PATENT CLAIM ANALYSIS

Application Number: 15861688
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-06
Patent Classification: ["514", "235200"]

Abstract:
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.

Claim (Index 1):
A compound having Formula (II): or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein:\n W is C 7 -C 12  spiro bicycloalkyl, C 7 -C 12  fused bicycloalkyl, 7-12 membered spiro heterobicyclyl or 7-12 membered fused heterobicycloalkyl, wherein W is substituted by 1, 2, 3, 4 or 5 R 14  groups; \n W 1  is H, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  alkoxyl, C 1 -C 6  aminoalkyl, C 1 -C 6  hydroxyalkyl, C 3 -C 6  cycloalkyl or 4-7 membered heterocyclyl; \n R 12  is H, F, Cl, Br, I, N 3 , CN, \u2014NO 2 , C 1 -C 12  alkyl, C 1 -C 12  alkoxyl, C 2 -C 12  alkenyl, C 2 -C 12  alkynyl, C 3 -C 12  cycloalkyl, 3-12 membered heterocyclyl, C 6 -C 12  aryl, 5-12 membered heteroaryl, \u2014NR 15a R 15b , \u2014OR 15c , \u2014C(\u2550O)OR 15c , \u2014C(\u2550O)NR 15a R 15b  or \u2014S(\u2550O) 2 NR 15a R 15b , wherein each of the C 1 -C 12  alkyl, C 1 -C 12  alkoxyl, C 2 -C 12  alkenyl, C 2 -C 12  alkynyl, C 3 -C 12  cycloalkyl, 3-12 membered heterocyclyl, C 6 -C 12  aryl and 5-12 membered heteroaryl is optionally independently substituted by 1, 2, 3, 4 or 5 R 17  groups; \n each R 13  is independently H, F, Cl, CN, C 1 -C 12  alkyl, C 2 -C 12  alkenyl, C 1 -C 12  alkoxyl, \u2014(C 0 -C 4  alkylene)-(C 3 -C 12  cycloalkyl), \u2014(C 0 -C 4  alkylene)-(3-12 membered heterocyclyl), C 6 -C 12  aryl or 5-12 membered heteroaryl, wherein each of the C 1 -C 12  alkyl, C 2 -C 12  alkenyl, C 1 -C 12  alkoxyl, \u2014(C 0 -C 4  alkylene)-(C 3 -C 12  cycloalkyl), \u2014(C 0 -C 4  alkylene)-(3-12 membered heterocyclyl), C 6 -C 12  aryl and 5-12 membered heteroaryl is optionally independently substituted by 1, 2, 3, 4 or 5 R 17  groups; \n each R 14  is independently F, Cl, Br, I, NO 2 , N 3 , CN, C 3 -C 12  alkyl, C 2 -C 12  alkenyl, C 2 -C 12  alkynyl, C 1 -C 12  hydroxyalkyl, C 3 -C 12  alkoxyl, C 1 -C 12  alkylamino, C 1 -C 12  aminoalkyl, C 3 -C 12  cycloalkyl, 4-7 membered heterocyclyl, C 6 -C 12  aryl, 6-cyanopyridazine-3-yl, \u2014CH 2 CN, \u2014CH 2 CH 2 CN, \u2014C(\u2550O)R 16d , \u2014S(\u2550O) 2 R 16e , \u2014C(\u2550O)NR 16a R 16b , \u2014S(\u2550O) 2 NR 16a R 16b , \u2014C(\u2550O)O\u2014R 16c , \u2014N(R 16a )C(\u2550O)R 16f , \u2014N(R 16a )S(\u2550O) 2 R 16g  or \u2014OC(\u2550O)R 16f  wherein each of the \u2014CH 2 CN, \u2014CH 2 CH 2 CN, C 3 -C 12  alkyl, C 2 -C 12  alkenyl, C 2 -C 12  alkynyl, C 1 -C 12  hydroxyalkyl, C 3 -C 12  alkoxyl, C 1 -C 12  alkylamino, C 1 -C 12  aminoalkyl, C 3 -C 12  cycloalkyl, 4-7 membered heterocyclyl, C 6 -C 12  aryl and 6-cyanopyridazine-3-yl is optionally independently substituted by 1, 2, 3, 4 or 5 R 17  groups; \n each R 15a , R 15b , R 15c , R 16a  and R 16b  is independently H, C 1 -C 12  alkyl, C 2 -C 12  alkenyl, C 2 -C 12  alkynyl, C 3 -C 12  cycloalkyl, 3-12 membered heterocyclyl, C 6 -C 12  aryl, 5-12 membered heteroaryl, \u2014(C 1 -C 4  alkylene)-(C 3 -C 12  cycloalkyl), \u2014(C 1 -C 4  alkylene)-(3-12 membered heterocyclyl), \u2014(C 1 -C 4  alkylene)-(C 6 -C 12  aryl), or \u2014(C 1 -C 4  alkylene)-(5-12 membered heteroaryl), or R 15a  and R 15b , taken together with the nitrogen atom to which they are attached form a 3-12 membered heterocyclyl group, wherein each of the C 1 -C 12  alkyl, C 2 -C 12  alkenyl, C 2 -C 12  alkynyl, C 3 -C 12  cycloalkyl, 3-12 membered heterocyclyl, C 6 -C 12  aryl, 5-12 membered heteroaryl, \u2014(C 1 -C 4  alkylene)-(C 3 -C 12  cycloalkyl), \u2014(C 1 -C 4  alkylene)-(3-12 membered heterocyclyl), \u2014(C 1 -C 4  alkylene)-(C 6 -C 12  aryl), and \u2014(C 1 -C 4  alkylene)-(5-12 membered heteroaryl) is optionally substituted by 1, 2 or 3 substitutents independently selected from F, Cl, Br, CN, N 3 , \u2014NO 2 , \u2014OH, \u2014NH 2 , C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, C 1 -C 4  alkoxy, C 1 -C 4  hydroxyalkyl, C 1 -C 4  aminoalkyl and C 1 -C 4  alkylamino; \n each R 16d , R 16e  and R 16g  is independently C 2 -C 12  alkyl, C 3 -C 12  cycloalkyl, 3-12 membered heterocyclyl, C 6 -C 12  aryl, 5-12 membered heteroaryl, \u2014(C 1 -C 4  alkylene)-(C 3 -C 12  cycloalkyl), \u2014(C 1 -C 4  alkylene)-(3-12 membered heterocyclyl), \u2014(C 1 -C 4  alkylene)-(C 6 -C 12  aryl) or \u2014(C 1 -C 4  alkylene)-(5-12 membered heteroaryl), wherein each of the above substituents is optionally substituted by 1, 2, 3 or 4 substitutents independently selected from F, Cl, Br, CN, N 3 , \u2014OH, \u2014NH 2 , C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, C 1 -C 4  alkoxy, C 1 -C 4  hydroxyalkyl, C 1 -C 4  aminoalkyl and C 1 -C 4  alkylamino; \n each R 16c  and R 16f  is independently C 1 -C 3  alkyl, C 3 -C 12  cycloalkyl, 3-12 membered heterocyclyl, C 6 -C 12  aryl, 5-12 membered heteroaryl, \u2014(C 1 -C 4  alkylene)-(C 3 -C 12  cycloalkyl), \u2014(C 1 -C 4  alkylene)-(3-12 membered heterocyclyl), \u2014(C 1 -C 4  alkylene)-(C 6 -C 12  aryl), or \u2014(C 1 -C 4  alkylene)-(5-12 membered heteroaryl), wherein each of the above substituents is optionally substituted by 1, 2, 3 or 4 substitutents independently selected from F, Cl, Br, CN, N 3 , \u2014OH, \u2014NH 2 , C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, C 1 -C 4  alkoxy, C 1 -C 4  hydroxyalkyl, C 1 -C 4  aminoalkyl and C 1 -C 4  alkylamino; \n each R 17  is independently F, Cl, Br, I, CN, NO 2 , N 3 , \u2014OH, \u2014NH 2 , C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  haloalkyl, C 3 -C 6  cycloalkyl, C 6 -C 12  aryl, 4-7 membered heterocyclyl, 5-12 membered heteroaryl, C 1 -C 6  aminoalkyl, C 1 -C 6  alkylamino, C 1 -C 6  alkoxyl, C 1 -C 6  hydroxyalkyl, \u2014NH(C 0 -C 4  alkylene)-(C 3 -C 6  cycloalkyl), \u2014NH(C 0 -C 4  alkylene)-(4-7 membered heterocyclyl), \u2014N[(C 0 -C 4  alkylene)-(C 3 -C 6  cycloalkyl)] 2 , \u2014N[(C 0 -C 4  alkylene)-(4-7 membered heterocyclyl)] 2 , \u2014O(C 0 -C 4  alkylene)-(C 3 -C 6  cycloalkyl) or \u2014O(C 0 -C 4  alkylene)-(4-7 membered heterocyclyl); and \n n is 0, 1 or 2.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 86.0
- Lexical Diversity: 1.48718
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15257926', '14670425', '14670421', '14670422', '15300284']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7957996071024174
- 35 USC 102 Novelty (BERT): 0.5785600363813025
- Combined Prediction Score: 0.7740756500303059
- Mean Citation Score: 402.676484
- Max Citation Score: 458.25174
- Similarity Product: 415.1717145142865

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