AR037973A1 - 4-arilquinazolinas - Google Patents

4-arilquinazolinas

Info

Publication number
AR037973A1
AR037973A1 ARP020105062A ARP020105062A AR037973A1 AR 037973 A1 AR037973 A1 AR 037973A1 AR P020105062 A ARP020105062 A AR P020105062A AR P020105062 A ARP020105062 A AR P020105062A AR 037973 A1 AR037973 A1 AR 037973A1
Authority
AR
Argentina
Prior art keywords
formula
hal
compounds
phenyl
polysubstituted
Prior art date
Application number
ARP020105062A
Other languages
English (en)
Inventor
Gericke Rolf Dr
Beier Norbert Dr
Wilm Claudia 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 AR037973A1 publication Critical patent/AR037973A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • C07D403/10Heterocyclic 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 aromatic rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuestos de la fórmula (1), y al uso de los mismos como inhibidores de NHE-3, procedimiento de preparación, preparación farmacéutica, medicamentos. Reivindicación 1: Compuestos de la fórmula (1) donde: Ar es fenilo o naftilo X-sustituido, que está adicionalmente sustituido por R3 y R4, Y es fórmula (2), (3) ó (4); X es H, NR6R7 o un anillo saturado de 5-7 miembros que tiene dos átomos de N; R1, R2, R3 y R4 son cada uno, independientemente entre sí, H, A, OA, Hal, CF3, OH, NO2, NH2, NHA, NA2, NH-CO-A, NH-CO-Ph, SA, SO-A, SO2-A, SO2-Ph, CN, OCF3, CO-A, CO2H, CO2A, CO-NH2, CO-NHA, CO-NA2, SO2NH2, SO2NHA, SO2NA2 o fenilo que está insustituido ó monosustituido ó polisustituido por A, OA, Hal ó CF3; A es alquilo que tiene 1, 2, 3, 4, 5 ó 6 átomos de carbono; Hal es F, Cl, Br ó I; R5 es H, A, OH, NO2, fenilo que está insustituido ó monosustituido ó polisustituido por A, OA, Hal ó CF3, un grupo de protección amino ó fórmula (5); R6 y R7 son cada uno, independientemente entre sí, H, A, fenilo que está insustituido ó monosustituido ó polisustituido por A, OA, Hal ó CF3, bencilo, un grupo de protección amino ó -(CH2)nNR10R11; R8 y R9 son cada uno, independientemente entre sí, H ó A; R10 y R11 son cada uno, independientemente entre sí, H, A, fenilo que está insustituido ó monosustituido ó polisustituido por A, OA, Hal ó CF3, bencilo o un grupo de protección amino; z es 0 ó 1; y n es 2, 3 ó 4; y sales solvatos y estereoisómeros de los mismos, incluyendo las mezclas de los mismos en todas las relaciones, y derivados de los mismos de uso farmacéutico, en particular, sales y solvatos de los mismos de tolerancia fisiológica, con la condición de que queden excluidos los compuestos de la fórmula (1) donde X es H y, simultáneamente, z es 0. Reivindicación 15: Uso de los compuestos de la fórmula (1) de acuerdo con una o varias de las reivindicaciones 1 a 11 y/o sus sales y/o solvatos fisiológicamente aceptables para preparar un medicamento para el tratamiento y la profilaxis de hipertonía, trombosis, estados isquémicos del corazón, del sistema nervioso periférico y central y de apoplejías, estados isquémicos de órganos y miembros periféricos, y para el tratamiento de estados de shock. Reivindicación 16: Uso de los compuestos de la fórmula (1) de acuerdo con una o varias de las reivindicaciones 1 a 11 y/o sus sales y/o solvatos fisiológicamente aceptables para preparar un medicamento para usar en operaciones quirúrgicas y trasplantes de órganos y para preservar y almacenar trasplantes para medidas quirúrgicas. Reivindicación 17: Uso de los compuestos de la fórmula (1) de acuerdo con una o varias de las reivindicaciones 1 a 11 y/o sus sales y/o solvatos fisiológicamente aceptables para preparar un medicamento para el tratamiento y la profilaxis de enfermedades en las cuales la proliferación celular representa una causa primaria o secundaria, para el tratamiento o la profilaxis de trastornos del metabolismo de las grasas o el impulso respiratorio alterado.
ARP020105062A 2001-12-24 2002-12-20 4-arilquinazolinas AR037973A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10163992A DE10163992A1 (de) 2001-12-24 2001-12-24 4-Aryl-chinazoline

Publications (1)

Publication Number Publication Date
AR037973A1 true AR037973A1 (es) 2004-12-22

Family

ID=7710890

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020105062A AR037973A1 (es) 2001-12-24 2002-12-20 4-arilquinazolinas

Country Status (11)

Country Link
US (1) US20050020612A1 (es)
EP (1) EP1458396A1 (es)
KR (1) KR20040066856A (es)
AR (1) AR037973A1 (es)
AU (1) AU2002356762A1 (es)
BR (1) BR0215294A (es)
CA (1) CA2471524A1 (es)
DE (1) DE10163992A1 (es)
MX (1) MXPA04006193A (es)
PL (1) PL369855A1 (es)
WO (1) WO2003055490A1 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10043667A1 (de) * 2000-09-05 2002-03-14 Merck Patent Gmbh 2-Guanidino-4-aryl-chinazoline
US8508508B2 (en) 2003-02-14 2013-08-13 Next Holdings Limited Touch screen signal processing with single-point calibration
US7629967B2 (en) * 2003-02-14 2009-12-08 Next Holdings Limited Touch screen signal processing
US8456447B2 (en) 2003-02-14 2013-06-04 Next Holdings Limited Touch screen signal processing
DE10312963A1 (de) * 2003-03-24 2004-10-07 Aventis Pharma Deutschland Gmbh Substituierte 4-Phenyltetrahydroisochinoline, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, sowie sie enthaltendes Medikament
US7241775B2 (en) 2003-03-24 2007-07-10 Sanofi-Aventis Deutschland Gmbh Composition, process of making, and medical use of substituted 4-phenyltetrahydroisoquinolines
US7538759B2 (en) 2004-05-07 2009-05-26 Next Holdings Limited Touch panel display system with illumination and detection provided from a single edge
GB0526515D0 (en) * 2005-12-28 2006-02-08 Merck Sharp & Dohme Modulation of signalling pathways
WO2008094706A2 (en) * 2007-02-01 2008-08-07 Cook Incorporated Closure device and method of closing a bodily opening
US8115753B2 (en) * 2007-04-11 2012-02-14 Next Holdings Limited Touch screen system with hover and click input methods
US8432377B2 (en) * 2007-08-30 2013-04-30 Next Holdings Limited Optical touchscreen with improved illumination
KR20100075460A (ko) 2007-08-30 2010-07-02 넥스트 홀딩스 인코포레이티드 저 프로파일 터치 패널 시스템
US20090213093A1 (en) * 2008-01-07 2009-08-27 Next Holdings Limited Optical position sensor using retroreflection
US20090207144A1 (en) * 2008-01-07 2009-08-20 Next Holdings Limited Position Sensing System With Edge Positioning Enhancement
US8405636B2 (en) * 2008-01-07 2013-03-26 Next Holdings Limited Optical position sensing system and optical position sensor assembly
WO2010039663A2 (en) * 2008-10-02 2010-04-08 Next Holdings, Inc. Stereo optical sensors for resolving multi-touch in a touch detection system
JP5502106B2 (ja) 2008-12-31 2014-05-28 アーデリクス,インコーポレーテッド 体液貯留または塩分過負荷と関連する障害および消化管障害の治療におけるnhe媒介性アンチポートを阻害するための組成物および方法
WO2018129556A1 (en) 2017-01-09 2018-07-12 Ardelyx, Inc. Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
US20120088737A2 (en) * 2009-10-02 2012-04-12 Ajinomoto Co., Inc Novel acyl guanidine derivatives
US20110199387A1 (en) * 2009-11-24 2011-08-18 John David Newton Activating Features on an Imaging Device Based on Manipulations
US20110221666A1 (en) * 2009-11-24 2011-09-15 Not Yet Assigned Methods and Apparatus For Gesture Recognition Mode Control
EP2507683A1 (en) * 2009-12-04 2012-10-10 Next Holdings Limited Methods and systems for position detection using an interactive volume
US20110234542A1 (en) * 2010-03-26 2011-09-29 Paul Marson Methods and Systems Utilizing Multiple Wavelengths for Position Detection
US10376481B2 (en) 2012-08-21 2019-08-13 Ardelyx, Inc. Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
CA2880338A1 (en) 2012-08-21 2014-02-27 Ardelyx, Inc. Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
CA2909169A1 (en) 2013-04-12 2014-10-16 Ardelyx, Inc. Nhe3-binding compounds and methods for inhibiting phosphate transport
RS58378B1 (sr) 2014-07-25 2019-04-30 Taisho Pharmaceutical Co Ltd Fenil tetrahidroizokvinolinsko jedinjenje supstituisano heteroarilom
UA126283C2 (uk) 2017-01-09 2022-09-14 Арделікс, Інк. Сполуки, придатні для лікування розладів шлунково-кишкового тракту
MX2019008171A (es) 2017-01-09 2020-02-05 Ardelyx Inc Inhibidores del antiporte mediado por nhe.
EP4397366A2 (en) 2017-08-04 2024-07-10 Ardelyx, Inc. Glycyrrhetinic acid derivatives for treating hyperkalemia
CA3129233A1 (en) 2019-02-07 2020-08-13 Ardelyx, Inc. Glycyrrhetinic acid derivatives for use in treating hyperkalemia
JP2022533251A (ja) 2019-05-21 2022-07-21 アルデリックス, インコーポレイテッド 患者において血清リン酸塩を低下させるための組み合わせ

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3131187A (en) * 1964-04-28 Certain z-guantoino-x-aryl-quinazolines
FR2460224A1 (fr) * 1979-06-29 1981-01-23 Renault Regulateur d'allure pour vehicule automobile
FR2685667B1 (fr) * 1991-12-26 1994-07-29 Landerretche Alain Dispositif d'assistance au controle de la puissance de vehicules equipes d'un moteur a combustion interne.
DE10019062A1 (de) * 2000-04-18 2001-10-25 Merck Patent Gmbh 2-Guanidino-4-aryl-chinazoline als NHE-3 Inhibitoren
DE10043667A1 (de) * 2000-09-05 2002-03-14 Merck Patent Gmbh 2-Guanidino-4-aryl-chinazoline

Also Published As

Publication number Publication date
US20050020612A1 (en) 2005-01-27
EP1458396A1 (de) 2004-09-22
BR0215294A (pt) 2005-02-09
KR20040066856A (ko) 2004-07-27
MXPA04006193A (es) 2004-12-06
AU2002356762A1 (en) 2003-07-15
PL369855A1 (en) 2005-05-02
WO2003055490A1 (de) 2003-07-10
DE10163992A1 (de) 2003-07-03
CA2471524A1 (en) 2003-07-10

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