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公开(公告)号：US08686010B2
公开(公告)日：2014-04-01
申请号：US13204093
申请日：2011-08-05
IPC分类号： A61K31/426 , A61K31/417 , A61K31/40
CPC分类号： C07D207/36 , A61K31/40 , A61K31/415 , A61K31/417 , A61K31/4178 , A61K31/426 , A61K31/4439 , C07D231/12 , C07D233/64 , C07D233/84 , C07D277/36 , C07D401/12 , C07D409/12
摘要： The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.A proton pump inhibitor containing a compound represented by the formula (I) wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms X1 and X2 are each a carbon atom or a nitrogen atom, a ring-constituting atom X3 is a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, R1 is an optionally substituted aryl group or an optionally substituted heteroaryl group, R2 is an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, R3 is an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X1, X2 and X3, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用，抗溃疡活性等的化合物。 含有式（I）表示的化合物的质子泵抑制剂，其中环A是饱和或不饱和的5-或6-元环基，任选具有除碳原子之外的环构成原子，含有1-4个选自 氮原子，氧原子和硫原子，构成环的原子X1和X2各自为碳原子或氮原子，构成环的原子X3为碳原子，氮原子，氧原子或硫原子 原子，R 1是任选取代的芳基或任选取代的杂芳基，R 2是任选取代的烷基，任选取代的芳基或任选取代的杂芳基，R 3是任选被1或2个低级烷基取代的氨基甲基 其是除X1，X2和X3以外的环构成原子上的取代基，环A任选地还具有选自低级烷基，卤素原子，氰基和氧代基的取代基，或 盐在那里 f或其前药。
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公开(公告)号：US07994205B2
公开(公告)日：2011-08-09
申请号：US12225851
申请日：2007-03-30
IPC分类号： A01N43/50
CPC分类号： C07D207/36 , A61K31/40 , A61K31/415 , A61K31/417 , A61K31/4178 , A61K31/426 , A61K31/4439 , C07D231/12 , C07D233/64 , C07D233/84 , C07D277/36 , C07D401/12 , C07D409/12
摘要： The present invention provides an aryl- or heteroaryl compound represented by the formula (Ia) or (Ib) wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. The compound has superior acid secretion inhibitory action, an antiulcer activity and the like.
摘要翻译： 本发明提供由式（Ia）或（Ib）表示的芳基或杂芳基化合物，其中每个符号如说明书中所定义，或其盐，或包含该化合物和药学上可接受的载体的药物组合物。 该化合物具有优异的酸分泌抑制作用，抗溃疡活性等。
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公开(公告)号：US20090118335A1
公开(公告)日：2009-05-07
申请号：US12225851
申请日：2007-03-30
IPC分类号： A61K31/437 , C07D207/36 , C07D233/60 , C07D401/12 , C07D231/18 , C07D409/12 , A61K31/40 , A61P1/00 , A61K31/4178 , A61K31/427 , A61K31/415 , A61K31/4164
CPC分类号： C07D207/36 , A61K31/40 , A61K31/415 , A61K31/417 , A61K31/4178 , A61K31/426 , A61K31/4439 , C07D231/12 , C07D233/64 , C07D233/84 , C07D277/36 , C07D401/12 , C07D409/12
摘要： The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.A proton pump inhibitor containing a compound represented by the formula (I) wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms X1 and X2 are each a carbon atom or a nitrogen atom, a ring-constituting atom X3 is a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, R1 is an optionally substituted aryl group or an optionally substituted heteroaryl group, R2 is an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, R3 is an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X1, X2 and X3, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用，抗溃疡活性等的化合物。 含有式（I）表示的化合物的质子泵抑制剂，其中环A是饱和或不饱和的5-或6-元环基，任选具有除碳原子之外的环构成原子，含有1-4个选自 氮原子，氧原子和硫原子，构成环的原子X1和X2各自为碳原子或氮原子，构成环的原子X3为碳原子，氮原子，氧原子或硫原子 原子，R 1是任选取代的芳基或任选取代的杂芳基，R 2是任选取代的烷基，任选取代的芳基或任选取代的杂芳基，R 3是任选被1或2个低级烷基取代的氨基甲基 其是除X1，X2和X3以外的环构成原子上的取代基，环A任选地还具有选自低级烷基，卤素原子，氰基和氧代基的取代基，或 盐在那里 f或其前药。
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4.发明申请ARYL- OR HETEROARYL-SULFONYL COMPOUNDS AS ACID SECRETION INHIBITORS 有权作为酸分泌抑制剂的ARYL-或HETEROARYL-SULFONYL化合物公开(公告)号：US20110288040A1
公开(公告)日：2011-11-24
申请号：US13204093
申请日：2011-08-05
IPC分类号： A61K31/7048 , A61K31/417 , A61K31/4439 , A61K31/4178 , A61P31/04 , A61K31/426 , A61K31/43 , A61P1/04 , A61P35/00 , A61P7/04 , A61K31/40 , A61K31/415
CPC分类号： C07D207/36 , A61K31/40 , A61K31/415 , A61K31/417 , A61K31/4178 , A61K31/426 , A61K31/4439 , C07D231/12 , C07D233/64 , C07D233/84 , C07D277/36 , C07D401/12 , C07D409/12
摘要： The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.A proton pump inhibitor containing a compound represented by the formula (I) wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms X1 and X2 are each a carbon atom or a nitrogen atom, a ring-constituting atom X3 is a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, R1 is an optionally substituted aryl group or an optionally substituted heteroaryl group, R2 is an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, R3 is an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X1, X2 and X3, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用，抗溃疡活性等的化合物。 含有式（I）表示的化合物的质子泵抑制剂，其中环A是饱和或不饱和的5-或6-元环基，任选具有除碳原子之外的环构成原子，含有1-4个选自 氮原子，氧原子和硫原子，构成环的原子X1和X2各自为碳原子或氮原子，构成环的原子X3为碳原子，氮原子，氧原子或硫原子 原子，R 1是任选取代的芳基或任选取代的杂芳基，R 2是任选取代的烷基，任选取代的芳基或任选取代的杂芳基，R 3是任选被1或2个低级烷基取代的氨基甲基 其是除X1，X2和X3以外的环构成原子上的取代基，环A任选地还具有选自低级烷基，卤素原子，氰基和氧代基的取代基，或 盐在那里 f或其前药。
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5.发明授权1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors 有权1-杂环基磺酰基，3-氨基甲基，5-（杂）芳基取代的1 H-吡咯衍生物作为酸分泌抑制剂公开(公告)号：US08338462B2
公开(公告)日：2012-12-25
申请号：US13156226
申请日：2011-06-08
IPC分类号： C07D401/02 , A61K31/444
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基小时，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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6.发明申请1-HETEROCYCLYLSULFONYL, 2-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS 有权作为酸分泌抑制剂的1-杂环甲硅烷基，2-氨基乙基，5-（异丁基）芳基取代的1-H-吡咯烷酮衍生物公开(公告)号：US20110144161A1
公开(公告)日：2011-06-16
申请号：US13037690
申请日：2011-03-01
IPC分类号： A61K31/444 , A61K31/4439 , C07D401/14 , C07D401/02 , A61P35/00 , A61P1/04
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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7.发明授权1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors 有权1-杂环基磺酰基，3-氨基甲基，5-（杂）芳基取代的1 H-吡咯衍生物作为酸分泌抑制剂公开(公告)号：US08436187B2
公开(公告)日：2013-05-07
申请号：US13156204
申请日：2011-06-08
IPC分类号： C07D401/02
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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8.发明授权1-heterocyclylsulfonyl, 2-aminomethyl, 5-(hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors 有权1-杂环基磺酰基，2-氨基甲基，5-（杂）芳基取代的1-H-吡咯衍生物作为酸分泌抑制剂公开(公告)号：US07977488B2
公开(公告)日：2011-07-12
申请号：US11991307
申请日：2006-08-29
IPC分类号： C07D401/02
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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9.发明申请1-HETEROCYCLYLSULFONYL, 2-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITOR 有权1-异喹啉基，2-氨基乙基，5-（异丁基）芳基取代的1-H-吡咯烷酮衍生物作为酸分泌抑制剂公开(公告)号：US20090275591A1
公开(公告)日：2009-11-05
申请号：US11991307
申请日：2006-08-29
IPC分类号： A61K31/4025 , C07D401/12 , C07D403/12 , C07D487/04 , C07D401/14 , A61K31/4439 , A61K31/4178 , A61K31/4155 , A61K31/444 , A61K31/519 , A61K31/501
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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公开(公告)号：US07498337B2
公开(公告)日：2009-03-03
申请号：US11512629
申请日：2006-08-29
IPC分类号： A61K31/435 , C07D401/06 , C07D257/08 , C07D257/12 , C07D253/04 , C07D253/06 , C07D253/10
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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