PATENT CLAIM ANALYSIS

Application Number: 15863498
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-07
Patent Classification: ["514", "183000"]

Abstract:
This invention describes the use of indane acetic acid derivatives which are dual PPAR delta/gamma agonists, and which penetrate the Blood Brain Barrier and achieve effective brain to plasma drug levels at non-toxic doses, for the treatment of neurodegenerative diseases including one or more of the following: Alzheimer's Disease (AD); Huntington's Disease (HD); Parkinson's Disease (PD); Amyotrophic Lateral Sclerosis (ALS); Frontal Temporal Dementia (FTD); Corticobasal Degeneration (CBD); Progressive Supranuclear Palsey (PSP); Dementia with Lewy Bodies (DLB); or Multiple Sclerosis (MS).

Claim (Index 1):
A method of treating a subject having a neurodegenerative disease comprising administering an indane acetic acid, dual Peroxisome Proliferator-Activated Receptor (PPAR) delta and gamma agonist, which penetrates the blood brain barrier (BBB) and achieves pharmacologically useful concentrations in the brain, wherein the neurodegenerative disease is selected from the group comprising:\n j) Alzheimer's Disease (AD); k) Huntington's Disease (HD); l) Parkinson's Disease (PD); m) Amyotrophic Lateral Sclerosis (ALS); n) Frontal Temporal Dementia (FTD); o) Corticobasal Degeneration (CBD); p) Progressive Supranuclear Palsey (PSP); q) Dementia with Lewy Bodies (DLB); r) Multiple Sclerosis (MS); and wherein, the indane acetic acid, comprises a compound of Formula I, or a pharmaceutically acceptable salt, ester prodrug, stereoisomer, enantiomer, racemate or a combination thereof wherein Formula I is: wherein R is H, Na + , Li + , Ca + , K + , N + (C1-C6) 4 , or C1-C6 alkyl; R 1  is H, COOR, C 3 -C 8  cycloalkyl, or C 1 -C 6  alkyl, C 2 -C 6  alkenyl, or C 1 -C 6  alkoxy, each of which may be unsubstituted or substituted with fluoro, methylenedioxyphenyl, or phenyl which may be unsubstituted or substituted with R 6 , \u201cc-2\u201d is defined as the second carbon of the acetic acid portion of Formula I, and \u201cc-1\u2032\u201d is the first carbon of the indane group of Formula I; R 2  is H, halo, or C 1 -C 6  alkyl which may be unsubstituted or substituted with C 1 -C 6  alkoxy, oxo, fluoro, or R 2  is phenyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, pyrrolidinyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, piperazinyl, or morpholinyl, each of which may be unsubstituted or substituted with R 6 ; R 3  is H, C 1 -C 6  alkyl, or phenyl, which may be unsubstituted or substituted with R 6 ; X is O or S; R 4  is phenyl, naphthyl, furyl, thienyl, pyrrolyl, tetrahydrofuryl, pyrrolidinyl, pyrrolinyl, tetrahydrothienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, morpholinyl, benzofuryl, dihydrobenzofuryl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, benzoxazolyl, benxothiazolyl, benzimidazolyl, benzisoxazolyl, benzisothiazolyl, benzodioxolyl, quinolyl, isoquinolyl, quinazolinyl, quinoxazolinyl, dihydrobenzopyranyl, dihydrobenzothiopyranyl, or 1,4-benzodioxanyl, each of which may be unsubstituted or singularly or multiply substituted with R 6 , or with phenyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, pyrrolidinyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, piperazinyl, morpholinyl, benzodioxolyl, dihydrobenzofuranyl, indolyl, pyrimidinyl or phenoxy, each of which may be unsubstituted or singularly or multiply substituted with R 6 ; or R 4  is C 1 -C 6  alkyl or C 3 -C 8  cycloalkyl, either of which may be unsubstituted or substituted with fluoro, oxo, or C 1 -C 6  alkoxy which may be unsubstituted or substituted with C 1 -C 6  alkoxy, or phenyl optionally substituted with R 6 , each of which may be substituted with phenyl, naphthyl, furyl, thienyl, pyrrolyl, tetrahydrofuryl, pyrrolidinyl, pyrrolinyl, tetrahydrothienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, morpholinyl, benzofuryl, dihydrobenzofuryl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, benzisoxazolyl, benzisothiazolyl, benzodioxolyl, quinolyl, isoquinolyl, quinazolinyl, quinoxazolinyl, dihydrobenzopyranyl, dihydrobenzothiopyranyl, or 1,4-benzodioxanyl, each of which may be unsubstituted or further substituted with R 6 , or any C 1 -C 6  alkyl may also be substituted with C 3 -C 8  cycloalkyl or with phenoxy which may be unsubstituted or substituted with R 6  or with phenyl, naphthyl, furyl, thienyl, pyrrolyl, tetrahydrofuryl, pyrrolidinyl, pyrrolinyl, tetrahydrothienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, morpholinyl, benzofuryl, dihydrobenzofuryl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, benzoxazolyl, benxothiazolyl, benzimidazolyl, benzisoxazolyl, benzisothiazolyl, benzodioxolyl, quinolyl, isoquinolyl, quinazolinyl, quinoxazolinyl, dihydrobenzopyranyl, dihydrobenzothiopyranyl, or 1,4-benzodioxanyl, each of which may be unsubstituted or substituted with R 6 , or R 5  is H, halo or C 1 -C 6  alkyl optionally substituted with oxo; and R 6  is halo, CF 3 , C 1 -C 6  alkyl optionally substituted with oxo or hydroxy, or C 1 -C 6  alkoxy optionally substituted with fluoro; and wherein R 3  may be attached to the heterocyclic moiety of the compound of Formula I at either the 4 or 5 position, and, accordingly, the remaining portion of the molecule will be attached at the remaining available carbon atom.

Metadata:
- Claim Count in Document: 13.0
- Percentile: 91.0
- Lexical Diversity: 1.50667
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15774638', '15830675', '15484445', '14429101', '14897396']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7599232999293519
- 35 USC 102 Novelty (BERT): 0.4933370054243432
- Combined Prediction Score: 0.7332646704788511
- Mean Citation Score: 249.04305400000004
- Max Citation Score: 259.62888
- Similarity Product: 214.8578124700069

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