公开(公告)号：US20050004149A1

公开(公告)日：2005-01-06

申请号：US10492905

申请日：2002-10-22

申请人： Hitoshi Harada ,  Osamu Asano ,  Masato Ueda ,  Shuhei Miyazawa ,  Yoshihiko Kotake ,  Yasuhiro Kabasawa ,  Masahiro Yasuda ,  Nobuyuki Yasuda ,  Daisuke Iida ,  Junichi Nagakawa ,  Kazuo Hirota ,  Makoto Nakagawa

发明人： Hitoshi Harada ,  Osamu Asano ,  Masato Ueda ,  Shuhei Miyazawa ,  Yoshihiko Kotake ,  Yasuhiro Kabasawa ,  Masahiro Yasuda ,  Nobuyuki Yasuda ,  Daisuke Iida ,  Junichi Nagakawa ,  Kazuo Hirota ,  Makoto Nakagawa

IPC分类号： A61K31/506 ,  A61P1/00 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/02 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  C07

CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

摘要： The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them. In the formula, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

公开(公告)号：US07396836B2

公开(公告)日：2008-07-08

申请号：US10492905

申请日：2002-10-22

申请人： Hitoshi Harada ,  Masato Ueda ,  Yoshihiko Kotake ,  Masahiro Yasuda ,  Daisuke Iida ,  Junichi Nagakawa ,  Makoto Nakagawa

发明人： Hitoshi Harada ,  Masato Ueda ,  Yoshihiko Kotake ,  Masahiro Yasuda ,  Daisuke Iida ,  Junichi Nagakawa ,  Makoto Nakagawa

IPC分类号： A61K31/505 ,  C07D239/02

CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

摘要： A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R1 and R2, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); R4 represents an aromatic hydrocarbon cyclic group which may be substituted, and R5 represents an aromatic hydrocarbon cyclic group which may be substituted.

摘要翻译： 具有优异的腺苷受体（A 1 H 1，A 2 A 2，A 2B 2受体）的化合物，下式的拮抗作用，其盐或 它们的溶剂化物：其中R 1，R 2和R 2相同或不同，各自表示氢原子，烷基，烯基，炔基， 环烷基，环烯基，芳香族烃基，酰基或烷基磺酰基，该基团可被取代（氢原子除外）。 R 3表示氢原子，卤素原子，氰基，烷基，烯基，炔基，芳族烃环状基团，氮原子，氧原子或硫原子 原子，该基团可被取代（氢原子，卤素原子和氰基除外）; R 4表示可以被取代的芳族烃环状基团，R 5表示可以被取代的芳族烃环状基团。

公开(公告)号：US20090030023A1

公开(公告)日：2009-01-29

申请号：US12054337

申请日：2008-03-24

申请人： Hitoshi Harada ,  Masato Ueda ,  Yoshihiko Kotake ,  Masahiro Yasuda ,  Daisuke Iida ,  Junichi Nagakawa ,  Makoto Nakagawa

发明人： Hitoshi Harada ,  Masato Ueda ,  Yoshihiko Kotake ,  Masahiro Yasuda ,  Daisuke Iida ,  Junichi Nagakawa ,  Makoto Nakagawa

IPC分类号： C07D239/42 ,  A61K31/505 ,  C12N5/00 ,  A61P1/00

CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

摘要： A compound represented by the following formula (I), a salt, or a solvate thereof: wherein, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a non-aromatic heterocyclic group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, an acyl group or an alkylsulfonyl group all of which may be substituted and wherein one, or both, of R1 or R2 is an aromatic, or non-aromatic, heterocyclic group which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, a nitrogen atom, an oxygen atom or a sulfur atom all of which may be substituted if possible; and R4 is a pyridyl group which may be substituted.

摘要翻译： 由下式（I）表示的化合物，其盐或溶剂化物：其中，R1和R2彼此相同或不同，各自表示氢原子，烷基，烯基，炔基 基团，环烷基，环烯基，非芳族杂环基，芳香族烃环基，芳香族杂环基，酰基或烷基磺酰基，其全部可以被取代，并且其中R1或 或R 2是可以被取代的芳族或非芳族杂环基; R3表示氢原子，卤原子，氰基，烷基，烯基，炔基，芳香族烃环基，芳香族杂环基，氮原子，氧原子或硫原子全部 如果可能的话可以被替代; R4为可被取代的吡啶基。

公开(公告)号：US20090203911A1

公开(公告)日：2009-08-13

申请号：US12189590

申请日：2008-08-11

申请人： Shuhei MIYAZAWA ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

发明人： Shuhei MIYAZAWA ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

IPC分类号： C07D405/14 ,  C07D401/12

CPC分类号： C07D491/04 ,  C07D405/14 ,  C07D493/08 ,  C07D493/10

摘要： A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

摘要翻译： 提供了可用作酸性相关疾病的治疗或预防剂的新型化合物，其对胃酸分泌具有优异的抑制作用，保持对胃酸分泌的抑制作用的优异效果，从而保持胃内pH高 长时间，具有更多的安全性和适当的物理化学稳定性。 提供一种化合物，其中R 1和R 3可以相同或不同，各自表示氢原子或C 1 -C 6烷基; R2代表（5,5-二甲基-1,3-二恶烷-2-基）甲氧基，5,7-二氧杂螺[2.5]辛-6-基甲氧基，1,5,9-三氧杂螺[5.5]十一烷-3 - 甲氧基或（2,2-二甲基-1,3-二恶烷-5-基）甲氧基; R4，R5，R6和R7表示氢原子，卤素原子，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基或C1-C6卤代烷氧基; W1表示单键，亚甲基或亚乙基，它们的盐或它们的溶剂合物。

公开(公告)号：US08124780B2

公开(公告)日：2012-02-28

申请号：US12189590

申请日：2008-08-11

申请人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

发明人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

IPC分类号： C07D401/12

CPC分类号： C07D491/04 ,  C07D405/14 ,  C07D493/08 ,  C07D493/10

摘要： A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

摘要翻译： 提供了可用作酸性相关疾病的治疗或预防剂的新型化合物，其对胃酸分泌具有优异的抑制作用，保持对胃酸分泌的抑制作用的优异效果，从而保持胃内pH高 长时间，具有更多的安全性和适当的物理化学稳定性。 提供一种化合物，其中R 1和R 3可以相同或不同，各自表示氢原子或C 1 -C 6烷基; R2代表（5,5-二甲基-1,3-二恶烷-2-基）甲氧基，5,7-二氧杂螺[2.5]辛-6-基甲氧基，1,5,9-三氧杂螺[5.5]十一烷-3 - 甲氧基或（2,2-二甲基-1,3-二恶烷-5-基）甲氧基; R4，R5，R6和R7表示氢原子，卤素原子，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基或C1-C6卤代烷氧基; W1表示单键，亚甲基或亚乙基，它们的盐或它们的溶剂合物。

公开(公告)号：US07425634B2

公开(公告)日：2008-09-16

申请号：US11520838

申请日：2006-09-14

申请人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

发明人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

IPC分类号： C07D401/12

CPC分类号： C07D491/04 ,  C07D405/14 ,  C07D493/08 ,  C07D493/10

摘要： An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability.Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

摘要翻译： 本发明的目的是提供一种新颖的化合物，其可用作酸性相关疾病的治疗或预防剂，对胃酸分泌具有优异的抑制作用，具有保持对胃酸分泌的抑制作用的优异效果，从而 长时间保持胃内pH高，并具有更多的安全性和适当的物理化学稳定性。 其中R 1和R 3可以相同或不同，表示氢原子或C1-C6烷基; R 5表示（5,5-二甲基-1,3-二恶烷-2-基）甲氧基，5,7-二氧杂螺[2.5]辛-6-基甲氧基，1,5,9 - 三氧杂螺[5.5]十一烷-3-基甲氧基或（2,2-二甲基-1,3-二恶烷-5-基）甲氧基; R 4，R 5，R 6和R 7表示氢原子，卤素原子，C 1 -C 6 烷基，C1-C6卤代烷基，C1-C6烷氧基或C1-C6卤代烷氧基; 和W 1表示单键，亚甲基或亚乙基，其盐或它们的溶剂合物。

公开(公告)号：US20070015782A1

公开(公告)日：2007-01-18

申请号：US11403815

申请日：2006-04-14

申请人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

发明人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

IPC分类号： A61K31/4747 ,  A61K31/4439 ,  C07D491/14

CPC分类号： C07D491/04 ,  C07D405/14 ,  C07D493/08 ,  C07D493/10

摘要： An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

公开(公告)号：US20070010542A1

公开(公告)日：2007-01-11

申请号：US11520838

申请日：2006-09-14

申请人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

发明人： Shuhei Miyazawa ,  Masanobu Shinoda ,  Tetsuya Kawahara ,  Nobuhisa Watanabe ,  Hitoshi Harada ,  Daisuke Iida ,  Hiroki Terauchi ,  Junichi Nagakawa ,  Hideaki Fujisaki ,  Atsuhiko Kubota ,  Masato Ueda

IPC分类号： A61K31/4747 ,  A61K31/4439 ,  C07D405/14

CPC分类号： C07D491/04 ,  C07D405/14 ,  C07D493/08 ,  C07D493/10

摘要： An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

摘要翻译： 本发明的目的是提供一种新颖的化合物，其可用作酸性相关疾病的治疗或预防剂，对胃酸分泌具有优异的抑制作用，具有保持对胃酸分泌的抑制作用的优异效果，从而 长时间保持胃内pH高，并具有更多的安全性和适当的物理化学稳定性。 其中R 1和R 3可以相同或不同，表示氢原子或C1-C6烷基; R 5表示（5,5-二甲基-1,3-二恶烷-2-基）甲氧基，5,7-二氧杂螺[2.5]辛-6-基甲氧基，1,5,9 - 三氧杂螺[5.5]十一烷-3-基甲氧基或（2,2-二甲基-1,3-二恶烷-5-基）甲氧基; R 4，R 5，R 6和R 7表示氢原子，卤素原子，C 1 -C 6 烷基，C1-C6卤代烷基，C1-C6烷氧基或C1-C6卤代烷氧基; 和W 1表示单键，亚甲基或亚乙基，其盐或它们的溶剂合物。

公开(公告)号：US07160892B2

公开(公告)日：2007-01-09

申请号：US10492547

申请日：2002-10-22

申请人： Hitoshi Harada ,  Osamu Asano ,  Masato Ueda ,  Shuhei Miyazawa ,  Yoshihiko Kotake ,  Yasuhiro Kabasawa ,  Masahiro Yasuda ,  Nobuyuki Yasuda

发明人： Hitoshi Harada ,  Osamu Asano ,  Masato Ueda ,  Shuhei Miyazawa ,  Yoshihiko Kotake ,  Yasuhiro Kabasawa ,  Masahiro Yasuda ,  Nobuyuki Yasuda

IPC分类号： A61K31/5377 ,  A61K31/513 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

CPC分类号： C07D239/34 ,  A61K31/513

摘要： The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).

摘要翻译： 本发明提供了对腺苷受体（A 1 SUB，A 2A和A 2B 2受体）表现出优异拮抗作用的新型嘧啶酮化合物，特别是表示的化合物 通式（1）表示的盐，其盐或两者的溶剂合物：（1）其中R 1和R 2各自独立地为氢，C 1〜 C 1-6烷基，C 2-6链烯基，C 2-6炔基，C 3-8环烷基，C 1 -C 6 - 3-8环烯基，5至14元非芳族杂环基，C 6-14芳族烃基，5至14元芳族杂环基，C _{1-6酰基或C 1-6烷基磺酰基; R 3是氢，C 1-6烷基，C 2-6链烯基或C 2-6亚烷基， 炔基; R 4是C 6-14芳族烃基; 5至14元芳族杂环基或具有至少一个不饱和键的5至14元非芳族杂环基; 和R 5是C 6-14芳族烃基或5至14元芳族杂环基（条件是除了氢以外的每个基团可以被取代） 。}

公开(公告)号：US06750232B2

公开(公告)日：2004-06-15

申请号：US10333689

申请日：2003-01-23

申请人： Hitoshi Harada ,  Osamu Asano ,  Shuhei Miyazawa ,  Masato Ueda ,  Masahiro Yasuda ,  Nobuyuki Yasuda

发明人： Hitoshi Harada ,  Osamu Asano ,  Shuhei Miyazawa ,  Masato Ueda ,  Masahiro Yasuda ,  Nobuyuki Yasuda

IPC分类号： C07D40102

CPC分类号： C07D213/80 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/455 ,  C07D213/82 ,  C07D213/85 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14

摘要： A class of substituted compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R1 is selected from hydrido, halo, alkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R5 and R6 are one more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R5 and R6 is substituted with alkysulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.

摘要翻译： 描述了一类取代的化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式（II）定义，其中R 1选自氢，卤素，烷氧基，芳基，烷硫基，烷基氨基，芳烷氧基，叠氮基和烯氧基; 氰基，羟基烷基，卤代烷基，氨基烷基，烷基氨基烷基，烷基羰氧基烷基，氨基羰基和烷基羰基氨基烷基;其中R 2选自氢，氰基， 并且其中R 5和R 6分别独立地选自卤素，烷基磺酰基，氨基磺酰基，烷氧基和烷硫基; 其中R 5和R 6之一被烷基磺酰基，氨基磺酰基或卤代烷基磺酰基取代; 或其药学上可接受的盐。