公开(公告)号：US20210060010A1

公开(公告)日：2021-03-04

申请号：US17015883

申请日：2020-09-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei YAO ,  Peng LI ,  Robert DAVIS ,  Sharon MATES ,  Kimberly VANOVER ,  Gretchen SNYDER

IPC: A61K31/4985 ,  A61P25/00 ,  C07D471/16 ,  A61K9/00 ,  A61K9/16 ,  A61K45/00 ,  C07D241/40 ,  A61K31/445 ,  A61K45/06

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：US20200289519A1

公开(公告)日：2020-09-17

申请号：US16892206

申请日：2020-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David KASS ,  Toru HASHIMOTO ,  Lawrence P. WENNOGLE ,  Joseph HENDRICK ,  Robert DAVIS

IPC: A61K31/519 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/216 ,  A61K31/197 ,  A61K31/7056 ,  A61P9/04

Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.

公开(公告)号：US20170183350A1

公开(公告)日：2017-06-29

申请号：US15301912

申请日：2015-04-03

Applicant: Intra-Cellular Therapies, Inc.

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

IPC: C07D471/16 ,  A61K45/06 ,  A61K31/4985

CPC classification number: C07D471/16 ,  A61K31/4985 ,  A61K45/06 ,  C07B59/002 ,  C07D471/14

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 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：US20170114037A1

公开(公告)日：2017-04-27

申请号：US15317876

申请日：2015-06-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Robert DAVIS ,  Peng LI

IPC: C07D401/06 ,  A61K31/454 ,  A61K45/06

CPC classification number: C07D401/06 ,  A61K31/454 ,  A61K45/06 ,  C07B2200/05 ,  Y02A50/475

Abstract: The invention relates to particular 2-((1-(2-hydroxy-2-phenylethyl)piperidin-4-yl)methyl)isoindolin-1-one analogs and pro-drugs, in free, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases that can be therapeutically and/or preventively treated by the nerve control function of sigma ligands.

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：US20150166540A1

公开(公告)日：2015-06-18

申请号：US14627968

申请日：2015-02-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Lawrence P. WENNOGLE ,  Peng LI ,  John Charles TOMESCH ,  Qiang ZHANG

IPC: C07D471/16

CPC classification number: C07D471/16 ,  A61K31/44 ,  C07D471/04

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 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.

公开(公告)号：US20240252491A1

公开(公告)日：2024-08-01

申请号：US18621067

申请日：2024-03-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen SNYDER ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: A61K31/4985 ,  A61K9/00 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/155 ,  A61K31/165 ,  A61K31/197 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/485 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/07 ,  A61P25/24

CPC classification number: A61K31/4985 ,  A61K9/006 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/155 ,  A61K31/165 ,  A61K31/197 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/485 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/07 ,  A61P25/24

Abstract: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A or 5-HT2A/D2 receptor ligand, e.g. lumateperone.

公开(公告)号：US20240245610A1

公开(公告)日：2024-07-25

申请号：US18593060

申请日：2024-03-01

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS ,  William Paul FINDLAY

IPC: A61K9/20 ,  A61K9/28 ,  A61K31/4985

CPC classification number: A61K9/2013 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/284 ,  A61K31/4985 ,  C07B2200/13

Abstract: The present disclosure relates to solid oral dosage forms 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：US20240091224A1

公开(公告)日：2024-03-21

申请号：US18504345

申请日：2023-11-08

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：US20230339951A1

公开(公告)日：2023-10-26

申请号：US18327607

申请日：2023-06-01

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: C07D471/14 ,  A61K47/38 ,  A61K9/48 ,  C07D471/16 ,  A61K9/50 ,  A61K47/34 ,  A61K31/4985

CPC classification number: C07D471/16 ,  A61K9/4825 ,  A61K9/4891 ,  A61K9/5031 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14

Abstract: The invention relates to pharmaceutical compositions comprising 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)-1-(4-fluorophenyl)-butan-1-one, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.