217972-87-7

Usage

Uses

Used in Pharmaceutical Industry:
1H-1,4-Diazepine-1-carboxylic acid, hexahydro-5-methyl-, phenylmethyl ester is used as an antipsychotic agent for the treatment of mental disorders such as schizophrenia and bipolar disorder. It modulates the activity of neurotransmitter receptors in the brain, including dopamine and serotonin receptors, to help regulate mood and behavior.
Used in Mood Regulation:
As a prodrug, 1H-1,4-Diazepine-1-carboxylic acid, hexahydro-5-methyl-, phenylmethyl ester is metabolized in the body to produce the active form of clozapine, which aids in mood regulation and behavior control for individuals suffering from mental disorders.
Used in Oral Medication:
1H-1,4-Diazepine-1-carboxylic acid, hexahydro-5-methyl-, phenylmethyl ester is typically administered orally in tablet form, making it a convenient and accessible treatment option for patients with mental disorders requiring antipsychotic medication.
However, it is important to note that 1H-1,4-Diazepine-1-carboxylic acid, hexahydro-5-methyl-, phenylmethyl ester is associated with a range of potential side effects, including drowsiness, weight gain, and an increased risk of seizures. These side effects should be considered and monitored when prescribing and administering this medication to patients.

Upstream product

• 1030377-23-1 benzyl (2-((tert-butoxycarbonyl)amino)ethyl)(3-oxobutanoyl)carbamate 
• 501-53-1 benzyl chloroformate 
• 22777-05-5 hexahydro-5-methyl-1H-1,4-diazepine 

Downstream Products

• 1030377-24-2 1-benzyl 4-tert-butyl 5-methyl-1,4-diazepane-1,4-dicarboxylate 
• 1001401-60-0 benzyl (R)-5-methyl-1,4-diazepane-1-carboxylate 
• 1001401-61-1 C₁₄H₂₀N₂O₂ 

Relevant academic research and scientific papers

PROCESS FOR THE RESOLUTION OF (R,S)-DIAZEPANE AND DIAZEPANONE DERIVATIVES

The present invention relates to a process for the preparation of an acid salt (T) of a compound of formula (A) (A) as well as to the acid salt (T) and the compound (A) as such,wherein R1 is selected from the group consisting of H, PG1 and RA, with RA being or and wherein PG1 is a suitable protecting group, and wherein n is 0 or 1, wherein the acid salt (T) is the salt of one stereoisomer of a chiral acid, preferably wherein the chiral acid salt is a tartaric acid derivative salt, preferably wherein the tartaric acid derivative salt is selected from the group consisting of 2,3-ditoluoyl tartaric acid salt, 2,3-dibenzoyl tartaric acid salt, 2,3-dianisoyl tartaric acid salt, 2,3-dibenzoyl tartaric acid mono(dimethylamide) salt and a mixture of two or more thereof. Further the present invention relates to use of (T) and/or (A) for the preparation of suvorexant.

Discovery of the dual orexin receptor antagonist [(7 R)-4-(5-chloro-1,3- benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2 H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia

Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified in recent years. One notable exception is inhibition of the excitatory neuropeptides orexins A and B by design of orexin receptor antagonists. Herein, we describe how efforts to understand the origin of poor oral pharmacokinetics in a leading HTS-derived diazepane orexin receptor antagonist led to the identification of compound 10 with a 7-methyl substitution on the diazepane core. Though 10 displayed good potency, improved pharmacokinetics, and excellent in vivo efficacy, it formed reactive metabolites in microsomal incubations. A mechanistic hypothesis coupled with an in vitro assay to assess bioactivation led to replacement of the fluoroquinazoline ring of 10 with a chlorobenzoxazole to provide 3 (MK-4305), a potent dual orexin receptor antagonist that is currently being tested in phase III clinical trials for the treatment of primary insomnia.

Substituted diazepan orexin receptor antagonists

The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

ISOQUINOLINESULFONAMIDE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

This invention relates to isoquinolinesulfonamide derivatives represented by the following formula (1): wherein A represents a linear or branched alkylene group, R1 represents a hydrogen atom, an hydroxyl, alkoxy or alkyl group or the like, R2 represents a hydrogen atom, an alkyl group or the like, R3 represents a hydrogen atom, an alkyl group or the like, and R4 and R5 may be the same or different and individually represent hydrogen atoms or lower alkyl groups; N-oxides and salts thereof; and solvates thereof. This invention is also concerned with pharmaceutical compositions, which contain the derivatives, N-oxides, salts, or solvates. These derivatives, N-oxides, salts, and solvates have viral proliferation inhibiting activities and are useful as AIDS therapeutics.