PATENT CLAIM ANALYSIS

Application Number: 15758098
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-09
Patent Classification: ["514", "312000"]

Abstract:
The present invention relates in a first aspect to compounds for use in the treatment of leukodystrophy whereby these compounds are quinoline derivatives, e.g. laquinimod. In a further aspect, the present invention relates to methods for the treatment of Leukodystrophy, in particular, peroxisomal disorders including Zellweger syndrome.

Claim (Index 1):
A method of treating a subject afflicted with (a) leukodystrophy, (b) hereditary central nervous systems disorders, or (c) peroxisomal disorders, the method comprising periodically administering to the subject an amount of a compound of the general formula (I) or a tautomer thereof wherein the groups A 1  and A 2  are interchanged and there is a 2,3-rather than a 3,4-double bond;\n where R 1 , R 2  and R 3  are the same or different and are selected from the group consisting of: hydrogen; C 1 -C 6  alkyl; C 1 -C 6  alkenyl; C 1 -C 5  alkoxy; C 1 -C 6  alkylene; C 3 -C 6  cycloalkyl; C 1 -C 6  alkylthio; C 3 -C 6  cycloakylthio; C 1 -C 6  alkylsulfinyl; C 3 -C 6  cycloalkylsulfinyl; aryl; acyl; heteroaryl; aralalkyl; allyl; carboxyl; amid; carbamoyl; carbonylamin; nitro; amino; cyano; trifluoromethyl; trifluoromethoxy; halogen; NO 2 ; OH; OCOR 8 ; NR 6 R 7 ; and NR 6 COR 8 ; and where R 1  and R 2  or R 2  and R 3  together may also be in the form of a methylenedioxy group; \n where R 4  is selected from the group consisting of: C 1 -C 6  alkyl; C 1 -C 6  alkenyl; C 1 -C 5  alkoxy; C 1 -C 6  alkylene; C 3 -C 6  cycloalkyl; C 1 -C 6  alkylthio; C 3 -C 6  cycloakylthio; C 1 -C 6  alkylsulfinyl; C 3 -C 6  cycloalkylsulfinyl; aryl; acyl; heteroaryl; aralalkyl; allyl; carboxyl; amid; carbamoyl; carbonylamin; nitro; amino; cyano; C 1 -C 6  alkylene forming a ring with the 8-position carbon atom of the quinoline ring system; cycloalkyl; optionally mono- or disubstituted; preferred optionally mono- or disubstituted with substituents selected from the group consisting of C 1 -C 6  alkyl, C 1 -C 6  alkoxy, OH and OCOR 8 ; and phenyl, optionally mono- or disubstituted, preferred optionally mono- or disubstituted with substituents selected from the group consisting of C 1 -C 6  alkyl, C 1 -C 6  alkoxy and halogen; \n and wherein R 5  is selected from the group consisting of a five- or six-membered heterocyclic ring containing at most two heteroatoms selected from the group consisting of S and N, and being optionally mono- or disubstituted, preferred optionally mono- or disubstituted with substituents selected from the group consisting of C 1 -C 6  alkyl, C 1 -C 6  alkoxy, hydroxy and halogen; and wherein R 5  may also be the group: \n wherein R 9 , R 10  and R 11  are the same or different and selected from the group consisting of: hydrogen; C 1 -C 6  alkyl; C 1 -C 6  alkenyl; C 1 -C 5  alkoxy; C 1 -C 6  alkylene; C 3 -C 6  cycloalkyl; C 1 -C 6  alkylthio; C 3 -C 6  cycloakylthio; C 1 -C 6  alkylsulfinyl; C 3 -C 6  cycloalkylsulfinyl; aryl; acyl; heteroaryl; aralalkyl; allyl; carboxyl; amid; carbamoyl; carbonylamin; nitro; amino; trifluoromethyl; trifluoromethoxy; halogen; CN; SO 2 CH 3 ; OH; OCOR 6 ; NR 6 R 7 ; NR 6 COR 8 ; COOR 12 ; OCH 2 COOR 12 ; CH 2 COOR 12 ; COR 8 ; and where each R 14  are the same or different and are selected from the group consisting of: hydrogen; C 1 -C 6  alkyl; C 1 -C 6  alkenyl; C 1 -C 5  alkoxy; C 1 -C 6  alkylene; C 3 -C 6  cycloalkyl; C 1 -C 6  alkylthio; C 3 -C 6  cycloakylthio; C 1 -C 6  alkylsulfinyl; C 3 -C 6  cycloalkylsulfinyl; aryl; acyl; heteroaryl; aralalkyl; allyl; carboxyl; amid; carbamoyl; carbonylamin; nitro; amino; cyano; trifluoromethyl; trifluoromethoxy; halogen; NO 2 ; OH; OCOR 8 ; NR 6 R 7 ; and NR 6 COR 8  preferably wherein at least one of R 14  are hydrogen; wherein m is four or five; and where R 9  and R 10  or R 10  and R 11  together also may be in the form of a methylenedioxy group; wherein A 1  is selected from the group consisting of OR 12 , OCOR 8 , NR 6 R 7  and NR 6 COR 8 , and wherein A 2  is selected from the group consisting of O and NR 6 ; wherein R 6 , R 7  and R 8  are the same or different and selected from the group consisting of hydrogen, C 1 -C 6  alkyl; C 1 -C 6  alkenyl; C 1 -C 5  alkoxy; C 1 -C 6  alkylene; C 3 -C 6  cycloalkyl; C 1 -C 6  alkylthio; C 3 -C 6  cycloakylthio; C 1 -C 6  alkylsulfinyl; C 3 -C 6  cycloalkylsulfinyl; aryl; acyl; heteroaryl; aralalkyl; allyl; carboxyl; amid; carbamoyl; carbonylamin; nitro; amino; cyano; wherein R 12  is selected from the group consisting of C 1 -C 6  alkyl and M; and wherein M is selected from the group consisting of hydrogen, O \u2212  and pharmaceutically acceptable inorganic and organic cations; and wherein R 13  is selected from the group consisting of hydrogen, C 1 -C 6  alkyl, C 1 -C 6  alkenyl, C 1 -C 5  alkoxy, C 1 -C 6  alkylene, C 3 -C 6  cycloalkyl, C 1 -C 6  alkylthio, C 3 -C 6  cycloakylthio, C 1 -C 6  alkylsulfinyl, C 3 -C 6  cycloalkylsulfinyl, aryl, acyl, heteroaryl, aralalkyl, allyl, carboxyl, amid, carbamoyl, carbonylamin, nitro, amino, cyano, preferred C 1 -C 6  alkyl, optionally substituted with a substituent selected from the group consisting of OH, OR 8  and OCOR 8 , and C 1 -C 6  alkenyl; provided that R 13  is selected from the group consisting of C 1 -C 6  alkyl, optionally substituted with a substituent selected from the group consisting of OH, OR 8  and OCOR 8 , and C 1 -C 6  alkenyl when R 9 , R 10  and R 11  are selected from the group consisting of C 1 -C 6  alkyl, C 1 -C 6  alkenyl and C 1 -C 6  alkoxy; and addition salts with pharmaceutically acceptable inorganic or organic acids.

Metadata:
- Claim Count in Document: 19.0
- Percentile: 90.0
- Lexical Diversity: 1.54286
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['13417030', '14182994', '13417028', '11482926', '16301711']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6888983230863558
- 35 USC 102 Novelty (BERT): 0.4966480039077331
- Combined Prediction Score: 0.6696732911684936
- Mean Citation Score: 176.222894
- Max Citation Score: 180.24554
- Similarity Product: 119.23721217274428

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

Dataset: test