EP1351691A4 - SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND THEIR ANALOGS AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCTORS, AND THEIR USE - Google Patents

SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND THEIR ANALOGS AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCTORS, AND THEIR USE

Info

Publication number
EP1351691A4
EP1351691A4 EP01990048A EP01990048A EP1351691A4 EP 1351691 A4 EP1351691 A4 EP 1351691A4 EP 01990048 A EP01990048 A EP 01990048A EP 01990048 A EP01990048 A EP 01990048A EP 1351691 A4 EP1351691 A4 EP 1351691A4
Authority
EP
European Patent Office
Prior art keywords
arylaminopyrimidines
caspases
inductors
activators
apoptosis
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.)
Withdrawn
Application number
EP01990048A
Other languages
German (de)
French (fr)
Other versions
EP1351691A1 (en
Inventor
Sui Xiong Cai
John A Drewe
Bao Nguyen
P Sanjeeva Reddy
Azra Pervin
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.)
Cytovia Therapeutics LLC
Original Assignee
Cytovia Inc
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 Cytovia Inc filed Critical Cytovia Inc
Publication of EP1351691A1 publication Critical patent/EP1351691A1/en
Publication of EP1351691A4 publication Critical patent/EP1351691A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP01990048A 2000-12-12 2001-12-12 SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND THEIR ANALOGS AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCTORS, AND THEIR USE Withdrawn EP1351691A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25458100P 2000-12-12 2000-12-12
US254581P 2000-12-12
PCT/US2001/047498 WO2002047690A1 (en) 2000-12-12 2001-12-12 Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof

Publications (2)

Publication Number Publication Date
EP1351691A1 EP1351691A1 (en) 2003-10-15
EP1351691A4 true EP1351691A4 (en) 2005-06-22

Family

ID=22964830

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01990048A Withdrawn EP1351691A4 (en) 2000-12-12 2001-12-12 SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND THEIR ANALOGS AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCTORS, AND THEIR USE

Country Status (3)

Country Link
EP (1) EP1351691A4 (en)
AU (1) AU2002228922A1 (en)
WO (1) WO2002047690A1 (en)

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WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6716851B2 (en) 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
EP1575506A4 (en) * 2002-07-25 2008-04-23 Scios Inc Methods for improvement of lung function using tgf-beta inhibitors
CN1319968C (en) 2002-08-02 2007-06-06 沃泰克斯药物股份有限公司 Pyrazole compositions useful as inhibitors of GSK-3
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
BR0314196A (en) * 2002-09-10 2005-07-26 Scios Inc Tgf-beta inhibitors
US20050014753A1 (en) * 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
JP4895806B2 (en) * 2003-04-09 2012-03-14 エクセリクシス， インク． TIE-2 modulator and usage
AU2004253967B2 (en) 2003-07-03 2010-02-18 Cytovia, Inc. 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US6818631B1 (en) 2003-08-15 2004-11-16 Nippon Soda Co. Ltd. Fungicidal pyrimidine derivatives
EP1678146A1 (en) * 2003-10-23 2006-07-12 Pharmacia Corporation Pyrimidine compounds for the treatment of inflammation
US8455489B2 (en) 2003-11-10 2013-06-04 Exelixis, Inc. Substituted pyrimidine compositions and methods of use
CA2545422C (en) 2003-12-03 2015-06-02 Cytopia Research Pty Ltd Tubulin inhibitors
CA2551944A1 (en) * 2003-12-15 2005-06-30 Almirall Prodesfarma Ag 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists
CA2561895A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyrimidines as potassium ion channel modulators
JP4602686B2 (en) * 2004-04-15 2010-12-22 広栄化学工業株式会社 Process for producing 2,6-dihalogeno-4-arylpyridines
WO2006007532A2 (en) * 2004-07-01 2006-01-19 Synta Pharmaceuticals Corp. 2-substituted heteroaryl compounds
WO2006027348A1 (en) * 2004-09-06 2006-03-16 Basilea Pharmaceutica Ag Phenylaminopyridines
CA2581454A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
CN101146789A (en) * 2005-01-25 2008-03-19 阿斯利康(瑞典)有限公司 compound
DE602006020864D1 (en) * 2005-04-11 2011-05-05 Almirall Sa 2, 6-DI- (HETERO-) ARYL-4-AMIDO-PYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
MX2008005814A (en) 2005-11-03 2008-10-15 Vertex Pharma Aminopyrimidines useful as kinase inhibitors.
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
PL2044056T3 (en) 2006-07-14 2013-01-31 Novartis Ag Pyrimidine derivatives as alk-5 inhibitors
EP1878733A1 (en) * 2006-07-14 2008-01-16 Novartis AG Pyrimidine derivatives as ALK-5 inhibitors
US20110144140A1 (en) * 2006-09-07 2011-06-16 Eriksen Birgitte L Pyridinyl-pyrimidine derivatives useful as potassium channel modulating agents
EA019869B1 (en) * 2007-11-28 2014-06-30 Дана Фарбер Кансер Инститьют, Инк. Small molecule myristate inhibitors of tyrosine kinase bcr-abl and methods of use thereof
JP2013544854A (en) * 2010-12-06 2013-12-19 グラクソ グループ リミテッド Compound
KR101861883B1 (en) * 2010-12-06 2018-05-28 글락소 그룹 리미티드 Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by lp-pla2
CA2840883C (en) 2011-07-07 2019-07-16 Merck Patent Gmbh Substituted azaheterocycles
JP2014237590A (en) * 2011-09-30 2014-12-18 アステラス製薬株式会社 2-(pyridine-2-yl) pyrimidine-4-amine compound or a salt thereof
ES2620316T3 (en) * 2012-05-11 2017-06-28 Bayer Pharma Aktiengesellschaft Cycloalkenopyrazoles substituted as BUB1 inhibitors for cancer treatment
WO2014015936A1 (en) * 2012-07-23 2014-01-30 Merck Patent Gmbh Ligands and their preparation
CN102887860B (en) * 2012-09-29 2015-07-01 上海泰坦科技有限公司 Preparation method of 4-chloro-6-trifluoromethylpyrimidine type compound
NZ746607A (en) * 2012-11-21 2019-11-29 Ptc Therapeutics Inc Substituted reverse pyrimidine bmi-1 inhibitors
CN103896856B (en) * 2012-12-25 2016-06-08 叶龙 A kind of polysubstituted monocycle miazines JNK kinase inhibitor and its production and use
CN108976172B (en) * 2017-05-31 2021-12-07 华东师范大学 4-pyrimidinediamine micromolecule organic compound and derivative and application thereof
CN108715589B (en) * 2018-06-19 2021-04-20 华侨大学 Coumarin derivative used as caspase-3 activator and application thereof
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US4041030A (en) * 1973-09-20 1977-08-09 Delalande S.A. Arylamino pyrimidinic derivatives
EP0629622A1 (en) * 1992-02-28 1994-12-21 Zenyaku Kogyo Kabushikikaisha s-TRIAZINE DERIVATIVE AND REMEDY FOR ESTROGEN-DEPENDENT DISEASES CONTAINING THE SAME AS ACTIVE INGREDIENT
EP0640599A1 (en) * 1993-08-26 1995-03-01 Ono Pharmaceutical Co., Ltd. 4-Aminopyrimidine derivatives
WO1997009315A1 (en) * 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions
US6103737A (en) * 1997-07-03 2000-08-15 Dupont Pharmaceuticals Company Aryl- and arylamino- substituted heterocycles as corticotropin releasing hormone antagonists

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Patent Citations (5)

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US4041030A (en) * 1973-09-20 1977-08-09 Delalande S.A. Arylamino pyrimidinic derivatives
EP0629622A1 (en) * 1992-02-28 1994-12-21 Zenyaku Kogyo Kabushikikaisha s-TRIAZINE DERIVATIVE AND REMEDY FOR ESTROGEN-DEPENDENT DISEASES CONTAINING THE SAME AS ACTIVE INGREDIENT
EP0640599A1 (en) * 1993-08-26 1995-03-01 Ono Pharmaceutical Co., Ltd. 4-Aminopyrimidine derivatives
WO1997009315A1 (en) * 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions
US6103737A (en) * 1997-07-03 2000-08-15 Dupont Pharmaceuticals Company Aryl- and arylamino- substituted heterocycles as corticotropin releasing hormone antagonists

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Title
CHEMICAL ABSTRACTS, vol. 134, 10 May 2001, Columbus, Ohio, US; abstract no. 295842 *
See also references of WO0247690A1 *

Also Published As

Publication number Publication date
AU2002228922A1 (en) 2002-06-24
WO2002047690A1 (en) 2002-06-20
EP1351691A1 (en) 2003-10-15

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