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 1):
A cereblon E3 ubiquitin ligase binding compound having a chemical structure selected from: wherein:\n W is selected from the group consisting of CH 2 , CHR, C\u2550O, SO 2 , NH, N, optionally substituted cyclopropyl group, optionally substituted cyclobutyl group, and N-alkyl; \n W 3  is selected from C or N; \n each X is independently selected from the group consisting of O, S, and H 2 , \n Y is selected from the group consisting of CH 2 , \u2014C\u2550CR\u2032, NH, N-alkyl, N-aryl, N-hetaryl, N-cycloalkyl, N-heterocyclyl, O, and S; \n Z is selected from the group consisting of O, S, and H 2 ; \n G and G\u2032 are independently selected from the group consisting of H, alkyl (linear, branched, optionally substituted), OH, R\u2032OCOOR, R\u2032OCONRR\u2033, CH 2 -heterocyclyl optionally substituted with R\u2032, and benzyl optionally substituted with R\u2032; \n Q 1 , Q 2 , Q 3 , and Q 4  represent a carbon C substituted with a group independently selected from R\u2032, N or N-oxide; \n A is independently selected from the group H, alkyl (linear, branched, optionally substituted), cycloalkyl, Cl and F; \n R comprises \u2014CONR\u2032R\u2033, \u2014OR\u2032, \u2014NR\u2032R\u2033, \u2014SR\u2032, \u2014SO 2 R\u2032, \u2014SO 2 NR\u2032R\u2033, \u2014CR\u2032R\u2033\u2014, \u2014CR\u2032NR\u2032R\u2033\u2014, (\u2014CR\u2032O) n\u2032 R\u2033, -aryl, -hetaryl, -alkyl (linear, branched, optionally substituted), -cycloalkyl, -heterocyclyl, \u2014P(O)(OR\u2032)R\u2033, \u2014P(O)R\u2032R\u2033, \u2014OP(O)(OR\u2032)R\u2033, \u2014OP(O)R\u2032R\u2033, \u2014Cl, \u2014F, \u2014Br, \u2014I, \u2014CF 3 , \u2014CN, \u2014NR\u2032SO 2 NR\u2032R\u2033, \u2014NR\u2032CONR\u2032R\u2033, \u2014CONR\u2032COR\u2033, \u2014NR\u2032C(\u2550N\u2014CN)NR\u2032R\u2033, \u2014C(\u2550N\u2014CN)NR\u2032R\u2033, \u2014NR\u2032C(\u2550N\u2014CN)R\u2033, \u2014NR\u2032C(\u2550C\u2014NO 2 )NR\u2032R\u2033, \u2014SO 2 NR\u2032COR\u2033, \u2014NO 2 , \u2014CO 2 R\u2032, \u2014C(C\u2550N\u2014OR\u2032)R\u2033, \u2014CR\u2032\u2550CR\u2032R\u2033, \u2014CCR\u2032, \u2014S(C\u2550O)(C\u2550N\u2014R\u2032)R\u2033, \u2014SF 5  and \u2014OCF 3 ; \n R\u2032 and R\u2033 are independently selected from the group consisting of a bond, H, alkyl, cycloalkyl, aryl, heteroaryl, heterocyclic, \u2014C(\u2550O)R, heterocyclyl, each of which is optionally substituted; \n n\u2032 integer from 1-10; \n  represents a single bond or a double bond; \n  represents a bond that may be stereospecific ((R) or (S)) or non-stereospecific; and \n Rn comprises 1-4 independent functional groups, optionally substituted linear or branched alkyl (e.g., a C1-C6 linear or branched alkyl optionally substituted with one or more halogen, cycloalkyl (e.g., a C3-C6 cycloalkyl), or aryl (e.g., C5-C7 aryl)), optionally substituted aryl (e.g., an optionally substituted C5-C7 aryl), optionally substituted alkyl-aryl (e.g., an alkyl-aryl comprising at least one of an optionally substituted C1-C6 alkyl, an optionally substituted C5-C7 aryl, or combinations thereof), optionally substituted alkoxyl group (e.g., a methoxy, ethoxy, butoxy, propoxy, pentoxy, or hexoxy; wherein the alkoxyl may be substituted with one or more halogen, alkyl, haloalky, fluoroalkyl, cycloalkyl (e.g., a C3-C6 cycloalkyl), or aryl (e.g., C5-C7 aryl)), optionally substituted \n (e.g., optionally substituted with one or more halogen, alkyl, haloalky, fluoroalkyl, cycloalkyl (e.g., a C3-C6 cycloalkyl), or aryl (e.g., C5-C7 aryl)), optionally substituted (e.g., optionally substituted with one or more halogen, alkyl, haloalky, fluoroalkyl, cycloalkyl (e.g., a C3-C6 cycloalkyl), or aryl (e.g., C5-C7 aryl)), or atoms; and\n each of x, y, and z are independently 0, 1, 2, 3, 4, 5, or 6, \n n is an integer from 1-10 (e.g., 1-4).

Metadata:
- Claim Count in Document: 1.0
- Percentile: 91.0
- Lexical Diversity: 1.675
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15881318', '14822309', '15730728', '16346483', '15148253']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.766923384678533
- 35 USC 102 Novelty (BERT): 0.5862025719024656
- Combined Prediction Score: 0.7488513034009263
- Mean Citation Score: 365.22769200000016
- Max Citation Score: 518.0048
- Similarity Product: 424.07531619472513

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