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：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：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：US07141598B2

公开(公告)日：2006-11-28

申请号：US10416986

申请日：2001-11-16

申请人： Akihiro Tasaka ,  Takenori Hitaka ,  Nobuyuki Matsunaga ,  Masami Kusaka

发明人： Akihiro Tasaka ,  Takenori Hitaka ,  Nobuyuki Matsunaga ,  Masami Kusaka

IPC分类号： A61K31/4184 ,  C07D235/02

CPC分类号： C07D233/64 ,  C07D471/04 ,  C07D487/04

摘要： The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula: wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.

摘要翻译： 本发明提供了具有类固醇C 17,20 - 酶抑制活性并可用于治疗和预防诸如前列腺症，乳腺癌等肿瘤的化合物和有效分离的方法 该化合物的旋光异构体的混合物的光学活性化合物，下式的化合物：其中每个符号如说明书中所定义，其盐或其前药，以及通过光学获得光学活性化合物的方法 通过使用诸如格列硝酸等拆分剂来拆分光学异构体的混合物。

公开(公告)号：US08883788B2

公开(公告)日：2014-11-11

申请号：US13814035

申请日：2011-08-03

申请人： Tomoaki Hasui ,  Makoto Fushimi ,  Hironori Kokubo ,  Takenori Hitaka ,  Shotaro Miura ,  Takahiko Taniguchi

发明人： Tomoaki Hasui ,  Makoto Fushimi ,  Hironori Kokubo ,  Takenori Hitaka ,  Shotaro Miura ,  Takahiko Taniguchi

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D403/14 ,  C07D401/12 ,  C07D471/04 ,  A61K9/20 ,  C07D487/04 ,  C07D401/14 ,  A61K31/00

CPC分类号： C07D403/14 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04

摘要： Provided is a compound having a PDE10A inhibitory action, and useful as a medicament for the prophylaxis or treatment of mental diseases such as schizophrenia and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.

摘要翻译： 提供具有PDE10A抑制作用的化合物，可用作预防或治疗精神疾病如精神分裂症等的药物等。 由式（I）表示的化合物或其盐，其中每个符号如说明书中所定义。