Intra-cellular Therapies, Inc.

Osi Pharmaceuticals, Inc.

James David Beard

Peng Li

Andrew S Thompson

Qiang Zhang

Wei Yao

John Charles Tomesch

Hua Cheng

Lawrence P Wennogle

Andrew Philip Crew

Jing Wang

Lee Daniel Arnold

Heather Renee Coate

Bijoy Panicker

Mark Joseph Mulvihill

Meizhong Jin

Douglas S Werner

Xin Chen

Ayako Honda

Kam W Siu

Brian Volk

Paula A R Tavares

Apoorba Bharadwaj

Han-Qing Dong

Kristen Michelle Mulvihill

Quinghua Weng

Qinghua Weng

Hanqing Dong

Andrew-Philip Crew

Lee D Arnoldd

Paula AR Tavares

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.

Process for preparing 1-(4-fluorophenyl)-4-((6bR, 10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3',4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)butan-1-one

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: 

Preparation of certain substituted 1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines and pharmaceutically acceptable salts thereof

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: 

Preparation of certain substituted 1-(4-fluorophenyl)-4-(2,3,6b,9,10,10a-hexahydro-1H-pyrido[3',4&#x2032;:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-YL)butan-1-ones and pharmaceutically acceptable salts thereof

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: 

Pharmaceutical compositions comprising ((6bR,10aS)-1-(4-fluorophenyl)-4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3',4&#x2032;:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)butan-1-one or pharmaceutically acceptable salts thereof

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: 

Preparation of certain substituted [((6bR,10aS)-2,3,6b,7,8,9,10,10a-octahydro-1H-pyrido[3',4&#x2032;:4,5]pyrrolo[1,2,3-de]quinoxalines and pharmaceutically acceptable salts thereof

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: 

Preparation of certain [((6BR,10AS)-2,3,6B,7,8,9,10, 10A-octahydro-1H-pyrido[3',4&#x2032;:4,5]pyrrolo [1,2,3-de]quinoxalines and pharmaceutically acceptable salts thereof

The present invention provides methods for the preparation of 4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3',4&#x2032;:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone in free form or a salt thereof.

Preparation of 4-((6BR,10AS)-3-methyl-2,3,6B,9,10, 10A-hexahydro-1H-pyrido[3',4&#x2032;:4,5]pyrrolo [1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone or a pharmaceutically acceptable salt thereof

Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

Fused bicyclic mTOR inhibitors

The present invention provides methods for the preparation of substituted 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivative useful as intermediates and methods for producing and using such intermediates.

Substituted 2,3,4,4A,5,9B-hexahydro-1H-pyrido[4,3-B]indole derivatives synthesis and uses thereof

Fused bicyclic motor inhibitors

The present invention provides 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.

Substituted heterocycle gamma-carbolines synthesis

Fused bicyclic mTor inhibitors

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New York, NY, United States of America

James David Beard