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1. WO2006040966 - AROMATIC-RING-FUSED PYRIMIDINE DERIVATIVE

Publication Number WO/2006/040966
Publication Date 20.04.2006
International Application No. PCT/JP2005/018412
International Filing Date 05.10.2005
IPC
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
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
A61K 31/5377 2006.01
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
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/54 2006.01
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
54having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
A61K 31/55 2006.01
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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 3/10 2006.01
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
CPC
A61P 3/10
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 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 5/50
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
48of the pancreatic hormones
50for increasing or potentiating the activity of insulin
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 495/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 513/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • アステラス製薬株式会社 Astellas Pharma Inc. [JP]/[JP] (AllExceptUS)
  • 米▲徳▼ 康博 YONETOKU, Yasuhiro [JP]/[JP] (UsOnly)
  • 根来 賢二 NEGORO, Kenji [JP]/[JP] (UsOnly)
  • 恩田 健一 ONDA, Kenichi [JP]/[JP] (UsOnly)
  • 早川 昌彦 HAYAKAWA, Masahiko [JP]/[JP] (UsOnly)
  • 流石 大輔 SASUGA, Daisuke [JP]/[JP] (UsOnly)
  • 二川原 充啓 NIGAWARA, Takahiro [JP]/[JP] (UsOnly)
  • 飯久保 一彦 IIKUBO, Kazuhiko [JP]/[JP] (UsOnly)
  • 森友 博幸 MORITOMO, Hiroyuki [JP]/[JP] (UsOnly)
  • 吉田 茂 YOSHIDA, Shigeru [JP]/[JP] (UsOnly)
  • 大石 崇秀 OHISHI, Takahide [JP]/[JP] (UsOnly)
Inventors
  • 米▲徳▼ 康博 YONETOKU, Yasuhiro
  • 根来 賢二 NEGORO, Kenji
  • 恩田 健一 ONDA, Kenichi
  • 早川 昌彦 HAYAKAWA, Masahiko
  • 流石 大輔 SASUGA, Daisuke
  • 二川原 充啓 NIGAWARA, Takahiro
  • 飯久保 一彦 IIKUBO, Kazuhiko
  • 森友 博幸 MORITOMO, Hiroyuki
  • 吉田 茂 YOSHIDA, Shigeru
  • 大石 崇秀 OHISHI, Takahide
Agents
  • 森田 拓 MORITA, Hiroshi
Priority Data
2004-29555908.10.2004JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) AROMATIC-RING-FUSED PYRIMIDINE DERIVATIVE
(FR) DÉRIVÉ POLYCYCLIQUE AROMATIQUE DE PYRIMIDINE
(JA) 芳香環縮合ピリミジン誘導体
Abstract
(EN)
A novel pyrimidine derivative in which pyrimidine has been fused with an aromatic heterocycle selected among thiophene, thiazole, and pyridine or a pharmaceutically acceptable salt of the derivative; and a medicinal composition containing the compound or salt as an active ingredient. These compounds have excellent activity in accelerating insulin secretion and excellent activity in inhibiting the increase of a blood sugar level. Therefore, the medicinal composition containing the compound or salt as an active ingredient is useful, based on these activities, for the treatment and/or prevention of insulin-dependent diabetes mellitus (type 1 diabetes), noninsulin-dependent diabetes mellitus (type 2 diabetes), insulin-resistant diseases, and obesity.
(FR)
La présente invention a pour objet un nouveau dérivé de pyrimidine, ou un sel de qualité pharmaceutique dudit dérivé, où la pyrimidine forme un système polycyclique avec un hétérocycle aromatique sélectionné parmi les cycles suivants : thiophène, thiazole, et pyridine. La présente invention décrit également une préparation thérapeutique contenant ledit dérivé ou son sel au titre de principe actif. Lesdits composés présentent d’excellentes propriétés en terme d’accélération de la sécrétion d’insuline et d’activité inhibitrice de l'augmentation de la glycémie sanguine. Ainsi la préparation thérapeutique contenant ledit dérivé ou son sel au titre de principe actif peut-elle être employée, en se basant sur ces propriétés, pour le traitement prophylactique et/ou thérapeutique de diabètes sucrés insulino-dépendants (diabètes de type 1), de diabètes sucrés non insulino-dépendants (diabètes de type 2), de maladies insulino-résistantes, et de l'obésité.
(JA)
 チオフェン、チアゾール、ピリジンから選択される芳香族へテロ環と縮合した、新規なピリミジン誘導体又はその製薬学的に許容される塩、及び該化合物を有効成分とする医薬組成物を提供する。これらの化合物は、優れたインスリン分泌促進作用及び血糖上昇抑制作用を示す。従って、これらの化合物を有効成分とする医薬組成物は、これらの作用に基づき、インスリン依存性糖尿病(1型糖尿病)、インスリン非依存性糖尿病(2型糖尿病)、インスリン抵抗性疾患及び肥満の治療及び/又は予防に有用である。
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