PATENT CLAIM ANALYSIS

Application Number: 16039301
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["514", "255050"]

Abstract:
1,8-naphthyridinone compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.

Claim (Index 1):
A compound of Formula (I): or a tautomer or isomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein:\n R 1  is H or C 1 -C 6  alkyl wherein the C 1 -C 6  alkyl of R 1  is optionally substituted with oxo or R a ; \n R 2  and R 4  are each independently H, R b  or oxo; \n R 3  and R 5  are each independently H or R c ; \n each R a , R b , and R c  is independently C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, \u2014CN, \u2014OR 8 , \u2014SR 8 , \u2014NR 9 R 10 , \u2014NO 2 , \u2014C\u2550NH(OR 8 ), \u2014C(O)R 8 , \u2014OC(O)R 8 , \u2014C(O)OR 8 , \u2014C(O)NR 9 R 10 , \u2014OC(O)NR 9 R 10 , \u2014NR 8 C(O)R 9 , \u2014NR 8 C(O)OR 9 , \u2014NR 8 C(O)NR 9 R 10 , \u2014S(O)R 8 , \u2014S(O) 2 R 8 , \u2014NR 8 S(O)R 9 , \u2014C(O)NR 8 S(O)R 9 , \u2014NR 8 S(O) 2 R 9 , \u2014C(O)NR 8 S(O) 2 R 9 , \u2014S(O)NR 9 R 10 , \u2014S(O) 2 NR 9 R 10 , \u2014P(O)(OR 9 )(OR 10 ), C 3 -C 6  cycloalkyl, 3-12-membered heterocyclyl, 5- to 10-membered heteroaryl, C 6 -C 14  aryl, \u2014(C 1 -C 3  alkylene)CN, \u2014(C 1 -C 3  alkylene)OR 8 , \u2014(C 1 -C 3  alkylene)SR 8 , \u2014(C 1 -C 3  alkylene)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)CF 3 , \u2014(C 1 -C 3  alkylene)NO 2 , \u2014C\u2550NH(OR 8 ), \u2014(C 1 -C 3  alkylene)C(O)R 8 , \u2014(C 1 -C 3  alkylene)OC(O)R 8 , \u2014(C 1 -C 3  alkylene)C(O)OR 8 , \u2014(C 1 -C 3  alkylene)C(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)OC(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)NR 8 C(O)R 9 , \u2014(C 1 -C 3  alkylene)NR 8 C(O)OR 9 , \u2014(C 1 -C 3  alkylene)NR 8 C(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)S(O)R 8 , \u2014(C 1 -C 3  alkylene)S(O) 2 R 8 , \u2014(C 1 -C 3  alkylene)NR 8 S(O)R 9 , \u2014C(O)(C 1 -C 3  alkylene)NR 8 S(O)R 9 , \u2014(C 1 -C 3  alkylene)NR 8 S(O) 2 R 9 , \u2014(C 1 -C 3  alkylene)C(O)NR 8 S(O) 2 R 9 , \u2014(C 1 -C 3  alkylene)S(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)S(O) 2 NR 9 R 10 , \u2014(C 1 -C 3  alkylene)P(O)(OR 9 )(OR 10 ), \u2014(C 1 -C 3  alkylene)(C 3 -C 6  cycloalkyl), \u2014(C 1 -C 3  alkylene)(3-12-membered heterocyclyl), \u2014(C 1 -C 3  alkylene)(5-10-membered heteroaryl) or \u2014(C 1 -C 3  alkylene)(C 6 -C 14  aryl), wherein each R a , R b , and R c  is independently optionally substituted by halogen, oxo, \u2014OR 11 , \u2014NR 11 R 12 , \u2014C(O)R 11 , \u2014CN, \u2014S(O)R 11 , \u2014S(O) 2 R 11 , \u2014P(O)(OR 11 )(OR 12 ), \u2014(C 1 -C 3  alkylene)OR 11 , \u2014(C 1 -C 3  alkylene)NR 11 R 12 , \u2014(C 1 -C 3  alkylene)C(O)R 11 , \u2014(C 1 -C 3  alkylene)S(O)R 11 , \u2014(C 1 -C 3  alkylene)S(O) 2 R 11 , \u2014(C 1 -C 3  alkylene)P(O)(OR 11 )(OR 12 ), C 3 -C 8  cycloalkyl, or C 1 -C 6  alkyl optionally substituted by oxo, \u2014OH or halogen;\n wherein when R 1  is C 1 -C 6  alkyl, R 4  is other than \u2014NR 9 R 10  and R 3  is other than \u2014C(O)R 8 ; \n \n ---- is a single bond or a double bond, wherein when ------ is a double bond, R 2  is oxo; \n  is a single bond or a double bond, wherein when   is a double bond, R 4  is oxo;\n one of ------ and   is a double bond and the other is a single bond; \n \n A is C 6 -C 12  aryl, 5- to 10-membered heteroaryl, 9- to 10-membered carbocycle, or 9- to 10-membered heterocycle, wherein the C 6 -C 12  aryl, 5- to 10-membered heteroaryl or 9- to 10-membered carbocycle, or 9- to 10-membered heterocycle of A is optionally further substituted with R 6 ; \n B is phenyl, 5- to 6-membered heteroaryl, 5- to 6-membered carbocycle, 5- to 6-membered heterocycle, or 9- to 10-membered heteroaryl, wherein the phenyl, 5- to 6-membered heteroaryl, 5- to 6-membered carbocycle, 5- to 6-membered heterocycle, or 9- to 10-membered heteroaryl of B is optionally further substituted with R 7 ; \n wherein when B is 5- to 6-membered heterocycle, A is other than phenyl optionally further substituted with R 6  or pyridyl optionally further substituted with R 6 ; \n each R 6  and R 7  is independently oxo, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, \u2014CN, \u2014OR 8 , \u2014SR 8 , \u2014NR 9 R 10 , \u2014NO 2 , \u2014C\u2550NH(OR 8 ), \u2014C(O)R 8 , \u2014OC(O)R 8 , \u2014C(O)OR 8 , \u2014C(O)NR 9 R 10 , \u2014OC(O)NR 9 R 10 , \u2014NR 8 C(O)R 9 , \u2014NR 8 C(O)OR 9 , \u2014NR 8 C(O)NR 9 R 10 , \u2014S(O)R 8 , \u2014S(O) 2 R 8 , \u2014NR 8 S(O)R 9 , \u2014C(O)NR 8 S(O)R 9 , \u2014NR 8 S(O) 2 R 9 , \u2014C(O)NR 8 S(O) 2 R 9 , \u2014S(O)NR 9 R 10 , \u2014S(O) 2 NR 9 R 10 , \u2014P(O)(OR 9 )(OR 10 ), C 3 -C 6  cycloalkyl, 3-12-membered heterocyclyl, 5- to 10-membered heteroaryl, C 6 -C 14  aryl, \u2014(C 1 -C 3  alkylene)CN, \u2014(C 1 -C 3  alkylene)OR 8 , \u2014(C 1 -C 3  alkylene)SR 8 , \u2014(C 1 -C 3  alkylene)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)CF 3 , \u2014(C 1 -C 3  alkylene)NO 2 , \u2014C\u2550NH(OR 8 ), \u2014(C 1 -C 3  alkylene)C(O)R 8 , \u2014(C 1 -C 3  alkylene)OC(O)R 8 , \u2014(C 1 -C 3  alkylene)C(O)OR 8 , \u2014(C 1 -C 3  alkylene)C(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)OC(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)NR 8 C(O)R 9 , \u2014(C 1 -C 3  alkylene)NR 8 C(O)OR 9 , \u2014(C 1 -C 3  alkylene)NR 8 C(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)S(O)R 8 , \u2014(C 1 -C 3  alkylene)S(O) 2 R 8 , \u2014(C 1 -C 3  alkylene)NR 8 S(O)R 9 , \u2014C(O)(C 1 -C 3  alkylene)NR 8 S(O)R 9 , \u2014(C 1 -C 3  alkylene)NR 8 S(O) 2 R 9 , \u2014(C 1 -C 3  alkylene)C(O)NR 8 S(O) 2 R 9 , \u2014(C 1 -C 3  alkylene)S(O)NR 9 R 10 , \u2014(C 1 -C 3  alkylene)S(O) 2 NR 9 R 10 , \u2014(C 1 -C 3  alkylene)P(O)(OR 9 )(OR 10 ), \u2014(C 1 -C 3  alkylene)(C 3 -C 6  cycloalkyl), \u2014(C 1 -C 3  alkylene)(3-12-membered heterocyclyl), \u2014(C 1 -C 3  alkylene)(5-10-membered heteroaryl) or \u2014(C 1 -C 3  alkylene)(C 6 -C 14  aryl), wherein each R 6  and R 7  is independently optionally substituted by halogen, oxo, \u2014OR 11 , \u2014NR 11 R 12 , \u2014C(O)R 11 , \u2014CN, \u2014S(O)R 11 , S(O) 2 R 11 , \u2014P(O)(OR 11 )(OR 12 ), \u2014(C 1 -C 3  alkylene)OR 11 , \u2014(C 1 -C 3  alkylene)NR 11 R 12 , \u2014(C 1 -C 3  alkylene)C(O)R 11 , \u2014(C 1 -C 3  alkylene)S(O)R 11 , \u2014(C 1 -C 3  alkylene)S(O) 2 R 11 , \u2014(C 1 -C 3  alkylene)P(O)(OR 11 )(OR 12 ), C 3 -C 8  cycloalkyl, or C 1 -C 6  alkyl optionally substituted by oxo, \u2014OH or halogen; \n R 8  is independently hydrogen, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 6 -C 14  aryl, 5-6-membered heteroaryl, 3-6-membered heterocyclyl, \u2014(C 1 -C 3  alkylene)(C 3 -C 6  cycloalkyl), \u2014(C 1 -C 3  alkylene)(C 6 -C 14  aryl), \u2014(C 1 -C 3  alkylene)(5-6-membered heteroaryl), or \u2014(C 1 -C 3  alkylene)(3-6-membered heterocyclyl), wherein the C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 6 -C 14  aryl, 5-6-membered heteroaryl, 3-6-membered heterocyclyl, \u2014(C 1 -C 3  alkylene)(C 3 -C 6  cycloalkyl), \u2014(C 1 -C 3  alkylene)(C 6 -C 14  aryl), \u2014(C 1 -C 3  alkylene)(5-6-membered heteroaryl), and \u2014(C 1 -C 3  alkylene)(3-6-membered heterocyclyl) are independently optionally substituted by halogen, oxo, \u2014CN, \u2014OR 13 , \u2014NR 13 R 14 , \u2014P(O)(OR 13 )(OR 14 ), phenyl optionally substituted by halogen, or C 1 -C 6  alkyl optionally substituted by halogen, \u2014OH or oxo; \n R 9  and R 10  are each independently hydrogen, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 6 -C 14  aryl, 5-6-membered heteroaryl, 3-6 membered heterocyclyl, \u2014(C 1 -C 3  alkylene)NR 11 R 12 , \u2014(C 1 -C 3  alkylene)(C 3 -C 6  cycloalkyl), \u2014(C 1 -C 3  alkylene)(3-6-membered heterocyclyl), \u2014(C 1 -C 3  alkylene)(5-6-membered heteroaryl) or \u2014(C 1 -C 3  alkylene)(C 6  aryl), wherein the C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 6 -C 14  aryl, 5-6-membered heteroaryl, 3-6 membered heterocyclyl, \u2014(C 1 -C 3  alkylene)(C 3 -C 6  cycloalkyl), \u2014(C 1 -C 3  alkylene)(3-6-membered heterocyclyl), \u2014(C 1 -C 3  alkylene)(5-6-membered heteroaryl) and \u2014(C 1 -C 3  alkylene)(C 6  aryl) are independently optionally substituted by halogen, oxo, \u2014CN, \u2014OR 13 , \u2014NR 13 R 14  or C 1 -C 6  alkyl optionally substituted by halogen, \u2014OH or oxo;\n or R 9  and R 10  are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo, \u2014OR 13 , \u2014NR 13 R 14  or C 1 -C 6  alkyl optionally substituted by halogen, oxo or \u2014OH; \n \n R 11  and R 12  are each independently hydrogen, C 1 -C 6  alkyl optionally substituted by halogen or oxo, C 2 -C 6  alkenyl optionally substituted by halogen or oxo, or C 2 -C 6  alkynyl optionally substituted by halogen or oxo;\n or R 11  and R 12  are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C 1 -C 6  alkyl optionally substituted by halogen or oxo; and \n \n R 13  and R 14  are each independently hydrogen, C 1 -C 6  alkyl optionally substituted by halogen or oxo, C 2 -C 6  alkenyl optionally substituted by halogen or oxo, or C 2 -C 6  alkynyl optionally substituted by halogen or oxo; \n or R 13  and R 14  are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C 1 -C 6  alkyl optionally substituted by oxo or halogen.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 95.0
- Lexical Diversity: 1.25806
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['13052544', '14383432', '15875106', '15151259', '14137438']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7878773314768763
- 35 USC 102 Novelty (BERT): 0.5060277406179436
- Combined Prediction Score: 0.7596923723909831
- Mean Citation Score: 284.784172
- Max Citation Score: 292.0291
- Similarity Product: 247.06877278621795

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

Dataset: test