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 4):
The compound, racemate, stereoisomer, tautomer, or oxynitride, or pharmaceutically acceptable salt thereof according to  claim 1 , wherein:\n R is selected from R 3a  is selected from C 1-40  alkyl which is unsubstituted or optionally substituted with one or more NR d R e ; R h  is selected from \u2003\u2014O(O)CR f , \u2014OP(O)(OM 1 )(OM 2 ), \u2014OS(O) 2 OM 3 , or C 1-40  alkoxy which is unsubstituted or optionally substituted with one or more R b ; preferably, R h  can be selected from, for example, preferably, when R is R 1a  can be selected from C 1-40  alkyl, C 6-20  aryl, C 6-20  arylalkyl, 5-20 membered heteroarylalkyl, 5-20 membered heteroaryl, which are unsubstituted or optionally substituted with one or more C(O)OR f , \u2014OP(O)(OM 1 )(OM 2 ), \u2014OS(O) 2 OM 3 ; preferably, R 1a  is selected from \u2014(CH 2 ) k \u2014C(O)OR f , \u2014(CH 2 ) k \u2014(C 6 H 4 )\u2014C(O)OR f , \u2014(CH 2 ) z \u2014OP(O)(OM 1 )(OM 2 ), \u2014(CH 2 ) k \u2014(C 6 H 4 )\u2014OP(O)(OM 1 )(OM 2 ), \u2014(CH 2 ) k \u2014(C 6 H 4 )\u2014OS(O) 2 OM 3 , \u2014(CH 2 ) z \u2014OS(O) 2 OM 3 ; wherein, k=an integer of 0-10; z and R f  have the definitions mentioned above; R 1b  can be selected from H or C 1-40  alkyl, for example H, methyl, ethyl, and isopropyl; R 9  is selected from the following groups which are unsubstituted or optionally substituted with one or more R b : R 10 \u2014Y 3 -Y 4 -, R 11 \u2014C(O)\u2014Y 5 -Y 6 -, C 1-40  alkyl, C 1-40  alkoxy, \u2014Y 2 \u2014N(R 4 )\u2014C(\u2550NH)\u2014NH 2 , \u2014Y 3 \u2014N(R 2 )\u2014C(O)\u2014Y 2 \u2014N(R 4 )\u2014C(\u2550NH)\u2014NH 2 , \u2014(CH 2 CH 2 O) z \u2014H, wherein z is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; R f  is selected from the following groups which are unsubstituted or optionally substituted with one or more R m : C 1-40  alkyl, COOH, 3-20 membered heterocyclyl, C 6-20  aryl, and 5-20 membered heteroaryl; each R m  is independently selected from H, F, Cl, Br, I, OH, SH, CN, or the following groups which are unsubstituted or optionally substituted with one or more R a : C 1-40  alkyl, C 1-40  alkoxy, C 3-20  cycloalkyl, 3-20 membered heterocyclyl, C 6-20  aryl, 5-20 membered heteroaryl, NR d R e , \u2014CONR d R e , C(O)Y 2 R f , Y 2 (O)CR f , \u2014Y 2 P(O)(OM 1 )(OM 2 ), and \u2014Y 2 S(O) 2 OM 3 ; M 1 , M 2 , and M 3  can be selected from H, methyl, ethyl, or isopropyl.

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): 0.7607042916414192
- 35 USC 102 Novelty (BERT): 0.507868222832075
- Combined Prediction Score: 0.7354206847604848
- Mean Citation Score: 272.868316
- Max Citation Score: 278.55414
- Similarity Product: 235.50341059232

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