Abstract: The present application relates to a crystalline sulfamide compound, and in particular relates to a crystalline (S)—N—((S)-1-(2-chlorphenyl)-2-((3,3-difluorocyclobutyl)amido)-2oxoethyl)-2-(4-cyanopyridin-2-base)-N-(3-fluorophenyl)-isothiazolidine-3-formamide 1,1-dioxide, and a preparation method therefor, a crystalline composition, a pharmaceutical composition and uses thereof. An X-ray powder diffraction spectrum of a crystalline hydrate of formula II of the present application has diffraction peaks at positions of about 14.40°, 20.28°, 20.94°, 22.02°, and 24.46°, represented by 2?. The crystalline hydrate of formula II of the present application has good IDH1 inhibitory activity and performs high stability, and therefore has advantages in physical property, safety and metabolic stability, and has high medicine value.

Abstract: The present application relates to a crystal of a tricyclic compound, in particular to a crystal of (S)-8-(4,4-difluorocyclohexyl)-8H-thieno[3,4]pyrrolo[1,5-a]imidazole, a preparation method therefor, a crystal composition and a pharmaceutical composition thereof and the use thereof. The X-ray powder diffraction spectrum of the crystal of the compound of formula I in the present application, represented by a 2? value, has a diffraction peak at about 11.49°, 15.05°, 20.14°, 21.53° or 21.79°. The crystal of the compound of formula I in the present application has excellent physical properties, high safety and metabolic stability, and has a good inhibitory effect on IDO and a high medicinal value.

Abstract: An iridinesulfonamide compound having isocitrate dehydrogenase 1 (IDH1) inhibitory activity, pharmaceutically acceptable salts, solvates or hydrates thereof, a pharmaceutical composition, as well as use of the compound or the pharmaceutically acceptable salts, solvates or hydrates thereof, and the pharmaceutical composition thereof in treating IDH1 mutation induced cancer.

Abstract: The present invention relates to a structurally novel TLR8 (Toll-like receptor 8) agonist and, in particular, to a compound thereof of formula (I), a pharmaceutically acceptable salt and an isomer thereof.

Abstract: The present application relates to a method for preparing trifluridine, comprising reacting a compound of formula III with a compound of formula IV in a first solvent in the presence of an acid to obtain a compound of formula II, and performing further reaction to obtain trifluridine.

Abstract: The present application relates to the field of pharmaceutical technology, specifically to the crystal habit and crystalline powder preparation of quinoline derivatives, and more specifically, to the crystal habit and crystalline powder preparation of anlotinib dihydrochloride. The compound of formula II disclosed herein is a crystalline powder with a flaky crystal habit having a specific surface area ?10 m2/g and a particle-size distribution of X50?50 ?m and/or X90?500 ?m, such that a large specific surface area is provided without reducing the particle size of the drug by a physical method under the condition of a broad particle-size distribution, and the drug can rapidly dissolving. In addition to excellent dissolution property, the crystalline powder is also beneficial to industrial manufacturing, featuring simplified process and cost-efficiency.

Abstract: A solid pharmaceutical composition containing a 1,3,5-triazine derivative or a pharmaceutically acceptable salt thereof and a preparation method therefor. In particular, involved are a solid pharmaceutical composition containing 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazine-2-amine or a pharmaceutically acceptable salt thereof and a preparation method therefor. The solid pharmaceutical composition has a good stability, a fast dissolution rate and a high bioavailability, and is suitable for clinical production and use.

Abstract: The present application relates to a method for preparing a cholic acid compound. Specifically, the method prepares a compound as shown in formula I, including subjecting a compound of formula 2 to an oxidization reaction to obtain a compound of formula 3; attaching a trimethylsilyl group to the compound of formula 3 to obtain a compound of formula 4; reacting the compound of formula 4 with acetaldehyde to obtain a compound of formula 5; subjecting the compound of formula 5 to a catalytic hydrogenation reaction to obtain a compound of formula 6; and converting a cyano group of the compound of formula 6 to a carboxyl group to give the compound of formula I.

Abstract: The present application relates to a macrocycle containing aminopyrazole and pyrimidine, which is represented by formula (I), a pharmaceutical composition thereof, and a use thereof in inhibiting tropomyosin receptor kinase (Trk) activity and in treating diseases in mammals that are mediated by Trk.

Abstract: Disclosed herein a crystal structure of a caspase inhibitor, and more specifically a crystal structure of an (S)-3-((S)-2-(5-(2-chlorophenyl)isoxazole-3-formylamide)proponamide)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)valeric acid, a preparation method therefor, a crystal polymer, a pharmaceutical composition and uses thereof. The compound A of formula (I) disclosed herein exhibits high crystal structure stability, low hygroscopicity, and advantageously shows physical properties, safety and metabolic stability while having relatively high pharmaceutical value.

Abstract: Provided are a Syk inhibitor and a use method therefor, and in particular, disclosed are quinolinone represented by formula (I) or quinazoline derivatives or pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition, and uses in preparing a medicament for treatment of Syk receptor related diseases.

Abstract: The present invention falls within the field of pharmaceutical chemistry, and relates to a method for preparing a steroid derivative FXR agonist and relevant intermediates. In particular, the present invention relates to a method for preparing a compound of formula I, comprising reacting a compound of formula 8 with a compound of formula 9 to obtain a compound of formula 10, obtaining a compound of formula 11 from a reaction of the compound of formula 10, and obtaining the compound of formula I from a reaction of the compound of formula 11, as well as the intermediates used, the methods for preparing the intermediates and the use of the intermediates. The reaction conditions of the preparation method are mild, and some of the steps can convert multiple groups simultaneously, thereby effectively shortening the sequence of steps. The preparation method is suitable for industrialized production.

Abstract: Disclosed are a crystalline or amorphous form of steroid derivative FXR agonist (formula I), and a preparation method therefor, and a crystalline composition and pharmaceutical composition comprising the crystalline or amorphous form, and the use of same in the preparation of a drug for treating or preventing various conditions associated with FXR.

Abstract: The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.

Abstract: Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.

Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.

Abstract: The present application falls within the field of medicinal chemistry, relates to the crystalline of a compound as a c-Met kinase inhibitor, and specifically relates to the crystalline of N-(4-((7-((1-(cyclopentylamino)cyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-3-fluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and a preparation method therefor, a crystalline composition thereof, and a pharmaceutical composition thereof, as well as the use of the crystalline for treating diseases associated with the inhibition of growth factor receptor protein tyrosine kinase activity. The crystalline of the present application has excellent properties in at least one of the following aspects: pharmacokinetics, bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, etc.

Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

Abstract: A pharmaceutical composition comprising dabigatran etexilate, and preparation method and use thereof, and solid preparation comprising the pharmaceutical composition; the pharmaceutical composition comprises a vitamin C layer and a dabigatran etexilate layer separated by a semipermeable film layer, and the semipermeable film layer comprises a water-soluble compound, a water-insoluble compound and an optional anti-sticking agent and/or plasticizer.