公开(公告)号：US11453670B2

公开(公告)日：2022-09-27

申请号：US16438163

申请日：2019-08-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang

IPC: C07D471/16 ,  C07D519/00

Abstract: The present invention provides improved methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.

公开(公告)号：US10221176B2

公开(公告)日：2019-03-05

申请号：US15660762

申请日：2017-07-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/22 ,  C07D487/22 ,  C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2F, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, such methods comprising the preparation of a Compound of Formula 2F, as shown below and as further defined herein:

公开(公告)号：US10072010B2

公开(公告)日：2018-09-11

申请号：US15629481

申请日：2017-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  C07D487/22 ,  C07D471/16 ,  C07D471/14 ,  A61K9/48 ,  A61K9/50 ,  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 substituted pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]-quinoxaline compounds, represented by Formula 1, defined herein, free base or pharmaceutically acceptable salt forms of the compounds, pharmaceutical compositions thereof, 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：US11066407B2

公开(公告)日：2021-07-20

申请号：US16711790

申请日：2019-12-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/16 ,  C07D471/04

Abstract: 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：US09751883B2

公开(公告)日：2017-09-05

申请号：US15066962

申请日：2016-03-10

Applicant: Intra-Cellular Therapies, Inc.

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

IPC: C07D487/22 ,  C07D471/22 ,  C07D471/16 ,  C07D471/04

CPC classification number: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, such methods comprising the preparation of a Compound of Formula 2G, as shown below, and use of said compound to produce the fused gamma-carbolines of Formula 2J, as defined herein:

公开(公告)号：US20170190703A9

公开(公告)日：2017-07-06

申请号：US15110613

申请日：2015-01-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Qiang Zhang ,  Youyi Peng ,  Peng Li ,  J. David Beard ,  Lawrence P. Wennogle ,  John Tomesch

IPC: C07D487/04 ,  C07D277/82 ,  C07D235/30 ,  C07B59/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D235/30 ,  C07D277/82 ,  C07D401/12

Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.

公开(公告)号：US20160326179A1

公开(公告)日：2016-11-10

申请号：US15110613

申请日：2015-01-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Qiang Zhang ,  Youyi Peng ,  Peng Li ,  J. David Beard ,  Lawrence P. Wennogle ,  John Tomesch

IPC: C07D487/04 ,  C07D277/82 ,  C07D235/30 ,  C07B59/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D235/30 ,  C07D277/82 ,  C07D401/12

Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.

Abstract translation: 本发明提供新型化合物，包含所述化合物的组合物和用于抑制CK1的方法以及治疗CK1相关病症如阿尔茨海默氏病的方法，包括向有需要的患者施用治疗有效量的CK1抑制剂。

公开(公告)号：US10597395B2

公开(公告)日：2020-03-24

申请号：US16244796

申请日：2019-01-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/16 ,  C07D471/04

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

公开(公告)号：US09315504B2

公开(公告)日：2016-04-19

申请号：US14323545

申请日：2014-07-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D241/38 ,  C07D471/16 ,  C07D471/04

CPC classification number: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of 4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3′,4′:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone in free form or a salt thereof.

Abstract translation: 本发明提供了制备4-（3-甲基-2,3,6b，9,10,10a-六氢-1H-吡啶并[3'，4'：4,5] - 吡咯并[ 2,3-de]喹喔啉-8-（7H） - 基）-1-（4-氟苯基）-1-丁酮或其盐。