DIHYDROIMIDAZOTHIAZOLE DERIVATIVESCompounds of formula (I): or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.A compound of formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, halo, Ci-6alkyl optionally substituted by one or more halo atoms or hydroxy groups, C3-6 cycloalkyl optionally substituted by one or more halo atoms or hydroxy groups, Ci-2alkylC3.6 cycloalkyl optionally substituted by one or more halo atoms or hydroxy groups, Ci-6alkoxycarbonyl, cyano, -C=N-OR7, C2-6 alkenyl optionally substituted by one or more halo atoms or hydroxy groups in which hydroxy is not directly attached to either carbon of the double bond, C2-6 alkynyl optionally substituted by one or more halo atoms or hydroxy groups in which hydroxy is not directly attached to either carbon of the triple bond, (CH2)JSIR5R6, Ci-3alkoxy, Ci-3 alkylthio, Ci-3 alkoxyCi-3 alkyl or Ci-3 alkylthioCi-3 alkyl; R2 is an 8- to 10-membered bicyclic aromatic group optionally containing up to 3 heteroatoms selected from N and S, or phenyl, provided that R2 is not benzo[b]thiophene;R2 may be optionally substituted by one or more groups selected from halo, cyano, hydroxy, NR5R6, CONR5R6, or COOR7, or Ci-3 alkyl, C2-3 alkenyl, Ci-3 alkynyl, C3-6 cycloalkyl, Ci-3 alkoxy, Ci-3 hydroxyalkyl, C2-3 alkoxyalkyl or Ci-3 alkylS(O)n any of which may be optionally substituted by one or more halo atoms; or when R2 is phenyl two substituents on phenyl may join to form a fused C5-6 carbocyclic ring;R3 and R4 are independently hydrogen or Ci-3 alkyl;R5 and R6 are independently hydrogen or Ci-3 alkyl, or together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclyl group; R7 is hydrogen or Ci-3 alkyl; m is 1, 2 or 3; and n is 0, 1 or 2; provided that the compound is not: a) 3-naphthalen-l-yl-5,6-dihydroimidazo[2,l-b]thiazole hydrobromide, b) 3-naphthalen-2-yl-5,6-dihydroimidazo[2,l-b]thiazole hydrobromide, c) 3-(3-chloro-4-propoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, d) 3-(4-chlorophenyl)-2-ethyl-5,6-dihydroimidazo[2,l-b]thiazole, e) 3-(4-chlorophenyl)-2-methyl-5,6-dihydroimidazo[2,l-b]thiazole, f) 3-(3 ,4-dichlorophenyl)-5 ,6-dihydroimidazo[2, 1 -b]thiazole, g) 3-(2-hydroxy-5-methylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, h) 3-(4-aminophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, i) 3-(2-chlorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, j) 3-(3-chlorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, k) 3-(4-chlorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, 1) 3-(2,4-dichlorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, m) 3-(2,5-dichlorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, n) 3-(4-bromophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, o) 3-(2,4-difluorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, p) 3-(2-methylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, q) 3-(3-methylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, r) 3-(4-methylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, s) 3-(2,4-dimethylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, t) 3-(3,4-dimethylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, u) 3-(4-cyanophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, v) 3-(4-carboxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, w) 3-(2-methoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, x) 3-(3-methoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, y) 3-(4-methoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, z) 3-(2-hydroxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, aa) 3-(3-hydroxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, ab) 3-(4-hydroxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, ac) 3-(3,4-dihydroxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, ad) 3-(2-hydroxy-4-methoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, ae) 3-(3-hydroxy-4-methoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, af) 3-(4-hydroxy-3-methoxyphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, ag) 3-(4-hydroxy-3-chlorophenyl)-5,6-dihydroimidazo[2,l-b]thiazole, ah) 3-(4-hydroxy-3-methylphenyl)-5,6-dihydroimidazo[2,l-b]thiazole, or ai) 3-(3,4-dichlorophenyl)-2-phenyl-5,6-dihydroimidazo[2,l-b]thiazole.A compound of formula (Ia): (Ia) or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, halo, Ci-6alkyl optionally substituted by one or more halo atoms or hydroxy groups, C3-6 cycloalkyl optionally substituted by one or more halo atoms or hydroxy groups, Ci-2alkylC3.6 cycloalkyl optionally substituted by one or more halo atoms or hydroxy groups, Ci-6alkoxycarbonyl, cyano, -C=N-OR7, C2-6 alkenyl optionally substituted by one or more halo atoms or hydroxy groups in which hydroxy is not directly attached to either carbon of the double bond, C2-6 alkynyl optionally substituted by one or more halo atoms or hydroxy groups in which hydroxy is not directly attached to either carbon of the triple bond, (CH2)JSIR5R6, Ci-3alkoxy, Ci-3 alkylthio, Ci-3 alkoxyCi-3 alkyl or Ci-3 alkylthioCi-3 alkyl; R2 is an 8- to 10-membered bicyclic aromatic group optionally containing up to 3 heteroatoms selected from N and S, provided that R2 is not benzo[b]thiophene;R2 may be optionally substituted by one or more groups selected from halo, cyano, hydroxy, NR5R6, CONR5R6, or COOR7, or Ci-3 alkyl, Ci-3alkoxy, Ci-3 hydroxyalkyl...
디하이드로이미다조티아졸 유도체본 발명은, 노르아드레날린 재흡수 억제 및 임의로 5-HT 재흡수 억제 이외에 5-HT1A 효능작용을 나타내며, 비만 치료에 유용한 화학식 I의 화합물 또는 약제학적으로 허용되는 이의 염에 관한 것이다. 화학식 I  위의 화학식 I에서, R1 내지 R4는 명세서에 정의된 바와 같다.화학식 I의 화합물 또는 약제학적으로 허용되는 이의 염. 화학식 I  위의 화학식 I에서, R1은 수소, 할로, 하나 이상의 할로 원자 또는 하이드록시 그룹으로 임의로 치환된 C1-6알킬, 하나 이상의 할로 원자 또는 하이드록시 그룹으로 임의로 치환된 C3-6사이클로알킬, 하나 이상의 할로 원자 또는 하이드록시 그룹으로 임의로 치환된 C1-2알킬C3-6사이클로알킬, C1-6알콕시카보닐, 시아노, -C=N-OR7, 하나 이상의 할로 원자 또는 하이드록시 그룹으로 임의로 치환된 C2-6알케닐(여기서, 하이드록시는 이중 결합을 구성하는 탄소들 중 어느 것에도 직접 결합하지 않는다), 하나 이상의 할로 원자 또는 하이드록시 그룹으로 임의로 치환된 C2-6알키닐(여기서, 하이드록시는 삼중 결합을 구성하는 탄소들 중 어느 것에도 직접 결합하지 않는다), (CH2)mNR5R6, C1-3알콕시, C1-3알킬티오, C1-3알콕시C1-3알킬 또는 C1-3알킬티오C1-3알킬이고, R2는 N 및 S로부터 선택된 3개 이하의 헤테로원자를 임의로 함유하는 8 내지 10원 바이사이클릭 방향족 그룹, 또는 페닐이고, 단 R2는 벤조[b]티오펜이 아니며, R2는 할로, 시아노, 하이드록시, NR5R6, CONR5R6, COOR7, 또는 하나 이상의 할로 원자로 임의로 치환될 수 있는 C1-3알킬, C2-3알케닐, C1-3알키닐, C3-6사이클로알킬, C1-3알콕시, C1-3하이드록시알킬, C2-3알콕시알킬 및 C1-3알킬S(O)n으로부터 선택된 하나 이상의 그룹으로 임의로 치환될 수 있거나, R2가 페닐인 경우, 페닐의 2개의 치환체가 결합하여 융합된 C5-6카보사이클릭 환을 형성할 수 있고, R3 및 R4는 독립적으로 수소 또는 C1-3알킬이며, R5 및 R6은 독립적으로 수소 또는 C1-3알킬이거나, R5와 R6이 결합하고 있는 질소원자와 함께, 5원 또는 6원 헤테로사이클릴 환을 형성할 수 있고, R7은 수소 또는 C1-3알킬이며, m은 1, 2 또는 3이고, n은 0, 1 또는 2이며, 단, 하기 화합물은 제외된다: a) 3-나프탈렌-l-일-5,6-디하이드로이미다조[2,l-b]티아졸 하이드로브로마이드, b) 3-나프탈렌-2-일-5,6-디하이드로이미다조[2,l-b]티아졸 하이드로브로마이드, c) 3-(3-클로로-4-프로폭시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, d) 3-(4-클로로페닐)-2-에틸-5,6-디하이드로이미다조[2,l-b]티아졸, e) 3-(4-클로로페닐)-2-메틸-5,6-디하이드로이미다조[2,l-b]티아졸, f) 3-(3 ,4-디클로로페닐)-5,6-디하이드로이미다조[2,1-b]티아졸, g) 3-(2-하이드록시-5-메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, h) 3-(4-아미노페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, i) 3-(2-클로로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, j) 3-(3-클로로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, k) 3-(4-클로로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, 1) 3-(2,4-디클로로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, m) 3-(2,5-디클로로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, n) 3-(4-브로모페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, o) 3-(2,4-디플루오로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, p) 3-(2-메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, q) 3-(3-메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, r) 3-(4-메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, s) 3-(2,4-디메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, t) 3-(3,4-디메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, u) 3-(4-시아노페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, v) 3-(4-카복시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, w) 3-(2-메톡시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, x) 3-(3-메톡시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, y) 3-(4-메톡시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, z) 3-(2-하이드록시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, aa) 3-(3-하이드록시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, ab) 3-(4-하이드록시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, ac) 3-(3,4-디하이드록시페닐)-5,6-디하이드로이미다조[2,1-b]티아졸, ad) 3-(2-하이드록시-4-메톡시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, ae) 3-(3-하이드록시-4-메톡시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, af) 3-(4-하이드록시-3-메톡시페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, ag) 3-(4-하이드록시-3-클로로페닐)-5,6-디하이드로이미다조[2,l-b]티아졸, ah) 3-(4-하이드록시-3-메틸페닐)-5,6-디하이드로이미다조[2,l-b]티아졸 또는 ai) 3-(3,4-디클로로페닐)-2-페닐-5,6-디하이드로이미다조[2,l-b]티아졸.