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

Derivados de 1,3- benzoxazolilo como inhibidores de quinasa

Info

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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Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Reproductive Health (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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RU2319693C9 (ru) 1999-01-13 2008-08-20 Байер Копэрейшн Производные мочевины (варианты), фармацевтическая композиция (варианты) и способ лечения заболевания, связанного с ростом раковых клеток (варианты)
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
ES2377847T3 (es) 1999-01-13 2012-04-02 Bayer Healthcare Llc Difenil ureas sustituidas con omega-carboxi arilo como agentes inhibidores de la cinasa p38
EP1478358B1 (en) 2002-02-11 2013-07-03 Bayer HealthCare LLC Sorafenib tosylate for the treatment of diseases characterized by abnormal angiogenesis
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
ES2288694T3 (es) 2003-05-20 2008-01-16 Bayer Pharmaceuticals Corporation Diaril ureas para enfermedades mediadas por el receptor del factor de crecimiento derivado de plaquetas.
KR101139557B1 (ko) 2003-07-23 2012-04-30 바이엘 파마슈티칼스 코포레이션 질환 및 상태의 치료 및 예방을 위한 플루오로 치환오메가-카르복시아릴 디페닐 우레아
US7517995B2 (en) 2006-04-06 2009-04-14 Boehringer Ingelheim International Gmbh Thiazolyl-dihydro-cyclopentapyrazole
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
EP1900729A1 (en) 2006-09-15 2008-03-19 Novartis AG Benzoxazoles and oxazolopyridines being useful as Janus kinases inhibitors
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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
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CN111372579B (zh) 2017-10-30 2023-08-22 神经孔疗法股份有限公司 取代的苯基磺酰基苯基三唑硫酮和其用途
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Also Published As

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

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