PATENT CLAIM ANALYSIS

Application Number: 16075514
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-02
Patent Classification: ["514", "254000"]

Abstract:
The present disclosure provides a posaconazole derivative, a pharmaceutical composition and use thereof, which specifically include a compound represented by the following formula (I), a racemate, stereoisomer, tautomer, oxynitride, or a pharmaceutically acceptable salt thereof: The compounds of the present disclosure have strong antifungal activity, high safety, and good water solubility, without the need for the addition of a cosolvent (such as hydroxypropyl-β-cyclodextrin, sulfobutyl ether-β-cyclodextrin, and the like) with potential safety risks. Furthermore, the formulation process of the compound could have less difficulty and less cost, and therefore can be used to prepare improved antifungal drugs.

Claim (Index 5):
The compound, racemate, stereoisomer, tautomer, oxynitride, or pharmaceutically acceptable salt thereof according to  claim 1 , wherein the pharmaceutically acceptable salt of the compounds of formula (I) includes, but is not limited to:\n alkali metal salts, alkaline earth metal salts, ammonium salts of compounds of formula (I), or salts of compounds of formula (I) with organic bases providing physiologically acceptable cations, for example salts of compounds of formula (I) formed with sodium ion, potassium ion, calcium ion, magnesium ion, N-methylglucosamine, dimethylglucosamine, ethylglucosamine, lysine, dicyclohexylamine, 1,6-hexamethylenediamine, ethanolamine, glycosamine, meglumine, sarcosine, serinol, trishydroxymethyl aminomethane, aminopropylene glycol, 1-amino-2,3,4-butanetriol; for example, when 1, 2, or 3 of M 1 , M 2 , and M 3  is/are H, the pharmaceutically acceptable salt includes, for example, salts formed from \u2014OP(O)(OM 1 )(OM 2 ), \u2014P(O)(OM 1 )(OM 2 ), \u2014OS(O) 2 OM 3 , or \u2014S(O) 2 OM 3 , with, for example, above-mentioned sodium ion, potassium ion, ammonium ion, and the like; or alternatively, acid addition salts of compounds of formula (I) with the following acids: inorganic acids such as hydrochloric acid, hydrofluoric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, pyrosulfuric acid, phosphoric acid or nitric acid; organic acids such as formic acid, acetic acid, acetoacetic acid, pyruvic acid, trifluoroacetic acid, propionic acid, butyric acid, caproic acid, heptanoic acid, undecanoic acid, lauric acid, benzoic acid, salicylic acid, 2-(4-hydroxyl) benzoyl) benzoic acid, camphoric acid, cinnamic acid, cyclopentane propionic acid, digluconic acid, 3-hydroxy-2-naphthoic acid, nicotinic acid, embonic acid, pectinic acid, persulfuric acid, 3-phenyl propionic acid, picric acid, pivalic acid, 2-hydroxyethanesulfonic acid, itaconic acid, sulfamic acid, trifluoromethanesulfonic acid, dodecyl sulfate, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, methanesulfonic acid, 2-naphthalenesulfonic acid, naphthalene disulfonic acid, camphorsulfonic acid, citric acid, tartaric acid, stearic acid, lactic acid, oxalic acid, malonic acid, succinic acid, malic acid, adipic acid, alginic acid, maleic acid, fumaric acid, D-gluconic acid, mandelic acid, ascorbic acid, gluconic acid, glycerophosphoric acid, aspartic acid, sulfosalicylic acid, hemisulfuric acid or thiocyanic acid.

Metadata:
- Claim Count in Document: 23.0
- Percentile: 96.0
- Lexical Diversity: 1.56
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['12226286', '12421230', '15380836', '10984522', '10984093']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7591939483793145
- 35 USC 102 Novelty (BERT): 0.5188066789546679
- Combined Prediction Score: 0.7351552214368499
- Mean Citation Score: 272.868316
- Max Citation Score: 278.55414
- Similarity Product: 193.46198488381145

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

Dataset: test