74 results about "Azepane" patented technology

The present disclosure relates to pharmaceutical compositions suitable for oral administration, and more particularly to pharmaceutical compositions, including pharmaceutical tablet compositions, containing (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide (Compound A) or a pharmaceutically acceptable salt thereof.

The invention relates to a preparation method of suvorexant, which comprises the following steps: (1) dissolving a compound VIII (R)-4-(5-chlorobenzo [d] oxazole-2-yl)-7-methyl-1, 4-diazacycloheptane-1-carboxylic acid tert-butyl ester in a reaction solvent, adding an acidic reagent at the temperature of 5-15 DEG C, and reacting at the temperature of 25-35 DEG C to prepare a compound IX (R)-5-chloro-2-(5-methyl-1, 4-diazacycloheptane-1-carboxylic acid tert-butyl ester; 2, 4-diazacycloheptane-1-yl) benzo [d] oxazole is used as a raw material; and (2) in an alkaline environment and an aprotic solvent, carrying out acylation nucleophilic reaction on the compound IX and 5-methyl-2-(2H-1, 2, 3-triazole-2-yl) benzoic acid to obtain the suvorexant. According to the preparation method, the obtained product is high in yield, the purity reaches 99.9% or above, and the intermediate product is good in character, few in impurity and suitable for industrial production.

Disclosed are a crystal of the compound (S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide salt or a salt thereof, a preparation method therefor, and the uses thereof in pharmaceutical compositions and in medicine.

The application discloses a kind of deuterated benzamide diazepine compounds and preparation method and purposes thereof, and structure is as shown in general formula I.The compound is used as selective OX2R antagonist, and shows good activity, selectivity, brain exposure, brain blood ratio (the ratio of drug concentration in brain and drug concentration in blood, is called B / P), little toxic side effect, moderate half-life effect etc..It can be used for preventing, treating and / or reducing the disease related to orexin receptor.General formula I

Medical electrode comprising a base body (101) on which an electrically conductive first layer (102) and a cover layer (103) are arranged, the cover layer comprising an overhang (107) which partially covers the first layer (102), and an electrically conductive second layer (105) which is arranged on the first layer (102), the second layer (105) comprising an electrically conductive polymer selected from the group consisting of a polyacetylene, a polyvinyl alcohol, a polyfluorene, a polyphenylene, a polyphenylene vinylene, a polypyrene, a polyazulene, a polynaphthalene, a polypyrrole, a polycarbazole, a polyindole, a polyazepine, a polyaniline, a polyacene, a polythiophene, a polythiophene vinylene, a poly-p-phenylene sulfide, a polypyridine or functionalized derivatives, precursors or mixtures thereof;wherein the top layer (103) further comprises a recess (108), wherein the second layer (105) is arranged exclusively within the recess (108), and wherein the outwardly facing surface of the second layer (105) is spaced apart from the outwardly facing surface of the top layer (103), leaving a free area within the recess (108).

The invention discloses a preparation method of a chiral intermediate (S)-3-methyl-1-tert-butoxycarbonyl-1,4-diazepane for treating ocular hypertension, relating to the technical field of pharmaceutical chemicals. The invention comprises the following steps: using 1-benzyl-3-methylpiperidin-4-one as a starting raw material, performing chiral resolution to obtain an intermediate 1, performing an addition-elimination reaction on the intermediate 1 and hydroxylamine hydrochloride to obtain an intermediate 2, performing a Beckmann rearrangement reaction on the intermediate 2 to obtain an intermediate 3, performing an amino deprotection reaction on the intermediate 3 to obtain an intermediate 4, performing an amino protection reaction on the intermediate 4 and di-tert-butyl dicarbonate to obtain an intermediate 5, and performing a decarbonylation reaction on the intermediate 5 to obtain the (S)-3-methyl-1-tert-butoxycarbonyl-1,4-diazepane. The preparation method has the characteristics of readily available raw materials, a simple process and a high product yield, and is suitable for the industrial production of the (S)-3-methyl-1-tert-butoxycarbonyl-1,4-diazepane.

The invention relates to the technical field of nanogel, and discloses functional polyurea nanogel with universal drug loading capacity as well as a preparation method and application of the functional polyurea nanogel. The invention relates to a functionally modified polyurea compound, which is prepared from the following raw materials: a double primary amine compound, double (2-oxo azacycloheptane-1-formamido alkyl) amine, a polyethylene glycol-amino compound, N, N '-carbonyl double (caprolactam), acid anhydride and an organic solvent. The functionally modified polyurea compound provided by the invention does not contain an isocyanate group and is high in biological safety; the functional polyurea nanogel synthesized by taking a functional modified polyurea compound as a raw material is high in biological safety, has charge overturning performance, has multiple intermolecular non-covalent interaction including hydrogen bond interaction, electrostatic interaction and hydrophobic interaction, can be used for universal drug loading, has pH value responsive swelling property, and can be applied to drug loading. The compound can be used for releasing pH-responsive drugs.

Mutants M203A and M203A / S241L of the reductive amination enzyme IR-G36-M5 are provided, as well as the use of said mutants in the catalytic asymmetric reductive amination synthesis of (R)-N-Boc-3-cyclopropylpiperidine or (R)-N-Boc-3-cyclopropylazheptanane.

The invention provides a synthesis method of a 6-hydroxy-6-methyl-1, 4-diazacycloheptane intermediate, and belongs to the field of pharmacy. The brand-new synthesis method for preparing the 6-hydroxy-6-methyl-1, 4-diazacycloheptane intermediate is provided, raw materials and reagents are low in price and safe, compared with the prior art, the method is convenient to operate, the process efficiency is improved by 28.6%, the total yield is improved to 46.3%, the requirement for large-scale preparation in a laboratory can be met, and good application prospects are achieved.

Disclosed herein are compounds and pharmaceutical compositions comprising such compounds for the treatment of conditions modulated by calcium channel ion activity, including compounds comprising a piperazine core, a 1, 4-diazepane core, or a 1, 5-diazepane core. Also disclosed herein are methods of using the compounds to treat diseases or conditions associated with aberrant function or activity of T-type calcium channels.

Provided herein are compounds, including compounds of any of the formulae described herein (e.g., Formula (I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, solvates, hydrates, isotopically labeled derivatives, and prodrugs thereof. Compounds provided herein can act as potentiators of voltage-gates potassium channels (e.g., Kv7 potassium channels such as Kv7.2 / Kv7.3) and are therefore useful in the treatment and / or prevention of diseases, disorders, and conditions (e.g., diseases, disorders, and conditions associated with Kv7 potassium channel dysfunction).

The present invention relates to a salt type and crystal form of a benzazepine fused ring compound and use thereof, and in particular to a maleate of a compound represented by formula (I), the structure of the maleate being represented by formula (II).

Provided herein are methods for preparing (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide and intermediates useful therein.

The present disclosure relates in some aspects to compositions, such as pharmaceutical compositions for topical administration, which are useful for treating or preventing hair loss, hair graying, and dermatological conditions in a subject, such as comprising a substituted diazepine, for example olanzapine. Also provided are kits comprising the compositions, and methods of using the compositions for treating or preventing hair loss, hair graying, and dermatological conditions.

The present invention relates to a novel cytomegalovirus (CMV) inhibitor represented by formula (I) or a salt thereof wherein Cy is optionally substituted 1, 4-diazacycloheptyl; ar1 is an optionally substituted phenyl group; optionally substituted naphthyl; or optionally substituted heteroaryl containing 5 to 10 ring atoms selected from C, N, O and S; ar2 is an optionally substituted heteroaryl group containing 5 or 6 ring atoms selected from C, N, O and S.

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and / or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

The present invention relates to the field of organic synthesis, and in particular to a 1,4-diazepine derivative series and a preparation method thereof. A synthetic reaction is performed with reference to the following synthetic route: #imgabs0# wherein R is selected from an alkyl group or an aromatic group, R1, R2 and R3 are independently selected from hydrogen or an alkyl group, and Ar represents an aromatic group. The finished product prepared by the method has a low impurity content and stable quality indicators, and a 1,4-diazepine derivative series can be obtained.

To provide a new compound capable of specifically detecting OX1R. To provide a compound usable for a OX1R specific PET probe.SOLUTION: A 1, 4-diazepane derivative compound represented by the following general formula (1): wherein R1 represents hydrogen, fluoro, or an alkyl group having 1 to 5 carbon atoms, and the alkyl group may be substituted with fluoro. R2 is hydrogen, fluoro or a C1-C5 alkyl group which may be substituted with fluoro. R3 represents hydrogen, an alkyl group having 1 to 5 carbon atoms, or a cycloalkyl group having 3 to 5 carbon atoms, and the alkyl group and the cycloalkyl group may be each independently substituted with at least one group selected from the group consisting of an alkyl group having 1 to 5 carbon atoms and a cycloalkyl group having 3 to 5 carbon atoms. However, at least one of R1 and R2 contains a fluoride atom. ] SELECTED DRAWING: None

This invention relates to azaheptanidine derivatives and their pharmaceutical uses, with specific structures shown in formula (I). It also relates to methods for preparing said compounds, pharmaceutical compositions, and their use as KRas G12C inhibitors in the treatment of cancer.

The present disclosure provides a compound of formula (I), a pharmaceutical composition thereof, and a use thereof in treating and / or preventing diseases or conditions related to the activity of RIPK1 kinase.

This disclosure relates to 1,4-oxazolidinyl heptane and 1,4-thioazolidinyl heptane derivatives, and their use in treating conditions and diseases associated with the lanodid receptor (RyR), which regulates calcium channel signaling in cells. This disclosure also discloses pharmaceutical compositions comprising these compounds and their use in treating diseases and conditions associated with RyR dysfunction, particularly cardiovascular, musculoskeletal, and central nervous system (CNS) disorders.

Provided herein are compositions comprising an effective amount of a DPP1 inhibitor of formula (I), or a pharmaceutically acceptable salt thereof, and their use in the treatment of dipeptidyl peptidase 1 (DPP1) mediated disorders. In embodiments of the methods provided herein, the compositions are administered orally once a day.

The present disclosure relates to 1,4-oxazepane and 1,4-thiazepane derivatives and their use to treat disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel signaling in cells. The present disclosure also discloses pharmaceutical compositions comprising these compounds and uses thereof to treat diseases and conditions associated with RyR dysfunction, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.

Provided herein are treatment methods including administering a 5-hydroxytryptamine (HT)2C receptor agonist to a patient in need thereof. An exemplary method includes treating or preventing a 5-hydroxytryptamine (HT)2C receptor-associated disorder in a patient in need thereof, wherein the method comprises administering to the patient (R)-N-(2,2-difluoroethyl)-7-methyl-1,2,3,4,6,7-hexahydro-[1,4]diazepino[6,7,1-hi]indole-8-carboxamide (Compound 1), or a pharmaceutically acceptable salt thereof, wherein Compound 1, or a pharmaceutically acceptable salt thereof.

This invention relates to a method and chemical apparatus for separating benzene from a liquid stream containing at least one pyrolysis oil manufactured from plastic waste and further converting said benzene into cyclohexanone. Cyclohexanone is suitable as a precursor for azircycloheptane-2-one (ε-caprolactam) and adipic acid (at least a portion of which is based on benzene manufactured from plastic waste). Furthermore, polyamide-6 and polyamide-66 can be manufactured by the method according to the invention.

A method for synthesis of Lorazepam in a continuous flow using continuous flow reactor, in which method comprises five steps including N-acylation, diazepine ring closure, imine N-oxidation, Polonovski-type rearrangement, and ester hydrolysis; a green reagent comprising a peroxide reagent and rhenium oxide catalyst for N-oxidation of delorazepam; and an ammonium source combination for the synthesis of delorazepam.

To provide pharmaceutical compositions comprising (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide or a salt thereof, and methods for treating obstructive airway diseases.SOLUTION: A pharmaceutical composition comprises from about 1.0 to about 30 wt.% of (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide; from about 55 to about 75 wt.% of a pharmaceutical diluent; from about 15% to about 25% of a compression aid; from about 3.0% to about 5.0 wt.% of a pharmaceutical disintegrant; from about 0.00 to about 1.0 wt.% of a pharmaceutical glidant; and from about 2 to about 6 wt.% of a pharmaceutical lubricant.SELECTED DRAWING: None