NEW COMPOUNDS VIIThe present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.A compound of formula (I)or a pharmaceutically acceptable salt, solvate, hydrate, geometrical isomer, tautomer, optical isomer or JV-oxide thereof, wherein:A is C5_8-cycloalkyl;X is N or C(H); Y is O, N(R3) or CH2;R1 is selected from hydrogen, Ci_6-alkyl, Ci_6-acyl (both optionally substituted with one or more substituents independently selected from halogen, hydroxy, cyano andCi_6-alkoxy), phenyl and benzyl (both optionally substituted with one or more substituents independently selected from halogen, hydroxy, cyano, nitro, CF3, Chalky 1 and Ci_6-alkoxy);each R2 is independently selected from halogen, hydroxy, Ci_6-alkyl and Ci_6-alkoxy(both optionally substituted with one or more substituents independently selected from halogen, hydroxy and Ci_6-alkoxy);each R3 is independently selected from H and Ci_4-alkyl;each R4 is independently selected from halogen, hydroxy, cyano, Ci_6-alkyl and C1-6- alkoxy (both optionally substituted with one or more substituents independently selected from halogen, hydroxy and Ci_6-alkoxy), phenyl and benzyl (both optionally substituted with one or more substituents independently selected from halogen, hydroxy, cyano, nitro, CF3, Ci_6-alkyl and Ci_6-alkoxy); - -a is 0, 1 or 2; b is 1 or 2; and c and d are each independently 0, 1, 2 or 3;provided that the compound is not selected from the group consisting of:• 1 -(3-chloro-2,2-dimethyl- 1 -oxopropyl)-N-[(cyclohexylamino)carbonyl]-4- piperidinemethanamine;• N-cyclohexyl-N'-[[ 1 -[(4-methoxyphenyl)methyl]-4-piperidinyl]methyl]urea; • N-cyclohexyl-N,N'-dimethyl-N'-(4-piperidinylmethyl)urea;• 4-piperidinylmethyl cyclohexylcarbamate;• 2-[l-(phenylmethyl)-4-piperidinyl]ethyl cyclohexylcarbamate;• 4-piperidinylmethyl cyclohexyl(methyl)carbamate;• 2-(4-piperidinyl)ethyl cyclohexylcarbamate; • N-cyclopentyl-N,N'-dimethyl-N'-[2-(4-piperidinyl)ethyl]urea;• N'-cyclohexyl-N-methyl-N-(4-piperidinylmethyl)urea;• N-cyclohexyl- 1 -piperazinepropanamide;• N-(3-methylcyclohexyl)- 1 -piperazinepropanamide;• N-(2-methylcyclohexyl)- 1 -piperazinepropanamide; • N-(2,3-dimethylcyclohexyl)-l -piperazinepropanamide;• N-cyclohexyl-N'-[2-(l-piperazinyl)ethyl]urea;• 2-(4-methylpiperazin- 1 -yl)ethyl (2-phenylbicyclo[2.2.1 ]hept-2-yl)carbamate;• N-cyclohexyl- 1 -piperazinebutanamide;• N-cyclohexyl-3-(l,4-diazepan-l-yl)propanamide; • 3-(l,4-diazepan-l-yl)-N-(4-methylcyclohexyl)propanamide;• 4-(4-chlorophenyl)-N-cyclohexyl- 1 -piperazinepropanamide;• 4-(2-chlorophenyl)-N-cyclohexyl-N-methyl- 1 -piperazinepropanamide;• 4-(3-chlorophenyl)-N-cyclohexyl-N-methyl- 1 -piperazinepropanamide;• 4-(4-chlorophenyl)-N-cyclohexyl-N-methyl- 1 -piperazinepropanamide; • N- [2- [4-(2-methoxyphenyl)- 1 -piperazinyl] ethyl] -N'-( 1 -methylcyclohexyl)-urea;• N-cyclohexyl-4-(4-fluorophenyl)-N-methyl- 1 -piperazinepropanamide;• 4-(2-methoxyphenyl)-N-( 1 -methylcyclohexyl)- 1 -piperazinepropanamide;• N-cyclohexyl-4-(4-methylphenyl)- 1 -piperazinepropanamide; - -• N-cyclohexyl-4-(4-methoxyphenyl)-N-methyl- 1 -piperazinepropanamide;• N-cyclohexyl-N-methyl-4-(4-methylphenyl)- 1 -piperazinepropanamide;• N-cyclohexyl-4-(2-methoxyphenyl)-N-methyl- 1 -piperazinepropanamide;• N-cyclohexyl-N-methyl-4-[3-(trifluoromethyl)phenyl]- 1 -piperazinepropanamide; • N-cyclopentyl-1 -piperazinepropanamide;• N-cycloheptyl-1 -piperazinepropanamide; and• N-cyclohexyl-N'-(4-piperidinylmethyl)urea.
신규한 화합물 ＶＩＩ본 발명은 하기 화학식 I의 신규한 화합물, 상기 화합물을 포함하는 약학적 조성물 및 체중 증가, 2형 당뇨병 및 이상지질혈증과 연관된 병태에 대한 약제의 제조에서 렙틴 수용체 조절제 유사체로서 상기 화합물의 용도에 관한 것이다: 화학식 I하기 화학식 I의 화합물 또는 이의 약학적으로 허용되는 염, 용매화물, 수화물, 기하 이성체, 호변 이성체, 광학 이성체 또는 N-옥시드:화학식 I상기 화학식에서,A는 C5-8-시클로알킬이고;X는 N 또는 C(H)이며;Y는 O, N(R3) 또는 CH2이며;R1은 수소, C1-6-알킬, C1-6-아실(마지막 2개는 할로겐, 히드록시, 시아노 및 C1-6-알콕시에서 독립적으로 선택되는 1 이상의 치환기로 임의로 치환됨), 페닐 및 벤질(이 둘은 할로겐, 히드록시, 시아노, 니트로, CF3, C1-6-알킬 및 C1-6-알콕시에서 독립적으로 선택되는 1 이상의 치환기로 임의로 치환됨)에서 선택되며;각각의 R2는 독립적으로 할로겐, 히드록시, C1-6-알킬 및 C1-6-알콕시(마지막 2개는 할로겐, 히드록시 및 C1-6-알콕시에서 독립적으로 선택되는 1 이상의 치환기로 임의로 치환됨)에서 선택되고;각각의 R3은 독립적으로 H 및 C1-4-알킬에서 선택되고;각각의 R4는 독립적으로 할로겐, 히드록시, 시아노, C1-6-알킬 및 C1-6-알콕시(마지막 2개는 할로겐, 히드록시 및 C1-6-알콕시에서 독립적으로 선택되는 1 이상의 치환기로 임의로 치환됨), 페닐 및 벤질(이 둘은 할로겐, 히드록시, 시아노, 니트로, CF3, C1-6-알킬 및 C1-6-알콕시에서 독립적으로 선택되는 1 이상의 치환기로 임의로 치환됨)에서 선택되고;a는 0, 1 또는 2이고;b는 1 또는 2이고;c 및 d는 각각 독립적으로 0, 1, 2 또는 3이며;단, 상기 화합물은 하기로 구성된 군에서 선택되지 않는다:· 1-(3-클로로-2,2-디메틸-1-옥소프로필)-N-[(시클로헥실아미노)카르보닐]-4-피페리딘메탄아민;· N-시클로헥실-N'-[[1-[(4-메톡시페닐)메틸]-4-피페리디닐]메틸]우레아;· N-시클로헥실-N,N'-디메틸-N'-(4-피페리디닐메틸)우레아;· 4-피페리디닐메틸 시클로헥실카르바메이트;· 2-[1-(페닐메틸)-4-피페리디닐]에틸 시클로헥실카르바메이트;· 4-피페리디닐메틸 시클로헥실(메틸)카르바메이트;· 2-(4-피페리디닐)에틸 시클로헥실카르바메이트;· N-시클로펜틸-N,N'-디메틸-N'-[2-(4-피페리디닐)에틸]우레아;· N'-시클로헥실-N-메틸-N-(4-피페리디닐메틸)우레아;· N-시클로헥실-1-피페라진프로판아미드;· N-(3-메틸시클로헥실)-1-피페라진프로판아미드;· N-(2-메틸시클로헥실)-1-피페라진프로판아미드;· N-(2,3-디메틸시클로헥실)-1-피페라진프로판아미드;· N-시클로헥실-N'-[2-(1-피페라지닐)에틸]우레아;· 2-(4-메틸피페라진-1-일)에틸 (2-페닐비시클로[2.2.1]헵트-2-일)카르바메이트;· N-시클로헥실-1-피페라진부탄아미드;· N-시클로헥실-3-(1,4-디아제판-1-일)프로판아미드;· 3-(1,4-디아제판-1-일)-N-(4-메틸시클로헥실)프로판아미드;· 4-(4-클로로페닐)-N-시클로헥실-1-피페라진프로판아미드;· 4-(2-클로로페닐)-N-시클로헥실-N-메틸-1-피페라진프로판아미드;· 4-(3-클로로페닐)-N-시클로헥실-N-메틸-1-피페라진프로판아미드;· 4-(4-클로로페닐)-N-시클로헥실-N-메틸-1-피페라진프로판아미드;· N-[2-[4-(2-메톡시페닐)-1-피페라지닐]에틸]-N'-(1-메틸시클로헥실)-우레아;· N-시클로헥실-4-(4-플루오로페닐)-N-메틸-1-피페라진프로판아미드;· 4-(2-메톡시페닐)-N-(1-메틸시클로헥실)-1-피페라진프로판아미드;· N-시클로헥실-4-(4-메틸페닐)-1-피페라진프로판아미드;· N-시클로헥실-4-(4-메톡시페닐)-N-메틸-1-피페라진프로판아미드;· N-시클로헥실-N-메틸-4-(4-메틸페닐)-1-피페라진프로판아미드;· N-시클로헥실-4-(2-메톡시페닐)-N-메틸-1-피페라진프로판아미드;· N-시클로헥실-N-메틸-4-[3-(트리플루오로메틸)페닐]-1-피페라진프로판아미드;· N-시클로펜틸-1-피페라진프로판아미드;· N-시클로헵틸-1-피페라진프로판아미드; 및· N-시클로헥실-N'-(4-피페리디닐메틸)우레아.