PATENT CLAIM ANALYSIS

Application Number: 15885671
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["514", "220000"]

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 9):
The compound of  claim 2 , wherein the linker (L) comprises a chemical structural unit represented by the formula:\n -(A L )q- wherein:\n (A L ) q  is a group which is connected to at least one of the CLM, the PTM, or a combination thereof; \n q is an integer greater than or equal to 1; \n each A L  is independently selected from the group consisting of, a bond, CR L1 R L2 , O, S, SO, SO 2 , NR L3 , SO 2 NR L3 , SONR L3 , CONR L3 , NR L3 CONR L4 , NR L3 SO 2 NR L4 , CO, CR L1 \u2550CR L2 , C\u2261C, SiR L1 R L2 , P(O)R L1 , P(O)OR L1 , NR L3 C(\u2550NCN)NR L4 , NR L3 C(\u2550NCN), NR L3 C(\u2550CNO 2 )NR L4 , C 3-11 cycloalkyl optionally substituted with 0-6 R L1  and/or R L2  groups, C 3-11 heterocyclyl optionally substituted with 0-6 R L1  and/or R L2  groups, aryl optionally substituted with 0-6 R L1  and/or R L2  groups, heteroaryl optionally substituted with 0-6 R L1  and/or R L2  groups, where R L1  or R L2 , each independently are optionally linked to other groups to form cycloalkyl and/or heterocyclyl moiety, optionally substituted with 0-4 R L5  groups; and \n R L1 , R L2 , R L3 , R L4  and R L5  are, each independently, H, halo, C 1-8 alkyl, OC 1-8 alkyl, SC 1-8 alkyl, NHC 1-8 alkyl, N(C 1-8 alkyl) 2 , C 3-11 cycloalkyl, aryl, heteroaryl, C 3-11 heterocyclyl, OC 1-8 cycloalkyl, SC 1-8 cycloalkyl, NHC 1-8 cycloalkyl, N(C 1-8 cycloalkyl) 2 , N(C 1-8 cycloalkyl)(C 1-8 alkyl), OH, NH 2 , SH, SO 2 C 1-8 alkyl, P(O)(OC 1-8 alkyl)(C 1-8 alkyl), P(O)(OC 1-8 alkyl) 2 , CC\u2014C 1-8 alkyl, C\u2261CH, CH\u2550CH(C 1-8 alkyl), C(C 1-8 alkyl)\u2550CH(C 1-8 alkyl), C(C 1-8 alkyl)\u2550C(C 1-8 alkyl) 2 , Si(OH) 3 , Si(C 1-8 alkyl) 3 , Si(OH)(C 1-8 alkyl) 2 , COC 1-8 alkyl, CO 2 H, halogen, CN, CF 3 , CHF 2 , CH 2 F, NO 2 , SF 5 , SO 2 NHC 1-8 alkyl, SO 2 N(C 1-8 alkyl) 2 , SONHC 1-8 alkyl, SON(C 1-8 alkyl) 2 , CONHC 1-8 alkyl, CON(C 1-8 alkyl) 2 , N(C 1-8 alkyl)CONH(C 1-8 alkyl), N(C 1-8 alkyl)CON(C 1-8 alkyl) 2 , NHCONH(C 1-8 alkyl), NHCON(C 1-8 alkyl) 2 , NHCONH 2 , N(C 1-8 alkyl)SO 2 NH(C 1-8 alkyl), N(C 1-8 alkyl) SO 2 N(C 1-8 alkyl) 2 , NH SO 2 NH(C 1-8 alkyl), NH SO 2 N(C 1-8 alkyl) 2 , NH SO 2 NH 2 .

Metadata:
- Claim Count in Document: 19.0
- Percentile: 86.0
- Lexical Diversity: 1.675
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15881318', '15730728', '14822309', '16346483', '15148253']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.808750687965311
- 35 USC 102 Novelty (BERT): 0.574676340244898
- Combined Prediction Score: 0.7853432531932698
- Mean Citation Score: 336.657926
- Max Citation Score: 477.86942
- Similarity Product: 361.513459880004

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