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 33):
A compound of  claim 10 , wherein the compound is:\n 4-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)butanoic acid (compound no. 1-1); (S)-4-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)butanoic acid (compound no. 1-2); (R)-4-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b] indol-2(3H,5H,6H)-yl)butanoic acid (compound no. 1-3); 3-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-4); 3-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-5; Enantiomer A); 3-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-6; Enantiomer B); 4-(1,3-dioxo-6-(3-phenylpropyl)-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b] indol-2(3H,5H,6H)-yl)butanoic acid (compound no. 1-7); 6-(4-fluorobenzyl)-5,6,11,11a-tetrahydrooxazolo[3\u2032,4\u2032:1,6]pyrido[3,4-b]indol-3(1H)-one (compound no. 1-8); (S)-6-(4-fluorobenzyl)-5,6,11,11a-tetrahydrooxazolo[3\u2032,4\u2032:1,6] pyrido[3,4-b]indol-3(1H)-one (compound no. 1-9); (R)-6-(4-fluorobenzyl)-5,6,11,11a-tetrahydrooxazolo[3\u2032,4\u2032:1,6] pyrido[3,4-b]indol-3(1H)-one (compound no. 1-10); (S)-4-(6-((6-methoxypyridin-3-yl)methyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)butanoic acid (compound no. 1-11); (S)-3-(6-((6-methoxypyridin-3-yl)methyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-12); 6-(4-fluorobenzyl)-2-methyl-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-3(2H)-one (compound no. 1-14); 6-(4-fluorobenzyl)-2-methyl-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indole-1,3(2H)-dione (compound no. 1-129); 6-(4-fluorobenzyl)-2-(2-hydroxyethyl)-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indole-1,3(2H)-dione (compound no. 1-121); 2-(6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6] pyrido[3,4-b]indol-2(3H)-yl)acetonitrile (compound no. 1-139); 2-(6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)acetic acid (compound no. 1-19); 7-(4-fluorobenzyl)-2,3,6,7,12,12a-hexahydropyrazino[1\u2032,2\u2032:1,6]pyrido[3,4-b]indole-1,4-dione (compound no. 1-16); 2-(7-(4-fluorobenzyl)-1,4-dioxo-3,4,6,7,12,12a-hexahydropyrazino [1\u2032,2\u2032:1,6]pyrido[3,4-b]indol-2(1H)-yl)acetic acid (compound no. 1-23); 3-(7-(4-fluorobenzyl)-1,4-dioxo-3,4,6,7,12,12a-hexahydropyrazino [1\u2032,2\u2032:1,6]pyrido[3,4-b]indol-2(1H)-yl)propanoic acid (compound no. 1-24); (S)-4-(6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)-2,2-dimethylbutanoic acid (compound no. 1-39); (S)-4-(6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)-3,3-dimethylbutanoic acid (compound no. 1-42); (S)-4-(8-chloro-6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)butanoic acid (compound no. 1-27); (S)-8-chloro-6-(4-fluorobenzyl)-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6] pyrido[3,4-b]indole-1,3(2H)-dione (compound no. 1-26); (S)-3-(6-((6-chloropyridin-3-yl)methyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)propanoic acid (compound no. 1-84); (S)-1-((6-((6-methoxypyridin-3-yl)methyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)methyl)cyclopropane-1-carboxylic acid (compound no. 1-18); (S)-3-(6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo [1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)-2,2-dimethylpropanoic acid (compound no. 1-30); (S)-1-((6-(4-fluorobenzyl)-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)methyl)cyclopropane-1-carboxylic acid (compound no. 1-34); 3-{8-[(4-fluorophenyl)methyl]-12,14-dioxo-6,8,11,13-tetraazatetracyclo [7.7.0.02, 7.011,15]hexadeca-1(9),2(7),3,5-tetraen-13-yl}propionic acid (compound no. C114) 3-{8-[(4-fluorophenyl)methyl]-12,14-dioxo-6,8,11,13-tetraazatetracyclo [7.7.0.02, 7.011,15]hexadeca-1(9),2(7),3,5-tetraen-13-yl}propionic acid (compound no. C114 Enantiomer A); 3-{8-[(4-fluorophenyl)methyl]-12,14-dioxo-6,8,11,13-tetraazatetracyclo [7.7.0.02, 7.011,15]hexadeca-1(9),2(7),3,5-tetraen-13-yl} propionic acid (compound no. C114 Enantiomer B); (S)-3-(6-(4-fluorobenzyl)-1-oxo-3-thioxo-5,6,11,11a-tetrahydro-1H-imidazo [1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)propanoic acid (compound no. E1); 3-(6-(4-fluorobenzyl)-11,11-dimethyl-1,3-dioxo-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)propanoic acid (compound no. A11); 2-(6-(4-fluorobenzyl)-3-oxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6] pyrido[3,4-b]indol-2(3H,5H,6H)-yl)acetic acid (compound no. 1-20); 3-(6-(4-fluorobenzyl)-3-oxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-21); (S)-3-(1,3-dioxo-6-((2-(trifluoromethyl)thiazol-5-yl)methyl)-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-102); (S)-3-(6-(4-methoxybenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-131); (S)-3-(6-(2,4-dichlorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-132); (S)-3-(6-(4-chloro-2-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-133); (S)-3-(6-(2,4-difluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-134); (S)-3-(6-((6-fluoropyridin-3-yl)methyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. 1-135); (S)-6-(4-fluorobenzyl)-3-thioxo-2,3,5,6,11,11a-hexahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-1-one (compound no. E2); (S)-3(6-(4-fluorobenzyl)-3-oxo-1-thioxo-5,6,11,11a-tetrahydro-1H-imidazo [1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H)-yl)propanoic acid (compound no. 1-141); 3-{8-[(p-fluorophenyl)methyl]-12,14-dioxo-6,8,11,13-tetrazatetracyclo [7.7.0.02,7.011,15]hexadeca-1(9),2(7),3,5-tetraene-13-yl}-2,2-dimethyl propionic acid (compound no. C111); 8-[p-fluorophenyl)methyl]-12-thioxo-6,8,11,13-tetrazatetracyclo [7.7.0.02,7.011,15]hexadeca-1(9),2(7),3,5-tetraen-14-one (compound no. E3); 3-{8-[(p-fluorophenyl)methyl]-16,16-dimethyl-12,14-dioxo-6,8,11,13-tetrazatetracyclo[7.7.0.02,7.011,15]hexadeca-1 (9),2(7),3,5-tetraene-13-yl}propionic acid (compound no. C11); (S)-3-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b] indol-2(3H,5H,6H)-yl)-N-(methylsulfonyl)propanamide (compound no. 1-142); (S)-3-(6-(4-fluorobenzyl)-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)-N-(phenylsulfonyl)propanamide (compound no. 1-143); 3-(6-(4-fluorobenzyl)-11a-methyl-1,3-dioxo-11,11a-dihydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indol-2(3H,5H,6H)-yl)propanoic acid (compound no. A113); 2-((2H-tetrazol-5-yl)methyl)-6-(4-fluorobenzyl)-5,6,11,11a-tetrahydro-1H-imidazo[1\u2032,5\u2032:1,6]pyrido[3,4-b]indole-1,3(2H)-dione (compound no. 1-140); or 3-{8-[(p-fluorophenyl)methyl]-16,16-dimethyl-12,14-dioxo-6,8,11,13-tetrazatetracyclo[7.7.0.02,7.011,15]hexadeca-1 (9),2(7),3,5-tetraene-13-yl}-2,2-dimethylpropionic acid (compound no. C13); or a pharmaceutically acceptable salt, or solvate thereof of any one of the preceding compounds.

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): 0.7475686052986273
- 35 USC 102 Novelty (BERT): 0.6458846090532289
- Combined Prediction Score: 0.7374002056740875
- Mean Citation Score: 400.506624
- Max Citation Score: 629.2572
- Similarity Product: 561.3019730070591

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