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 10):
A method for preparing the crystal according to  claim 8 , which is one of the following preparation methods A and B:\n preparation method A, comprising: 1) dissolving Compound 1 hydrochloride in water; 2a) cooling the aqueous solution of step 1) to crystallize; or 2b) adding sodium chloride to the aqueous solution of step 1) and stirring to crystallize; and 3) filtering, and drying, to give Crystal Form VII; preferably, in step 1), the amount of water used is 10 to 500 times, for example, 20 to 200 times, such as 60 or 180 times, the weight of Compound 1 hydrochloride; preferably, water is heated before or after Compound 1 hydrochloride is added; preferably, a step of hot filtration to remove insolubles is also included; water may be heated to 70-100\u00b0 C., such as 75\u00b0 C., 80\u00b0 C., 85\u00b0 C., 90\u00b0 C. or 95\u00b0 C.; in step 2a), the aqueous solution of step 1) is cooled down to below 40\u00b0 C., for example, below 30\u00b0 C., such as at 20-25\u00b0 C., to crystallize; in step 2b), the solution is stirred at below 40\u00b0 C., for example, below 30\u00b0 C., such as 20 to 25\u00b0 C., to crystallize; sodium chloride may be in a suitable form thereof, for example, a sodium chloride solution or sodium chloride solid may be used; preferably, sodium chloride is added and then dissolved by stirring; for example, the amount of sodium chloride used may be 1 to 15 times, for example, 4 to 8 times, that of Compound 1 hydrochloride; in step 3), the filtering may be filtering by suction, and the drying may be drying in vacuo; or, preparation method B, comprising: mixing and beating one or more of the above-mentioned Crystal Forms I-VI with water for 3 days to give Crystal Form VII preferably, the mixing and beating in the method are performed at below 40\u00b0 C., for example, below 30\u00b0 C., such as at 20-25\u00b0 C.; the amount of water used in the mixing and beating is 20 to 200 times, for example, 100 times, the total weight of Crystal Forms I-VI.

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): 0.7779234031077179
- 35 USC 102 Novelty (BERT): 0.5047041436534947
- Combined Prediction Score: 0.7506014771622956
- Mean Citation Score: 283.1884639999999
- Max Citation Score: 293.41843
- Similarity Product: 225.89059642061832

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