1104546-96-4Relevant academic research and scientific papers
Palladium-Catalyzed Decarboxylative Asymmetric Allylic Alkylation of 1,4-Diazepan-5-ones
Sercel, Zachary P.,Sun, Alexander W.,Stoltz, Brian M.
, p. 9158 - 9161 (2019)
We report the palladium-catalyzed asymmetric allylic alkylation of 1,4-diazepan-5-ones. This reaction proceeds smoothly to give gem-disubstituted diazepanone heterocycles bearing various functional groups in up to >99% yield and up to 95% ee. An electron-
Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia
Aoki, Takeshi,Futamura, Aya,Hino, Noriko,Hiyoshi, Tetsuaki,Kambe, Daiji,Kawamoto, Hiroshi,Kirinuki, Sora,Nozawa, Dai,Ohmichi, Mari,Suzuki, Ryo,Tamura, Yunoshin,Tokumaru, Yuichi
, (2020)
Here, we present the design, synthesis, and SAR of dual orexin 1 and 2 receptor antagonists, which were optimized by balancing the antagonistic activity for orexin receptors and lipophilicity. Based on the prototype compound 1, ring construction and the i
METHOD FOR PRODUCING (2S)-2-[(1H-PYRAZOL-1-YL)METHYL]-1,3-OXAZINANE DERIVATIVE
-
Paragraph 0270-0274, (2021/05/21)
Provided is a novel process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative. More specifically, provided is a process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative represented by formula (1): the process comprising reacting 3-aminopropan-1-ol with glyoxylic acid.
The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders
Boss, Christoph,Gatfield, John,Brotschi, Christine,Heidmann, Bibia,Sifferlen, Thierry,von Raumer, Markus,Schmidt, Gunther,Williams, Jodi T.,Treiber, Alexander,Roch, Catherine
supporting information, p. 2286 - 2305 (2020/10/30)
Since its discovery in 1998, the orexin system has been of interest to the research community as a potential therapeutic target for the treatment of sleep/wake disorders, stress and anxiety disorders, addiction or eating disorders. It consists of two G protein-coupled receptors, the orexin 1 and orexin 2 receptors, and two neuropeptides with agonistic effects, the orexin A and orexin B peptides. Herein we describe our efforts leading to the identification of a promising set of dual orexin receptor antagonists (DORAs) which subsequently went through physiology-based pharmacokinetic and pharmacodynamic modelling>[1] and finally led to the selection of daridorexant, currently in phase 3 clinical trials for the treatment of insomnia disorders.
Octahydropyrrolo[3,4-c]pyrrole derivative and application method and application thereof
-
Paragraph 0188-0189, (2018/03/24)
The invention relates to an octahydropyrrolo[3,4-c]pyrrole derivative and an application method and application thereof. The compound and a pharmaceutical composition containing the compound are usedfor antagonizing orexin receptors. The invention also re
Octahydropyrrolo[3,4-c]pyrrole derivatives and use thereof
-
Paragraph 0193; 0199; 0200, (2020/02/06)
The invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives and a use thereof. The above compounds and a medicinal composition containing the compounds are used for suppressing an orexin receptor. The invention also relates to a method for preparing the compounds and the medicinal composition, and the use of the compounds and the medicinal composition in the treatment or prevention of orexin receptor related diseases.
SUBSTITUTED QUINAZOLINE COMPOUNDS AND PREPARATION AND USES THEREOF
-
Page/Page column 54, (2017/03/08)
The present invention relates quinazolinone compounds of Formula (I), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses; wherein the compounds or pharmaceutical compositions disclosed herein can be used for antagonizing the orexin receptor. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing neurological and psychiatric disorders and diseases of the central nervous system in mammals, especially in humans.
OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
-
Paragraph 00183, (2017/07/04)
The invention relates to octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof. Compounds and pharmaceutical compositions comprising the compounds provided herein are used for antagonizing orexin receptors. The invention also relates to processes for preparing the compounds and pharmaceutical compositions, and uses thereof in treating or preventing a disease related to orexin receptors.
Indole derivative and uses thereof
-
Paragraph 0190; 0191, (2017/09/01)
The present invention relates to an indole derivative and uses thereof, wherein the compound and the pharmaceutical composition comprising the compound can be used for antagonizing orexin receptors. The present invention further relates to a method for preparing the compound and the pharmaceutical composition, and uses of the compound and the pharmaceutical composition in treatment or prevention of diseases associated with orexin receptors.
Method for preparing N-heterocyclic compound
-
Paragraph 0052; 0054, (2017/11/18)
The invention provides a method for preparing an N-heterocyclic compound and belongs to the technical field of pharmacy. The method for preparing the N-heterocyclic compound comprises the steps of carrying out condensation reaction on an N-heterocyclic intermediate compound and 2-ethoxy-5-chlorobenzoxazole under an acid condition, and carrying out aftertreatment to prepare the compound (1). The method is simple and convenient, and can be applied to industrial production.
