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1. 发明申请

WO2010086646A1 SCRIPTAID ISOSTERES AND THEIR USE IN THERAPY 审中-公开
标题翻译： SCRIPTID ISOSTERES及其在治疗中的使用
公开(公告)号：WO2010086646A1
公开(公告)日：2010-08-05
申请号：PCT/GB2010/050116
申请日：2010-01-26
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen Joseph , TOMASSI, Cyrille Davy
发明人： SHUTTLEWORTH, Stephen Joseph , TOMASSI, Cyrille Davy
IPC分类号： C07D213/24 , C07D213/74 , C07D401/06 , C07D401/12 , A61K31/4402 , A61K31/444 , A61P1/00 , A61P3/10 , A61P9/00 , A61P35/00 , A61P37/00
CPC分类号： C07D213/55 , A61K31/4433 , A61K31/444 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K45/06 , C07D213/22 , C07D213/24 , C07D213/34 , C07D213/38 , C07D213/40 , C07D213/74 , C07D401/06 , C07D401/12
摘要： Compounds of the invention are of the formula (I); wherein: … is a double bond and X is C; or … is a single bond and X is N, CH or CQR 1 ; and wherein: n is 1 to 10; R is H or QR 1 ; each R' is independently selected from H and QR 1 ; each Q is independently selected from a bond, CO, NH, S, SO, SO 2 or O; each R 1 is independently selected from C 1 -C 10 alkyl, C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C 1 -C 10 cycloalkyl, halogen, C 1 -C 10 alkylaryl or C 1 -C 10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.
摘要翻译：本发明的化合物具有式（I）; 其中：...为双键，X为C; 或...是单键，X是N，CH或CQR1; 并且其中：n为1至10; R为H或QR1; 每个R'独立地选自H和QR1; 每个Q独立地选自键，CO，NH，S，SO，SO 2或O; C 1 -C 10烷基，C 2 -C 10炔基，取代或未取代的芳基或杂芳基，酰基，C 1 -C 10环烷基，卤素，C 1 -C 10烷基芳基或C 1 -C 10杂环烷基; L是含氮杂芳基; W是锌螯合残基; 或其药学上可接受的盐。这些化合物可用于治疗。

2. 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。

3. 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。

4. 发明申请

WO2006004703A3 PYRROLO[2,3-d]PYRIMIDINES THAT MODULATE ACK1 AND LCK ACTIVITY 审中-公开
标题翻译：吡咯并[2,3-d]嘧啶类化合物调节ACK1和LCK活性
公开(公告)号：WO2006004703A3
公开(公告)日：2006-03-09
申请号：PCT/US2005022836
申请日：2005-06-29
申请人： AMGEN INC , FARTHING CHRISTOPHER N , FAULDER PAUL , FRENKEL ALEXANDER DAVID , HARRISON MARTIN JAMES , JIAO XIANYUN , KAYSER FRANK , KOPECKY DAVID J , LIU JINQIAN , LIVELY SARAH E , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH
发明人： FARTHING CHRISTOPHER N , FAULDER PAUL , FRENKEL ALEXANDER DAVID , HARRISON MARTIN JAMES , JIAO XIANYUN , KAYSER FRANK , KOPECKY DAVID J , LIU JINQIAN , LIVELY SARAH E , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH
IPC分类号： C07D487/00 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.
摘要翻译：描述了调节ACK1和LCK作用的化合物，以及用于治疗ACK1-和LCK介导的疾病的相关组合物方法。在一个方面，化合物具有通式结构：其中取代基的值在本文中提供。

5. 发明申请

WO2008125839A3 PYRIMIDINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3-KINASE 审中-公开
公开(公告)号：WO2008125839A3
公开(公告)日：2008-10-23
申请号：PCT/GB2008/001301
申请日：2008-04-14
申请人： PIRAMED LIMITED , THE INSTITUTE OF CANCER RESEARCH , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
发明人： GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
IPC分类号： C07D403/04 , C07D401/14 , C07D417/14 , A61K31/506 , A61P35/00
摘要： The invention provides compounds which are pyrimidines for formula (i): wherein R 1, R 2 are as described herein, and/or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising form abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

6. 发明申请

WO2008125833A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008125833A1
公开(公告)日：2008-10-23
申请号：PCT/GB2008/001292
申请日：2008-04-14
申请人： PIRAMED LIMITED , THE INSTITUTE OF CANCER RESEARCH , BAKER, Stewart, James , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , KRINTEL, Sussie, Lerche , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
发明人： BAKER, Stewart, James , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , KRINTEL, Sussie, Lerche , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D487/04 , A61K31/5377 , A61P35/00
CPC分类号： C07D487/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14
摘要： The invention provides a compound which is a pyrimidine of formula (I): The compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了一种化合物，其是式（I）的嘧啶：该化合物是PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症，免疫疾病相关的异常细胞生长，功能或行为引起的疾病和病症，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

7. 发明申请

WO2007122410A1 PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：吡嗪衍生物作为PI3K抑制剂
公开(公告)号：WO2007122410A1
公开(公告)日：2007-11-01
申请号：PCT/GB2007/001504
申请日：2007-04-25
申请人： PIRAMED LIMITED , BAKER, Stewart, James , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , PRICE, Stephen , SHUTTLEWORTH, Stephen, Joseph , SOHAL, Sukhjit
发明人： BAKER, Stewart, James , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , PRICE, Stephen , SHUTTLEWORTH, Stephen, Joseph , SOHAL, Sukhjit
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： Thienopyrimidines of formula (Ia) or (Ib): wherein R 1 , R 2 , R 3 , are as defined in the claims.
摘要翻译：式（Ia）或（Ib）的噻吩并嘧啶：其中R 1，R 2，R 3，3如权利要求中所定义。

8. 发明申请

WO2006004658A3 FURANOPYRIMIDINES 审中-公开
公开(公告)号：WO2006004658A3
公开(公告)日：2006-01-12
申请号：PCT/US2005/022727
申请日：2005-06-29
申请人： AMGEN INC. , BUCHANAN, John L. , BUCKNER, William H. , BURKITT, Simon A. , DIMAURO, Erin F. , FARTHING, Christopher N. , FRENKEL, Alexander David , HARRISON, Martin J. , KAYSER, Frank , LIU, Jinqian , LIVELY, Sarah E. , MARSHALL, Teresa L. , MCGOWAN, David C. , SHARMA, Rajiv , SHUTTLEWORTH, Stephen Joseph , ZHU, Xiaotian
发明人： BUCHANAN, John L. , BUCKNER, William H. , BURKITT, Simon A. , DIMAURO, Erin F. , FARTHING, Christopher N. , FRENKEL, Alexander David , HARRISON, Martin J. , KAYSER, Frank , LIU, Jinqian , LIVELY, Sarah E. , MARSHALL, Teresa L. , MCGOWAN, David C. , SHARMA, Rajiv , SHUTTLEWORTH, Stephen Joseph , ZHU, Xiaotian
IPC分类号： C07D498/04 , A61K31/519
摘要： The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).

9. 发明申请

WO2006004658A2 FURANOPYRIMIDINES 审中-公开
公开(公告)号：WO2006004658A2
公开(公告)日：2006-01-12
申请号：PCT/US2005022727
申请日：2005-06-29
申请人： AMGEN INC , BUCHANAN JOHN L , BUCKNER WILLIAM H , BURKITT SIMON A , DIMAURO ERIN F , FARTHING CHRISTOPHER N , FRENKEL ALEXANDER DAVID , HARRISON MARTIN J , KAYSER FRANK , LIU JINQIAN , LIVELY SARAH E , MARSHALL TERESA L , MCGOWAN DAVID C , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH , ZHU XIAOTIAN
发明人： BUCHANAN JOHN L , BUCKNER WILLIAM H , BURKITT SIMON A , DIMAURO ERIN F , FARTHING CHRISTOPHER N , FRENKEL ALEXANDER DAVID , HARRISON MARTIN J , KAYSER FRANK , LIU JINQIAN , LIVELY SARAH E , MARSHALL TERESA L , MCGOWAN DAVID C , SHARMA RAJIV , SHUTTLEWORTH STEPHEN JOSEPH , ZHU XIAOTIAN
IPC分类号： C07D498/00
CPC分类号： C07D491/04 , C07D495/04
摘要： The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).
摘要翻译：本发明涉及具有通式（I）的呋喃并嘧啶化合物及其立体异构体，互变异构体，溶剂化物，药学上可接受的盐和衍生物以及前药。本发明还包括包含式（I）化合物的药物组合物，治疗哺乳动物各种疾病和病症的方法，包括炎症，抑制T细胞活化，增殖，关节炎，器官移植，局部缺血或再灌注损伤，心肌梗塞，中风，多发性硬化症，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺机能亢进症，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，癌症，结肠癌和胸腺瘤，所述方法包括给所述哺乳动物施用治疗有效量的式（I）化合物。本发明还涉及制造包含一种或多种式（I）化合物的药物的方法。

10. 发明申请

WO2011135351A1 NAPHTHRIDINE DERIVATIVES AS PI3K INHIBITORS FOR THE TREATMENT OF CANCER AND IMMUNE - INFLAMMATORY DISEASES 审中-公开
标题翻译：作为治疗癌症和免疫的PI3K抑制剂的萘普生衍生物 - 炎症性疾病
公开(公告)号：WO2011135351A1
公开(公告)日：2011-11-03
申请号：PCT/GB2011/050824
申请日：2011-04-26
申请人： KARUS THERAPEUTICS LIMITED , SHUTTLEWORTH, Stephen, Joseph , SILVA, Franck, Alexandre
发明人： SHUTTLEWORTH, Stephen, Joseph , SILVA, Franck, Alexandre
IPC分类号： C07D471/04 , A61K31/4375 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D471/04
摘要： Compounds of formulae (I) and (II): or a pharmaceutically acceptable salt thereof, wherein: R 1 is a nitrogen-containing 5 to 7-membered heteroaryl or heterocycle; R 2 and R 3 are each independently (LQ) m Y, are described. The compounds are PI3K inhibitors and are useful for the treatment of cancer and immune-inflammatory diseases.
摘要翻译：式（I）和（II）的化合物或其药学上可接受的盐，其中：R 1是含氮的5至7元杂芳基或杂环; R2和R3各自独立地为（LQ）mY。这些化合物是PI3K抑制剂，可用于治疗癌症和免疫炎性疾病。

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