PATENT CLAIM ANALYSIS

Application Number: 16064242
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-12
Patent Classification: ["544", "106000"]

Abstract:
The present invention relates to the crystal form of imidazolone type compounds, and a preparation method, pharmaceutical composition and use thereof, and falls within the field of pharmaceutical compound crystals. The crystal form provided by the present invention has a good stability, comprising good stability under the three extreme conditions of high temperature, high humidity and strong illumination, and can also maintain a good stability during the tablet compressing process. The crystal form provided by the present invention has good absorption and metabolism properties in vivo, comprising the drug concentration of blood, the drug concentration-time curve AUC, the half-life period, etc. In addition, the dissolving rate of the crystal form of the present invention is improved, wherein same is beneficial for the applications thereof in preparations.

Claim (Index 9):
A method for preparing the crystal according to  claim 2 , which is one of the following preparation methods A and B:\n preparation method A, comprising: 1) dissolving Compound 1 hydrochloride in water; 2) adding sodium chloride to the solution of step 1); and 3) cooling down, crystallizing, filtering, and drying to give Crystal Form I, preferably, in step 1), water may be heated before or after the addition of Compound 1 hydrochloride to dissolve Compound 1 hydrochloride; wherein water may be used in an amount 2-80 times, for example, 4-70 times, 6-60 times, 8-50 times, or 10-25 times, the weight of Compound 1 hydrochloride; and water may be heated to, for example, 70-100\u00b0 C., such as 75\u00b0 C., 80\u00b0 C., 85\u00b0 C., 90\u00b0 C. or 95\u00b0 C.; in step 2), sodium chloride may be added while maintaining the temperature of the solution of step 1); as an example, the amount of sodium chloride may be controlled so that it makes up 0.1-26%, for example, 0.5-20%, 0.8-15%, or 1-10%, for example, 3-5%, of the total weight of the solution; said sodium chloride may be in its suitable form, for example, a sodium chloride solution or sodium chloride solid can be used; preferably, sodium chloride is added and then stirred to dissolve; the sodium chloride solution is preferably an aqueous solution of sodium chloride, wherein the weight percentage content of sodium chloride may be in the range from 10% to the saturated concentration, for example, 12%, 15%, 16%, 17%, 18%, 20%, 22%, 24%, 25%, or 26%; in step 3), the mixture may be slowly cooled down to below 60\u00b0 C. (e.g., 20 to 50\u00b0 C.) under stirring to crystallize, followed by filtration by suction, rinsing, and drying in vacuo at 15-35\u00b0 C. (e.g., 20\u00b0 C., 25\u00b0 C., or 30\u00b0 C.), to give Crystal Form I of Compound 1 hydrochloride monohydrate; or, preparation method B, comprising: 1) dissolving Compound 1 hydrochloride in an aqueous solution of ethanol; and 2) cooling down, crystallizing, filtering, and drying to give Crystal Form I. preferably, in step 1), the aqueous solution of ethanol may be heated before or after the addition of Compound 1 hydrochloride to dissolve Compound 1 hydrochloride; wherein the amount of the aqueous solution of ethanol used may be 5-80 times, for example, 10-70 times, 20-60 times, or 30-50 times the weight of Compound 1 hydrochloride; the aqueous solution of ethanol may be heated to, for example, 50-100\u00b0 C., e.g., 55\u00b0 C., 60\u00b0 C., 65\u00b0 C., 70\u00b0 C., 75\u00b0 C., 80\u00b0 C., 85\u00b0 C., 90\u00b0 C. or 95\u00b0 C.; the mass percentage of ethanol in the aqueous solution of ethanol may be, for example, 30 to 99%, such as 40 to 98%, 45 to 95%, 46 to 85%, 48 to 80%, 50 to 75%, or 60 to 70%; in step 2), the mixture may be slowly cooled down to below 40\u00b0 C. (e.g., 20 to 30\u00b0 C.) under stirring to crystallize, followed by filtration by suction, and drying in vacuo at 15 to 35\u00b0 C. (e.g., room temperature, i.e. 25\u00b0 C.) to give Crystal Form I of Compound 1 hydrochloride monohydrate.

Metadata:
- Claim Count in Document: 7.0
- Percentile: 94.0
- Lexical Diversity: 1.89333
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16065880', '15820241', '15186415', '16065884', '16318055']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.77778146089192
- 35 USC 102 Novelty (BERT): 0.5059606354995032
- Combined Prediction Score: 0.7505993783526783
- Mean Citation Score: 283.1884639999999
- Max Citation Score: 293.41843
- Similarity Product: 219.8440369640797

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test