PATENT CLAIM ANALYSIS

Application Number: 15892142
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-06
Patent Classification: ["426", "648000"]

Abstract:
Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.

Claim (Index 10):
A compound having the structure of Formula (Ia), or a pharmaceutically acceptable salt or solvate thereof: wherein, R 1  is H, halogen, \u2014CN, C 1 -C 4 alkyl, \u2014CF 3 , or C 1 -C 4 deuteroalkyl; R 2  is H, halogen, \u2014CN, \u2014OH, C 1 -C 4 alkyl, C 1 -C 4 fluoroalkyl, C 1 -C 4 deuteroalkyl, C 1 -C 4 alkoxy, or C 1 -C 4 fluoroalkoxy; R 3  is H, F, C 1 -C 4 alkyl, or C 1 -C 4 fluoroalkyl; R 4  is H, F, C 1 -C 4 alkyl, or C 1 -C 4 fluoroalkyl; R 5  is H, F, C 1 -C 4 alkyl, or C 1 -C 4 fluoroalkyl; R 6  is H, F, C 1 -C 4 alkyl, or C 1 -C 4 fluoroalkyl; R 7  is H, or F; R 8  is independently selected from H, \u2014OH, \u2014OR 9 , C 1 -C 6 alkyl, and C 1 -C 6 fluoroalkyl; L 1  is absent, substituted or unsubstituted C 1 -C 4 alkylene, or substituted or unsubstituted C 3 -C 7  cycloalkylene; A is a substituted or unsubstituted aryl, substituted or unsubstituted monocyclic heteroaryl, substituted or unsubstituted bicyclic heteroaryl, substituted or unsubstituted monocyclic heterocycloalkyl, or substituted or unsubstituted bicyclic heterocycloalkyl; each R A  substituent is independently H, halogen, OH, \u2014OR 9 , \u2014CN, \u2014NO 2 , C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, C 1 -C 6 deuteroalkyl, C 1 -C 6 heteroalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, substituted or unsubstituted C 2 -C 10 heterocycloalkyl, substituted or unsubstituted aryl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted heteroaryl, \u2014C(\u2550O)R 9 , \u2014S(\u2550O) 2 R 9 , \u2014S(\u2550O)R 9 , \u2014SR 9 , \u2014S(\u2550O) 2 N(R 10 ) 2 , \u2014NR 10 S(\u2550O) 2 R 9 , \u2014OC(\u2550O)R 9 , \u2014CO 2 R 10 , \u2014OCO 2 R 9 , \u2014N(R 10 ) 2 , \u2014C(\u2550O)N(R 10 ) 2 , \u2014OC(\u2550O)N(R 10 ) 2 , \u2014NHC(\u2550O)R 9 , or \u2014NHC(\u2550O)OR 9 ;\n or two R A  groups may be taken together with the intervening atoms connecting the two R A  groups to form a substituted or unsubstituted ring containing 0-3 heteroatoms selected from \u2014O\u2014, \u2014NR 11 \u2014 and \u2014S\u2014; \n n is 0, 1, 2, 3, or 4; \n X is \u2014CH\u2550, \u2014N\u2550, or \u2014CF\u2550; W is \u2014C(\u2550O)\u2014, \u2014C(\u2550S)\u2014, or \u2014CH 2 \u2014; Y is \u2014C(\u2550O)\u2014, \u2014C(\u2550S)\u2014, \u2014CH 2 \u2014 or \u2014CF 2 \u2014; Z is \u2014CH 2 \u2014, \u2014O\u2014, >N\u2014(C 1 -C 6 alkyl), \u2014Z\u2032\u2014, \u2014Z\u2032\u2014NH\u2014 or \u2014NH\u2014Z\u2032\u2014;\n Z\u2032 is >N-L 2 -B-L 3 -Q;\n L 2  is absent, substituted or unsubstituted C 1 -C 6 alkylene, substituted or unsubstituted C 1 -C 6 fluoroalkylene, or substituted or unsubstituted C 3 -C 6 cycloalkylene; \n B is absent, \u2014O\u2014, \u2014S\u2014, \u2014S(\u2550O)\u2014, \u2014S(\u2550O) 2 \u2014, \u2014NR 11 \u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550O)NR 10 \u2014, or \u2014NR 10 C(\u2550O)\u2014; \n L 3  is absent, substituted or unsubstituted C 1 -C 6 alkylene, substituted or unsubstituted C 1 -C 6 fluoroalkylene, or substituted or unsubstituted C 3 -C 6 cycloalkylene; \n Q is \u2014CO 2 H, \u2014CO 2 (C 1 -C 6 alkyl), \u2014OH, \u2014B(OH) 2 , \u2014C(\u2550O)NHSO 2 R 9 , \u2014C(\u2550O)N(R 10 ) 2 , \u2014C(\u2550O)NH\u2014OH, \u2014C(\u2550O)NH\u2014CN, \u2014SO 2 NHC(\u2550O)R 9 , \u2014OP(\u2550O)(OH) 2 , \u2014P(\u2550O)(OH) 2 , tetrazolyl, carboxylic acid bioisostere, substituted or unsubstituted monocyclic heterocycle, \u2014S(\u2550O) 2 R 9 , \u2014S(\u2550O)R 9 , \u2014SR 9 , \u2014S(\u2550O) 2 N(R 10 ) 2 , \u2014NR 10 S(\u2550O) 2 R 9 , \u2014OC(\u2550O)R 9 , \u2014OCO 2 R 9 , \u2014N(R 10 ) 2 , \u2014C(\u2550O)N(R 10 ) 2 , \u2014OC(\u2550O)N(R 10 ) 2 , \u2014NHC(\u2550O)R 9 , or \u2014NHC(\u2550O)OR 9 ; \n \n each R 9  is independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, C 1 -C 6 deuteroalkyl, C 3 -C 6 cycloalkyl, a substituted or unsubstituted phenyl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted aryl, a substituted or unsubstituted monocyclic heteroaryl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted monocyclic heteroaryl, or a substituted or unsubstituted bicyclic heteroaryl; each R 10  is independently H, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, C 1 -C 6 deuteroalkyl, C 3 -C 6 cycloalkyl, a substituted or unsubstituted phenyl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted aryl, a substituted or unsubstituted monocyclic heteroaryl, or \u2014C 1 -C 4 alkylene-substituted or unsubstituted monocyclic heteroaryl;\n or two R 10  groups attached to the same N atom are taken together with the N atom to which they are attached to form a substituted or unsubstituted heterocycle; \n R 11  is H, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, C 1 -C 6 deuteroalkyl, C 3 -C 6 cycloalkyl, a substituted or unsubstituted phenyl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted aryl, a substituted or unsubstituted monocyclic heteroaryl, \u2014C 1 -C 4 alkylene-substituted or unsubstituted monocyclic heteroaryl, \u2014S(\u2550O) 2 R 9 , \u2014C(\u2550O)R 9 , \u2014CO 2 R 10 , or \u2014C(\u2550O)N(R 10 ) 2 ; t is 0 or 1; and u is 0 or 1.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 88.0
- Lexical Diversity: 1.51724
- Patent Class: 426.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15036370', '14361278', '14411515', '14207854', '15130362']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7482105909168483
- 35 USC 102 Novelty (BERT): 0.6437978497307062
- Combined Prediction Score: 0.7377693167982341
- Mean Citation Score: 400.506624
- Max Citation Score: 629.2572
- Similarity Product: 554.1323889672518

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

Dataset: test