Neurocrine Biosciences, Inc.

Ionis Pharmaceuticals, Inc.

Jinghua Yu

Timothy Richard Coon

Graham Beaton

Eric E Swayze

Punit P Seth

Thazha P Prakash

Martin W Rowbottom

Warren Stanfield Wade

Mi Chen

Neil Ashweek

Michael T Migawa

Todd Ewing

Yun-Fei Zhu

Garth A Kinberger

Wanlong Jiang

Willy Moree

Liren Zhao

W Brad Wan

Guillermo Vasquez

Florence Jovic

Sayten P Patel

Satyen P Patel

Wilna (Willy) J Moree

Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.

Method for synthesis of reactive conjugate clusters

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R, R, R, R, R, R, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R, R, R, R, R, R, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof. 

Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R, R, R, R, L, Land n are as defined herein. Such compounds generally function as Hreceptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

Sleep inducing compounds and methods relating thereto

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San Marcos, CA, United States of America

Jinghua Yu