公开(公告)号：US08470829B2

公开(公告)日：2013-06-25

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： A61K31/426 ,  A61K31/454 ,  A61K31/428 ,  A61K31/4166 ,  C07D401/12 ,  C07D403/12 ,  C07D277/82 ,  C07D233/72 ,  C07D233/70

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

摘要： An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted C1-4 alkyl group; E is independently selected from a C1-6 alkyl group; R2 and R3 are independently selected from C1-6 alkyls; X1 and X2 are independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is —CON(—Ra)—, —CO—, —OOO—, —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, or substituted or unsubstituted group selected from C1-6 alkyl group, heterocyclic group, aryl group, C3-8 cycloalkyl group and C3-8 cycloalkenyl group; or salt or prodrug thereof.

摘要翻译： 由式（I）表示的咪唑衍生物：其中Q是：A是氢，卤素或取代或未取代的C1-4烷基; E独立地选自C 1-6烷基; R2和R3独立地选自C1-6烷基; X1和X2独立地选自O和S; Y选自取代或未取代的亚芳基和取代或未取代的二价5元或6元单环或8至10元稠合杂环基; Z是-CON（-R a） - ， - CO - ， - OO-，-NR a -C（= NH）NR b - ， - NR a -C（= N-CN）NR b - ， - N（-R a） ，-C（= NH） - ， - SO 2 - ， - SO 2 N（-R a） - ， - SO 2 NR 1 - ， - N（-R a）CO - ， - N（-R a）CON（-R b） COR 1）CO - ， - N（-R a）SO 2 - ， - N（SO 2 R 1）SO 2 - ， - N（-R a） - 或-N（-R a）SO 2 N（-R b） R 1独立地为氢原子，羟基或取代或未取代的选自C 1-6烷基，杂环基，芳基，C 3-8环烷基和C 3-8环烯基的基团; 或其盐或前药。

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：US08173824B2

公开(公告)日：2012-05-08

申请号：US12095918

申请日：2006-12-04

申请人： Kunio Ogasawara ,  Takashi Emura ,  Akira Kawase ,  Koji Takano ,  Keisuke Yamamoto ,  Yoshiaki Kato

发明人： Kunio Ogasawara ,  Takashi Emura ,  Akira Kawase ,  Koji Takano ,  Keisuke Yamamoto ,  Yoshiaki Kato

IPC分类号： C07C401/00 ,  C07C35/00 ,  C07C233/00

CPC分类号： C07C33/44 ,  C07C235/06 ,  C07C401/00 ,  C07C2602/24 ,  C07D301/26 ,  C07D303/08

摘要： There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is shown in the following reaction scheme: an intermediate useful for carrying out the process, and a process for producing the intermediate.

摘要翻译： 提供了一种制备[{（5Z，7E） - （1S，3R，20S）-1,3-二羟基-9,10-断孕甾-5,7,10（19），16-四烯-20 - 基}氧基] -N-（2,2,3,3,3-五氟丙基）乙酰胺，该方法显示在以下反应方案中：可用于实施该方法的中间体及其制备方法。

公开(公告)号：US6127544A

公开(公告)日：2000-10-03

申请号：US182491

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): 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：US06114536A

公开(公告)日：2000-09-05

申请号：US182463

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.

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：US07985744B2

公开(公告)日：2011-07-26

申请号：US10311538

申请日：2001-06-14

申请人： Kazumi Morikawa ,  Masayuki Ohmori ,  Kazuki Shimizu ,  Akira Kawase ,  Takashi Emura

发明人： Kazumi Morikawa ,  Masayuki Ohmori ,  Kazuki Shimizu ,  Akira Kawase ,  Takashi Emura

IPC分类号： A61K31/59 ,  C07C401/00

CPC分类号： C07D295/185 ,  A61K31/592 ,  A61K31/593 ,  C07C235/06 ,  C07C401/00 ,  C07C2601/14 ,  C07C2602/24 ,  C07F7/1804 ,  C07J7/00 ,  C07J9/00 ,  Y02P20/55

摘要： The object of the present invention is to provide vitamin D derivatives that have excellent physiological activities as medicines, particularly as therapeutic agents for skin diseases such as psoriasis, and that have a reduced hypercalcemic effect.The present invention provides a vitamin D derivative of Formula (1): wherein X represents an oxygen atom or a sulfur atom; m represents a number of 1 to 3; R1 and R2 each represent a hydrogen atom or an alkyl group; R4 and R5 each represent a hydrogen atom or a hydroxyl group, etc.; R3 represents —YR8, etc.; R6 represents a hydrogen atom, etc.; R7 represents a hydrogen atom, etc.

摘要翻译： 本发明的目的是提供作为药物具有优异的生理活性的维生素D衍生物，特别是作为皮肤病如银屑病的治疗剂，具有降低的高钙血症效果。 本发明提供式（1）的维生素D衍生物：其中X表示氧原子或硫原子; m表示1〜3的数; R1和R2各自表示氢原子或烷基; R4和R5各自表示氢原子或羟基等; R3表示-YR8等; R6代表氢原子等; R7表示氢原子等

公开(公告)号：US06960689B2

公开(公告)日：2005-11-01

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 ,  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.

公开(公告)号：US20050049421A1

公开(公告)日：2005-03-03

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

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：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：US09126931B2

公开(公告)日：2015-09-08

申请号：US13377300

申请日：2010-06-09

申请人： Kazutomo Kinoshita ,  Kohsuke Asoh ,  Noriyuki Furuichi ,  Toshiya Ito ,  Hatsuo Kawada ,  Nobuya Ishii ,  Hiroshi Sakamoto ,  WooSang Hong ,  MinJeong Park ,  Yoshiyuki Ono ,  Yasuharu Kato ,  Kenji Morikami ,  Takashi Emura ,  Nobuhiro Oikawa

发明人： Kazutomo Kinoshita ,  Kohsuke Asoh ,  Noriyuki Furuichi ,  Toshiya Ito ,  Hatsuo Kawada ,  Nobuya Ishii ,  Hiroshi Sakamoto ,  WooSang Hong ,  MinJeong Park ,  Yoshiyuki Ono ,  Yasuharu Kato ,  Kenji Morikami ,  Takashi Emura ,  Nobuhiro Oikawa

IPC分类号： C07D207/30 ,  C07D209/80 ,  C07D333/50 ,  C07D307/77 ,  C07D209/56 ,  C07D209/88 ,  C07D307/92 ,  C07D333/76 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D491/107

CPC分类号： C07D209/58 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/7056 ,  C07D209/56 ,  C07D209/88 ,  C07D307/77 ,  C07D307/78 ,  C07D307/92 ,  C07D333/50 ,  C07D333/52 ,  C07D333/76 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07F7/0834 ,  C07H15/26

摘要： A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

摘要翻译： 由下述通式（I）表示的化合物或其盐或溶剂化物，其可用作ALK抑制剂，并且可用于预防或治疗伴有ALK异常的疾病，例如癌症，癌症转移 ，抑郁症或认知功能障碍（包括在公式中的符号的含义如说明书中所给出）。