PATENT CLAIM ANALYSIS

Application Number: 15747952
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-09
Patent Classification: ["548", "143000"]

Abstract:
The present invention relates to novel compounds represented by the formula I having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. (I) The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases.

Claim (Index 1):
An 1,3,4-oxadiazole sulfonamide derivative compound represented by the following formula I, a stereoisomer thereof or a pharmaceutically acceptable salt thereof: wherein R 1  is \u2014CX 2 H or \u2014CX 3 ; R 2  is \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-O(C 1 -C 4  alkyl), \u2014(C 1 -C 4 )\u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-O\u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-NR A R B , \u2014(C 1 -C 4  alkyl)-aryl, \u2014(C 1 -C 4  alkyl)-heteroaryl, -aryl, -heteroaryl, wherein at least one H of the \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-O\u2014C(\u2550O)\u2014(C 1 -C 4  alkyl) or \u2014(C 1 -C 4  alkyl)-NR A R B  may be substituted with \u2014X or \u2014OH, at least one H of the \u2014(C 1 -C 4  alkyl)-aryl, \u2014(C 1 -C 4  alkyl)heteroaryl, -aryl or -heteroaryl may be substituted with \u2014X, \u2014OH, \u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl), \u2014CF 3 , \u2014CF 2 H, \u2014(C 1 -C 4  alkyl)-OH, \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014CF 3  or \u2014C(\u2550O)\u2014CF 2 H, and at least one H of may be substituted with \u2014X, \u2014OH, \u2014O(C 1 -C 4  alkyl), \u2014NR A R B , \u2014CN, \u2014(C 1 -C 4  alkyl), \u2014CF 3 , \u2014CF 2 H, \u2014(C 1 -C 4  alkyl)-OH, \u2014(C 1 -C 4  alkyl)-NR A R B , \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014CF 3 , \u2014C(\u2550O)\u2014CF 2 H, \u2014C(\u2550O)\u2014NR A R B , \u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-OC(\u2550O)\u2014CF 2 H, \u2014(C 3 -C 6  heterocycloalkyl), \u2014(C 1 -C 4  alkyl)-aryl, -aryl or -heteroaryl, wherein at least one H of the \u2014(C 1 -C 4  alkyl)-aryl, -aryl or -heteroaryl may be substituted with \u2014X, \u2014OH, \u2014O(C 1 -C 4  alkyl) or \u2014(C 1 -C 4  alkyl);\n R 3  is \u2014H, \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014O(C 1 -C 4  alkyl), -aryl, -heteroaryl, \n wherein at least one H of the \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-O(C 1 -C 4  alkyl) or \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014O(C 1 -C 4  alkyl) may be substituted with \u2014X or \u2014OH, at least one H of the -aryl or -heteroaryl may be substituted with \u2014X, \u2014OH, \u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl), \u2014CF 3 , \u2014CF 2 H, alkyl)-OH, \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014CF 3 , \u2014C(\u2550O)\u2014CF 2 H, at least one H of may be substituted with \u2014X, \u2014OH, \u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl) or \u2014(C 3 -C 6  heterocycloalkyl);\n R 4  is \u2014CX 2 H or \u2014CX 3 ; \n L 1  to L 4  are each independently \u2014(C 0 -C 2  alkyl)-; \n Z 1  to Z 8  are each independently N or CR Z , wherein at least three of Z 1  to Z 4  or Z 5  to Z 8  may not be simultaneously N, and R Z  is \u2014H, \u2014X or \u2014O(C 1 -C 4  alkyl); \n Z 9  and Z 10  are each independently N or S; \n Y 1  to Y 3  are each independently \u2014CH 2 \u2014, \u2014NR C \u2014, \u2014O\u2014 or \u2014S(\u2550O) 2 \u2014; \n Y 4  to Y 7  are each independently \u2014CH 2 \u2014, \u2014NR D \u2014 or \u2014O\u2014; \n Y 8  is \u2014C(\u2550O), \u2014CH 2 \u2014 or \u2014NR E \u2014; \n Y 9  and Y 10  are each independently \u2014NR F \u2014 or \u2014S(\u2550O) 2 \u2014; \n R A  and R B  are each independently \u2014H, \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-aryl, \u2014C(\u2550O)\u2014CF 2 H or \u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl); \n R C  to R E  are each independently \u2014H, \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-OH, \u2014(C 1 -C 4  alkyl)-O\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014O(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014(C 3 -C 7  cycloalkyl), \u2014(C 1 -C 4  alkyl)-C(\u2550O)\u2014(C 2 -C 6  heterocycloalkyl), \u2014S(\u2550O) 2 \u2014(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl)-aryl, \u2014C( 2 -C 4  alkenyl)-aryl, \u2014(C 1 -C 4  alkyl)-heteroaryl, -aryl, -heteroaryl, \n wherein at least one H of the \u2014(C 1 -C 4  alkyl)-aryl, \u2014C( 2 -C 4  alkenyl)-aryl, \u2014(C 1 -C 4  alkyl)-heteroaryl, -aryl, -heteroaryl, may be substituted with \u2014X, \u2014OH, \u2014O(C 1 -C 4  alkyl), \u2014(C 1 -C 4  alkyl) or \u2014CF 3 ;\n Y 11  is \u2014CH 2 \u2014, \u2014NR F \u2014 or \u2014O\u2014; \n R F  is \u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl), \u2014C(\u2550O)\u2014(C 1 -C 4  alkyl)-OH, \u2014C(\u2550O)\u2014(C 3 -C 7  cycloalkyl) or \u2014S(\u2550O) 2 \u2014(C 1 -C 4  alkyl); \n  is a single bond or a double bond, provided that   is a double bond, Y 1  or Y 2  is \u2014CH\u2014; \n a to e are each independently an integer of 0, 1, 2 or 3, provided that a and b may not be simultaneously 0, and c and d may not be simultaneously 0; and \n X is F, Cl, Br or I.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 86.0
- Lexical Diversity: 1.82143
- Patent Class: 548.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15747850', '15748081', '15763972', '13093729', '14099276']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7755551838554401
- 35 USC 102 Novelty (BERT): 0.5464614256205113
- Combined Prediction Score: 0.7526458080319472
- Mean Citation Score: 349.8987160000001
- Max Citation Score: 412.90927
- Similarity Product: 311.78860683312587

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

Dataset: test