PATENT CLAIM ANALYSIS

Application Number: 16186333
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-03
Patent Classification: ["514", "176000"]

Abstract:
This invention provides amine-linked C 3 -glutarimide Degronimers and Degrons for therapeutic applications as described further herein, and methods of use and compositions thereof as well as methods for their preparation.

Claim (Index 1):
A Degronimer consisting of a Degron covalently linked to a Targeting Ligand, wherein the Degronimer is of Formula: or a pharmaceutically acceptable salt or N-oxide thereof; wherein:\n W 1  is CR 6 R 7 , C\u2550O, C\u2550S, C\u2550CH 2 , SO 2 , S(O), P(O)Oalkyl, P(O)NHalkyl, P(O)N(alkyl) 2 , P(O)alkyl, P(O)OH, or P(O)NH 2 ; \n W 2  is CR 8 R 9 , C\u2550O, C\u2550S, C\u2550CH 2 , SO 2 , S(O), P(O)Oalkyl, P(O)NHalkyl, P(O)N(alkyl) 2 , P(O)alkyl, P(O)OH, or P(O)NH 2 ; \n X is NH, NR 3 , CH 2 , CHR 3 , C(R 3 ) 2 , O, or S; \n n is 0, 1, or 2; \n  is a single or double bond; \n R 1  is selected from: \n R 2  is alkyl or hydrogen; or R 1  and R 2  are combined to form a 4, 5, 6, 7, 8, 9, or 10 membered heterocyclo or heteroaryl species, wherein the heterocyclo or heteroaryl species is substituted with R 12  at any desired position, and wherein the heterocyclo or heteroaryl species is optionally further substituted with one or more substituents selected from R 5 ; R 3  is selected at each instance from: alkyl, \u2014C(O)H, \u2014C(O)OH, \u2014C(O)alkyl, \u2014C(O)Oalkyl, alkene, and alkyne; R 4  is selected at each instance from: alkyl, alkene, alkyne, halogen, hydroxyl, alkoxy, azide, amino, \u2014NHalkyl, \u2014N(alkyl) 2 , \u2014NHSO 2 alkyl, \u2014N(alkyl)SO 2 alkyl, \u2014NHSO 2 aryl, \u2014N(alkyl)SO 2 aryl, \u2014NHSO 2 alkenyl, \u2014N(alkyl)SO 2 alkenyl, \u2014NHSO 2 alkynyl, \u2014N(alkyl)SO 2 alkynyl, and haloalkyl; or two R 4  substituents together with the carbon atom(s) to which they are bound can form a 3, 4, 5 or 6 membered ring; R 5  and R 14  are independently selected at each instance from: hydrogen, alkyl, alkene, alkyne, halogen, hydroxyl, alkoxy, azide, amino, \u2014NHalkyl, \u2014N(alkyl) 2 , \u2014NHSO 2 alkyl, \u2014N(alkyl)SO 2 alkyl, \u2014NHSO 2 aryl, \u2014N(alkyl)SO 2 aryl, \u2014NHSO 2 alkenyl, \u2014N(alkyl)SO 2 alkenyl, \u2014NHSO 2 alkynyl, \u2014N(alkyl)SO 2 alkynyl, and haloalkyl; R 6 , R 7 , R 8 , R 9 , R 10 , and R 11 , are independently selected from hydrogen, alkyl, hydroxyl, alkoxy, amine, \u2014NHalkyl, and \u2014Nalkyl 2 ; or R 6  and R 7  together with the carbon to which they are bound form a 3-, 4-, 5-, or 6-membered spirocarbocycle, or a 4-, 5-, or 6-membered spiroheterocycle comprising 1 or 2 heteroatoms selected from N and O; or R 8  and R 9  together with the carbon to which they are bound form a 3-, 4-, 5-, or 6-membered spirocarbocycle, or a 4-, 5-, or 6-membered spiroheterocycle comprising 1 or 2 heteroatoms selected from N and O; or R 10  and R 11  together with the carbon to which they are bound form a 3-, 4-, 5-, or 6-membered spirocarbocycle, or a 4-, 5-, or 6-membered spiroheterocycle comprising 1 or 2 heteroatoms selected from N and O; or R 6  and R 8  form a 1 or 2 carbon bridged ring; or R 6  and R 10  form a 1 or 2 carbon bridged ring; or R 8  and R 10  form a 1 or 2 carbon bridged ring; or R 14  and R 6  form a 3, 4, 5, or 6 carbon fused ring; or R 14  and R 10  form a 3, 4, 5, or 6 carbon fused ring; or R 14  and R 8  form a 1 or 2 carbon bridged ring; or R 14  and R 4  form a 3, 4, 5, or 6 carbon fused ring wherein R 5  is on the carbon alpha to R 13  or a 1, 2, 3, or 4 carbon bridged ring wherein R 5  is not on the carbon alpha to R 13 ; R 12  is Linker-Targeting Ligand; Linker is a chemical group that covalently attaches the Degron to a Targeting Ligand; and Targeting Ligand is a small molecule that binds to a Targeted Protein, wherein the Targeted Protein is a mediator of abnormal cellular proliferation in a host in need of such therapy.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 98.0
- Lexical Diversity: 1.22222
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16186339', '16186334', '16163254', '15148262', '16167091']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7625775664119268
- 35 USC 102 Novelty (BERT): 0.6421247050868503
- Combined Prediction Score: 0.7505322802794192
- Mean Citation Score: 448.087808
- Max Citation Score: 633.1144400000002
- Similarity Product: 553.9133979857161

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