14 results about "Azetidine derivative" patented technology

The invention relates to the technical field of medicinal chemistry and organic synthetic chemistry, in particular to a preparation method of a 1, 3-amino ether compound. The preparation method comprises the following steps: in an inert atmosphere, taking an azetidine derivative and a hydroxyl-containing compound as raw materials, taking aryl diazonium salt as a catalyst, and carrying out regioselective nucleophilic ring-opening reaction on the azetidine derivative and the hydroxyl-containing compound in the presence of an organic solvent, so as to obtain the 1, 3-amino ether compound. The aryl diazonium salt is used as the catalyst, so that the use of a traditional metal salt catalyst is avoided. Compared with a traditional method, the problem that metal salt residues are difficult to thoroughly remove is solved, and the dosage of the catalyst is remarkably reduced. Meanwhile, the preparation method disclosed by the invention realizes efficient and high-selectivity preparation of the 1, 3-amino ether compound.

This invention relates to the ability of formula (I) to function as α v Novel compounds of β6 integrin antagonists, their use in treating diseases, methods of their manufacture, and compositions comprising said compounds for this purpose, wherein R 1 Selected from: R 1a 、-C(O)R 1a -C(O)OR 1a -C(O)NHR 1a 、-C(O)N(R 1a )2、-SO2R 1a , where R 1a Each is independently selected from: alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylaryl, or alkylheteraryl, wherein each can be optionally substituted; R 2 Selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxy; R 2a Each is independently selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxy; R 3 Selected from: hydrogen, optionally substituted alkyl, or optionally substituted alkoxy; R 4 For hydroxyl group; Ar 1 It is optionally substituted heteroaryl or bicyclic heteroaryl; and L is a linker; or a pharmaceutically acceptable salt thereof.

This solution discloses an azetidine derivative in the field of organic chemistry and its preparation and application. The chemical structure of the azetidine derivative is generally represented by formula III: #imgabs0# wherein R 1 is one of methyl, ethyl, cyclopropyl, phenyl, substituted phenyl, and thiazolyl; R 2 The azetidine derivative has significant antibacterial activity and can be used to prepare drugs for treating S. aureus, E. coli, and MRSA infections. It can also be used in combination with other antibacterial active substances.

The present invention relates to the field of medicine, relates to a substituted azetidine derivative, a preparation method therefor, and a medical use thereof, and specifically relates to a compound represented by general formula I or a pharmaceutically acceptable salt or stereoisomer thereof, a pharmaceutical composition comprising the compound, and a use thereof in the field of medicine. The present invention also relates to a method for preparing the compound, and an intermediate.

The invention relates to a compound shown in a general formula I or pharmaceutically acceptable salt, stereoisomer, tautomer and deuterated compound thereof, a composition containing the compound, a preparation method of the compound, an intermediate and application of the compound in the field of medicine.

Provided is the use of the compound of formula I, its pharmaceutically acceptable salt, stereoisomer, polymorph, solvate, metabolite or prodrug, or their composition in the preparation of the medicine for treating alopecia such as alopecia areata.Azetidine derivative has a clear mechanism of action and pharmacodynamic effect, good pharmacokinetic properties and good safety, and greatly improves patient's compliance with medication.

The invention relates to an azetidine derivative, a preparation method thereof, an intermediate, a composition containing the azetidine derivative and application of the azetidine derivative in the field of medicine. Particularly, the invention relates to an azetidine derivative shown in a general formula I, a preparation method and an intermediate of the azetidine derivative, a pharmaceutical composition containing the azetidine derivative, and application of the azetidine derivative or the pharmaceutical composition of the azetidine derivative as an M4 receptor modulator in preparation of drugs for preventing and / or treating M4 receptor related diseases.

The present invention relates to compounds of formula (I) or a salt, stereoisomer, tautomer or N-oxide thereof. Furthermore, the present invention relates to compounds of formula (I), or a salt, stereoisomer, tautomer or N-oxide thereof, which are suitable for inducing and / or stimulating the process of autophagy, as well as compounds of formula (I) for use in medicine and for use in the treatment of autophagy-related diseases.

A method for preparing an azetidine derivative, comprising the following steps: using proline hydrochloride as a raw material, esterifying L-proline hydrochloride or D-proline hydrochloride to obtain a compound of formula 3; reacting the compound of formula 3 with epichlorohydrin to obtain a compound of formula 4S or 4R, subjecting the compound of formula 4S or 4R to a cyclization reaction to obtain a compound of formula 5R or 5S, performing a fluorination reaction on the compound of formula 5R or 5S to obtain a compound of formula 6, and reducing the compound of formula 6 to obtain the azetidine derivative of formula 1. This application is a synthetic route starting from L-proline hydrochloride. The improved route has only 5 or 6 reaction steps, and the raw materials are all cheap and easily available. The relatively costly fluorination and reduction reactions are also in the later stage of the route. Therefore, this route has high value.

The invention discloses a preparation method of an azetidine derivative, which comprises the following steps: by taking tert-butyl azetidine-3-yl carbamate as a raw material, carrying out amino protection, nitrogen methylation and catalytic hydrogenolysis debenzylation to obtain a target product tert-butyl (methyl) (azetidine-3-yl methyl) carbamate. The synthetic route is mild in reaction condition, simple and convenient to operate, relatively high in reaction yield in each step, high in product purity, good in total yield and suitable for large-scale production, and can be widely applied to the fields of medicines and organic synthesis as a key intermediate.

The present invention generally relates to compounds inhibiting dipeptidyl peptidase 1 activity; particularly the invention relates to compounds that are azetidine derivatives, including pharmaceutically acceptable salts thereof, methods of preparing such compounds, and therapeutic use thereof. The compounds of the invention may be useful for instance in the treatment of many disorders associated with DPP1 receptors mechanisms, in particular respiratory diseases.

The invention relates to novel compounds of formula (I), the compounds being capable of acting as avβ6 integrin antagonists, their use in the treatment of disease, their methods of manufacture and compositions comprising said compounds for such purposes (I) wherein R1 is selected from: R1a, —C(O)R1a, —C(O)OR1a —C(O)NHR1a, —C(O)N(R1a)2, —SO2R1a, wherein R1a are each independently selected from: alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl, each of which may be optionally substituted; R2 is selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxyl; R2a are each independently selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxyl; R3 is selected from: hydrogen, optionally substituted alkyl or optionally substituted alkoxyl; R4 is hydroxyl; Ar1 is an optionally substituted heteroaryl or bicyclic heteroaryl; and L is a linker; or a pharmaceutically acceptable salt thereof.

The invention relates to an azetidine derivative, a preparation method thereof, an intermediate, a composition containing the azetidine derivative and application of the azetidine derivative in the field of medicine. In particular, the present application relates to an azetidine derivative represented by general formula (I), a preparation method and an intermediate thereof, a pharmaceutical composition containing the azetidine derivative, and an application of the azetidine derivative or the pharmaceutical composition thereof as an M4 receptor modulator in preparation of drugs for prevention and / or treatment of M4 receptor related diseases.