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1. WO2013058258 - BICYCLIC HETEROCYCLIC COMPOUND

Publication Number WO/2013/058258
Publication Date 25.04.2013
International Application No. PCT/JP2012/076771
International Filing Date 17.10.2012
IPC
C07D 231/56 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54condensed with carbocyclic rings or ring systems
56Benzopyrazoles; Hydrogenated benzopyrazoles
A61K 31/416 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
416condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4184 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
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 2006.1
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
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
A61K 31/4245 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4245Oxadiazoles
A61K 31/437 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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
CPC
A61P 19/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
A61P 25/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A61P 25/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
24Antidepressants
Applicants
  • アステラス製薬株式会社 ASTELLAS PHARMA INC. [JP]/[JP]
Inventors
  • 川上 晋平 KAWAKAMI, Shimpei
  • 桜井 稔 SAKURAI, Minoru
  • 河野 則征 KAWANO, Noriyuki
  • 鈴木 貴之 SUZUKI, Takayuki
  • 白石 宜之 SHIRAISHI, Nobuyuki
  • ▲浜▼口 渉 HAMAGUCHI, Wataru
  • 関岡 竜一 SEKIOKA, Ryuichi
  • 森友 博幸 MORITOMO, Hiroyuki
  • 森友 紋子 MORITOMO, Ayako
Agents
  • 森田 拓 MORITA, Hiroshi
Priority Data
2011-22882218.10.2011JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) BICYCLIC HETEROCYCLIC COMPOUND
(FR) COMPOSÉ HÉTÉROCYCLIQUE BICYCLIQUE
(JA) 二環式ヘテロ環化合物
Abstract
(EN) [Problem] To provide a compound useful as the active ingredient in a drug composition for treating diseases to which 11β-hydroxysteroid dehydrogenase type 1 contributes such as dementia, schizophrenia, depression, pain (particularly neuropathic pain and fibromyalgia), diabetes (particularly type 2 diabetes), and insulin resistance. [Solution] It was discovered that a bicyclic heterocyclic compound substituted with an acylamino group such as a (hetero)aroylamino group (the bicyclic heterocycle being formed by condensing a cyclohexane ring and a 5- or 6-membered monocyclic heterocycle having only a nitrogen atom as the heteroatom) or a pharmaceutically acceptable salt thereof has a superior selective inhibitory action with respect to 11β-HSD1. Thus, the bicyclic heterocyclic compound can be used in the treatment of dementia, schizophrenia, depression, pain (particularly neuropathic pain and fibromyalgia), diabetes (particularly type 2 diabetes), insulin resistance, and the like
(FR) L'objectif de cette invention est de pouvoir à un composé utile à titre de principe actif dans une composition médicamenteuse destinée à traiter les maladies auxquelles la 11β-hydroxystéroïde déshydrogénase de type 1 contribue telles que la démence, la schizophrénie, la dépression, la douleur (en particulier, la douleur névropathique et la fibromyalgie), le diabète (en particulier le diabète de type 2), et la résistance à l'insuline. A cet égard, on a découvert qu'un composé hétérocyclique bicyclique substitué par un groupe acylamino tel qu'un groupe (hétéro)aroylamino (l'hétérocycle bicyclique étant formé par condensation d'un cycle cyclohexane et d'un hétérocycle monocyclique ayant 5 ou 6 chaînons et seulement un atome d'azote à titre d'hétéroatome) ou un sel pharmaceutiquement acceptable de celui-ci a une action d'inhibition sélective supérieure envers la 11β-HSD1. Par conséquent, le composé hétérocyclique bicyclique selon l'invention peut être utilisé pour traiter la démence, la schizophrénie, la dépression, la douleur (en particulier, la douleur névropathique et la fibromyalgie), le diabète (en particulier le diabète de type 2), et la résistance à l'insuline et autre.
(JA) 【課題】認知症、統合失調症、うつ、疼痛(特に神経障害性疼痛、線維筋痛症)、糖尿病(特に2型糖尿病)、インスリン抵抗性等の11β-ヒドロキシステロイド デヒドロゲナーゼ タイプ1の関与する疾患治療用医薬組成物の有効成分としてとして有用な化合物の提供。 【解決手段】(ヘテロ)アロイルアミノ基等のアシルアミノ基で置換された二環式ヘテロ環化合物(該二環式ヘテロ環は、シクロヘキサン環と、ヘテロ原子として窒素原子のみを有する5乃至6員単環式ヘテロ環とが縮合して形成されている。)またはその製薬学的に許容される塩が11β-HSD1に優れた選択的阻害作用を有することを見出した。このことから、本発明の二環式ヘテロ環化合物は認知症、統合失調症、うつ、疼痛(特に神経障害性疼痛、線維筋痛症)、糖尿病(特に2型糖尿病)、インスリン抵抗等の治療に用いることができる。
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