54 results about "Azepane" patented technology

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.

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.

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.

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.

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.

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

Provided is crystalline (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) hydrochloric acid (HCl) salt. Also are provided pharmaceutical compositions comprising the salt form and methods for its use.

The present disclosure relates to methods for treating hidradenitis suppurativa with a composition comprising an effective amount of a N-(1-cyano-2-phenylethyl)-1, 4-oxazepane-2-carboxamide DPP1 inhibitor compound of Formula (I) or a pharmaceutically acceptable salt thereof. In one embodiment, the compound of Formula (I) is (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 (brensocatib).

The present invention provides a compound of formula (I) or a salt, solvate or stereoisomer thereof as a G9a inhibitor, wherein: R1 is CRxR'xR; a represents (CH2) m, wherein m is 0 or 1; z represents (CH2) n, wherein n is 2 or 3; r2 is selected from: (a) an aromatic 5-or 6-membered ring system wherein the ring atoms are selected from: CRz1, S, N, NH and O; and (b) an aromatic fused ring system consisting of two rings wherein one or both rings are aromatic rings and each aromatic ring has 5 or 6 ring atoms selected from the group consisting of CRz2, S, N, NH and O. The invention also provides the use of the compounds of formula (I) in the treatment of G9a-mediated diseases, as well as pharmaceutical compositions comprising these compounds. Advantageously, the compounds of the present invention are particularly efficient and selective for G9a targets and the like. (I)

The invention provides a preparation method and application of 7-(10-methyl undecyl) azacycloheptane-2-ketone, and the method comprises the following steps: fermenting and culturing wetland streptomyces 13-3 to obtain a fermentation product, extracting the fermentation product with ethyl acetate, and concentrating under reduced pressure to obtain a crude extract; the crude extract is subjected to rapid preparative chromatography, Sephadex LH-20 gel column chromatography and silica gel column chromatography purification, and 7-(10-methyl undecyl) azacycloheptane-2-one is obtained; according to the invention, the new compound 7-(10-methyl undecyl) azacycloheptane-2-ketone is obtained from wetland streptomyces for the first time, and the 7-(10-methyl undecyl) azacycloheptane-2-ketone has a relatively strong inhibition effect on alpha-glucosidase and can be used for preparing a medicine for treating diabetes.

The present invention provides a curable composition comprising a reactive silicon group-containing organic polymer, wherein the curability is improved and the composition exhibits a low modulus after curing. [Solution] A curable composition containing an organic polymer (A) having a reactive silicon group and a curing catalyst (B). The reactive silicon group is of formula:-SiR 1 3-a X a (R 1 is a substituted or unsubstituted hydrocarbon group having 1 to 20 carbon atoms, or R 0 Represents a triorganosiloxy group represented as 3SiO-. 0 ) represents a hydrocarbon group having 1 to 20 carbon atoms. X represents a hydroxyl group or a hydrolyzable group. a represents 1, 2, or 3. The curing catalyst (B) comprises a tin carboxylate compound (b1), a cyclic secondary amine compound (b2), and a β-dicarbonyl compound (b3), wherein compound (b2) has one or more skeletons selected from the group consisting of a pyrrolidine skeleton, a piperidine skeleton, a piperazine skeleton, and an azepane skeleton.

The application relates to the technical field of nanogel, and discloses a functional polyurea nanogel with universal drug loading capacity as well as a preparation method and application thereof. A functional modified polyurea compound comprises the following raw materials: a double primary amine compound, a double (2-oxoazepan-1-formamide alkyl) amine, a polyethylene glycol-amino compound, N,N'-carbonyl bis (caprolactam), an acid anhydride and an organic solvent. The functional modified polyurea compound provided by the application is free of isocyanate groups and has high biological safety; the functional polyurea nanogel synthesized from the functional modified polyurea compound has high biological safety, charge flipping performance, multiple intermolecular non-covalent interactions including hydrogen bond interaction, electrostatic interaction and hydrophobic interaction, can be used for universal drug loading, and has pH value responsive swelling properties and can be used for pH responsive drug release.

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

This curable composition comprises an organic polymer (A) having a reactive silicon group and a curing catalyst (B), wherein: the curing catalyst (B) contains a carboxylic acid metal compound (b1) and a cyclic secondary amine compound (b2); the carboxylic acid metal compound (b1) contains at least one metal selected from the group consisting of tin, titanium, bismuth, zirconium, iron, aluminum, and zinc; and the cyclic secondary amine compound (b2) has at least one skeleton selected from the group consisting of a pyrrolidine skeleton, a piperidine skeleton, a piperazine skeleton, and an azepane skeleton.