公开(公告)号：US20050043569A1

公开(公告)日：2005-02-24

申请号：US10956040

申请日：2004-10-04

申请人： Takashi Emura ,  Tsuyoshi Haneishi

发明人： Takashi Emura ,  Tsuyoshi Haneishi

IPC分类号： C07C231/02 ,  C07C233/07 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C279/18 ,  C07C335/32 ,  C07C257/02

CPC分类号： C07C335/32 ,  C07C231/02 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C233/07 ,  C07C279/18

摘要： A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

公开(公告)号：US20100234609A1

公开(公告)日：2010-09-16

申请号：US12375378

申请日：2007-07-27

申请人： Tsutomu Sato ,  Yoshihito Ohtake ,  Masahiro Nishimoto ,  Takashi Emura ,  Takamitsu Kobayashi ,  Marina Yamaguchi ,  Kyouko Takami

发明人： Tsutomu Sato ,  Yoshihito Ohtake ,  Masahiro Nishimoto ,  Takashi Emura ,  Takamitsu Kobayashi ,  Marina Yamaguchi ,  Kyouko Takami

IPC分类号： C07D493/10 ,  C07D513/20 ,  C07D498/20 ,  C07D491/20 ,  C07F7/08 ,  C07D495/20

CPC分类号： C07H19/01

摘要： Provided are a compound represented by Formula (I): wherein R1, R2, R3, and R4 are each independently selected from a hydrogen atom, a C1-6 alkyl group which may be substituted, a C7-14 aralkyl group which may be substituted and —C(═O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f). or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.

摘要翻译： 提供由式（I）表示的化合物：其中R 1，R 2，R 3和R 4各自独立地选自氢原子，可被取代的C 1-6烷基，可被取代的C 7-14芳烷基 和-C（= O）Rx; n表示选自1和2的整数; 并且环Ar选自由下式（a）至（f）表示的基团。 或其前药或其药学上可接受的盐，以及药物和含有这种化合物或其前药的药物组合物或其药学上可接受的盐。

公开(公告)号：US07087783B2

公开(公告)日：2006-08-08

申请号：US10956040

申请日：2004-10-04

申请人： Takashi Emura ,  Tsuyoshi Haneishi

发明人： Takashi Emura ,  Tsuyoshi Haneishi

IPC分类号： C07C231/02 ,  C07C277/02 ,  C07C257/10 ,  C07C335/30 ,  C07C335/32

CPC分类号： C07C335/32 ,  C07C231/02 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C233/07 ,  C07C279/18

摘要： A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitriles or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

摘要翻译： 一种合成方法，其包括在甲硅烷基化剂存在下使含NH基的化合物与硫氰酸酯，氰胺，腈或酯反应以合成相应的含氮添加或取代产物。 该方法不仅可以直接有效地合成含氮化合物，包括异硫脲，胍，脒和酰胺，而且还具有广泛的应用范围，适用于大规模合成。

公开(公告)号：US06946576B2

公开(公告)日：2005-09-20

申请号：US10957603

申请日：2004-10-05

申请人： Takashi Emura ,  Tsuyoshi Haneishi

发明人： Takashi Emura ,  Tsuyoshi Haneishi

IPC分类号： C07C231/02 ,  C07C233/07 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C279/18 ,  C07C335/32 ,  C07C257/10 ,  C07C335/30

CPC分类号： C07C335/32 ,  C07C231/02 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C233/07 ,  C07C279/18

摘要： A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

摘要翻译： 一种合成方法，其包括在甲硅烷基化剂存在下使含NH基的化合物与硫氰酸酯，氰胺，亚硝酸酯或酯反应以合成相应的含氮加成或取代产物。 该方法不仅可以直接有效地合成含氮化合物，包括异硫脲，胍，脒和酰胺，而且还具有广泛的应用范围，适用于大规模合成。

公开(公告)号：US20050075513A1

公开(公告)日：2005-04-07

申请号：US10954605

申请日：2004-10-01

申请人： Takashi Emura ,  Tsuyoshi Haneishi

发明人： Takashi Emura ,  Tsuyoshi Haneishi

IPC分类号： C07C231/02 ,  C07C233/07 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C279/18 ,  C07C335/32

CPC分类号： C07C335/32 ,  C07C231/02 ,  C07C257/14 ,  C07C257/18 ,  C07C277/02 ,  C07C233/07 ,  C07C279/18

摘要： A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

公开(公告)号：US06207836B1

公开(公告)日：2001-03-27

申请号：US09182490

申请日：1998-10-30

申请人： Toru Esaki ,  Takashi Emura ,  Eiichi Hoshino

发明人： Toru Esaki ,  Takashi Emura ,  Eiichi Hoshino

IPC分类号： C07D40112

CPC分类号： C07D405/12 ,  C07D209/34 ,  C07D209/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06

摘要： A compound represented by formula (I): wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, —OR5, —SR5 or —NR6R7 (wherein R5, R6, and R7 each represent a lower alkyl group, etc.); X and Y each represent —CH2—, —NH— or —O—; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

摘要翻译： 由式（I）表示的化合物：其中R1表示卤素原子，低级烷基，低级烷氧基，羟基，硝基，三氟甲基，低级烷硫基，酰基，羧基 ，巯基或氨基; R2表示氢原子，低级烷基，低级烯基，低级炔基，烷氧基，酰基，芳基或杂环基; R3表示低级烷基，环烷基，芳基或杂环基; R4表示氢原子，低级烷基，芳基，杂环基，-OR5，-SR5或-NR6R7（其中R5，R6和R7各自表示低级烷基等）; X和Y各自表示-CH 2 - ， - NH-或-O-; 并且n表示0至4的整数，并且公开了其合成中间体。 本发明化合物对胃泌素受体表现出选择性拮抗作用，而不引起归因于CCK-A受体拮抗作用的副作用，并且可用于治疗和预防消化性溃疡，胃炎，反流性食管炎和佐林格 - 埃里森综合征，并用于治疗 的起源于胃肠系统的肿瘤。

公开(公告)号：US5952511A

公开(公告)日：1999-09-14

申请号：US963547

申请日：1997-11-03

申请人： Toru Esaki ,  Takashi Emura ,  Eiichi Hoshino

发明人： Toru Esaki ,  Takashi Emura ,  Eiichi Hoshino

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P25/00 ,  A61P25/18 ,  A61P43/00 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D209/42 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12

CPC分类号： C07D405/12 ,  C07D209/34 ,  C07D209/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06

摘要： A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

公开(公告)号：US20110306615A1

公开(公告)日：2011-12-15

申请号：US11662289

申请日：2005-09-09

申请人： Kazutaka Tachibana ,  Haruhiko Sato ,  Masateru Ohta ,  Mitsuaki Nakamura ,  Takuya Shiraishi ,  Hitoshi Yoshino ,  Takashi Emura ,  Akie Honma ,  Etsuro Onuma ,  Hiromitsu Kawata ,  Kenji Taniguchi

发明人： Kazutaka Tachibana ,  Haruhiko Sato ,  Masateru Ohta ,  Mitsuaki Nakamura ,  Takuya Shiraishi ,  Hitoshi Yoshino ,  Takashi Emura ,  Akie Honma ,  Etsuro Onuma ,  Hiromitsu Kawata ,  Kenji Taniguchi

IPC分类号： A61K31/454 ,  C07D233/74 ,  C07D417/10 ,  C07D403/12 ,  C07D233/86 ,  C07D413/12 ,  A61K31/4166 ,  A61K31/428 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/5377 ,  A61P35/00 ,  A61P13/08 ,  A61Q7/00 ,  A61P15/00 ,  A61P17/10 ,  C07D401/04

CPC分类号： C07D417/04 ,  C07D211/58 ,  C07D233/74 ,  C07D233/86 ,  C07D277/82 ,  C07D401/04

摘要： According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)sulfamoyl group; Z is —CON(—Ra)—, —CO—, —COO—, —NRa—C(═NH)NRb—, —NRa—C(═N—CN)NRb—, —N(—Ra)COO—, —C(═NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, a C1-6 alkyl group which may be substituted by one or more substituents, a heterocyclic group which may be substituted by one or more substituents, an aryl group which may be substituted by one or more substituents, a C3-8 cycloalkyl group which may be substituted by one or more substituents or a C3-8 cycloalkenyl group which may be substituted by one or more substituents, or a salt, prodrug or solvate thereof is provided. Furthermore, a pharmaceutical composition containing the compound, and the like are also provided.

公开(公告)号：US6031111A

公开(公告)日：2000-02-29

申请号：US182638

申请日：1998-10-30

申请人： Toru Esaki ,  Takashi Emura ,  Eiichi Hoshino

发明人： Toru Esaki ,  Takashi Emura ,  Eiichi Hoshino

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P25/00 ,  A61P25/18 ,  A61P43/00 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D209/42 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12

CPC分类号： C07D405/12 ,  C07D209/34 ,  C07D209/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06

摘要： A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

公开(公告)号：US08207134B2

公开(公告)日：2012-06-26

申请号：US12375378

申请日：2007-07-27

申请人： Tsutomu Sato ,  Yoshihito Ohtake ,  Masahiro Nishimoto ,  Takashi Emura ,  Takamitsu Kobayashi ,  Marina Yamaguchi ,  Kyouko Takami

发明人： Tsutomu Sato ,  Yoshihito Ohtake ,  Masahiro Nishimoto ,  Takashi Emura ,  Takamitsu Kobayashi ,  Marina Yamaguchi ,  Kyouko Takami

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H1/00 ,  C07H3/00 ,  C08B37/00

CPC分类号： C07H19/01

摘要： Provided are a compound represented by Formula (I): wherein R1, R2, R3, and R4 are each independently selected from a hydrogen atom, a C1-6 alkyl group which may be substituted, a C7-14 aralkyl group which may be substituted and —C(═O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f). or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.

摘要翻译： 提供由式（I）表示的化合物：其中R 1，R 2，R 3和R 4各自独立地选自氢原子，可被取代的C 1-6烷基，可被取代的C 7-14芳烷基 和-C（= O）Rx; n表示选自1和2的整数; 并且环Ar选自由下式（a）至（f）表示的基团。 或其前药或其药学上可接受的盐，以及药物和含有这种化合物或其前药的药物组合物或其药学上可接受的盐。