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

Info

Publication number
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
Authority
CN
China
Prior art keywords
pac
cancer
compound
caspase
compounds
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.)
Active
Application number
CN201610922720.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN106946812A (zh
Inventor
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Illinois System
Original Assignee
University of Illinois System
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by University of Illinois System filed Critical University of Illinois System
Publication of CN106946812A publication Critical patent/CN106946812A/zh
Application granted granted Critical
Publication of CN106946812B publication Critical patent/CN106946812B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • 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
    • C07D295/145—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K11/00—Luminescent, e.g. electroluminescent, chemiluminescent materials
    • C09K11/06—Luminescent, e.g. electroluminescent, chemiluminescent materials containing organic luminescent materials
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K2211/00—Chemical nature of organic luminescent or tenebrescent compounds
    • C09K2211/10—Non-macromolecular compounds
    • C09K2211/1018—Heterocyclic compounds
    • C09K2211/1025—Heterocyclic compounds characterised by ligands
    • C09K2211/1044—Heterocyclic compounds characterised by ligands containing two nitrogen atoms as heteroatoms
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K2211/00—Chemical nature of organic luminescent or tenebrescent compounds
    • C09K2211/10—Non-macromolecular compounds
    • C09K2211/1018—Heterocyclic compounds
    • C09K2211/1025—Heterocyclic compounds characterised by ligands
    • C09K2211/1059—Heterocyclic compounds characterised by ligands containing three nitrogen atoms as heteroatoms
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K2211/00—Chemical nature of organic luminescent or tenebrescent compounds
    • C09K2211/10—Non-macromolecular compounds
    • C09K2211/1018—Heterocyclic compounds
    • C09K2211/1025—Heterocyclic compounds characterised by ligands
    • C09K2211/1088—Heterocyclic compounds characterised by ligands containing oxygen as the only heteroatom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Materials Engineering (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
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)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15106409P 2009-02-09 2009-02-09
US61/151,064 2009-02-09
CN2010800160157A CN102438998A (zh) 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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2010800160157A Division CN102438998A (zh) 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

Publications (2)

Publication Number Publication Date
CN106946812A CN106946812A (zh) 2017-07-14
CN106946812B true CN106946812B (zh) 2020-10-09

Family

ID=42542422

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201610922720.2A Active CN106946812B (zh) 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
CN2010800160157A Pending CN102438998A (zh) 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

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2010800160157A Pending CN102438998A (zh) 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

Country Status (8)

Country Link
US (3) US8778945B2 (OSRAM)
EP (1) EP2393794B1 (OSRAM)
JP (2) JP5896746B2 (OSRAM)
CN (2) CN106946812B (OSRAM)
AU (1) AU2010210403B2 (OSRAM)
BR (1) BRPI1008651B1 (OSRAM)
CA (1) CA2751987C (OSRAM)
WO (1) WO2010091382A1 (OSRAM)

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
CA2865983C (en) 2012-03-02 2021-10-19 The Board Of Trustees Of The University Of Illinois Potent anticancer activity via dual compound activation
DK2822558T3 (da) 2012-03-06 2020-03-23 The Board Of Trustees Of The Univ Of Illionis Procaspase 3 aktivering ved hjælp af kombinations terapi
EP3290035B1 (en) 2012-03-06 2019-05-15 The Board of Trustees of the University of Illinois Procaspase combination therapy for treating cancer
BR112015002357B1 (pt) * 2012-08-03 2022-03-15 The Board Of Trustees Of The University Of Illinois Compostos e composições ativadores de enzimas
AU2015357487A1 (en) 2014-12-05 2017-06-08 An2H Discovery Limited Parkin ligase activation methods and compositions
BR112017026140A2 (pt) 2015-06-05 2018-08-14 The Board Of Trustees Of The University Of Illinois método para inibir o crescimento ou a proliferação de células cancerígenas, método para induzir apoptose em célula cancerígena, método para tratar câncer, composição e seu uso
WO2017012113A1 (zh) * 2015-07-23 2017-01-26 王智民 化合物pac-1或其盐及包含它们的药物组合物
CN109922802A (zh) 2016-06-03 2019-06-21 An2H探索有限公司 三唑苯甲酰胺衍生物及其相关组合物和治疗方法
CN111491927A (zh) 2017-11-17 2020-08-04 伊利诺伊大学董事会 通过降解双mek信号传导的癌症疗法
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
MX2021003490A (es) 2018-10-05 2021-06-18 Univ Illinois Terapia combinada para el tratamiento de melanoma uveal.
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
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
AU2195297A (en) 1996-02-20 1997-09-02 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
WO1999060171A1 (en) 1998-05-18 1999-11-25 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
JP2002522032A (ja) 1998-07-27 2002-07-23 ファルマシア・アンド・アップジョン・カンパニー プロカスパーゼ８の自己活性化方法
EP1110960A4 (en) 1998-08-31 2001-12-12 Kyowa Hakko Kogyo Kk Apoptosis inducing agents
HK1042496B (zh) 1998-09-09 2006-01-27 症变治疗公司 新的果糖1，6-二磷酸酶的杂芳族抑制剂
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
AU2002346620A1 (en) 2001-11-30 2003-06-17 Department Of Veteran Affairs 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

Also Published As

Publication number Publication date
EP2393794B1 (en) 2017-03-22
CN102438998A (zh) 2012-05-02
US20150344452A1 (en) 2015-12-03
JP5896746B2 (ja) 2016-03-30
US20140315915A1 (en) 2014-10-23
BRPI1008651B1 (pt) 2020-01-21
CA2751987A1 (en) 2010-08-12
EP2393794A1 (en) 2011-12-14
CN106946812A (zh) 2017-07-14
US8778945B2 (en) 2014-07-15
US9643960B2 (en) 2017-05-09
CA2751987C (en) 2017-11-28
BRPI1008651A2 (pt) 2016-03-08
US20120040995A1 (en) 2012-02-16
EP2393794A4 (en) 2012-10-31
AU2010210403B2 (en) 2016-07-28
JP2015025021A (ja) 2015-02-05
AU2010210403A1 (en) 2011-09-01
US9102661B2 (en) 2015-08-11
WO2010091382A1 (en) 2010-08-12
JP2012517442A (ja) 2012-08-02

Similar Documents

Publication Publication Date Title
CN106946812B (zh) 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
Sheppard et al. Discovery of N-Ethyl-4-[2-(4-fluoro-2, 6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl) phenyl]-6-methyl-7-oxo-1 H-pyrrolo [2, 3-c] pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
JP6399660B2 (ja) 癌治療用組成物および方法
von Nussbaum et al. Freezing the bioactive conformation to boost potency: The identification of BAY 85‐8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases
AU2013296187B2 (en) Enzyme-activating compounds and compositions
Mitrović et al. Organoruthenated nitroxoline derivatives impair tumor cell invasion through inhibition of cathepsin B activity
AU2012322660B2 (en) Pyrazol-3-ones that activate pro-apoptotic BAX
US20210024464A1 (en) Binding function 3 (bf3) site compounds as therapeutics and methods for their use
WO2008134474A2 (en) Compositions and methods including cell death inducers and procaspase activation
JP2018508563A (ja) Ｕｓｐ７阻害剤化合物及び使用方法
Mohassab et al. Design and synthesis of new quinoline-ester/-amide derivatives as potent antiproliferative agent targeting EGFR and BRAFV600E kinases
EP3568391B1 (en) Benzene disulfonamide for the treatment of cancer
Bannister et al. ML311: a small molecule that potently and selectively disrupts the protein-protein interaction of Mcl-1 and Bim: a probe for studying lymphoid tumorigenesis
EP4393908A1 (en) Bis-pyrazolyl-methane compounds affecting kras
Lee et al. A structure− activity relationship study of novel hydroxamic acid inhibitors around the S1 Subsite of Human Aminopeptidase N
Kungyal et al. Computational, In Vitro and In Vivo Studies to Evaluate Anti-Cancer Activity of Benzisothiazole Derivative
Miller Multifunctional ligand design for modulating protein stability and aggregation for cancer treatment
Zoppi Studies on Proteolysis Targeting Chimeras: platform technology for targeted protein degradation in drug discovery
Schenone et al. Synthesis of 6-Ethoxyphenyl-4-Fluorobenzenesulfonate-Tagged Thiosemicarbazones as Carbonic Anhydrase Inhibitors: In-Vitro and in Silico Approaches
Ghith Design, synthesis and molecular modeling study of iminodiacetyl monohydroxamic acid derivatives as MMP inhibitors
Matthews Synthesis and biological evaluation of plasminogen activation inhibitors as antitumour/antimetastasis agents
Roth Improving the process synthesis, potency, and pharmacokinetics of the anticancer compound PAC-1
MXPA00003589A (en) 2-pyridinylguanidine urokinase inhibitors

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant