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1. WO2016027757 - NOVEL 2-AMINBENZOYL DERIVATIVE

Publication Number WO/2016/027757
Publication Date 25.02.2016
International Application No. PCT/JP2015/073002
International Filing Date 17.08.2015
IPC
C07C 225/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a -CHO group, e.g. amino ketones
22having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
A61K 31/137 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
135having aromatic rings, e.g. methadone
137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/397 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
397having four-membered rings, e.g. azetidine
A61K 31/40 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/4462 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4462only substituted in position 3
A61P 25/04 2006.01
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
CPC
A61K 31/137
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine ; or methadone
A61K 31/397
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
397having four-membered rings, e.g. azetidine
A61K 31/40
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/4462
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
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4462only substituted in position 3
C07C 225/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
22having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07D 205/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
Applicants
  • 国立大学法人大阪大学 OSAKA UNIVERSITY [JP]/[JP]
Inventors
  • ▲高▼井 健太郎 TAKAI, Kentaro
  • 水嶋 真吾 MIZUSHIMA, Shingo
  • 島田 昌一 SHIMADA, Shoichi
  • 山本 雪子 YAMAMOTO, Yukiko
Agents
  • 鮫島 睦 SAMEJIMA, Mutsumi
Priority Data
2014-16614018.08.2014JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) NOVEL 2-AMINBENZOYL DERIVATIVE
(FR) NOUVEAU DÉRIVÉ DE 2-AMINOBENZOYLE
(JA) 新規2-アミノベンゾイル誘導体
Abstract
(EN)
The present invention addresses the problem of providing a novel compound for realizing an effect on a therapeutic and/or preventive drug for mental illnesses, such as depression, atypical depression, treatment-resistant depression, anxiety neurosis, bipolar disorder, obsessive-compulsive disorder, and PTSD, for chronic pain symptoms such as fibromyalgia, and for chronic pruritus, such effect due to the conversion of a metabolic structure product which exists in the tryptophan metabolic pathway. The present invention relates to a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a hydrate or solvate of the compound or salt, and the medical use of same. [In the formula, Q is the following formulas (2a) through (2c) (where R1 is a hydrogen atom, and the like; R2 and R3 are the same or different and are selected from a hydrogen atom, and the like, or together with carbon atoms that bond therewith, optionally form a 3- to 8-member cycloalkane ring; R4 and R5 are the same or different and are selected from a hydrogen atom, and the like, or together with the nitrogen atoms that bond therewith, optionally form a 3- to 8-member cyclic amine; and n is 0, 1, 2, 3, 4 or 5.)]
(FR)
Le problème abordé par cette invention est de pourvoir à un nouveau composé pour produire un effet sur un médicament destiné à traiter et/ou à prévenir les maladies mentales, telles que la dépression, la dépression atypique, la dépression résistant aux traitements, la névrose d'angoisse, les troubles bipolaires, un trouble obsessionnel compulsif, et le PTSD, des symptômes de douleur chronique tels que la fibromyalgie, et le prurit chronique, cet effet étant dû à la conversion d'un produit à structure métabolique qui est présent dans la voie métabolique du tryptophane. La solution selon l'invention porte sur un composé représenté par la formule (1) ou un sel pharmaceutiquement acceptable de celui-ci, ou un hydrate ou un solvate du composé ou du sel, et son utilisation en médecine. [Dans la formule, Q représente les formules (2a) à (2c) suivantes (où R1 est un atome d'hydrogène, et autre ; R2 et R3 sont identiques ou différents et sont choisis parmi un atome d'hydrogène, et autre, ou ensemble avec les atomes de carbone auxquels ils sont liés, ils forment éventuellement un cycle cycloalcane de 3 à 8 chaînons ; R4 et R5 sont identiques ou différents et sont choisis parmi un atome d'hydrogène, et autre, ou ensemble avec les atomes d'azote ils sont liés, ils forment éventuellement une amine cyclique ; et n est 0, 1, 2, 3, 4 ou 5)].
(JA)
 本発明の課題は、トリプトファン代謝経路に存在する代謝産物の構造を変換することにより、うつ病、非定型うつ病、治療抵抗性うつ病、不安神経症、双極性障害、強迫性障害、PTSDなどの精神疾患並びに線維筋痛症のような慢性疼痛症状および慢性掻痒の治療および/または予防薬に効果を発揮する新規化合物を提供することである。本発明は、式(1)で表される化合物もしくはその薬学上許容される塩、またはそれらの水和物もしくは溶媒和物およびその医薬用途に関する。 [式中、Qは下記式(2a)~(2c): (式中、Rは水素原子等を表し;RおよびRは、同一または異なって、水素原子等を表すか;あるいは、それらが結合する炭素原子と一緒になって、3員~8員のシクロアルカン環を形成してもよく;RおよびRは、同一または異なって、水素原子等を表すか;あるいは、それらが結合する窒素原子と一緒になって、3員~8員の環状アミンを形成してもよく;nは0、1、2、3、4、または5を表す]
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