PATENT CLAIM ANALYSIS

Application Number: 15953494
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["514", "235800"]

Abstract:
Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Claim (Index 1):
A compound of Formula Ia, or a pharmaceutically acceptable salt, solvate, stereoisomer, tautomer, or prodrug thereof, wherein:\n X is NH or S; \n Y is O or S; \n Z is O, S, CHR 1a  or NR 1a ;\n R 1a  is hydrogen, C 1-6 alkyl, or C 1-6 alkyl selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 alkoxy, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, or azido groups; \n \n G is N or C;\n if G is N, R 1  is hydrogen C 1-6 alkyl, or C 1-6 alkyl selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 alkoxy, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, or azido groups, \n if G is N and if Z includes R 1a , R 1 \u2014R 1a  is connected as a \u2014CH 2 CH 2 \u2014, \u2014CH 2 CH 2 CH 2 \u2014, \u2014CH\u2550CH\u2014, \u2014C(CH 3 )\u2550CH\u2014 or \u2014CH\u2550C(CH 3 )\u2014 group; and \n if G is C and if Z includes R 1a , R 1 \u2014R 1a  is connected as a \u2550CH\u2014CH\u2550CH\u2014, \u2550N\u2014CH\u2550CH\u2014, or \u2550CH\u2014N\u2550CH\u2014 group; \n \n R 1  is hydrogen or C 1-6 alkyl, or R 1 \u2014R 1a  are connected form a \u2014CH 2 CH 2 \u2014, \u2014CH 2 CH 2 CH 2 \u2014, \u2014CH\u2550CH\u2014, \u2014C(CH 3 )\u2550CH\u2014, or \u2014CH\u2550C(CH 3 )\u2014 group or together with carbon or nitrogen atoms to which they are attached form a pyridine, pyrimidine or pyrazine ring; \n R 2  is hydrogen, halogen, C 1-6 alkyl, or C 1-6 alkyl selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 alkoxy, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, or azido groups; \n R 2a  is phenyl or a heteroaryl group selected from the group consisting of imidazolyl, pyridyl, pyridizinyl, pyrimidinyl, and pyrazinyl, wherein the phenyl or heterocyclic group is optionally substituted with 1-4 substituents independently selected from halo the group consisting of halogen, \u2014SR 3a , \u2014S(O)R 3a , \u2014OR 3a , \u2014OCH 2 R 3b , \u2014OCH(CH 3 )R 3b , \u2014OC(O)NHR 3a , \u2014NR 3a R 4 , \u2014NHSO 2 R 3a , azido, \u2014CHO, \u2014CO 2 R 3a , cyano, C 1-6 alkyl or \u2014CR 5a R 6a R 7a , C 2-6 alkenyl, \u2014C(R 5a )\u2550C(R 8a )(R 9a ), C 2-6 alkynyl, and \u2014C\u2261CR 8a ;\n R 3a , R 3b , and R 4a  are independently hydrogen, phenyl, naphthyl, pyridyl, pyrimidinyl, imidazolyl, 1,2,3-triazolyl, quinolinyl, isoquinolinyl, thiazolyl, tetrazolyl groups, C 1-6 alkyl, cyclic \u2014(C 1-8 alkyl)-, cyclic \u2014(C 1-6 oxaalkyl)-, cyclic \u2014(C 1-6 azaalkyl)-, C 2-6 alkenyl, or C 2-6 alkynyl;\n wherein the phenyl, naphthyl, pyridyl, pyrimidinyl, imidazolyl, 1,2,3-triazolyl, quinolinyl, isoquinolinyl, thiazolyl, or tetrazolyl groups are optionally substituted with 1-3 substituents independently selected from the group consisting of halogen, thiol, C 1-6 alkyl thioether, C 1-6 alkyl sulfoxide, C 1-6 alkyl, C 1-6 alkoxyl, amino, C 1-6 alkylamino, C 1-6 dialkylamino, C 1-6 alkyl sulfonamide, azido, \u2014CHO, \u2014CO 2 H, C 1-6 alkyl carboxylate, cyano, C 2-6 alkenyl, and C 2-6 alkynyl group; and the C 1-6 alkyl, cyclic \u2014(C 1-8 alkyl)-, cyclic \u2014(C 1-6 oxaalkyl)-, cyclic \u2014(C 1-4 azaalkyl)-, C 2-6 alkenyl, or C 2-6 alkynyl groups are selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 alkoxy, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, azido, piperidinyl, phenyl, naphthyl, pyridyl, pyrimidinyl, imidazolyl, 1,2,3-triazolyl, quinolinyl, isoquinolinyl, thiazolyl, or tetrazolyl groups; and \n \n R 5a , R 6a , R 7a , R 8a  and R 9a  are independently hydrogen, phenyl, naphthyl, pyridyl, pyrimidinyl, imidazolyl, 1,2,3-triazolyl, quinolinyl, isoquinolinyl, thiazolyl, tetrazolyl groups, C 1-6 alkyl, cyclic \u2014(C 1-8 alkyl)-, cyclic \u2014(C 1-6 oxaalkyl)-, cyclic \u2014(C 1-6 azaalkyl)-, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxyl, cyclic \u2014(C 1-8 alkoxyl)-, cyclic \u2014(C 1-6 oxaalkoxyl)-, cyclic \u2014(C 1-6 azaalkoxyl)-;\n wherein the phenyl, naphthyl, pyridyl, pyrimidinyl, imidazolyl, 1,2,3-triazolyl, quinolinyl, isoquinolinyl, or thiazolyl, tetrazolyl groups are optionally substituted with 1-3 substituents independently selected from the group consisting of halogen, thiol, C 1-6 alkyl thioether, C 1-6 alkyl sulfoxide, C 1-6  alkyl, C 1-6 alkoxyl, amino, C 1-6 alkylamino, C 1-6 dialkylamino, C 1-6 alkyl sulfonamide, azido, \u2014CHO, \u2014CO 2 H, C 1-6 alkyl carboxylate, cyano, C 2-6 alkenyl, and C 2-6 alkynyl group, and the C 1-6 alkyl, cyclic \u2014(C 1-8 alkyl)-, cyclic \u2014(C 1-6 oxaalkyl)-, cyclic \u2014(C 1-6 azaalkyl)-, C 2-6 alkenyl, or C 2-6 alkynyl groups are selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 alkoxy, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, azido, piperidinyl, phenyl, naphthyl, pyridyl, pyrimidinyl, imidazolyl, 1,2,3-triazolyl, quinolinyl, isoquinolinyl, thiazolyl, or tetrazolyl groups.

Metadata:
- Claim Count in Document: 14.0
- Percentile: 91.0
- Lexical Diversity: 1.33333
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15953492', '12096432', '14343410', '12312749', '15522969']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.789731446077977
- 35 USC 102 Novelty (BERT): 0.5599756053018975
- Combined Prediction Score: 0.766755862000369
- Mean Citation Score: 329.689702
- Max Citation Score: 430.0401
- Similarity Product: 339.47600516334774

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