PATENT CLAIM ANALYSIS

Application Number: 15917973
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-10
Patent Classification: ["546", "089000"]

Abstract:
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b  and R 5  are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

Claim (Index 1):
A method for treating an eIF4A dependent condition in a mammal in need thereof comprising administering to the mammal a therapeutically effective amount of at least one compound according to Formula (I) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein:\n X is O, S, S(O) or S(O) 2 ; \n Y is a 5-membered heteroaryl or a 6-membered aryl or heteroaryl; \n R 1  and R 2  independently are aryl; \n R 3a , R 3b , R 4a  and R 4b  independently are H, halogen, CN, C 1 -C 8 (alkyl), (C 1 -C 8 )haloalkyl, C 2 -C 8 (alkenyl), (C 2 -C 8 )alkynyl, OR 9 , NHR 9 , NR 9 R 9 , [(C 1 -C 8 )alkylene]OR 9 , [(C 1 -C 8 )alkylene]NHR 9 , [(C 1 -C 8 )alkylene]NR 9 R 9 , C(O)R 8 , C(O)NHR 9 , C(O)NR 9 R 9 , C(O)[(C 1 -C 8 )alkylene]NHR 9 , C(O)[(C 1 -C 8 )alkylene]NR 9 R 9 , CO 2 R 9 , C(S)NHR 9 , C(S)NR 9 R 9 , SR 9 , S(O)R 9 , SO 2 R 9 , SO 2 NHR 9 , SO 2 NR 9 R 9 , NH(CO)R 8 , NR 9 (CO)R 8 , NH(CO)NHR 9 , NH(CO)NR 9 R 9 , NR 9 (CO)NHR 9 , NR 9 (CO)NR 9 R 9 , P(O)(OH)(OR 9 ), P(O)(OR 9 ) (OR 9 ), aryl, heteroaryl, cycloalkyl or heterocyclyl; \n R 3a  and R 3b , and R 4a  and R 4b  independently combine to form oxo or alkenyl, or a cycloalkyl or heterocyclyl ring; or \n R 3a  and R 4a , R 3b  and R 4b  or R 4a  and R 5  together with the carbon atom to which they are attached form a cycloalkyl or heterocyclyl ring; \n R 5  is H, halogen, OH, CN, N 3 , SR 9 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, O(C 1 -C 8 )alkyl, O(C 1 -C 8 )haloalkyl, (C 2 -C 8 )alkynyl, NHC(O)(C 1 -C 8 )alkyl or heteroaryl; \n R 6  and R 7  independently are H, CN, halogen, OR 9 , SR 9 , (C 1 -C 8 )alkyl, NH(R 9 ) or NR 9 R 9 ; \n R 8  is H, (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, O(C 1 -C 8 )alkyl, O(C 1 -C 8 )haloalkyl, cycloalkyl, O(cycloalkyl), heterocyclyl, O(heterocyclyl), aryl, O(aryl), heteroaryl or O(heteroaryl); \n R 9  is H, (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, cycloalkyl, heterocyclyl, [(C 1 -C 8 )alkylene] heterocyclyl, aryl, [(C 1 -C 8 )alkylene] aryl or heteroaryl; \n wherein the two R 9 's together with the nitrogen atom to which they are attached of NR 9 R 9 , [(C 1 -C  8 )alkylene]NR 9 R 9 , C(O)NR 9 R 9 , C(O)[(C 1 -C 8)alkylene]NR 9 R 9 , C(S)NR 9 R 9 , SO 2 NR 9 R 9 , NH(CO)NR 9 R 9  or NR 9 (CO)NR 9 R 9 , optionally form a heterocyclyl ring; \n wherein any alkyl, alkenyl, cycloalkyl, heterocyclyl, heteroaryl or aryl is optionally substituted with 1, 2, or 3 groups selected from OH, CN, SH , SO 2 NH 2 , SO 2 (C 1 -C 4 )alkyl, SO 2 NH(C 1 -C 4 )alkyl, halogen, NH 2 , NH(C 1 -C 4 )alkyl, NRC 1 -C 4 )alkyl[ 2 , C(O)NH 2 , COOH, COOMe, acetyl, (C 1 -C 8 )alkyl, O(C 1 -C 8 )alkyl, O(C 1 -C 8 )haloalkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, haloalkyl, thioalkyl, cyanomethylene, alkylaminyl, NH 2 \u2014C(O)-alkylene , NH(Me)-C(O)-alkylene, CH 2 \u2014C(O)-lower alkyl, C(O)-lower alkyl, alkylcarbonylaminyl, CH 2 \u2014[CH(OH)] m \u2014(CH 2 ) p \u2014OH, CH 2 \u2014[CH(OH)] m \u2014(CH 2 ) p \u2014NH 2  or CH 2 -aryl-alkoxy; \n or wherein any alkyl, cycloalkyl or heterocyclyl is optionally substituted with oxo; \n \u201cm\u201d and \u201cp\u201d are 1, 2, 3, 4, 5 or 6; and \n wherein when Y is a 6-membered aryl then X is not O.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 90.0
- Lexical Diversity: 1.62712
- Patent Class: 546.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15358761', '14772731', '15676726', '15108391', '10420390']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7390711154106921
- 35 USC 102 Novelty (BERT): 0.6939128123379046
- Combined Prediction Score: 0.7345552851034134
- Mean Citation Score: 432.51935
- Max Citation Score: 864.5835599999997
- Similarity Product: 680.9430578907536

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