ECSP055899A - Pirimidinas inhibidoras de chk, pdk y akt, su producción y su uso como agentes farmacéuticos - Google Patents

Pirimidinas inhibidoras de chk, pdk y akt, su producción y su uso como agentes farmacéuticos

Info

Publication number
ECSP055899A
ECSP055899A EC2005005899A ECSP055899A ECSP055899A EC SP055899 A ECSP055899 A EC SP055899A EC 2005005899 A EC2005005899 A EC 2005005899A EC SP055899 A ECSP055899 A EC SP055899A EC SP055899 A ECSP055899 A EC SP055899A
Authority
EC
Ecuador
Prior art keywords
production
pyrimidins
pdk
chk
pharmaceutical agents
Prior art date
Application number
EC2005005899A
Other languages
English (en)
Inventor
Judi Bryant
Monica Kochanny
Shendong Yuan
Seock Kyu Khim
Brad Buckman
Damian Arnaiz
Ulf Bomer
Hans Briem
Peter Esperling
Christoph Huwe
Joachim Kuhnke
Martina Schafer
Lars Wortmann
Dirk Kosemund
Emil Eckle
Richard Feldman
Gary Phillips
Original Assignee
Schering 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 Schering Ag filed Critical Schering Ag
Publication of ECSP055899A publication Critical patent/ECSP055899A/es

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
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • 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
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D239/30—Halogen atoms or nitro radicals
    • 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
    • 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
    • C07D239/50—Three nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

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

Abstract

Esta invención se relaciona con derivados de pirimidina de formula general (I) como inhibidores de quinasas, su producción y su uso como medicación para el tratamiento de diversas enfermedades.
EC2005005899A 2002-11-28 2005-06-28 Pirimidinas inhibidoras de chk, pdk y akt, su producción y su uso como agentes farmacéuticos ECSP055899A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02026607 2002-11-28

Publications (1)

Publication Number Publication Date
ECSP055899A true ECSP055899A (es) 2005-11-22

Family

ID=32338009

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005005899A ECSP055899A (es) 2002-11-28 2005-06-28 Pirimidinas inhibidoras de chk, pdk y akt, su producción y su uso como agentes farmacéuticos

Country Status (20)

Country Link
US (1) US7504410B2 (es)
EP (1) EP1565446A1 (es)
JP (1) JP2006508997A (es)
KR (1) KR20050084027A (es)
CN (1) CN1717396A (es)
AU (1) AU2003288198A1 (es)
BR (1) BR0316680A (es)
CA (1) CA2502970A1 (es)
EA (1) EA200500721A1 (es)
EC (1) ECSP055899A (es)
HR (1) HRP20050601A2 (es)
IL (1) IL168102A0 (es)
IS (1) IS7881A (es)
MX (1) MXPA05005547A (es)
NO (1) NO20053144L (es)
NZ (1) NZ539823A (es)
PL (1) PL377795A1 (es)
RS (1) RS20050363A (es)
WO (1) WO2004048343A1 (es)
ZA (1) ZA200505184B (es)

Families Citing this family (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MEP13408A (en) * 2001-05-29 2010-06-10 Bayer Schering Pharma Ag Cdk inhibiting pyrimidines, production thereof and their use as medicaments
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
UA80767C2 (en) * 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
US7157455B2 (en) 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
EP1624873A2 (en) * 2003-04-28 2006-02-15 AB Science Use of tyrosine kinase inhibitors for treating cerebral ischemia
JP4886511B2 (ja) 2003-07-30 2012-02-29 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療または予防方法
US7332521B2 (en) * 2003-09-25 2008-02-19 Wyeth Substituted indoles
AU2004284084A1 (en) 2003-10-24 2005-05-06 Schering Aktiengesellschaft Indolinone derivatives and their use in treating disease-states such as cancer
KR20070057798A (ko) * 2004-09-30 2007-06-07 티보텍 파마슈티칼즈 리미티드 Ｈｉｖ를 저해하는 5-탄소환 또는 복소환으로 치환된피리미딘
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
CA2590250A1 (en) * 2004-12-14 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrimidine inhibitors of erk protein kinase and uses therof
US8716299B2 (en) * 2004-12-20 2014-05-06 University Of South Florida XIAP-targeted prostate cancer therapy
WO2006076706A1 (en) * 2005-01-14 2006-07-20 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
CN101115761B (zh) 2005-01-19 2012-07-18 里格尔药品股份有限公司 2,4-嘧啶二胺化合物的前药及其应用
WO2006105262A1 (en) 2005-03-29 2006-10-05 Icos Corporation HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
EA015890B1 (ru) * 2005-06-14 2011-12-30 Тайджен Байотекнолоджи Ко. Лтд. Производные пиримидина
EP1931322B1 (en) * 2005-09-07 2012-08-15 Merck Serono SA Ikk inhibitors for the treatment of endometriosis
KR20080066949A (ko) * 2005-10-11 2008-07-17 인터뮨, 인크. 바이러스 복제 억제제
US7705009B2 (en) 2005-11-22 2010-04-27 Hoffman-La Roche Inc. 4-aminopyrimidine-5-thione derivatives
WO2007072158A2 (en) * 2005-12-21 2007-06-28 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
DE102005062742A1 (de) * 2005-12-22 2007-06-28 Bayer Schering Pharma Ag Sulfoximin substituierte Pyrimidine, Verfahren zu deren Herstellung und ihre Verwendung als Arzneimittel
CA2646316C (en) 2006-03-15 2016-05-24 Theralogics, Inc. Methods of treating muscular wasting diseases using nf-kb activation inhibitors
DE102006027156A1 (de) * 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
AU2007257650A1 (en) * 2006-06-15 2007-12-21 Boehringer Ingelheim International Gmbh 2-anilino-4-(heterocyclic)amino-pyrimidines as inhibitors of protein kinase C-alpha
US20070293525A1 (en) 2006-06-15 2007-12-20 Djung Jane F 2-anilino-4-aminoalkyleneaminopyrimidines
CA2656618C (en) 2006-07-06 2014-08-26 Array Biopharma Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
EP2086644A2 (en) * 2006-11-17 2009-08-12 Schering Corporation Combination of an inhibitor of dna polymerase-alpha and an inhibitor of a checkpoint kinase for proliferative disorders
EP2136635A4 (en) * 2007-03-20 2011-07-27 Glaxosmithkline Llc CHEMICAL COMPOUNDS
NZ580671A (en) 2007-04-16 2012-03-30 Hutchison Medipharma Entpr Ltd Pyrimidine derivatives
DK2146779T3 (en) 2007-04-18 2016-11-28 Pfizer Prod Inc Sulfonylamid derivatives to treat abnormal cell growth.
WO2009030890A1 (en) * 2007-09-03 2009-03-12 University Court Of The University Of Dundee Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma
CN104628654A (zh) * 2007-09-17 2015-05-20 艾伯维巴哈马有限公司 抗感染嘧啶及其用途
EP2227460B1 (en) * 2007-10-24 2012-06-20 Cancer Research Technology Limited Therapeutic oxy-phenyl-aryl compounds and their use
WO2009071535A1 (en) * 2007-12-03 2009-06-11 Boehringer Ingelheim International Gmbh Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
WO2009122180A1 (en) * 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
CA2728228A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
NZ602832A (en) 2008-07-14 2014-04-30 Gilead Sciences Inc Fused heterocyclic hdac inhibitor compounds
WO2010009139A2 (en) 2008-07-14 2010-01-21 Gilead Colorado, Inc. Imidazolyl pyrimidine inhibitor compounds
MX2011001090A (es) 2008-07-28 2011-03-15 Gilead Sciences Inc Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno.
BRPI0918472A2 (pt) * 2008-09-01 2015-12-01 Astellas Pharma Inc composto 2,4-diaminopirimidina
WO2010027448A1 (en) * 2008-09-02 2010-03-11 Actimis Pharmaceuticals Inc. Isotopically enriched pyrimidin-5-yl acetic acid derivatives as crth2 antagonists
CN102203070A (zh) * 2008-09-03 2011-09-28 拜尔农作物科学股份公司 烷氧基-和烷硫基-取代的苯胺基嘧啶类化合物
EP2161259A1 (de) * 2008-09-03 2010-03-10 Bayer CropScience AG 4-Halogenalkylsubstituierte Diaminopyrimidine als Fungizide
KR20110051266A (ko) * 2008-09-03 2011-05-17 바이엘 크롭사이언스 아게 살진균제로서의 헤테로사이클 치환된 아닐리노피리미딘
EP2179992A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfonsubstituierte Anlinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
EP2179991A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfoximinsubstituierte Anilino-Pyrimidinderivate als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
UY32240A (es) 2008-11-14 2010-06-30 Boeringer Ingelheim Kg Nuevas 2,4-diaminopirimidinas, sus sales farmacéuticamente aceptables, composiciones conteniéndolas y aplicaciones.
TWI491605B (zh) 2008-11-24 2015-07-11 Boehringer Ingelheim Int 新穎化合物
AR074209A1 (es) * 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina utiles para el tratamiento del cancer
DE102009001438A1 (de) 2009-03-10 2010-09-16 Bayer Schering Pharma Aktiengesellschaft Carbonylamino-substituierte Anilino-Pyrimidinderivate als Tyk-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
DE102009015070A1 (de) 2009-03-30 2010-10-14 Bayer Schering Pharma Aktiengesellschaft Aminocabonylamino-substituierte Anilino-Pyrimidinderivate als Tyk-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
WO2010144371A1 (en) 2009-06-08 2010-12-16 Gilead Colorado, Inc. Alkanoylamino benzamide aniline hdac inihibitor compounds
ES2463826T3 (es) 2009-06-08 2014-05-29 Gilead Sciences, Inc. Compuestos inhibidores de HDAC de cicloalquilcarbamato benzamida anilina
EP2464633A1 (en) 2009-08-14 2012-06-20 Boehringer Ingelheim International GmbH Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
IN2012DN02534A (es) 2009-09-16 2015-08-28 Avila Therapeutics Inc
US20110065776A1 (en) * 2009-09-17 2011-03-17 Keng-Hsin Lan Method for Treating Hepatitis C Infection
US20110269244A1 (en) * 2009-12-30 2011-11-03 Petter Russell C Ligand-directed covalent modification of protein
CN103003264B (zh) 2010-05-21 2014-08-06 切米利亚股份公司 嘧啶衍生物
HUE029196T2 (en) 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidine derivatives as LRRK2 modulators
JPWO2012005299A1 (ja) * 2010-07-07 2013-09-05 日本新薬株式会社 Ｒｏｓチロシンキナーゼ阻害剤
SG189043A1 (en) 2010-11-10 2013-05-31 Hoffmann La Roche Pyrazole aminopyrimidine derivatives as lrrk2 modulators
US8546443B2 (en) * 2010-12-21 2013-10-01 Boehringer Ingelheim International Gmbh Benzylic oxindole pyrimidines
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CA2830129C (en) 2011-03-24 2016-07-19 Chemilia Ab Novel pyrimidine derivatives
CN103841975A (zh) 2011-04-01 2014-06-04 基因泰克公司 Akt抑制剂化合物和厄洛替尼的组合以及使用方法
CN103841976A (zh) 2011-04-01 2014-06-04 基因泰克公司 Akt和mek抑制剂化合物的组合及其使用方法
DE102011083283A1 (de) 2011-09-23 2013-03-28 Beiersdorf Ag Heteroalkylamidothiazole, deren kosmetische oder dermatologische Verwendung sowie kosmetische oder dermatologische Zubereitungen mit einem Gehalt an solchen Heteroalkylamidothiazolen
US8791130B2 (en) * 2011-11-29 2014-07-29 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 modulators
AR089182A1 (es) * 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
KR20160125527A (ko) * 2012-04-17 2016-10-31 후지필름 가부시키가이샤 함질소 복소환 화합물 또는 그 염
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
CN102746337B (zh) * 2012-06-21 2014-12-17 成都苑东药业有限公司 一种2，4-嘧啶二胺类化合物及其制备方法
US9333219B2 (en) 2012-08-03 2016-05-10 Albert Einstein College Of Medicine, Inc. Method to treat or prevent herpesvirus infections
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US10130632B2 (en) * 2012-11-27 2018-11-20 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
EP3030241A4 (en) * 2013-08-06 2019-06-19 H. Lee Moffitt Cancer Center And Research Institute, Inc. INHIBITORS OF ACK1 / TNK2.TYROSINE KINASE
CN103539744B (zh) * 2013-10-17 2016-03-23 北京颖泰嘉和生物科技股份有限公司 一种制备3-(3,5-二氯苯基)-2,4-咪唑烷二酮的方法
CA2937967C (en) * 2014-01-29 2022-07-26 Neuropore Therapies, Inc. Heteroaryl amides as inhibitors of protein aggregation
GB201402277D0 (en) * 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
JP6431294B2 (ja) * 2014-06-16 2018-11-28 東ソー・ファインケム株式会社 ５−（トリフルオロメチル）ピリミジン誘導体及びその製造法
WO2016014542A1 (en) 2014-07-21 2016-01-28 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
EP3172213B1 (en) 2014-07-21 2021-09-22 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
AU2015300782B2 (en) 2014-08-08 2020-04-16 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (SIK) inhibitors
CN105399685B (zh) 2014-09-16 2018-05-22 深圳微芯生物科技有限责任公司 作为选择性jak3和/或jak1激酶抑制剂的芳杂环化合物的制备方法及其应用
CN105481778B (zh) * 2014-09-16 2019-06-04 深圳微芯生物科技股份有限公司 嘧啶衍生物、其制备方法及其应用
MX2017003181A (es) 2014-10-13 2017-07-20 Yuhan Corp Compuestos y composiciones para modular actividades de quinasa de mutante de receptor del factor de crecimiento epidermico.
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JP6479486B2 (ja) * 2015-01-16 2019-03-06 東ソー・ファインケム株式会社 ４−アルコキシ−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CA2989651A1 (en) * 2015-07-09 2017-01-12 Merck Patent Gmbh Pyrimidine derivatives as btk inhibitors and uses thereof
WO2017115372A1 (en) 2015-12-30 2017-07-06 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Pt(IV) PRODRUGS
CN106083828A (zh) * 2016-06-30 2016-11-09 浙江大学 含吖丙啶环侧链的芳胺嘧啶衍生物及制备和应用
US10954242B2 (en) 2016-07-05 2021-03-23 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
KR101876514B1 (ko) * 2016-11-08 2018-07-10 한국화학연구원 신규한 피리미딘화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암 및 염증질환의 예방 또는 치료용 약학적 조성물
US11285158B2 (en) 2017-02-28 2022-03-29 The General Hospital Corporation Uses of pyrimidopyrimidinones as SIK inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN109928935B (zh) * 2017-12-19 2023-03-10 沈阳化工研究院有限公司 一种苯胺基嘧啶类化合物及其医药用途
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
WO2020023851A1 (en) * 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
RS65019B1 (sr) * 2019-05-10 2024-01-31 Deciphera Pharmaceuticals Llc Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primene
AU2020274011B2 (en) 2019-05-10 2024-02-15 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
CN119241444A (zh) 2019-06-17 2025-01-03 德西费拉制药有限责任公司 氨基嘧啶酰胺自噬抑制剂及其使用方法
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN116528869A (zh) * 2020-11-27 2023-08-01 安锐生物医药科技(广州)有限公司 氨基杂芳基激酶抑制剂
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN116947715A (zh) * 2022-04-19 2023-10-27 帕潘纳(北京)科技有限公司 硝磺草酮中间体的制备方法
CN115413669B (zh) * 2022-06-14 2024-03-15 湖南大学 激酶抑制剂及其组合剂在提高植物青枯病抗性中的应用
KR20240017731A (ko) * 2022-08-01 2024-02-08 동아대학교 산학협력단 Pdh 억제제의 신경 퇴행성 질환 치료 용도

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3055900A (en) * 1957-12-06 1962-09-25 Ciba Geigy Corp Pyrimido pyrimidines and process of making same
ES477520A1 (es) * 1978-02-25 1979-06-01 Thomae Gmbh Dr K Procedimiento para la preparacion de nuevas penicilinas.
JPS60100559A (ja) * 1983-11-05 1985-06-04 Morishita Seiyaku Kk ２−アニリノ−１，６−ジヒドロ−６−オキソ−５−ピリミジンカルボン酸誘導体，その製法及び該化合物を含有する抗アレルギ−剤
JPS6110563A (ja) * 1984-06-25 1986-01-18 Hokuriku Seiyaku Co Ltd ピリミジルアミノフエニルプロピオン酸誘導体
JPH0625161B2 (ja) * 1984-10-09 1994-04-06 森下ルセル株式会社 ２−アニリノ−１，６−ジヒドロ−６−オキソ−５−ピリミジンカルボン酸誘導体の製造法
JPS61112059A (ja) * 1984-11-06 1986-05-30 Morishita Seiyaku Kk ２−アニリノ−１，６−ジヒドロ−６−オキソ−５−ピリミジンカルボニトリル誘導体
GB8506318D0 (en) * 1985-03-12 1985-04-11 Smith Kline French Lab Chemical compounds
JPH0629263B2 (ja) * 1985-10-30 1994-04-20 クミアイ化学工業株式会社 ピリミジン誘導体および農園芸用殺菌剤
JPH03127790A (ja) * 1989-10-11 1991-05-30 Morishita Pharmaceut Co Ltd Ｎ―（１ｈ―テトラゾール―５―イル）―２―アニリノ―５―ピリミジンカルボキシアミド類及びその合成中間体
DE4029650A1 (de) * 1990-09-19 1992-03-26 Hoechst Ag 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide
PL313973A1 (en) * 1993-10-12 1996-08-05 Du Pont Merck Pharma 1 n-alkyl-n-arylopyrimidin amines and their derivatives
US5516905A (en) * 1994-08-30 1996-05-14 University Of Massachusetts Medical Center Antibiotic compounds and methods to treat gram-positive bacterial and mycoplasmal infections
IL115256A0 (en) * 1994-11-14 1995-12-31 Warner Lambert Co 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use
US5620981A (en) * 1995-05-03 1997-04-15 Warner-Lambert Company Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
IL117923A (en) * 1995-05-03 2000-06-01 Warner Lambert Co Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds
DE69839338T2 (de) * 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
ES2218820T3 (es) * 1997-05-15 2004-11-16 Sagami Chemical Research Center Agentes insecticidas/acaricidas.
NZ506679A (en) * 1998-03-27 2002-11-26 Janssen Pharmaceutica Nv HIV inhibiting pyrimidine derivatives
BRPI9909191B8 (pt) * 1998-03-27 2021-07-06 Janssen Pharmaceutica Nv derivados de pirimidina inibidores do hiv, seu uso e composição farmacêutica que os compreende
SK287269B6 (sk) * 1998-11-10 2010-05-07 Janssen Pharmaceutica N. V. Derivát pyrimidínu, jeho použitie, spôsob jeho prípravy a farmaceutická kompozícia, kombinácia a produkt s jeho obsahom
EP1132387B1 (en) * 1998-11-17 2005-09-28 Kumiai Chemical Industry Co., Ltd. Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultural/horticultural fungicides
KR20010108394A (ko) * 1999-03-26 2001-12-07 다비드 에 질레스 신규 화합물
EA005287B1 (ru) * 1999-09-15 2004-12-30 Уорнер-Ламберт Компани Птеридиноны в качестве ингибиторов киназ
JP4919566B2 (ja) * 1999-09-24 2012-04-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 抗ウイルス組成物
CA2397961C (en) * 2000-01-25 2008-08-26 Richard John Booth Pyrido[2,3-d]pyrimidine-2,7-diamine kinase inhibitors
CN1433417A (zh) * 2000-01-27 2003-07-30 沃尼尔·朗伯公司 用于治疗神经变性疾病的吡啶并嘧啶酮衍生物
GB0007371D0 (en) * 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
DK1282607T3 (en) * 2000-05-08 2016-02-01 Janssen Pharmaceutica Nv Prodrugs of HIV replication inhibiting pyrimidines
GB0016877D0 (en) * 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
MEP13408A (en) * 2001-05-29 2010-06-10 Bayer Schering Pharma Ag Cdk inhibiting pyrimidines, production thereof and their use as medicaments
HUP0402352A2 (hu) * 2001-06-19 2005-02-28 Bristol-Myers Squibb Co. Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
HUP0401711A3 (en) * 2001-06-26 2009-07-28 Bristol Myers Squibb Co N-heterocyclic inhibitors of tnf-alpha and pharmaceutical compositions containing them
JO3429B1 (ar) * 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
EP1438053B1 (de) * 2001-10-17 2008-09-10 Boehringer Ingelheim Pharma GmbH & Co.KG Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
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
IL161663A0 (en) * 2001-11-01 2004-09-27 Janssen Pharmaceutica Nv AMINOBENZAMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3beta INHIBITORS
BR0213792A (pt) * 2001-11-01 2004-12-07 Janssen Pharmaceutica Nv Heteroaril aminas como inibidores de glicogênio sintase cinase 3beta (inibidores de gsk3)
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
HRP20050089B1 (hr) * 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
PL208533B1 (pl) * 2002-08-09 2011-05-31 Janssen Pharmaceutica Nv Sposób otrzymywania 4-[[4-[[4-(2-cyjanoetenylo)-2,6-dimetylofenylo]amino]-2-pirymidynylo]amino]benzonitrylu oraz sposób otrzymywania związku pośredniego

Also Published As

Publication number Publication date
EA200500721A1 (ru) 2005-12-29
NZ539823A (en) 2008-04-30
BR0316680A (pt) 2005-10-18
NO20053144D0 (no) 2005-06-27
EP1565446A1 (en) 2005-08-24
IS7881A (is) 2005-06-02
AU2003288198A1 (en) 2004-06-18
US7504410B2 (en) 2009-03-17
JP2006508997A (ja) 2006-03-16
RS20050363A (sr) 2007-11-15
IL168102A0 (en) 2009-02-11
PL377795A1 (pl) 2006-02-20
ZA200505184B (en) 2006-09-27
NO20053144L (no) 2005-06-27
US20040186118A1 (en) 2004-09-23
MXPA05005547A (es) 2005-07-26
CN1717396A (zh) 2006-01-04
WO2004048343A1 (en) 2004-06-10
HRP20050601A2 (en) 2005-10-31
CA2502970A1 (en) 2004-06-10
KR20050084027A (ko) 2005-08-26

Similar Documents

Publication Publication Date Title
ECSP055899A (es) Pirimidinas inhibidoras de chk, pdk y akt, su producción y su uso como agentes farmacéuticos
UY27714A1 (es) 2 - heteroaril - pirimidinas inhibidoras de cdk, su preparación y su uso como medicamentos.
UY28059A1 (es) Nuevos derivados de dihidropirimido (4,5-d) pirimidona sustituida por amino. fabricacion y uso de los mismos como agentes farmaceuticos.
BRPI0413452A (pt) composto, composição farmacêutica, kit, artigo de fabricação, e, métodos de inibir dpp-iv, terapêutico e de tratar um estado de doença, cáncer, distúrbios autoimunes, uma condição einfecção por hiv
TN2012000062A1 (en) Jak 2 inhibitors and their use for the treatment of myeloproliferative deseases and cancer
UY27234A1 (es) Inhibidores novedosos de tirosina cinasa
BR0318383A (pt) derivados de pirazoloisoquinolina como inibidores de cinase
SV1999000047A (es) Nuevas dihidropirimidinas fef. lea 32792-sv
ECSP056194A (es) Derivados de pirazolo-quinazolina, procedimiento para su preparacion y su uso como inhibidores de quinasa
CL2011003346A1 (es) Compuestos derivados de 2,3-dihidro-5h-[1,3]tiazolo[3,2-a]pirimidin-5-ona, moduladores de pi3k; composicion farmaceutica; y uso para tratar una enfermedad de base inmunologica, cancer o enfermedad pulmonar en un paciente.
PA8680701A1 (es) Derivados de oxindol
CL2011003082A1 (es) Compuestos derivados de [1,2,4]triazolo[1,5-a]piridina, inhibidores de jak2 o fak; composiciones farmaceuticas que los comprenden; y su uso para el tratamiento de una enfermedad hiperproliferativa.
CR10072A (es) Derivados de pirimidinil-aril-urea que son inhibidores de fgf
TW200730528A (en) Bicyclic protein kinase inhibitors
ATE520668T1 (de) Sigmarezeptor-inhibitoren
CR7643A (es) Derivados de 1-heterociclialquil -3-sulfonilazaindol o azaindazol como ligandos de 5-hidroxitriptamina-6
GT200500363A (es) 3-amino-pirazol [3,4b] piridinas con inhibidores de proteintirosinquinasas, su preparacion y uso como medicamento.
MX2009006885A (es) Derivados de pirrolo[3,2-a]piridina para inhibir la actividad de la proteina cinesina del huso.
ECSP045156A (es) Derivados de indolilalquilamina como ligandos 5-hidroxitriptamina-6
DOP2005000014A (es) Derivados 1h-tieno[2, 3-c] pirazol utiles como inhibidores de quinasa
TW200628153A (en) Novel compounds
DOP2006000024A (es) Tiazolidinonas, su preparación y su uso como medicamento
UY29264A1 (es) Tiazolidinonas metasustituidas, su preparación y su uso como medicamento
TW200801018A (en) 6,6-bicyclic ring substituted sulfur containing heterobicyclic protein kinase inhibitors
UY27733A1 (es) Derivados de ciclopenteno.