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 7):
A method for preparing the compound, racemate, stereoisomer, tautomer, oxynitride, or pharmaceutically acceptable salt thereof according to  claim 1 , comprising using the compound represented by the following formula (II) as a raw material to obtain the compound of the formula (I): wherein X 1  and X 2  have the definitions of  claim 1 ; preferably, the preparation method includes, for example, reacting a compound of the formula (II) with a compound R z -L, wherein R z  is selected from R h , R t  or a group that can be derivatized as R h  or R t ; R h  and R t  have the definitions of  claim 1 , and L is a leaving group; for example, R z -L can be selected from R h -L 1  or R t -L 2 , wherein R h  and R t  have definitions as defined in  claim 1 , and L 1  and L 2  are leaving groups; wherein the leaving group represents a charged or uncharged atom or group that is detached during the substitution or displacement reaction; for example, H, F, Br, Cl, I, mesylate ester group, tosylate ester group, and the like; the preparation method can be carried out in the presence of a catalyst; for example, the preparation method can be performed in the absence of solvent or in the presence of a solvent; if desired, the compound of formula (II) can be first reacted with R h -L 1  and the resulting compound can be further reacted with R t -L 2 ; alternatively, the compound of formula (II) is first reacted with R t -L 2 , and the resulting compound is further reacted with R h -L 1 ; if desired, one or more functional groups in the compound of formula (II) and/or compound R z -L can be first protected with a protecting group (PG) and then subjected to the reaction.

Metadata:
- Claim Count in Document: 23.0
- Percentile: 96.0
- Lexical Diversity: 1.56
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12226286', '12421230', '15380836', '10984522', '10984093']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.736716151204097
- 35 USC 102 Novelty (BERT): 0.5170564729119215
- Combined Prediction Score: 0.7147501833748795
- Mean Citation Score: 272.868316
- Max Citation Score: 278.55414
- Similarity Product: 191.3671691620732

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