公开(公告)号：US20110288040A1

公开(公告)日：2011-11-24

申请号：US13204093

申请日：2011-08-05

申请人： Atsushi Hasuoka ,  Terufumi Takagi ,  Masahiro Kajino ,  Haruyuki Nishida

发明人： Atsushi Hasuoka ,  Terufumi Takagi ,  Masahiro Kajino ,  Haruyuki Nishida

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。

公开(公告)号：US20090118335A1

公开(公告)日：2009-05-07

申请号：US12225851

申请日：2007-03-30

申请人： Atsushi Hasuoka ,  Terufumi Takagi ,  Masahiro Kajino ,  Haruyuki Nishida

发明人： Atsushi Hasuoka ,  Terufumi Takagi ,  Masahiro Kajino ,  Haruyuki Nishida

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。

公开(公告)号：US20080139639A1

公开(公告)日：2008-06-12

申请号：US11664346

申请日：2005-09-30

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

IPC分类号： A61K31/40 ,  C07D207/48 ,  A61P1/04

CPC分类号： C07D207/48 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04

摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

摘要翻译： 一种质子泵抑制剂，其含有式（I）表示的化合物，其中X和Y相同或不同，并且各自是主链中具有1至20个碳原子的键或间隔基，R 1 >是任选取代的烃基或任选取代的杂环基，R 2，R 3和R 4相同或不同，并且各自 任选取代的苯并[b]噻吩基，任选取代的呋喃基，任意取代的吡啶基，任意取代的吡唑基，任意取代的嘧啶基 ，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或任选地 取代烃基，其具有优异的质子泵作用，并显示出抗溃疡活性等 转化为体内的质子泵抑制剂或其盐。 或其前药。

公开(公告)号：US08048909B2

公开(公告)日：2011-11-01

申请号：US11664346

申请日：2005-09-30

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Terufumi Takagi

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Terufumi Takagi

IPC分类号： A61K31/40 ,  C07D207/48 ,  A61P1/04

CPC分类号： C07D207/48 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04

摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug thereof is provided.

摘要翻译： 一种含有式（I）表示的化合物的质子泵抑制剂，其中X和Y相同或不同，并且各自是主链中的键或具有1至20个碳原子的间隔基，R 1是任选取代的烃基或 任选取代的杂环基，R 2，R 3和R 4相同或不同，各自为氢原子，任选取代的烃基，任选取代的噻吩基，任选取代的苯并[b]噻吩基，任选取代的呋喃基 ，任选取代的吡啶基，任选取代的吡唑基，任选取代的嘧啶基，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或 任选取代的烃基，其具有优异的质子泵作用，并且在体内转化为质子泵抑制剂之后显示出抗溃疡活性等，或其中的盐 或其前药。

公开(公告)号：US08686010B2

公开(公告)日：2014-04-01

申请号：US13204093

申请日：2011-08-05

申请人： Atsushi Hasuoka ,  Terufumi Takagi ,  Haruyuki Nishida

发明人： Atsushi Hasuoka ,  Terufumi Takagi ,  Haruyuki Nishida

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。

公开(公告)号：US07994205B2

公开(公告)日：2011-08-09

申请号：US12225851

申请日：2007-03-30

申请人： Atsushi Hasuoka ,  Terufumi Takagi ,  Haruyuki Nishida

发明人： Atsushi Hasuoka ,  Terufumi Takagi ,  Haruyuki Nishida

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。

公开(公告)号：US20110028476A1

公开(公告)日：2011-02-03

申请号：US12873971

申请日：2010-09-01

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Naoki Tarui ,  Terufumi Takagi

IPC分类号： A61K31/5377 ,  C07D207/48 ,  A61K31/40 ,  C07D409/12 ,  A61K31/4025 ,  C07D403/12 ,  A61K31/506 ,  C07D401/12 ,  A61K31/4439 ,  C07D405/12 ,  C07D417/12 ,  A61K31/428 ,  A61K31/4178 ,  C07D403/04 ,  A61K31/4155 ,  C07D487/04 ,  A61K31/519 ,  A61K31/501 ,  C07D413/12 ,  A61P1/00

CPC分类号： C07D207/48 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04

摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

摘要翻译： 一种含有式（I）表示的化合物的质子泵抑制剂，其中X和Y相同或不同，并且各自是主链中的键或具有1至20个碳原子的间隔基，R 1是任选取代的烃基或 任选取代的杂环基，R 2，R 3和R 4相同或不同，各自为氢原子，任选取代的烃基，任选取代的噻吩基，任选取代的苯并[b]噻吩基，任选取代的呋喃基 ，任选取代的吡啶基，任选取代的吡唑基，任选取代的嘧啶基，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或 任选取代的烃基，其具有优异的质子泵作用，并且在体内转化为质子泵抑制剂之后显示出抗溃疡活性等，或其中的盐 的。 或其前药。

公开(公告)号：US08338462B2

公开(公告)日：2012-12-25

申请号：US13156226

申请日：2011-06-08

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

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。

公开(公告)号：US20110144161A1

公开(公告)日：2011-06-16

申请号：US13037690

申请日：2011-03-01

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

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。

公开(公告)号：US08436187B2

公开(公告)日：2013-05-07

申请号：US13156204

申请日：2011-06-08

申请人： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

发明人： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

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。