JP2012517442A5 - - Google Patents
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- JP2012517442A5 JP2012517442A5 JP2011549318A JP2011549318A JP2012517442A5 JP 2012517442 A5 JP2012517442 A5 JP 2012517442A5 JP 2011549318 A JP2011549318 A JP 2011549318A JP 2011549318 A JP2011549318 A JP 2011549318A JP 2012517442 A5 JP2012517442 A5 JP 2012517442A5
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- JP
- Japan
- Prior art keywords
- compound
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- hydrogen
- composition
- alkyl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 104
- 229910052739 hydrogen Inorganic materials 0.000 claims description 42
- 239000001257 hydrogen Substances 0.000 claims description 42
- 206010028980 Neoplasm Diseases 0.000 claims description 35
- 201000011510 cancer Diseases 0.000 claims description 35
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 31
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 23
- 238000000034 method Methods 0.000 claims description 20
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 18
- 150000002431 hydrogen Chemical class 0.000 claims description 18
- 239000012190 activator Substances 0.000 claims description 14
- 102000003952 Caspase 3 Human genes 0.000 claims description 8
- 108090000397 Caspase 3 Proteins 0.000 claims description 8
- 125000003277 amino group Chemical group 0.000 claims description 8
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 230000001939 inductive effect Effects 0.000 claims description 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 8
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 6
- 230000006907 apoptotic process Effects 0.000 claims description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 6
- 150000007942 carboxylates Chemical group 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims description 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 239000001301 oxygen Substances 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 230000008499 blood brain barrier function Effects 0.000 claims description 3
- 210000001218 blood-brain barrier Anatomy 0.000 claims description 3
- 230000002887 neurotoxic effect Effects 0.000 claims description 3
- 102000004041 Caspase 7 Human genes 0.000 claims description 2
- 108090000567 Caspase 7 Proteins 0.000 claims description 2
- 230000034994 death Effects 0.000 claims description 2
- 239000007850 fluorescent dye Substances 0.000 claims description 2
- 125000000565 sulfonamide group Chemical group 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 2
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 210000004100 adrenal gland Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000000481 breast Anatomy 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15106409P | 2009-02-09 | 2009-02-09 | |
| US61/151,064 | 2009-02-09 | ||
| PCT/US2010/023543 WO2010091382A1 (en) | 2009-02-09 | 2010-02-09 | Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014224365A Division JP2015025021A (ja) | 2009-02-09 | 2014-11-04 | 個別化された抗癌薬としてのプロカスパーゼ活性化化合物の設計、合成および評価 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012517442A JP2012517442A (ja) | 2012-08-02 |
| JP2012517442A5 true JP2012517442A5 (https=) | 2013-03-14 |
| JP5896746B2 JP5896746B2 (ja) | 2016-03-30 |
Family
ID=42542422
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011549318A Active JP5896746B2 (ja) | 2009-02-09 | 2010-02-09 | 個別化された抗癌薬としてのプロカスパーゼ活性化化合物の設計、合成および評価 |
| JP2014224365A Pending JP2015025021A (ja) | 2009-02-09 | 2014-11-04 | 個別化された抗癌薬としてのプロカスパーゼ活性化化合物の設計、合成および評価 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014224365A Pending JP2015025021A (ja) | 2009-02-09 | 2014-11-04 | 個別化された抗癌薬としてのプロカスパーゼ活性化化合物の設計、合成および評価 |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US8778945B2 (https=) |
| EP (1) | EP2393794B1 (https=) |
| JP (2) | JP5896746B2 (https=) |
| CN (2) | CN106946812B (https=) |
| AU (1) | AU2010210403B2 (https=) |
| BR (1) | BRPI1008651B1 (https=) |
| CA (1) | CA2751987C (https=) |
| WO (1) | WO2010091382A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008134474A2 (en) | 2007-04-27 | 2008-11-06 | The Board Of Trustees Of The University Of Illinois | Compositions and methods including cell death inducers and procaspase activation |
| US8778945B2 (en) | 2009-02-09 | 2014-07-15 | The Board Of Trustees Of The University Of Illinois | Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs |
| US8916705B2 (en) | 2011-10-14 | 2014-12-23 | The Board of Trustees of The University of Illilnois | Procaspase-activating compounds and compositions |
| AU2013225682B2 (en) | 2012-03-02 | 2016-04-14 | The Board Of Trustees Of The University Of Illinois | Potent anticancer activity via dual compound activation |
| AU2013230985B2 (en) | 2012-03-06 | 2016-05-12 | The Board Of Trustees Of The University Of Illinois | Procaspase combination therapy for glioblastoma |
| CA2866021C (en) | 2012-03-06 | 2020-09-22 | The Board Of Trustees Of The University Of Illinois | Procaspace 3 activation by pac-1 combination therapy |
| US9249116B2 (en) | 2012-08-03 | 2016-02-02 | The Board Of Trustees Of The University Of Illinois | Enzyme-activating compounds and compositions |
| US10155936B2 (en) | 2014-12-05 | 2018-12-18 | An2H Discovery Limited | Parkin ligase activation methods and compositions |
| IL256111B2 (en) * | 2015-06-05 | 2023-09-01 | Univ Illinois | Treatment of pac combinations |
| JP6538976B2 (ja) * | 2015-07-23 | 2019-07-03 | ワン，チミン | 化合物ｐａｃ−１またはその塩及びそれらを含有する医薬組成物 |
| US10308617B2 (en) | 2016-06-03 | 2019-06-04 | An2H Discovery Limited | Triazole benzamide derivatives and the compositions and methods of treatment regarding the same |
| AU2018368453B2 (en) | 2017-11-17 | 2024-05-30 | The Board Of Trustees Of The University Of Illinois | Cancer therapy by degrading dual MEK signaling |
| US10889553B2 (en) | 2017-12-01 | 2021-01-12 | Nysnobio Ireland Dac | Asymmetric triazole benzamide derivatives and the compositions and methods of treatment regarding the same |
| CA3114385A1 (en) | 2018-10-05 | 2020-04-09 | The Board Of Trustees Of The University Of Illinois | Combination therapy for the treatment of uveal melanoma |
| CN117886779A (zh) * | 2023-12-21 | 2024-04-16 | 徐州医科大学 | 一种具有手性羟基的哌嗪醇类化合物及其制备方法和医药用途 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1263001B (de) | 1965-07-12 | 1968-03-14 | Dr Miltiadis Ioannu Hiopulos | Verfahren zur Herstellung von 1, 1-Bis-(p-hydroxyphenyl)-alkan-1-phosphonsaeure-diestern |
| US3847866A (en) | 1965-07-12 | 1974-11-12 | H Bredereck | Bis-(p-hydroxyphenyl)alkylphosphonic acid esters |
| US3879498A (en) | 1971-08-31 | 1975-04-22 | Miltiadis I Iliopulos | Dialkyl 1-acryloyloxy-2-alkenyl-1-phosphonates and dialkyl 1-methacryloxy-2-alkenyl-1-phosphonates |
| DE3222571A1 (de) | 1982-06-16 | 1983-12-22 | Röhm GmbH, 6100 Darmstadt | Phosphorhaltige polyarylenester und verfahren zu ihrer herstellung |
| US5569673A (en) | 1994-05-24 | 1996-10-29 | Purdue Research Foundation | Capsacinoid compounds as proliferation inhibitors |
| EP0888458A4 (en) | 1996-02-20 | 2004-05-06 | Sloan Kettering Institutefor C | COMBINATION OF PKC INHIBITORS AND THERAPEUTIC AGENTS FOR TREATING CANCER |
| US6558900B2 (en) | 1996-07-12 | 2003-05-06 | Emory University | Regulation of apoptosis and in vitro model for studies thereof |
| EP1080233A4 (en) | 1998-05-18 | 2003-02-05 | Apoptosis Technology Inc | COMPOUNDS, SCREENING METHODS, AND USES USING ANTI-APOPTIC GENES AND GENE PRODUCTS |
| US6403765B1 (en) | 1998-06-16 | 2002-06-11 | Thomas Jefferson University | Truncated Apaf-1 and methods of use thereof |
| EP1100932A2 (en) | 1998-07-27 | 2001-05-23 | PHARMACIA & UPJOHN COMPANY | Method for autoactivation of procaspase 8 |
| CA2342325A1 (en) | 1998-08-31 | 2000-03-09 | Kyowa Hakko Kogyo Co., Ltd. | An agent for inducing apoptosis |
| KR100818845B1 (ko) | 1998-09-09 | 2008-04-01 | 메타베이시스 테라퓨틱스, 인크. | 신규한 프럭토스 1,6-비스포스파타제의 헤테로방향족 억제제 |
| US6110691A (en) | 2000-01-06 | 2000-08-29 | Board Of Regents, The University Of Texas System | Activators of caspases |
| US6605589B1 (en) | 2000-03-31 | 2003-08-12 | Parker Hughes Institute | Cathepsin inhibitors in cancer treatment |
| US6608026B1 (en) | 2000-08-23 | 2003-08-19 | Board Of Regents, The University Of Texas System | Apoptotic compounds |
| WO2002048329A2 (en) | 2000-11-20 | 2002-06-20 | Idun Pharmaceuticals, Inc. | Membrane derived caspase-3, compositions comprising the same and methods of use therefor |
| CA2438932A1 (en) | 2001-02-21 | 2002-09-06 | Rutgers, The State University Of New Jersey | Compositions and methods for cancer prevention and treatment derived from inula britannica |
| KR100439425B1 (ko) | 2001-03-22 | 2004-07-05 | (주)바이오케어 | 잔토리졸을 포함하는 조성물 및 그 용도 |
| WO2003024955A2 (en) | 2001-09-18 | 2003-03-27 | Sunesis Pharmaceuticals, Inc. | Small molecule inhibitors of caspases |
| CA2468745A1 (en) | 2001-11-30 | 2003-06-12 | The Burnham Institute | Induction of apoptosis in cancer cells |
| US20030148966A1 (en) | 2002-01-30 | 2003-08-07 | Hiremagalur Jayaram | Method and composition for inducing apoptosis in cells |
| WO2004066958A2 (en) | 2003-01-30 | 2004-08-12 | The Trustees Of Princeton University | Caspase-9:bir3 domain of xiap complexes and methods of use |
| US7632972B2 (en) | 2003-10-30 | 2009-12-15 | The Board Of Trustees Of The University Of Illionis | Compounds and methods for treatment of cancer and modulation of programmed cell death for melanoma and other cancer cells |
| WO2005090370A1 (en) | 2004-02-05 | 2005-09-29 | The Regents Of The University Of California | Pharmacologically active agents containing esterified phosphonates and methods for use thereof |
| US20070049602A1 (en) * | 2005-05-26 | 2007-03-01 | The Board Of Trustees Of The University Of Illinois | Selective Apoptotic Induction in Cancer Cells Including Activation of Procaspase-3 |
| WO2008134474A2 (en) * | 2007-04-27 | 2008-11-06 | The Board Of Trustees Of The University Of Illinois | Compositions and methods including cell death inducers and procaspase activation |
| CN101184491A (zh) * | 2005-05-26 | 2008-05-21 | 伊利诺伊大学评议会 | 包括活化半胱天冬酶-3酶原的癌细胞内选择性细胞凋亡诱导 |
| WO2007008529A2 (en) | 2005-07-08 | 2007-01-18 | Kalypsys, Inc | Celullar cholesterol absorption modifiers |
| GB0523609D0 (en) * | 2005-11-19 | 2005-12-28 | Vernalis R&D Ltd | Piperazine derivatives |
| KR100848601B1 (ko) * | 2007-03-06 | 2008-07-28 | 한국과학기술연구원 | 알카노일 피페라진 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 신경성 통증의 예방 및 치료용 약학적 조성물 |
| US8778945B2 (en) | 2009-02-09 | 2014-07-15 | The Board Of Trustees Of The University Of Illinois | Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs |
-
2010
- 2010-02-09 US US13/148,350 patent/US8778945B2/en active Active
- 2010-02-09 JP JP2011549318A patent/JP5896746B2/ja active Active
- 2010-02-09 CN CN201610922720.2A patent/CN106946812B/zh active Active
- 2010-02-09 CA CA2751987A patent/CA2751987C/en active Active
- 2010-02-09 AU AU2010210403A patent/AU2010210403B2/en active Active
- 2010-02-09 WO PCT/US2010/023543 patent/WO2010091382A1/en not_active Ceased
- 2010-02-09 EP EP10739254.0A patent/EP2393794B1/en active Active
- 2010-02-09 CN CN2010800160157A patent/CN102438998A/zh active Pending
- 2010-02-09 BR BRPI1008651A patent/BRPI1008651B1/pt active IP Right Grant
-
2014
- 2014-07-01 US US14/321,514 patent/US9102661B2/en active Active
- 2014-11-04 JP JP2014224365A patent/JP2015025021A/ja active Pending
-
2015
- 2015-08-10 US US14/822,830 patent/US9643960B2/en active Active
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