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1. WO2007069712 - AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Publication Number WO/2007/069712
Publication Date 21.06.2007
International Application No. PCT/JP2006/325016
International Filing Date 15.12.2006
IPC
C07C 217/64 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
64with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
A61K 31/137 2006.1
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 31/165 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
165having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/222 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
22of acyclic acids, e.g. pravastatin
222with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/277 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
275Nitriles; Isonitriles
277having a ring, e.g. verapamil
A61K 31/325 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
325Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof
CPC
A61P 11/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
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
A61P 13/12
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
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
A61P 19/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
Applicants
  • MITSUBISHI TANABE PHARMA CORPORATION [JP]/[JP] (AllExceptUS)
  • 城内 正壽 KIUCHI, Masatoshi [JP]/[JP] (UsOnly)
  • 丸川 薫 MARUKAWA, Kaoru [JP]/[JP] (UsOnly)
  • 小林 信教 KOBAYASHI, Nobutaka [JP]/[JP] (UsOnly)
  • 菅原 邦夫 SUGAHARA, Kunio [JP]/[JP] (UsOnly)
Inventors
  • 城内 正壽 KIUCHI, Masatoshi
  • 丸川 薫 MARUKAWA, Kaoru
  • 小林 信教 KOBAYASHI, Nobutaka
  • 菅原 邦夫 SUGAHARA, Kunio
Priority Data
2005-36136315.12.2005JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
(FR) COMPOSE AMINE ET UTILISATION DE CELUI-CI POUR DES APPLICATIONS MEDICALES
(JA) アミン化合物及びその医薬用途
Abstract
(EN) Disclosed is a novel amine compound represented by the general formula (I) below, a pharmaceutically acceptable acid addition salt of the compound, or a hydrate or solvate of the compound or the salt, which is excellent in an immunosuppressing effect, a rejection response-suppressing effect and the like and is reduced in adverse side effects such as bradycardia. Also disclosed is a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. (I) wherein R represents a hydrogen atom or P(=O)(OH)2; X represents an oxygen or sulfur atom; Y represents CH2CH2 or CH=CH; R1 represents an alkyl having 1-4 carbon atoms which is substituted by a halogen atom or a cyano; R2 represents an alky having 1-4 carbon atoms which may be substituted by a hydroxyl group or a halogen atom; R3 and R4 independently represent a hydrogen atom or an alkyl having 1-4 carbon atoms; and n represents 5-8.
(FR) La présente invention concerne un nouveau composé aminé représenté par la formule générale (I) ci-dessous, un sel d'addition d'acide pharmaceutiquement acceptable du composé, ou un hydrate ou solvate du composé ou du sel, qui est excellent en terme d'effet immunosuppresseur, d'effet de suppression de réponse de rejet et similaire et a des effets secondaires indésirables tels que la brachycardie réduits. La présente invention concerne en outre une composition pharmaceutique comprenant le composé et un véhicule pharmaceutiquement acceptable. (I) où R représente un atome d'hydrogène ou P(=O)(OH)2 ; X représente un atome d'oxygène ou de soufre ; Y représente CH2CH2 ou CH=CH ; R1 représente un alkyle ayant de 1 à 4 atomes de carbone qui est substitué par un atome d'halogène ou un cyano ; R2 représente un alkyle ayant de 1 à 4 atomes de carbone qui peut être substitué par un groupe hydroxyle ou un atome d'halogène ; R3 et R4 représentent indépendamment un atome d'hydrogène ou un alkyle ayant de 1 à 4 atomes de carbone ; et n représente 5 à 8.
(JA)  免疫抑制作用、拒絶反応抑制作用等に優れ、徐脈等の副作用が軽減された下記一般式(I)で示される新規なアミン化合物、若しくはその製薬上許容しうる酸付加塩、又はそれらの水和物、若しくは溶媒和物並びにこれら化合物及び製薬上許容しうる担体を含有する医薬組成物。 (式中、Rは水素原子又はP(=O)(OH)、Xは酸素原子又は硫黄原子、YはCHCH又はCH=CH、Rはハロゲン原子で置換された炭素数1~4のアルキル又はシアノ、Rは水酸基で置換されていても良いか又はハロゲン原子で置換されていても良い炭素数1~4のアルキル、R及びRは同一又は異なっていても良く、それぞれ水素原子又は炭素数1~4のアルキル、nは5~8を示す。)
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