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1. WO2006126695 - PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME

Publication Number WO/2006/126695
Publication Date 30.11.2006
International Application No. PCT/JP2006/310603
International Filing Date 22.05.2006
IPC
C07D 231/40 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Nitrogen atoms
40Acylated on said nitrogen atom
A61K 31/41 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/415 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
A61K 31/4155 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
4155not condensed and containing further heterocyclic rings
A61K 31/4184 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4184condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4192 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41921,2,3-Triazoles
CPC
A61K 31/41
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
A61K 31/415
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4151,2-Diazoles
A61K 31/4155
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4151,2-Diazoles
4155non condensed and containing further heterocyclic rings
A61K 31/4184
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4184condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4192
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41921,2,3-Triazoles
A61K 31/4196
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41961,2,4-Triazoles
Applicants
  • 日本たばこ産業株式会社 JAPAN TOBACCO INC. [JP]/[JP] (AllExceptUS)
  • 高木 正樹 TAKAGI, Masaki [JP]/[JP] (UsOnly)
  • 中村 健 NAKAMURA, Takeshi [JP]/[JP] (UsOnly)
  • 松田 勇 MATSUDA, Isamu [JP]/[JP] (UsOnly)
  • 福田 賢治 FUKUDA, Kenji [JP]/[JP] (UsOnly)
  • 小澤 浩一 OZAWA, Koichi [JP]/[JP] (UsOnly)
  • 上田 順久 UEDA, Nobuhisa [JP]/[JP] (UsOnly)
  • 坂田 薫 SAKATA, Kaoru [JP]/[JP] (UsOnly)
  • 野村 幸広 NOMURA, Yukihiro [JP]/[JP] (UsOnly)
Inventors
  • 高木 正樹 TAKAGI, Masaki
  • 中村 健 NAKAMURA, Takeshi
  • 松田 勇 MATSUDA, Isamu
  • 福田 賢治 FUKUDA, Kenji
  • 小澤 浩一 OZAWA, Koichi
  • 上田 順久 UEDA, Nobuhisa
  • 坂田 薫 SAKATA, Kaoru
  • 野村 幸広 NOMURA, Yukihiro
Agents
  • 大東 輝雄 DAITO, Teruo
Priority Data
2005-14884723.05.2005JP
2005-36728620.12.2005JP
60/685,03726.05.2005US
60/755,82003.01.2006US
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME
(FR) COMPOSÉ DE PYRAZOLE ET AGENT THÉRAPEUTIQUE POUR LE DIABÈTE COMPRENANT CELUI-CI
(JA) ピラゾール化合物及びそれらピラゾール化合物を含んでなる糖尿病治療薬
Abstract
(EN)
A pyrazole compound represented by the general formula (I) or a salt thereof which has a hepatic glycogen phosphorylase inhibitory activity and therefore is useful as a therapeutic or prophylactic agent for diabetes or a pharmacologically salt thereof : wherein the ring Q represents an aryl group or an aromatic heterocyclic group; R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azide group; R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo-C1-6 alkyl group, a C1-6 alkoxy group, an azide group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group; R4 and R5 independently represent a hydrogen atom, a C1-6 alkyl group which may be substituted, a a C3-8 cycloalkyl group, a saturated heterocyclic group which may be substituted, an aryl group which may be substituted, a C7-14 aralkyl group, an aromatic heterocyclic group or the like.
(FR)
Composé de pyrazole représenté par la formule générale (I) ou sel de celui-ci qui a une activité d'inhibition de la phosphorylase du glycogène hépatique et par conséquent qui est utile comme agent thérapeutique ou prophylactique pour le diabète ou sel acceptable du point de vue pharmacologique de celui-ci : (I) dans laquelle le cycle Q représente un groupe aryle ou un groupe hétérocyclique aromatique ; R1 représente un atome d'hydrogène, un atome d'halogène, un groupe alkyle en C1-6 ou un groupe alcoxy en C1-6 ; R2 représente un atome d'halogène, un groupe alkyle en C1-6, un groupe alcoxy en C1-6 ou un groupe azide ; R3 représente un atome d'halogène, un groupe hydroxyle, un groupe alkyle en C1-6, un groupe halo(alkyle en C1-6), un groupe alcoxy en C1-6, un groupe azide, un groupe amino, un groupe acylamino ou un groupe (alkyle en C1-6)sulfonylamino ; R4 et R5 représentent indépendamment un atome d'hydrogène, un groupe alkyle en C1-6 qui peut être substitué, un groupe cycloalkyle en C3-8, un groupe hétérocyclique saturé qui peut être substitué, un groupe aryle qui peut être substitué, un groupe aralkyle en C7-14, un groupe hétérocyclique aromatique ou similaire.
(JA)
本発明は、肝グリコーゲンホスホリラーゼ阻害活性を有し、糖尿病治療薬又はその予防薬として有用な下記一般式(I)で表されるピラゾール化合物又はその薬理学上許容される塩を提供する。(I)〔式中、環Qは、アリール基または芳香族複素環基を意味し、R1は、水素原子、ハロゲン原子、C1-6アルキル基またはC1-6アルコキシ基を意味し、R2は、ハロゲン原子、C1-6アルキル基、C1-6アルコキシ基またはアジド基を意味し、R3は、ハロゲン原子、水酸基、C1-6アルキル基、ハロC1-6アルキル基、C1-6アルコキシ基、アジド基、アミノ基、アシルアミノ基またはC1-6アルキルスルホニルアミノ基を意味し、R4、R5は同一又は異なって、水素原子、置換されてもよいC1-6アルキル基、C3-8シクロアルキル基、置換されてもよい飽和複素環基、置換されてもよいアリール基、C7-14アラルキル基、芳香族複素環基他を意味する。〕
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