PATENT CLAIM ANALYSIS

Application Number: 15885671
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["514", "220000"]

Abstract:
The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

Claim (Index 1):
A cereblon E3 ubiquitin ligase binding compound having a chemical structure selected from: wherein:\n W is independently selected from CH 2 , CHR, C\u2550O, SO 2 , NH, and N-alkyl; \n Q 1 , Q 2 , Q 3 , Q 4 , Qs are each independently represent a carbon C or N substituted with a group independently selected from R\u2032, N or N-oxide; \n R 1  is selected from absent, H, OH, CN, C1-C3 alkyl, C\u2550O; \n R 2  is selected from the group absent, H, OH, CN, C1-C3 alkyl, CHF 2 , CF 3 , CHO, C(\u2550O)NH 2 ; \n R 3  is selected from absent, H, alkyl (e.g., C1-C6 or C1-C3 alkyl), substituted alkyl (e.g., substituted C1-C6 or C1-C3 alkyl), alkoxy (e.g., C1-C6 or C1-C3 alkoxyl), substituted alkoxy (e.g., substituted C1-C6 or C1-C3 alkoxyl); \n R 4  is selected from H, alkyl, substituted alkyl; \n R 5  and R 6  are each independently H, halogen, C(\u2550O)R\u2032; CN, OH, CF 3 ; \n X is C, CH, C\u2550O, or N; \n X 1  is C\u2550O, N, CH, or CH 2 ; \n R\u2032 is selected from H, halogen, amine, alkyl (e.g., C1-C3 alkyl), substituted alkyl (e.g., substituted C1-C3 alkyl), alkoxy (e.g., C1-C3 alkoxyl), substituted alkoxy (e.g., substituted C1-C3 alkoxyl), NR 2 R 3 , C(\u2550O)OR 2 , optionally substituted phenyl; \n n is 0-4; and \n  is a single or double bond.

Metadata:
- Claim Count in Document: 19.0
- Percentile: 86.0
- Lexical Diversity: 1.675
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15881318', '15730728', '14822309', '16346483', '15148253']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7847885565795287
- 35 USC 102 Novelty (BERT): 0.5793012802069712
- Combined Prediction Score: 0.7642398289422729
- Mean Citation Score: 336.657926
- Max Citation Score: 477.86942
- Similarity Product: 372.4669450283015

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