公开(公告)号：US11839614B2

公开(公告)日：2023-12-12

申请号：US16966818

申请日：2019-01-31

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David Kass ,  Toru Hashimoto ,  Lawrence Wennogle ,  Joseph Hendrick ,  Robert Davis

IPC: A61K31/519 ,  A61P9/04 ,  A61K31/41 ,  A61K31/7056 ,  A61K9/00 ,  A61K45/06 ,  A61K31/197 ,  A61K31/216 ,  A61K31/4178 ,  A61K31/04

CPC classification number: A61K31/519 ,  A61K9/0053 ,  A61K31/04 ,  A61K31/197 ,  A61K31/216 ,  A61K31/4178 ,  A61K31/7056 ,  A61K45/06 ,  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：US11826367B2

公开(公告)日：2023-11-28

申请号：US17659063

申请日：2022-04-13

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

IPC: A61K31/4985 ,  A61K9/20 ,  A61K9/16 ,  A61K9/00 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/06 ,  A61K9/48 ,  C07D471/16 ,  A61K9/10 ,  A61K47/38

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 ,  A61K9/10 ,  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-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20230355625A1

公开(公告)日：2023-11-09

申请号：US17780660

申请日：2020-11-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Robert DAVIS ,  Peng LI

IPC: A61K31/519 ,  A61K45/06 ,  A61P25/28

CPC classification number: A61K31/519 ,  A61K45/06 ,  A61P25/28

Abstract: The present disclosure relates to inhibitors of phosphodiesterase 1 (PDE1) useful for the engagement with the central nervous system. The disclosure further relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of a condition, disease or disorder associated with the dopamine D1 receptor intracellular pathway, e.g., a condition, disease or disorder characterized by a deficit in attention, cognition, memory and/or inhibitory processing.

公开(公告)号：US11806347B2

公开(公告)日：2023-11-07

申请号：US17338573

申请日：2021-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis

IPC: A61K31/498 ,  A61K31/4985 ,  A61K9/06 ,  A61K9/00

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

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：US11773095B2

公开(公告)日：2023-10-03

申请号：US17813473

申请日：2022-07-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  C07D471/16 ,  A61P25/36 ,  A61P1/00 ,  A61P11/00 ,  A61P29/00 ,  A61K45/06

CPC classification number: C07D471/16 ,  A61K45/06 ,  A61P1/00 ,  A61P11/00 ,  A61P25/36 ,  A61P29/00 ,  A61K31/485 ,  A61K2300/00 ,  A61K31/4985 ,  A61K2300/00 ,  A61K31/137 ,  A61K2300/00

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：US20230271962A1

公开(公告)日：2023-08-31

申请号：US18314785

申请日：2023-05-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

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-ol, 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.

公开(公告)号：US11680065B2

公开(公告)日：2023-06-20

申请号：US17072933

申请日：2020-10-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/437 ,  C07D471/22 ,  C07D471/16 ,  C07D471/14 ,  A61K9/50 ,  A61K9/48 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38

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, compounds of Formula Q:




wherein W is —N(H)—, or —N(CH3)—, and Y is —C(═O)— or —O—, in free base or pharmaceutically acceptable salt form, 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.

公开(公告)号：US20230174543A1

公开(公告)日：2023-06-08

申请号：US17997983

申请日：2021-05-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D487/14

CPC classification number: C07D487/14 ,  C07B2200/13

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-α]pyrazolo[4,3-e]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.

公开(公告)号：US11504372B2

公开(公告)日：2022-11-22

申请号：US16879676

申请日：2020-05-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. Wennogle

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

Abstract: 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

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

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

Abstract: 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.