomas James , SILVA, Franck Alexandre
IPC分类号： C07D495/14 , C07D519/00 , C07D491/147 , A61K31/519 , A61P35/02
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-(C 1 -C 10 alkyl) or S; each X is independently CH or N; R 1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R 2 is (LQ) m Y; and each R 3 is independently H, C 1 -C 10 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-p110d的抑制剂，因此在治疗中具有效用。

2. 发明申请

WO2010116173A1 DEPSIPEPTIDES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：杀虫剂及其治疗用途
公开(公告)号：WO2010116173A1
公开(公告)日：2010-10-14
申请号：PCT/GB2010/050585
申请日：2010-04-01
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen Joseph , TOMASSI, Cyrille Davy , SILVA, Franck Alexandre , CECIL, Alexander Richard Liam , HILL, Thomas James
发明人： SHUTTLEWORTH, Stephen Joseph , TOMASSI, Cyrille Davy , SILVA, Franck Alexandre , CECIL, Alexander Richard Liam , HILL, Thomas James
IPC分类号： C07K5/02 , C07K11/00
CPC分类号： C07K5/0205
摘要： Compounds are provided of the general structure:(IX and X) wherein at least one of R 1 and R 5 is a carbon linked sulphone or sulphoxide. The compounds are inhibitors of HDAC and are useful in therapy.
摘要翻译：提供了通式结构：（IX和X）的化合物，其中R 1和R 5中的至少一个是碳连接的砜或亚砜。这些化合物是HDAC的抑制剂，可用于治疗。

3. 发明申请

WO2009141658A1 DEPSIPEPTIDES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：杀虫剂及其治疗用途
公开(公告)号：WO2009141658A1
公开(公告)日：2009-11-26
申请号：PCT/GB2009/050554
申请日：2009-05-22
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen, Joseph , SILVA, Franck, Alexandre , TOMASSI, Cyrille, Davy , CECIL, Alexander, Richard, Liam , HILL, Thomas, James
发明人： SHUTTLEWORTH, Stephen, Joseph , SILVA, Franck, Alexandre , TOMASSI, Cyrille, Davy , CECIL, Alexander, Richard, Liam , HILL, Thomas, James
IPC分类号： A61P35/00 , C07K5/02
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(R 10 )- or -CH(OPr 3 ) -; R 7 , R 9 and R 10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr 1 and Pr 2 are the same or different and represent hydrogen or a thiol protecting group; Pr 3 is hydrogen or an alcohol protecting group; R 1 , R 2 , R 5 and R 6 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 R 1 and R 2 and/or R 5 and R 6 , taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R 1 and R 2 is not hydrogen, or each of R 5 and R 6 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是-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。

4. 发明申请

WO2009141657A1 DEPSIPEPTIDES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：杀虫剂及其治疗用途
公开(公告)号：WO2009141657A1
公开(公告)日：2009-11-26
申请号：PCT/GB2009/050553
申请日：2009-05-22
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen, Joseph , SILVA, Franck, Alexandre , TOMASSI, Cyrille, Davy , CECIL, Alexander, Richard, Liam , GANESAN, Arasu , HILL, Thomas, James
发明人： SHUTTLEWORTH, Stephen, Joseph , SILVA, Franck, Alexandre , TOMASSI, Cyrille, Davy , CECIL, Alexander, Richard, Liam , GANESAN, Arasu , HILL, Thomas, James
IPC分类号： A61P35/00 , C07K5/02 , C07K5/10 , C07K5/113 , C07K5/117
CPC分类号： C07K5/02 , C07K5/1016 , C07K5/1019 , C07K5/1021 , C07K5/1024 , Y02P20/55
摘要： A compound of formula (IX) or (X): including pharmaceutically acceptable salts thereof; wherein: X is -C(=O)N(R 10 )- or -CH(OPr 3 ) -; R 7 and R 9 are the same or different and represent hydrogen or a natural or unnatural amino acid side chain moiety; each R 10 is the same or different and represents hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; Pr 1 and Pr 2 are the same or different and represent hydrogen or a thiol protecting group; Pr 3 is hydrogen or an alcohol protecting group; R 1 and R 5 are the same or different and represent Y or a natural or unnatural amino acid side-chain moiety, provided that R 1 and R 5 are not both a natural or unnatural amino acid side chain moiety; and Y is as defined in the application.
摘要翻译：式（IX）或（X）的化合物：包括其药学上可接受的盐; 其中：X是-C（= O）N（R 10） - 或-CH（OPr 3） - ; R7和R9相同或不同，表示氢或天然或非天然氨基酸侧链部分; 每个R 10相同或不同，表示氢，C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基; 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; R1和R5相同或不同，表示Y或天然或非天然氨基酸侧链部分，条件是R 1和R 5不是天然或非天然氨基酸侧链部分; 和Y如申请中所定义。

5. 发明申请

WO2011012883A1 BENZO [E] [1, 3 ] OXAZIN-4-ONE DERIVATIVES AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS 审中-公开
标题翻译：苯并[E] [1,3]氧嗪-4-酮衍生物作为磷酸三磷酸酶抑制剂
公开(公告)号：WO2011012883A1
公开(公告)日：2011-02-03
申请号：PCT/GB2010/051221
申请日：2010-07-23
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen Joseph , SILVA, Franck Alexandre , CECIL, Alexander Richard Liam , HILL, Thomas James
发明人： SHUTTLEWORTH, Stephen Joseph , SILVA, Franck Alexandre , CECIL, Alexander Richard Liam , HILL, Thomas James
IPC分类号： C07D265/24 , A61K31/536 , A61P35/00 , A61P9/00 , A61P37/00 , A61P29/00 , A61P5/00
CPC分类号： C07D265/24
摘要： Compounds of formula (I): wherein: W is O, N-H, N-alky!, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R 1 is formula (b) or R 3 is H, alkyl, NH 2 , OH, =0 or halogen; each A and B are independently CH or N; D is NHR 4 ; R 4 is H, alkyl, -C(O)- alkyl. -C(O)-NH 2 , -C(O)-NH- alkyl, -SO 2 - alky!, -SO 2 -NH 2 or -SO 2 -NH- alkyl; R 2 is aryl substituted with at least one nitrogen-containing group or R 2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C 1 -C 6 mono alkylamino, C 1 C 6 bis alkylamino, C 1 C 6 acylamino, C 1 -C 6 aminoalkyl, mono (C 1 C 6 alkyl) amino C 1 -C 6 alkyl, bis (C 1 C 6 alkyl) amino C 1 C 6 alkyl, C 1 -C 6 -acylamino or C 1 C 6 alkynyl-NR 11 ; R 11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, -C(O)-R 7 , -C(O)-NH 2 , -C(O)-NH-R 7 , -SO 2 -R 7 , -SO 2 -NH 2 , -SO 2 -NH- R 7 , NH-acyl, NH-sulfonyl, NR 7 -acyl, NR 7 -suIfonyl, N-C(O)-NH-R 7 , N-SO 2 -NH-R 7 , N-C(O)-NR 7 R 7 or N-SO 2 -NR 7 R 7 ; and R 7 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）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，卤素，O-烷基，NH-烷基，N-二烷基，-C（O）-R 7，-C（O）-NH 2，-C（O） NH-R7，-SO2-R7，-SO2-NH2，-SO2-NH-R7，NH-酰基，NH-磺酰基，NR7-酰基，NR7-磺酰基，NC（O） NH-R7，NC（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. 发明申请

WO2009141659A1 DEPSIPEPTIDES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：杀虫剂及其治疗用途
公开(公告)号：WO2009141659A1
公开(公告)日：2009-11-26
申请号：PCT/GB2009/050555
申请日：2009-05-22
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen Joseph , SILVA, Franck Alexandre , TOMASSI, Cyrille Davy , CECIL, Alexander Richard Liam , HILL, Thomas James
发明人： SHUTTLEWORTH, Stephen Joseph , SILVA, Franck Alexandre , TOMASSI, Cyrille Davy , CECIL, Alexander Richard Liam , HILL, Thomas James
IPC分类号： A61P35/00 , C07K5/02
CPC分类号： C07K5/06 , C07K5/06026 , C07K5/06139 , Y02P20/55
摘要： Compounds of the invention have Structure (III) or (IV) or a pharmaceutically acceptable salt thereof, wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 9 are the same or different and represent hydrogen or natural or unnatural amino acid side-chain moiety; each R 10 is the same of different and represents hydrogen or C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; Pr is hydrogen or an alcohol protecting group; R 8 represents -CR 11 R 11 -CR 11 R 11 -(CH 2 ) n -R 12, CR 11 =CR 11 -(CH 2 ) n -R 12, or -C≡C-(CH 2 )n-R 12 ; R 11 is hydrogen, C 1 -C 6 alkyl, aryl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or heteroaryl; R 12 is a linear or cyclic metal-chelating moiety; and n is an integer between 0 and 7, with the proviso that R 12 is not -SH or -SPr 2, wherein Pr 2 is a thiol protecting group.
摘要翻译：本发明化合物具有结构（III）或（IV）或其药学上可接受的盐，其中：R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 9相同或不同，表示氢或天然或非天然氨基酸侧链部分; 每个R 10是不同的并且表示氢或C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基; Pr是氢或醇保护基; R8表示-CR11R11-CR11 R11-（CH2）n-R12，CR11 = CR11-（CH2）n-R12或-C = C-（CH2）n-R12; R 11是氢，C 1 -C 6烷基，芳基，C 2 -C 6烯基，C 2 -C 6炔基或杂芳基; R12是线性或环状金属螯合部分; 并且n是0和7之间的整数，条件是R 12不是-SH或-SPr 2，其中Pr 2是硫醇保护基。

7. 发明申请

WO2009022182A1 DEPSIPEPTIDE DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：杀虫剂衍生物及其治疗用途
公开(公告)号：WO2009022182A1
公开(公告)日：2009-02-19
申请号：PCT/GB2008/050705
申请日：2008-08-13
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Steven Joseph , GANESAN, Arasu , CECIL, Alexander Richard Liam , HILL, Thomas James , TOMASSI, Cyrille Davy , SILVA, Franck Alexandre
发明人： SHUTTLEWORTH, Steven Joseph , GANESAN, Arasu , CECIL, Alexander Richard Liam , HILL, Thomas James , TOMASSI, Cyrille Davy , SILVA, Franck Alexandre
IPC分类号： C07K5/02 , A61K38/00
CPC分类号： C07K5/0207 , A61K38/00 , C07K5/021 , Y02P20/55
摘要： A compound of structure VII, VIII, IX or X wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 9 are the same or different and each represents an amino-acid side-chain moiety; each R 10 is the same or different and represents hydrogen or C 1 -C 6 alkyl, C 2 - C 6 alkenyl, C 2 -C 6 alkynyl or 5- or 6-membered aryl or heteroaryl; Pr is hydrogen or an alcohol protecting group; X 1 and X 2 are the same or different and each represents a non -peptide moiety; and R 8 is a metallophile capable of binding with zinc in the active site of HDAC; with the proviso that X1 is not the group -CHR 1 -CH(OPr-)-CHR 9 -, wherein R 1 , Pr and R 9 are as defined above; and pharmaceutically acceptable salts thereof.
摘要翻译：结构VII，VIII，IX或X的化合物，其中：R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 9相同或不同，各自表示氨基酸侧链部分。每个R 10相同或不同，表示氢或C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或5-或6-元芳基或杂芳基; Pr是氢或醇保护基; X1和X2相同或不同，各代表非肽部分; 并且R8是能够与HDAC的活性位点中的锌结合的金属离子; 条件是X1不是基团-CHR1-CH（OPr - ） - CHR9-，其中R1，Pr和R9如上所定义; 及其药学上可接受的盐。

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