PATENT CLAIM ANALYSIS

Application Number: 15953108
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["514", "279000"]

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 20):
The bifunctional compound according to any of  claims 2 - 16 , wherein the PTM is a BET/BRD4 targeting moiety comprising a group according to the chemical structure PTM-a: wherein:\n Y 1 , Y 2  and Y 3  are independently selected from the group of carbon, nitrogen or oxygen and together with the atoms to form an aromatic fused ring. \n A and B are independently selected from the group of a 5-membered aromatic ring, a 6-membered aromatic ring, a heteroaromatic ring, a carbocyclic, a thiophene a pyrrole ring, a pyridine, a pyrimidine, a pyrazine, a pyrazole ring each optionally substituted with alkyl, alkoxy, halogen, an aromatic and a heteroaromatic ring; wherein ring A is fused to the central azepine (Y1=C) or diazepine (Y1=N) moiety; and \n Z1 is selected from the group of methyl or analkyl group, and \n wherein the dashed line indicates the site of attachment of at least one of the linker, the CLM, a CLM\u2032, or a combination thereof.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 91.0
- Lexical Diversity: 1.675
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15881318', '14822309', '15730728', '16346483', '15148253']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7720788464132398
- 35 USC 102 Novelty (BERT): 0.5689546258258273
- Combined Prediction Score: 0.7517664243544985
- Mean Citation Score: 365.22769200000016
- Max Citation Score: 518.0048
- Similarity Product: 343.40605348186494

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