TWI369351B - 2,4-diamino-pyrimidines as aurora inhibitors - Google Patents

2,4-diamino-pyrimidines as aurora inhibitors

Info

Publication number
TWI369351B
TWI369351B TW095123919A TW95123919A TWI369351B TW I369351 B TWI369351 B TW I369351B TW 095123919 A TW095123919 A TW 095123919A TW 95123919 A TW95123919 A TW 95123919A TW I369351 B TWI369351 B TW I369351B
Authority
TW
Taiwan
Prior art keywords
pyrimidines
diamino
aurora inhibitors
aurora
inhibitors
Prior art date
Application number
TW095123919A
Other languages
English (en)
Other versions
TW200726753A (en
Inventor
Stephan Karl Zahn
Guido Boehmelt
Andreas Mantoulidis
Ulrich Reiser
Matthias Treu
Ulrich Guertler
Andreas Schoop
Flavio Solca
Ulrike Tontsch-Grunt
Ralph Brueckner
Charlotte Reither
Lars Herfurth
Oliver Kraemer
Heinz Stadtmueller
Harald Engelhardt
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of TW200726753A publication Critical patent/TW200726753A/zh
Application granted granted Critical
Publication of TWI369351B publication Critical patent/TWI369351B/zh

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
TW095123919A 2005-07-01 2006-06-30 2,4-diamino-pyrimidines as aurora inhibitors TWI369351B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05106007 2005-07-01

Publications (2)

Publication Number Publication Date
TW200726753A TW200726753A (en) 2007-07-16
TWI369351B true TWI369351B (en) 2012-08-01

Family

ID=35431858

Family Applications (1)

Application Number Title Priority Date Filing Date
TW095123919A TWI369351B (en) 2005-07-01 2006-06-30 2,4-diamino-pyrimidines as aurora inhibitors

Country Status (30)

Country Link
US (3) US20070032514A1 (zh)
EP (1) EP1902037B1 (zh)
JP (1) JP5179357B2 (zh)
KR (1) KR20080031362A (zh)
CN (1) CN101213179A (zh)
AR (1) AR057423A1 (zh)
AT (1) ATE441639T1 (zh)
AU (1) AU2006264958B2 (zh)
BR (1) BRPI0613096A2 (zh)
CA (1) CA2613664A1 (zh)
CY (1) CY1109644T1 (zh)
DE (1) DE502006004750D1 (zh)
DK (1) DK1902037T3 (zh)
EA (1) EA016358B1 (zh)
EC (1) ECSP078060A (zh)
ES (1) ES2330045T3 (zh)
IL (1) IL188452A (zh)
MX (1) MX2007015992A (zh)
MY (1) MY142496A (zh)
NO (1) NO20076059L (zh)
NZ (1) NZ565475A (zh)
PE (1) PE20070121A1 (zh)
PL (1) PL1902037T3 (zh)
PT (1) PT1902037E (zh)
SI (1) SI1902037T1 (zh)
TW (1) TWI369351B (zh)
UA (1) UA92355C2 (zh)
UY (1) UY29636A1 (zh)
WO (1) WO2007003596A1 (zh)
ZA (1) ZA200709763B (zh)

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GB2420559B (en) * 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
PE20080068A1 (es) * 2006-05-15 2008-03-17 Boehringer Ingelheim Int Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
US20100144706A1 (en) * 2006-12-22 2010-06-10 Boehringer Ingelheim International Gmbh Compounds
US20100056524A1 (en) * 2008-04-02 2010-03-04 Mciver Edward Giles Compound
LT2300013T (lt) 2008-05-21 2017-12-27 Ariad Pharmaceuticals, Inc. Fosforo dariniai kaip kinazių inhibitoriai
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
WO2010022125A1 (en) * 2008-08-20 2010-02-25 Schering Corporation Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
ES2439009T3 (es) 2008-08-20 2014-01-21 Merck Sharp & Dohme Corp. Derivados de piridina y pirimidina sustituidos con etenilo y su uso en el tratamiento de infecciones virales
CA2734486A1 (en) * 2008-08-20 2010-02-25 Southern Research Institute Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
TW201019939A (en) 2008-08-20 2010-06-01 Schering Corp Azo-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
EP2161259A1 (de) 2008-09-03 2010-03-10 Bayer CropScience AG 4-Halogenalkylsubstituierte Diaminopyrimidine als Fungizide
CN102143750B (zh) * 2008-09-08 2014-04-02 默克专利有限公司 用作蛋白激酶抑制剂的大环嘧啶
AR074210A1 (es) 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina como inhibidores de ptk2-quinasa
TW201024281A (en) 2008-11-24 2010-07-01 Boehringer Ingelheim Int New compounds
US20110071158A1 (en) * 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
US8410126B2 (en) * 2009-05-29 2013-04-02 Boehringer Ingelheim International Gmbh Pyrimidine inhibitors of PKTK2
CA2764983A1 (en) 2009-06-10 2010-12-16 Abbott Laboratories 2- ( lh-pyrazol-4 -ylamino ) -pyrimidine as kinase inhibitors
JP2012197231A (ja) * 2009-08-06 2012-10-18 Oncotherapy Science Ltd Ttk阻害作用を有するピリジンおよびピリミジン誘導体
JP5539518B2 (ja) 2009-08-14 2014-07-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 2−アミノ−5−トリフルオロメチルピリミジン誘導体の位置選択的調製
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
US8466155B2 (en) * 2009-10-02 2013-06-18 Boehringer Ingelheim International Gmbh Pyrimidines
US20120107304A1 (en) 2010-04-27 2012-05-03 Boehringer Ingelheim International Gmbh Combination therapy in treatment of oncological and fibrotic diseases
MX2012014158A (es) 2010-06-04 2013-02-07 Hoffmann La Roche Derivados de aminopirimidina como moduladores de proteina cinasa rica repeticiones leucina 2 (lrrk2).
HUE037844T2 (hu) 2010-11-10 2018-09-28 Genentech Inc Pirazol-aminopirimidin-származékok mint LRRK2 modulátorok
BR112013019942B1 (pt) * 2011-02-25 2022-01-11 Yuhan Corporation Uso de composto ou de seu sal farmaceuticamente aceitável, composição farmacêutica, compostos ou seus sais farmaceuticamente aceitáveis e respectivos processos de preparação
WO2012151561A1 (en) 2011-05-04 2012-11-08 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Egfr発動性がんの細胞増殖阻害用化合物
WO2014151871A2 (en) 2013-03-14 2014-09-25 Tolero Pharmaceuticals, Inc. Jak2 and alk2 inhibitors and methods for their use
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
CA2934061A1 (en) * 2013-12-20 2015-06-25 Signal Pharmaceuticals, Llc Substituted diaminopyrimidyl compounds, compositions thereof, and methods of treatment therewith
JP6637880B2 (ja) 2014-05-08 2020-01-29 東ソー・ファインケム株式会社 5−(トリフルオロメチル)ピリミジン誘導体及びその製造方法
ES2940911T3 (es) * 2016-06-27 2023-05-12 Rigel Pharmaceuticals Inc Compuestos de 2,4-diamino-pirimidina y su uso como inhibidores de IRAK4
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MXPA03010810A (es) * 2001-05-29 2004-03-22 Schering Ag Pirimidinas inhibidoras de cdk, su obtencion y su uso como medicamentos.
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IL166241A (en) * 2002-07-29 2011-12-29 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds for use in the treatment of autoimmune diseases
UA80767C2 (en) * 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
JP2007514775A (ja) * 2003-12-19 2007-06-07 ライジェル ファーマシューティカルズ, インコーポレイテッド 1−(2,4−ピリミジンジアミノ)−2−シクロペンタンカルボキサイミド合成中間体の立体異性体および立体異性体混合物
CN1976905A (zh) * 2004-03-30 2007-06-06 大正制药株式会社 嘧啶衍生物以及与其应用有关的治疗方法
KR100886990B1 (ko) * 2004-05-14 2009-03-04 화이자 프로덕츠 인크. 비정상적인 세포성장의 치료를 위한 피리미딘 유도체
JP4812763B2 (ja) * 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ, インコーポレイテッド シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
GB2420559B (en) * 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
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CA2634646C (en) * 2005-12-21 2012-04-10 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth

Also Published As

Publication number Publication date
IL188452A (en) 2012-02-29
EP1902037B1 (de) 2009-09-02
WO2007003596A1 (de) 2007-01-11
UA92355C2 (en) 2010-10-25
MY142496A (en) 2010-11-30
NZ565475A (en) 2010-01-29
JP5179357B2 (ja) 2013-04-10
ECSP078060A (es) 2008-01-23
TW200726753A (en) 2007-07-16
IL188452A0 (en) 2008-04-13
EP1902037A1 (de) 2008-03-26
US20110251174A1 (en) 2011-10-13
NO20076059L (no) 2008-01-30
CN101213179A (zh) 2008-07-02
EA016358B1 (ru) 2012-04-30
US20130281429A1 (en) 2013-10-24
CY1109644T1 (el) 2014-08-13
PT1902037E (pt) 2009-10-13
AU2006264958B2 (en) 2012-05-03
BRPI0613096A2 (pt) 2010-12-21
KR20080031362A (ko) 2008-04-08
MX2007015992A (es) 2008-03-07
UY29636A1 (es) 2007-01-31
DE502006004750D1 (de) 2009-10-15
PL1902037T3 (pl) 2010-02-26
EA200800172A1 (ru) 2008-08-29
JP2008544972A (ja) 2008-12-11
ES2330045T3 (es) 2009-12-03
CA2613664A1 (en) 2007-01-11
AU2006264958A1 (en) 2007-01-11
US20070032514A1 (en) 2007-02-08
AR057423A1 (es) 2007-12-05
DK1902037T3 (da) 2009-12-21
PE20070121A1 (es) 2007-03-05
SI1902037T1 (sl) 2010-01-29
ATE441639T1 (de) 2009-09-15
ZA200709763B (en) 2008-12-31

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