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INHIBITOR OF THE ACID SECRETION.

机译：抑制酸分泌。

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摘要

A compound represented by the formula (I): in which R1 is a heterocyclic monocyclic group containing saturated or unsaturated aromatic or non-aromatic nitrogen containing, as an atom constituting a ring, at least one nitrogen atom and which is optionally condensed with a benzene ring or an aromatic or non-aromatic heterocycle, the heterocyclic monocyclic group containing nitrogen optionally fused with a benzene ring or a heterocycle optionally has 1 to 5 substituents selected from the group consisting of (1) a halogen atom, (2) nitro, (3) cyano, (4) hydroxy, (5) C1-6 alkoxy having optionally 1 to 3 halogen atoms, (6) C6-14 aryloxy, (7) C7- aralkyloxy 16, (8) mercapto, (9) C1-6 alkylthio which optionally has 1 to 3 halogen atoms, (10) C6-14 arylthio, (11) C7-16 aralkylthio, (12) amino, ( 13) C1-6-amino mono-alkyl, (14) C6-14-amino mono-aryl, (15) C7-16-amino mono-aralkyl, (16) C1-6-amino di-alkyl, (17) C6-14-amino di-aryl, (18) C7-16-amino di-aralkyl, (19) formyl, (20) C1-6- alkyl carbonyl, (21) C6-14-carbonyl aryl, (22) carboxyl, (23) C1-6-carbonyl alkoxy, (24) C6-14-carbonyl aryloxy, (25) carbamoyl, (26) thiocarbamoyl, (27) C1-6-carbamoyl mono-alkyl, (28) C1-6-carbamoyl di-alkyl, (29) C6-14-carbamoyl aryl, (30) C1-6-sulfonyl alkyl, (31 ) C6-14-sulfonyl aryl, (32) C1-6-sulfinyl alkyl, (33) C6-14-sulfinyl aryl, (34) formylamino, (35) C1-6-carbonylamino alkyl, (36) C6-14-carbonylamino aryl, (37) C1-6-carbonylamino alkoxy, (38) C1-6-sulfonylamino alkyl, (39) C6-14-sulfonylamino aryl, (40) C1-6 alkyl carbonyloxy, (41) C6-14-carbonyloxy aryl, (42) C1-6-carbonyloxy alkoxy, (43) C1-6-carbamoyloxy mono-alkyl, (44) C1-6-carbamoyloxy di-alkyl, (45) C6-14-carbamoyloxy aryl, (46) a 5- to 7-membered saturated cyclic amino optionally containing, in addition to an atom or of nitrogen and carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, (47) a 5 to 10-membered aromatic heterocyclic group which also contains of carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, (48) C1-3-dioxy alkylene, (49) C3-7 cycloalkyl , (50) C1-6 alkyl group optionally having 1 to 3 halogen atoms, (51) a C2-6 alkenyl group optionally having 1 to 3 halogen atoms, (52) a C2 alkynyl group -6, and (53) a C1-6 alkyl group substituted with 1 to 3 hydroxy, R2 is (i) a C6-14 aryl group that optionally has 1 to 5 substituents selected from the group consisting of (1) a halogen atom, (2) nitro, (3) cyano, (4) hydroxy, (5) C1-6 alkoxy optionally having 1 to 3 halogen atoms, (6) C6-14 aryloxy, (7 ) C7-16 aralkyloxy, (8) mercap to, (9) C1-6 alkylthio having optionally 1 to 3 halogen atoms, (10) C6-14 arylthio, (11) C7-16 aralkylthio, (12) amino, (13) mono-alkyl C1-6-amino, (14) C6-14-amino mono-aryl, (15) C7-16-amino mono-aralkyl, (16) C1-6-amino di-alkyl, (17) di C6-14-amino aryl, (18) C7-16-amino di-aralkyl, (19) formyl, (20) C1-6-carbonyl alkyl, (21) C6-14-carbonyl aryl, ( 22) carboxyl, (23) C1-6-carbonyl alkoxy, (24) C6-14-carbonyl aryloxy, (25) carbamoyl, (26) thiocarbamoyl, (27) C1-6-carbamoyl mono-alkyl, ( 28) C1-6-carbamoyl di-alkyl, (29) C6-14-carbamoyl aryl, (30) C1-6-sulfonyl alkyl, (31) C6-14-sulfonyl aryl, (32) alkyl of C1-6-sulfinyl, (33) C6-14-sulfinyl aryl, (34) formylamino, (35) C1-6-carbonylamino alkyl, (36) C6-14-carbonylamino aryl, (37) C1 alkoxy -6-carbonylamino, (38) C1-6-sulfonylamino alkyl, (39) C6-14-sulfonylamino, (40) C1-6-carbonyloxy alkyl, (41) C6-14-carbonyl aryl loxy, (42) C1-6-carbonyloxy alkoxy, (43) C1-6-carbamoyloxy monoalkyl, (44) C1-6-carbamoyloxy di-alkyl, (45) C6-14-carbamoyloxy aryl, (46 ) a saturated 5- to 7-membered cyclic amino optionally containing, in addition to a nitrogen atom and carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom , (47) a 5 to 10-membered aromatic heterocyclic group containing, in addition to carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, (48 ) C1-3-dioxy alkylene, (49) C3-7 cycloalkyl, (50) C1-6 alkyl group optionally having 1 to 3 halogen atoms, (51) a C2-6 alkenyl group having optionally 1 to 3 halogen atoms, (52) a C2-6 alkynyl group, and (53) a C1-6 alkyl group substituted with 1 to 3 hydroxy, (ii) a thienyl group optionally having 1 to 4 sel substituents from the group consisting of (1) a halogen atom, (2) nitro, (3) cyano, (4) hydroxy, (5) C1-6 alkoxy which optionally has 1 to 3 halogen atoms, (6 ) C6-14 aryloxy, (7) C7-16 aralkyloxy, (8) mercapto, (9) C1-6 alkylthio optionally having 1 to 3 halogen atoms, (10) C6-14 arylthio, ( 11) C7-16 aralkylthio, (12) amino, (13) C1-6-amino mono-alkyl, (14) C6-14-amino mono-aryl, (15) C7-16 mono-aralkyl- amino, (16) C1-6-amino di-alkyl, (17) C6-14-amino di-aryl, (18) C7-16-amino di-aralkyl, (19) formyl, (20) alkyl C1-6-carbonyl, (21) C6-14-carbonyl aryl, (22) carboxyl, (23) C1-6-carbonyl alkoxy, (24) C6-14-carbonyl aryloxy, (25) carbamoyl, (26) thiocarbamoyl, (27) C1-6-carbamoyl mono-alkyl, (28) C1-6-carbamoyl di-alkyl, (29) C6-14-carbamoyl aryl, (30) C1-6 alkyl -sulfonyl, (31) C6-14-sulfonyl aryl, (32) C1-6-sulfinyl alkyl, (33) C6-14-sulfinyl aryl, (34) formylamino, (35) C1-6-carbonylamino alkyl, (36) C6-14-carbonylamino aryl, (37) C1-6-carbonylamino alkoxy, (38) C1-6-sulfonylamino alkyl, (39) C6-14- aryl sulfonylamino, (40) C1-6-carbonyloxy alkyl, (41) C6-14-carbonyloxy aryl, (42) C1-6-carbonyloxy alkoxy, (43) C1-6-carbamoyloxy monoalkyl, (44) di -C1-6-carbamoyloxy alkyl, (45) C6-14-carbamoyloxy aryl, (46) a 5- to 7-membered saturated cyclic amino which optionally contains, in addition to a nitrogen atom and carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, (47) a 5- to 10-membered aromatic heterocyclic group containing, in addition to carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, (48) C1-3-dioxy alkylene, (49) C3-7 cycloalkyl, (50) C1-6 alkyl group which optionally has 1 to 3 halogen atoms, (51) an alkenyl group d and C2-6 optionally having 1 to 3 halogen atoms, (52) a C2-6 alkynyl group, and (53) a C1-6 alkyl group substituted with 1 to 3 hydroxy, or (iii) a group pyridyl having optionally 1 to 4 substituents selected from the group consisting of (1) a halogen atom, (2) nitro, (3) cyano, (4) hydroxy, (5) C1-6 alkoxy optionally having 1 to 3 halogen atoms, (6) C6-14 aryloxy, (7) C7-16 aralkyloxy, (8) mercapto, (9) C1-6 alkylthio having optionally 1 to 3 halogen atoms, ( 10) C6-14 arylthio, (11) C7-16 aralkylthio, (12) amino, (13) C1-6-amino mono-alkyl, (14) C6-14-amino mono-aryl, (15 ) C7-16-amino mono-aralkyl, (16) C1-6-amino di-alkyl, (17) C6-14-amino di-aryl, (18) C7-16-amino di-aralkyl, (19) formyl, (20) C1-6-carbonyl alkyl, (21) C6-14-carbonyl aryl, (22) carboxyl, (23) C1-6-carbonyl alkoxy, (24) C6- aryloxy 14-carbonyl, (25) carbamoyl, (26) thiocarbamoyl, (27) mono-alk C1-6-carbamoyl, (28) di-C1-6-carbamoyl, (29) C6-14-carbamoyl aryl, (30) C1-6-sulfonyl alkyl, (31) C6- aryl 14-sulfonyl, (32) C1-6-sulfinyl alkyl, (33) C6-14-sulfinyl aryl, (34) formylamino, (35) C1-6-carbonylamino alkyl, (36) C6-14 aryl -carbonylamino, (37) C1-6-carbonylamino alkoxy, (38) C1-6-sulfonylamino alkyl, (39) C6-14-sulfonylamino aryl, (40) C1-6-carbonyloxy alkyl, (41) C6-14-carbonyloxy aryl, (42) C1-6-carbonyloxy alkoxy, (43) C1-6-carbamoyloxy monoalkyl, (44) C1-6-carbamoyloxy di-alkyl, (45) C6- aryl 14-carbamoyloxy, (46) a saturated 5- to 7-membered cyclic amino containing optionally, in addition to a nitrogen atom and carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selected from a nitrogen atom, an atom of sulfur and an oxygen atom, (47) a 5 to 10-membered aromatic heterocyclic group containing, in addition to carbon atoms, 1 or 2 types of 1 to 4 heteroatoms selects two of a nitrogen atom, a sulfur atom and an oxygen atom, (48) C1-3-dioxy alkylene, (49) C3-7 cycloalkyl, (50) C1-6 alkyl group optionally having 1 to 3 halogen atoms, (51) a C2-6 alkenyl group optionally having 1 to 3 halogen atoms, (52) a C2-6 alkynyl group, and (53) a C1-6 alkyl group substituted with 1 to 3 hydroxy, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is (i) a C1-4 alkyl group optionally having 1 to 3 substituents selected from the group consisting of (1) a halogen atom, (2) nitro, (3) cyano, (4) hydroxy, (5) C1-6 alkoxy optionally having 1 to 3 halogen atoms, ( 6) C6-14 aryloxy, (7) C7-16 aralkyloxy, (8) mercapto, (9) C1-6 alkylthio having optionally 1 to 3 halogen atoms, (10) C6-14 arylthio, (11) C7-16 aralkylthio, (12) amino, (13) C1-6-amino mono-alkyl, (14) C6-14-amino mono-aryl,
机译：由式（I）表示的化合物：其中R 1为含有饱和或不饱和芳族或非芳族氮的杂环单环基，该氮含至少一个氮原子作为构成环的原子，并且任选地与苯稠合环或芳族或非芳族杂环，含氮的杂环单环基团任选与苯环或杂环稠合，任选具有1-5个选自以下的取代基：（1）卤原子，（2）硝基，（ 3）氰基，（4）羟基，（5）具有1-3个卤素原子的C1-6烷氧基，（6）C6-14芳氧基，（7）C7-芳烷氧基16，（8）巯基，（9）C1- 6个可任选具有1-3个卤原子的烷硫基;（10）C6-14芳硫基;（11）C7-16芳烷硫基;（12）氨基;（13）C1-6-氨基单烷基;（14）C6-14 -氨基单芳基，（15）C7-16-氨基单芳烷基，（16）C1-6-氨基二烷基，（17）C6-14-氨基二芳基，（18）C7-16-氨基二芳烷基，（19）甲酰基，（20）C1-6-烷基碳乙烯基，（21）C6-14-羰基芳基，（22）羧基，（23）C1-6-羰基烷氧基，（24）C6-14-羰基芳氧基，（25）氨基甲酰基，（26）硫代氨基甲酰基，（27） C1-6-氨基甲酰基单烷基，（28）C1-6-氨基甲酰基二烷基，（29）C6-14-氨基甲酰基芳基，（30）C1-6-磺酰基烷基，（31）C6-14-磺酰基芳基，（32）C1-6-亚磺酰基烷基，（33）C6-14-亚磺酰基芳基，（34）甲氨基，（35）C1-6-羰基氨基烷基，（36）C6-14-羰基氨基芳基，（37）C1 -6-羰基氨基烷氧基，（38）C1-6-磺酰基氨基烷基，（39）C6-14-磺酰基氨基芳基，（40）C1-6烷基羰氧基，（41）C6-14-羰基氧基芳基，（42）C1- 6-羰氧基烷氧基，（43）C1-6-氨基甲酰氧基单烷基，（44）C1-6-氨基甲酰氧基二烷基，（45）C6-14-氨基甲酰氧基芳基，（46）5至7元饱和除了原子或氮原子和碳原子以外，还任选包含选自氮原子，硫原子和氧原子的1至2种1-4个杂原子的环状氨基，（47）5-10元芳香族含碳的杂环基原子，选自氮原子，硫原子和氧原子的1或2种类型的1-4个杂原子，（48）C1-3-二氧亚烷基，（49）C3-7环烷基，（50）C1-6烷基任选具有1-3个卤原子的基团，（51）任选具有1-3个卤原子的C2-6烯基，（52）C2炔基-6，和（53）被1至1取代的C1-6烷基R 3为羟基，R2为（i）C6-14芳基，其任选具有1-5个选自以下的取代基：（1）卤素原子，（2）硝基，（3）氰基，（4）羟基，（ 5）任选具有1-3个卤原子的C1-6烷氧基，（6）C6-14芳氧基，（7）C7-16芳烷氧基，（8）巯基，（9）任选具有1-3个卤原子的C1-6烷硫基，（10）C6-14芳硫基，（11）C7-16芳烷硫基，（12）氨基，（13）单烷基C1-6-氨基，（14）C6-14-氨基单芳基，（15）C7 -16-氨基单芳烷基，（16）C1-6-氨基二烷基，（17）二C6-14-氨基芳基，（18）C7-16-氨基二芳烷基，（19）甲酰基，（20 ）C1-6-羰基烷基，（21）C6-14-羰基芳基，（2 2）羧基，（23）C1-6-羰基烷氧基，（24）C6-14-羰基芳氧基，（25）氨基甲酰基，（26）硫代氨基甲酰基，（27）C1-6-氨基甲酰基单烷基，（28）C1 -6-氨基甲酰基二烷基，（29）C6-14-氨基甲酰基芳基，（30）C1-6-磺酰基烷基，（31）C6-14-磺酰基芳基，（32）C1-6-磺酰基烷基，（ 33）C6-14-亚磺酰基芳基，（34）甲酰氨基，（35）C1-6-羰基氨基烷基，（36）C6-14-羰基氨基芳基，（37）C1烷氧基-6-羰基氨基，（38）C1-6 -磺酰基氨基烷基，（39）C6-14-磺酰基氨基，（40）C1-6-羰氧基烷基，（41）C6-14-羰基芳氧基，（42）C1-6-羰氧基烷氧基，（43）C1-6 -氨基甲酰氧基单烷基，（44）C1-6-氨基甲酰氧基二烷基，（45）C6-14-氨基甲酰氧基芳基，（46）饱和的5至7元环氨基，除了氮原子和碳原子外，还含有（47）一个除碳原子外还包含1或2种类型的5至10元芳族杂环基的选自氮原子，硫原子和氧原子的1或2种类型的1至4个杂原子。 1至4升选自氮原子，硫原子和氧原子的碳原子，（48）C1-3-二氧亚烷基，（49）C3-7环烷基，（50）C1-6烷基，其任选具有1-3个卤原子， 51）具有任选地1-3个卤原子的C2-6烯基，（52）C2-6炔基，和（53）被1-3个羟基取代的C1-6烷基，（ii）噻吩基具有1至4个选自以下的取代基的sel取代基：（1）卤原子，（2）硝基，（3）氰基，（4）羟基，（5）任选具有1-3个卤原子的C1-6烷氧基，（ 6）C6-14芳氧基，（7）C7-16芳烷氧基，（8）巯基，（9）任选具有1-3个卤原子的C1-6烷硫基，（10）C6-14芳硫基，（11）C7-16芳烷硫基，（12）氨基，（13）C1-6-氨基单烷基，（14）C6-14-氨基单芳基，（15）C7-16单芳烷基-氨基，（16）C1-6-氨基二烷基，（17）C6-14-氨基二芳基，（18）C7-16-氨基二芳烷基，（19）甲酰基，（20）C1-6-羰基烷基，（21）C6-14-羰基芳基，（22）羧基，（23）C1-6-羰基烷氧基，（24）C6-14-羰基芳氧基，（25）氨基甲酰基，（26）硫代氨基甲酰基，（27）C1-6-氨基甲酰基单烷基，（28）C1-6-氨基甲酰基二烷基，（29）C6- 14-氨基甲酰基芳基，（30）C1-6烷基-磺酰基，（31）C6-14-磺酰基芳基，（32）C1-6-亚磺酰基烷基，（33）C6-14-亚磺酰基芳基，（34）甲酰氨基， （35）C1-6-羰基氨基烷基，（36）C6-14-羰基氨基芳基，（37）C1-6-羰基氨基烷氧基，（38）C1-6-磺酰基氨基烷基，（39）C6-14-芳基磺酰基氨基， （40）C1-6-羰基氧基烷基，（41）C6-14-羰基氧基芳基，（42）C1-6-羰基氧基烷氧基，（43）C1-6-氨基甲酰氧基单烷基，（44）二-C1-6-氨基甲酰氧基烷基，（45）C6-14-氨基甲酰氧基芳基，（46）5至7元饱和环状氨基，其除了氮原子和碳原子外，还包含选自以下的一种或两种类型的1-4个杂原子（47）5至10元芳香族杂环基，除了碳原子外，还包含选自氮原子中的1至4种1-4个杂原子tom，硫原子和氧原子，（48）C 1-3-二氧亚烷基，（49）C 3-7环烷基，（50）任选具有1-3个卤原子的C 1-6烷基，（51）烯基d和C2-6基团任选具有1-3个卤原子，（52）C2-6炔基，和（53）被1-3个羟基取代的C1-6烷基，或（iii）吡啶基，其任选具有1-4个选自以下的取代基：（1）卤素原子，（2）硝基，（3）氰基，（4）羟基，（5）任选具有1-3个卤素原子的C1-6烷氧基，（6） C6-14芳氧基，（7）C7-16芳烷氧基，（8）巯基，（9）具有1-3个卤素原子的C1-6烷硫基，（10）C6-14芳硫基，（11）C7-16芳硫基，（ 12）氨基，（13）C1-6-氨基单芳基，（14）C6-14-氨基单芳基，（15）C7-16-氨基单芳烷基，（16）C1-6-氨基二芳基烷基，（17）C6-14-氨基二芳基，（18）C7-16-氨基二芳烷基，（19）甲酰基，（20）C1-6-羰基烷基，（21）C6-14-羰基芳基，（22）羧基，（23）C1-6-羰基烷氧基，（24）C6-芳氧基14-羰基l，（25）氨基甲酰基，（26）硫代氨基甲酰基，（27）单链C1-6-氨基甲酰基，（28）二-C1-6-氨基甲酰基，（29）C6-14-氨基甲酰基芳基，（30）C1- 6-磺酰基烷基，（31）C6-芳基14-磺酰基，（32）C1-6-亚磺酰基烷基，（33）C6-14-亚磺酰基芳基，（34）甲酰氨基，（35）C1-6-羰基氨基烷基， （36）C6-14芳基-羰基氨基，（37）C1-6-羰基氨基烷氧基，（38）C1-6-磺酰基氨基烷基，（39）C6-14-磺酰基氨基芳基，（40）C1-6-羰基氧基烷基， （41）C6-14-羰基氧基芳基，（42）C1-6-羰基氧基烷氧基，（43）C1-6-氨基甲酰氧基单烷基，（44）C1-6-氨基甲酰氧基二烷基，（45）C6-芳基14-氨基甲酰氧基，（46）饱和的5至7元环氨基，除氮原子和碳原子外，还任选包含1或2种选自氮原子，硫原子和氧的1-4个杂原子原子，（47）除碳原子外还含有1或2种1-4个杂原子的5-10元芳族杂环基团，选择氮原子，硫原子和氧原子中的两个m，（48）C 1-3-二氧亚烷基，（49）C 3-7环烷基，（50）任选具有1-3个卤原子的C 1-6烷基，（51）任选具有1-3的C 2-6烯基卤素原子，（52）C2-6炔基和（53）被1-3个羟基取代的C1-6烷基，R3和R4各自为氢原子，或R3和R4之一为氢原子，另一个是（i）C 1-4烷基，其任选地具有1-3个选自以下的取代基：（1）卤素原子，（2）硝基，（3）氰基，（4）羟基，（5）C1 -6个烷氧基，可选具有1-3个卤原子，（6）C6-14芳氧基，（7）C7-16芳烷氧基，（8）巯基，（9）C1-6烷硫基，可选具有1-3个卤原子，（10） C6-14芳硫基，（11）C7-16芳硫基，（12）氨基，（13）C1-6-氨基单烷基，（14）C6-14-氨基单芳基，

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