PATENT CLAIM ANALYSIS

Application Number: 16053412
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2018-11
Patent Classification: ["514", "183000"]

Abstract:
Described are a group of isoxazol-3(2H)-one analogues and their use in topical formulations for the treatment and prophylaxis of dermatological disorders.

Claim (Index 1):
A method of treatment of a dermatological disorder, comprising administering to a mammal having a dermatological disorder a compound of Formula 1 wherein R1 and R2 are each selected from the group consisting of hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is selected from the group consisting of an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorines, a C 1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-C6 alkyl, a C1-C6 alkoxy, a nitrile, and a C1-C6 alkyl optionally substituted with one or more groups selected from the group consisting of COOR4, OCOR4, CONR5R6, NR5COR6 and OR4; wherein R4 is a C1-C10 alkyl optionally substituted with one or more of fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are selected from the group consisting of hydrogen, alkyl and a 4-8 membered carbon ring formed by R5 and R6; and including pharmaceutically suitable salts, hydrates or solvates thereof, for use in the treatment of a dermatological disorder, wherein the compound is selected from the group consisting of: 5-[(2S,4R)-2-benzylpiperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2S,4S)-2-benzylpiperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2S,4S)-2-(2-methylpropyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2-methylpropyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4R)-2-benzylpiperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2,4,5-trifluorophenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-{[3-(trifluoromethyl)-5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methyl}piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-{[3-fluoro-4-(trifluoromethyl)phenyl]methyl}piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(3,5-di-tert-butylphenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(2,4-difluorophenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(3,4-difluorophenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[4-(trifluoromethyl)phenyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2S,4S)-2-[(4-tert-butylphenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(4-tert-butylphenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[2-fluoro-4-(trifluoromethyl)phenyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2,4-difluorophenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(3-tert-butylphenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[3-methyl-4-(trifluoromethyl)phenyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[6-(trifluoro pyridin-3-yl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[3-fluoro-4-(trifluoromethyl)phenyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(4-fluorophenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(4-chlorophenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(cyclohexyloxy)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[2-methyl-4-(tri fluoromethyl)phenyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2-methyl-2H-1,2,3,4-tetrazol-5-yl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4 S)-[2-fluoro-4-(trifluoromethoxy)phenyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-{[(2S)-2-(trifluoromethyl)pyrrolidin-1-yl]methyl}piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(4-methanesulfonylphenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2,4-dichlorophenyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(4-methanesulfonylphenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-[(3,4,5-trifluorophenyl)methyl]piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2-phenylethyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2S,4S)-2-(2-phenylethyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2R,4S)-2-(2,2-diethylpropyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one, 5-[(2S,4S)-2-(2,2-dimethylpropyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one and 5-[(2R,4S)-2-benzylpiperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one.

Metadata:
- Claim Count in Document: 3.0
- Percentile: 96.0
- Lexical Diversity: 1.08333
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['12755010', '14778046', '11737069', '11595187', '14345982']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7666750476776452
- 35 USC 102 Novelty (BERT): 0.4863240870290441
- Combined Prediction Score: 0.7386399516127851
- Mean Citation Score: 218.8076
- Max Citation Score: 229.31332
- Similarity Product: 179.5787619912672

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

Dataset: test