PATENT CLAIM ANALYSIS

Application Number: 15878305
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["536", "017400"]

Abstract:
The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one antifungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA) m -X-(L) n ; (ii) [(AFA) m′ -X] p -L; (iii) AFA-[X-(L) n′ ] q ; or (iv) (AFA) m″ -X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nonaparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.

Claim (Index 7):
The conjugate-based prodrug of  claim 1 , wherein the linker is selected from group consisting of; wherein R 2a  is a hydroxyl protecting group; R 2b  is C 1 -C 6 alkyl, which can be optionally substituted or interspersed with one or more heteroatoms, aryls, heteroaryls, cyclyls and heterocyclyls; and R N  is absent, H, C 1 -C 6 alkyl, or acyl, each of which can be optionally substituted;\n (ii) a polyethylene glycol of formula \u2014CH 2 CH 2 [OCH 2 CH 2 ] a OHC 2 CH 2 \u2014, wherein a is 1-50; \n (iii) \u2014CH 2 C(R 3a R 3b )CH(OR 3c )C(O)N(R 3d )\u2014(CH 2 ) b \u2014, wherein R 3a  and R 3b  are independently H or C 1 -C 6 alkyl, which can be optionally substituted and/or interspersed with one or more heteroatoms, aryls, heteroaryls, cyclyls, and heterocyclyls; R 3c  is H or a carrier; R 3d  is H, alkyl, alkenyl, alkynyl, cyclyl, heterocyclyl, aryl, or heteroaryl, each of which can be optionally substituted; and b is 1-10; \n wherein R 4  is halo, CN, CF 3 , alkyl, alkenyl, cyclyl, heterocyclyl, aryl, heteroaryl, NO 2 , OR 6 , OC(O)R 4a , OC(O)OR 4a , N(R 4a ) 2 , NHC(O)R 4a , NHC(O)OR 4a , C(O)R 4a , C(O)OR 4a , SR 4a , or SO 2 R 4a , each of which can be optionally substituted; R 48  is independently for each occurrence, H, alkyl, alkenyl, alkynyl, cyclyl, heterocyclyl, aryl, or heteroaryl, each of which can be optionally substituted; and c is 0 to 4;\n (v) \u2014CH 2 CH(R 6 )\u2014, wherein R is H or C 1 -C 6  alkyl, which can be optionally substituted and/or interspersed with one or more heteroatoms, aryls, heteroaryls, cyclyls, and heterocyclyls; \n (vi) \u2014CH(R 7 )C(O)\u2014, wherein R 7  is H, C 1 -C 6 alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl, each of which can be optionally substituted and/or interspersed with one or more heteroatoms, aryls, heteroaryls, cyclyls and heterocyclyls; \n (vii) \u2014CH(R 8 )OC(O)-L\u2032-C(O)O\u2014, wherein Re is H or C 1 -C 6 alkyl; and L\u2032 is an alkyl group, which can be optionally substituted and/or interspersed with one or more heteroatoms, aryls, heteroaryls, cyclyls or heterocylcyls, each of which can also be optionally substituted; \n (viii) \u2014CH(R 9 )OC(O)\u2014, \u2014CH(R 9 )OC(O)-L\u2032-, \u2014CH(R 9 )OC(O)-L\u2032-Y\u2014 or \u2014CH(R 9 )OC(O)-L\u2032-Y\u2014C(O)\u2014, wherein R 9  is H or C 1 -C 6  alkyl; Y is O, S, or NH; and L\u2032 is an alkyl, which can be optionally substituted and/or interspersed one or more heteroatoms, aryls, heteroaryls, cyclyls or heterocylcyls, each of which can be optionally substituted; \n (ix) \u2014CH(R 10a )OC(O)-L\u2032-C(O)OCH(R 10b )\u2014, wherein R 10a  and R 10b  are independently H or C 1 -C 6  alkyl, which can be optionally substituted; and L\u2032 is C 1 -C 20  alkyl, which can be optionally substituted and/or interspersed one or more heteroatoms, aryls, heteroaryls, cyclyls or heterocylcyls, each of which can be optionally substituted; \n (x) \u2014C(O)-L\u2032-C(O)\u2014, \u2014C(O)-L\u2032-, \u2014C(O)-L\u2032-Y\u2014, or \u2014C(O)-L\u2032-Y\u2014C(O)\u2014, wherein Y is O, S, or NH; and L\u2032 is an alkyl, which can be optionally substituted and/or interspersed one or more heteroatoms, aryls, heteroaryls, cyclyls or heterocylcyls, each of which can be optionally substituted; \n (xi) \u2014C(O)-L\u2032-C(O)O\u2014[CH 2 CH 2 O] v\u2032 \u2014, wherein v\u2032 is 1-500 and L\u2032 is an alkyl, which can be optionally substituted and/or interspersed one or more heteroatoms, aryls, heteroaryls, cyclyls or heterocylcyls, each of which can be optionally substituted; \n (xii) PLGA; \n (xiii) a direct bond; \n (xiv) a dicarboxylic acid; \n (xv) a beta-hydroxy acid; \n (xvi) a polyhydroxy acid; and \n (xvii) any combinations of (i)-(xvi).

Metadata:
- Claim Count in Document: 22.0
- Percentile: 86.0
- Lexical Diversity: 2.49333
- Patent Class: 536.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14128281', '12865693', '14674928', '13574092', '15502131']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6807960210099978
- 35 USC 102 Novelty (BERT): 0.5664215360330358
- Combined Prediction Score: 0.6693585725123017
- Mean Citation Score: 277.632242
- Max Citation Score: 515.3456
- Similarity Product: 354.963187693882

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

Dataset: test