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 19):
The bifunctional compound according to any of  claims 2 - 16 , wherein the PTM is an androgen receptor (AR) binding moiety (ABM) represented by a structure selected from the group consisting of: wherein:\n W 1  is aryl, heteroaryl, bicyclic, or biheterocyclic, each independently substituted by 1 or more H, halo, hydroxyl, nitro, CN, C\u2261CH, C 1-6  alkyl (linear, branched, optionally substituted; for example, optionally substituted by 1 or more halo, C 1-6  alkoxyl), C 1-6  alkoxyl (linear, branched, optionally substituted; for example, optionally substituted by 1 or more halo), C 2-6  alkenyl, C 2-6  alkynyl, or CF 3 ; \n Y 1 , Y 2  are each independently NR Y1 , O, S, SO2, heteroaryl, or aryl; \n Y 3 , Y 4 , Y 5  are each independently a bond, O, NR Y2 , CR Y1 R Y2 , C\u2550O, C\u2550S, SO, SO 2 , heteroaryl, or aryl; \n Q is a 3-6 membered ring with 0-4 heteroatoms, optionally substituted with 0-6 R Q , each R Q , is independently H, C 1-6  alkyl (linear, branched, optionally substituted, for example, optionally substituted by 1 or more halo, C 1-6  alkoxyl), halogen, C 1-6 alkoxy, or 2 R Q  groups taken together with the atom they are attached to, form a 3-8 membered ring system containing 0-2 heteroatoms); \n R 1 , R 2 , R a , R b , R Y1 , R Y2  are each independently H, C 1-6  alkyl (linear, branched, optionally substituted; for example, optionally substituted by 1 or more halo, C 1-6  alkoxyl), halogen, C 1-6 alkoxy, cyclic, heterocyclic or R 1 , R 2  together with the atom they are attached to, form a 3-8 membered ring system containing 0-2 heteroatoms); \n W 2  is a bond, C 1-6  alkyl, C 1-6  heteroalkyl, O, aryl, heteroaryl, alicyclic, heterocyclic, biheterocyclic, biaryl, or biheteroaryl, each optionally substituted by 1-10 R W2 ; \n each R W2  is independently H, halo, C 1-6  alkyl (linear or branched optionally substituted; for example, optionally substituted by 1 or more F), \u2014OR W2A , C 3-6  cycloalkyl, C 4-6  cycloheteroalkyl, C 1-6  alkyl (optionally substituted), heterocyclic (optionally substituted), aryl (optionally substituted), or heteroaryl (optionally substituted), bicyclic hereoaryl or aryl, OC 1-3 alkyl (optionally substituted; for example, optionally substituted by 1 or more \u2014F), OH, NH 2 , NR Y1 R Y2 , CN; \n R W2A  is H, C 1-6  alkyl (linear, branched), or C 1-6 heteroalkyl (linear, branched), each optionally substituted by a cycloalkyl, cycloheteroalkyl, aryl, heterocyclic, heteroaryl, halo, or OC 1-3 alkyl; and \n 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: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15881318', '14822309', '15730728', '16346483', '15148253']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8109178717473261
- 35 USC 102 Novelty (BERT): 0.584890806999465
- Combined Prediction Score: 0.78831516527254
- Mean Citation Score: 365.22769200000016
- Max Citation Score: 518.0048
- Similarity Product: 420.42969246549615

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