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.
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.
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
A61K 31/553 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
2.
PREPARATION METHOD OF NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
Disclosed is a preparation method of a nitrogen-containing heterocyclic compound represented by formula (I). The method comprises: carrying out a coupling reaction on a compound 1A and a compound 2a, and sequentially carrying out deprotection, amidation and deprotection reactions, which are four steps in total, to obtain a target compound. The method is short in reaction route, mild in condition, simple to operate, convenient in post-treatment, high in yield and high in purity, and is suitable for industrial amplification production.
Disclosed is a preparation method of a nitrogen-containing heterocyclic compound represented by formula (I). The method comprises: carrying out a coupling reaction on a compound 1A and a compound 2a, and sequentially carrying out deprotection, amidation and deprotection reactions, which are four steps in total, to obtain a target compound. The method is short in reaction route, mild in condition, simple to operate, convenient in post-treatment, high in yield and high in purity, and is suitable for industrial amplification production.
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
3.
DIPEPTIDYL PEPTIDASE 1 INHIBITOR POLYMORPH, PREPARATION METHOD AND USE THEREFOR
Disclosed in the present invention are a polymorph of a compound as shown in formula I, and a preparation method and use therefor. The polymorph of the present invention comprises a crystal form B, a crystal form C, and a crystal form D. The polymorph has excellent characteristics of high purity, good solubility, stable physical and chemical properties, resistance to high temperature, high humidity, and strong illumination, low hygroscopicity, etc.
Disclosed in the present invention are a polymorph of a compound as shown in formula I, and a preparation method and use therefor. The polymorph of the present invention comprises a crystal form B, a crystal form C, and a crystal form D. The polymorph has excellent characteristics of high purity, good solubility, stable physical and chemical properties, resistance to high temperature, high humidity, and strong illumination, low hygroscopicity, etc.
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
4.
DPP1 INHIBITOR INTERMEDIATE, AND PREPARATION METHOD THEREFOR AND USE THEREOF IN MEDICINES
The present invention relates to a compound as represented by formula (I) and a method for preparing an intermediate thereof. The method uses inexpensive starting materials and multi-step telescoping reactions, is simple and convenient in terms of post-treatment operation, achieves a high yield, is high in terms of the chemical and chiral purity of a product, and is suitable for large-scale industrial production.
C07C 269/04 - Préparation de dérivés d'acide carbamique, c.-à-d. de composés contenant l'un des groupes l'atome d'azote ne faisant pas partie de groupes nitro ou nitroso à partir d'amines avec formation de groupes carbamate
5.
PHARMACEUTICAL COMPOSITION CONTAINING DIPEPTIDYL PEPTIDASE SMALL MOLECULE INHIBITOR
A pharmaceutical composition containing a dipeptidyl peptidase 1 (DPP1) small molecule inhibitor compound A, a preparation method therefor, and a use thereof in treatment of diseases or conditions associated with fibrosis bronchiectasis.
A61K 31/553 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
Disclosed is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used to prepare a drug for treating diseases including obstructive airway diseases, bronchiectasis, cystic fibrosis, asthma, emphysema, and chronic obstructive pulmonary diseases.
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 267/10 - Cycles à sept chaînons les hétéro-atomes étant en positions 1, 4 non condensés avec d'autres cycles
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07F 9/6527 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle
7.
SALT OF COMPOUND FOR DEGRADING BTK, CRYSTAL FORM THEREOF, AND USE THEREOF IN MEDICINE
Provided are a salt of a compound for degrading BTK, and/or a crystal form, preparation therefor, and an application thereof. The pharmaceutical salt of the compound as shown in formula (I) and the crystal form, wherein the pharmaceutical salt is selected from maleate, fumarate, halogen acid salt (preferably hydrobromide and hydrochloride), sulfate, phosphate, L-tartrate, citrate, L-malate, hippurate, D-glucuronate, glycollate, mucate, succinate, lactate, orotate, pamoate, glycinate, alanine salt, arginine salt, cinnamate, benzoate, benzenesulfonate, p-toluenesulfonate, acetate, propionate, valerianate, triphenyl acetate, L-proline salt, ferulate, 2-hydroxyethanesulfonate, mandelate, nitrate, mesylate, malonate, gentisate, salicylate, oxalate, or glutarate:
Provided are a salt of a compound for degrading BTK, and/or a crystal form, preparation therefor, and an application thereof. The pharmaceutical salt of the compound as shown in formula (I) and the crystal form, wherein the pharmaceutical salt is selected from maleate, fumarate, halogen acid salt (preferably hydrobromide and hydrochloride), sulfate, phosphate, L-tartrate, citrate, L-malate, hippurate, D-glucuronate, glycollate, mucate, succinate, lactate, orotate, pamoate, glycinate, alanine salt, arginine salt, cinnamate, benzoate, benzenesulfonate, p-toluenesulfonate, acetate, propionate, valerianate, triphenyl acetate, L-proline salt, ferulate, 2-hydroxyethanesulfonate, mandelate, nitrate, mesylate, malonate, gentisate, salicylate, oxalate, or glutarate:
A method for preparing a compound as represented by formula (I) and an intermediate thereof. The method has mild reaction conditions, does not involve a high-temperature and high-pressure reaction, has low-toxicity or non-toxicity raw materials, simple operation, a high reaction yield, a high product purity, convenient work-up, and good reproducibility, and is suitable for industrial production.
A method for preparing a compound as represented by formula (I) and an intermediate thereof. The method has mild reaction conditions, does not involve a high-temperature and high-pressure reaction, has low-toxicity or non-toxicity raw materials, simple operation, a high reaction yield, a high product purity, convenient work-up, and good reproducibility, and is suitable for industrial production.
Disclosed is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used to prepare a drug for treating diseases including obstructive airway diseases, bronchiectasis, cystic fibrosis, asthma, emphysema, and chronic obstructive pulmonary diseases.
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 267/10 - Cycles à sept chaînons les hétéro-atomes étant en positions 1, 4 non condensés avec d'autres cycles
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07F 9/6527 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle
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