CA2498781A1 - Indolinones substituted by heterocycles, their preparation thereof and their use as medicaments - Google Patents

Indolinones substituted by heterocycles, their preparation thereof and their use as medicaments Download PDF

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Publication number
CA2498781A1
CA2498781A1 CA002498781A CA2498781A CA2498781A1 CA 2498781 A1 CA2498781 A1 CA 2498781A1 CA 002498781 A CA002498781 A CA 002498781A CA 2498781 A CA2498781 A CA 2498781A CA 2498781 A1 CA2498781 A1 CA 2498781A1
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CA
Canada
Prior art keywords
group
alkyl
amino
methylene
denotes
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.)
Abandoned
Application number
CA002498781A
Other languages
English (en)
French (fr)
Inventor
Joerg Kley
Armin Heckel
Frank Hilberg
Gerald Juergen Roth
Thorsten Lehmann-Lintz
Ralf R. H. Lotz
Ulrike Tontsch-Grunt
Jacobus C. A. Van Meel
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.)
Boehringer Ingelheim Pharma GmbH and Co KG
Original Assignee
Individual
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
Priority claimed from DE2002142350 external-priority patent/DE10242350A1/de
Priority claimed from DE10252969A external-priority patent/DE10252969A1/de
Application filed by Individual filed Critical Individual
Publication of CA2498781A1 publication Critical patent/CA2498781A1/en
Abandoned legal-status Critical Current

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    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA002498781A 2002-09-12 2003-09-09 Indolinones substituted by heterocycles, their preparation thereof and their use as medicaments Abandoned CA2498781A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE10242350.4 2002-09-12
DE2002142350 DE10242350A1 (de) 2002-09-12 2002-09-12 Heterocyclisch substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
DE10252969.8 2002-11-14
DE10252969A DE10252969A1 (de) 2002-11-14 2002-11-14 Heterocyclisch substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
PCT/EP2003/009978 WO2004026829A2 (de) 2002-09-12 2003-09-09 Heterocyclisch substituierte indolinone und deren verwendung als rezeptor-tyrosinkinasen inhibitoren

Publications (1)

Publication Number Publication Date
CA2498781A1 true CA2498781A1 (en) 2004-04-01

Family

ID=32031471

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002498781A Abandoned CA2498781A1 (en) 2002-09-12 2003-09-09 Indolinones substituted by heterocycles, their preparation thereof and their use as medicaments

Country Status (12)

Country Link
US (1) US7148249B2 (enExample)
EP (1) EP1551830B1 (enExample)
JP (1) JP2006501273A (enExample)
AR (1) AR041194A1 (enExample)
AT (1) ATE427947T1 (enExample)
AU (1) AU2003273842A1 (enExample)
CA (1) CA2498781A1 (enExample)
DE (1) DE50311397D1 (enExample)
ES (1) ES2324710T3 (enExample)
PE (1) PE20041080A1 (enExample)
TW (1) TW200407125A (enExample)
WO (1) WO2004026829A2 (enExample)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009079767A1 (en) * 2007-12-21 2009-07-02 University Health Network Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer
WO2010115279A1 (en) * 2009-04-06 2010-10-14 University Health Network Kinase inhibitors and method of treating cancer with same
WO2011123947A1 (en) * 2010-04-06 2011-10-13 University Health Network Synthesis of chiral 2-(1h-indazol-6-yl)-spiro[cyclopropane-1,3'- indolin]-2'-ones
US8067617B2 (en) 2007-12-03 2011-11-29 Boehringer Ingelheim International Gmbh Indolinone derivatives and process for their manufacture
WO2012048411A1 (en) * 2010-10-13 2012-04-19 University Health Network Plk-4 inhibitors and method of treating cancer with same
US8304541B2 (en) 2007-12-03 2012-11-06 Boehringer Ingelheim International Gmbh Process for the manufacture of an indolinone derivative
US20160250220A1 (en) 2013-10-18 2016-09-01 University Health Network Treatment for pancreatic cancer

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6982260B1 (en) 1999-11-22 2006-01-03 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
EP1330444B1 (en) 2000-11-01 2011-03-23 Millennium Pharmaceuticals, Inc. Nitrogenous heterocyclic compounds and process for making them
US20040204458A1 (en) * 2002-08-16 2004-10-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of Lck inhibitors for treatment of immunologic diseases
ES2305887T3 (es) 2003-12-18 2008-11-01 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidinas como agentes antiproliferativos.
KR100629713B1 (ko) * 2004-04-10 2006-09-29 (주)아모레퍼시픽 펜타에리스리톨 유도체와 이의 제조방법, 및 이를포함하는 액정베이스
NI200700147A (es) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv Derivados de quinazolina inhibidores de cinasas dirigidos a multip
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
EP2044084B1 (en) 2006-07-13 2016-02-17 Janssen Pharmaceutica NV Mtki quinazoline derivatives
US7928136B2 (en) * 2006-09-11 2011-04-19 Curis, Inc. Substituted 2-indolinone as PTK inhibitors containing a zinc binding moiety
AU2008265104B2 (en) 2007-06-21 2013-09-12 Janssen Pharmaceutica Nv Indolin-2-ones and aza-indolin-2-ones
DK2185562T3 (en) 2007-07-27 2016-02-22 Janssen Pharmaceutica Nv PYRROLOPYRIMIDINES SUITABLE FOR TREATING PROLIFERATIVE DISEASES
EA020046B1 (ru) * 2008-06-06 2014-08-29 Бёрингер Ингельхайм Интернациональ Гмбх Фармацевтическая комбинация
EA201100254A1 (ru) * 2008-07-29 2011-08-30 Бёрингер Ингельхайм Интернациональ Гмбх Новые соединения
CN103848814B (zh) * 2012-12-06 2016-08-17 山东亨利医药科技有限责任公司 作为酪氨酸激酶抑制剂的取代吲哚满酮衍生物
EP2930167B1 (en) * 2012-12-06 2018-11-21 KBP Biosciences Co., Ltd. An indolinone derivative as tyrosine kinase inhibitor
EP3012248B1 (en) * 2013-06-20 2019-09-11 Institute of Radiation Medicine, Academy of Military Medical Sciences, People's Liberation Army of China Substance having tyrosine kinase inhibitory activity and preparation method and use thereof
CA3048376A1 (en) 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
CN112174943A (zh) * 2019-07-03 2021-01-05 四川大学 一种吲哚-2-酮类化合物在制备防治口腔细菌产品中的用途
CN114213396B (zh) * 2022-01-27 2023-03-24 深圳市乐土生物医药有限公司 一种吲哚-2-酮类化合物及其制备方法与用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU763361B2 (en) * 1998-09-25 2003-07-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel substituted indolinones with an inhibitory effect on various kinases and cyclin/CDK complexes
CA2381821A1 (en) 1999-08-27 2001-03-08 Boehringer Ingelheim Pharma Kg Substituted indolinones, their manufacture and their use as medicaments
US6762180B1 (en) * 1999-10-13 2004-07-13 Boehringer Ingelheim Pharma Kg Substituted indolines which inhibit receptor tyrosine kinases
DE19949209A1 (de) 1999-10-13 2001-04-19 Boehringer Ingelheim Pharma In 5-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
UA75054C2 (uk) 1999-10-13 2006-03-15 Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу
DE10117204A1 (de) * 2001-04-06 2002-10-10 Boehringer Ingelheim Pharma In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8304541B2 (en) 2007-12-03 2012-11-06 Boehringer Ingelheim International Gmbh Process for the manufacture of an indolinone derivative
US8067617B2 (en) 2007-12-03 2011-11-29 Boehringer Ingelheim International Gmbh Indolinone derivatives and process for their manufacture
WO2009079767A1 (en) * 2007-12-21 2009-07-02 University Health Network Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer
US8765748B2 (en) 2007-12-21 2014-07-01 University Health Network Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer
USRE47731E1 (en) 2009-04-06 2019-11-19 University Health Network Kinase inhibitors and method of treating cancer with same
US8481525B2 (en) 2009-04-06 2013-07-09 University Of Health Network Kinase inhibitors and method of treating cancer with same
WO2010115279A1 (en) * 2009-04-06 2010-10-14 University Health Network Kinase inhibitors and method of treating cancer with same
US8999968B2 (en) 2009-04-06 2015-04-07 University Health Network Kinase inhibitors and method of treating cancer with same
US8263596B2 (en) 2010-04-06 2012-09-11 University Health Network Kinase inhibitors and method of treating cancer
WO2011123947A1 (en) * 2010-04-06 2011-10-13 University Health Network Synthesis of chiral 2-(1h-indazol-6-yl)-spiro[cyclopropane-1,3'- indolin]-2'-ones
US8481533B2 (en) 2010-04-06 2013-07-09 University Health Network Kinase inhibitors and method of treating cancer
US9139563B2 (en) 2010-04-06 2015-09-22 University Health Network Kinase inhibitors and method of treating cancer
US9907800B2 (en) 2010-04-06 2018-03-06 University Health Network Kinase inhibitors and method of treating cancer
US9579327B2 (en) 2010-04-06 2017-02-28 University Health Network Synthesis of chiral 2-(1H-indazol-6-yl)-spiro[cyclopropane-1,3′-indolin]-2′-ones
US10077255B2 (en) 2010-04-06 2018-09-18 University Health Network Synthesis of chiral 2-(1H-indazol-6-yl)-spiro[cyclopropane-1,3′-indolin]-2′-ones
US9796703B2 (en) 2010-04-06 2017-10-24 University Health Network Synthesis of chiral 2-(1H-indazol-6-yl)-spiro[cyclopropane-1,3′-indolin]-2′-ones
WO2012048411A1 (en) * 2010-10-13 2012-04-19 University Health Network Plk-4 inhibitors and method of treating cancer with same
US9642856B2 (en) 2013-10-18 2017-05-09 University Health Network Treatment for pancreatic cancer
US20160250220A1 (en) 2013-10-18 2016-09-01 University Health Network Treatment for pancreatic cancer

Also Published As

Publication number Publication date
ATE427947T1 (de) 2009-04-15
PE20041080A1 (es) 2005-02-17
WO2004026829A3 (de) 2004-10-07
ES2324710T3 (es) 2009-08-13
EP1551830B1 (de) 2009-04-08
AU2003273842A1 (en) 2004-04-08
EP1551830A2 (de) 2005-07-13
AR041194A1 (es) 2005-05-04
WO2004026829A2 (de) 2004-04-01
US7148249B2 (en) 2006-12-12
AU2003273842A8 (en) 2004-04-08
JP2006501273A (ja) 2006-01-12
TW200407125A (en) 2004-05-16
US20050054710A1 (en) 2005-03-10
DE50311397D1 (de) 2009-05-20

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued