公开(公告)号：US20160145261A1

公开(公告)日：2016-05-26

申请号：US14900589

申请日：2014-06-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  INTRA-CELLULAR THERAPIES, INC.

Inventor： Takashi ABE ,  Graham Buckton ,  Robert DAVIS ,  Mark HOOPER ,  Peng LI ,  Hideaki MARUYAMA ,  Masahiro TAKASUGA ,  Lawrence P. Wennogle ,  Yuhei YAMAMOTO ,  Hinori YAMASHITA

IPC: C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.

Abstract translation: 本发明涉及（6aR，9aS）-5,6a，7,8,9,9a-六氢-5-甲基-3-（苯基氨基）-2 - （（4-（6-氟吡啶-2-基） 苯基）甲基） - 环戊并[4,5]咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4（2H） - 酮，以及制备和使用这种晶体的方法。

公开(公告)号：US20240327436A1

公开(公告)日：2024-10-03

申请号：US18741739

申请日：2024-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert E. DAVIS ,  Kimberly Vanover

IPC: 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：US20240216368A1

公开(公告)日：2024-07-04

申请号：US18602981

申请日：2024-03-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

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

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/4825 ,  A61K9/485 ,  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：US20240115565A1

公开(公告)日：2024-04-11

申请号：US18488513

申请日：2023-10-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

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

CPC classification number: A61K31/4985 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/0053 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/38 ,  A61P3/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D471/16

Abstract: 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-l-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20240016802A1

公开(公告)日：2024-01-18

申请号：US18476138

申请日：2023-09-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

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

CPC classification number: A61K31/4985 ,  A61K9/06 ,  A61K9/006 ,  A61K9/0043 ,  A61K9/0036

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：US20240009195A1

公开(公告)日：2024-01-11

申请号：US18007018

申请日：2021-07-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  David KASS ,  Robert DAVIS ,  Gretchen SNYDER

IPC: A61K31/519 ,  A61K31/7034 ,  A61K45/06 ,  A61P9/04

CPC classification number: A61K31/519 ,  A61K31/7034 ,  A61K45/06 ,  A61P9/04

Abstract: The disclosure provides methods, treatments and materials for treating diseases or disorders mediated by cyclic nucleotides and/or sodium glucose cotransporter 2. In particular, the present disclosure provides for methods of treating such diseases and disorders with a PDE1 inhibitor in combination with additional therapeutic agents.

公开(公告)号：US20230312573A1

公开(公告)日：2023-10-05

申请号：US18043959

申请日：2021-09-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D471/16

CPC classification number: C07D471/16 ,  C07B2200/13

Abstract: The disclosure provides salts and crystal forms of a substituted heterocycle fused gamma-carboline, the manufacture thereof, pharmaceutical compositions thereof, and use thereof, e.g., in the treatment of diseases or abnormal conditions involving or mediated by the 5-HT2A receptor, serotonin transporter (SERT), and/or dopamine D1/D2 receptor signaling pathways.

公开(公告)号：US20230301995A1

公开(公告)日：2023-09-28

申请号：US18319425

申请日：2023-05-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

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

CPC classification number: A61K31/4985 ,  A61K9/06 ,  A61K9/006 ,  A61K9/0043 ,  A61K9/0036

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：US20230203037A1

公开(公告)日：2023-06-29

申请号：US18067387

申请日：2022-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

CPC classification number: C07D471/16 ,  C07D471/14 ,  A61K45/06 ,  C07B59/002 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18 ,  A61K31/4985

Abstract: 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.

公开(公告)号：US20230071934A1

公开(公告)日：2023-03-09

申请号：US17757572

申请日：2020-12-18

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Peng LI

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/445 ,  A61K31/53

Abstract: The disclosure provides methods, treatments and materials for treating diseases or disorders mediated by cyclic nucleotides and/or epoxygenated fatty acids. In particular, the present disclosure provides for methods of treating such diseases and disorders with a PDE1 inhibitor in combination with additional therapeutic agents.