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1. WO2004076458 - PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES

Publication Number WO/2004/076458
Publication Date 10.09.2004
International Application No. PCT/JP2004/002522
International Filing Date 01.03.2004
IPC
A61K 31/519 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 1/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 7/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
A61P 13/12 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
CPC
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
Applicants
  • TEIJIN PHARMA LIMITED [JP]/[JP] (AllExceptUS)
  • KATAOKA, Kenichiro [JP]/[JP] (UsOnly)
  • SUZUKI, Naotaka [JP]/[JP] (UsOnly)
  • KOSUGI, Tomomi [JP]/[JP] (UsOnly)
  • IMAI, Minoru [JP]/[JP] (UsOnly)
  • MAKINO, Hiroaki [JP]/[JP] (UsOnly)
  • TAKAKUWA, Mika [JP]/[JP] (UsOnly)
  • UNOKI, Gen [JP]/[JP] (UsOnly)
  • FUJINO, Aiko [JP]/[JP] (UsOnly)
  • OUE, Yasuhiro [JP]/[JP] (UsOnly)
  • YAMAKOSHI, Yuko [JP]/[JP] (UsOnly)
  • SUGIURA, Satoshi [JP]/[JP] (UsOnly)
  • MITCHELL, Dale Robert [GB]/[GB] (UsOnly)
  • SIMPSON, Donald James [GB]/[GB] (UsOnly)
  • HARRIS, Clifford John [GB]/[GB] (UsOnly)
  • LE, Joelle [GB]/[GB] (UsOnly)
Inventors
  • KATAOKA, Kenichiro
  • SUZUKI, Naotaka
  • KOSUGI, Tomomi
  • IMAI, Minoru
  • MAKINO, Hiroaki
  • TAKAKUWA, Mika
  • UNOKI, Gen
  • FUJINO, Aiko
  • OUE, Yasuhiro
  • YAMAKOSHI, Yuko
  • SUGIURA, Satoshi
  • MITCHELL, Dale Robert
  • SIMPSON, Donald James
  • HARRIS, Clifford John
  • LE, Joelle
Agents
  • MIHARA, Hideko
Priority Data
0304665.328.02.2003GB
0329446.919.12.2003GB
60/500,69508.09.2003US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES
(FR) DERIVES DE PYRAZOLO[1,5-A]PYRIMIDINE
Abstract
(EN) The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth. H,N,R3
(FR) La présente invention a trait à des dérives de pyrazolo[1,5-a]pyrimidine de formule (I) et leurs sels pharmaceutiquement acceptables présentant une excellente activité inhibitrice de la kinase. L'invention a également trait à des médicaments comportant les composés comme principes actifs utiles en tant qu'agents thérapeutiques ou prophylactiques pour un trouble lié à la protéine kinase dans lequel la kinase est impliquée, tel que la maladie inflammatoire, la maladie auto-immune, le trouble destructeur d'os, le cancer et/ou la croissance tumorale.
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