AR046086A1 - Derivados de 1,3- benzoxazolilo como inhibidores de quinasa - Google Patents

Derivados de 1,3- benzoxazolilo como inhibidores de quinasa

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Publication number
AR046086A1
AR046086A1 ARP040103452A ARP040103452A AR046086A1 AR 046086 A1 AR046086 A1 AR 046086A1 AR P040103452 A ARP040103452 A AR P040103452A AR P040103452 A ARP040103452 A AR P040103452A AR 046086 A1 AR046086 A1 AR 046086A1
Authority
AR
Argentina
Prior art keywords
hal
atoms
mono
scf3
unsubstituted
Prior art date
Application number
ARP040103452A
Other languages
English (en)
Inventor
Staehle Wolfgang Dr
Jonczyk Alfred Dr
Rautenberg Wilfried Dr
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR046086A1 publication Critical patent/AR046086A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

El presente se refiere a su composición y uso para el tratamiento de enfermedades, en especial tumores y/o enfermedades que son causadas, mediadas y/o propagadas por angiogénesis. Los compuesos de la fórmula (1) son inhibidores eficaces de las tirosina quinasas, en particular TIE-2 y VEGFR, y de las Raf-quinasas. Reivindicación 1: Compuestos de la fórmula (1), en donde significan: R1, R2, R3 en cada caso, de modo independiente entre sí, R, Hal, CN, NO2, NHR, NRR, NHCOR, NHSO2R, OR, CO-R, CO-NHR, CF3, OCF3, SCF3, SO3R, SO2R, SO2NR, SR, COOH o COOR; R es H o A, AR, Het, (CH2)qHet o (CH2)qAr insustituido o mono, di, tri o tetrasustituido con R4; a es alquilo no ramificado, ramificado o cíclico C1-14, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F y/o Cl; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con A, Hal, OH, OA, CN, NO2, NH2, NHA, NA2, NHCOA, SCF3, SO2A, CO-OH,COOA, CONH2, CONHA, CONA2, NHSO2A, SO2NH2, SO2NHA, SO2NA2, CHO o COA; Het es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con el oxígeno del carbonilo, Hal, A, -(CH2)b-Ar, -(CH2)b-cicloalquilo, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 y/o S(O)gA; Hal es F, Cl, Br o I; R4 es Hal, OH, CN, NO2, CF3, OCF3, SCF3, SO2A, u OA; X es O, S,SO2NH o NH; el circulo Y es fenilo o un heterociclo aromático monocíclico con 1 a 4 átomos de N, O y/o S; b es 0, 1, 2, 3 o 4; g es 0, 1 o 2; n, m, p, q son en cada caso, de modo independiente entre sí, 1, 2, 3 ó 4; así como sus sales, derivados, solvatos y estereoisómeros farmacéuticamente inocuos, incluyendo sus mezclas en todas las proporciones.
ARP040103452A 2003-09-24 2004-09-24 Derivados de 1,3- benzoxazolilo como inhibidores de quinasa AR046086A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10344223A DE10344223A1 (de) 2003-09-24 2003-09-24 1,3-Benzoxazolylderivate als Kinase-Inhibitoren

Publications (1)

Publication Number Publication Date
AR046086A1 true AR046086A1 (es) 2005-11-23

Family

ID=34353052

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103452A AR046086A1 (es) 2003-09-24 2004-09-24 Derivados de 1,3- benzoxazolilo como inhibidores de quinasa

Country Status (8)

Country Link
US (2) US8242128B2 (es)
EP (1) EP1664039B1 (es)
JP (1) JP5103013B2 (es)
AR (1) AR046086A1 (es)
AU (1) AU2004281879B2 (es)
CA (1) CA2539767C (es)
DE (1) DE10344223A1 (es)
WO (1) WO2005037829A1 (es)

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US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
JP2002534468A (ja) 1999-01-13 2002-10-15 バイエル コーポレイション p38キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
WO2003068228A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Aryl ureas with angiogenesis inhibiting activity
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
PT1636585E (pt) 2003-05-20 2008-03-27 Bayer Pharmaceuticals Corp Diarilureias com actividade inibidora de cinase
US8637553B2 (en) 2003-07-23 2014-01-28 Bayer Healthcare Llc Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions
US20070238718A1 (en) * 2006-04-06 2007-10-11 Matthias Grauert Thiazolyl-dihydro-indazole
US20070259855A1 (en) * 2006-04-06 2007-11-08 Udo Maier Thiazolyl-dihydro-indazole
US7517995B2 (en) 2006-04-06 2009-04-14 Boehringer Ingelheim International Gmbh Thiazolyl-dihydro-cyclopentapyrazole
EP1900729A1 (en) 2006-09-15 2008-03-19 Novartis AG Benzoxazoles and oxazolopyridines being useful as Janus kinases inhibitors
JP2011513332A (ja) * 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド 癌の治療のためのraf阻害剤としてのn−(6−アミノピリジン−3−イル)−3−(スルホンアミド)ベンズアミド誘導体
TW200940539A (en) * 2008-02-29 2009-10-01 Array Biopharma Inc RAF inhibitor compounds and methods of use thereof
KR20100122505A (ko) * 2008-02-29 2010-11-22 어레이 바이오파마 인크. Raf 저해물질 화합물 및 이들의 이용 방법
WO2009111277A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Imdizo [4. 5-b] pyridine derivatives used as raf inhibitors
WO2009158432A2 (en) 2008-06-27 2009-12-30 Amgen Inc. Ang-2 inhibition to treat multiple sclerosis
TWI396689B (zh) 2008-11-14 2013-05-21 Amgen Inc 作為磷酸二酯酶10抑制劑之吡衍生物
TW201030001A (en) 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
CA2803118C (en) 2010-07-09 2015-11-03 Pfizer Limited Sulfonamide derivatives as nav 1.7 inhibitors
WO2015066241A1 (en) * 2013-10-30 2015-05-07 Novartis Ag 2-benzyl-benzimidazole complement factor b inhibitors and uses thereof
MX2020004202A (es) 2017-10-30 2020-08-13 Neuropore Therapies Inc Fenil sulfonil fenil triazol tionas sustituidas y usos de las mismas.
KR20240043869A (ko) * 2022-09-27 2024-04-04 이화여자대학교 산학협력단 4-아미노-부탄아미드를 포함하는 신규한 벤조옥사졸 유도체 및 이의 용도

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Also Published As

Publication number Publication date
JP5103013B2 (ja) 2012-12-19
US20060281762A1 (en) 2006-12-14
AU2004281879B2 (en) 2011-04-07
JP2007506687A (ja) 2007-03-22
US20120220611A1 (en) 2012-08-30
EP1664039B1 (de) 2014-03-05
US8242128B2 (en) 2012-08-14
CA2539767C (en) 2013-02-05
DE10344223A1 (de) 2005-04-21
CA2539767A1 (en) 2005-04-28
AU2004281879A1 (en) 2005-04-28
EP1664039A1 (de) 2006-06-07
WO2005037829A1 (de) 2005-04-28

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