SUBSTITUTED 2-MERCAPTO-3-AMINOPYRIDINES AS KCNQ2/3 MODULATORSThe invention relates to substituted 2-mercapto-3-aminopyridines, methods for the production thereof, medicaments containing said compounds, and the use of said compounds for producing medicaments.The substituted 2-sulfydryl-3-aminopyridines that has general formula (1),, whereinr 1represent c 1-6alkyl, it is saturated or undersaturated, side chain or non-side chain, unsubstituted or coverlet-or multiple substituted; c 3-10naphthenic base or heterocyclic radical, it respectively does for oneself saturated or undersaturated, unsubstituted or coverlet-or multiple substituted; aryl or heteroaryl, it respectively does for oneself unsubstituted or coverlet-or multiple substituted; condition is to work as r 1when representing heterocyclic radical, said heterocyclic radical links to each other with high-grade formula more through assorted intra-annular carbon atom; r 2represent aryl or heteroaryl, it is respectively unsubstituted or coverlet-or multiple substituted; y is selected from you – (cr 9ar 9b)-, s (=o) 2, s (=o) ,-s-,-o-, the c (=group that o) constitutes; r 3, r 4, r 5, r 6a, r 6b, r 7a, r 7b, r 8a,r 8b, r 9aand r 9brepresent h separately independently of each other; f; cl; br; i; no 2cf 3cn; oh; ocf 3sh; scf 3nh 2c 1-6alkyl, o-c 1-6alkyl, o-c (=o)-c 1-6alkyl, s-c 1-6alkyl, nh (c 1-6alkyl), n (c 1-6alkyl) 2, nh-c (=o)-c 1-6alkyl, n (c (=o)-c 1-6alkyl) 2or c (=o)-c 1-6alkyl, it is respectively saturated or undersaturated, side chain or non-side chain, unsubstituted or coverlet-or multiple substituted; c 3-7naphthenic base or heterocyclic radical, it is respectively saturated or undersaturated, side chain or non-side chain, unsubstituted or coverlet-or multiple substituted; r wherein 7acan with r 8aform c together 3-7group of naphthene base, it can be saturated or undersaturated, unsubstituted or coverlet-or multiple substituted; wherein ' substituted alkyl ' is meant that one or more wasserstoffatomss are separately independently of each other by f; cl; br; i; no 2cf 3cn; c 1-8alkyl; c 2-8assorted alkyl; aryl; heteroaryl; c 3-10naphthenic base; heterocyclic radical; through c 1-8alkyl-or c 2-8aryl, heteroaryl, the c of assorted alkyl bridge joint 3-10naphthenic base or heterocyclic radical; cho; c (=o) c 1-8alkyl; c (=o) aryl; c (=o) heteroaryl; co 2h; c (=o) o-c 1-8alkyl; c (=o) o-aryl; c (=o) o-heteroaryl; conh 2c (=o) nh-c 1-8alkyl; c (=o) n (c 1-8alkyl) 2c (=o) nh-aryl; c (=o) n (aryl) 2c (=o) nh-heteroaryl; c (=o) n (heteroaryl) 2c (=o) n (c 1-8alkyl) (aryl); c (=o) n (c 1-8alkyl) (heteroaryl); c (=o) n (heteroaryl) (aryl); oh; o-c 1-8alkyl; ocf 3o-(c 1-8alkyl)-oh; o-(c 1-8alkyl)-o-c 1-8alkyl; the o-benzyl; the o-aryl; the o-heteroaryl; o-c (=o) c 1-8alkyl; o-c (=o) aryl; o-c (=o) heteroaryl; nh 2nh-c 1-8alkyl; n (c 1-8alkyl) 2nh-c (=o) c 1-8alkyl; n (c 1-8alkyl)-c (=o) c 1-8alkyl; n (c (=o) c 1-8alkyl) 2nh-c (=o)-aryl; nh-c (=o)-heteroaryl; sh; s-c 1-8alkyl; scf 3the s-benzyl; the s-aryl; the s-heteroaryl; s (=o) 2c 1-8alkyl; s (=o) 2aryl; s (=o) 2heteroaryl; s (=o) 2oh; s (=o) 2o-c 1-8alkyl; s (=o) 2the o-aryl; s (=o) 2the o-heteroaryl; s (=o) 2-nh-c 1-8alkyl; s (=o) 2-nh-aryl; and s (=o) 2-nh-c 1-8-heteroaryl replaces; wherein ' substituted heterocyclic radical ' and ' substituted naphthenic base ' is meant that one or more wasserstoffatomss are separately independently of each other by f; cl; br; i; no 2cf 3=o; cn; c 1-8alkyl; c 2-8assorted alkyl; aryl; heteroaryl; c 3-10naphthenic base; heterocyclic radical; through c 1-8alkyl-or c 2-8aryl, heteroaryl, the c of assorted alkyl bridge joint 3-10naphthenic base or heterocyclic radical; cho; c (=o) c 1-8alkyl; c (=o) aryl; c (=o) heteroaryl; co 2h; c (=o) o-c 1-8alkyl; c (=o) o-aryl; c (=o) o-heteroaryl; conh 2c (=o) nh-c 1-8alkyl; c (=o) n (c 1-8alkyl) 2c (=o) nh-aryl; c (=o) n (aryl) 2c (=o) nh-heteroaryl; c (=o) n (heteroaryl) 2c (=o) n (c 1-8alkyl) (aryl); c (=o) n (c 1-8alkyl) (heteroaryl); c (=o) n (heteroaryl) (aryl); oh; o-c 1-8alkyl; ocf 3o-(c 1-8alkyl)-oh; o-(c 1-8alkyl)-o-c 1-8alkyl; the o-benzyl; the o-aryl; the o-heteroaryl; o-c (=o) c 1-8alkyl; o-c (=o) aryl; o-c (=o) heteroaryl; nh 2;nh-c 1-8alkyl; n (c 1-8alkyl) 2nh-c (=o) c 1-8alkyl; n (c 1-8alkyl)-c (=o) c 1-8alkyl; n (c (=o) c 1-8alkyl) 2nh-c (=o)-aryl; nh-c (=o)-heteroaryl; sh; s-c 1-8alkyl; scf 3the s-benzyl; the s-aryl; the s-heteroaryl; s (=o) 2c 1-8alkyl; s (=o) 2aryl; s (=o) 2heteroaryl; s (=o) 2oh; s (=o) 2o-c 1-8alkyl; s (=o) 2the o-aryl; s (=o) 2the o-heteroaryl; s (=o) 2-nh-c 1-8alkyl; s (=o) 2-nh-aryl; and s (=o) 2-nh-c 1-8heteroaryl replaces; wherein ' substituted aryl ' and ' substituted heteroaryl ' is meant that one or more wasserstoffatomss are separately independently of each other by f; cl; br; i; no 2cf 3cn; c 1-8alkyl; or c 2-8assorted alkyl; aryl; heteroaryl; c 3-10naphthenic base; heterocyclic radical; through c 1-8alkyl-or c 2-8aryl, heteroaryl, the c of assorted alkyl bridge joint 3-10naphthenic base or heterocyclic radical; cho; c (=o) c 1-8alkyl; c (=o) aryl; c (=o) heteroaryl; co 2h; c (=o) o-c 1-8alkyl; c (=o) o-aryl; c (=o) o-heteroaryl; conh 2c (=o) nh-ch 3c (=o) nh-c 2h 5c (=o) n (c 1-8alkyl) 2c (=o) nh-aryl; c (=o) n (aryl) 2c (=o) nh-hete...
ＫＣＮＱ２／３ 조절제로서의 치환된 2-머캅토-3-아미노피리딘본 발명은 치환된 2-머캅토-3-아미노피리딘, 이의 제조방법, 상기 화합물을 함유하는 약제 및 약제를 제조하기 위한 상기 화합물의 용도에 관한 것이다.유리 화합물 또는 생리학적으로 상용성(compatibile)인 산 또는 염기의 염 형태의, 화학식 1의 치환된 2-머캅토-3-아미노피리딘.화학식 1[이미지]위의 화학식 1에서, R1은 포화되거나 불포화된 측쇄 또는 직쇄의 치환되지 않거나 일치환 또는 다치환된 C1-6 알킬; 각각 포화되거나 불포화된 치환되지 않거나 일치환 또는 다치환된 C3-10 사이클로알킬 또는 헤테로사이클릴; 각각 치환되지 않거나 일치환 또는 다치환된 아릴 또는 헤테로아릴이고; 단, R1이 헤테로사이클릴인 경우, 상기 고차 구조(higher-order general structure)에 대한 헤테로사이클릴의 결합은 헤테로사이클릴의 탄소원자를 통해 이루어지며;R2는 아릴 또는 헤테로아릴이고, 이들 각각은 치환되지 않거나 일치환 또는 다치환되며; Y는 -(CR9aR9b)-, S(=O)2, S(=O), -S-, -O-, C(=O)로 이루어진 그룹으로부터 선택되고;R3, R4, R5, R6a, R6b, R7a, R7b, R8a, R8b, R9a 및 R9b는 각각 서로 독립적으로 H; F; Cl; Br; I; NO2; CF3; CN; OH; OCF3; SH; SCF3; NH2; 각각 포화되거나 불포화된 측쇄 또는 직쇄의 치환되지 않거나 일치환 또는 다치환된 C1-6 알킬, O-C1-6 알킬, O-C(=O)-C1-6 알킬, S-C1-6 알킬, NH(C1-6 알킬), N(C1-6 알킬)2, NH-C(=O)-C1-6 알킬, N(C(=O)-C1-6 알킬)2 또는 C(=O)-C1-6 알킬; 각각 포화되거나 불포화된 측쇄 또는 직쇄의 치환되지 않거나 일치환 또는 다치환된 C3-7 사이클로알킬 또는 헤테로사이클릴이고;여기서, R7a는 R8a와 함께 C3-7 사이클로알킬 라디칼을 형성할 수 있고, 이것은 포화되거나 불포화되고 치환되지 않거나 일치환 또는 다치환될 수 있으며;여기서, "알킬-치환된"은 하나 이상의 수소원자가 각각 서로 독립적으로 F; Cl; Br; I; NO2; CF3; CN; C1-8 알킬; C2-8 헤테로알킬; 아릴; 헤테로아릴; C3-10 사이클로알킬; 헤테로사이클릴; C1-8 알킬- 또는 C2-8 헤테로알킬-브릿징된 아릴, 헤테로아릴, C3-10 사이클로알킬 또는 헤테로사이클릴; CHO; C(=O)C1-8 알킬; C(=O)아릴; C(=O)헤테로아릴; CO2H; C(=O)O-C1-8 알킬; C(=O)O-아릴; C(=O)O-헤테로아릴; CONH2; C(=O)NH-C1-8 알킬; C(=O)N(C1-8 알킬)2; C(=O)NH-아릴; C(=O)N(아릴)2; C(=O)NH-헤테로아릴; C(=O)N(헤테로아릴)2; C(=O)N(C1-8 알킬)(아릴); C(=O)N(C1-8 알킬)(헤테로아릴); C(=O)N(헤테로아릴)(아릴); OH; O-C1-8 알킬; OCF3; O-(C1-8 알킬)-OH; O-(C1-8 알킬)-O-C1-8 알킬; O-벤질; O-아릴; O-헤테로아릴; O-C(=O)C1-8 알킬; O-C(=O)아릴; O-C(=O)헤테로아릴; NH2; NH-C1-8 알킬; N(C1-8 알킬)2; NH-C(=O)C1-8 알킬; N(C1-8 알킬)-C(=O)C1-8 알킬; N(C(=O)C1-8 알킬)2; NH-C(=O)-아릴; NH-C(=O)-헤테로아릴; SH; S-C1-8 알킬; SCF3; S-벤질; S-아릴; S-헤테로아릴; S(=O)2C1-8 알킬; S(=O)2아릴; S(=O)2헤테로아릴; S(=O)2OH; S(=O)2O-C1-8 알킬; S(=O)2O-아릴; S(=O)2O-헤테로아릴; S(=O)2-NH-C1-8 알킬; S(=O)2-NH-아릴; S(=O)2-NH-C1-8-헤테로아릴로 치환됨을 나타내고;"헤테로사이클릴-치환된" 및 "사이클로알킬-치환된"은 하나 이상의 수소원자가 각각 서로 독립적으로 F; Cl; Br; I; NO2; CF3; =O; CN; C1-8 알킬; C2-8 헤테로알킬; 아릴; 헤테로아릴; C3-10 사이클로알킬; 헤테로사이클릴; C1-8 알킬- 또는 C2-8 헤테로알킬-브릿징된 아릴, 헤테로아릴, C3-10 사이클로알킬 또는 헤테로사이클릴; CHO; C(=O)C1-8 알킬; C(=O)아릴; C(=O)헤테로아릴; CO2H; C(=O)O-C1-8 알킬; C(=O)O-아릴; C(=O)O-헤테로아릴; CONH2; C(=O)NH-C1-8 알킬; C(=O)N(C1-8 알킬)2; C(=O)NH-아릴; C(=O)N(아릴)2; C(=O)NH-헤테로아릴; C(=O)N(헤테로아릴)2; C(=O)N(C1-8 알킬)(아릴); C(=O)N(C1-8 알킬)(헤테로아릴); C(=O)N(헤테로아릴)(아릴); OH; O-C1-8 알킬; OCF3; O-(C1-8 알킬)-OH; O-(C1-8 알킬)-O-C1-8 알킬; O-벤질; O-아릴; O-헤테로아릴; O-C(=O)C1-8 알킬; O-C(=O)아릴; O-C(=O)헤테로아릴; NH2; NH-C1-8 알킬; N(C1-8 알킬)2; NH-C(=O)C1-8 알킬; N(C1-8 알킬)-C(=O)C1-8 알킬; N(C(=O)C1-8 알킬)2; NH-C(=O)-아릴; NH-C(=O)-헤테로아릴; SH; S-C1-8 알킬; SCF3; S-벤질; S-아릴; S-헤테로아릴; S(=O)2C1-8 알킬; S(=O)2 아릴; S(=O)2 헤테로아릴; S(=O)2OH; S(=O)2O-C1-8 알킬; S(=O)2O-아릴; S(=O)2O-헤테로아릴; S(=O)2-NH-C1-8 알킬; S(=O)2-NH-아릴; 및 S(=O)2-NH-C1-8 헤테로아릴로 치환됨을 나타내고;"아릴-치환된" 및 "헤테로아릴-치환된"은 하나 이상의 수소원자가 각각 서로 독립적으로 F; Cl; Br; I; NO2; CF3; CN; C1-8 알킬; 또는 C2-8 헤테로알킬; 아릴; 헤테로아릴; C3-10 사이클로알킬; 헤테로사이클릴; C1-8 알킬- 또는 C2-8 헤테로알킬-브릿징된 아릴, 헤테로아릴, C3-10 사이클로알킬 또는 헤테로사이클릴; CHO; C(=O)C1-8 알킬; C(=O)아릴; C(=O)헤테로아릴; CO2H; C(=O)O-C1-8 알킬; C(=O)O-아릴; C(=O)O-헤테로아릴; CONH2; C(=O)NH-CH3; C(=O)NH-C2H5; C(=O)N(C1-8 알킬)2; C(=O)NH-아릴; C(=O)N(아릴)2; C(=O)NH-헤테로아릴; C(=O)N(헤테로아릴)2; C(=O)N(C1-8 알킬)(아릴); C(=O)N(C1-8 알킬)(헤테로아릴); C(=O)N(헤테로아릴)(아릴); OH; O-C1-8 알킬; OCF3; O-(C1-8 알킬)-OH; O-(C1-8 알킬)-O-C1-8 알킬; O-벤질; O-아릴; O-헤테로아릴; O-C(=O)C1-8 알킬; O-C(=O)아릴; O-C(=O)헤테로아릴; NH2; NH-C1-8 알킬; N(C1-8 알킬)2; NH-C(=O)C1-8 알킬; N(C1-8 알킬)-C(=O)C1-8 알킬; N(C(=O)C1-8 알킬)2; NH-C(=O)-아릴; NH-C(=O)-헤테로아릴; SH; S-C1-8 알킬; SCF3; S-벤질; S-아릴; S-헤테로아릴; S(=O)2C1-8 알킬; S(=O)2아릴; S(=O)2헤테로아릴; S(=O)2OH; S(=O)2O-C1-8 알킬; S(=O)2O-아릴; S(=O)2O-헤테로아릴; S(=O)2-NH-C1-8 알킬; S(=O)2-NH-아릴; S(=O)2-NH-C1-8 헤테로아릴로 치환됨을 나타낸다.