EP1654237A1 - Derives de 2-aminopyrimidine - Google Patents

Derives de 2-aminopyrimidine

Info

Publication number
EP1654237A1
EP1654237A1 EP04763418A EP04763418A EP1654237A1 EP 1654237 A1 EP1654237 A1 EP 1654237A1 EP 04763418 A EP04763418 A EP 04763418A EP 04763418 A EP04763418 A EP 04763418A EP 1654237 A1 EP1654237 A1 EP 1654237A1
Authority
EP
European Patent Office
Prior art keywords
amino
alkyl
halogen
phenyl
hydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP04763418A
Other languages
German (de)
English (en)
Inventor
Hiroki Sato
Keiko Fukushima
Makoto Shimazaki
Klaus Urbahns
Katsuya Sakai
Florian Ganter
Kevin c/o Actimis Pharmaceuticals BACON
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer AG
Original Assignee
Bayer Healthcare 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
Application filed by Bayer Healthcare AG filed Critical Bayer Healthcare AG
Priority to EP04763418A priority Critical patent/EP1654237A1/fr
Publication of EP1654237A1 publication Critical patent/EP1654237A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

Definitions

  • Rb 2 is halogen, alkyl, OH, (un)substituted heteroaryl, (un)substituted heterocyclyl, etc;
  • WOOl/062233 discloses pyrimidine derivatives represented by the general formula:
  • R 11 and R 12 independently represent hydrogen or C 1-6 alkyl optionally substituted by halogen, cyano, hydroxy, carboxy, amino, Ci- ⁇ alkylamino, N,N-di(C ⁇ - 6 alkyl)arnino, Ci. 6 alkylthio, C ⁇ -6 alkoxy, or C 3-8 cycloalkyl; and
  • the compound of the formula (I) of the present invention can be, but not limited to be, prepared by combining various known methods.
  • one or more of the substituents, such as amino group, carboxyl group, and hydroxyl group of the compounds used as starting materials or intermediates are advantageously protected by a protecting group known to those skilled in the art. Examples of the protecting groups are described in "Protective Groups in Organic Synthesis (3rd Edition)" by Greene and Wuts, John Wiley and Sons, New York 1999.
  • the compound of the formula (I) of the present invention can be, but not limited to be, prepared by the Method [A] and [B] below.
  • compound of formula (XIII) (wherein R 2 is the same as defined above) can be prepared by the oxidation of sulfur atom of compound of formula (XII) (wherein R 2 is the same as defined above) .
  • the carrier may be a finely divided solid which is in admixture with the finely divided active ingredient.
  • the active ingredient may be mixed with a carrier having binding properties in suitable proportions and compacted in the shape and size desired to produce tablets.
  • the powders and tablets preferably contain from about 1 to about 99 weight percent of the active ingredient which is the novel composition of the present invention.
  • Suitable solid carriers are magnesium carboxymethyl cellulose, low melting waxes, and cocoa butter.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne de nouveaux dérivés de 2-aminopyrimidine, ainsi que des procédés de préparation de ces dérivés et de compositions pharmaceutiques les contenant. Ces dérivés présentent une puissance accrue d'antagonisme du récepteur H4 de l'histamine, et peuvent être utilisés dans la prévention et le traitement de maladies liées à l'activité du récepteur H4 de l'histamine. Les dérivés de 2-aminopyrimidine selon l'invention sont utiles en particulier dans la prévention et le traitement des maladies suivantes : l'asthme, la rhinite, les maladies allergiques, la broncho-pneumopathie chronique obstructive (BPCO), l'athérosclérose et la polyarthrite rhumatoïde.
EP04763418A 2003-08-05 2004-07-23 Derives de 2-aminopyrimidine Withdrawn EP1654237A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP04763418A EP1654237A1 (fr) 2003-08-05 2004-07-23 Derives de 2-aminopyrimidine

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP03017810A EP1505064A1 (fr) 2003-08-05 2003-08-05 Dérivés de 2-aminopyrimidine
PCT/EP2004/008225 WO2005014556A1 (fr) 2003-08-05 2004-07-23 Derives de 2-aminopyrimidine
EP04763418A EP1654237A1 (fr) 2003-08-05 2004-07-23 Derives de 2-aminopyrimidine

Publications (1)

Publication Number Publication Date
EP1654237A1 true EP1654237A1 (fr) 2006-05-10

Family

ID=33547634

Family Applications (2)

Application Number Title Priority Date Filing Date
EP03017810A Withdrawn EP1505064A1 (fr) 2003-08-05 2003-08-05 Dérivés de 2-aminopyrimidine
EP04763418A Withdrawn EP1654237A1 (fr) 2003-08-05 2004-07-23 Derives de 2-aminopyrimidine

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP03017810A Withdrawn EP1505064A1 (fr) 2003-08-05 2003-08-05 Dérivés de 2-aminopyrimidine

Country Status (2)

Country Link
EP (2) EP1505064A1 (fr)
WO (1) WO2005014556A1 (fr)

Families Citing this family (36)

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US20070265289A1 (en) * 2004-04-15 2007-11-15 Yoshinori Okamoto 2-Aminopyrimidine Derivative
CA2622372A1 (fr) * 2005-09-13 2007-03-22 Palau Pharma, S.A. Derives de 2-aminopyrimidine en tant que modulateurs de l'activite du recepteur h4 de l'histamine
EP1767537A1 (fr) * 2005-09-21 2007-03-28 Cellzome (UK) Ltd. Dérivés de pyrimidine pour le traitement de troubles inflammatoires
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
EP1860109A1 (fr) * 2006-05-24 2007-11-28 Cellzome (UK) Ltd. Composés d'amino pyrimidine substitués avec une azetidine pour traiter les maladies inflammatoires
WO2007090853A1 (fr) * 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomères de composes d'amino pyrimidine destinés à traiter des troubles inflammatoires
WO2007090854A1 (fr) * 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Composés d'amino pyrimidine d'azétidine destinés à traiter des troubles inflammatoires
EP1860108A1 (fr) * 2006-05-24 2007-11-28 Cellzome (UK) Ltd. Enantiomères d'aminopyrimidines utilisés dans le traitement de maladies inflammatoires.
EP2010172B1 (fr) * 2006-04-07 2012-08-29 Janssen Pharmaceutica N.V. Indoles et benzoimidazoles modulateurs du récepteur de l'histamine h4
US20100035863A1 (en) * 2006-09-12 2010-02-11 Ucb Pharma, S.A. 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions
US7985745B2 (en) 2006-10-02 2011-07-26 Abbott Laboratories Method for pain treatment
CL2008000467A1 (es) * 2007-02-14 2008-08-22 Janssen Pharmaceutica Nv Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
WO2008122378A1 (fr) * 2007-04-04 2008-10-16 Ucb Pharma, S.A. Nouveaux derives de pyridine, procedes de preparation et compositions pharmaceutiques associes
CA2705719C (fr) 2007-09-14 2016-10-11 Janssen Pharmaceutica N.V. Modulateurs du recepteur d'histamine h<sb>4</sb> de types thieno- et furo-pyrimidine
US20100298289A1 (en) * 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
WO2009068512A1 (fr) * 2007-11-30 2009-06-04 Palau Pharma, S. A. Dérivés de 2-aminopyrimidine en tant qu'antagonistes d'histamine h4
PE20091524A1 (es) * 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina
CN101903385B (zh) * 2007-12-21 2013-11-06 帕劳制药股份有限公司 作为组胺h4受体拮抗剂的4-氨基嘧啶衍生物
US8436005B2 (en) * 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
MX2010013726A (es) 2008-06-12 2011-01-14 Janssen Pharmaceutica Nv Moduladores de diamino-piridina, pirimidina, y piridazina del receptor h4 de histamina.
WO2010075270A1 (fr) 2008-12-22 2010-07-01 Incyte Corporation 2-amino-pyrimidines 4,6-disubstituées, convenant comme modulateurs du récepteur h4 de l'histamine
EP2201982A1 (fr) 2008-12-24 2010-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Antagonistes du récepteur H4 de l'histamine pour le traitement de troubles vestibulaires
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
TW201035078A (en) 2009-03-20 2010-10-01 Incyte Corp Substituted heterocyclic compounds
ES2629006T3 (es) 2009-10-29 2017-08-07 Vectura Limited Derivados que contienen N-heteroarilo como inhibidores de la quinasa jak3
WO2011076878A1 (fr) * 2009-12-23 2011-06-30 Palau Pharma, S.A. Dérivés d'aminoalkylpyrimidine au titre d'antagonistes du récepteur histaminique h4
PH12012501556A1 (en) 2009-12-30 2012-10-22 Arqule Inc Substituted naphthalenyl-pyrimidine compounds
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー ＣＲＦ−１受容体アンタゴニストとしてのピラゾロ［５，１ｂ］オキサゾール誘導体
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Ｃｒｆ受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
UY34094A (es) 2011-05-27 2013-01-03 Novartis Ag Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina
CA2867043A1 (fr) 2012-05-03 2013-11-07 Novartis Ag Sel de l-malate de derives de 2,7-diaza-spiro[4.5]dec-7-yle et ses formes cristallines a titre d'agonistes des recepteurs de ghreline
HUE039713T2 (hu) 2012-06-08 2019-02-28 Sensorion H4 receptor inhibitorok tinnitus kezelésére
KR20180100705A (ko) * 2016-01-29 2018-09-11 메이지 세이카 파루마 가부시키가이샤 신규 화합물 및 이의 약학적으로 허용 가능한 염
CA3240192A1 (fr) * 2021-12-09 2023-06-15 Daniel L. Flynn Inhibiteurs de kinase raf et leurs procedes d'utilisation

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US5256659A (en) * 1989-01-09 1993-10-26 Janssen Pharmaceutica N.V. 2-aminopyrimidinone derivatives
GB9012311D0 (en) * 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
WO2001062233A2 (fr) * 2000-02-25 2001-08-30 F. Hoffmann La Roche Ag Modulateurs de recepteurs de l'adenosine
WO2002096867A2 (fr) * 2001-05-30 2002-12-05 Lg Biomedical Institute Inhibiteurs de la proteine kinase destines au traitement d'une maladie

Non-Patent Citations (1)

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Also Published As

Publication number Publication date
EP1505064A1 (fr) 2005-02-09
WO2005014556A1 (fr) 2005-02-17

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Inventor name: SAKAI, KATSUYA

Inventor name: SATO, HIROKI

Inventor name: URBAHNS, KLAUS

Inventor name: FUKUSHIMA, KEIKO

Inventor name: GANTNER, FLORIAN

Inventor name: SHIMAZAKI, MAKOTO

Inventor name: BACON, KEVIN C/O ACTIMIS PHARMACEUTICALS

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Inventor name: SHIMAZAKI, MAKOTO

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Inventor name: FUKUSHIMA, KEIKO

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