PATENT CLAIM ANALYSIS

Application Number: 16190669
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-08
Patent Classification: ["424", "649000"]

Abstract:
The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.

Claim (Index 1):
A process for preparing a compound of formula VI or a pharmaceutically-acceptable salt thereof, wherein: R 1  is hydrogen, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, aryl or substituted aryl, OR a , SR a , S(\u2550O) 2 R e , S(\u2550O) 2 R e , C(\u2550O)OR d , C(\u2550O)R a , or C(\u2550O)NR b R c ; R 4 , R 7 , and R 8  are each independently hydrogen, halogen, cyano, nitro, CF 3 , OCF 3 , alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, aryl or substituted aryl, OR a , SR a , S(\u2550O)R e , S(\u2550O) 2 R e , P(\u2550O) 2 R e , S(\u2550O) 2 OR e , P(\u2550O) 2 OR e , NR b R c , NR b S(\u2550O) 2 R e , NR b P(\u2550O) 2 R e , S(\u2550O) 2 NR b R c , P(\u2550O) 2 NR b R c , C(\u2550O)OR e , C(\u2550O)R a , C(\u2550O)NR b R c , OC(\u2550O)R a , OC(\u2550O)NR b R c , NR b C(\u2550O)OR e , NR d C(\u2550O)NR b R c , NR d S(\u2550O) 2 NR b R c , NR d P(\u2550O) 2 NR b R c , NR b C(\u2550O)R a , or NR b P(\u2550O) 2 R e ; R 5  is alkyl or substituted alkyl, heterocycle or substituted heterocycle, aryl or substituted aryl; R 6  is hydrogen, halogen, cyano, nitro, CF 3 , OCF 3 , alkyl or substituted alkyl, heterocycle or substituted heterocycle, aryl or substituted aryl, or OR a ; R a  is hydrogen, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, or aryl or substituted aryl; R b , R c  and R d  are independently hydrogen, alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, heterocycle or substituted heterocycle, or aryl or substituted aryl, or said R b  and R c  together with the N to which they are bonded optionally form a heterocycle or substituted heterocycle; and R e  is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, or aryl or substituted aryl, comprising reacting a compound of formula VII, wherein R 1 , R 4 , R 7 , and R 8  are defined as hereinabove, and X is a leaving group selected from Cl Br, I, and \u2014OSO 2 R, in which R is alkyl, substituted alkyl, aryl or substituted aryl, with a compound of formula VIII, wherein R 5  is defined as hereinabove, to provide the compound of formula VI.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 98.0
- Lexical Diversity: 1.59524
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14445783', '14208170', '14499299', '11168682', '11396888']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7849859571353095
- 35 USC 102 Novelty (BERT): 0.5811687141043861
- Combined Prediction Score: 0.7646042328322172
- Mean Citation Score: 433.34546
- Max Citation Score: 490.76813
- Similarity Product: 441.1345800921953

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test