CN106946812B - 作为个性化抗癌药的胱天蛋白酶原活化化合物的设计、合成和评价 - Google Patents

作为个性化抗癌药的胱天蛋白酶原活化化合物的设计、合成和评价 Download PDF

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CN106946812B
CN106946812B CN201610922720.2A CN201610922720A CN106946812B CN 106946812 B CN106946812 B CN 106946812B CN 201610922720 A CN201610922720 A CN 201610922720A CN 106946812 B CN106946812 B CN 106946812B
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cancer
compound
caspase
compounds
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CN106946812A (zh
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P·J·赫根罗特
Q·P·彼得森
D·C·许
D·C·韦斯特
T·M·范
C·J·诺沃特尼
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University of Illinois System
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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CN201610922720.2A 2009-02-09 2010-02-09 作为个性化抗癌药的胱天蛋白酶原活化化合物的设计、合成和评价 Active CN106946812B (zh)

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Families Citing this family (15)

* Cited by examiner, † Cited by third party
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
EP2393794B1 (en) 2009-02-09 2017-03-22 The Board of Trustees of the University of Illionis 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
EP2819661B1 (en) 2012-03-02 2016-11-09 The Board of Trustees of the University of Illionis 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
ES2774930T3 (es) 2012-03-06 2020-07-23 Univ Illinois Activación de procaspasa 3 mediante terapia de combinación
KR102157912B1 (ko) 2012-08-03 2020-09-21 더 보드 오브 트러스티즈 오브 더 유니버시티 오브 일리노이 효소-활성화 화합물 및 조성물
KR20170092634A (ko) 2014-12-05 2017-08-11 에이엔2에이치 디스커버리 리미티드 파킨 리가제 활성화 방법 및 조성물
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
WO2017210694A1 (en) 2016-06-03 2017-12-07 An2H Discovery Limited Triazole benzamide derivatives and the compositions and methods of treatment regarding the same
SG11202004384YA (en) 2017-11-17 2020-06-29 Univ 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
WO2020072774A1 (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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3847866A (en) 1965-07-12 1974-11-12 H Bredereck Bis-(p-hydroxyphenyl)alkylphosphonic acid esters
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
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
CA2246734A1 (en) 1996-02-20 1997-08-21 Sloan-Kettering Institute For Cancer Research Combinations of pkc inhibitors and therapeutic agents for treating cancers
US6558900B2 (en) 1996-07-12 2003-05-06 Emory University Regulation of apoptosis and in vitro model for studies thereof
AU762756B2 (en) 1998-05-18 2003-07-03 Apoptosis Technology, Inc. Compounds, screening methods, and uses involving anti-apoptotic genes and gene products
US6403765B1 (en) 1998-06-16 2002-06-11 Thomas Jefferson University Truncated Apaf-1 and methods of use thereof
WO2000006750A2 (en) 1998-07-27 2000-02-10 Pharmacia & Upjohn Company Method for autoactivation of procaspase 8
AU5446499A (en) 1998-08-31 2000-03-21 Kyowa Hakko Kogyo Co. Ltd. Apoptosis inducing agents
DE69910045T2 (de) 1998-09-09 2004-04-22 Metabasis Therapeutics Inc., San Diego Neue heteroaromatische fructose 1,6-bisphosphatase inhibitoren
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
US6627623B2 (en) 2001-02-21 2003-09-30 Rutgers, The State University Inducing cell apoptosis and treating cancer using 1-O-acetylbritannilactone or 1,6-O,O-diacetylbritannilactone
KR100439425B1 (ko) 2001-03-22 2004-07-05 (주)바이오케어 잔토리졸을 포함하는 조성물 및 그 용도
US6878743B2 (en) 2001-09-18 2005-04-12 Sunesis Pharmaceuticals, Inc. Small molecule inhibitors of caspases
US7053071B2 (en) 2001-11-30 2006-05-30 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
US20040180828A1 (en) 2003-01-30 2004-09-16 Yigong Shi Caspase-9 : BIR 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
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
EP2393794B1 (en) 2009-02-09 2017-03-22 The Board of Trustees of the University of Illionis Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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