EP1351691A4 - Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof - Google Patents

Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof

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
inducers
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Withdrawn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Withdrawn legal-status Critical Current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
EP01990048A 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 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 analogs as activators of caspases and inducers of apoptosis and the use thereof

Country Status (3)

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

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US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2001292670A1 (en) 2000-09-15 2002-03-26 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
BR0116411A (en) 2000-12-21 2003-11-11 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
EP1575506A4 (en) * 2002-07-25 2008-04-23 Scios Inc Methods for improvement of lung function using tgf-beta inhibitors
BR0313176A (en) 2002-08-02 2005-06-14 Vertex Pharma Pyrazole compositions useful as gsk-3 inhibitors
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2003272324A1 (en) * 2002-09-10 2004-04-30 Scios Inc. INHIBITORS OF TFGBeta
US20050014753A1 (en) * 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
EP1610774A4 (en) * 2003-04-09 2008-07-16 Exelixis Inc Tie-2 modulators and methods of use
WO2005003100A2 (en) 2003-07-03 2005-01-13 Myriad Genetics, 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
CN102358738A (en) 2003-07-30 2012-02-22 里格尔药品股份有限公司 2,4-pyrimidinediamine compounds and uses of treating or preventing autoimmune diseases thereof
US6818631B1 (en) 2003-08-15 2004-11-16 Nippon Soda Co. Ltd. Fungicidal pyrimidine derivatives
BRPI0415678A (en) * 2003-10-23 2006-12-19 Pharmacia Corp pyrimidine compounds for treating inflammation
US8455489B2 (en) 2003-11-10 2013-06-04 Exelixis, Inc. Substituted pyrimidine compositions and methods of use
KR101206843B1 (en) 2003-12-03 2012-11-30 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 Tubulin inhibitors
CA2551944A1 (en) * 2003-12-15 2005-06-30 Almirall Prodesfarma Ag 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists
AU2005232745A1 (en) 2004-04-13 2005-10-27 Astellas Pharma 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
JP4990766B2 (en) * 2004-07-01 2012-08-01 シンタ ファーマシューティカルズ コーポレーション Disubstituted heteroaryl compounds
ES2352748T3 (en) 2004-09-06 2011-02-22 Basilea Pharmaceutica Ag PHENYLAMINOPIRIDINS AND PHENYLAMINOPIRACINES.
AU2005286593A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyridine compounds, process for their preparation and compositions containing them
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
BRPI0606930A2 (en) * 2005-01-25 2009-12-01 Astrazeneca Ab compound or a pharmaceutically acceptable salt thereof, process for preparing a compound or a pharmaceutically acceptable salt thereof, pharmaceutical composition, use of a compound or a pharmaceutically acceptable salt thereof, and methods for producing a drug inhibiting effect. b-raf in a warm-blooded animal, for producing an anti-cancer effect on a warm-blooded animal and for treating diseases of an animal in a warm-blooded animal
EP1888565B1 (en) * 2005-04-11 2011-03-23 Almirall, S.A. 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
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
JP4960450B2 (en) 2006-07-14 2012-06-27 ノバルティス アーゲー Pyrimidine derivatives as ALK-5 inhibitors
EP1878733A1 (en) * 2006-07-14 2008-01-16 Novartis AG Pyrimidine derivatives as ALK-5 inhibitors
JP2010502674A (en) * 2006-09-07 2010-01-28 ノイロサーチ アクティーゼルスカブ Pyridinyl-pyrimidine derivatives useful as potassium channel modulators
CN104327084B (en) 2007-11-28 2017-06-06 达那-法伯癌症研究所 The small molecule myristate inhibitors and its application method of BCR ABL
EP2649053B1 (en) * 2010-12-06 2015-11-04 Glaxo Group Limited Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by lp-pla2
JP2013544854A (en) * 2010-12-06 2013-12-19 グラクソ グループ リミテッド Compound
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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
EP2875015A1 (en) * 2012-07-23 2015-05-27 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
CN104918919A (en) * 2012-11-21 2015-09-16 Ptc医疗公司 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
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See also references of WO0247690A1 *

Also Published As

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

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