HUP0202713A2 - Kináz inhibitorokként alkalmazható pteridinonok - Google Patents

Kináz inhibitorokként alkalmazható pteridinonok

Info

Publication number
HUP0202713A2
HUP0202713A2 HU0202713A HUP0202713A HUP0202713A2 HU P0202713 A2 HUP0202713 A2 HU P0202713A2 HU 0202713 A HU0202713 A HU 0202713A HU P0202713 A HUP0202713 A HU P0202713A HU P0202713 A2 HUP0202713 A2 HU P0202713A2
Authority
HU
Hungary
Prior art keywords
group
alkyl
optionally substituted
aryl
amino
Prior art date
Application number
HU0202713A
Other languages
English (en)
Inventor
Williams Alexander Denny
Ellen Myra Dobrusin
James Bernard Kramer
Dennis Joseph Mcnamara
Gordon William Rewcastle
Howard Daniel Hollis Showalter
Peter Laurence Toogood
Original Assignee
Warner-Lambert Co.
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 Warner-Lambert Co. filed Critical Warner-Lambert Co.
Publication of HUP0202713A2 publication Critical patent/HUP0202713A2/hu
Publication of HUP0202713A3 publication Critical patent/HUP0202713A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring 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
    • 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
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biotechnology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)

Abstract

A találmány (Ia), (Ib , (Ic), (Id) és (Ie) általános képletűvegyületekre és gyógyászatilag elfogadható sóikra, észtereikre,amidjaikra és prodrogjaikra vonatkozik, ahol az általános képletekben W NH, O, S, SO vagy S02 csoport; R2 alkil-, alkenil-, alkinil-, cikloalkil-, aril-(CH2)n-, -COR4, heteroaril- (CH2)n- vagy heterociklil-(CH2)n- képletű csoport, ahol az előbbi alkil-, alkenil-, alkinil-, cikloalkil-, aril-, heteroaril- és heterociklilcsoportok mindegyike adott esetben szubsztituált; R4, R6, R6' és R9 jelentése (a) hidrogén-, halogénatom, alkil-, alkoxicsoport, szubsztituált alkilcsoport, alkenil-(CH2)n-, alkinil(CH2)n-, ciano-(CH2)n-, amino-, amino-alkoxi-, fenoxi-, hidroxi-, trifluor-metil-, mono- vagy dialkil-amino-, (mono- vagy dialkil-amino)- alkoxi-, merkapto-, alkil-tio-, ciano-, nitro-, karboxilcsoport, észteresített karboxilcsoport, szubsztituált karbamoilcsoport, -S03Z, -P03Z, amino-alkanoil-, karbamoil-,[amino-(3-7 szénatomos cikloalkil)]-karbonil-, valamint (alkil-amino)-karbonil- és (dialkil-amino)-karbonil-csoport: (b) aril-(CH2)n-, heteroaril-(CH2)n-, aril-alkil- vagy heteroaril-alkil-csoport, ahol valamennyi aril- és heteroarilcsoport adott esetben szubsztituált; R8 jelentése (a) hidrogénatom, alkil-, szubsztituált alkil-, alkenil- (CH2)n-, alkinil-(CH2)n- csoport vagy egy olyan karbocikil- (CH2)n- csoport, amelyben a karbociklusos csoport 3-7 tagú, ahol a gyűrűtagok közül legfeljebb kettő oxigén- és/vagy nitrogénatom, és ahol a karbociklusos csoport adott esetben szubsztituált; (b) aril- (CH2)n-, heteroaril-(CH2)n-, aril- alkil- vagy heteroaril-alkil-csoport, ahol az aril- vagy heteroarilcsoportok mindegyike adott esetben szubsztituált; Z jelentése hidrogénatom, alkilcsoport, szubsztituált alkilcsoport, hidroxi-, alkoxi-, amino-, alkil-amino-, dialkil-amino-csoport, adott esetben szubsztituált piperidilcsoport, adott esetben szubsztituált morfolinilcsoport vagy adott esetben szubsztituált piperazinilcsoport; és n értéke 0, 1, 2, 3, 4, 5 vagy 6; azzal a megkötéssel, hogy R8 jelentése hidrogénatomtól vagy 1-3 szénatomos alkilcsoporttól eltérő, ha R2 jelentése metil-, etil- vagy acetilcsoport. A találmány olyan 8H- pteridin-8-on-, tetrahidropteridin-7-on-, 5H,8H-pteridin-6,7- dion- és pteridin-7-karbamid-származékokra vonatkozik, amelyek gátolják a ciklinfüggő szerin/treonin-kinázt, a Wee 1 tirozin-kinázt, valamint a növekedési faktor által mediált tirozin-kináz enzimet, és amelyek így fel
HU0202713A 1999-09-15 2000-06-21 Pteridinones as kinase inhibitors HUP0202713A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15409599P 1999-09-15 1999-09-15
PCT/US2000/017037 WO2001019825A1 (en) 1999-09-15 2000-06-21 Pteridinones as kinase inhibitors

Publications (2)

Publication Number Publication Date
HUP0202713A2 true HUP0202713A2 (hu) 2002-12-28
HUP0202713A3 HUP0202713A3 (en) 2005-02-28

Family

ID=22549985

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0202713A HUP0202713A3 (en) 1999-09-15 2000-06-21 Pteridinones as kinase inhibitors

Country Status (29)

Country Link
US (2) US7169778B2 (hu)
EP (1) EP1409487A1 (hu)
JP (1) JP2003509425A (hu)
KR (1) KR20020027649A (hu)
CN (1) CN1373763A (hu)
AP (1) AP2002002479A0 (hu)
AU (1) AU777468B2 (hu)
BG (1) BG106594A (hu)
BR (1) BR0013952A (hu)
CA (1) CA2393896A1 (hu)
CR (1) CR6586A (hu)
CZ (1) CZ2002846A3 (hu)
DZ (1) DZ3186A1 (hu)
EA (1) EA005287B1 (hu)
EE (1) EE200200140A (hu)
HK (1) HK1048992A1 (hu)
HU (1) HUP0202713A3 (hu)
IL (1) IL148614A0 (hu)
IS (1) IS6298A (hu)
MA (1) MA26819A1 (hu)
MX (1) MXPA02001108A (hu)
NO (1) NO20021239D0 (hu)
NZ (1) NZ516872A (hu)
OA (1) OA12010A (hu)
PL (1) PL353269A1 (hu)
SK (1) SK3542002A3 (hu)
WO (1) WO2001019825A1 (hu)
YU (1) YU18502A (hu)
ZA (1) ZA200200896B (hu)

Families Citing this family (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7276506B2 (en) 1998-12-28 2007-10-02 4 Aza Bioscience Nv Immunosuppressive effects of pteridine derivatives
SE9903544D0 (sv) 1999-10-01 1999-10-01 Astra Pharma Prod Novel compounds
GB2359081A (en) 2000-02-11 2001-08-15 Astrazeneca Uk Ltd Pharmaceutically active thiazolopyrimidines
GB2359078A (en) 2000-02-11 2001-08-15 Astrazeneca Uk Ltd Pharmaceutically active pyrimidine derivatives
GB2359551A (en) * 2000-02-23 2001-08-29 Astrazeneca Uk Ltd Pharmaceutically active pyrimidine derivatives
SE0003828D0 (sv) 2000-10-20 2000-10-20 Astrazeneca Ab Novel compounds
US6858608B2 (en) * 2001-01-09 2005-02-22 Aventis Pharma S.A. Chemical derivatives and their application as antitelomerase agents
US6887873B2 (en) 2001-03-23 2005-05-03 Aventis Pharma S.A. Triazine derivatives and their application as antitelomerase agents
WO2002076985A1 (en) * 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
SE0101322D0 (sv) 2001-04-12 2001-04-12 Astrazeneca Ab Novel compounds
US20030176443A1 (en) * 2001-05-16 2003-09-18 Matthias Stein-Gerlach Pyridylpyrimidine derivatives as effective compounds against prion diseases
JP4510442B2 (ja) * 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー ＴＮＦ−α発現のＮ−ヘテロ環インヒビター
SE0102716D0 (sv) * 2001-08-14 2001-08-14 Astrazeneca Ab Novel compounds
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US6806272B2 (en) 2001-09-04 2004-10-19 Boehringer Ingelheim Pharma Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
NZ531928A (en) * 2001-09-04 2005-10-28 Boehringer Ingelheim Pharma Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
EP1453516A2 (de) 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
EP2090571B1 (de) 2001-10-17 2012-05-16 Boehringer Ingelheim Pharma GmbH & Co. KG Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung
KR20060111716A (ko) 2002-01-22 2006-10-27 워너-램버트 캄파니 엘엘씨 2-(피리딘-2-일아미노)-피리도[2,3-ｄ]피리미딘-7-온
DE10212100A1 (de) * 2002-03-11 2003-10-23 Schering Ag CDK inhibitorische 2-Heteroaryl-Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
PA8577501A1 (es) * 2002-07-25 2004-02-07 Warner Lambert Co Inhibidores de quinasas
WO2004011456A1 (en) * 2002-07-31 2004-02-05 Danter Wayne R Protein tyrosine kinase inhibitors
GB0221828D0 (en) * 2002-09-20 2002-10-30 Astrazeneca Ab Novel compound
GB0221829D0 (en) * 2002-09-20 2002-10-30 Astrazeneca Ab Novel compound
US7067658B2 (en) 2002-09-30 2006-06-27 Bristol-Myers Squibb Company Pyridino and pyrimidino pyrazinones
RU2351586C2 (ru) * 2002-10-03 2009-04-10 Таргеджен, Инк. Васкулостатические агенты и способы их применения
WO2004033446A1 (en) * 2002-10-09 2004-04-22 Danter Wayne R Protein tyrosine kinase inhibitors
CN1717396A (zh) * 2002-11-28 2006-01-04 舍林股份公司 Chk－、Pdk－和Akt－抑制嘧啶,其制备及作为药物的用途
MXPA05007503A (es) * 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
US7157455B2 (en) 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
MXPA05009068A (es) * 2003-02-26 2005-10-19 Boehringer Ingelheim Pharma Dihidro-pteridinonas, metodo para la produccion y uso del mismo en la forma de farmacos.
US6861422B2 (en) * 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
US8178671B2 (en) 2003-07-30 2012-05-15 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds
GB0328243D0 (en) * 2003-12-05 2004-01-07 Astrazeneca Ab Methods
US7405220B2 (en) 2004-06-09 2008-07-29 Hoffmann-La Roche Inc. Pyrazolopyrimidines
DE102004029784A1 (de) * 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
EP1765820A4 (en) * 2004-06-23 2010-07-21 Irm Llc COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF PROTEIN KINASES
DE102004033670A1 (de) * 2004-07-09 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel
US7423051B2 (en) 2004-07-15 2008-09-09 Hoffmann-La Roche Inc. 2,6-diaminopyridine derivatives
US7423053B2 (en) 2004-07-15 2008-09-09 Hoffmann-La Roche Inc. 4-Aminothiazole derivatives
DE102004034623A1 (de) 2004-07-16 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 6-Formyl-tetrahydropteridine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7728134B2 (en) * 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060074088A1 (en) * 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060035903A1 (en) * 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
EP1630163A1 (de) * 2004-08-25 2006-03-01 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1632493A1 (de) * 2004-08-25 2006-03-08 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
WO2006021547A1 (de) * 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinone als plk (polo like kinase) inhibitoren
JP2008510771A (ja) * 2004-08-27 2008-04-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用
DE102004058337A1 (de) * 2004-12-02 2006-06-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten
US7767687B2 (en) * 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US7439358B2 (en) 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
KR20080095902A (ko) 2006-02-14 2008-10-29 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로서 유용한 디하이드로디아제핀
ATE542823T1 (de) * 2006-04-12 2012-02-15 Vertex Pharma 4,5-dihydro-ä1,2,4ütriazoloä4,3-füpteridine als plk1-proteinkinasehemmer zur behandlung proliferativer erkrankungen
WO2007135374A1 (en) * 2006-05-19 2007-11-29 Astrazeneca Ab Dihydropteridine compounds as anti proliferative agents
WO2008009909A1 (en) * 2006-07-17 2008-01-24 Astrazeneca Ab Pteridimones as modulators of polo-like kinase
US10144736B2 (en) 2006-07-20 2018-12-04 Gilead Sciences, Inc. Substituted pteridines useful for the treatment and prevention of viral infections
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
WO2008040951A1 (en) * 2006-10-03 2008-04-10 Astrazeneca Ab Compounds
WO2008043087A2 (en) 2006-10-05 2008-04-10 Cv Therapeutics, Inc. Bicyclic nitrogen-containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors
US7893066B2 (en) 2006-10-05 2011-02-22 Gilead Palo Alto, Inc. Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors
US8138191B2 (en) 2007-01-11 2012-03-20 Critical Outcome Technologies Inc. Inhibitor compounds and cancer treatment methods
CA2673683C (en) 2007-01-11 2014-07-29 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
EP1953163A1 (en) * 2007-02-01 2008-08-06 Boehringer Ingelheim Pharma GmbH & Co. KG Pteridinone derivatives as PI3-kinases inhibitors
JP2010523653A (ja) 2007-04-09 2010-07-15 ギリアード・パロ・アルト・インコーポレイテッド ステアロイルＣｏＡデサチュラーゼのインヒビターとして使用するためのプテリジノン誘導体
EP2185559A1 (en) 2007-08-03 2010-05-19 Boehringer Ingelheim International GmbH Crystalline form of a dihydropteridione derivative
NZ584760A (en) 2007-09-25 2012-03-30 Takeda Pharmaceutical Polo-like kinase inhibitors
US8598172B2 (en) 2007-12-04 2013-12-03 Nerviano Medical Sciences S.R.L. Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
US8466151B2 (en) * 2007-12-26 2013-06-18 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
JP2011516498A (ja) 2008-04-04 2011-05-26 ギリアード サイエンシーズ， インコーポレイテッド ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するためのトリアゾロピリジノン誘導体
EA026557B1 (ru) 2008-12-09 2017-04-28 Джилид Сайэнс, Инк. Промежуточные соединения для получения модуляторов толл-подобных рецепторов
CA2772253C (en) 2009-09-14 2018-02-27 Gilead Sciences, Inc. Modulators of toll-like receptors
CN102020643A (zh) 2009-09-22 2011-04-20 上海恒瑞医药有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
NZ599342A (en) 2009-09-25 2014-04-30 Vertex Pharma Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
AU2010299579A1 (en) 2009-09-25 2012-05-03 Vertex Pharmaceuticals Incorporated Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
WO2011050245A1 (en) * 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
WO2011101369A1 (en) 2010-02-17 2011-08-25 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for production and use thereof
EP3235818A3 (en) 2010-04-01 2018-03-14 Critical Outcome Technologies, Inc. Compounds for the treatment of hiv
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
US8546566B2 (en) 2010-10-12 2013-10-01 Boehringer Ingelheim International Gmbh Process for manufacturing dihydropteridinones and intermediates thereof
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
US9370535B2 (en) 2011-05-17 2016-06-21 Boehringer Ingelheim International Gmbh Method for treatment of advanced solid tumors
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
EP2776444A4 (en) 2011-11-10 2015-07-22 Osi Pharmaceuticals Llc dihydropteridinones
DE112013002484B4 (de) * 2012-05-14 2023-05-04 Shanghai Yidian Pharmaceutical Technology Development Co., Ltd. Pteridinketon-Derivat und Anwendungen desselben als EGFR-, BLK- und FLT3-Inhibitor
GB201209613D0 (en) * 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
AU2014228746B2 (en) 2013-03-15 2018-08-30 Celgene Car Llc Heteroaryl compounds and uses thereof
NZ711376A (en) 2013-03-15 2020-01-31 Sanofi Sa Heteroaryl compounds and uses thereof
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US20150031699A1 (en) 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
PL3122358T3 (pl) 2014-03-26 2021-06-14 Astex Therapeutics Ltd. Połączenia inhibitorów fgfr i cmet w leczeniu nowotworu
BR112016022062B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico
WO2015193228A1 (de) * 2014-06-19 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 1,4-dihydropyrido[3,4-b]pyrazinone mit para-substituierter aromatischer amino- oder ethergruppe
PT3166607T (pt) 2014-07-11 2022-12-07 Gilead Sciences Inc Moduladores de receptores de tipo toll para o tratamento do vih
AU2015318061B2 (en) 2014-09-16 2018-05-17 Gilead Sciences, Inc. Solid forms of a toll-like receptor modulator
CN107074860B (zh) 2014-09-16 2022-07-15 吉利德科学公司 制备toll样受体调节剂的方法
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
KR102394917B1 (ko) 2015-03-04 2022-05-09 길리애드 사이언시즈, 인코포레이티드 톨 유사 수용체 조정제 화합물
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
CN106279173A (zh) * 2015-05-29 2017-01-04 华东理工大学 蝶啶酮衍生物作为egfr抑制剂的应用
BR112018005637B1 (pt) 2015-09-23 2023-11-28 Janssen Pharmaceutica Nv Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos
HRP20220012T1 (hr) 2015-09-23 2022-04-01 Janssen Pharmaceutica Nv Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka
CN106892922B (zh) * 2015-12-18 2019-04-19 华东理工大学 作为egfr抑制剂的5,8-二氢蝶啶-6,7-二酮衍生物及其应用
CN107151249B (zh) * 2016-03-04 2020-08-14 华东理工大学 作为flt3抑制剂的蝶啶酮衍生物及应用
WO2018045150A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
PT3507276T (pt) 2016-09-02 2022-01-11 Gilead Sciences Inc Compostos moduladores do recetor de tipo toll
CN108721298A (zh) * 2017-04-19 2018-11-02 华东理工大学 作为布鲁顿酪氨酸激酶抑制剂的嘧啶并杂环化合物及其应用
EP3833353A4 (en) * 2018-08-10 2022-08-24 Yale University Small-molecule pi5p4k alpha/beta inhibitors and methods of treatment using same
TWI831829B (zh) 2018-09-12 2024-02-11 美商建南德克公司 苯氧基-吡啶基-嘧啶化合物及使用方法
CN111217815B (zh) * 2018-11-27 2021-06-18 沈阳药科大学 含有喋啶酮骨架的化合物及其制备方法和应用
WO2020142612A1 (en) * 2019-01-03 2020-07-09 Genentech, Inc. Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases.
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI879779B (zh) 2019-06-28 2025-04-11 美商基利科學股份有限公司 類鐸受體調節劑化合物的製備方法
CN110357885A (zh) * 2019-07-24 2019-10-22 江南大学 一种蝶啶类化合物及其在药学上的应用
CN113801118A (zh) * 2020-06-12 2021-12-17 华东理工大学 作为rsk抑制剂的蝶啶酮衍生物及其应用
WO2022177302A1 (ko) * 2021-02-17 2022-08-25 보령제약 주식회사 Dna-pk 억제 활성을 갖는 피리미딘-융합 고리 화합물 및 이의 용도
CN113087708A (zh) * 2021-04-06 2021-07-09 南方医科大学 一种蝶啶酮类化合物及其应用
CN115850281A (zh) * 2021-09-24 2023-03-28 华东理工大学 蝶啶酮衍生物及其应用
CN115010711B (zh) * 2022-07-12 2024-12-03 江南大学 一种蝶啶7（8h）-酮类化合物及其在药学上的应用
CN118047779B (zh) * 2022-11-09 2025-02-11 沈阳药科大学 含苯联杂芳基的二氢喋啶酮衍生物及其用途
WO2024199388A1 (zh) * 2023-03-29 2024-10-03 微境生物医药科技(上海)有限公司 作为myt1抑制剂的化合物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS53124296A (en) * 1977-04-05 1978-10-30 Mitsubishi Chem Ind Ltd Penicillin derivatives
US6395733B1 (en) * 1995-06-07 2002-05-28 Pfizer Inc Heterocyclic ring-fused pyrimidine derivatives
SK72996A3 (en) * 1995-06-07 1997-04-09 Pfizer Heterocyclic ring-fused pyrimidine derivatives and pharmaceutical compositions on their base
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
JPH1180131A (ja) * 1997-09-01 1999-03-26 Mitsubishi Chem Corp エチニルピリミジン誘導体
WO2002076985A1 (en) * 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases

Also Published As

Publication number Publication date
WO2001019825A1 (en) 2001-03-22
NO20021239L (no) 2002-03-13
US20070049600A1 (en) 2007-03-01
NZ516872A (en) 2003-10-31
EE200200140A (et) 2003-04-15
AU5629500A (en) 2001-04-17
CA2393896A1 (en) 2001-03-22
AP2002002479A0 (en) 2002-06-30
HUP0202713A3 (en) 2005-02-28
BR0013952A (pt) 2002-05-14
SK3542002A3 (en) 2003-04-01
CR6586A (es) 2004-02-02
NO20021239D0 (no) 2002-03-13
IS6298A (is) 2002-03-13
CN1373763A (zh) 2002-10-09
OA12010A (en) 2006-04-19
PL353269A1 (en) 2003-11-03
US20030130286A1 (en) 2003-07-10
DZ3186A1 (fr) 2001-03-22
KR20020027649A (ko) 2002-04-13
IL148614A0 (en) 2002-09-12
EA005287B1 (ru) 2004-12-30
ZA200200896B (en) 2003-07-30
YU18502A (sh) 2004-12-31
EP1409487A1 (en) 2004-04-21
JP2003509425A (ja) 2003-03-11
US7169778B2 (en) 2007-01-30
CZ2002846A3 (cs) 2003-02-12
HK1048992A1 (zh) 2003-04-25
MXPA02001108A (es) 2002-08-20
MA26819A1 (fr) 2004-12-20
AU777468B2 (en) 2004-10-21
BG106594A (en) 2002-12-29
EA200200078A1 (ru) 2002-12-26

Similar Documents

Publication Publication Date Title
HUP0202713A2 (hu) Kináz inhibitorokként alkalmazható pteridinonok
HUP0300195A2 (hu) Heterociklusos nátrium/proton-csere inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HUP0001446A2 (hu) HIV reverz transzkriptáz inhibitor hatású 4,4-diszubsztituált-3,4-dihidro-2(1H)-kinazolinon-származékok, alkalmazásuk és a vegyületeket tartalmazó gyógyszerkészítmények
HUP0300743A2 (hu) Heteroarilszármazékok és alkalmazásuk gyógyszerként
NZ334531A (en) Quinoxalin derivatives as Protein kinase C inhibitors
HUP0000658A2 (hu) Szulfonamidszármazékok, eljárás előállításukra és gyógyszerként való alkalmazásuk
NO972666L (no) Anilinderivater med nitrogenmonoksyd-synteseinhiberende aktivitet
IL100899A (en) Beta-amino-alpha- hydroxycarboxylic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same
HUP0104177A2 (hu) HIV-vírus szaporodását gátló pirimidin-származékok, eljárás az előállításukra, illetve ezeket tartalmazó gyógyászati készítmények
HUP0401423A2 (hu) Izoxazolidin-, pirazolidin- és dihidropirazol-származékok mint dipeptidil-peptidáz IV inhibitorok, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
CA2186508A1 (en) Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors
HUP0300138A2 (en) Cyclic amine derivatives as ccr5 antagonists, their production and use and pharmaceutical compositions containing them
PL349036A1 (en) Quinoline derivatives and quinazoline derivatives
HUP0204418A2 (hu) NHE-1 inhibitor hatású N-[(helyettesített öttagú, di- vagy triaza-, kétszeresen telítetlen gyűrű)-karbonil]-guanidin-származékok és alkalmazásuk
EP1529047B8 (en) New purine derivatives
DK1117297T3 (da) Syntetiske analoger af ecteinascidin-743
CA2203237A1 (en) Aminotetrazole derivatives useful as nitric oxide synthase inhibitors
HUT60271A (en) Process for producing tricyclic compounds, functioning as enzyme inhibitior and comprising amino or nitro group and pharmaceutical compositions comprising same as active ingredient
YU25201A (sh) Derivati izosorbid mononitrata i njihova upotreba kao vazodilatacionih agensa sa redukovanom tolerancijom
MY131641A (en) Indoline derivatives, process of preparation and use
MXPA04003729A (es) Compuestos de 4-imidazolin-2-ona.
SI2298780T1 (sl) Anti-tumorski derivati ecteinascidina et-743
TR199801380T2 (xx) Hidroksamik asit temelli kollajenaz �nleyicileri.
ES2055651A1 (es) Procedimiento para la obtencion de nuevas amidinas derivadas de 3-aminoetilindoles.
TW200407315A (en) Pyrimidine derivatives