公开(公告)号：US11504372B2

公开(公告)日：2022-11-22

申请号：US16879676

申请日：2020-05-20

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Lawrence P. Wennogle

IPC分类号： A61K31/519 ,  A61P25/16 ,  A61P25/14 ,  A61P25/28 ,  A61P25/02 ,  A61K31/527 ,  A61K31/53 ,  A61K31/517 ,  G01N33/84

摘要： The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

公开(公告)号：US20220354851A1

公开(公告)日：2022-11-10

申请号：US17640050

申请日：2020-09-03

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Peng LI ,  Robert DAVIS

IPC分类号： A61K31/519 ,  A61K31/505 ,  A61K38/00 ,  A61P35/00

摘要： The disclosure relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) useful for the treatment of certain cancers or tumors, such as colon cancer. In another embodiment, the disclosure relates to the use of inhibitors of PDE1 and an optional antitumor agent for the treatment of certain cancers or tumors.

公开(公告)号：US20220313692A1

公开(公告)日：2022-10-06

申请号：US17659063

申请日：2022-04-13

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Peng LI

IPC分类号： A61K31/4985 ,  A61K9/20 ,  A61K9/16 ,  A61K9/00 ,  A61K47/38 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/06 ,  A61K9/48

摘要： The disclosure provides new, stable, pharmaceutically acceptable amorphous solid dispersions of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20220008423A1

公开(公告)日：2022-01-13

申请号：US17379399

申请日：2021-07-19

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Wei YAO ,  Peng LI

IPC分类号： A61K31/519 ,  C07D471/14 ,  A61P25/28 ,  A61K31/4985 ,  A61K45/06 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24

摘要： The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

公开(公告)号：US20210379072A1

公开(公告)日：2021-12-09

申请号：US17287478

申请日：2019-10-21

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Robert E. DAVIS ,  Kimberly E. VANOVER

IPC分类号： A61K31/519 ,  A61P25/16

摘要： The disclosure provides methods, treatments and materials for treating diseases or disorders associated with the dopamine D1 receptor intracellular pathway. In particular, the present disclosure provides for methods of treating such diseases and disorders in combination with a dopamine replacement therapy.

公开(公告)号：US20210361648A1

公开(公告)日：2021-11-25

申请号：US17338573

申请日：2021-06-03

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Peng LI ,  Wei YAO ,  Robert DAVIS

IPC分类号： A61K31/4985 ,  A61K9/06 ,  A61K9/00

摘要： The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.

公开(公告)号：US11066407B2

公开(公告)日：2021-07-20

申请号：US16711790

申请日：2019-12-12

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： John Charles Tomesch ,  Peng Li ,  Wei Yao ,  Qiang Zhang ,  James David Beard ,  Andrew S. Thompson ,  Hua Cheng ,  Lawrence P. Wennogle

IPC分类号： C07D471/16 ,  C07D471/04

摘要： The present invention provides methods for the preparation of certain optionally substituted heterocycle fused gamma-carbolines of Formula 2F, as shown below and as further defined herein:

公开(公告)号：US20210205310A1

公开(公告)日：2021-07-08

申请号：US17059160

申请日：2019-05-24

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Lawrence P. WENNOGLE ,  Joseph HENDRICK ,  Robert DAVIS

IPC分类号： A61K31/519 ,  A61P35/00

摘要： The disclosure relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) useful for the treatment of certain cancers or tumors, such as gliomas. In another embodiment, the disclosure relates to the combination of inhibitors of PDE1 and an antitumor agent for the treatment of certain cancers or tumors, such as gliomas.

公开(公告)号：US11053245B2

公开(公告)日：2021-07-06

申请号：US14394469

申请日：2013-04-14

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Sharon Mates ,  Robert Davis ,  Kimberly Vanover

IPC分类号： C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  C07D471/16 ,  A61K31/445

摘要： Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.

公开(公告)号：US20210188850A1

公开(公告)日：2021-06-24

申请号：US17124224

申请日：2020-12-16

申请人： INTRA-CELLULAR THERAPIES, INC.

发明人： Sharon MATES ,  Peng LI ,  Lawrence P. WENNOGLE ,  Robert DAVIS

IPC分类号： C07D471/16 ,  C07D471/14 ,  A61K45/06 ,  C07B59/00 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18 ,  A61K31/4985

摘要： This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.