AR071586A1 - Tienopirimidinas - Google Patents

Tienopirimidinas

Info

Publication number
AR071586A1
AR071586A1 ARP090101244A ARP090101244A AR071586A1 AR 071586 A1 AR071586 A1 AR 071586A1 AR P090101244 A ARP090101244 A AR P090101244A AR P090101244 A ARP090101244 A AR P090101244A AR 071586 A1 AR071586 A1 AR 071586A1
Authority
AR
Argentina
Prior art keywords
hal
mono
trisubstituted
atoms
alko
Prior art date
Application number
ARP090101244A
Other languages
English (en)
Inventor
Christiane Amendt
Guenter Hoelzemann
Hartmut Greiner
Frank Zenke
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 AR071586A1 publication Critical patent/AR071586A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Las tienopirimidinas de la formula 1 en donde R1 es benzofuranilo, benzotiazolilo, benzotiofenilo, imidazo[1,2a)piridina, quinolinilo, isoquinolinilo o furanilo no sustituido o mono-, di- o trisustituido con A y/o Hal, o piridinilo mono-, di- o trisustituido con A y/o Hal, R2 es H, Alk, Het1, Cyc, AlkNH2, AlkNHA, AlkNAA', AlkOH, AlkOA, AlkCyc, AlkHet1, AlkOAlkOH, AlkO(CH2)mNAA', AlkCHOH(CH2)mOH, AlkO(CH2)mHet1, AlkAr o AlkO(CH2)mAr, X es un enlace simple, NH, S o SO2, Alk es alquileno o alquinilo C1-6, en donde 1 a 4 átomos de H pueden estar sustituidos con F, Cl, Br y/o CN, Cyc es cicloalquilo C3-7, en donde 1 a 4 átomos de H pueden estar reemplazados por A, Hal, OH y/u OA; Het1 es un heterociclo saturado, insaturado o aromático mono- o bicíclico con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con A, OH, OA, Hal, SO2A y/u =O (oxígeno del carbonilo), Ar es fenilo, que no está sustituido o que está mono-, di- o trisustituido con A, OH, OA, Hal, SO2NH2, SO2NA y/o SO2NAA', A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 que pueden estar reemplazados, de modo independiente entre sí, por grupos -CH=CH- y/o -C:::C- y/o 1-5 átomos de H pueden estar reemplazados por F, Cl y/o Br, Hal es F, Cl, Br o I, m es 1,2, 3 o 4, así como sus derivados, sales, solvatos, tautomeros y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones, procedimiento de preparacion, composicion farmacéutica y uso como inhibidores de la quinasa del receptor TGF-beta, y se pueden emplear, por ejemplo, para el tratamiento de tumores.
ARP090101244A 2008-04-09 2009-04-08 Tienopirimidinas AR071586A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102008017853A DE102008017853A1 (de) 2008-04-09 2008-04-09 Thienopyrimidine

Publications (1)

Publication Number Publication Date
AR071586A1 true AR071586A1 (es) 2010-06-30

Family

ID=40765631

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090101244A AR071586A1 (es) 2008-04-09 2009-04-08 Tienopirimidinas

Country Status (15)

Country Link
US (1) US20110028472A1 (es)
EP (1) EP2260044A2 (es)
JP (1) JP2011518132A (es)
KR (1) KR20110010721A (es)
CN (1) CN102015724A (es)
AR (1) AR071586A1 (es)
AU (1) AU2009235729A1 (es)
BR (1) BRPI0911364A2 (es)
CA (1) CA2720878A1 (es)
DE (1) DE102008017853A1 (es)
EA (1) EA201001576A1 (es)
IL (1) IL208066A0 (es)
MX (1) MX2010011015A (es)
WO (1) WO2009124653A2 (es)
ZA (1) ZA201007979B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2445916A1 (en) * 2009-06-22 2012-05-02 Merck Patent GmbH Alkoxy-thienopyrimidines as tgf-beta receptor kinase modulators
CN102596961B (zh) 2009-10-30 2015-12-02 詹森药业有限公司 咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途
CA2789021C (en) 2010-02-05 2018-02-06 Merck Patent Gmbh Hetaryl-[1,8]naphthyridine derivatives
ES2528441T3 (es) 2010-02-22 2015-02-10 Merck Patent Gmbh Hetarilaminonaftiridinas
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
ES2575092T3 (es) 2011-06-27 2016-06-24 Janssen Pharmaceutica, N.V. Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxalina
FR2988722B1 (fr) 2012-04-03 2014-05-09 Sanofi Sa Nouveaux derives de thienopyrimidines, leurs procedes de preparation et leurs utilisations therapeutiques
EP2863909B1 (en) 2012-06-26 2020-11-04 Janssen Pharmaceutica N.V. Combinations comprising 4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline compounds as pde 2 inhibitors and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders
EP2869822B1 (en) 2012-07-09 2016-09-14 Janssen Pharmaceutica, N.V. Inhibitors of phosphodiesterase 10 enzyme

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
JPWO2005080377A1 (ja) * 2004-02-20 2007-10-25 キリンホールディングス株式会社 TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
WO2006090094A1 (en) * 2005-02-28 2006-08-31 Vernalis R & D Ltd Pyrimidothiophene compounds for use as hsp90 inhibitors
DE102005013621A1 (de) * 2005-03-24 2006-09-28 Curacyte Discovery Gmbh Substituierte 2-Aryl(Hetaryl)-5-aminothieno[2,3-d]pyrimidin-6-carbonsäureamide, Verfahren zu ihrer Herstellung und Verwendung als Pharmazeutika
JP2009523805A (ja) * 2006-01-17 2009-06-25 シグナル ファーマシューティカルズ,エルエルシー TNFα、PDE4及びB−RAFの阻害剤、それらの組成物及びそれらの使用法
WO2008020622A1 (fr) * 2006-08-17 2008-02-21 Kyorin Pharmaceutical Co., Ltd. NOUVEAU COMPOSÉ DE THIÉNO[2,3-d]PYRIMIDINE

Also Published As

Publication number Publication date
DE102008017853A1 (de) 2009-10-15
AU2009235729A1 (en) 2009-10-15
ZA201007979B (en) 2011-07-27
US20110028472A1 (en) 2011-02-03
KR20110010721A (ko) 2011-02-07
EP2260044A2 (de) 2010-12-15
WO2009124653A2 (de) 2009-10-15
CN102015724A (zh) 2011-04-13
JP2011518132A (ja) 2011-06-23
EA201001576A1 (ru) 2011-04-29
BRPI0911364A2 (pt) 2015-12-29
MX2010011015A (es) 2010-11-22
IL208066A0 (en) 2010-12-30
WO2009124653A3 (de) 2009-12-03
CA2720878A1 (en) 2009-10-15

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