公开(公告)号：US08735401B2

公开(公告)日：2014-05-27

申请号：US13242541

申请日：2011-09-23

申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusuka ,  Nobuhiro Suzuki

发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusuka ,  Nobuhiro Suzuki

IPC分类号： A61K31/519 ,  A61P35/04 ,  C07D495/04

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

摘要翻译： 本发明提供由下式表示的化合物：其中R1是C1-4烷基; R2是（1）可以具有选自（1'）卤素，（2'）羟基，（3'），C 1〜C 6的取代基的5〜7元含氮杂环基， 4烷基和（4'）C 1-4烷氧基，（2）可具有选自（1'）卤素，（2'）C 1-4烷氧基-C 1-4烷基的取代基的苯基 ，（3'）单-C 1-4烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单-C 1-4烷基氨基甲酰基-C 1-4烷氧基等 ; R3是C1-4烷基; R4是C1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

公开(公告)号：US07300935B2

公开(公告)日：2007-11-27

申请号：US10544069

申请日：2004-01-28

申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： C07D495/04 ,  C07D237/04 ,  A61K31/519 ,  A61K31/501 ,  A61P5/04

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4alkyl and (4′) a C1-4alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4alkoxy-C1-4alkyl, (3′) a mono-C1-4alkyl-carbamoyl-C1-4alkyl, (4′) a C1-4alkoxy and (5′) a mono-C1-4alkylcarbamoyl-C1-4alkoxy, or the like; R3 is a C1-4alkyl; R4 is a C1-4alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

摘要翻译： 本发明提供由下式表示的化合物：其中R 1是C 1-4烷基; R 2是（1）可以具有选自（1'）卤素，（2'）羟基的取代基的5-至7-元含氮杂环基 ，（3'）C 1-4烷基和（4'）C 1-4烷氧基，（2）可具有选自以下的取代基的苯基： （1'）卤素，（2'），C 1-4烷氧基-C 1-4烷基，（3'）单-C 烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单 -C 1-4烷基氨基甲酰基-C 1-4烷氧基等; R 3是C 1-4烷基; R 4是C 1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

公开(公告)号：US20080108623A1

公开(公告)日：2008-05-08

申请号：US11848939

申请日：2007-08-31

申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： A61K31/495 ,  A61K31/519 ,  C07D495/04 ,  C07D401/02 ,  A61P5/04

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

摘要翻译： 本发明提供由下式表示的化合物：其中R 1是C 1-4烷基; R 2是（1）可以具有选自（1'）卤素，（2'）羟基的取代基的5-至7-元含氮杂环基 ，（3'）C 1-4烷基和（4'）C 1-4烷氧基，（2）可以具有选自以下的取代基的苯基： （1'）卤素，（2'），C 1-4烷氧基-C 1-4烷基，（3'）单-C 烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单 -C 1-4烷基氨基甲酰基-C 1-4烷氧基等; R 3是C 1-4烷基; R 4是C 1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

公开(公告)号：US20120071486A1

公开(公告)日：2012-03-22

申请号：US13242541

申请日：2011-09-23

申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： A61K31/519 ,  A61P35/04 ,  A61P13/08 ,  A61P15/00 ,  A61P17/10 ,  A61P15/18 ,  A61P25/28 ,  A61P15/08 ,  A61P1/00 ,  A61P15/16 ,  A61P5/24 ,  A61P35/00 ,  A61P17/14

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

摘要翻译： 本发明提供由下式表示的化合物：其中R1是C1-4烷基; R2是（1）可以具有选自（1'）卤素，（2'）羟基，（3'），C 1〜C 6的取代基的5〜7元含氮杂环基， 4烷基和（4'）C 1-4烷氧基，（2）可具有选自（1'）卤素，（2'）C 1-4烷氧基-C 1-4烷基的取代基的苯基 ，（3'）单-C 1-4烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单-C 1-4烷基氨基甲酰基-C 1-4烷氧基等 ; R3是C1-4烷基; R4是C1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

公开(公告)号：US08058280B2

公开(公告)日：2011-11-15

申请号：US11848939

申请日：2007-08-31

申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P5/06

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

摘要翻译： 本发明提供由下式表示的化合物：其中R1是C1-4烷基; R2是（1）可以具有选自（1'）卤素，（2'）羟基，（3'），C 1〜C 6的取代基的5〜7元含氮杂环基， 4烷基和（4'）C 1-4烷氧基，（2）可具有选自（1'）卤素，（2'）C 1-4烷氧基-C 1-4烷基的取代基的苯基 ，（3'）单-C 1-4烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单-C 1-4烷基氨基甲酰基-C 1-4烷氧基等 ; R3是C1-4烷基; R4是C1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

公开(公告)号：US20060160829A1

公开(公告)日：2006-07-20

申请号：US10544069

申请日：2004-01-28

申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  C07D498/02

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

摘要翻译： 本发明提供由下式表示的化合物：其中R 1是C 1-4烷基; R 2是（1）可以具有选自（1'）卤素，（2'）羟基的取代基的5-至7-元含氮杂环基 ，（3'）C 1-4烷基和（4'）C 1-4烷氧基，（2）可以具有选自以下的取代基的苯基： （1'）卤素，（2'），C 1-4烷氧基-C 1-4烷基，（3'）单-C 烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单 -C 1-4烷基氨基甲酰基-C 1-4烷氧基等; R 3是C 1-4烷基; R 4是C 1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

公开(公告)号：US07569570B2

公开(公告)日：2009-08-04

申请号：US10502903

申请日：2003-01-29

申请人： Shuichi Furuya ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Shuichi Furuya ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： A61K31/519 ,  C07D495/04

CPC分类号： C07D495/04

摘要： The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino, or (2) a heterocyclic group optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino and the like, R3 is a hydrogen atom or C1-4 alkyl, R4 is C1-4 alkyl optionally having a substituent such as C1-4 alkoxy-carbonyl, carboxyl, mono C1-4 alkylamino and N—C1-4 alkyl-N—C7-10 aralkylamino and the like] or a salt thereof, which has antagonistic action for gonadotropin-releasing hormone.

摘要翻译： 本发明提供由式[其中，R 1为C 1-4烷基，R 2为（1）任选具有取代基的苯基，例如氨基，单C 1-4烷基氨基和二C 1-4烷基氨基的噻吩并嘧啶化合物或（ 2）任选具有取代基的杂环基，例如氨基，单C 1-4烷基氨基和二C 1-4烷基氨基等，R 3是氢原子或C 1-4烷基，R 4是任选具有取代基的C 1-4烷基 作为对促性腺激素释放激素具有拮抗作用的C 1-4烷氧基 - 羰基，羧基，单C 1-4烷基氨基和N-C 1-4烷基-N C 7-10芳烷基氨基等]或其盐。

公开(公告)号：US20050222174A1

公开(公告)日：2005-10-06

申请号：US10502903

申请日：2003-01-29

申请人： Shuichi Furuya ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

发明人： Shuichi Furuya ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

IPC分类号： A61P5/08 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P17/10 ,  A61P17/14 ,  A61P25/28 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D495/04 ,  A61K31/519 ,  C07D498/02

CPC分类号： C07D495/04

摘要： The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino, or (2) a heterocyclic group optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino and the like, R3 is a hydrogen atom or C1-4 alkyl, R4 is C1-4 alkyl optionally having a substituent such as C1-4 alkoxy-carbonyl, carboxyl, mono C1-4 alkylamino and N—C1-4 alkyl-N—C7-10 aralkylamino and the like] or a salt thereof, which has antagonistic action for gonadotropin-releasing hormone.

摘要翻译： 本发明提供由式[其中R 1为C 1-4烷基，R 2为（1）表示的噻吩并嘧啶化合物为（1 ）任选具有取代基的苯基，例如氨基，单C 1-4烷基氨基和二-C 1-4烷基氨基，或（2）任选具有取代基的杂环基 作为氨基，单C 1-4烷基氨基和二C 1-4烷基氨基等，R 3是氢原子或C < C 1-4烷基，R 4是任选具有取代基的C 1-4烷基，例如C 1-4烷基， 烷氧基羰基，羧基，单C 1-4烷基氨基和NC 1-4烷基-NC 7-10芳烷基氨基等]或 其盐对促性腺激素释放激素具有拮抗作用。

公开(公告)号：US08418932B2

公开(公告)日：2013-04-16

申请号：US12745243

申请日：2008-11-28

申请人： Masaki Seki ,  Kazuhiro Miwa ,  Tomomi Funada ,  Hironari Muramatsu ,  Takaaki Irie ,  Yoshio Morikawa ,  Katsunari Konishi ,  Tetsuya Hanazaki

发明人： Masaki Seki ,  Kazuhiro Miwa ,  Tomomi Funada ,  Hironari Muramatsu ,  Takaaki Irie ,  Yoshio Morikawa ,  Katsunari Konishi ,  Tetsuya Hanazaki

IPC分类号： E01B5/18

CPC分类号： E01B5/18

摘要： A wheel guard apparatus capable of preventing a wheel from derailing and preventing a vehicle from seriously deviating from a track even if the wheel has derailed includes a fixed portion fixed to a railroad tie located between main line rails; a movable portion supported by a rotating shaft provided on the fixed portion and extending in a horizontal direction and configured to be rotatable around the rotating shaft toward a track center side; and a guard rail located at a position separated from the rotating shaft of the movable portion and held to extend in parallel with the main line rail. The guard rail includes an outer stopper portion configured to prevent the wheel from derailing toward an inner side of the main line rail and an inner stopper portion configured to prevent a derailed vehicle from deviating to an outer side of a track.

摘要翻译： 即使车轮脱轨，也能够防止车轮脱轨并防止车辆严重偏离轨道的车轮防护装置包括固定在位于主线轨道之间的铁路连接线的固定部分; 可动部，其由设置在所述固定部上的旋转轴支撑，并且在水平方向上延伸并且能够围绕所述旋转轴向轨道中心侧旋转; 以及位于与可动部的旋转轴分离的位置并与主线轨道平行地延伸的保护轨道。 保护轨包括：外止动部，其构造成防止车轮朝向主线轨道的内侧脱轨;以及内止挡部，其构造成防止脱轨车辆偏离轨道的外侧。

公开(公告)号：US20100216788A1

公开(公告)日：2010-08-26

申请号：US12095543

申请日：2006-12-01

申请人： Tomoyasu Ishikawa ,  Kazuhiro Miwa ,  Masaki Seto ,  Hiroshi Banno ,  Youichi Kawakita

发明人： Tomoyasu Ishikawa ,  Kazuhiro Miwa ,  Masaki Seto ,  Hiroshi Banno ,  Youichi Kawakita

IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/519 ,  C07D413/14 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The present invention provides a compound represented by the formula: wherein R1a is a hydrogen atom, R2a is a C1-6 alkyl group substituted by a group represented by —NR6a—CO—(CH2)n—SO2— optionally halogenated C1-4 alkyl wherein n is an integer of 1 to 4, R6a is a hydrogen atom or a C1-4 alkyl group, and —(CH2)n— is optionally substituted by C1-4 alkyl, R3a is a hydrogen atom or a C1-6 alkyl group, R4a is a halogen atom or a C1-6 alkyl group, R5a is a halogen atom or a C1-6 alkyl group, and Xa is a hydrogen atom or a halogen atom, or a salt thereof. The compound of the present invention has a superior tyrosine kinase inhibitory action, is highly safe, and is sufficiently satisfactory as a pharmaceutical product.

摘要翻译： 本发明提供由下式表示的化合物：其中R1a是氢原子，R2a是被-NR6a-CO-（CH2）n-SO2-代表的基团取代的C1-6烷基，任选被卤代的C 1-4烷基 其中n为1〜4的整数，R6a为氢原子或C1-4烷基， - （CH2）n-为C1-4烷基，R3a为氢原子或C1-6烷基 基团，R 4a是卤素原子或C 1-6烷基，R 5a是卤素原子或C 1-6烷基，X a是氢原子或卤素原子或其盐。 本发明的化合物具有优异的酪氨酸激酶抑制作用，是高度安全的，并且作为药物产品足够令人满意。