HUP0401654A2 - Heterokondenzált pirimidinszármazékok, intermedierjeik, a vegyületek előállítása és az ezeket tartalmazó gyógyszerkészítmények - Google Patents

Heterokondenzált pirimidinszármazékok, intermedierjeik, a vegyületek előállítása és az ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0401654A2
HUP0401654A2 HU0401654A HUP0401654A HUP0401654A2 HU P0401654 A2 HUP0401654 A2 HU P0401654A2 HU 0401654 A HU0401654 A HU 0401654A HU P0401654 A HUP0401654 A HU P0401654A HU P0401654 A2 HUP0401654 A2 HU P0401654A2
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Hungary
Prior art keywords
group
general formula
hal
compounds
alkyl
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HU0401654A
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English (en)
Inventor
Hans-Michael Eggenweiler
Manfred Baumgarth
Pierre Schelling
Norbert Beier
Maria Christadler
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Merck Patent Gmbh
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Publication of HUP0401654A2 publication Critical patent/HUP0401654A2/hu
Publication of HUP0401654A3 publication Critical patent/HUP0401654A3/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Nutrition Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

A találmány az (I) általános képletű vegyületekre, gyógyászatilagalkalmazható származékaikra, szolvátjaikra, sztereoizomerjeikre ésezek tetszőleges arányú keverékeire, előállításukra, valamint avegyületeket tartalmazó gyógyszerkészítményekre vonatkozik. Az (I)általános képletben R1 és R2 jelentése H, A, OH, OA vagy Hal, vagy R1és R2 együttes jelentése alkiléncsoport, -O-CH2-CH2-, -CH2-O-CH2-, -O-CH2-O- vagy jelentése -O-CH2-CH2-O- képletű csoport; R3 és R4jelentése H, A vagy Hal vagy R3 <>és R4 együttes jelentése alkilén-vagy alkilidéncsoport vagy (a) általános képletű csoport; W jelentéseH vagy alkilcsoport; X jelentése CH vagy NA'; Y jelentése -(CH2)qR7vagy R5, R6 vagy R9, amely csoportok egy -(CH2)nR20 általános képletűcsoporttal lehetnek helyettesítve; Z jelentése O, NH vagy NA; A'jelentése alkilcsoport, -CHAr vagy -CHAr-A" általános képletű csoport;A< jelentése alkilcsoport; R5 jelentése alkilcsoport, amelyben egyvagy két CH2 csoport helyén -CH=CH-, -C=C- csoport, -O-, -CO-, -S- -SO-, -SO2-, -NH- képletű vagy -NA- általános képletű csoport állhat;R6 jelentése cikloalkil vagy cikloalkil-alkilén-csoport, R7 jelentésetelített vagy telítetlen 5-7 tagú, 1-4 N, O vagy S atomot tartalmazóheterociklusos csoport, amely R20, A, Hal vagy CF3 csoportokkal lehethelyettesítve; R9 jelentése Ar vagy (CH2)k-Ar; Rl0, R11 R12 és R13jelentése H, A, Hal, OA, OH, NH2, NHA, NA2 vagy R20; R20 jelentése -COOH, -COOA, -CONH2, -CONHA, -CONA2, -CN, tetrazol-5-il- képletű vagy-S(O)mA, -S(O)mNH2 vagy S(O)mOH általános képletű csoport vagy (b),(c), (d) vagy (e) képletű csoport; A jelentése alkil- vagyalkenilcsoport, amelyben 1-7 hidrogénatom helyén F- atom állhat; Arjelentése fenilcsoport, amely adott esetben Hal, A, OA, OH, SO2NH2,SO2NHA, SO2NA2 vagy CN csoporttal lehet helyettesítve; Hal jelentéseF,Cl, Br vagy I; k és q jelentése 0, 1, 2, 3, vagy 4; m jelentése 1 vagy2; és n jelentése 0, 1, 2 vagy 3. Az (I) általános képletű vegyületekcGMP foszfodiészteráz gátló hatásúak, így különösen szív- ésérrendszeri megbetegedések kezelésére alkalmas gyógyszerekelőállítására alkalmazhatók. A találmány tárgya továbbá a (II)általános képletű intermedierek - ahol Y, Z, R3 és R4 jelentése, afentebb megadott L jelkentése pedig Cl, Br, OH, SCH3 vagy reaktívészterezett OH-csoport - melyekből az (I) általános képletű vegyületekelőállíthatók. Ó
HU0401654A 2001-10-04 2002-09-05 Heterokondensated pyrimidine derivatives, their intermediates, preparations of the compounds and pharmaceutical compositions containing them HUP0401654A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10148883A DE10148883A1 (de) 2001-10-04 2001-10-04 Pyrimidinderivate
PCT/EP2002/009935 WO2003031447A2 (de) 2001-10-04 2002-09-05 Pyrimidinderivate mit pde-v hemmender wirkung

Publications (2)

Publication Number Publication Date
HUP0401654A2 true HUP0401654A2 (hu) 2004-11-29
HUP0401654A3 HUP0401654A3 (en) 2006-02-28

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HU0401654A HUP0401654A3 (en) 2001-10-04 2002-09-05 Heterokondensated pyrimidine derivatives, their intermediates, preparations of the compounds and pharmaceutical compositions containing them

Country Status (16)

Country Link
US (1) US7312224B2 (hu)
EP (1) EP1432715B1 (hu)
JP (1) JP4782376B2 (hu)
KR (1) KR20040041166A (hu)
CN (1) CN1863803A (hu)
AT (1) ATE389655T1 (hu)
AU (1) AU2002362806B2 (hu)
BR (1) BR0213037A (hu)
CA (1) CA2462799C (hu)
DE (2) DE10148883A1 (hu)
ES (1) ES2303564T3 (hu)
HU (1) HUP0401654A3 (hu)
PL (1) PL369819A1 (hu)
RU (1) RU2004114239A (hu)
WO (1) WO2003031447A2 (hu)
ZA (1) ZA200403334B (hu)

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DE102005061170A1 (de) * 2005-12-21 2007-07-05 Bayer Healthcare Ag Neue, acyclisch substituierte Furopyrimidin-Derivate und ihre Verwendung
DE102005061171A1 (de) * 2005-12-21 2007-07-05 Bayer Healthcare Ag Neue, cyclisch substituierte Furopyrimidin-Derivate und ihre Verwendung
AR062501A1 (es) * 2006-08-29 2008-11-12 Actelion Pharmaceuticals Ltd Composiciones terapeuticas
JP5284977B2 (ja) * 2006-12-07 2013-09-11 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ホスホイノシチド３−キナーゼ阻害剤化合物及び使用方法
DE102007027799A1 (de) * 2007-06-16 2008-12-18 Bayer Healthcare Ag Substituierte Furopyrimidine und ihre Verwendung
DE102007027800A1 (de) * 2007-06-16 2008-12-18 Bayer Healthcare Ag Substituierte bicyclische Heteroaryl-Verbindungen und ihre Verwendung
DE102007051762A1 (de) * 2007-10-30 2009-05-07 Bayer Healthcare Ag Substituierte Pyrrolotriazine und ihre Verwendung
DE102007054786A1 (de) * 2007-11-16 2009-05-20 Bayer Healthcare Ag Trisubstituierte Furopyrimidine und ihre Verwendung
WO2011143607A1 (en) * 2010-05-14 2011-11-17 The Regents Of The University Of California Modulation of bioactive epoxy-fatty acid levels by phosphodiesterase inhibitors
AU2011281015B2 (en) 2010-07-23 2015-09-24 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
EP2806875B1 (en) * 2012-01-25 2017-07-19 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
WO2016042349A1 (en) 2014-09-17 2016-03-24 Pécsi Tudományegyetem New agents for treating neurogenic inflammation and neuropathic hyperalgesia related disorders
US10813894B2 (en) 2015-02-20 2020-10-27 The Regents Of The University Of California Methods of inhibiting pain
CN108137614B (zh) * 2015-12-02 2021-01-05 深圳市塔吉瑞生物医药有限公司 一种稠合嘧啶化合物及包含该化合物的组合物及其用途
CN105461728A (zh) * 2015-12-29 2016-04-06 中山大学 一种4-取代胺基-6-甲氧羰基苯并呋喃并[2,3-d]嘧啶类化合物及制备方法
RU2625316C1 (ru) * 2016-04-13 2017-07-13 Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) 2-АМИНОЗАМЕЩЕННЫЕ 6-МЕТОКСИ-4-ТРИФТОРМЕТИЛ-9Н-ПИРИМИДО[4,5b]ИНДОЛЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ПРИМЕНЕНИЕ И ПРЕДШЕСТВЕННИКИ

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ATE389655T1 (de) 2008-04-15
EP1432715B1 (de) 2008-03-19
RU2004114239A (ru) 2005-10-27
WO2003031447A3 (de) 2003-08-28
JP4782376B2 (ja) 2011-09-28
WO2003031447A2 (de) 2003-04-17
CA2462799C (en) 2010-11-02
JP2005504847A (ja) 2005-02-17
PL369819A1 (en) 2005-05-02
ZA200403334B (en) 2006-05-31
KR20040041166A (ko) 2004-05-14
CA2462799A1 (en) 2003-04-17
EP1432715A2 (de) 2004-06-30
AU2002362806B2 (en) 2008-09-18
DE10148883A1 (de) 2003-04-10
US20040242595A1 (en) 2004-12-02
BR0213037A (pt) 2004-10-05
ES2303564T3 (es) 2008-08-16
CN1863803A (zh) 2006-11-15
DE50211929D1 (en) 2008-04-30
HUP0401654A3 (en) 2006-02-28
US7312224B2 (en) 2007-12-25

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