1059630-11-3Relevant articles and documents
Preparation method of Lumateperone intermediate
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Paragraph 0019; 0045-0056, (2021/06/26)
The invention discloses a preparation method of a Lumateperone intermediate. The Lumateperone intermediate (6bR, 10aS)-2, 3, 6b, 9, 10, 10a-hexahydro-3-methyl-1H-pyridine[3', 4':4, 5] pyrrolo [1, 2, 3-de] quinoxaline-8 (7H) carboxylic acid ethyl ester is
SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SYNTHESIS
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Paragraph 00104, (2020/07/14)
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.
SOLID STATE FORMS OF LUMATEPERONE SALTS AND PROCESSES FOR PREPARATION OF LUMATEPERONE AND SALTS THEREOF
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Paragraph 00303, (2020/06/19)
The present disclosure relates to solid state forms of Lumateperone besylate, processes for preparation thereof and pharmaceutical compositions thereof.
SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SYNTHESIS
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Paragraph 000105, (2020/01/08)
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.
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders
Li, Peng,Zhang, Qiang,Robichaud, Albert J.,Lee, Taekyu,Tomesch, John,Yao, Wei,Beard, J. David,Snyder, Gretchen L.,Zhu, Hongwen,Peng, Youyi,Hendrick, Joseph P.,Vanover, Kimberly E.,Davis, Robert E.,Mates, Sharon,Wennogle, Lawrence P.
, p. 2670 - 2682 (2014/04/17)
We report the synthesis and structure-activity relationships of a class of tetracyclic butyrophenones that exhibit potent binding affinities to serotonin 5-HT2A and dopamine D2 receptors. This work has led to the discovery of 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 4-methylbenzenesulfonate (ITI-007), which is a potent 5-HT2A antagonist, postsynaptic D2 antagonist, and inhibitor of serotonin transporter. This multifunctional drug candidate is orally bioavailable and exhibits good antipsychotic efficacy in vivo. Currently, this investigational new drug is under clinical development for the treatment of neuropsychiatric and neurological disorders.
SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SYNTHESIS
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Page/Page column 82, (2008/12/07)
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 heterocycl fused gamma-carbolines.