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TAAR SUBSTITUTED AZETIDINE DERIVATIVES AS TAAR LIGANDS
专利权人:
에프. 호프만-라 로슈 아게
发明人:
세세레 쥬셉페,갈레이 귀도,놀크로스 로거,플리제 필립,라우버 에띠앙
申请号:
KR1020177004440
公开号:
KR1020170031763A
申请日:
2015.08.24
申请国别(地区):
KR
年份:
2017
代理人:
摘要:
The present invention relates to compounds of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein: In this formula, R <; 1 >; is hydrogen, methoxy or fluoro; R 2 and R 2 ' are independently of each other hydrogen, methoxy or fluoro; R 3 and R 4 independently from each other are hydrogen or halogen; R <; 5 >; is hydrogen or fluoro; L 1 is -CH 2 -, -NR'-, -O-, -S-, CF 2 - or -CH =; Wherein R ' is hydrogen or lower alkyl; L 2 is a bond, -C (O) NH-, -NH-, -CH 2 NHC (O) -, -NHC (O) - or -NHC (O) NH-; R is hydrogen, halogen, lower alkoxy, or cyano; Or phenyl optionally substituted with one or more substituents selected from halogen, halogen-substituted lower alkyl and lower alkoxy; Or 5 or 6 membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl and pyrazolyl wherein the heteroaryl is optionally substituted by one or more substituents selected from halogen, lower alkyl, lower alkoxy, cyano, cycloalkyl , Halogen-substituted lower alkyl, halogen-substituted lower alkoxy and halogen-substituted phenyl; N is a ring nitrogen atom at the 1 or 2 position. The compounds of formula I have excellent affinity for the microamine binding receptor (TAAR), particularly TAAR1, and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress- Neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, energy expenditure and assimilation Disorders, body temperature homeostatic and dysfunction, sleep and physiological functional cycle disorders, and cardiovascular disorders.본 발명은 하기 화학식 I의 화합물 또는 이의 약학적으로 적합한 산 부가 염에 관한 것이다:상기 식에서,R1은 수소, 메톡시 또는 플루오로이고;R2 및 R2'는 서로 독립적으로 수소, 메톡시 또는 플루오로이고;R3 및 R4는 서로 독립적으로 수소 또는 할로겐이고;R5는 수소 또는 플루오로이고;L1은 -CH2-, -NR'-, -O-, -S-, CF2- 또는 -CH=이고; 이때 R'는 수소
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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