10 results about "Azetidine derivative" patented technology

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.

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.

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 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.