公开(公告)号：US12139490B2

公开(公告)日：2024-11-12

申请号：US17808836

申请日：2022-06-24

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 substituted heterocycle fused gamma-carbolines, such as the compound of Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, and as further defined herein.

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：US11407751B2

公开(公告)日：2022-08-09

申请号：US16594603

申请日：2019-10-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Charles Tomesch ,  Peng Li ,  Qiang Zhang ,  Andrew S. Thompson

IPC: C07D471/16 ,  C07D471/04

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

公开(公告)号：US10464938B2

公开(公告)日：2019-11-05

申请号：US16439361

申请日：2019-06-12

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: A61K31/4353 ,  C07D471/06 ,  C07D471/16 ,  C07D471/04

Abstract: The present invention provides pharmaceutical compositions comprising certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, and as further defined herein:

公开(公告)号：US09371324B2

公开(公告)日：2016-06-21

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: A61K31/4985 ,  C07D241/38 ,  C07D471/16 ,  C07D471/04 ,  A61K31/44

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

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, of Formula I as described herein, 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, such as diseases of the central nervous system.

Abstract translation: 本发明涉及如本文所述的本发明式I的特定的取代的杂环稠合的γ-咔啉，其前药具有本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式，其药物组合物，以及在 治疗涉及5-HT2A受体，血清素转运蛋白（SERT）和/或涉及多巴胺D2受体信号传导系统的途径（例如中枢神经系统疾病）的疾病。

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：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。