公开(公告)号：US20210053939A1

公开(公告)日：2021-02-25

申请号：US16929230

申请日：2020-07-15

申请人： MyoKardia, Inc.

发明人： Min Zhong ,  Olivier Monnier ,  Jean-Philippe Jelin ,  Richard Duvoux ,  Jean Alié ,  Philippe Ochsenbein

IPC分类号： C07D401/12

摘要： The present invention provides novel polymorphs of (R)-4-(1-(3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-N-(isoxazol-3-yl)piperidine-1-carboxamide (I-491) that are useful for the treatment of cardiac disorders including systolic dysfunction, dilated cardiomyopathy (DCM), heart failure with reserved ejection fraction (HFrEF), and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the polymorphs is described, as well as methods for treating systolic dysfunction, DCM, HFrEF, and other forms of heart disease.

公开(公告)号：US09925177B2

公开(公告)日：2018-03-27

申请号：US15003662

申请日：2016-01-21

申请人： MyoKardia, Inc.

发明人： Johan Oslob ,  Danielle Aubele ,  Jae Kim ,  Robert McDowell ,  Yonghong Song ,  Arvinder Sran ,  Min Zhong

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/454 ,  C07D401/02 ,  C07D407/02 ,  C07D407/14 ,  C07D409/02 ,  C07D411/14 ,  A61K31/496 ,  A61K31/506 ,  A61K45/06

CPC分类号： A61K31/4545 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D401/02 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/02 ,  C07D407/14 ,  C07D409/02 ,  C07D411/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

摘要： The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

公开(公告)号：US20220289709A1

公开(公告)日：2022-09-15

申请号：US17678569

申请日：2022-02-23

申请人： MyoKardia, Inc.

发明人： Min Zhong ,  Olivier Monnier ,  Jean-Philippe Jelin ,  Richard Duvoux ,  Jean Alie ,  Philippe Ochsenbein

IPC分类号： C07D401/12

摘要： The present invention provides novel polymorphs of (R)-4-(1-((3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-N-(isoxazol-3-yl)piperidine-1-carboxamide (I-491) that are useful for the treatment of cardiac disorders including systolic dysfunction, dilated cardiomyopathy (DCM), heart failure with reserved ejection fraction (HFrEF), and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the polymorphs is described, as well as methods for treating systolic dysfunction, DCM, HFrEF, and other forms of heart disease.

公开(公告)号：US20220106314A1

公开(公告)日：2022-04-07

申请号：US17554353

申请日：2021-12-17

申请人： MYOKARDIA, INC.

发明人： Mark Grillo ,  Brian Kane ,  Johan Oslob ,  Min Zhong ,  Fabienne Thompson

IPC分类号： C07D471/04

摘要： The present disclosure provides novel tetrahydropyran (THP)-substituted bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM), conditions associated with left ventricular hypertrophy, conditions associated with diastolic dysfunction, and/or symptoms associated thereof. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

公开(公告)号：US09663516B2

公开(公告)日：2017-05-30

申请号：US14973132

申请日：2015-12-17

申请人： MyoKardia, Inc.

发明人： Johan Oslob ,  Danielle Aubele ,  Marc Evanchik ,  Jonathan Charles Fox ,  Mark Grillo ,  Brian Kane ,  Robert McDowell ,  Yonghong Song ,  Min Zhong

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/55 ,  A61K45/06

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04

摘要： The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

公开(公告)号：US20220117955A1

公开(公告)日：2022-04-21

申请号：US17407545

申请日：2021-08-20

申请人： MYOKARDIA, INC.

发明人： Johan Oslob ,  Danielle Aubele ,  Jae Kim ,  Robert McDowell ,  Yonghong Song ,  Arvinder Sran ,  Min Zhong

IPC分类号： A61K31/4545 ,  A61K31/454 ,  C07D401/14 ,  A61K31/496 ,  A61K31/506 ,  C07D413/14 ,  C07D417/12 ,  A61K45/06 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D411/14 ,  C07D409/02 ,  C07D407/14 ,  C07D407/02 ,  C07D401/02 ,  A61K31/501

摘要： The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

公开(公告)号：US20200113887A9

公开(公告)日：2020-04-16

申请号：US16149912

申请日：2018-10-02

申请人： MyoKardia, Inc.

发明人： Johan Oslob ,  Danielle Aubele ,  Jae Kim ,  Robert McDowell ,  Yonghong Song ,  Arvinder Sran ,  Min Zhong

IPC分类号： A61K31/4545 ,  A61K31/501 ,  C07D401/14 ,  A61K31/496 ,  A61K31/506 ,  C07D413/14 ,  C07D417/12 ,  A61K45/06 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D411/14 ,  C07D409/02 ,  C07D407/14 ,  C07D407/02 ,  C07D401/02 ,  A61K31/454

摘要： The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

公开(公告)号：US20160243100A1

公开(公告)日：2016-08-25

申请号：US15003662

申请日：2016-01-21

申请人： MyoKardia, Inc.

发明人： Johan Oslob ,  Danielle Aubele ,  Jae Kim ,  Robert McDowell ,  Yonghong Song ,  Arvinder Sran ,  Min Zhong

IPC分类号： A61K31/4545 ,  A61K45/06 ,  C07D401/12 ,  A61K31/501 ,  C07D413/12 ,  A61K31/506 ,  C07D413/14 ,  C07D471/04 ,  C07D417/12 ,  C07D405/14 ,  A61K31/496 ,  C07D401/14 ,  A61K31/454

CPC分类号： A61K31/4545 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D401/02 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/02 ,  C07D407/14 ,  C07D409/02 ,  C07D411/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

摘要： The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

摘要翻译： 本发明提供可用于治疗扩张型心肌病（DCM）的新型4-甲基砜取代的哌啶脲化合物和与左心室收缩功能障碍或/或右心室收缩功能障碍或收缩储备相关的病症。 描述了化合物的合成和表征，以及用于治疗DCM和其它形式的心脏病的方法。

公开(公告)号：US20220340569A1

公开(公告)日：2022-10-27

申请号：US17854398

申请日：2022-06-30

申请人： MYOKARDIA, INC.

发明人： Mark Grillo ,  Brian Kane ,  Johan Oslob ,  Min Zhong ,  Fabienne Thompson

IPC分类号： C07D471/04

摘要： The present disclosure provides novel tetrahydropyran (THP)-substituted bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM), conditions associated with left ventricular hypertrophy, conditions associated with diastolic dysfunction, and/or symptoms associated thereof. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

公开(公告)号：US11123337B2

公开(公告)日：2021-09-21

申请号：US16934463

申请日：2020-07-21

申请人： MYOKARDIA, INC.

发明人： Johan Oslob ,  Danielle Aubele ,  Jae Kim ,  Robert McDowell ,  Yonghong Song ,  Arvinder Sran ,  Min Zhong

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D417/14 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K45/06 ,  C07D405/14 ,  C07D411/14 ,  C07D409/02 ,  C07D407/14 ,  C07D407/02 ,  C07D401/02 ,  A61K31/501

摘要： The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.