JP2005502656A5 - - Google Patents
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- Publication number
- JP2005502656A5 JP2005502656A5 JP2003520749A JP2003520749A JP2005502656A5 JP 2005502656 A5 JP2005502656 A5 JP 2005502656A5 JP 2003520749 A JP2003520749 A JP 2003520749A JP 2003520749 A JP2003520749 A JP 2003520749A JP 2005502656 A5 JP2005502656 A5 JP 2005502656A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- group
- nitrogen atom
- heterocycle
- optionally substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000004429 atoms Chemical group 0.000 claims 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 1
- YYFXSRHYTXNLCL-UHFFFAOYSA-N N[N-]C(O)=O Chemical compound N[N-]C(O)=O YYFXSRHYTXNLCL-UHFFFAOYSA-N 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005488 carboaryl group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atoms Chemical class [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrugs Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Claims (10)
- 式(I)：
Ｒ1及びＲ2は独立して、水素、場合により置換されていてもよいＣ1-7アルキル基、Ｃ3-20ヘテロシクリル基若しくはＣ5-20アリール基であるか、又は、Ｒ1とＲ2はそれらが結合している窒素原子と一緒に4〜8個の環原子を有する、場合により置換されていてもよいヘテロ環を形成していてもよく、
Ｒ3は、場合により置換されていてもよいＣ5-20アリール基である]
で表される化合物並びにその異性体、塩、溶媒和物、化学的に保護されている形態及びプロドラッグ。 - Ｒ1とＲ2が、それらが結合している窒素原子と一緒に、5個、6個又は7個の環原子を有するヘテロ環を形成している、請求項1に記載の化合物。
- Ｒ1とＲ2及びそれらが結合している窒素原子によって形成されているヘテロ環が6個の環原子を有する、請求項2に記載の化合物。
- 前記ヘテロ環が、前記窒素原子の他にさらに1個の環ヘテロ原子を有している、請求項2又は3に記載の化合物。
- Ｒ3がＣ5-20カルボアリール基である、請求項1〜4のいずれか1項に記載の化合物。
- Ｒ3が、ヒドロキシ、ハロ、カルボキシ、アミノ、アミド、ホルミル、シアノ、Ｃ5-20アリール、Ｃ1-7アルキル、アシル、アシルアミド、エステル及びエーテルから選択される1個以上の置換基を有するフェニル基である、請求項5に記載の化合物。
- 請求項1〜6のいずれか1項に記載の化合物と製薬上許容される担体又は希釈剤を含む組成物。
- ヒト又は動物の体の治療方法で使用される、請求項1〜6のいずれか1項に記載の化合物。
- DNA-PKの活性を阻害するための薬物を調製するための、請求項1〜6のいずれか1項に記載の化合物の使用。
- 癌治療における補助薬として使用される薬物を調製するための、又は、電離放射線若しくは化学療法薬を用いた腫瘍細胞の治療効果を増強するための薬物を調製するための、請求項1〜6のいずれか1項に記載の化合物の使用。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0119863.9A GB0119863D0 (en) | 2001-08-14 | 2001-08-14 | DNA-PK inhibitors |
| PCT/GB2002/003740 WO2003015790A1 (en) | 2001-08-14 | 2002-08-14 | Thiopyrane-4-ones as dna protein kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005502656A JP2005502656A (ja) | 2005-01-27 |
| JP2005502656A5 true JP2005502656A5 (ja) | 2005-12-22 |
| JP4299666B2 JP4299666B2 (ja) | 2009-07-22 |
Family
ID=9920418
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003520749A Expired - Fee Related JP4299666B2 (ja) | 2001-08-14 | 2002-08-14 | Ｄｎａプロテインキナーゼ阻害剤としてのチオピラン−４−オン類 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7105518B2 (ja) |
| EP (1) | EP1416936B1 (ja) |
| JP (1) | JP4299666B2 (ja) |
| AT (1) | ATE296633T1 (ja) |
| DE (1) | DE60204468T2 (ja) |
| ES (1) | ES2243750T3 (ja) |
| GB (1) | GB0119863D0 (ja) |
| WO (1) | WO2003015790A1 (ja) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0119865D0 (en) * | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
| GB0209891D0 (en) * | 2002-04-30 | 2002-06-05 | Glaxo Group Ltd | Novel compounds |
| DE602004026071D1 (de) * | 2003-08-13 | 2010-04-29 | Kudos Pharm Ltd | Aminopyrone und ihre verwendung als atm inhibitoren |
| BRPI0515498A (pt) | 2004-09-20 | 2008-07-29 | Kudos Pharm Ltd | inibidores de dna-pk |
| TW200638938A (en) * | 2005-02-09 | 2006-11-16 | Kudos Pharm Ltd | ATM inhibitors |
| AR054438A1 (es) * | 2005-04-15 | 2007-06-27 | Kudos Pharm Ltd | Inhibidores de adn -pk |
| JP2008542253A (ja) * | 2005-05-26 | 2008-11-27 | クドス ファーマシューティカルズ リミテッド | Ｄｎａ損傷癌療法に対してａｔｍ欠損癌を感作するためのｄｎａ−ｐｋ阻害の使用 |
| UY31232A1 (es) * | 2007-07-19 | 2009-03-02 | Compuestos derivados de dibenzotifenilamino-cromen-4-onas activas sustituidas y sus isomeros y aplicaciones | |
| JP2022532178A (ja) * | 2019-05-10 | 2022-07-13 | 上海海雁医薬科技有限公司 | 置換フェニルプロペニルピリジン誘導体、その調製方法及びその医学的使用 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1303724A (ja) | 1969-05-14 | 1973-01-17 | ||
| JPH0753725B2 (ja) * | 1987-10-08 | 1995-06-07 | 富山化学工業株式会社 | ４ｈ―１―ベンゾピラン―４―オン誘導体およびその塩、それらの製造法並びにそれらを含有する抗炎症剤 |
| US5284856A (en) * | 1988-10-28 | 1994-02-08 | Hoechst Aktiengesellschaft | Oncogene-encoded kinases inhibition using 4-H-1-benzopyran-4-one derivatives |
| US5703075A (en) * | 1988-12-21 | 1997-12-30 | Pharmacia & Upjohn Company | Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones |
| AU634994B2 (en) | 1988-12-21 | 1993-03-11 | Pharmacia & Upjohn Company | Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones |
| JPH03215423A (ja) | 1990-01-18 | 1991-09-20 | Kyowa Hakko Kogyo Co Ltd | 血管拡張剤 |
| WO1991019707A2 (en) | 1990-06-20 | 1991-12-26 | The Upjohn Company | Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones |
| US5302613A (en) * | 1990-06-29 | 1994-04-12 | The Upjohn Company | Antiatheroscleroic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones |
| US5252735A (en) * | 1990-06-29 | 1993-10-12 | The Upjohn Company | Antiatherosclerotic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones |
| JPH05501886A (ja) | 1990-06-29 | 1993-04-08 | ジ・アップジョン・カンパニー | 抗アテローム性動脈硬化症性および抗血栓性２―アミノ―６―フェニル―４ｈ―ピラン―４―オン類 |
| EP0610519B1 (en) | 1992-09-02 | 1999-12-01 | Kyowa Hakko Kogyo Co., Ltd. | Anti-hiv drug |
| KR960701633A (ko) * | 1993-04-09 | 1996-03-28 | 가쯔히꼬 나까노 | 면역조절제, 세포 접착 억제제, 및 자기면역 질병의 치료 및 예방제(immunomo-dulator, cell adhesion inhibitor, and agent for treating and preventing autoimmune diseases) |
| US5378725A (en) | 1993-07-19 | 1995-01-03 | The Arizona Board Of Regents | Inhibition of phosphatidylinositol 3-kinase with wortmannin and analogs thereof |
| US5441947A (en) | 1993-08-25 | 1995-08-15 | Eli Lilly And Company | Methods of inhibiting vascular restenosis |
| US5468773A (en) | 1993-08-25 | 1995-11-21 | Eli Lilly And Company | Methods for inhibiting bone loss and cartilage degradation using wortmannin and its analogs |
| US5504103A (en) | 1993-08-25 | 1996-04-02 | Eli Lilly And Company | Inhibition of phosphatidylinositol 3-kinase with 17 β-hydroxywortmannin and analogs thereof |
| CA2133815A1 (en) | 1993-10-12 | 1995-04-13 | Jeffrey Alan Dodge | Inhibition of phosphatidylinositol 3-kinase with viridin, demethoxyviridin, viridiol, demethoxyviridiol, virone, wortmannolone, and analogs thereof |
| US6632789B1 (en) | 1994-04-29 | 2003-10-14 | The United States Of America As Represented By The Secretary Of The Navy | Methods for modulating T cell responses by manipulating intracellular signal transduction |
| US5480906A (en) | 1994-07-01 | 1996-01-02 | Eli Lilly And Company | Stereochemical Wortmannin derivatives |
| GB9521987D0 (en) | 1995-10-26 | 1996-01-03 | Ludwig Inst Cancer Res | Phosphoinositide 3-kinase modulators |
| US5733920A (en) * | 1995-10-31 | 1998-03-31 | Mitotix, Inc. | Inhibitors of cyclin dependent kinases |
| AU1461197A (en) | 1995-11-16 | 1997-06-05 | Icos Corporation | Cell cycle checkpoint pik-related kinase materials and methods |
| GB2302021A (en) | 1996-10-16 | 1997-01-08 | Lilly Co Eli | Inhibiting bone loss or resorption |
| CA2292540A1 (en) | 1997-06-06 | 1998-12-10 | Jann N. Sarkaria | Screening for phosphatidylinositol related-kinase inhibitors |
| WO1998056391A1 (en) | 1997-06-13 | 1998-12-17 | President And Fellows Of Harvard College | Methods for treating human cancers |
| FR2776291B1 (fr) | 1998-03-18 | 2000-06-16 | Pf Medicament | Nouveaux derives bis-benzamides, leur procede de fabrication, les compositions pharmaceutiques les contenant et leur utilisation comme medicament |
| US6387640B1 (en) * | 1999-02-10 | 2002-05-14 | St. Jude Children's Research Hospital | ATM kinase modulation for screening and therapies |
| US6348311B1 (en) * | 1999-02-10 | 2002-02-19 | St. Jude Childre's Research Hospital | ATM kinase modulation for screening and therapies |
| CA2398163C (en) | 2000-01-24 | 2011-02-22 | Kinacia Pty Ltd. | Therapeutic morpholino-substituted compounds |
| US7179912B2 (en) | 2000-09-01 | 2007-02-20 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| ATE290882T1 (de) | 2001-01-16 | 2005-04-15 | Glaxo Group Ltd | Pharmazeutische mischung gegen krebs, die ein 4- chinazolinamin in kombination mit paclitaxel, carboplatin or vinorelbine enthält |
| GB0119865D0 (en) * | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
| US6908932B2 (en) | 2001-10-24 | 2005-06-21 | Iconix Pharmaceuticals, Inc. | Modulators of phosphoinositide 3-kinase |
| WO2003034997A2 (en) | 2001-10-24 | 2003-05-01 | Iconix Pharmaceuticals, Inc. | Modulators of phosphoinositide 3-kinase |
| US7049313B2 (en) * | 2002-02-25 | 2006-05-23 | Kudos Pharmaceuticals Ltd. | ATM inhibitors |
| DK1485377T5 (da) | 2002-02-25 | 2010-12-06 | Kudos Pharm Ltd | Pyranoner egnede som ATM-inhibitorer |
| DE60335359D1 (de) | 2002-04-30 | 2011-01-27 | Kudos Pharm Ltd | Phthalazinonderivate |
-
2001
- 2001-08-14 GB GBGB0119863.9A patent/GB0119863D0/en not_active Ceased
-
2002
- 2002-08-14 JP JP2003520749A patent/JP4299666B2/ja not_active Expired - Fee Related
- 2002-08-14 DE DE60204468T patent/DE60204468T2/de not_active Expired - Lifetime
- 2002-08-14 EP EP02751427A patent/EP1416936B1/en not_active Expired - Lifetime
- 2002-08-14 ES ES02751427T patent/ES2243750T3/es not_active Expired - Lifetime
- 2002-08-14 WO PCT/GB2002/003740 patent/WO2003015790A1/en active IP Right Grant
- 2002-08-14 US US10/486,811 patent/US7105518B2/en not_active Expired - Fee Related
- 2002-08-14 AT AT02751427T patent/ATE296633T1/de not_active IP Right Cessation
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