JP2004525908A5 - - Google Patents
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- Publication number
- JP2004525908A5 JP2004525908A5 JP2002569071A JP2002569071A JP2004525908A5 JP 2004525908 A5 JP2004525908 A5 JP 2004525908A5 JP 2002569071 A JP2002569071 A JP 2002569071A JP 2002569071 A JP2002569071 A JP 2002569071A JP 2004525908 A5 JP2004525908 A5 JP 2004525908A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- fluorostyryl
- alkoxy
- group
- radioprotective
- 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 12
- -1 penta-substituted phenyl Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 230000004223 radioprotective effect Effects 0.000 claims 5
- 230000005865 ionizing radiation Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 230000001950 radioprotection Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 2
- OVFAELKNQAHPES-UHFFFAOYSA-N cyano phosphono carbonate Chemical compound C(#N)OC(=O)OP(=O)(O)O OVFAELKNQAHPES-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- LSQPHWBCMFQPAP-XPWSMXQVSA-N 1,3,5-trimethoxy-2-[(e)-3-(4-methoxyphenyl)-3-[(e)-1-(4-methoxyphenyl)-3-(2,4,6-trimethoxyphenyl)prop-2-enyl]sulfonylprop-1-enyl]benzene Chemical compound C1=CC(OC)=CC=C1C(S(=O)(=O)C(\C=C\C=1C(=CC(OC)=CC=1OC)OC)C=1C=CC(OC)=CC=1)\C=C\C1=C(OC)C=C(OC)C=C1OC LSQPHWBCMFQPAP-XPWSMXQVSA-N 0.000 claims 1
- LRHCIAKITMHSNT-FDWQPRGYSA-N 1-[(z)-3-(4-chlorophenyl)-3-[(z)-1-(4-chlorophenyl)-3-(4-fluorophenyl)prop-2-enyl]sulfonylprop-1-enyl]-4-fluorobenzene Chemical compound C1=CC(F)=CC=C1\C=C/C(S(=O)(=O)C(\C=C/C=1C=CC(F)=CC=1)C=1C=CC(Cl)=CC=1)C1=CC=C(Cl)C=C1 LRHCIAKITMHSNT-FDWQPRGYSA-N 0.000 claims 1
- PTXRVHYRFPXJKU-OGBZJDJUSA-N 1-fluoro-4-[(e)-3-[(e)-3-(4-fluorophenyl)-1-[4-(trifluoromethyl)phenyl]prop-2-enyl]sulfonyl-3-[4-(trifluoromethyl)phenyl]prop-1-enyl]benzene Chemical compound C1=CC(F)=CC=C1\C=C\C(S(=O)(=O)C(\C=C\C=1C=CC(F)=CC=1)C=1C=CC(=CC=1)C(F)(F)F)C1=CC=C(C(F)(F)F)C=C1 PTXRVHYRFPXJKU-OGBZJDJUSA-N 0.000 claims 1
- XHHUIUHBUNSNOW-LQGKIZFRSA-N 4-[(e)-1-[(e)-1-(4-cyanophenyl)-3-(4-fluorophenyl)prop-2-enyl]sulfonyl-3-(4-fluorophenyl)prop-2-enyl]benzonitrile Chemical compound C1=CC(F)=CC=C1\C=C\C(S(=O)(=O)C(\C=C\C=1C=CC(F)=CC=1)C=1C=CC(=CC=1)C#N)C1=CC=C(C#N)C=C1 XHHUIUHBUNSNOW-LQGKIZFRSA-N 0.000 claims 1
- SNGZRCQJDGCGEF-OGBZJDJUSA-N 4-[(e)-3-[(e)-3-(4-carboxyphenyl)-1-(4-chlorophenyl)prop-2-enyl]sulfonyl-3-(4-chlorophenyl)prop-1-enyl]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1\C=C\C(S(=O)(=O)C(\C=C\C=1C=CC(=CC=1)C(O)=O)C=1C=CC(Cl)=CC=1)C1=CC=C(Cl)C=C1 SNGZRCQJDGCGEF-OGBZJDJUSA-N 0.000 claims 1
- ARXGEFCQNAWAPD-FACPPWRESA-N 4-chloro-1-[4-chloro-2-[(e)-2-(4-fluorophenyl)ethenyl]phenyl]sulfonyl-2-[(e)-2-(4-fluorophenyl)ethenyl]benzene Chemical compound C1=CC(F)=CC=C1\C=C\C1=CC(Cl)=CC=C1S(=O)(=O)C1=CC=C(Cl)C=C1\C=C\C1=CC=C(F)C=C1 ARXGEFCQNAWAPD-FACPPWRESA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000005362 aryl sulfone group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000004224 protection Effects 0.000 claims 1
- 230000001681 protective effect Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27199001P | 2001-02-28 | 2001-02-28 | |
| PCT/US2002/006107 WO2002069892A2 (en) | 2001-02-28 | 2002-02-28 | METHOD FOR PROTECTING CELLS AND TISSUES FROM IONIZING RADIATION TOXICITY WITH α, β UNSATURATED ARYL SULFONES |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004525908A JP2004525908A (ja) | 2004-08-26 |
| JP2004525908A5 true JP2004525908A5 (https=) | 2005-12-22 |
| JP4302986B2 JP4302986B2 (ja) | 2009-07-29 |
Family
ID=23037934
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002569071A Expired - Lifetime JP4302986B2 (ja) | 2001-02-28 | 2002-02-28 | 細胞及び組織をα，β不飽和アリールスルホンにより電離放射線から防護する方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6667346B2 (https=) |
| EP (1) | EP1370253B8 (https=) |
| JP (1) | JP4302986B2 (https=) |
| KR (1) | KR100850331B1 (https=) |
| AT (1) | ATE406881T1 (https=) |
| AU (1) | AU2002305942B2 (https=) |
| CA (1) | CA2439288C (https=) |
| DE (1) | DE60228692D1 (https=) |
| IL (2) | IL157541A0 (https=) |
| WO (1) | WO2002069892A2 (https=) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002028828A1 (en) | 2000-10-05 | 2002-04-11 | Temple University - Of The Commonwealth System Of Higher Education | Substituted (e)-styryl benzylsulfones for treating proliferative disorders |
| EP1534284B1 (en) * | 2002-02-28 | 2011-07-27 | Temple University - Of The Commonwealth System of Higher Education | Amino-substituted sulfonanilides and derivatives thereof for treating proliferative disorders |
| WO2003072062A2 (en) * | 2002-02-28 | 2003-09-04 | Temple University-Of The Commonwealth System Of Higher Education | Amino-substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones for treating proliferative disorders |
| JP5196787B2 (ja) * | 2003-11-14 | 2013-05-15 | テンプル・ユニバーシティ−オブ・ザ・コモンウェルス・システム・オブ・ハイアー・エデュケイション | 増殖性疾患を治療するためのα，β−不飽和スルホキシド |
| US7649013B2 (en) * | 2003-11-26 | 2010-01-19 | Arqule, Inc. | Methods of protecting against radiation injury |
| KR101274524B1 (ko) | 2004-03-16 | 2013-06-19 | 온코노바 테라퓨틱스, 인코포레이티드 | 증식성 질병 치료용 치환 페녹시- 및 페닐티오- 유도체 |
| EP1773310B9 (en) | 2004-06-24 | 2012-04-25 | Temple University - Of The Commonwealth System of Higher Education | Alpha, beta-unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides and therapeutic uses thereof |
| CA2574491C (en) * | 2004-07-19 | 2011-05-24 | Onconova Therapeutics, Inc. | Formulations for parenteral administration of (e)-2,6-dialkoxystryryl 4-substituted benzylsulfones |
| US7537572B2 (en) | 2004-10-22 | 2009-05-26 | General Patent, Llc | Treatment or pre-treatment for radiation/chemical exposure |
| US20090306207A1 (en) * | 2005-01-05 | 2009-12-10 | Reddy M V Ramana | Treatment of Drug-Resistant Proliferative Disorders |
| AU2006216544B2 (en) * | 2005-02-25 | 2012-04-05 | Onconova Therapeutics, Inc. | Unsaturated sulfides, sulfones, sulfoxides and sulfonamides synthesis |
| WO2006104668A2 (en) * | 2005-03-11 | 2006-10-05 | Temple University - Of The Commonwealth System Of Higher Education | Composition and methods for the treatment of proliferative diseases |
| AU2006275822B2 (en) * | 2005-07-29 | 2012-02-02 | Onconova Therapeutics, Inc. | Formulation of radioprotective alpha, beta unsaturated aryl sulfones |
| EP1864692A1 (en) * | 2006-06-07 | 2007-12-12 | Biotempt B.V. | Use of peptides for the control of radiation injury |
| JP2007302640A (ja) * | 2006-05-15 | 2007-11-22 | Natl Inst Of Radiological Sciences | 抗放射線被ばく障害剤 |
| CA2659222C (en) * | 2006-07-28 | 2012-01-31 | Onconova Therapeutics, Inc. | Formulations of radioprotective .alpha., .beta. unsaturated aryl sulfones |
| JP5278968B2 (ja) | 2006-08-30 | 2013-09-04 | テンプル・ユニバーシティ−オブ・ザ・コモンウェルス・システム・オブ・ハイアー・エデュケイション | 骨髄異形性症候群及び急性骨髄性白血病の治療のための組成物及び方法 |
| CA2663375A1 (en) * | 2006-09-15 | 2008-03-20 | Onconova Therapeutics, Inc. | Activated cytotoxic compounds for attachment to targeting molecules for the treatment of mammalian disease conditions |
| WO2008076270A2 (en) * | 2006-12-13 | 2008-06-26 | Temple University-Of The Commonwealth System Of Higher Education | Sulfide, sulfoxide and sulfone chalcone analogues, derivatives thereof and therapeutic uses thereof |
| US20100049284A1 (en) * | 2008-05-15 | 2010-02-25 | The Catholic University Of America | Use of heat to treat biological systems exposed to damaging radiation |
| JP2012504646A (ja) * | 2008-10-01 | 2012-02-23 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 選択的サイクリン依存性キナーゼ４／６阻害剤を用いた化学療法化合物に対する造血系の防護 |
| CN102231983A (zh) * | 2008-10-01 | 2011-11-02 | 北卡罗来纳大学查珀尔希尔分校 | 使用选择性细胞周期蛋白依赖性激酶4/6抑制剂对抗电离辐射的造血防护 |
| JP5734869B2 (ja) * | 2008-12-16 | 2015-06-17 | オンコノバ・セラピューティックス・インコーポレーテッド | ヒトにおける細胞毒性物質の有害作用に対する治療レジメンの有効性を決定する方法 |
| JP2012526850A (ja) | 2009-05-13 | 2012-11-01 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | サイクリン依存性キナーゼ阻害剤及びその用法 |
| CA2792883A1 (en) * | 2010-03-24 | 2011-09-29 | Onconova Therapeutics, Inc. | Compositions and methods for prevention and treatment of wounds |
| KR101838764B1 (ko) * | 2010-03-26 | 2018-03-14 | 온코노바 테라퓨틱스, 인코포레이티드 | (ｅ)-4-카복시스티릴-4-클로로벤질설폰의 개선된 안정한 수성 제형 |
| GB201010359D0 (en) | 2010-06-21 | 2010-08-04 | Univ Nottingham | Compounds for treating proliferative disorders |
| WO2012068381A2 (en) | 2010-11-17 | 2012-05-24 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from schema through inhibition of the proliferative kisses cdk4 and cdk6 |
| KR101992929B1 (ko) | 2012-09-20 | 2019-06-25 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 치환된 알킬 디아릴 유도체, 제조방법 및 용도 |
| CA2906157C (en) | 2013-03-15 | 2022-05-17 | G1 Therapeutics, Inc. | Highly active anti-neoplastic and anti-proliferative agents |
| ME03557B (me) | 2013-03-15 | 2020-07-20 | G1 Therapeutics Inc | Privremena zaštiтa normalnih ćelija током hemoterapije |
| CN104230770B (zh) * | 2013-06-17 | 2017-11-21 | 华夏生生药业(北京)有限公司 | 苯乙烯基砜类化合物、其制备方法以及其作为神经保护剂的应用 |
| US10195466B2 (en) * | 2014-01-06 | 2019-02-05 | Hackensack University Medical Center | Method for treating skin cancer using radiation therapy |
| WO2015161288A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use as anti-neoplastic and anti-proliferative agents |
| EP3191098A4 (en) | 2014-09-12 | 2018-04-25 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| US10383831B2 (en) | 2015-08-03 | 2019-08-20 | Temple University—Of the Commonwealth System of Higher Education | 2,4,6-trialkoxystryl aryl sulfones, sulfonamides and carboxamides, and methods of preparation and use |
| CN106432011B (zh) * | 2016-09-18 | 2018-11-02 | 中国医学科学院放射医学研究所 | 一类具有辐射防护作用的新化合物、其制备方法及其药物应用 |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| BR112020006677A2 (pt) | 2017-10-05 | 2020-10-06 | Fulcrum Therapeutics, Inc. | uso de inibidores p38 para reduzir a expressão de dux4 |
| JP7324930B2 (ja) * | 2019-07-18 | 2023-08-10 | フアシアシェンシェン ファーマシューティカル ベイジン カンパニー リミテッド | カルバメート置換スチリルスルホン類化合物及びその製造方法ならびにその使用 |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU741042B2 (en) | 1997-10-03 | 2001-11-22 | Temple University - Of The Commonwealth System Of Higher Education | Styryl sulfone anticancer agents |
| US6201154B1 (en) * | 1999-03-31 | 2001-03-13 | Temple University-Of The Commonwealth Of Higher Education | Z-styryl sulfone anticancer agents |
| EP1173160B1 (en) * | 1999-04-02 | 2005-06-22 | Temple University of the Commonwealth System of Higher Education | (e)-styryl sulfone anticancer agents |
| AU3381399A (en) * | 1999-04-02 | 2000-10-23 | Temple University - Of The Commonwealth System Of Higher Education | Styryl sulfone anticancer agents |
| AU780844B2 (en) * | 1999-10-12 | 2005-04-21 | Temple University-Of The Commonwealth System Of Higher Education | Method for protecting normal cells from cytotoxicity of chemotherapeutic agents |
| US6664287B2 (en) * | 2000-03-15 | 2003-12-16 | Bethesda Pharmaceuticals, Inc. | Antioxidants |
| US7271187B2 (en) * | 2000-04-06 | 2007-09-18 | Tim Neuberger | Compositions and methods for promoting tissue regeneration |
| US6486210B2 (en) | 2000-04-14 | 2002-11-26 | Temple University—Of the Commonwealth System of Higher Education | Substituted styryl benzylsulfones for treating proliferative disorders |
| US6646009B2 (en) * | 2001-02-28 | 2003-11-11 | Temple University — Of Commonwealth System of Higher Education | N-(aryl)-2-arylethenesulfonamides and therapeutic uses thereof |
-
2002
- 2002-02-28 AU AU2002305942A patent/AU2002305942B2/en not_active Expired
- 2002-02-28 DE DE60228692T patent/DE60228692D1/de not_active Expired - Lifetime
- 2002-02-28 IL IL15754102A patent/IL157541A0/xx unknown
- 2002-02-28 EP EP02733811A patent/EP1370253B8/en not_active Expired - Lifetime
- 2002-02-28 JP JP2002569071A patent/JP4302986B2/ja not_active Expired - Lifetime
- 2002-02-28 AT AT02733811T patent/ATE406881T1/de not_active IP Right Cessation
- 2002-02-28 KR KR1020037011357A patent/KR100850331B1/ko not_active Expired - Lifetime
- 2002-02-28 WO PCT/US2002/006107 patent/WO2002069892A2/en not_active Ceased
- 2002-02-28 CA CA2439288A patent/CA2439288C/en not_active Expired - Lifetime
- 2002-02-28 US US10/085,745 patent/US6667346B2/en not_active Expired - Lifetime
-
2003
- 2003-08-21 IL IL157541A patent/IL157541A/en active IP Right Grant
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