MA33606B1 - Dérivés de pyrimidine en tant qu'inhibiteurs de protéine tyrosine kinase 2 - Google Patents

Dérivés de pyrimidine en tant qu'inhibiteurs de protéine tyrosine kinase 2

Info

Publication number
MA33606B1
MA33606B1 MA34719A MA34719A MA33606B1 MA 33606 B1 MA33606 B1 MA 33606B1 MA 34719 A MA34719 A MA 34719A MA 34719 A MA34719 A MA 34719A MA 33606 B1 MA33606 B1 MA 33606B1
Authority
MA
Morocco
Prior art keywords
tyrosine kinase
pyrimidine derivatives
protein inhibitors
compounds
relates
Prior art date
Application number
MA34719A
Other languages
Arabic (ar)
English (en)
Inventor
Heinz Stadtmueller
Ioannis Sapountzis
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43048878&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA33606(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of MA33606B1 publication Critical patent/MA33606B1/fr

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
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • 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
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La présente invention concerne des composés de formule générale (1a) et (1b), où les groupes r1 à r5, a, q, m, n, p et q sont tels que définis dans la revendication 1, composés qui sont des inhibiteurs de fak/ptk2 et qui peuvent ainsi être utilisés dans le cadre du traitement de maladies caractérisées par une prolifération cellulaire excessive ou anormale. L'invention concerne également l'utilisation desdits composés en tant que médicaments.
MA34719A 2009-10-02 2012-03-26 Dérivés de pyrimidine en tant qu'inhibiteurs de protéine tyrosine kinase 2 MA33606B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09172026 2009-10-02
EP10172460 2010-08-11
PCT/EP2010/064628 WO2011039344A1 (fr) 2009-10-02 2010-10-01 Dérivés de pyrimidine utilisables en tant qu'inhibiteurs de la protéine qu'est la tyrosine kinase 2

Publications (1)

Publication Number Publication Date
MA33606B1 true MA33606B1 (fr) 2012-09-01

Family

ID=43048878

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34719A MA33606B1 (fr) 2009-10-02 2012-03-26 Dérivés de pyrimidine en tant qu'inhibiteurs de protéine tyrosine kinase 2

Country Status (25)

Country Link
US (1) US8466155B2 (fr)
EP (1) EP2483249B1 (fr)
JP (1) JP5702390B2 (fr)
KR (1) KR20120092617A (fr)
CN (1) CN102695700A (fr)
AP (1) AP2012006166A0 (fr)
AR (1) AR078513A1 (fr)
AU (1) AU2010302648A1 (fr)
BR (1) BR112012007300A2 (fr)
CA (1) CA2775418A1 (fr)
CL (1) CL2012000825A1 (fr)
EA (1) EA201200552A1 (fr)
EC (1) ECSP12011830A (fr)
IL (1) IL218543A0 (fr)
IN (1) IN2012DN02714A (fr)
MA (1) MA33606B1 (fr)
MX (1) MX2012003101A (fr)
NZ (1) NZ598614A (fr)
PE (1) PE20121431A1 (fr)
PH (1) PH12012500527A1 (fr)
TN (1) TN2012000142A1 (fr)
TW (1) TW201124386A (fr)
UY (1) UY32916A (fr)
WO (1) WO2011039344A1 (fr)
ZA (1) ZA201201703B (fr)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120244141A1 (en) 2010-09-28 2012-09-27 Boehringer Ingelheim International Gmbh Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors
WO2012088266A2 (fr) 2010-12-22 2012-06-28 Incyte Corporation Imidazopyridazines et benzimidazoles substitués en tant qu'inhibiteurs de fgfr3
US20130324532A1 (en) 2011-02-17 2013-12-05 Cancer Therapeutics Crc Pty Limited Fak inhibitors
AU2012216894B2 (en) 2011-02-17 2016-07-14 Cancer Therapeutics Crc Pty Limited Selective FAK inhibitors
US20150132301A1 (en) * 2011-12-09 2015-05-14 Oncomed Pharmaceuticals, Inc. Combination Therapy for Treatment of Cancer
EP2832734A4 (fr) * 2012-03-28 2015-08-26 Takeda Pharmaceutical Composé hétérocyclique
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
WO2014026125A1 (fr) 2012-08-10 2014-02-13 Incyte Corporation Dérivés de pyrazine en tant qu'inhibiteurs de fgfr
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
EP2999472B1 (fr) 2013-05-22 2020-07-22 The Regents of The University of California Inhibiteurs d'aurora kinase
US10851105B2 (en) 2014-10-22 2020-12-01 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
SG11201706287PA (en) 2015-02-20 2017-09-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2016134294A1 (fr) 2015-02-20 2016-08-25 Incyte Corporation Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
ES3061844T3 (en) 2018-05-04 2026-04-07 Incyte Corp Salts of an fgfr inhibitor
MX2020011718A (es) 2018-05-04 2021-02-15 Incyte Corp Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
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
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之雙環雜環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3163875A1 (fr) 2019-12-04 2021-06-10 Incyte Corporation Heterocycles tricycliques en tant qu'inhibiteurs de fgfr
WO2021113462A1 (fr) 2019-12-04 2021-06-10 Incyte Corporation Dérivés d'un inhibiteur de fgfr
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
EP4352060A1 (fr) 2021-06-09 2024-04-17 Incyte Corporation Hétérocycles tricycliques utiles en tant qu'inhibiteurs de fgfr
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
AU2002312933B2 (en) * 2001-05-29 2007-12-06 Schering Ag CDK inhibiting pyrimidines, production thereof and their use as medicaments
DK1438053T3 (da) 2001-10-17 2008-12-08 Boehringer Ingelheim Pharma Pyrimidinderivater, lægemiddel indeholdende disse forbindelser, deres anvendelse og fremgangsmåder til deres fremstilling
EP1483260A1 (fr) * 2002-03-11 2004-12-08 Schering Aktiengesellschaft 2-heteroaryle-pyrimidines inhibitrices de la kinase dependante des cyclines, leur production et leur utilisation comme medicaments
AR042486A1 (es) * 2002-12-18 2005-06-22 Glaxo Group Ltd Compuesto de quinolina y naftiridina halosustituido en la posicion 3, procedimiento para preparar el compuesto, composicion farmaceutica que lo comprende y su uso para preparar dicha composicion .
US7754714B2 (en) 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1794134A1 (fr) * 2004-09-29 2007-06-13 Bayer Schering Pharma Aktiengesellschaft 2-anilinopyrimidine substituee utilisee en tant que kinase a cycle cellulaire ou recepteur de la tyrosine kinase, leur production et leur utilisation en tant que medicament
US20070032514A1 (en) * 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
RS20080272A (sr) * 2005-12-21 2009-07-15 Pfizer Products Inc., Derivati pirimidina za tretman neprirodnog rasta ćelija
US8623887B2 (en) 2006-05-15 2014-01-07 Boehringer Ingelheim International Gmbh Compounds
TW200808325A (en) * 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
GB0619343D0 (en) 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
CA2673184A1 (fr) * 2006-12-22 2008-07-03 Boehringer Ingelheim International Gmbh Nouveaux composes
EP2154967B9 (fr) 2007-04-16 2014-07-23 Hutchison Medipharma Enterprises Limited Dérivés de pyrimidine
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TW201024281A (en) 2008-11-24 2010-07-01 Boehringer Ingelheim Int New compounds
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法

Also Published As

Publication number Publication date
IL218543A0 (en) 2012-05-31
TN2012000142A1 (en) 2013-09-19
EP2483249B1 (fr) 2015-12-23
AU2010302648A1 (en) 2012-04-05
IN2012DN02714A (fr) 2015-09-11
BR112012007300A2 (pt) 2017-11-07
UY32916A (es) 2011-04-29
ZA201201703B (en) 2014-05-28
TW201124386A (en) 2011-07-16
WO2011039344A1 (fr) 2011-04-07
JP2013506636A (ja) 2013-02-28
CL2012000825A1 (es) 2012-08-24
AP2012006166A0 (en) 2012-04-30
CA2775418A1 (fr) 2011-04-07
EP2483249A1 (fr) 2012-08-08
NZ598614A (en) 2013-08-30
EA201200552A1 (ru) 2013-03-29
US8466155B2 (en) 2013-06-18
KR20120092617A (ko) 2012-08-21
PH12012500527A1 (en) 2012-10-22
AR078513A1 (es) 2011-11-16
ECSP12011830A (es) 2012-06-29
PE20121431A1 (es) 2012-11-10
US20110237598A1 (en) 2011-09-29
MX2012003101A (es) 2012-04-11
CN102695700A (zh) 2012-09-26
JP5702390B2 (ja) 2015-04-15

Similar Documents

Publication Publication Date Title
MA31167B1 (fr) Inhibiteurs de l'activite de akt
MA64509B1 (fr) Composés hétérocycliques utilisés comme immunomodulateurs
MA64121B1 (fr) Composés hétérocycliques utilisés comme immunomodulateurs
TN2009000551A1 (fr) Nouveaux composes chimiques
MA33302B1 (fr) 2, 4-diaminopyrimidines pour le traitement de maladies caracterisees par une proliferation cellulaire excessive ou anormale
MA30333B1 (fr) Aminotetrahydropyranes utiles en tant qu'inhibiteurs de la dipeptidyle peptidase-iv pour le traitement ou la prevention du diabete.
MA31117B1 (fr) Composes tricycliques et leur utilisation comme modulateurs du recepteur de glucocorticoïdes
MA31521B1 (fr) Dérivés de 2,3-dihydrobenzo[1,4] dioxin-2-ylméthyle utilisés en tant qu'antagonistes des alpha2c pour traiter des maladies des systèmes nerveux périphérique et central
MA40290A1 (fr) Agents immunorégulateurs
EP1841770A4 (fr) Pyrimidines bicycliques en tant qu'inhibiteurs de la dipeptidyl-peptidase-iv dans le traitement ou la prevention de diabetes
MA32729B1 (fr) Derives d'acide 1-amino-2-cyclobutylethylboronique
EA200901166A1 (ru) Соединения и композиции в качестве модуляторов активности gpr 119
MA30358B1 (fr) Quinazolines pour l'inhibition de pdk1
EP1796669A4 (fr) Aminopiperidines utilisees comme inhibiteurs de la dipeptidyle peptidase-iv pour le traitement ou la prevention du diabete
MA34299B1 (fr) Dérivés d'aminopyrimidine au titre de modulateurs de lrrk2
MXPA05010711A (es) Compuestos y composiciones novedosos como inhibidores de proteina-quinasa.
MA29444B1 (fr) Antagonistes npy, preparation et utilisations
EP1888066A4 (fr) Aminocyclohexanes en tant qu'inhibiteurs de dipeptidyle peptidase-iv pour le traitement ou la prevention du diabete
EP2091328A4 (fr) Composés de spiropipéridine inhibiteurs de la bêta-sécrétase pour le traitement de la maladie d'alzheimer
EA200802054A1 (ru) Ингибиторы фермента
DE602005024004D1 (de) Als beta-sekretase (bace)-hemmer nützliche 2-amino-chinazolinderivate
MA40955A (fr) 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
MA38648B1 (fr) Composés carboxamide de carbazole et de tétrahydrocarbazole substitués convenant comme inhibiteurs de kinases
MA31336B1 (fr) Inhibiteurs de pi3k alpha a base de pyridopyrimidinone
EA200602242A1 (ru) 3-аминоциклопентанкарбоксамиды в качестве модуляторов хемокиновых рецепторов