公开(公告)号：US09056837B2

公开(公告)日：2015-06-16

申请号：US13728514

申请日：2012-12-27

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Peng Li

IPC: A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  C07D239/42 ,  C07D405/12

CPC classification number: C07D405/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

Abstract: The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which penetrate the blood brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.

Abstract translation: 本发明涉及式（I）的化合物或其药学上可接受的盐：其渗透血脑屏障，抑制β-淀粉样蛋白的形成和积累，并且可用于治疗神经变性疾病，特别是阿尔茨海默病。 此外，本发明的化合物抑制某些激酶，因此可用于治疗中枢神经系统的癌症。

公开(公告)号：US12144808B2

公开(公告)日：2024-11-19

申请号：US17271965

申请日：2019-08-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

IPC: A61K31/4985 ,  A61K9/70

Abstract: The disclosure provides new transdermal 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：US12122792B2

公开(公告)日：2024-10-22

申请号：US18240951

申请日：2023-08-31

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert E Davis ,  Kimberly Vanover

IPC: A61K31/4985 ,  C07D471/22 ,  C07D487/22 ,  C07D519/00

CPC classification number: C07D519/00

Abstract: The invention relates to pharmaceutical compositions comprising the compound of Formula I,




and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.

公开(公告)号：US11690842B2

公开(公告)日：2023-07-04

申请号：US17332417

申请日：2021-05-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

IPC: A61K31/4985 ,  A61K9/48 ,  A61K9/00 ,  A61K9/16

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/485 ,  A61K9/4825 ,  A61K9/4858 ,  A61K9/4891

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

公开(公告)号：US11427587B2

公开(公告)日：2022-08-30

申请号：US16634059

申请日：2018-07-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: C07D471/16 ,  A61P25/36 ,  A61P1/00 ,  A61P11/00 ,  A61P29/00 ,  A61K45/06

Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, 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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US11376249B2

公开(公告)日：2022-07-05

申请号：US16634055

申请日：2018-07-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  A61P25/36 ,  A61K9/00 ,  A61K9/16 ,  A61K45/06 ,  A61P23/00 ,  A61K31/137 ,  A61K31/485

Abstract: The 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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US11052083B2

公开(公告)日：2021-07-06

申请号：US16900746

申请日：2020-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis

IPC: A61K31/498 ,  A61P15/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61K31/4985 ,  A61K9/06 ,  A61K9/00

Abstract: 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：US11014925B2

公开(公告)日：2021-05-25

申请号：US16090152

申请日：2017-03-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Edwin Aret

IPC: C07D471/16 ,  C07D213/82 ,  A61K31/519 ,  C07D213/81 ,  A61K9/00 ,  A61P25/18

Abstract: The disclosure provides new, stable, pharmaceutically acceptable co-crystal forms 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：US10961245B2

公开(公告)日：2021-03-30

申请号：US16473693

申请日：2017-12-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

IPC: C07D471/14 ,  C07D471/16 ,  A61K31/4985 ,  A61K9/51 ,  A61K47/34 ,  A61K31/44 ,  A61K9/00 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P1/00 ,  A61P15/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/20 ,  A61P25/32 ,  A61P25/36 ,  A61P3/04

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, the compounds of Formula I: 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 central nervous system (CNS) diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US10960009B2

公开(公告)日：2021-03-30

申请号：US16392409

申请日：2019-04-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly Vanover ,  Peng Li ,  Sharon Mates ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K9/00 ,  A61K9/51 ,  A61K31/5383 ,  A61K45/06 ,  A61K31/4985

Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.