PATENT CLAIM ANALYSIS

Application Number: 15953492
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["544", "277000"]

Abstract:
Disclosed are cyclic-di-nucleotide cGAMP analogs, methods of synthesizing the compounds, pharmaceutical compositions comprising the compounds thereof, and use of compounds and compositions in medical therapy.

Claim (Index 1):
A compound of Formula Ia, or a pharmaceutically acceptable salt thereof, wherein: a and b are independently 0 or 1 and a+b=1, when a is 1, b is 0 and R 5  is not present; and when a is 0, b is 1 and R 4  is not present; X 1  and X 2  are independently O, S or Se in a five-membered ring; L 1 , starting from the carbon alpha to X 1 , and L 2 , starting from the carbon alpha to X 2 , are independently \u2014CH 2 O\u2014P(O)R 6 \u2014O\u2014, \u2014CH 2 O\u2014P(S)R 6 \u2014O\u2014, \u2014C(Y 1 )(Y 2 )O\u2014P(O)R 6 \u2014C(Y 3 )(Y 4 )\u2014, \u2014CH 2 NHSO 2 NH\u2014, \u2014CH 2 NHC(O)NH\u2014, \u2014CH 2 NHC(S)NH\u2014, \u2014CH 2 NHC(NH)NH\u2014, \u2014CH 2 NHC(O)CH 2 \u2014, \u2014CH 2 NHSO 2 CH 2 \u2014, \u2014CH 2 CH 2 C(O)NH\u2014, \u2014CH 2 CH 2 SO 2 NH\u2014, \u2014CH 2 NH(3,4-dioxocyclobuten-1,2-diyl)NH\u2014, c is 0, 1, or 2; d, e, and f are independently 0 or 1; Y 1 , Y 2 , Y 3 , and Y 4  are independently H or F; R 6  is hydroxyl, thiol, C 1-6 alkyl, 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, C 1-6 alkoxy, C 1-6 alkoxy selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, or azido groups, C 3-5 alkenyl-O\u2014, C 3-5 alkynyl-O\u2014, oligo(ethylene glycol), poly(ethylene glycol), borano (\u2014BH 3 \u2212 ), or \u2014NR 7 R 8 ;\n R 7  and R 8  are independently hydrogen, C 1-6 alkyl, 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, cyclic \u2014(C 1-6 alkyl)-, cyclic \u2014(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, or di(C 1-6 alkyl)amino groups, cyclic \u2014(C 1-6 oxaalkyl)-, or cyclic \u2014(C 1-6 oxaalkyl)-selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, or di(C 1-6 alkyl)amino groups; \n R 1  and R 2  are independently aromatic rings or heteroaromatic rings with the following general structure including its tautomeric forms: g and h are independently 0 or 1; W 1  and W 2  are independently hydrogen, halogen, hydroxyl, C 1-6 alkyl, 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, C 1-6 alkoxy, C 1-6 alkoxy selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, or azido groups, C 3-5 alkenyl-O\u2014, C 3-5 alkynyl-O\u2014, oligo(ethylene glycol), poly(ethylene glycol), azido, or \u2014NR 7 R 8 ; Z 1 , Z 2 , Z 3 , Z 4 , Z 5 , and Z 6  are independently CH or N; if present, Z 7 , Z 8 , Z 9 , Z 10 , and Z 11  are independently CH or N, and then W 1  is CH or N; R 3 , R 4 , and R 5  are independently hydrogen, halogen, hydroxyl, amino, C 1-6 alkyl, 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, C 1-6 alkoxy, C 1-6 alkoxy selectively functionalized with one or more halogen, thiol, hydroxyl, carbonyl, carboxyl, carbonyloxyl, C 1-6 hydroxyalkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, or azido groups, C 3-5 alkenyl-O\u2014, C 3-5 alkynyl-O\u2014, oligo(ethylene glycol), poly(ethylene glycol), azido, or \u2014NR 7 R 8 ; and the compound is not 2\u20323\u2032-cGAMP.

Metadata:
- Claim Count in Document: 17.0
- Percentile: 91.0
- Lexical Diversity: 1.38095
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['13974261', '09526348', '13912431', '11317907', '10550857']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7892948241700711
- 35 USC 102 Novelty (BERT): 0.5203753101199872
- Combined Prediction Score: 0.7624028727650627
- Mean Citation Score: 320.80648
- Max Citation Score: 334.80106
- Similarity Product: 261.88433548707724

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