Melanocortin receptor agonists

PURPOSE: Provided is a melanocortin 4 receptor(MC4R) agonist, to accelerate the function of the melanocortin 4 receiptor(MC4R) and to prevent and treat diseases associated with the MC4R such as obesity, diabetes and sexual disorder. CONSTITUTION: Compounds functioning as a melanocortin 4 receptor(MC...

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Hauptverfasser: AHN, IN AE, CHOI, DEOK YEONG, PARK, HUI SUL, LEE, GU, LIM, HYEON JU, JUNG, WON HYEOK, PARK, SUK GYEONG, YOO, HYEON JU
Format: Patent
Sprache:eng ; kor
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Zusammenfassung:PURPOSE: Provided is a melanocortin 4 receptor(MC4R) agonist, to accelerate the function of the melanocortin 4 receiptor(MC4R) and to prevent and treat diseases associated with the MC4R such as obesity, diabetes and sexual disorder. CONSTITUTION: Compounds functioning as a melanocortin 4 receptor(MC4R) agonist are represented by formula(1), wherein A is hydrogen, COR1, CO2R1, SO2R1, SO2NHR1, SO2N(R1)2, PO(OR1)2, C1-8-alkyl, (CH2)n, (CH2)n-aryl or (CH2)n-heteroaryl in which R1 is hydrogen, C1-8-alkyl, (CH2)n-C3-7-cycloalkyl, (CH2)n-aryl or (CH2)n-heteroaryl, n is an integer of 1 to 7; B and E are independently hydrogen, C1-8-alkyl, (CH2)n-C3-7-cycloalkyl, (CH2)n-aryl, (CH2)n-heteroaryl, (CH2)n-heterocycle, (CH2)n-amino, (CH2)n-(alkyl)amino, (CH2)n-(dialkyl)amino, (CH2)n-amide(CONH2) or (CH2)n-O(CH2)aryl in which n is an integer of 0 to 7; C is (CH2)m-heteroaryl, (CH2)m-heterocycle, (CH2)m-NH-heteroaryl, (CH2)m-NH-heterocycle, (CH2)m-NH-(alkylsulfonyl), (CH2)m-NH-(arylsulfonyl), (CH2)m-NH-alkoxycarbonyl, (CH2)m-NH-alkylamino carbamoyl, (CH2)m-NH-C(O)-heteroaryl, (CH2)m-NH-C(O)-heterocycle, (CH2)m-NH-(CH2)m-heteroaryl, (CH2)m-NH-(CH2)m-heterocycle, (CH2)m-NH-C(O)-(CH2)m-heteroaryl, (CH2)m-NH-C(O)-(CH2)m-heterocycle, C(O)-heterocycle, (CH2)m-NH-alkylester, (CH2)m-NH-alkyl amide, alkoxycarbonyl, (CH2)m-O-(alkylsulfonyl), (CH2)m-O-(arylsulfonyl), alkylamino carbamoyl, hydroxyalkyl amino carbamoyl, arylamino carbamoyl or hydrogen which are substituted or unsubstituted by a substituent selected from the group consisting of halogen, C1-5 alkyl, trifluoromethyl, hydroxy, C1-3 alkyloxy, amino, (C1-3 alkyl)amino, (C1-3 alkyl)2amino, cyano, carboxy(CO2H), CO2-C1-3 alkyl, CONH2, amidine(C(NH)NH2), nitro and oxo(C=O) in which m is an integer of 0 to 2; D is piperidine, pyrrolidine, hexamethyleneimine, 2 or 3 oxo piperidine and hexamethyleneimine, pyrrolidine or dialkylamine; and Cy is C5-C7-aryl or C5-7 cycloalkyl which is substituted or unsubstituted by a substituent selected from the group consisting of C1-C5-alkyl, halogen, trifluoromethyl, hydroxy, C1-C3-alkyloxy, amino, (C1-C3-alkyl)amino, di(C1-C3-alkyl)amino and oxo(C=O). 본 발명은 멜라노코틴 수용체에 대한 항진활성이 우수한 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염, 용매화물 및 이성체, 및 이를 유효 성분으로 함유함을 특징으로 하는 멜라노코틴 수용체의 기능항진제 조성물에 관한 것이다: 상기식에서, B, C, D, G 및 Cy는 명세서에 정의한 바와 같다.