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 (enExample) | 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 (enExample) |
| EP (1) | EP1370253B8 (enExample) |
| JP (1) | JP4302986B2 (enExample) |
| KR (1) | KR100850331B1 (enExample) |
| AT (1) | ATE406881T1 (enExample) |
| AU (1) | AU2002305942B2 (enExample) |
| CA (1) | CA2439288C (enExample) |
| DE (1) | DE60228692D1 (enExample) |
| IL (2) | IL157541A0 (enExample) |
| WO (1) | WO2002069892A2 (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1328511B1 (en) | 2000-10-05 | 2010-03-24 | Temple University of the Commonwealth System of Higher Education | Substituted (e)-styryl benzylsulfones for treating proliferative disorders |
| JP4538233B2 (ja) * | 2002-02-28 | 2010-09-08 | 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 | 増殖性障害治療用の、アミノ置換されたスルホンアニリド及びその誘導体 |
| AU2003213660C1 (en) * | 2002-02-28 | 2010-10-28 | Onconova Therapeutics, Inc. | Amino-substituted (E)-2,6-dialkoxystyryl 4-substituted benzylsulfones for treating proliferative disorders |
| KR20060109871A (ko) * | 2003-11-14 | 2006-10-23 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 증식성 질병 치료용 알파, 베타-불포화 설폭시드 |
| WO2005053682A2 (en) * | 2003-11-26 | 2005-06-16 | Arqule, Inc. | Use of beta-lapachone for protecting against radiation injury |
| WO2005089269A2 (en) * | 2004-03-16 | 2005-09-29 | Temple University - Of The Commonwealth System Of Higher Education | Substituted phenoxy- and phenylthio- derivatives for treating proliferative disorders |
| CA2577309C (en) | 2004-06-24 | 2013-10-22 | Temple University - Of The Commonwealth System Of Higher Education | Alpha, beta-unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides and therapeutic uses thereof |
| WO2006010152A2 (en) * | 2004-07-19 | 2006-01-26 | 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 |
| KR20070094956A (ko) * | 2005-01-05 | 2007-09-27 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 약-내성 증식성 질병의 치료 |
| PT1896401E (pt) * | 2005-02-25 | 2013-07-17 | Univ Temple | Síntese de sulfuretos, sulfonas, sulfóxidos e sulfonamidas não saturados |
| US8106033B2 (en) * | 2005-03-11 | 2012-01-31 | Temple University - Of The Commonwealth System Of Higher Education | Composition and methods for the treatment of proliferative diseases |
| NZ565561A (en) | 2005-07-29 | 2011-01-28 | 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 |
| WO2008105808A2 (en) * | 2006-07-28 | 2008-09-04 | Onconova Therapeutics, Inc. | FORMULATIONS OF RADIOPROTECTIVE α, β UNSATURATED ARYL SULFONES |
| CA2661983C (en) | 2006-08-30 | 2015-05-05 | Mount Sinai School Of Medicine Of New York University | Composition and methods for the treatment of myelodysplastic syndrome and acute myeloid leukemia |
| US8273787B2 (en) * | 2006-09-15 | 2012-09-25 | Onconova Therapeutics, Inc | Activated cytotoxic compounds for attachment to targeting molecules for the treatment of mammalian disease conditions |
| US8808702B2 (en) * | 2006-12-13 | 2014-08-19 | 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 |
| 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 |
| 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 |
| CA2747418A1 (en) * | 2008-12-16 | 2010-07-01 | Onconova Therapeutics, Inc. | Methods for determining efficacy of a therapeutic regimen against deleterious effects of cytotoxic agents |
| CA2761896A1 (en) | 2009-05-13 | 2010-11-18 | The University Of North Carolina At Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| EA022360B1 (ru) * | 2010-03-24 | 2015-12-30 | Онконова Терапьютикс, Инк. | Композиции и способы для профилактики и лечения ран |
| AU2011232341B2 (en) | 2010-03-26 | 2014-05-01 | Onconova Therapeutics, Inc. | Improved stable aqueous formulation of (E)-4-carboxystyryl-4-chlorobenzyl sulfone |
| 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 |
| CA2885217C (en) | 2012-09-20 | 2019-10-08 | Temple University - Of The Commonwealth System Of Higher Education | Substituted alkyl diaryl derivatives, methods of preparation and uses |
| US9527857B2 (en) | 2013-03-15 | 2016-12-27 | GI Therapeutics, Inc. | HSPC-sparing treatments for RB-positive abnormal cellular proliferation |
| US20140271460A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Highly Active Anti-Neoplastic and Anti-Proliferative Agents |
| 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 |
| CA2936036C (en) * | 2014-01-06 | 2022-08-16 | Hackensack University Medical Center | Method for treating skin cancer using radiation therapy |
| WO2015161283A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use in hspc-sparing treatments for rb-positive abnormal cellular proliferation |
| 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 |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| 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 |
| JP2021501130A (ja) | 2017-10-05 | 2021-01-14 | フルクラム セラピューティクス,インコーポレイテッド | DUX4の発現を低減するためのp38阻害剤の使用 |
| CN118239868A (zh) | 2019-07-18 | 2024-06-25 | 华夏生生药业(北京)有限公司 | 氨基甲酸酯取代的苯乙烯基砜类化合物及其制备方法和用途 |
| 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 |
|---|---|---|---|---|
| JP4294217B2 (ja) * | 1997-10-03 | 2009-07-08 | 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 | スチリルスルホン抗癌剤 |
| US6201154B1 (en) | 1999-03-31 | 2001-03-13 | Temple University-Of The Commonwealth Of Higher Education | Z-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 |
| AU774738B2 (en) | 1999-04-02 | 2004-07-08 | Temple University - Of The Commonwealth System Of Higher Education | (E)-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 |
| WO2001076592A1 (en) * | 2000-04-06 | 2001-10-18 | Acorda Therapeutics, Inc. | Compositions and methods for promoting neural 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 |
| AU2002306604B2 (en) * | 2001-02-28 | 2007-09-13 | Onconova Therapeutics, Inc. | N-(Aryl)-2-arylethenesulfonamides and therapeutic uses thereof |
-
2002
- 2002-02-28 US US10/085,745 patent/US6667346B2/en not_active Expired - Lifetime
- 2002-02-28 AT AT02733811T patent/ATE406881T1/de not_active IP Right Cessation
- 2002-02-28 AU AU2002305942A patent/AU2002305942B2/en not_active Expired
- 2002-02-28 JP JP2002569071A patent/JP4302986B2/ja not_active Expired - Lifetime
- 2002-02-28 EP EP02733811A patent/EP1370253B8/en not_active Expired - Lifetime
- 2002-02-28 CA CA2439288A patent/CA2439288C/en not_active Expired - Lifetime
- 2002-02-28 KR KR1020037011357A patent/KR100850331B1/ko not_active Expired - Lifetime
- 2002-02-28 IL IL15754102A patent/IL157541A0/xx unknown
- 2002-02-28 DE DE60228692T patent/DE60228692D1/de not_active Expired - Lifetime
- 2002-02-28 WO PCT/US2002/006107 patent/WO2002069892A2/en not_active Ceased
-
2003
- 2003-08-21 IL IL157541A patent/IL157541A/en active IP Right Grant
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