PATENT CLAIM ANALYSIS

Application Number: 15780328
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-12
Patent Classification: ["514", "228200"]

Abstract:
The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

Claim (Index 34):
A process for preparing a compound of Formula IIa from a compound of Formula I in a reaction mixture according to the following reaction scheme: the process comprising: (i) forming a reaction mixture comprising compound Formula I, organic halide, a solvent system, a phase transfer catalyst, and a base, (ii) reacting the reaction mixture to form a reaction product mixture comprising compound Formula IIa, a stereoisomer, geometric isomer, tautomer, or a pharmaceutically acceptable salt thereof, and (iii) isolating compound Formula IIa from the reaction product mixture, wherein\n the solvent system comprises at least 5 v/v % water; \n X is a halide; \n Each R 5 , R 10  and R 15  are independently selected from H, C 1 -C 10  hydrocarbyl or from C 1 -C 5  hydrocarbyl, wherein each hydrocarbyl is optionally substituted, two geminal R 5 , R 10  and/or R 15  groups are oxo, or two geminal R 5 , R 10  and/or R 15  groups form a 3, 4, 5, 6, or 7-membered carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted; \n mor is selected from: \n wherein mor is optionally substituted with one or more R 7  groups independently selected from F, Cl, Br, I, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CH 2 CH 2 CH 3 , \u2014CH(CH 3 ) 2 , \u2014C(CH 3 ) 3 , \u2014CH 2 OCH 3 , \u2014CHF 2 , \u2014CN, \u2014CF 3 , \u2014CH 2 OH, \u2014CH 2 OCH 3 , \u2014CH 2 CH 2 OH, \u2014CH 2 C(CH 3 ) 2 OH, \u2014CH(CH 3 )OH, \u2014CH(CH 2 CH 3 )OH, \u2014CH 2 CH(OH)CH 3 , \u2014C(CH 3 ) 2 OH, \u2014C(CH 3 ) 2 OCH 3 , \u2014CH(CH 3 )F, \u2014C(CH 3 )F 2 , \u2014CH(CH 2 CH 3 )F, \u2014C(CH 2 CH 3 ) 2 F, \u2014CO 2 H, \u2014CONH 2 , \u2014CON(CH 2 CH 3 ) 2 , \u2014COCH 3 , \u2014CON(CH 3 ) 2 , \u2014NO 2 , \u2014NH 2 , \u2014NHCH 3 , \u2014N(CH 3 ) 2 , \u2014NHCH 2 CH 3 , \u2014NHCH(CH 3 ) 2 , \u2014NHCH 2 CH 2 OH, \u2014NHCH 2 CH 2 OCH 3 , \u2014NHCOCH 3 , \u2014NHCOCH 2 CH 3 , \u2014NHCOCH 2 OH, \u2014NHS(O) 2 CH 3 , \u2014N(CH 3 )S(O) 2 CH 3 , \u2550O, \u2014OH, \u2014OCH 3 , \u2014OCH 2 CH 3 , \u2014OCH(CH 3 ) 2 , \u2014SH, \u2014NHC(O)NHCH 3 , \u2014NHC(O)NHCH 2 CH 3 , \u2014S(O)CH 3 , \u2014S(O)CH 2 CH 3 , \u2014S(O) 2 CH 3 , \u2014S(O) 2 NH 2 , \u2014S(O) 2 NHCH 3 , \u2014S(O) 2 N(CH 3 ) 2 , and \u2014CH 2 S(O) 2 CH 3 ; and wherein in formula I R 20  is \u2014OH or \u2014NHR 21  wherein R 21  is as defined for R 5 , and wherein in formula IIa R 20  is \u2014O\u2014 or \u2014NR 21 \u2014.

Metadata:
- Claim Count in Document: 22.0
- Percentile: 93.0
- Lexical Diversity: 1.1
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14524204', '14972333', '13018068', '12586241', '14930929']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.795694904864272
- 35 USC 102 Novelty (BERT): 0.5236387582072443
- Combined Prediction Score: 0.7684892901985693
- Mean Citation Score: 302.856558
- Max Citation Score: 309.51782000000014
- Similarity Product: 166.91455530503634

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