PATENT CLAIM ANALYSIS

Application Number: 16167091
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-03
Patent Classification: ["514", "414000"]

Abstract:
The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

Claim (Index 1):
A compound selected from: or an enantiomer, diastereomer, or stereoisomer thereof, wherein: Y is a bond, Y 1 , O, NH, NR 2 , C(O)O, OC(O), C(O)NR 2 \u2032, NR 2 \u2032C(O), Y 1 \u2014O, Y 1 \u2014NH, Y 1 \u2014NR 2 , Y 1 \u2014C(O), Y 1 \u2014C(O)O, Y 1 \u2014OC(O), Y 1 \u2014C(O)NR 2 \u2032, or Y 1 \u2014NR 2 \u2032C(O); Y 1  is C 1 -C 6  alkylene, C 2 -C 6  alkenylene, or C 2 -C 6  alkynylene; X is C(O) or C(R 3 ) 2 ; X 1 \u2014X 2  is C(R 3 )\u2550N or C(R 3 ) 2 \u2014C(R 3 ) 2 ; each R 1  is independently halogen, OH, C 1 -C 6  alkyl, or C 1 -C 6  alkoxy; R 2  is C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 3 -C 8  cycloalkyl, 3- to 8-membered heterocycloalkyl, C(O)\u2014C 1 -C 6  alkyl, C(O)\u2014C 2 -C 6  alkenyl, C(O)\u2014C 3 -C 8  cycloalkyl, or C(O)-3- to 8-membered heterocycloalkyl, and R 2  is optionally substituted with one or more of halogen, N(R a ) 2 , NHC(O)R a , NHC(O)OR a , OR b , C 3 -C 8  cycloalkyl, 3- to 8-membered heterocycloalkyl, C 6 -C 10  aryl, or 5- to 10-membered heteroaryl, wherein each of the C 3 -C 8  cycloalkyl, 3- to 8-membered heterocycloalkyl, C 6 -C 10  aryl or 5- to 10-membered heteroaryl is optionally further substituted with one or more of halogen, NH 2 , CN, nitro, OH, C(O)OH, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  alkoxy, or C 1 -C 6  haloalkoxy; R 2 \u2032 is H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 3 -C 8  cycloalkyl, or 3- to 8-membered heterocycloalkyl; wherein each R 2 \u2032 other than H is optionally substituted with one or more of halogen, N(R a ) 2 , NHC(O)R a , NHC(O)OR a , OR b , C 3 -C 8  cycloalkyl, 3- to 8-membered heterocycloalkyl, C 6 -C 10  aryl, or 5- to 10-membered heteroaryl, wherein each of the C 3 -C 8  cycloalkyl, 3- to 8-membered heterocycloalkyl, C 6 -C 10  aryl or 5- to 10-membered heteroaryl is optionally further substituted with one or more of halogen, NH 2 , CN, nitro, OH, C(O)OH, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  alkoxy, or C 1 -C 6  haloalkoxy; each R 3  is independently H or C 1 -C 3  alkyl optionally substituted with C 6 -C 10  aryl or 5- to 10-membered heteroaryl; each R 3 \u2032 is independently C 1 -C 3  alkyl; each R 4  is independently H or C 1 -C 3  alkyl; or two R 4 , together with the carbon atom to which they are attached, form C(O), a C 3 -C 6  carbocycle, or a 4-, 5-, or 6-membered heterocycle comprising 1 or 2 heteroatoms selected from N and 0; R 5  is H, C 1 -C 3  alkyl, F, or Cl; each R a  independently is H or C 1 -C 6  alkyl; R b  is H or tosyl; t is 0 or 1; m is 0, 1, 2, or 3; n is 0, 1, or 2; the Linker is a group that covalently binds to the Targeting Ligand and Y; and the Targeting Ligand binds to a targeted protein selected from SMARCA2 and Ras; wherein the Targeting Ligand is selected from: R is the attachment point to the Linker; o is 0, 1, 2, 3, 4, 5, 6, 7, or 8; and A is N or CH.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 97.0
- Lexical Diversity: 1.71739
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15632023', '15863760', '15148262', '14707930', '15148257']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.892315687537788
- 35 USC 102 Novelty (BERT): 0.6339636265111662
- Combined Prediction Score: 0.8664804814351258
- Mean Citation Score: 762.696502
- Max Citation Score: 785.68005
- Similarity Product: 541.154343592152

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

Dataset: test