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 57):
The process of  claim 34  further comprising preparing a compound of Formula IIIa from a compound of Formula IIa in a reaction mixture according to the following reaction scheme: the process comprising:\n (i) forming a reaction mixture comprising compound Formula IIa, organoboron-R 4 , the solvent system comprising at least 5 v/v % water, the base and the catalyst; \n (ii) reacting the reaction mixture to form a reaction product mixture comprising compound Formula IIIa; and \n (iii) isolating compound Formula IIIa, a stereoisomer, geometric isomer, tautomer, or a pharmaceutically acceptable salt thereof, from the reaction product mixture by solid liquid separation wherein the yield of compound Formula IIIa is at least 75%, \n wherein\n the catalyst comprises palladium and the reaction mixture comprises less than 0.05 equivalents of catalyst per equivalent of compound Formula IIa; and \n R 4  is selected from C 6 -C 20  aryl, C 2 -C 20  heterocyclyl and C 1 -C 20  heteroaryl, each of which are optionally substituted with one or more groups independently selected from F, CI, Br, I, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CH(CH 3 ) 2 , \u2014CH 2 CH(CH 3 ) 2 , \u2014CH 2 CH 3 , \u2014CH 2 CN, \u2014CN, \u2014CF 3 , \u2014CH 2 OH, \u2014CO 2 H, \u2014CONH 2 , CONH(CH 3 ), \u2014CON(CH 3 ) 2 , \u2014NO 2 , \u2014NH 2 , \u2014NHCH 3 , \u2014NHCOCH 3 , \u2014OH, \u2014OCH 3 , \u2014OCH 2 CH 3 , \u2014OCH(CH 3 ) 2 , \u2014SH, \u2014NHC(O)NHCH 3 , \u2014NHC(O)NHCH 2 CH 3 , \u2014NHS(O) 2 CH 3 , \u2014N(CH 3 )C(O)OC(CH 3 ) 3 , \u2014S(O) 2 CH 3 , benzyl, benzyloxy, morpholinyl, morpholinomethyl, and 4-methylpiperazin-yl.

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): 0.7960339386429547
- 35 USC 102 Novelty (BERT): 0.5193651137056576
- Combined Prediction Score: 0.768367056149225
- Mean Citation Score: 302.856558
- Max Citation Score: 309.51782000000014
- Similarity Product: 194.25375720416432

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