PATENT CLAIM ANALYSIS

Application Number: 15771550
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["514", "224500"]

Abstract:
The present invention relates to small molecule compounds based on benzopyrimido- or benzoimidazo-thiazin-imine as well as their (synthesis) intermediates and their use as HDAC inhibitors, in particular HDAC8 inhibitors. The present invention also relates to the use of said compounds in the treatment of cancer and as therapeutic agents for eukaryotic parasites and respective methods of treatment.

Claim (Index 33):
A pharmaceutical composition comprising:\n (a) at least one a compound having the general formula III wherein\n n is an integer of 1 to 7, \n R 1 , R 2 , R 3 , R 4 , R 5 , R 6  and R 7  are each independently selected from \n hydrogen, \n halogen, \n NO 2 , CN, SO 3 , N(R 10 ) 2 , \n O\u2014X, S\u2014X, NR 8 \u2014X, \u2014NR 10 C(\u2550O)\u2014X, S(\u2550O)\u2014X, S(\u2550O) 2 \u2014X, NHS(\u2550O) 2 \u2014X, \n C 1 -C 6 alkyl-X, C 2 -C 6 alkenyl-X, C 2 -C 6 alkynyl-X, C 1 -C 6 heteroalkyl-X, C 1 -C 6 fluoroalkyl-X, partially fluorinated C 1 -C 6 alkyl-X, C 1 -C 6 alkyl-O\u2014X, C 1 -C 3 alkyl-O\u2014C 1 -C 3 alkyl-X, C 1 -C 6 alkyl-NR 8 \u2014X, C 1 -C 3 alkyl-NR 8 \u2014C 1 -C 3 alkyl \u2014X, C 1 -C 6 alkyl-C(\u2550O)NR 8 \u2014X, C 1 -C 3 alkyl-C(\u2550O)NR 8 \u2014C 1 -C 3 alkyl-X, C 1 -C 6 alkyl-NR 8 C(\u2550O)\u2014X, C 1 -C 3 alkyl-NR 8 C(\u2550O)\u2014C 1 -C 3 alkyl-X, C 1 -C 6 alkyl-S\u2014X, C 1 -C 3 alkyl-S\u2014C 1 -C 3 alkyl-X, C 1 -C 6 alkyl-S(\u2550O)\u2014X, C 1 -C 3 alkyl-S(\u2550O)\u2014C 1 -C 3 alkyl-X, C 1 -C 6 alkyl-S(\u2550O) 2 \u2014X, C 1 -C 3 alkyl-S(\u2550O) 2 \u2014C 1 -C 3 alkyl-X, C(\u2550O)\u2014X, C(\u2550O)\u2014NR 8 \u2014X, C(\u2550O)\u2014C 1 -C 6 alkyl-X, \n substituted or unsubstituted C 2 -C 10 heterocycloalkyl, substituted or unsubstituted aryl, heteroaryl, \n Si 1 \u2014Si 3 silyl-X, Si 2 \u2014Si 4 siloxane-X; \n X is hydrogen, or a substituted or unsubstituted group selected from aryl, heteroaryl, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 1 -C 6 fluoroalkyl, partially fluorinated C 1 -C 6 alkyl, C 1 -C 3 alkylaminoC 1 -C 3 alkoxy, hydroxyC 1 -C 3 alkylaminoC 1 -C 3 alkoxy, C 2 -C 5 heterocycloalkylC 1 -C 3 alkoxy, C 2 -C 8 heterocycloalkylC 1 -C 2 alkyl, CN, NO 2 , SO 3 , CO 2 R 9 , C(\u2550O)R 9 , S\u2014R 9 , S(\u2550O)\u2014R 9 , S(\u2550O) 2 \u2014R 9 , NR 10 C(\u2550O)\u2014R 9 , C(\u2550O)N(R 10 ) 2 , S(\u2550O) 2 N(R 10 ) 2 , NR 10 S(\u2550O) 2 \u2014R 9 , OC(\u2550O)N(R 10 ) 2 , NR 10 C(\u2550O)O\u2014R 9 , \u2014OC(\u2550O)O\u2014R 9 , NHC(\u2550O)NH\u2014R 9 , OC(\u2550O)R 9 , N(R 10 ) 2 , C 1 -C 2 alkylN(R 10 ) 2 , C 2 -C 6 alkyne, C 1 -C 6 heteroalkyl, C 3 -C 10 cycloalkyl, C 2 -C 10 heterocycloalkyl, Si 1 \u2014Si 3 silyl, and Si 2 \u2014Si 4 siloxane; \n R 8  is selected from hydrogen, C 1 -C 6 alkyl, phenyl and benzyl; \n R 9  is a substituted or unsubstituted group selected from C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, partially fluorinated C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, C 2 -C 8 heterocycloalkyl, aryl, and heteroaryl; and \n R 10  and R 11  are each independently hydrogen or a substituted or unsubstituted group selected from C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, partially fluorinated C 1 -C 6 alkyl, C 1 -C 6 heteroalkyl, C 3 -C 8 cycloalkyl, C 2 -C 8 heterocycloalkyl, aryl, and heteroaryl; \n or a pharmaceutically accepted salt or pharmaceutically acceptable prodrug thereof, and (b) a pharmaceutically acceptable excipient(s) and/or carrier.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 91.0
- Lexical Diversity: 1.47619
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['11687565', '12988271', '13897582', '13683880', '13821190']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7600190142035652
- 35 USC 102 Novelty (BERT): 0.5372165303545802
- Combined Prediction Score: 0.7377387658186668
- Mean Citation Score: 341.70378
- Max Citation Score: 360.39923
- Similarity Product: 255.85343595576165

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

Dataset: test