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 2):
The compound, racemate, stereoisomer, tautomer, oxynitride, or pharmaceutically acceptable salt thereof according to  claim 1 , wherein:\n X 1  and X 2  are independently from each other selected from F, C 1  or Br; X 3  can represent an acid ion generated by ionization of an inorganic acid or an organic acid; for example, X 3  can represent a monovalent acid ion generated by ionization of an inorganic or organic acid; alternatively, when a plurality of cations are present in the structure of the compound of formula (I), X 3  can represent a plurality of monovalent acid ions generated by ionization of an inorganic acid or an organic acid, preferably 2 or 3 monovalent acid ions generated by ionization of an inorganic acid or an organic acid; alternatively, when a plurality of cations in the structure of the compound of formula (I) share one polyvalent acid ion, X 3  can also represent a part of the polyvalent acid ion, for example, \u00bd, \u2153, \u2154 of the polyvalent acid ion; alternatively, X 3  can also represent a mixture of the monovalent acid ions as mentioned above, a mixture of the polyvalent acid ions as mentioned above, or a mixture of the monovalent acid ions and the polyvalent acid ions as mentioned above; for example, X 3  can represent Cl \u2212 , Br \u2212 , I \u2212 , HSO 4 \u2212 , NO 3 \u2212 , \u00bdSO 4 2\u2212 , SO 4 2\u2212 , 3/2SO 4 2\u2212 , H 2 PO 4 \u2212 , \u00bdHPO 4 2\u2212 , 3/2HPO 4 2\u2212 , \u2153PO 4 3\u2212 , \u2154PO 4 3\u2212 , or PO 4 3\u2212 ; R 2  is selected from H, or C 1-40  alkyl (for example, methyl, ethyl, propyl, isopropyl, or tert-butyl) which is unsubstituted or optionally substituted with one or more R a ; R 3  is selected from C 1-40  alkyl which is unsubstituted or optionally substituted with one or more R b ; for example, R 3  can be C 1-40  alkyl substituted with 1, 2, or 3 substituents independently selected from C 1-6  alkyl, \u2014NH 2 , \u2014COOH, \u2014OH, \u2014CONH 2 , N(CH 3 ) 2 , NH(CH 3 ), NHCONH 2 , (C 6 H 4 )\u2014OH, or NH(CH 2 ) k CH 3 ; for example, R 3  can be \u2014(CH 2 ) k \u2014NH 2 , \u2014CH(NH 2 )\u2014(CH 2 ) k \u2014COOH, NH 2 (CH 2 ) k CH(NH 2 ), CH 2 CH(NH 2 )COOH, \u2014(CH 2 ) k \u2014COOH, \u2014CH(NH 2 )\u2014(CH 2 ) k \u2014NH\u2014CONH 2 , CH(NH 2 )\u2014(CH 2 ) k \u2014CONH 2 , \u2014CH(NH 2 )\u2014(CH 2 ) k \u2014OH, \u2014CH(NH 2 )\u2014(CH 2 ) k \u2014CH(OH)\u2014CH 3 , \u2014CH(NH 2 )\u2014(CH 2 ) k \u2014(C 6 H 4 )\u2014OH, \u2014CH(NH 2 )\u2014(CH 2 ) k \u2014NH\u2014(CH 2 ) k \u2014CH 3 , \u2014(CH 2 ) k \u2014NH\u2014(CH 2 ) k \u2014CH 3 , \u2014(CH 2 ) k \u2014N(CH 3 ) 2 , wherein k is independently an integer of 0 to 16, such as 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10; Ar can be selected from the following groups which are unsubstituted or optionally substituted with one or more R c : C 6-10  aryl, 5-10 membered heteroaryl; for example, Ar can be selected from pyridyl, phenyl, and specifically can be \u2003wherein the C atom at 2-position of the pyridyl is connected to N atom, and the C atom at 3-position is connected to methylene group.

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): 0.7597431832289644
- 35 USC 102 Novelty (BERT): 0.5148359403580279
- Combined Prediction Score: 0.7352524589418707
- Mean Citation Score: 272.868316
- Max Citation Score: 278.55414
- Similarity Product: 208.72913535292983

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