PATENT CLAIM ANALYSIS

Application Number: 15764088
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2019-02
Patent Classification: ["546", "122000"]

Abstract:
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, R 1 , R 3a , R 3b , R 4a , R 4b , G 2 , G 3 , G 4 , m 1 , m 2 , m 3 , m 4 , L 1 , L 2  and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Claim (Index 1):
A compound having the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein:\n A is an aryl or heteroaryl ring; \n G 2 , G 3  and G 4  are each independently N or CR, where R is H, cyano, halo or C 1 -C 6 alkyl; \n R 1  is aryl or heteroaryl; \n R 3a  and R 3b  are, at each occurrence, independently H, \u2014OH, \u2014NH 2 , \u2014CO 2 H, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkynyl, hydroxylalkly, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl or aminocarbonyl; or one R 3a  and one R 3b  join to form a carbocyclic or heterocyclic ring, and each remaining R 3a  and R 3b  are, at each occurrence, independently H, \u2014OH, \u2014NH 2 , \u2014CO 2 H, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkynyl, hydroxylalkly, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl or aminocarbonyl; or one R 3b  joins with one R 4b  to form a carbocyclic or heterocyclic ring, and each R 3a  and each remaining R 3b  are, at each occurrence, independently H, \u2014OH, \u2014NH 2 , \u2014CO 2 H, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkynyl, hydroxylalkly, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl or aminylcarbonyl; \n R 4a  and R 4b  are, at each occurrence, independently H, \u2014OH, \u2014NH 2 , \u2014CO 2 H, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkynyl, hydroxylalkly, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl or aminocarbonyl; or one R 4a  and one R 4b  join to form a carbocyclic or heterocyclic ring, and each remaining R 4a  and R 4b  are, at each occurrence, independently H, \u2014OH, \u2014NH 2 , \u2014CO 2 H, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkynyl, hydroxylalkly, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl or aminocarbonyl; or one R 4b  joins with one R 3b  to form a carbocyclic or heterocyclic ring, and each R 4a  and each remaining R 4b  are, at each occurrence, independently H, \u2014OH, \u2014NH 2 , \u2014CO 2 H, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkynyl, hydroxylalkly, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl or aminylcarbonyl; \n L 1  is a bond or alkylene; \n L 2  is a linker of one two or three atoms in length, the linker comprising carbon or nitrogen atoms or combinations thereof; \n m 1  and m 2 , are each independently 1 or 2; \n m 3  and m 4  are each independently 1, 2 or 3; and \n E is an electrophilic moiety capable of forming a covalent bond with the cysteine residue at position 12 of a KRAS, HRAS or NRAS G12C mutant protein, \n wherein all valences are satisfied.

Metadata:
- Claim Count in Document: 54.0
- Percentile: 90.0
- Lexical Diversity: 1.85294
- Patent Class: 546.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15916075', '15217304', '15093951', '15566648', '15353402']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8606336248029476
- 35 USC 102 Novelty (BERT): 0.601769386640568
- Combined Prediction Score: 0.8347472009867096
- Mean Citation Score: 557.45574
- Max Citation Score: 572.1037
- Similarity Product: 482.6263260794461

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

Dataset: test