PATENT CLAIM ANALYSIS

Application Number: 15996151
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-12
Patent Classification: ["514", "248000"]

Abstract:
The present disclosure relates to bifunctional compounds, which find utility as modulators of c-Met and/or p38 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, 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 3):
The compound according to  claim 1 , wherein ULM is a Von Hippel-Lindau (VHL) ligase-binding moiety (VLM) with a chemical structure represented by: wherein:\n X 1 , X 2  are each independently selected from the group of a bond, O, NR Y3 , CR Y3 R Y4 , C\u2550O, C\u2550S, SO, and SO 2 ; \n R Y3 , R Y4  are each independently selected from the group of H, linear or branched C 1-6  alkyl, optionally substituted by 1 or more halo, optionally substituted C 1-6  alkoxyl (e.g., optionally substituted by 0-3 R P  groups); \n R P  is 0, 1, 2, or 3 groups, each independently selected from the group H, halo, \u2014OH, C 1-3  alkyl, C\u2550O; \n W 3  is selected from the group of an optionally substituted T, an optionally substituted -T-N(R 1a R 1b )X 3 , optionally substituted -T-N(R 1a R 1b ), optionally substituted -T-Aryl, an optionally substituted -T-Heteroaryl, an optionally substituted T-biheteroaryl, an optionally substituted -T-Heterocycle, an optionally substituted -T-biheterocycle, an optionally substituted \u2014NR 1 -T-Aryl, an optionally substituted \u2014NR 1 -T-Heteroaryl or an optionally substituted \u2014NR 1 -T-Heterocycle; \n X 3  is C\u2550O, R 1 , R 1a , R 1b  are independently selected from the group of H, linear or branched C 1 -C 6  alkyl group optionally substituted by 1 or more halo or \u2014OH groups, R Y3 C\u2550O, R Y3 C\u2550S, R Y3 SO, R Y3 SO 2 , N(R Y3 R Y4 )C\u2550O, N(R Y3 R Y4 )C\u2550S, N(R Y3 R Y4 )SO, and N(R Y3 R Y4 )SO 2 ; \n T is selected from the group of an optionally substituted alkyl, \u2014(CH 2 ) n \u2014 group, wherein each one of the methylene groups is optionally substituted with one or two substituents selected from the group of halogen, methyl, a linear or branched C 1 -C 6  alkyl group optionally substituted by 1 or more halogen or \u2014OH groups or an amino acid side chain optionally substituted; and \n n is 0 to 6, \n W 4  is \n R 14a , R 14b , are each independently selected from the group of H, haloalkyl, or optionally substituted alkyl; W 5  is selected from the group of a phenyl or a 5-10 membered heteroaryl, R 15  is selected from the group of H, halogen, CN, OH, NO 2 , NR 14a R 14b , OR 14a , CONR 14a R 14b , NR 14a COR 14b , SO 2 NR 14a R 14b , NR 14a  SO 2 R 14b , optionally substituted alkyl, optionally substituted haloalkyl, optionally substituted haloalkoxy; optionally substituted aryl; optionally substituted heteroaryl; optionally substituted cycloalkyl; or optionally substituted cycloheteroalkyl; and wherein the dashed line indicates the site of attachment of at least one PTM, another ULM (ULM\u2032) or a chemical linker moiety coupling at least one PTM or a ULM\u2032 or both to ULM.

Metadata:
- Claim Count in Document: 34.0
- Percentile: 94.0
- Lexical Diversity: 1.83333
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15881318', '14822309', '15341275', '15730728', '15847628']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7981523215912157
- 35 USC 102 Novelty (BERT): 0.6480413796857164
- Combined Prediction Score: 0.7831412274006658
- Mean Citation Score: 439.84440000000006
- Max Citation Score: 695.188
- Similarity Product: 567.8242119066715

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