JP5629752B2 - キナーゼインヒビターおよびこれを用いた癌の治療方法 - Google Patents

キナーゼインヒビターおよびこれを用いた癌の治療方法 Download PDF

Info

Publication number
JP5629752B2
JP5629752B2 JP2012502408A JP2012502408A JP5629752B2 JP 5629752 B2 JP5629752 B2 JP 5629752B2 JP 2012502408 A JP2012502408 A JP 2012502408A JP 2012502408 A JP2012502408 A JP 2012502408A JP 5629752 B2 JP5629752 B2 JP 5629752B2
Authority
JP
Japan
Prior art keywords
alkyl
phenyl
group
halogen
haloalkyl
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
JP2012502408A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012522729A (ja
JP2012522729A5 (enExample
Inventor
ブレント サンプソン,ピーター
ブレント サンプソン,ピーター
リー,セー−ワン
リウ,ヨン
ダブリュ. ポールズ,ハインズ
ダブリュ. ポールズ,ハインズ
ジー. エドワーズ,ルイーズ
ジー. エドワーズ,ルイーズ
ティー. フォレスト,ブライアン
ティー. フォレスト,ブライアン
フェーヘル,ミクロス
クマール ビー. パテル,ナレンドラ
クマール ビー. パテル,ナレンドラ
パン,クオホア.
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 Health Network
Original Assignee
University Health Network
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 Health Network filed Critical University Health Network
Publication of JP2012522729A publication Critical patent/JP2012522729A/ja
Publication of JP2012522729A5 publication Critical patent/JP2012522729A5/ja
Application granted granted Critical
Publication of JP5629752B2 publication Critical patent/JP5629752B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • C07D401/14Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems

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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2012502408A 2009-04-06 2010-04-06 キナーゼインヒビターおよびこれを用いた癌の治療方法 Active JP5629752B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21198809P 2009-04-06 2009-04-06
US61/211,988 2009-04-06
PCT/CA2010/000518 WO2010115279A1 (en) 2009-04-06 2010-04-06 Kinase inhibitors and method of treating cancer with same

Publications (3)

Publication Number Publication Date
JP2012522729A JP2012522729A (ja) 2012-09-27
JP2012522729A5 JP2012522729A5 (enExample) 2014-01-09
JP5629752B2 true JP5629752B2 (ja) 2014-11-26

Family

ID=42935603

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012502408A Active JP5629752B2 (ja) 2009-04-06 2010-04-06 キナーゼインヒビターおよびこれを用いた癌の治療方法

Country Status (6)

Country Link
US (3) US8481525B2 (enExample)
EP (1) EP2417127B1 (enExample)
JP (1) JP5629752B2 (enExample)
CA (1) CA2756568C (enExample)
ES (1) ES2465971T3 (enExample)
WO (1) WO2010115279A1 (enExample)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011506494A (ja) 2007-12-21 2011-03-03 ユニバーシティ・ヘルス・ネットワーク 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体
CA2756568C (en) 2009-04-06 2018-02-13 University Health Network Kinase inhibitors and method of treating cancer with same
WO2011069298A1 (en) * 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag Novel cyclopropane indolinone derivatives
WO2011123937A1 (en) * 2010-04-06 2011-10-13 University Health Network Kinase inhibitors and method of treating cancer with same
PT2556071T (pt) 2010-04-06 2016-11-22 Univ Health Network Inibidores de quinase e seus usos no tratamento de cancro
US8933070B2 (en) 2010-07-02 2015-01-13 University Health Network Methods of targeting PTEN mutant diseases and compositions therefor
WO2012048411A1 (en) * 2010-10-13 2012-04-19 University Health Network Plk-4 inhibitors and method of treating cancer with same
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
HUE042374T2 (hu) 2012-06-13 2019-06-28 Incyte Holdings Corp Szubsztituált triciklusos vegyületek mint FGFR inhibitorok
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102469849B1 (ko) 2013-04-19 2022-11-23 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
JP6525983B2 (ja) * 2013-10-18 2019-06-05 ユニバーシティー ヘルス ネットワーク 膵癌の治療法
PT3057965T (pt) 2013-10-18 2019-04-23 Univ Health Network Formas de sal e cristal de inibidor de plk-4
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CN108947970B (zh) * 2017-05-18 2022-04-05 四川大学 吲唑类衍生物及其制备方法和用途
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
RS65335B1 (sr) 2018-10-05 2024-04-30 Annapurna Bio Inc Jedinjenja i kompozicije za lečenje stanja povezanih sa aktivnošću receptora apj
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
BR112021021106A2 (pt) 2019-04-24 2021-12-14 Univ Health Network Forma cristalina s4 do inibidor plk4 fumarato (ir,2s)-(e)-2-(3-(4-((cis-2,6-dimetilmorfolino)metil)estiril)-1h-imidazol-6-il)-5'-metoxiespiro[ciclopropano-1,3'-indolin]-2'ona
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
CN115397429A (zh) * 2019-12-06 2022-11-25 大学健康网络 急性髓性白血病或骨髓增生异常综合征治疗
CN111171003B (zh) * 2020-01-06 2020-12-22 温州市中心医院 作为用于预防或治疗由人乳头状瘤病毒(hpv)诱导的宫颈癌的化合物
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021203190A1 (en) * 2020-04-06 2021-10-14 University Health Network Combination therapies for inhibition of polo-like kinase 4
CN112250614B (zh) * 2020-10-20 2022-02-01 苏州大学 3-螺三元环吲哚酮衍生物的合成方法
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
IL308346A (en) * 2021-05-11 2024-01-01 Oric Pharmaceuticals Inc Polo like kinase 4 inhibitors
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4598912A1 (en) * 2022-10-03 2025-08-13 Oric Pharmaceuticals, Inc. Polo like kinase 4 inhibitors

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA238362A (en) 1924-03-04 The Port Arthur Shipbuilding Co. Screw feed magazine
DE3310891A1 (de) 1983-03-25 1984-09-27 Boehringer Mannheim Gmbh, 6800 Mannheim Neue indolinon-(2)-derivate, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und zwischenprodukte
US5182397A (en) 1990-05-31 1993-01-26 American Cyanamid Company Aryloxyspiroalkylindolinone herbicides
GB9507298D0 (en) 1995-04-07 1995-05-31 Pharmacia Spa Substituted indolylmethylene-oxindale analogues as tyrosine kinase inhibitors
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
ATE308520T1 (de) 1996-08-23 2005-11-15 Sugen Inc Kombinatorische bibliotheken von indolinone und verwandte produkte und verfahren zur behandlung von krankheiten
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6133305A (en) 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
AU5468499A (en) * 1998-08-04 2000-02-28 Sugen, Inc. 3-methylidenyl-2-indolinone modulators of protein kinase
EP1165513A1 (en) * 1999-03-24 2002-01-02 Sugen, Inc. Indolinone compounds as kinase inhibitors
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
JP2003535847A (ja) * 2000-06-02 2003-12-02 スージェン・インコーポレーテッド 蛋白質キナーゼ/ホスファターゼ阻害剤としてのインドリノン誘導体
US6897231B2 (en) 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
US7429609B2 (en) 2002-05-31 2008-09-30 Eisai R & D Management Co., Ltd. Pyrazole compound and medicinal composition containing the same
US7148249B2 (en) * 2002-09-12 2006-12-12 Boehringer Ingelheim Pharma Gmbh & Co. Kg Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments
US7205328B2 (en) 2002-10-21 2007-04-17 Irm Llc Oxindoles with anti-HIV activity
WO2005058309A1 (en) 2003-12-16 2005-06-30 Leo Pharma A/S Novel therapeutic use of indolinone derivatives
DE102005005395A1 (de) 2005-02-03 2006-08-10 Schering Aktiengesellschaft Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
US7309787B2 (en) 2005-07-13 2007-12-18 Allergan, Inc. Kinase inhibitors
WO2007058626A1 (en) 2005-11-16 2007-05-24 S*Bio Pte Ltd Indazole compounds
US20070135509A1 (en) 2005-12-09 2007-06-14 Blackburn Thomas P Indolone compounds useful to treat cognitive impairment
FR2896503B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives soufres d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
WO2007109026A2 (en) 2006-03-15 2007-09-27 The Trustees Of Columbia University In The City Of New York Pten compositions and methods for detecting breast cancer
GB0606234D0 (en) 2006-03-29 2006-05-10 Pliva Istrazivanje I Razvoj D Pharmaceutically acceptable salts and polymorphic forms
US8207179B2 (en) 2007-06-12 2012-06-26 Boehringer Ingelheim International Gmbh Substituted indolines as tyrosine kinase inhibitors
NZ584760A (en) 2007-09-25 2012-03-30 Takeda Pharmaceutical Polo-like kinase inhibitors
CA2706075A1 (en) 2007-11-20 2009-05-28 University Health Network Cancer diagnostic and therapeutic methods that target plk4/sak
JP2009173629A (ja) 2007-12-21 2009-08-06 Banyu Pharmaceut Co Ltd Rsk1阻害作用を有する新規スピロインダン誘導体
JP2011506494A (ja) 2007-12-21 2011-03-03 ユニバーシティ・ヘルス・ネットワーク 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体
JP5593234B2 (ja) 2008-03-11 2014-09-17 ユニバーシティー ヘルス ネットワーク ニューロペプチドy5r(npy5r)アンタゴニストを使用して癌を治療する方法
EP2108641A1 (en) 2008-04-11 2009-10-14 Laboratorios Almirall, S.A. New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
EP2113503A1 (en) 2008-04-28 2009-11-04 Laboratorios Almirall, S.A. New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
EP2303260A1 (en) 2008-06-16 2011-04-06 Tigris Pharmaceuticals, Inc. Methods for determining sensitivity to aminoflavones
DE102008040187A1 (de) 2008-07-04 2010-01-07 Robert Bosch Gmbh Sensorelement, Verfahren zu seiner Herstellung sowie Verwendung
WO2010017047A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
CA2756568C (en) 2009-04-06 2018-02-13 University Health Network Kinase inhibitors and method of treating cancer with same
WO2011069298A1 (en) 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag Novel cyclopropane indolinone derivatives
JP5056876B2 (ja) 2010-03-19 2012-10-24 Jfeスチール株式会社 冷間加工性と焼入れ性に優れた熱延鋼板およびその製造方法
PT2556071T (pt) 2010-04-06 2016-11-22 Univ Health Network Inibidores de quinase e seus usos no tratamento de cancro
US8933070B2 (en) 2010-07-02 2015-01-13 University Health Network Methods of targeting PTEN mutant diseases and compositions therefor
WO2012048411A1 (en) 2010-10-13 2012-04-19 University Health Network Plk-4 inhibitors and method of treating cancer with same
WO2012121764A1 (en) 2010-11-25 2012-09-13 Ratiopharm Gmbh Novel salts and polymorphic forms of afatinib
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
GB201109966D0 (en) 2011-06-10 2011-07-27 Cancer Res Inst Royal Materials and methods for treating pten mutated or deficient cancer
CA2850394C (en) 2011-10-12 2019-05-21 University Health Network Indazole compounds as kinase inhibitors and method of treating cancer with same
JP6525983B2 (ja) 2013-10-18 2019-06-05 ユニバーシティー ヘルス ネットワーク 膵癌の治療法
PT3057965T (pt) 2013-10-18 2019-04-23 Univ Health Network Formas de sal e cristal de inibidor de plk-4

Also Published As

Publication number Publication date
US8481525B2 (en) 2013-07-09
WO2010115279A1 (en) 2010-10-14
US20120149686A1 (en) 2012-06-14
ES2465971T3 (es) 2014-06-09
EP2417127A4 (en) 2012-08-29
JP2012522729A (ja) 2012-09-27
EP2417127A1 (en) 2012-02-15
CA2756568A1 (en) 2010-10-14
US20140045822A1 (en) 2014-02-13
EP2417127B1 (en) 2014-02-26
CA2756568C (en) 2018-02-13
USRE47731E1 (en) 2019-11-19
US8999968B2 (en) 2015-04-07

Similar Documents

Publication Publication Date Title
JP5629752B2 (ja) キナーゼインヒビターおよびこれを用いた癌の治療方法
US10358436B2 (en) Kinase inhibitors and method of treating cancer
CN109790166A (zh) 咪唑并吡啶化合物用于治疗癌症
JP2011506494A (ja) 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体
CN108069938A (zh) 2,4-二取代吡啶类化合物及其制备方法和应用
RS55471B1 (sr) Inhibitori kinaze i njihova upotreba za lečenje kancera
HK1180315B (en) Kinase inhibitors and their use in treating cancer
JPWO2013168759A1 (ja) 芳香環化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130312

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20130312

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131108

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20140501

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140514

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140813

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140909

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20141006

R150 Certificate of patent or registration of utility model

Ref document number: 5629752

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250