WO2002088095A1 - Fused pyrimidines as antagonists of the corticotropin releasing factor (crf) - Google Patents

Fused pyrimidines as antagonists of the corticotropin releasing factor (crf) Download PDF

Info

Publication number
WO2002088095A1
WO2002088095A1 PCT/GB2002/002029 GB0202029W WO02088095A1 WO 2002088095 A1 WO2002088095 A1 WO 2002088095A1 GB 0202029 W GB0202029 W GB 0202029W WO 02088095 A1 WO02088095 A1 WO 02088095A1
Authority
WO
WIPO (PCT)
Prior art keywords
methyl
dihydro
pyrrolo
dichlorophenyl
compounds
Prior art date
Application number
PCT/GB2002/002029
Other languages
English (en)
French (fr)
Inventor
Anna Maria Capelli
Romano Di Fabio
Chiara Marchionni
Fabrizio Micheli
Alessandra Pasquarello
Benedetta Perini
Yves St-Denis
Original Assignee
Glaxo Group Limited
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
Priority claimed from GB0110570A external-priority patent/GB0110570D0/en
Priority claimed from GB0110567A external-priority patent/GB0110567D0/en
Priority claimed from GB0110569A external-priority patent/GB0110569D0/en
Priority claimed from GB0117399A external-priority patent/GB0117399D0/en
Priority claimed from GB0117420A external-priority patent/GB0117420D0/en
Priority claimed from GB0117401A external-priority patent/GB0117401D0/en
Priority claimed from GB0203201A external-priority patent/GB0203201D0/en
Priority claimed from GB0206834A external-priority patent/GB0206834D0/en
Priority to AU2002253357A priority Critical patent/AU2002253357B2/en
Priority to HU0304054A priority patent/HUP0304054A2/hu
Priority to DE60225127T priority patent/DE60225127T2/de
Priority to JP2002585397A priority patent/JP2004528349A/ja
Priority to EP02722478A priority patent/EP1383747B1/en
Priority to US10/476,368 priority patent/US7279474B2/en
Priority to KR10-2003-7014160A priority patent/KR20040015206A/ko
Priority to BR0209267-0A priority patent/BR0209267A/pt
Priority to ES02722478T priority patent/ES2301633T3/es
Priority to MXPA03009938A priority patent/MXPA03009938A/es
Application filed by Glaxo Group Limited filed Critical Glaxo Group Limited
Priority to IL15806202A priority patent/IL158062A0/xx
Priority to CA002446514A priority patent/CA2446514A1/en
Publication of WO2002088095A1 publication Critical patent/WO2002088095A1/en
Priority to NO20034836A priority patent/NO20034836L/no

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0463Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0465Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/40Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
PCT/GB2002/002029 2001-04-30 2002-04-30 Fused pyrimidines as antagonists of the corticotropin releasing factor (crf) WO2002088095A1 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
US10/476,368 US7279474B2 (en) 2001-04-30 2002-04-30 Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF)
KR10-2003-7014160A KR20040015206A (ko) 2001-04-30 2002-04-30 코르티코트로핀 방출 인자 (crf)의 길항제로서의 접합피리미딘
CA002446514A CA2446514A1 (en) 2001-04-30 2002-04-30 Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
IL15806202A IL158062A0 (en) 2001-04-30 2002-04-30 Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
AU2002253357A AU2002253357B2 (en) 2001-04-30 2002-04-30 Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
MXPA03009938A MXPA03009938A (es) 2001-04-30 2002-04-30 Pirimidinas fusionadas como antagonistas del factor liberador de corticotropina.
ES02722478T ES2301633T3 (es) 2001-04-30 2002-04-30 Pirimidinas condensadas como antagonistas del factor de liberacion de corticotropina (crf).
HU0304054A HUP0304054A2 (hu) 2001-04-30 2002-04-30 A kortikotropin-realising faktor (CRF) antagonistáiként alkalmazható kondenzált pirimidinek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
BR0209267-0A BR0209267A (pt) 2001-04-30 2002-04-30 Pirimidinas fundidas como antagonistas do fator de liberação de corticotropina (crf)
DE60225127T DE60225127T2 (de) 2001-04-30 2002-04-30 Kondensierte pyrimidine als antagonisten des corticotropin releasing factor (crf)
JP2002585397A JP2004528349A (ja) 2001-04-30 2002-04-30 副腎皮質刺激ホルモン放出因子(crf)のアンタゴニストとしての縮合ピリミジン類
EP02722478A EP1383747B1 (en) 2001-04-30 2002-04-30 Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
NO20034836A NO20034836L (no) 2001-04-30 2003-10-29 Sammensmeltede pyrimidiner som antagonister av kortikotropinfrigivelsesfaktoren (CRF)

Applications Claiming Priority (16)

Application Number Priority Date Filing Date Title
GB0110569.1 2001-04-30
GB0110570A GB0110570D0 (en) 2001-04-30 2001-04-30 Chemical compounds
GB0110569A GB0110569D0 (en) 2001-04-30 2001-04-30 Chemical compounds
GB0110570.9 2001-04-30
GB0110567.5 2001-04-30
GB0110567A GB0110567D0 (en) 2001-04-30 2001-04-30 Chemical compounds
GB0117401.0 2001-07-17
GB0117401A GB0117401D0 (en) 2001-07-17 2001-07-17 Chemical compounds
GB0117420A GB0117420D0 (en) 2001-07-17 2001-07-17 Chemical compounds
GB0117399.6 2001-07-17
GB0117399A GB0117399D0 (en) 2001-07-17 2001-07-17 Chemical compounds
GB0117420.0 2001-07-17
GB0203201.9 2002-02-11
GB0203201A GB0203201D0 (en) 2002-02-11 2002-02-11 Chemical compounds
GB0206834.4 2002-03-22
GB0206834A GB0206834D0 (en) 2002-03-22 2002-03-22 Chemical compounds

Publications (1)

Publication Number Publication Date
WO2002088095A1 true WO2002088095A1 (en) 2002-11-07

Family

ID=27571152

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2002/002029 WO2002088095A1 (en) 2001-04-30 2002-04-30 Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)

Country Status (19)

Country Link
US (1) US7279474B2 (US20040176400A1-20040909-C00062.png)
EP (1) EP1383747B1 (US20040176400A1-20040909-C00062.png)
JP (1) JP2004528349A (US20040176400A1-20040909-C00062.png)
KR (1) KR20040015206A (US20040176400A1-20040909-C00062.png)
CN (1) CN1649848A (US20040176400A1-20040909-C00062.png)
AR (1) AR033295A1 (US20040176400A1-20040909-C00062.png)
AT (1) ATE386727T1 (US20040176400A1-20040909-C00062.png)
AU (1) AU2002253357B2 (US20040176400A1-20040909-C00062.png)
BR (1) BR0209267A (US20040176400A1-20040909-C00062.png)
CA (1) CA2446514A1 (US20040176400A1-20040909-C00062.png)
CZ (1) CZ20032946A3 (US20040176400A1-20040909-C00062.png)
DE (1) DE60225127T2 (US20040176400A1-20040909-C00062.png)
ES (1) ES2301633T3 (US20040176400A1-20040909-C00062.png)
HU (1) HUP0304054A2 (US20040176400A1-20040909-C00062.png)
IL (1) IL158062A0 (US20040176400A1-20040909-C00062.png)
MX (1) MXPA03009938A (US20040176400A1-20040909-C00062.png)
NO (1) NO20034836L (US20040176400A1-20040909-C00062.png)
PL (1) PL366934A1 (US20040176400A1-20040909-C00062.png)
WO (1) WO2002088095A1 (US20040176400A1-20040909-C00062.png)

Cited By (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004094420A1 (en) * 2003-04-09 2004-11-04 Sb Pharmco Puerto Rico Inc Condensed n-heterocyclic compounds and their use as crf receptor antagonists
WO2004099209A1 (en) * 2003-05-05 2004-11-18 F. Hoffmann-La-Roche Ag Fused pyrimidine derivatives with crf activity
WO2005014557A1 (en) * 2003-08-12 2005-02-17 F.Hoffmann-La Roche Ag Tetrahydroquinazoline derivatives as cfr antagonists
WO2005085253A1 (en) * 2004-03-05 2005-09-15 Taisho Pharmaceutical Co., Ltd. Pyrrolopyrimidine derivatives
WO2006001501A1 (en) * 2004-06-25 2006-01-05 Taisho Pharmaceutical Co., Ltd. Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with tetrahydropyridine as crf antagonists
JP2006515334A (ja) * 2003-01-16 2006-05-25 エスビー ファームコ プエルト リコ インコーポレーテッド CRF受容体アンタゴニストとしてのヘテロアリール置換ピロロ[2,3−b]ピリジン誘導体
US7135476B2 (en) 2003-08-12 2006-11-14 Roche Palo Alto Llc Spiro tetrahydroquinazolines and dihydrocyclopentapyrimidines as CRF antagonists
JP2007517793A (ja) * 2004-01-06 2007-07-05 大正製薬株式会社 環状アミノ基によって置換されたチエノピリミジン及びチエノピリジン誘導体
WO2009107767A1 (ja) * 2008-02-29 2009-09-03 大日本住友製薬株式会社 H4受容体アンタゴニスト作用を有する新規2環性ピリミジン誘導体
US8178543B2 (en) 2004-06-02 2012-05-15 Takeda Pharmaceutical Company Limited Bi- and tricyclic fused pyrimidines as tyrosine kinase inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US9533954B2 (en) 2010-12-22 2017-01-03 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US9708318B2 (en) 2015-02-20 2017-07-18 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9890156B2 (en) 2015-02-20 2018-02-13 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10611762B2 (en) 2017-05-26 2020-04-07 Incyte Corporation Crystalline forms of a FGFR inhibitor and processes for preparing the same
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
US11407750B2 (en) 2019-12-04 2022-08-09 Incyte Corporation Derivatives of an FGFR inhibitor
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11607416B2 (en) 2019-10-14 2023-03-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002100863A1 (en) * 2001-06-12 2002-12-19 Glaxo Group Limited Corticotropin releasing factor antagonists
GB0117396D0 (en) * 2001-07-17 2001-09-05 Glaxo Group Ltd Chemical compounds
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
CA2550948A1 (en) * 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc. Crf receptor antagonists and methods relating thereto
GB0519957D0 (en) * 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
WO2006044821A1 (en) * 2004-10-19 2006-04-27 Sb Pharmco Puerto Rico Inc. Crf receptor antagonists and methods relating thereto
US8088779B2 (en) * 2005-09-30 2012-01-03 Smithkline Beecham (Cork) Limited Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (CRF) receptor antagonists
US8063050B2 (en) * 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ATE523499T1 (de) * 2006-07-06 2011-09-15 Array Biopharma Inc Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer
DE602007011628D1 (de) 2006-07-06 2011-02-10 Array Biopharma Inc Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren
CA2656364C (en) 2006-07-06 2014-11-25 Array Biopharma Inc. Dihydrothieno pyrimidines as akt protein kinase inhibitors
WO2008008887A2 (en) * 2006-07-13 2008-01-17 Smithkline Beecham Corporation Gpr119 agonists for treating metabolic disorders
DE102007004303A1 (de) 2006-08-04 2008-02-07 Osram Opto Semiconductors Gmbh Dünnfilm-Halbleiterbauelement und Bauelement-Verbund
US7879802B2 (en) 2007-06-04 2011-02-01 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
TWI450720B (zh) 2007-07-05 2014-09-01 Array Biopharma Inc 作為akt蛋白質激酶抑制劑之嘧啶環戊烷
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
US8377937B2 (en) * 2007-07-05 2013-02-19 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
AU2009204025B2 (en) * 2008-01-09 2014-02-20 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ES2401685T3 (es) * 2008-01-09 2013-04-23 Array Biopharma, Inc. Pirimidil ciclopentano hidroxilado como inhibidor de la proteína quinasa AKT
EP3239170B1 (en) 2008-06-04 2019-03-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
CN103874689B (zh) 2011-04-01 2016-04-27 基因泰克公司 Akt抑制剂化合物和威罗菲尼的组合及使用方法
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
EP2748166B1 (en) 2011-08-23 2018-07-11 Asana BioSciences, LLC Pyrimido-pyridazinone compounds and use thereof
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
WO2014145576A2 (en) 2013-03-15 2014-09-18 Northwestern University Substituted pyrrolo(2,3-d)pyrimidines for the treatment of cancer
US9708367B2 (en) 2013-03-15 2017-07-18 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase and their uses
CN104193745B (zh) * 2014-07-30 2016-09-28 斯芬克司药物研发(天津)股份有限公司 一种咪唑并嘧啶羧酸类化合物及其制备方法
MX2020010568A (es) 2018-04-09 2020-10-22 Raqualia Pharma Inc Derivados de urea ciclica fusionada como antagonista de crhr2.
WO2021247862A1 (en) * 2020-06-03 2021-12-09 Yumanity Therapeutics, Inc. Bicyclic heteroarenes and methods of their use

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995033750A1 (en) * 1994-06-08 1995-12-14 Pfizer Inc. Corticotropin releasing factor antagonists
WO1998008846A1 (en) * 1996-08-27 1998-03-05 Pfizer Inc. Substituted 6,6-hetero-bicyclic derivatives
EP1082960A2 (en) * 1999-08-27 2001-03-14 Pfizer Products Inc. Use of CRF antagonists and related compositions for treating depression and modifying the circadian rhytm
EP1097709A2 (en) * 1999-10-29 2001-05-09 Pfizer Products Inc. Use of corticotropin releasing factor antagonists for treating syndrome X
EP1149583A2 (en) * 2000-04-13 2001-10-31 Pfizer Products Inc. Combinations of corticotropin releasing factor antagonists and growth hormone secretagogues

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9022644D0 (en) 1990-10-18 1990-11-28 Ici Plc Heterocyclic compounds
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
US6387894B1 (en) 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
SK3812002A3 (en) 1999-09-17 2003-09-11 Abbott Gmbh & Co Kg Pyrazolopyrimidines as therapeutic agents
EA200200424A1 (ru) 1999-09-30 2002-12-26 Ньюроджен Корпорейшн Некоторые гетероциклы, замещенные алкилендиамином

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995033750A1 (en) * 1994-06-08 1995-12-14 Pfizer Inc. Corticotropin releasing factor antagonists
WO1998008846A1 (en) * 1996-08-27 1998-03-05 Pfizer Inc. Substituted 6,6-hetero-bicyclic derivatives
EP1082960A2 (en) * 1999-08-27 2001-03-14 Pfizer Products Inc. Use of CRF antagonists and related compositions for treating depression and modifying the circadian rhytm
EP1097709A2 (en) * 1999-10-29 2001-05-09 Pfizer Products Inc. Use of corticotropin releasing factor antagonists for treating syndrome X
EP1149583A2 (en) * 2000-04-13 2001-10-31 Pfizer Products Inc. Combinations of corticotropin releasing factor antagonists and growth hormone secretagogues

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHRISTOS ET AL: "Corticotropin-releasing factor antagonists", EXPERT OPINION ON THERAPEUTIC PATENTS, ASHLEY PUBLICATIONS, GB, vol. 8, no. 2, February 1998 (1998-02-01), pages 143 - 152, XP002109498, ISSN: 1354-3776 *
MCCARTHY J R ET AL: "RECENT ADVANCES WITH THE CRF1 RECEPTOR: DESIGN OF SMALL MOLECULE INHIBITORS, RECEPTOR SUBTYPES AND CLINICAL INDICATIONS", CURRENT PHARMACEUTICAL DESIGN, BENTHAM SCIENCE PUBLISHERS, SCHIPHOL, NL, vol. 5, no. 5, 1999, pages 289 - 315, XP000882142, ISSN: 1381-6128 *

Cited By (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006515334A (ja) * 2003-01-16 2006-05-25 エスビー ファームコ プエルト リコ インコーポレーテッド CRF受容体アンタゴニストとしてのヘテロアリール置換ピロロ[2,3−b]ピリジン誘導体
JP2006522799A (ja) * 2003-04-09 2006-10-05 エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド 縮合n−ヘテロサイクリック化合物およびcrf受容体アンタゴニストとしてのその使用
WO2004094420A1 (en) * 2003-04-09 2004-11-04 Sb Pharmco Puerto Rico Inc Condensed n-heterocyclic compounds and their use as crf receptor antagonists
JP4866722B2 (ja) * 2003-04-09 2012-02-01 スミスクライン ビーチャム (コーク) リミテッド 縮合n−ヘテロサイクリック化合物およびcrf受容体アンタゴニストとしてのその使用
AU2004232551C1 (en) * 2003-04-09 2010-06-17 Neurocrine Biosciences Inc Condensed N-heterocyclic compounds and their use as CRF receptor antagonists
EP2186813A1 (en) * 2003-04-09 2010-05-19 SmithKline Beecham (Cork) Limited Condensed N-heterocyclic compounds and their use as CRF receptor antagonists
US7427630B2 (en) 2003-04-09 2008-09-23 Sb Pharmaco Puerto Rico Inc. Condensed N-heterocyclic compounds and their use as CRF receptor antagonists
AU2004232551B2 (en) * 2003-04-09 2008-09-11 Neurocrine Biosciences Inc Condensed N-heterocyclic compounds and their use as CRF receptor antagonists
WO2004099209A1 (en) * 2003-05-05 2004-11-18 F. Hoffmann-La-Roche Ag Fused pyrimidine derivatives with crf activity
CN100372851C (zh) * 2003-05-05 2008-03-05 弗·哈夫曼-拉罗切有限公司 具有crf活性的稠合的嘧啶衍生物
JP2006525261A (ja) * 2003-05-05 2006-11-09 エフ.ホフマン−ラ ロシュ アーゲー Crf活性を有する縮合ピリミジン誘導体
KR100767272B1 (ko) * 2003-05-05 2007-10-17 에프. 호프만-라 로슈 아게 Crf 활성을 갖는 융합 피리미딘 유도체
US7307082B2 (en) 2003-05-05 2007-12-11 Roche Palo Alto Llc Heterocyclic derivatives as CRF antagonists
US7135476B2 (en) 2003-08-12 2006-11-14 Roche Palo Alto Llc Spiro tetrahydroquinazolines and dihydrocyclopentapyrimidines as CRF antagonists
US7223767B2 (en) 2003-08-12 2007-05-29 Roche Palo Alto Llc Tetrahydroquinazolines and dihydrocyclopentapyrimidines as CRF antagonists
WO2005014557A1 (en) * 2003-08-12 2005-02-17 F.Hoffmann-La Roche Ag Tetrahydroquinazoline derivatives as cfr antagonists
CN100398524C (zh) * 2003-08-12 2008-07-02 弗·哈夫曼-拉罗切有限公司 作为crf拮抗剂的四氢喹唑啉衍生物
JP2007517793A (ja) * 2004-01-06 2007-07-05 大正製薬株式会社 環状アミノ基によって置換されたチエノピリミジン及びチエノピリジン誘導体
WO2005085253A1 (en) * 2004-03-05 2005-09-15 Taisho Pharmaceutical Co., Ltd. Pyrrolopyrimidine derivatives
US8178543B2 (en) 2004-06-02 2012-05-15 Takeda Pharmaceutical Company Limited Bi- and tricyclic fused pyrimidines as tyrosine kinase inhibitors
WO2006001501A1 (en) * 2004-06-25 2006-01-05 Taisho Pharmaceutical Co., Ltd. Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with tetrahydropyridine as crf antagonists
WO2009107767A1 (ja) * 2008-02-29 2009-09-03 大日本住友製薬株式会社 H4受容体アンタゴニスト作用を有する新規2環性ピリミジン誘導体
US9533954B2 (en) 2010-12-22 2017-01-03 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US10213427B2 (en) 2010-12-22 2019-02-26 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US10813930B2 (en) 2010-12-22 2020-10-27 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US11053246B2 (en) 2012-06-13 2021-07-06 Incyte Corporation Substituted tricyclic compounds as FGFR inhibitors
US11840534B2 (en) 2012-06-13 2023-12-12 Incyte Corporation Substituted tricyclic compounds as FGFR inhibitors
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US10131667B2 (en) 2012-06-13 2018-11-20 Incyte Corporation Substituted tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9745311B2 (en) 2012-08-10 2017-08-29 Incyte Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US10947230B2 (en) 2013-04-19 2021-03-16 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US10450313B2 (en) 2013-04-19 2019-10-22 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US11530214B2 (en) 2013-04-19 2022-12-20 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US10040790B2 (en) 2013-04-19 2018-08-07 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11173162B2 (en) 2015-02-20 2021-11-16 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10214528B2 (en) 2015-02-20 2019-02-26 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10632126B2 (en) 2015-02-20 2020-04-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10738048B2 (en) 2015-02-20 2020-08-11 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9801889B2 (en) 2015-02-20 2017-10-31 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10251892B2 (en) 2015-02-20 2019-04-09 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9708318B2 (en) 2015-02-20 2017-07-18 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11014923B2 (en) 2015-02-20 2021-05-25 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11667635B2 (en) 2015-02-20 2023-06-06 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9890156B2 (en) 2015-02-20 2018-02-13 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10016438B2 (en) 2015-02-20 2018-07-10 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11472801B2 (en) 2017-05-26 2022-10-18 Incyte Corporation Crystalline forms of a FGFR inhibitor and processes for preparing the same
US10611762B2 (en) 2017-05-26 2020-04-07 Incyte Corporation Crystalline forms of a FGFR inhibitor and processes for preparing the same
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11607416B2 (en) 2019-10-14 2023-03-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11407750B2 (en) 2019-12-04 2022-08-09 Incyte Corporation Derivatives of an FGFR inhibitor
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors

Also Published As

Publication number Publication date
NO20034836D0 (no) 2003-10-29
HUP0304054A2 (hu) 2004-04-28
MXPA03009938A (es) 2005-09-07
ES2301633T3 (es) 2008-07-01
KR20040015206A (ko) 2004-02-18
CA2446514A1 (en) 2002-11-07
IL158062A0 (en) 2004-03-28
AR033295A1 (es) 2003-12-10
PL366934A1 (en) 2005-02-07
EP1383747A1 (en) 2004-01-28
AU2002253357B2 (en) 2006-08-24
NO20034836L (no) 2003-10-29
ATE386727T1 (de) 2008-03-15
DE60225127D1 (en) 2008-04-03
CN1649848A (zh) 2005-08-03
CZ20032946A3 (en) 2004-05-12
DE60225127T2 (de) 2009-02-19
BR0209267A (pt) 2004-06-15
US7279474B2 (en) 2007-10-09
JP2004528349A (ja) 2004-09-16
EP1383747B1 (en) 2008-02-20
US20040176400A1 (en) 2004-09-09

Similar Documents

Publication Publication Date Title
AU2002253357B2 (en) Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
AU2002253357A1 (en) Fused pyrimidines as antagonists of the corticotropin releasing factor (CRF)
US7427630B2 (en) Condensed N-heterocyclic compounds and their use as CRF receptor antagonists
US20070219232A1 (en) Chemical Compounds
AU2002328899A1 (en) Hetero-bicyclic CRF antagonists
US7462622B2 (en) Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists
AU2002354916B2 (en) Chemical compounds
AU2002354916A1 (en) Chemical compounds
US20070021429A1 (en) Condensed n-heterocyclic compounds and their use as crf receptor antagonists
US7273871B2 (en) Phenyl-5,6,6A,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene derivatives as CRF antagonists
ZA200307367B (en) Fused pyrimidines as antagonists of the corticotropin releasing factor (CRF).
JP2004528342A (ja) Crf受容体アンタゴニスト

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 01499/DELNP/2003

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 2003/07367

Country of ref document: ZA

Ref document number: 158062

Country of ref document: IL

Ref document number: 200307367

Country of ref document: ZA

Ref document number: 528365

Country of ref document: NZ

WWE Wipo information: entry into national phase

Ref document number: 2002253357

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2002722478

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 1-2003-501064

Country of ref document: PH

WWE Wipo information: entry into national phase

Ref document number: PA/a/2003/009938

Country of ref document: MX

Ref document number: PV2003-2946

Country of ref document: CZ

Ref document number: 1020037014160

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: 2002585397

Country of ref document: JP

Ref document number: 2446514

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 028107462

Country of ref document: CN

WWP Wipo information: published in national office

Ref document number: 2002722478

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWE Wipo information: entry into national phase

Ref document number: 10476368

Country of ref document: US

WWP Wipo information: published in national office

Ref document number: PV2003-2946

Country of ref document: CZ

WWR Wipo information: refused in national office

Ref document number: PV2003-2946

Country of ref document: CZ

WWG Wipo information: grant in national office

Ref document number: 2002253357

Country of ref document: AU

WWG Wipo information: grant in national office

Ref document number: 2002722478

Country of ref document: EP