PATENT CLAIM ANALYSIS

Application Number: 15770162
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["544", "359000"]

Abstract:
The invention provides a series of substituted aryl pyrimidine compounds and the use of these compounds as therapeutics to treat or prevent neurodegenerative disorders, including Parkinson's disease. Compounds of the invention are also able to treat the symptoms of such diseases and therefore represent a new treatment modality for ameliorating chronic and acute conditions. The compounds of the invention are capable of selectively potentiating the activity of the Nurr1:RXRα heterodimer, and are able to treat diseases or conditions associated with aberrant Nurr1:RXRα function. The invention further provides methods for treating neurodegenerative disorders by administration of Nurr1:RXRα activating agents.

Claim (Index 49):
A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein n is 0 to 2, p is 0 to 2, X is N(R 6 ) or O; Cy is a phenyl ring or a heteroaromatic 5- or 6-membered ring containing between 1 and 4 heteroatoms; each R 1  is independently selected from the group consisting of halogen, cyanate, isocyanate, thiocyanate, isothiocyanate, selenocyanate, isoselenocyanate, alkoxy, trifluoromethoxy, azido, cyano, nitro, hydroxy, acyl, mercapto, carboxyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, \u2014OR 7 , \u2014SR 7 , and \u2014N(R 8 )R 7 ; each R 2  is independently selected from the group consisting of halogen, cyanate, isocyanate, thiocyanate, isothiocyanate, selenocyanate, isoselenocyanate, alkoxy, trifluoromethoxy, azido, cyano, nitro, hydroxy, acyl, mercapto, carboxyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, \u2014OR 7 , \u2014SR 7 , and \u2014N(R 8 )R 7 ; R 3  is selected from the group consisting of halogen, cyanate, isocyanate, thiocyanate, isothiocyanate, selenocyanate, isoselenocyanate, alkoxy, trifluoromethoxy, azido, cyano, nitro, hydroxy, acyl, mercapto, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, OR 7 , \u2014SR 7 , \u2014N(R 8 )R 7 , optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl and optionally substituted heterocyclyl, or R 3  and R 6 , when present, combine with the atoms to which they are bound to form an optionally substituted 5-membered heteroaryl or heterocyclyl; R 4  is selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted aryl-alkyl, optionally substituted heterocyclyl, optionally substituted heteroaryl, optionally substituted heteroaryl-alkyl, optionally substituted heterocyclolalkyl, OR 7 , and \u2014N(R 8 )R 7 ; R 5  is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, and optionally substituted aryl; R 6  is selected from the group consisting of hydrogen and optionally substituted alkyl; each R 7  is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted aryl-alkyl, and optionally substituted heterocyclyl; and each R 8  is independently selected from the group consisting of hydrogen and optionally substituted alkyl; and wherein the compound is not a compound selected from the group consisting of:\n i. ethyl 4-(5-allyl-6-methyl-2-phenylpyrimidin-4-ylamino)benzoate; \n ii. methyl 4-(5-allyl-6-methyl-2-phenylpyrimidin-4-ylamino)benzoate; \n iii. 4-(6-methyl-2-phenyl-5-propylpyrimidin-4-ylamino)benzoic acid; \n iv. 4-(5-isopropyl-6-methyl-2-phenylpyrimidin-4-ylamino)benzoic acid; \n v. 4-(5-ethyl-6-methyl-2-phenylpyrimidin-4-ylamino)benzoic acid; \n vi. 4-(2-(4-chlorophenyl)-5-ethyl-6-methylpyrimidin-4-ylamino)benzoic acid; \n vii. 4-(5-ethyl-6-methyl-2-phenylpyrimidin-4-yloxy)benzoic acid; \n viii. 4-(2-(4-chlorophenyl)-5-ethyl-6-methylpyrimidin-4-yloxy)benzoic acid; and \n ix. 4-(5-allyl-6-methyl-2-phenylpyrimidin-4-ylamino)benzoic acid;

Metadata:
- Claim Count in Document: 14.0
- Percentile: 91.0
- Lexical Diversity: 1.73438
- Patent Class: 544.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['13770706', '14339772', '13770676', '14886332', '13594223']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8057576895904549
- 35 USC 102 Novelty (BERT): 0.51294580898317
- Combined Prediction Score: 0.7764765015297264
- Mean Citation Score: 320.490044
- Max Citation Score: 323.06412
- Similarity Product: 255.5885499451589

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

Dataset: test