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1. 发明授权

KR100661118B1 멜라노코틴 수용체의 항진제 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：KR100661118B1
公开(公告)日：2006-12-26
申请号：KR1020040092249
申请日：2004-11-12
申请人： 주식회사 엘지생명과학 , 아스텔라스세이야쿠 가부시키가이샤
发明人： 이구 , 박희술 , 안인애 , 유현주 , 김종엽 , 최덕영 , 임현주 , 정경하 , 심동섭 , 이상균 , 콘도유타카 , 히라바야시료지 , 혼다슈고 , 가쿠히데다카 , 시시쿠라준이치 , 이토히로유키 , 쿠라마다케시
IPC分类号： C07D207/14 , C07D403/12 , A61P3/00 , A61P15/10
CPC分类号： C04B35/632 , C07D205/04 , C07D207/14 , C07D211/58 , C07D401/12 , C07D403/12 , C07D405/12
摘要： 본 발명은 멜라노코틴 수용체에 대한 항진활성이 우수한 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염, 수화물, 용매화물 또는 이성체, 및 이를 유효성분으로 함유함을 특징으로 하는 멜라노코틴 수용체의 기능항진제 조성물에 관한 것이다:

상기 식에서 R
1 , R
2 , R
3 , R
4 , R
5 , n 및 m은 명세서에 정의한 바와 같다.

2. 发明公开

KR1020050045927A 멜라노코틴 수용체의 항진제 无效
标题翻译：黑皮质素受体激动剂
公开(公告)号：KR1020050045927A
公开(公告)日：2005-05-17
申请号：KR1020040092245
申请日：2004-11-12
申请人： 주식회사 엘지생명과학 , 아스텔라스세이야쿠 가부시키가이샤
发明人： 이구 , 박희술 , 안인애 , 유현주 , 최성필 , 최덕영 , 임현주 , 권오환 , 콘도유타카
IPC分类号： C07D211/34 , C07D211/32
CPC分类号： C07D401/04 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/34 , C07D211/58 , C07D401/14
摘要： 본 발명은 멜라노코틴 수용체에 대한 항진활성이 우수한 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염, 수화물, 용매화물 또는 이성체, 및 이를 유효성분으로 함유함을 특징으로 하는 멜라노코틴 수용체의 기능항진제 조성물에 관한 것이다:

상기 식에서 R
1 , R
2 , R
3 , R
4 , 및 R
5 는 명세서에 정의한 바와 같다.

3. 发明公开

KR1020050045928A 멜라노코틴 수용체의 항진제 失效
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020050045928A
公开(公告)日：2005-05-17
申请号：KR1020040092249
申请日：2004-11-12
申请人： 주식회사 엘지생명과학 , 아스텔라스세이야쿠 가부시키가이샤
发明人： 이구 , 박희술 , 안인애 , 유현주 , 김종엽 , 최덕영 , 임현주 , 정경하 , 심동섭 , 이상균 , 콘도유타카 , 히라바야시료지 , 혼다슈고 , 가쿠히데다카 , 시시쿠라준이치 , 이토히로유키 , 쿠라마다케시
IPC分类号： C07D207/14 , C07D403/12 , A61P3/00 , A61P15/10
CPC分类号： C04B35/632 , C07D205/04 , C07D207/14 , C07D211/58 , C07D401/12 , C07D403/12 , C07D405/12
摘要： 본 발명은 멜라노코틴 수용체에 대한 항진활성이 우수한 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염, 수화물, 용매화물 또는 이성체, 및 이를 유효성분으로 함유함을 특징으로 하는 멜라노코틴 수용체의 기능항진제 조성물에 관한 것이다:

상기 식에서 R
1 , R
2 , R
3 , R
4 , R
5 , n 및 m은 명세서에 정의한 바와 같다.

4. 发明公开

KR1020030035592A 멜라노코틴 수용체의 항진제 无效
标题翻译： MELANOCORTIN 4 RECEPTOR（MC4R）AGONIST
公开(公告)号：KR1020030035592A
公开(公告)日：2003-05-09
申请号：KR1020010067706
申请日：2001-10-31
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박희술 , 정원혁 , 안인애 , 유현주 , 임현주 , 박숙경 , 최덕영
IPC分类号： C07D417/14
摘要： 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).
摘要翻译：目的：提供黑皮质素4受体（MC4R）激动剂，以加速黑皮质素4受体（MC4R）的功能，并预防和治疗与MC4R相关的疾病，如肥胖症，糖尿病和性障碍。构成：作为黑皮质素4受体（MC4R）激动剂起作用的化合物由式（1）表示，其中A为氢，COR1，CO2R1，SO2R1，SO2NHR1，SO2N（R1）2，PO（OR1）2，烷基，（CH 2）n - ，（CH 2）n - 芳基或（CH 2）n - 杂芳基，其中R 1是氢，C 1-8 - 烷基，（CH 2）n -C 3 -7-环烷基，（CH 2）（CH 2）n - 杂芳基，n为1〜7的整数。 B和E独立地是氢，C 1-8烷基，（CH 2）n -C 3 -7-环烷基，（CH 2）n - 芳基，（CH 2）n - 杂芳基，（CH 2）n - 杂环，（CH 2）氨基，（CH2）n-（烷基）氨基，（CH2）n-（二烷基）氨基，（CH2）n-酰胺（CONH2）或（CH2）nO（CH2）芳基，其中n为0至7的整数 ; C（CH 2）m - 杂芳基，（CH 2）m - 杂环，（CH 2）m -NH-杂芳基，（CH 2）m -NH-杂环，（CH 2）m -NH-（烷基磺酰基）（CH2）m-NH-烷氧基羰基，（CH2）m-NH-烷基氨基氨基甲酰基，（CH2）m-NH-C（O） - 杂芳基，（CH2）m-NH-C（O） - 杂环，（CH 2）m -NH-（CH 2）m - 杂芳基，（CH 2）m -NH-（CH 2）m - 杂环，（CH 2）m -NH-C（O） - （CH 2）（CH 2）m -NH-C（O） - （CH 2）m - 杂环，C（O） - 杂环，（CH 2）m -NH-烷基酯，（CH 2）m -NH-烷基酰胺，烷氧基羰基，（CH 2） mO-（烷基磺酰基），（CH 2）m O-（芳基磺酰基），烷基氨基氨基甲酰基，羟烷基氨基氨基甲酰基，芳基氨基氨基甲酰基或氢，其被选自卤素，C 1-5烷基，三氟甲基，羟基，C 1-3烷氧基，氨基，（C 1-3烷基）氨基，（C 1-3烷基）2氨基，氰基，羧基（CO 2 H），CO 2 -C 1-3烷基，CONH 2，脒（C（NH）NH 2）和氧代（C = O），其中m为0-2的整数; D是哌啶，吡咯烷，六亚甲基亚胺，2或3个氧代哌啶和六亚甲基亚胺，吡咯烷或二烷基胺; 并且Cy是被选自C 1 -C 5 - 烷基，卤素，三氟甲基，羟基，C 1 -C 3 - 烷氧基，氨基，（C 1 -C 3 - 烷氧基） C3-烷基）氨基，二（C1-C3-烷基）氨基和氧代（C = O）。

5. 发明公开

KR1020030035586A 멜라노코틴 수용체의 항진제 无效
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020030035586A
公开(公告)日：2003-05-09
申请号：KR1020010067699
申请日：2001-10-31
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박희술 , 정원혁 , 안인애 , 유현주 , 임현주 , 박숙경 , 권오환 , 심동섭
IPC分类号： C07D403/12
摘要： PURPOSE: Provided is a composition of melanocortin receptor(MRC) agonists, containing, as an active ingredient, a compound of formula(1), its pharmaceutically acceptable salt, a hydrate, a solvate and an isomer. CONSTITUTION: The composition of melanocortin receptor(MRC) agonists comprises a compound of the formula(1) having excellent antagonistic action on melanocortin receptor. In the formula(1), Y is as defined in the specification; X is H2, O or S; B is hydrogen, substituted or unsubstituted C1-C8 alkyl, (CH2)n-C3-C8 cyclo alkyl, (CH2)n-C3-C10 aryl, (CH2)n-C3-C10-hetero aryl, (CH2)n-C3-C10-hetero cyclo alkyl or (CH2)n-O(CH2)-C3-C10-aryl, wherein n is an integer of from 1 to 7; C is substituted or unsubstituted C1-C8 alkyl, (CH2)m-C3-C8 cyclo alkyl, (CH2)m-C3-C10 aryl, (CH2)m-C3-C10-hetero aryl, (CH2)m-C3-C10-hetero cyclo alkyl, wherein m is an integer of from 0 to 2; and D is (CH2)m-R2, wherein m is an integer of from 0 to 3.
摘要翻译：目的：提供含有作为活性成分的式（1）化合物，其药学上可接受的盐，水合物，溶剂合物和异构体的黑皮质素受体（MRC）激动剂的组合物。构成：黑皮质素受体（MRC）激动剂的组成包含对黑皮质素受体具有优异拮抗作用的式（1）化合物。在式（1）中，Y如说明书中所定义; X为H 2，O或S; B是氢，取代或未取代的C 1 -C 8烷基，（CH 2）n -C 3 -C 8环烷基，（CH 2）n -C 3 -C 10芳基，（CH 2）n -C 3 -C 10杂芳基，（CH 2） C 3 -C 10杂环烷基或（CH 2）n O（CH 2）-C 3 -C 10 - 芳基，其中n为1至7的整数; C是取代或未取代的C 1 -C 8烷基，（CH 2）m -C 3 -C 8环烷基，（CH 2）m -C 3 -C 10芳基，（CH 2）m -C 3 -C 10杂芳基，（CH 2）m -C 3- C 10 - 杂环烷基，其中m为0〜2的整数; D为（CH 2）m -R 2，m为0〜3的整数。

6. 发明公开

KR1020030027439A 멜라노코틴 수용체의 항진제 无效
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020030027439A
公开(公告)日：2003-04-07
申请号：KR1020010060726
申请日：2001-09-28
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박희술 , 정원혁 , 안인애 , 유현주 , 최덕영 , 권오환 , 심동섭 , 임현주 , 박숙경
IPC分类号： C07D417/14
摘要： PURPOSE: Provided are a compound of the formula(1) having excellent antibiotic activity, and a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof. Also, provided is a composition of melanocortin receptor agonists which contains them as active ingredients. CONSTITUTION: The compound represented by the formula(1) as defined in the specification is manufactured by the steps of: reaction of B-amino acid compound of the formula(2) with a compound of the formula(3) and followed by hydrolysis to give dipeptide compound of the formula(4); amide-coupling reaction of the compound of the formula(4) and a piperidine derivative of the formula(5), then followed by deprotection to give a compound of the formula(6); and coupling reaction of the compound of the formula(6) to introduce A group thereinto.
摘要翻译：目的：提供具有优异抗生素活性的式（1）化合物及其药学上可接受的盐，水合物，溶剂合物或异构体。此外，提供含有它们作为活性成分的黑皮质素受体激动剂的组合物。构成：本说明书中定义的由式（1）表示的化合物通过以下步骤制备：将式（2）的B-氨基酸化合物与式（3）的化合物反应，然后水解至得到式（4）的二肽化合物; 式（4）化合物与式（5）的哌啶衍生物的酰胺偶联反应，然后脱保护，得到式（6）化合物; 和式（6）化合物的偶联反应以引入A基团。

7. 发明公开

KR1020030035588A 멜라노코틴 수용체의 항진제 无效
标题翻译： MELANOCORTIN 4 RECEIPTOR（MC4R）AGONIST
公开(公告)号：KR1020030035588A
公开(公告)日：2003-05-09
申请号：KR1020010067701
申请日：2001-10-31
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박희술 , 정원혁 , 안인애 , 유현주 , 최덕영 , 권오환
IPC分类号： C07D403/14
摘要： PURPOSE: A melanocortin 4 receptor(MC4R) agonist is provided, thereby accelerating the function of the melanocortin 4 receiptor(MC4R), and consequently preventing and treating diseases associated with the MC4R such as obesity, penile erection disorder, diabetes and inflammation. 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-C8-alkyl, (CH2)n-C5-C10-aryl or (CH2)n-C5-C10-heteroaryl in which R1 is hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C10-aryl or (CH2)n-C5-C10-heteroaryl, n is an integer of 0 to 7; B and C are independently hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C10-aryl, (CH2)n-C5-C10-heteroaryl, (CH2)n-C5-C10-heterocycle or (CH2)n-O(CH2)-C5-C10-aryl in which n is an integer of 1 to 7; D is hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C10-aryl, (CH2)n-C5-C10-heteroaryl, (CH2)n-C5-C10-heterocycle or (CH2)n-O(CH2)-C5-C10-aryl in which n is an integer of 1 to 7; E is C5-C10-alkyl or (CH2)m-C5-C7-cycloalkyl in which m is an integer of 0 to 2; and F is (CH2)m-C5-C10-heteroaryl or (CH2)m-C5-C10-heterocycle in which n is an integer of 0 to 2.
摘要翻译：目的：提供黑皮质素4受体（MC4R）激动剂，从而加速黑皮质素4受体（MC4R）的功能，从而预防和治疗与MC4R相关的疾病，如肥胖，阴茎勃起障碍，糖尿病和炎症。构成：作为黑皮质素4受体（MC4R）激动剂起作用的化合物由式（1）表示，其中A为氢，COR1，CO2R1，SO2R1，SO2NHR1，SO2N（R1）2，PO（OR1）2，C1-C8- 烷基，（CH2）n-C5-C10-芳基或（CH2）n-C5-C10-杂芳基，其中R1是氢，C1-C8-烷基，（CH2）n-C3-C7-环烷基，（CH2）n -C 5 -C 10 - 芳基或（CH 2）n -C 5 -C 10 - 杂芳基，n为0〜7的整数。 B和C独立地是氢，C1-C8-烷基，（CH2）n-C3-C7-环烷基，（CH2）n-C5-C10-芳基，（CH2）n-C5-C10-杂芳基，（CH2）n -C 5 -C 10 - 杂环或（CH 2）n O（CH 2）-C 5 -C 10 - 芳基，其中n为1至7的整数; D是氢，C 1 -C 8 - 烷基，（CH 2）n -C 3 -C 7 - 环烷基，（CH 2）n -C 5 -C 10 - 芳基，（CH 2）n -C 5 -C 10杂芳基，（CH 2）n -C 5 - C10-杂环或（CH2）nO（CH2）-C5-C10-芳基，其中n为1至7的整数; E为C 5 -C 10 - 烷基或（CH 2）m -C 5 -C 7 - 环烷基，其中m为0〜2的整数; 并且F是（CH 2）m -C 5 -C 10 - 杂芳基或（CH 2）m -C 5 -C 10 - 杂环，其中n是0至2的整数。

8. 发明公开

KR1020030035589A 멜라노코틴 수용체의 항진제 无效
标题翻译： MELANOCORTIN 4 RECEPTOR（MC4R）AGONIST
公开(公告)号：KR1020030035589A
公开(公告)日：2003-05-09
申请号：KR1020010067702
申请日：2001-10-31
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박희술 , 정원혁 , 안인애 , 유현주 , 최덕영 , 심동섭
IPC分类号： C07D417/14
摘要： PURPOSE: Provided are a melanocortin 4 receptor(MC4R) agonist and a composition for containing the same, to accelerate the function of the melanocortin 4 receiptor(MC4R), so as to prevent and treat diseases associated with the MC4R such as obesity, penile erection disorder, diabetes and inflammation. 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-C8-alkyl, (CH2)n-C5-C7-aryl, or (CH2)n-C5-C7-heteroaryl in which R1 is hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C7-aryl or (CH2)n-C5-C7-heteroaryl and n is an integer of 1 to 7; B and E are independently hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C7-aryl, (CH2)n-C5-C7-heteroaryl, (CH2)n-C5-C7-heterocycle or (CH2)n-O(CH2)-C5-C7-aryl in which n is an integer of 1 to 7; Cy is C5-C7-aryl or C5-C7-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, oxo(C=O) and nitro; C is hydrogen, COR1, CO2R1, SO2R1, SO2NHR1, (CH2)m-C1-C8-alkylsulfonyl, (CH2)m-C1-C8-alkoxycarbonyl, amide(CONH2), (CH2)m-C1-C8-alkylcarbamoyl, C(O)-C5-C7-heteroaryl, (CO)-C5-C7-heterocycle, C(O)-(CH2)m-C5-C7-heteroaryl, C(O)-(CH2)m-C5-C7-heterocycle, (CH2)m-C5-C7-heteroaryl or (CH2)m-C5-C7-heterocycle in which R1 is C1-C8-alkyl or C5-C7-aryl and m is an integer of 0 to 2; and D is C5-C10-alkyl, (CH2)m-C5-C7-cycloalkyl, (CH2)m-C5-C7-aryl, (CH2)m-C5-C7-heterocycloalkyl I which m is an integer of 0 to 2.
摘要翻译：目的：提供黑皮质素4受体（MC4R）激动剂和含有它的组合物，以加速黑皮质素4受体（MC4R）的功能，以预防和治疗与MC4R相关的疾病，如肥胖，阴茎勃起疾病，糖尿病和炎症。构成：作为黑皮质素4受体（MC4R）激动剂起作用的化合物由式（1）表示，其中A为氢，COR1，CO2R1，SO2R1，SO2NHR1，SO2N（R1）2，PO（OR1）2，C1-C8- 烷基，（CH2）n-C5-C7-芳基或（CH2）n-C5-C7-杂芳基，其中R1是氢，C1-C8-烷基，（CH2）n-C3-C7-环烷基，（CH2） n-C 5 -C 7 - 芳基或（CH 2）n -C 5 -C 7 - 杂芳基，n为1至7的整数; B和E独立地是氢，C 1 -C 8 - 烷基，（CH 2）n -C 3 -C 7 - 环烷基，（CH 2）n -C 5 -C 7 - 芳基，（CH 2）n -C 5 -C 7 - 杂芳基，（CH 2）n C 5 -C 7 - 杂环或（CH 2）n O（CH 2）-C 5 -C 7 - 芳基，其中n为1至7的整数; Cy是C 1 -C 5 - 烷基，卤素，三氟甲基，羟基，C 1 -C 3 - 烷氧基，氨基，（C 1 -C 6 - C3-烷基）氨基，二（C1-C3-烷基）氨基，氧代（C = O）和硝基; （CH2）m-C1-C8-烷基磺酰基，（CH2）m-C1-C8-烷氧基羰基，酰胺（CONH2），（CH2）m-C1-C8-烷基氨基甲酰基， C（O）-C 5 -C 7 - 杂芳基，（CO）-C 5 -C 7 - 杂环，C（O） - （CH 2）m -C 5 -C 7 - 杂芳基，C（O） - （CH 2）m -C 5 -C - 杂环，（CH 2）m -C 5 -C 7 - 杂芳基或（CH 2）m -C 5 -C 7 - 杂环，其中R 1是C 1 -C 8 - 烷基或C 5 -C 7 - 芳基，m是0-2的整数; D为C 5 -C 10 - 烷基，（CH 2）m -C 5 -C 7 - 环烷基，（CH 2）m -C 5 -C 7 - 芳基，（CH 2）m -C 5 -C 7 - 杂环烷基，m为0〜 2。

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