公开(公告)号：US20210284653A1

公开(公告)日：2021-09-16

申请号：US17126581

申请日：2020-12-18

申请人： Neurocrine Biosciences, Inc.

发明人： Graham BEATON ,  Mi CHEN ,  Timothy Richard COON ,  Todd EWING ,  Wanlong JIANG ,  Willy MOREE ,  Martin ROWBOTTOM ,  Warren WADE ,  Liren ZHAO ,  Richard LOWE ,  Nicole SMITH ,  Neil ASHWEEK ,  Yun-Fei ZHU

IPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D239/36 ,  C07D213/58

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

公开(公告)号：US20200095259A1

公开(公告)日：2020-03-26

申请号：US16460781

申请日：2019-07-02

申请人： Neurocrine Biosciences, Inc.

发明人： Graham BEATON ,  Mi CHEN ,  Timothy Richard COON ,  Todd EWING ,  Wanlong JIANG ,  Willy MOREE ,  Martin ROWBOTTOM ,  Warren WADE ,  Liren ZHAO ,  Richard LOWE ,  Nicole SMITH ,  Neil ASHWEEK ,  Yun-Fei ZHU

IPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D239/36 ,  C07D213/58

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.