PATENT CLAIM ANALYSIS

Application Number: 15881318
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["514", "443000"]

Abstract:
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Claim (Index 1):
A bifunctional compound having the chemical structure:\n ULM-L-PTM, or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph or prodrug thereof, wherein:\n the PTM has a structure selected from the group PTM-I and PTM-II: \n the ULM is a small molecule E3 ubiquitin ligase binding moiety that binds or targets an E3 ubiquitin ligase selected from the group consisting of Von Hippel-Lindau (VLM), cereblon (CLM), mouse double-minute homolog2 (MLM), and IAP (ILM); the L is a bond or a chemical linking moiety connecting the ULM and the PTM; X PTM  is O or C\u2550O; each of X PTM1  and X PTM2  is independently selected from N or CH; R PTM1  is independently selected from OH, O(CO)R PTM , O-lower alkyl, wherein R PTM  is an alkyl or aryl group in the ester; R PTM2  and R PTM4  are independently selected from H, OH, halogen, CN, CF 3 , SO 2 -alkyl, O-lower alkyl; R PTM3  and R PTM5  are independently selected from H, halogen; and PTM-I has at least one R PTM2  and at least one R PTM3  on each respective rings.

Metadata:
- Claim Count in Document: 24.0
- Percentile: 86.0
- Lexical Diversity: 1.88462
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14822309', '15730728', '16094102', '16346483', '14707930']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8176017695519345
- 35 USC 102 Novelty (BERT): 0.5500723064954344
- Combined Prediction Score: 0.7908488232462845
- Mean Citation Score: 301.119948
- Max Citation Score: 412.60214
- Similarity Product: 316.0191175290585

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

Dataset: test