AR035877A1 - Derivados de n-oxido-antranilamida, su uso para preparar un medicamento y los medicamentos que los contienen - Google Patents

Derivados de n-oxido-antranilamida, su uso para preparar un medicamento y los medicamentos que los contienen

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Publication number
AR035877A1
AR035877A1 ARP020101679A ARP020101679A AR035877A1 AR 035877 A1 AR035877 A1 AR 035877A1 AR P020101679 A ARP020101679 A AR P020101679A AR P020101679 A ARP020101679 A AR P020101679A AR 035877 A1 AR035877 A1 AR 035877A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
hydrogen
halogen
polysubstituted
Prior art date
Application number
ARP020101679A
Other languages
English (en)
Inventor
Alexander Ernst
Andreas Huth
Martin Kruger
Andreas Menrad
Martin Haberey
Karl-Heinz Thierauch
Original Assignee
Schering Ag
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 DE2001123573 external-priority patent/DE10123573B4/de
Priority claimed from DE2001125293 external-priority patent/DE10125293A1/de
Application filed by Schering Ag filed Critical Schering Ag
Publication of AR035877A1 publication Critical patent/AR035877A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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 chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de N-óxido-antranilamida de fórmula general (1) en donde A representa el grupo -N(R7)-; W es oxígeno, azufre, dos átomos de hidrógeno o el grupo -N(R8)-; Z es una unión, el grupo -N(R10)- ó =N-, alquilo C1-12 ramificado o no ramificado o el grupo -(CRaRb)m-(CRcRd)n-(CReRf)o-, donde m, n y o son 0-3, Ra, Rb, Rc, Rd, Re, Rf son, independientemente entre sí, hidrógeno, flúor, alquilo C1-4 o el grupo -N(R11)- y/o Ra y/o Rb con Rc y/o Rd o Rc con Re y/o Rf pueden formar una unión, o hasta dos de los radicales Ra-Rf pueden formar un puente, cada uno de ellos con hasta 3 átomos de C hacia R1 o hacia R7; X es alquilo C1-6; R1 es alquilo C1-12 o alquenilo C2-12 ramificado o no ramificado, que puede ser mono- o polisustituido de modo igual o diferente por halógeno, hidroxi, ciano, alquiloxi C1-6, aralquiloxi, alquilo C1-6 y/o por el grupo NR12R13; o es cicloalquilo C3-10 o cicloalquenilo C3-10, que puede ser mono- o polisustituido de modo igual o diferente por halógeno, hidroxi, ciano, alquiloxi C1-6, alquilo C1-6 y/o por el grupo NR12R13; o es arilo o hetarilo, que puede ser mono- o polisustituido de modo igual o diferente por halógeno, hidroxi, ciano, cianoalquilo C1-6, alquiloxi C1-6, aralquiloxi, alquilo C1-6, haloalquilo C1-6 o por el grupo =O, -OR14 ó -R14; R2 es hetarilo no sustituido o en caso dado, mono- o polisustituido de modo igual o diferente por ciano, halógeno, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, amino, hidroxi y/o por el grupo -OR18 ó -R19, que tiene por lo menos un grupo N-óxido; D es un átomo de nitrógeno o el grupo C-R3; E es un átomo de nitrógeno o un grupo C-R4; F es un átomo de nitrógeno o un grupo C-R5; G es un átomo de nitrógeno o un grupo C-R6, en donde R3, R4, R5 y R6 son hidrógeno, halógeno o alcoxi C1-6, alquilo C1-6 o carboxialquilo C1-6 no sustituido o en caso dado, mono- o polisustituido por halógeno; R7 es hidrógeno o alquilo C1-6 o forma un puente con Ra-Rf desde Z o hacia R1 con hasta 3 miembros de anillo; R8, R9, R10 y R11 son hidrógeno o alquilo C1-6; R12 y R13 son hidrógeno, alquilo C1-6 o forman un anillo que puede contener otro heteroátomo; R14 es el grupo (CH2-CH2-O)u(CH2)v-R15; R15 es arilo, hetarilo, alquilo C1-6, aralquilo, -CH2CN o el grupo NR16R17; R16 y R17 es hidrógeno, alquilo C1-6, acilo C1-6 o forman un anillo que puede contener otro heteroátomo; R18 es el grupo (CH2-CH2-O)w(CH2)p-R15; R19 es arilo, hetarilo, alquilo C1-6, aralquilo, -CH2CN o el grupo NR16R17 y u, v, w y p son 0-5, y sus isómeros y sales. Estos compuestos son identificados como inhibidores de la tirosinakinasa KDR y FLT, y son particularmente apropiados para el tratamiento de aquellas enfermedades que son originadas o estimuladas por la angiogénesis persistente provocada por el receptor VEGF o un aumento de la permeabilidad vascular. Los compuestos de fórmula (1) también presentan una excelente acción como inhibidores de la VEGFR-kinasa 3 y por ello son apropiados como inhibidores eficaces de la linfangiogénesis. Medicamentos que contienen al menos un compuesto de fórmula (1) y uso de estos compuestos para preparar un medicamento destinado al tratamiento de psoriasis, sarcoma de Kaposi, restenosis, endometriosis, mal de Crohn, enfermedad de Hodkin, leucemia, artritis tal como la artritis reumatoide, hemangioma, angiofibroma, enfermedades oculares tal como retinopatía diabética, el glaucoma neovascular, enfermedades renales tal como la glomerulonefritis, nefropatía diabética, nefroesclerosis maligna, síndromes microangiopáticos trómbicos, rechazos de transplantes y glomerulopatía, enfermedades fibróticas como cirrosis hepática, enfermedades proliferativas de células masangiales, ateroesclerosis, lesiones del tejido nervioso, inhibición de la reoclusión de vasos después de cateterismo con globo dilatable, a la colocación de prótesis vasculares o de dispositivos mecánicos para mantener abiertos los vasos como, por ejemplo, stents, a actuar como inmunosupresores y favorecer la curación de heridas sin dejar cicatriz, y a los casos de léntigo senil y dermatitis de contacto.
ARP020101679A 2001-05-08 2002-05-08 Derivados de n-oxido-antranilamida, su uso para preparar un medicamento y los medicamentos que los contienen AR035877A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2001123573 DE10123573B4 (de) 2001-05-08 2001-05-08 N-Oxidanthranylamid-Derivate und deren Verwendung als Arzneimittel
DE2001125293 DE10125293A1 (de) 2001-05-15 2001-05-15 N-Oxidanthranylamid-Derivate und deren Verwendung als Arzneimittel (II)

Publications (1)

Publication Number Publication Date
AR035877A1 true AR035877A1 (es) 2004-07-21

Family

ID=26009295

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020101679A AR035877A1 (es) 2001-05-08 2002-05-08 Derivados de n-oxido-antranilamida, su uso para preparar un medicamento y los medicamentos que los contienen

Country Status (6)

Country Link
US (1) US7459470B2 (es)
EP (1) EP1389201A1 (es)
JP (1) JP2004528378A (es)
AR (1) AR035877A1 (es)
PE (1) PE20021074A1 (es)
WO (1) WO2002090349A1 (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US7105682B2 (en) * 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7307088B2 (en) * 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
US7615565B2 (en) 2002-07-31 2009-11-10 Bayer Schering Pharma Aktiengesellschaft VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
UA89035C2 (ru) 2003-12-03 2009-12-25 Лео Фарма А/С Эфиры гидроксамовых кислот и их фармацевтическое применение
EP1657241A1 (en) * 2004-11-03 2006-05-17 Schering Aktiengesellschaft Novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors
EP1655295A1 (en) * 2004-11-03 2006-05-10 Schering Aktiengesellschaft Anthranilamide pyridinureas as VEGF receptor kinase inhibitors
US7906533B2 (en) 2004-11-03 2011-03-15 Bayer Schering Pharma Ag Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
US8604055B2 (en) 2004-12-31 2013-12-10 Dr. Reddy's Laboratories Ltd. Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors
WO2006073973A2 (en) 2004-12-31 2006-07-13 Reddy Us Therapeutics, Inc. Novel benzylamine derivatives as cetp inhibitors
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
US8987262B2 (en) 2007-10-19 2015-03-24 Universite de Bordeaux Use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas
EP2050441A1 (en) * 2007-10-19 2009-04-22 Université Victor Segalen Bordeaux 2 Use of beta blocker for the manufacture of a medicament for the treatment of hemangiomas
KR20110045095A (ko) 2008-08-27 2011-05-03 레오 파마 에이/에스 Ｖｅｇｆｒ-2 수용체 및 단백질 티로신 키나아제 억제제인 피리딘 유도체
CN103827105B (zh) 2011-08-18 2016-08-17 雷迪博士实验室有限公司 作为胆固醇酯转移蛋白(cetp)抑制剂的取代的杂环胺化合物
CN103958511A (zh) 2011-09-27 2014-07-30 雷迪博士实验室有限公司 作为胆固醇酯转移蛋白(CETP)抑制剂用于治疗动脉粥样硬化的5-苄基氨基甲基-6-氨基吡唑并[3,4-b]吡啶衍生物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) * 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
DE10023484A1 (de) * 2000-05-09 2001-11-22 Schering Ag Anthranylamide und deren Verwendung als Arzneimittel

Also Published As

Publication number Publication date
US20050032816A1 (en) 2005-02-10
WO2002090349A1 (de) 2002-11-14
JP2004528378A (ja) 2004-09-16
US7459470B2 (en) 2008-12-02
EP1389201A1 (de) 2004-02-18
PE20021074A1 (es) 2003-01-11

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