金屬​酶​抑制劑​化合物

源语言标题
(TWI561515) 金屬​酶​抑制劑​化合物
公开号/公开日
TW201339147 A 2013-10-01 [TW201339147]TWI561515 B 2016-12-11 [TWI561515] / 2013-10-012016-12-11
申请号/申请日
2012TW-0124178 / 2012-07-05
发明人
HOEKSTRA WILLIAM;YATES CHRISTOPHER;SCHOTZINGER ROBERT J;LOSO MICHAEL R;BUCHAN ZACHARY A;SULLENBERGER MICHAEL T;
申请人
VIAMET PHARMACEUTICALS;
主分类号
IPC分类号
A01N-043/647A01N-043/653A01N-043/713A01N-043/78A01P-003/00A61K-031/4439A61K-031/444A61K-031/506A61P-031/10C07D-401/06C07D-401/14C07D-409/14C07D-417/14
摘要
(TWI561515) 本​發明​說明​一種​具有​金屬​酶​調控​活性​之​化合物,及​一種​處理​由​此等​金屬​酶​介​導​之​疾病、病變​或​症狀​之​方法。
地址
代理人
代理机构
;
优先权号
2012US-61611897 2012-03-16 2012WO-US43140 2012-06-19
主权利要求
(TW201339147) 1. Kinds of type I chemical compound or its salt: MBG is to regard to need, to regard to need after the triazolyl of substitution, to regard after the tetrazolyl of substitution to need after the substitution [chart] azole base, regards to need after the pyrimidyl of substitution, to regard to need after the thiazolyl of substitution, or regards to need to pass through the pyrazolyl of substitution; R 1 is H and halogen base, alkyl group or halogen alkyl group; R 2 is H and halogen base, alkyl group or halogen alkyl group; R 3 independent are H, alkyl group, nitro group, cyano, the halogen alkyl group, alkoxyl, the halogen base, the halogen alkoxyl, the olefin base and halogen olefin base, naphthenic base, the halogen naphthenic base, the alkyne base and halogen alkyne base, the sulfur alkyl group and SF 3, SF 6, SCN and SO 2 R 6, -c(o)- alkyl group, -c(o)oh, -c(o)o- alkyl group, C(O)H and CH=N-O- alkyl group, -ch=n-o- aryl residue alkyl group; R 4 are the aryl residue, the mixed aryl residue or the naphthenic base, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence; R 5 are the alkyl group, halogen alkyl group, naphthenic base and C 2 - C 8 olefin bases and C 2 - C 8 alkyne base, aryl residue, mixed aryl residue and aryl residue alkyl groups, either the mixed aryl residue alkyl group, regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence respectively; R 6 are the alkyl group, aryl residue, after substitution aryl residue, the mixed aryl residue or after the substitution the mixed aryl residue; R 7 are H and alkyl group, -si (R 8) 3, -p(o)(oh) 2, -ch 2 - O-P(O)(OH) 2, or regards to need after the amidogen to substitute for it alkyl group; R 8 independent are the alkyl group or the aryl residue; R 9 independent are H, alkyl group and halogen base, or the halogen alkyl group; And X is O or S. 2. According to claim 1, item of institute stated the chemical compound or its salt, R 1 was the fluorine. 3. According to claim 1, item of institute stated the chemical compound or its salt, R 2 was the fluorine. 4. According to claim 1, item of institute stated the chemical compound or its salt, R 1 and R 2 was the fluorine. 5. According to claim 1, item of institute stated the chemical compound or its salt, R 4 were the benzyl, it regarded to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 6. According to claim 1, item of institute stated the chemical compound or its salt, R 4 were the benzyl, it regarded to need to pass through 0, 1, 2 or halogen of base substitutions 3 independence. 7. According to claim 1, item of institute stated the chemical compound or its salt, R 4 were the benzyl, it regarded to need to pass through 0, 1, 2 or fluorine of substitutions 3 independence. 8. According to claim 1, item of institute stated the chemical compound or its salt, R 4 were 2,4- two fluorine benzyl. 9. According to claim 1, item of institute stated the chemical compound or its salt, R 5 were the aryl residue, it regarded to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 10. According to claim 1, item of institute stated the chemical compound or its salt, R 5 were the aryl residue alkyl groups, it regarded to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 11. According to claim 1, item of institute stated the chemical compound or its salt, R 5 were the mixed aryl residue alkyl groups, it regarded to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 12. According to claim 1, item of institute stated the chemical compound or its salt, R 5 were the mixed aryl residue, it regarded to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 13. According to claim 1, item of institute stated the chemical compound or its salt: R 1 is the fluorine; R 2 is the fluorine; R 4 are 2,4- two fluorine benzyl; With R 5 are the aryl residue, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 14. According to claim 1, item of institute stated the chemical compound or its salt: R 1 is the fluorine; R 2 is the fluorine; R 4 are 2,4- two fluorine benzyl; With R 5 are the mixed aryl residue, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 15. According to claim 1, item of institute stated the chemical compound or its salt: R 1 is the fluorine; R 2 is the fluorine; R 4 are 2,4- two fluorine benzyl; With R 5 are the aryl residue alkyl groups, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 16. According to claim 15, item of institute stated the chemical compound or its salt: R 5 are the benzyls, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 17. According to claim 15, item of institute stated the chemical compound or its salt: R 5 are 2 - mixed aryl residue, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 18. According to claim 15, item of institute stated the chemical compound or its salt: R 5 are 2 - CF 2 - aryl residue, it regards to need to pass through 0, 1, 2 or R of 3 substitutions 3 independence. 19. According to claim 1, item of institute stated the chemical compound or its salt, it was below one: 1- (5- (4- chlorine - 2- fluorobenzene methoxyl groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (1); 1- (5- (2,4- two fluorobenzene methoxyl groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (2); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (3- fluorobenzene methoxyl groups) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (3); 1- (5- (4- chlorobenzene methoxyl groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (4); 4- (6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- base oxygen radicals) benzonitrile nitrile (5); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (4- fluorobenzene oxygen radicals) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (6); 1- (5- (4- chlorobenzene oxygen radicals) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (7); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- methoxyl group pyridines - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (8); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) benzonitrile nitrile (9); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 2- fluorine benzonitrile nitrile (10); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- phenoxy pyridines - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (11); Or 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- (2,2,2- three fluorine ethoxy groups) pyridine - 2- bases) C - 2- mellow (12); 1- (4- ((2,4- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (13); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- (ethenyl oxygen radical) pyridine - 2- bases) C - 2- mellow (14); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) sulfenyl) methyl) - 3- fluorine benzonitrile nitrile (15); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) sulfenyl) methyl) - 3- fluorine benzonitrile nitrile (16); 4- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) - 2- fluorine benzonitrile nitrile (17); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((2,2,2- three fluorine ethyl groups) sulfenyl) pyridine - 2- bases) C - 2- mellow (18); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- ((4- fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (19); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((4- (2,2,2- three fluorine ethoxy groups) benzyl) oxygen radical) pyridine - 2- bases) C - 2- mellow (20); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((4- (three fluorine methoxyl groups) benzyl) oxygen radical) pyridine - 2- bases) C - 2- mellow (21); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((4- (three fluorine methyl) benzyl) oxygen radical) pyridine - 2- bases) C - 2- mellow (22); 1- (5- ((2,3- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (23); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- ((2- fluorine - 4- (three fluorine methyl) benzyl) oxygen radical) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (24); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((3- (2,2,2- three fluorine ethoxy groups) benzyl) oxygen radical) pyridine - 2- bases) C - 2- mellow (25); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((3- (three fluorine methyl) benzyl) oxygen radical) pyridine - 2- bases) C - 2- mellow (26); 1- (5- ((4- chlorine - 3- fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (27); 1- (5- ((3,4- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (28); 2- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) acetonitrile (29); 1- (5- (benzyl oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (30); 1- (5- (benzyl oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (31); 1- (5- (Ding - 2- alkyne - 1- base oxygen radicals) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (32); 1- (5- (Ding - 2- alkyne - 1- base oxygen radicals) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (33); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- ((3- methoxyl group benzyls) oxygen radical) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (34); 1- (5- ((3,5- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (35); 1- (5- ((3,5- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (36); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (pyridine - 2- base methoxyl groups) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (37); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (pyridine - 2- base methoxyl groups) pyridine - 2- bases) - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (38); 1- (5- (cyclopropyl methoxyl group) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (39); 1- (5- (cyclopropyl methoxyl group) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (40); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- ((4- methoxyl group benzyls) oxygen radical) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (41); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- isopropoxy pyridines - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (42); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- isobutoxy pyridines - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (43); 1- (5- ((2,3- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H -1,2,3- triazoles - 1- bases) C - 2- mellow (44); 1- (5- ((2,3- two fluorobenzene methyl) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H -1,2,4- triazoles - 1- bases) C - 2- mellow (45) 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- ((2- fluorobenzene methyl) oxygen radical)  pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (46); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- ((1,1,1- three fluorine C - 2- bases) oxygen radical) pyridine - 2- bases) C - 2- mellow (47); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) - 1- (5- ((1,1,1- three fluorine C - 2- bases) oxygen radical) pyridine - 2- bases) C - 2- mellow (48); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- (thiophen - 2- base methoxyl groups) pyridine - 2- bases) C - 2- mellow (49); 6- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) nicotine A nitrile (50); 6- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) nicotine A nitrile (51); 3- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) benzonitrile nitrile (52); 3- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) benzonitrile nitrile (53); 2- (4- chlorine - 2- fluorine benzyl) - 1- (5- (cyclopropyl methoxyl group) pyridine - 2- bases) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (54); 4- (((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) benzonitrile nitrile (55); 4- (((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) benzonitrile nitrile (56); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 3- fluorine benzonitrile nitrile (57); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 3- fluorine benzonitrile nitrile (58); 3- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 4- fluorine benzonitrile nitrile (59); 2- (2,4- two fluorine benzyl) - 1- (5- ((3,5- two fluorine pyridines - 2- bases) methoxyl group) pyridine - 2- bases) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (60); 6- (((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) nicotine A nitrile (61); 6- (((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) nicotine A nitrile (62); 1- (5- (Ding - 2- alkyne - 1- base oxygen radicals) pyridine - 2- bases) - 2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (63); 1- (5- (Ding - 2- alkyne - 1- base oxygen radicals) pyridine - 2- bases) - 2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (64); 5- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 2- fluorine benzonitrile nitrile (65); 5- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 2- fluorine benzonitrile nitrile (66); 3- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 2- fluorine benzonitrile nitrile (67); 3- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) - 2- fluorine benzonitrile nitrile (68); 2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 1- (5- isobutoxy pyridines - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (69); 2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 1- (5- isobutoxy pyridines - 2- bases) - 3- (2 H - tetrazolo - 2- bases) C - 2- mellow (70); 2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- (2,2,2- three fluorine ethoxy groups) pyridine - 2- bases) C - 2- mellow (71); 2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 3- (2 H - tetrazolo - 2- bases) - 1- (5- (2,2,2- three fluorine ethoxy groups) pyridine - 2- bases) C - 2- mellow (72); 5- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) thiophen - 2- A nitrile (73); 5- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) thiophen - 2- A nitrile (74); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- (4- (three fluorine methyl) phenoxy) pyridine - 2- bases) C - 2- mellow (75); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) - 1- (5- (4- (three fluorine methoxyl groups) phenoxy) pyridine - 2- bases) C - 2- mellow (76); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (3- fluorobenzene oxygen radicals) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (77); 3- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) benzonitrile nitrile (78); 4- ((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) benzonitrile nitrile (79); 4- ((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) benzonitrile nitrile (80); 4- ((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) - 2- fluorine benzonitrile nitrile (81); 4- ((6- (2- (4- chlorine - 2- fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) - 2- fluorine benzonitrile nitrile (82); 4- (((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen radical) methyl) benzonitrile nitrile (83); 1- (5- (3- chlorobenzene oxygen radicals) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (84); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (3- methoxyl group phenoxies) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (85); 1- (5- (3,4- two fluorobenzene oxygen radicals) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (86); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (4- methoxyl group phenoxies) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (87); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (2- fluorobenzene oxygen radicals) pyridine - 2- bases) - 3- (1 H - tetrazolo - 1- bases) C - 2- mellow (88); 4- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) - 3- fluorine benzonitrile nitrile (89); 4- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (2 H - tetrazolo - 2- bases) propyl) pyridine - 3- bases) oxygen  radical) - 3- fluorine benzonitrile nitrile (90); 2- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1 H - tetrazolo - 1- bases) propyl) pyridine - 3- bases) sulfenyl) methyl acetate (91); 1- (5- ((3- chlorine - 5- (three fluorine methyl) pyridine - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (92); 6- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) nicotine A nitrile (93); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) - 1- (5- ((5- (three fluorine methyl) pyridine - 2- bases) oxygen radical) pyridine - 2- bases) C - 2- mellow (94); 1- (5- ((5- chloropyridine - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (95); 4- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) - 2- cyano pyridines (96); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (metadiazine - 2- base oxygen radicals) pyridine - 2- bases) - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (97); 1- (5- ((5- chlorine metadiazines - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (98); 1- (5- ((5- bromine metadiazines - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (99); 5- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) metadiazine - 2- A nitrile (100); 6- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) nicotine aldehyde (101); (E) - 6- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) nicotine aldehyde O- methyl oxime (102); (E) - 6- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) nicotine aldehyde O- benzyl oxime (103); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- ((3- fluorine - 5- (three fluorine methyl) pyridine - 2- bases) oxygen radical) pyridine - 2- bases) - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (104); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) - 1- (5- ((5- (three fluorine methyl) metadiazine - 2- bases) oxygen radical) pyridine - 2- bases) C - 2- mellow (105); 1- (5- ((5- bromopyridines - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (106); 2- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) thiazole - 5- A nitrile (107); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (quinoline - 2- base oxygen radicals) pyridine - 2- bases) - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (108); 1- (5- ((5- chlorobenzene and [d] thiazoles - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (109); 1- (5- ((6- chlorobenzene and [d] thiazoles - 2- bases) oxygen radical) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (110); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) - 1- (5- ((6- (three fluorine methyl) pyridine - 3- bases) oxygen radical) pyridine - 2- bases) C - 2- mellow (111); 5- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) - 2- cyano pyridines (112); 1- (5- ((5- chloropyridine - 2- bases) methoxyl group) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (113); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) - 1- (5- ((5- (three fluorine methyl) pyridine - 2- bases) methoxyl group) pyridine - 2- bases) C - 2- mellow (114); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) - 1- (5- ((6- (three fluorine methyl) pyridine - 3- bases) methoxyl group) pyridine - 2- bases) C - 2- mellow (115); 1- (5- ((6- chloropyridine - 3- bases) methoxyl group) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (116); 1- (5- ((2- chloropyridine - 4- bases) methoxyl group) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (117); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (pyridine - 4- base methoxyl groups) pyridine - 2- bases) - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (118); 1- (5- (2,2- two fluorine - 2- benzyl ethoxy groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (119); 1- (5- (2- (4- (two fluorine methoxyl groups) benzyl) - 2,2- two fluorine ethoxy groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (120); 1- (5- (2- (4- chlorine benzyl) - 2,2- two fluorine ethoxy groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (121); 4- (2- ((6- (2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 2- hydroxyl - 3- (1H- tetrazolo - 1- bases) propyl) pyridine - 3- bases) oxygen radical) - 1,1- two fluorine ethyl groups) benzonitrile nitrile (122); 1- (5- (2- (4- (two fluorine methoxyl groups) benzyl) - 2- fluorine ethoxy groups) pyridine - 2- bases) - 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (123); 2- (2,4- two fluorine benzyl) - 1,1- two fluorine - 1- (5- (2- fluorine - 2- benzyl ethoxy groups) pyridine - 2- bases) - 3- (1H- tetrazolo - 1- bases) C - 2- mellow (124). 20. Like the application patent scope the 1st to 19 items of any item of institute stated the chemical compound or its salt, this chemical compound because of formed following one with the metal kind of either many kinds of chemistry correlation or the key knot, but achieved with the endophilicity of metalloenzyme: Sigma key, covalent bond, coordinate covalent bond and ionic bond, Pi key, Delta key or feedback linkage correlation. 21. Like the application patent scope the 1st to 19 items of any item of institute stated the chemical compound or its salt, this chemical compound union to metal. 22. Like the application patent scope the 1st to 19 items of any item of institute stated the chemical compound or its salt, this chemical compound union to iron, zinc and blood matrix iron, manganese, magnesium and iron sulfide variety collection, nickel, molybdenum or copper. 23. Like the application patent scope the 1st to 19 items of any item of institute stated the chemical compound or its salt, this chemical compound suppressed to elect from the following enzyme class: The cytochrome P450 family and histone escape the acetyl enzyme and matrix metal proteinase, the orthophosphoric acid diesterase, the epoxy synthase, carbonic anhydrase and nitrogen oxide synzyme. 24. Like the application patent scope the 1st to 19 items of any item of institute stated the chemical compound or its salt, this chemical compound suppressed to elect from the following enzyme: 4- the hydroxyl benzyl pyroracemic acid double oxygenases, 5- fat oxygenases and adenosines escape the amine enzyme, acetaldehyde reductase and amidogen peptidase N and vasoconstriction element saccharase and fragrant enzyme (CYP19), calcium accent phosphatase and amine formyl phosphate synzyme, the carbonic anhydrase family and catecha Phenol-o- methyl transferase and epoxy synthase family and dihydro metadiazine Dehydrogenase-one, DNA polymerase and France the base two phosphat(...)
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(TWI561515) LEGAL DETAILS FOR TW201339147  Actual or expected expiration date=2032-06-19    Legal state=ALIVE    Status=GRANTED     Event publication date=2012-07-05  Event code=TW/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=TW TW101124178  Application date=2012-07-05  Standardized application number=2012TW-0124178     Event publication date=2013-10-01  Event code=TW/A  Event indicator=Pos  Event type=Examination events  Laid open application for patent or patent of addition  Publication country=TW  Publication number=TW201339147  Publication stage Code=A  Publication date=2013-10-01  Standardized publication number=TW201339147     Event publication date=2016-12-11  Event code=TW/B  Event indicator=Pos  Event type=Event indicating In Force  Granted patent or patent of addition  Publication country=TW  Publication number=TWI561515  Publication stage Code=B  Publication date=2016-12-11  Standardized publication number=TWI561515
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