PATENT CLAIM ANALYSIS

Application Number: 15755558
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-09
Patent Classification: ["514", "468000"]

Abstract:
A derivative of  inula lineariifolia  lactone A, and in particular, a dimethylamine 4-O-acetyl  inula lineariifolia  lactone A or a salt thereof, preparation of same, and an application of same in preparation of medicine for treating multiple sclerosis. The dimethylamine 4-O-acetyl  inula lineariifolia  lactone A compound is represented by formula I:

Claim (Index 6):
A preparation method of a dimethylamine 4-O-acetyl  inula lineariifolia  lactone A compound and its pharmaceutically acceptable salt, comprising the following steps of:\n (I) preparing the dimethylamine 4-O-acetyl  inula lineariifolia  lactone A compound, comprising the following steps of:\n (1) adding an organic solvent to dissolve  inula lineariifolia  lactone A, a base and acetic anhydride (Ac 2 O) in a reaction container, stirring at 0-50\u00b0 C. for 12-24 hours, TLC monitoring the reaction until the reaction material is consumed completely and then quenched by water, and retaining an organic layer; \n (2) extracting the organic layer with water several times until a reaction product 4-O-acetyl  inula lineariifolia  lactone A in the organic layer is pure without other impurities by TLC monitoring, discarding an aqueous layer, washing the organic layer with saturated brine, drying with anhydrous sodium sulfate (Na 2 SO 4 ), and concentrating to 1/10-1/20 of an original volume under reduced pressure 0.01-0.1 MPa at 20-80\u00b0 C.; \n (3) purifying a concentrated solution by silica-gel column chromatography with gradient elution using petroleum ether (PE)/ethyl acetate (EA) 15:1-5:1 to obtain 4-O-acetyl  inula lineariifolia  lactone A, monitored by TLC;\n its reaction equation being shown below: \n \n (4) adding an organic solvent to dissolve the 4-O-acetyl  inula lineariifolia  lactone A and dimethylamine hydrochloride (CH 3 NHCH 3 .HCl) in a reaction container disposed in a cooling tank at \u221220 to 0\u00b0 C., slowly adding a base, then slowly increasing a temperature of the reaction mixture to room temperature 25-30\u00b0 C., and stirring for 2-12 hours, the reaction being monitored by TLC, until the reaction material is consumed completely, evaporating the solvent under reduced pressure 0.01-0.1 MPa at 20-80\u00b0 C. to obtain a rude product, then adding an organic reagent to dissolve the rude product, extracting with water, discarding an aqueous layer, repeating the same procedure until a reaction product dimethylamino-4-O-acetyl  inula lineariifolia  lactone A in an organic layer is pure without other impurities by TLC monitoring, washing the organic layer with saturated brine, drying with anhydrous sodium sulfate (Na 2 SO 4 ), performing silica-gel column chromatography with gradient elution using PE/EA 15:1-1:1, monitored by TLC, collecting eluent including the dimethylamino-4-O-acetyl  inula lineariifolia  lactone A compound (compound I), evaporating the solvent under reduced pressure 0.01-0.1 MPa at 20-80\u00b0 C. to obtain the compound I;\n its reaction equation being shown below: \n (II) preparing the salt of dimethylamino-4-O-acetyl  inula lineariifolia  lactone A compound: 1.0eq of compound I being dissolved in a solvent, and being stirred with 1.0-1.5eq of an acid (HX) at 0-50\u00b0 C. for 2-24 hours, concentrating under reduced pressure 0.01-0.1 MPa at 20-80\u00b0 C. to obtaining the salt of compound II,\n its reaction equation being shown below:

Metadata:
- Claim Count in Document: 41.0
- Percentile: 88.0
- Lexical Diversity: 1.64706
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15504018', '11404267', '13119692', '15101582', '10530776']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7146396360487189
- 35 USC 102 Novelty (BERT): 0.5047540533389707
- Combined Prediction Score: 0.6936510777777442
- Mean Citation Score: 227.362856
- Max Citation Score: 233.85928
- Similarity Product: 163.66281221158982

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 0
- Combined Label: 1
- Label 101 Adjusted: 0

Dataset: test