PATENT CLAIM ANALYSIS

Application Number: 15770824
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-12
Patent Classification: ["549", "406000"]

Abstract:
The present invention provides novel heterocyclic compounds as anticancer agents, especially as estrogen receptor (ER) antagonists/degraders and process for their preparation.

Claim (Index 1):
A compound of Formula I or salts or stereoisomers thereof wherein, R 1  is mono or di-substitution on ring A and is selected from a group comprising \u2014R 3 , \u2014OR 3 , halogen, \u2014C 1-6  haloalkyl, \u2014OC 1-6  haloalkyl, \u2014CN, \u2014N(R 3 ) 2 , \u2014NR 3 SO 2 R 3 , \u2014NR 3 CHO, \u2014NR 3 COR 3 , \u2014OC(O)R 3 , \u2014OC(O)N(R 3 ) 2 , \u2014OP(O)(OH) 2  and \u2014OC(O)OR 3  wherein R 3  at each occurrence is selected from hydrogen, C 1-6  linear, branched or cyclic alkyl and C 1-6  linear, branched or cyclic haloalkyl; R 2  is mono or di-substitution and is selected from a group comprising \u2014R 11 , \u2014OR 11 , halogen, \u2014C 1-6  haloalkyl, \u2014OC 1-6  haloalkyl, \u2014CN, \u2014N(R 11 ) 2 , \u2014NR 11 SO 2 R 11 , \u2014NR 11 CHO, \u2014NR 11 COR 11 , \u2014OC(O)R 11 , \u2014OC(O)N(R 11 ) 2 , \u2014OP(O)(OH) 2  and \u2014OC(O)OR 11  wherein R 11  at each occurrence is selected from hydrogen, C 1-6  linear, branched or cyclic alkyl and C 1-6  linear, branched or cyclic haloalkyl; R 4  is selected from hydrogen, \u2014C 1-5  alkyl, \u2014C 3-4  cycloalkyl, \u2014OC 1-5  alkyl, \u2014C 1-5  haloalkyl, halogen; L is selected from C 1-7  linear or branched alkyl; R 7  and R 8  are absent or independently selected from hydrogen and C 1-5  alkyl; R 9  and R 10  are independently selected from hydrogen or C 1-20  linear, branched or cyclic alkyl or C 1-20  haloalkyl optionally interrupted with one or more radicals independently selected from \u2014O\u2014, \u2014NR 5 \u2014, \u2014S\u2014, \u2014SO\u2014, \u2014S(O 2 )\u2014, \u2014CR 5 \u2550CR 5 \u2014, \u2014C\u2261C\u2014, \u2014NR 5 CO\u2014, \u2014NR 5 CO\u2014, \u2014NR 5 CONR 5 \u2014, NR 5 C(O)O\u2014, and \u2014OC(O)O\u2014; wherein R 5  at each occurrence is selected from a group comprising hydrogen or C 1-6  linear, branched or cyclic alkyl; or R 9  and R 10  together with the nitrogen atom to which they are attached forms a 4 to 7 membered ring optionally containing 1 to 2 additional heteroatoms selected from oxygen, nitrogen or sulfur; and the ring is optionally substituted with one or more group selected from halogen, \u2014OR 6 , \u2014N(R 6 ) 2  and R 6  wherein R 6 , at each occurrence is selected from a group comprising hydrogen, C 1-20  linear, branched or cyclic alkyl optionally interrupted with one or more radicals independently selected from \u2014O\u2014, \u2014NR 5 \u2014, \u2014S\u2014, \u2014SO\u2014, \u2014S(O) 2 \u2014, \u2014CR 5 \u2550CR 5 \u2014, \u2014C\u2261C\u2014, \u2014NR 5 CO\u2014, \u2014CONR 5 \u2014, \u2014NR 5 CONR 5 \u2014, NR 5 C(O)O\u2014 and \u2014OC(O)O\u2014; optionally, R 6  is further substituted with one or more groups selected from a group comprising halogen, \u2014OR 12 , \u2014N(R 12 ) 2 , and \u2014COOR 12 , \u2014CON(R 12 ) 2  or \u2014CON(R 12 )OH; wherein R 12  at each occurrence is selected from hydrogen or C 1-6  linear, branched or cyclic alkyl;\n  is a double or a triple bond; \n ring D is optionally further substituted with a group selected from \u2014R 13 , \u2014OR 13 , halogen, \u2014C 1-6  haloalkyl, \u2014OC 1-6  haloalkyl, \u2014CN, \u2014N(R 13 ) 2 , \u2014NR 13 SO 2 R 13 , \u2014NR 13 CHO, \u2014NR 13 COR 13 , \u2014OC(O)R 13 , \u2014OC(O)N(R 13 ) 2 , \u2014OP(O)(OH) 2  and \u2014OC(O)OR 13  wherein R 13  at each occurrence is selected from hydrogen, and C 1-6  linear, branched or cyclic alkyl; and \n X is selected from NH, sulfur and oxygen \n with a proviso that, when R 13  is hydrogen, R 1  and R 2  are mono-substitution and are hydroxyl group and R 2  is present at 4 position of the ring C, then R 1  is not at position 8 of the ring A.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 91.0
- Lexical Diversity: 1.04167
- Patent Class: 549.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14900425', '15103215', '14968405', '11268374', '10758675']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7412312978976783
- 35 USC 102 Novelty (BERT): 0.5092865334114713
- Combined Prediction Score: 0.7180368214490577
- Mean Citation Score: 288.6774440000001
- Max Citation Score: 291.9329
- Similarity Product: 217.19571627483964

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