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1. 发明专利

JP2014196365A （ヒドロキシアルキル）ピロール誘導体のアトロプ異性体有权
标题翻译：（羟基烷基）吡咯烷酮衍生物的ATROPISOMER
公开(公告)号：JP2014196365A
公开(公告)日：2014-10-16
申请号：JP2014148858
申请日：2014-07-22
申请人：エグゼリクシス, インコーポレイテッド , Exelixis Inc , エグゼリクシス, インコーポレイテッド , 第一三共株式会社 , Daiichi Sankyo Co Ltd
发明人： JOHN NUSS , MATTHEW WILLIAMS , MOHAN RAJU , MARTIN RICHARD , WANG TIE-LIN , AOKI KAZUMA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , HONMA TAKESHI
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P43/00
CPC分类号： C07D207/34
摘要：【課題】(ヒドロキシアルキル)ピロール誘導体のアトロプ異性体の提供。【解決手段】本願発明は、心血管疾患の予防および/または治療のための化合物から成る。該化合物は、以下の一般式(I)によって表される、化合物のアトロプ異性体である。式中、R1は、C1−C3アルキル基を表し、R2は、2−ヒドロキシ−C4−C6アルキル基を表し、R3は、ハロゲノ基、ハロゲノ−C1−C3アルキル基等を表し、R4は、水素原子、ハロゲノ基等を表し、R5は、C1−C3アルキル基を表し、R6は、水素原子、ハロゲノ基等、またはそのアトロプ異性体を表す。【選択図】なし
摘要翻译：要解决的问题：提供（羟烷基）吡咯衍生物的阻转异构体。解决方案：本发明由用于预防和/或治疗心血管疾病的化合物组成。该化合物是由以下通式（I）表示的化合物的阻转异构体。在该式中，R 1表示C 1 -C 3烷基; R表示2-羟基-C 4 -C 6烷基; R代表卤代基，卤代-C 1 -C 3烷基等; R表示氢原子，卤代基等; 表示C1-C3烷基; 并且R表示氢原子，卤代基等或它们的阻转异构体。

2. 发明专利

JP2014101287A Indole derivative 审中-公开
标题翻译： INDOLE DERIVATIVE
公开(公告)号：JP2014101287A
公开(公告)日：2014-06-05
申请号：JP2012252499
申请日：2012-11-16
申请人： Daiichi Sankyo Co Ltd , 第一三共株式会社
发明人： NARAYAN KARANJULE , HAYASHI NORIYUKI , TSUDA SATOSHI , SHINOZUKA TAKESHI
IPC分类号： C07D209/42 , A61K31/404 , A61K31/4439 , A61P3/10 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/22 , A61P43/00 , C07D401/04
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic drug and/or prophylactic drug for pains or a therapeutic drug and/or prophylactic drug for diseases mediated by sodium channels.SOLUTION: The provided compound is expressed by the formula (I): [Ar denotes a heteroaryl group or aryl group; Rdenotes a C1-C6 alkyl group, halogenated C1-C6 alkyl group, C1-C6 alkoxy-C1-C6 alkyl group, or C3-C7 cycloalkyl group; Rand Rare mutually independent and each denote a hydrogen atom, halogen atom, C1-C6 alkyl group, halogenated C1-C6 alkyl group, C1-C6 alkoxy-C1-C6 alkyl group, or C3-C7 cycloalkyl group; in the above, the heteroaryl group and aryl group may each possess one or two groups selected independently from among halogen atoms, C1-C6 alkyl groups, halogenated C1-C6 alkyl groups, hydroxyl group, C1-C6 alkoxy-C1-C6 alkyl groups, C3-C7 cycloalkyl groups, carboxyl group, cyano group, and amino group, and in a case where the number is 2, the respective groups may be mutually identical or different].
摘要翻译：要解决的问题：提供治疗药物和/或预防药物用于由钠通道介导的疾病的疼痛或治疗药物和/或预防药物。解决方案：所提供的化合物由式（I）表示：[Ar表示杂芳基或芳基; R表示C1-C6烷基，卤代C1-C6烷基，C1-C6烷氧基-C1-C6烷基或C3-C7环烷基; Rare相互独立，分别表示氢原子，卤素原子，C1-C6烷基，卤代C1-C6烷基，C1-C6烷氧基-C1-C6烷基或C3-C7环烷基; 在上述中，杂芳基和芳基各自可具有独立地选自卤素原子，C 1 -C 6烷基，卤代C 1 -C 6烷基，羟基，C 1 -C 6烷氧基-C 1 -C 6烷基中的一个或两个基团，C 3 -C 7环烷基，羧基，氰基和氨基，在数为2的情况下，各基团可以相同或不同]。

3. 发明专利

JP2010111657A Pharmaceutical containing atropisomer of pyrrole derivative 审中-公开
标题翻译：含吡啶衍生物的药物包含ATROPISOMER
公开(公告)号：JP2010111657A
公开(公告)日：2010-05-20
申请号：JP2009231148
申请日：2009-10-05
申请人： Daiichi Sankyo Co Ltd , 第一三共株式会社
发明人： AOKI KAZUMA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , YOSHIDA JURI , ASAO YUSUKE
IPC分类号： A61K31/40 , A61P5/42 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P43/00 , C07D207/416
摘要： PROBLEM TO BE SOLVED: To provide a prophylactic or curative agent for circulatory diseases.
SOLUTION: The pharmaceutical contains the atropisomer(s) of a compound represented by general formula (I) (wherein R
1 is 1-3C alkyl or hydroxy 1-3C alkyl; and R
2 is H or 1-3C alkoxy). One of the atropisomers is excellent in mineralocorticoid receptor antagonism (in vitro activity and in-vivo activity) and medicinal sustainability, and also has excellent properties in solubility, oral peroral absorbability, blood levels, metabolism stability, safety, etc.; as a pharmaceutical, preferably, diseases including hypertension, angina pectoris, acute crown syndrome, congestive heart failure, nephropathy, arteriosclerosis, cerebral infarction, fibrosis, primary hyperaldosteronism and cardiopathy; more preferably, congestive heart failure, nephropathy and hypertension, etc.; particularly preferably, hypertension. This isomer is useful as a prophylactic or curative agent (especially, curative agent).
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供循环系统疾病的预防或治疗剂。解决方案：药物含有由通式（I）表示的化合物的阻转异构体（其中R 1 SP 1是1-3C烷基或羟基1-3C烷基; R SP > 2 是H或1-3C烷氧基）。其中一个阻转异构体具有优异的盐皮质激素受体拮抗作用（体外活性和体内活性）和药物可持续性，并且在溶解性，口服口服吸收性，血液水平，代谢稳定性，安全性等方面也具有优异的性质。作为药物，优选包括高血压，心绞痛，急性冠状综合征，充血性心力衰竭，肾病，动脉硬化，脑梗塞，纤维化，原发性醛固酮增多症和心脏病的疾病; 更优选充血性心力衰竭，肾病和高血压等; 特别优选高血压。该异构体可用作预防或治疗剂（特别是治疗剂）。版权所有（C）2010，JPO＆INPIT

4. 发明专利

AU2009302371B2 Atropisomers of (hydroxyalkyl) pyrrole derivatives 未知
公开(公告)号：AU2009302371B2
公开(公告)日：2015-02-12
申请号：AU2009302371
申请日：2009-10-07
申请人： DAIICHI SANKYO CO LTD , EXELIXIS INC
发明人： NUSS JOHN , WILLIAMS MATTHEW , MOHAN RAJU , MARTIN RICHARD , WANG TIE-LIN , AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , HOMMA TSUYOSHI
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00
摘要： The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I ) : wherein R

5. 发明专利

CA2736923A1 ATROPISOMERS OF (HYDROXYALKYL) PYRROLE DERIVATIVES 未知
公开(公告)号：CA2736923A1
公开(公告)日：2010-04-15
申请号：CA2736923
申请日：2009-10-07
申请人： EXELIXIS INC , DAIICHI SANKYO CO LTD
发明人： NUSS JOHN , WILLIAMS MATTHEW , MOHAN RAJU , MARTIN RICHARD , WANG TIE-LIN , AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , HOMMA TSUYOSHI
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00
摘要： The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I ) : wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy- C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.

6. 发明专利

CA2736923C ATROPISOMERS OF (HYDROXYALKYL) PYRROLE DERIVATIVES 未知
公开(公告)号：CA2736923C
公开(公告)日：2016-11-22
申请号：CA2736923
申请日：2009-10-07
申请人： EXELIXIS INC , DAIICHI SANKYO CO LTD
发明人： NUSS JOHN , WILLIAMS MATTHEW , MOHAN RAJU , MARTIN RICHARD , WANG TIE-LIN , AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , HOMMA TSUYOSHI
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00
摘要： The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I ) : wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy- C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.

7. 发明专利

ES2547697T3 Atropisómeros de (hidroxialquil)pirrol derivados 未知
公开(公告)号：ES2547697T3
公开(公告)日：2015-10-08
申请号：ES09737501
申请日：2009-10-07
申请人： EXELIXIS INC , DAIICHI SANKYO CO LTD
发明人： NUSS JOHN , WILLIAMS MATTHEW , MOHAN RAJU , MARTIN RICHARD , WANG TIE-LIN , AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , HOMMA TSUYOSHI
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00
摘要： Un antagonista de los receptores de los mineralocorticoides de fórmula general (I):**Fórmula** un N-óxido del mismo; un diastereómero, racemato, o compuesto enriquecido en un diastereómero del mismo; un atropisómero, mezclas iguales de atropisómeros, o un compuesto enriquecido en un atropisómero del mismo; o una sal farmacéuticamente aceptable de cualquiera de los precedentes, donde R1 representa un grupo alquilo de C1-C3; R2 representa un grupo 2-hidroxi-alquilo de C4-C6; R3 representa un grupo halógeno, un grupo alquilo de C1-C3, un grupo alcoxi de C1-C3, un grupo halógeno-alquilo de C1-C3 o un grupo halógeno-alcoxi de C1-C3; R4 representa un átomo de hidrógeno, un grupo halógeno o un grupo alquilo de C1-C3; R5 representa un grupo alquilo de C1-C3; y R6 representa un átomo de hidrógeno, un grupo halógeno, un grupo alquilo de C1-C3 o un grupo alcoxi de C1-C3.

8. 发明专利

AU2009302371A1 Atropisomers of (hydroxyalkyl) pyrrole derivatives 未知
公开(公告)号：AU2009302371A1
公开(公告)日：2010-04-15
申请号：AU2009302371
申请日：2009-10-07
申请人： EXELIXIS INC , DAIICHI SANKYO CO LTD
发明人： NUSS JOHN , WILLIAMS MATTHEW , MOHAN RAJU , MARTIN RICHARD , WANG TIE-LIN , AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , HOMMA TSUYOSHI
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00
摘要： The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy-C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.

9. 发明专利

CA2683059C ATROPISOMER OF PYRROLE DERIVATIVE 未知
公开(公告)号：CA2683059C
公开(公告)日：2012-09-25
申请号：CA2683059
申请日：2008-04-08
申请人： DAIICHI SANKYO CO LTD
发明人： AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , YOSHIDA JURI , ASOH YUSUKE
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P43/00
摘要： [Object] A prophylactic or therapeutic agent for a cardiovascular disease is provided. [Means for Resolution] An atropisomer of a compound represented by the following general formula (I): (see formula I) (wherein R1 is a C1-C3 alkyl group or a hydroxy-C1-C3 alkyl group; and R2 is a hydrogen atom or a C1-C3 alkoxy group).

10. 发明专利

BRPI0809656A2 未知
公开(公告)号：BRPI0809656A2
公开(公告)日：2014-10-07
申请号：BRPI0809656
申请日：2008-04-08
申请人： DAIICHI SANKYO CO LTD
发明人： AOKI KAZUMASA , TSURUOKA HIROYUKI , HAYASHI NORIYUKI , YOSHIDA JURI , ASOH YUSUKE
IPC分类号： C07D207/34 , A61K31/40 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P43/00
摘要： [Object] A prophylactic or therapeutic agent for a cardiovascular disease is provided. [Means for Resolution] An atropisomer of a compound represented by the following general formula (I): (wherein R 1 is a C1-C3 alkyl group or a hydroxy-C1-C3 alkyl group; and R 2 is a hydrogen atom or a C1-C3 alkoxy group).

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