公开(公告)号：US09676713B2

公开(公告)日：2017-06-13

申请号：US15352407

申请日：2016-11-15

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

公开(公告)号：US20170233341A1

公开(公告)日：2017-08-17

申请号：US15582064

申请日：2017-04-28

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

公开(公告)号：US20160096803A1

公开(公告)日：2016-04-07

申请号：US14879814

申请日：2015-10-09

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

摘要翻译： 本发明提供具有优异的盐皮质激素受体拮抗作用的吡咯衍生物的阻转异构体的制造中间体及其制造方法及其结晶。 一种制备吡咯衍生物的阻转异构体的方法，包括拆分由下列通式（I）表示的化合物的步骤[其中R1表示甲基或三氟甲基，R2表示氢原子或C1-C3烷氧基 ，并且n表示1至3的整数]转化成其阻转异构体，其特征在于使用具有辛可宁骨架配方的光学活性胺和（S）-1-（2-羟乙基）-4-甲基-N - [4-（甲基磺酰基）苯基] -5- [2-（三氟甲基）苯基] -1H-吡咯-3-甲酰胺。

公开(公告)号：US09776961B2

公开(公告)日：2017-10-03

申请号：US15582064

申请日：2017-04-28

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

公开(公告)号：US20170057915A1

公开(公告)日：2017-03-02

申请号：US15352407

申请日：2016-11-15

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

摘要翻译： 本发明提供具有优异的盐皮质激素受体拮抗作用的吡咯衍生物的阻转异构体的制造中间体及其制造方法及其结晶。 一种制备吡咯衍生物的阻转异构体的方法，其包括以下通式（I）表示的化合物的拆分步骤[其中R 1表示甲基或三氟甲基，R 2表示氢原子或C1-C3 烷氧基，n表示1〜3的整数]转变为其阻转异构体，其特征在于使用具有辛可宁骨架配方的光学活性胺和（S）-1-（2-羟乙基）-4-甲基 -N- [4-（甲基磺酰基）苯基] -5- [2-（三氟甲基）苯基] -1H-吡咯-3-甲酰胺。

公开(公告)号：US09499483B2

公开(公告)日：2016-11-22

申请号：US14879814

申请日：2015-10-09

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C07D471/08

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

摘要翻译： 本发明提供具有优异的盐皮质激素受体拮抗作用的吡咯衍生物的阻转异构体的制造中间体及其制造方法及其结晶。 一种制备吡咯衍生物的阻转异构体的方法，其包括以下通式（I）表示的化合物的拆分步骤[其中R 1表示甲基或三氟甲基，R 2表示氢原子或C1-C3 烷氧基，n表示1〜3的整数]转变为其阻转异构体，其特征在于使用具有辛可宁骨架配方的光学活性胺和（S）-1-（2-羟乙基）-4-甲基 -N- [4-（甲基磺酰基）苯基] -5- [2-（三氟甲基）苯基] -1H-吡咯-3-甲酰胺。