PATENT CLAIM ANALYSIS

Application Number: 15996151
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-12
Patent Classification: ["514", "248000"]

Abstract:
The present disclosure relates to bifunctional compounds, which find utility as modulators of c-Met and/or p38 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Claim (Index 31):
A composition comprising a pharmaceutically acceptable carrier and an effective amount of at least one compound of  claim 1  for treating a disease or disorder associated with at least one of p38, p38\u03b1, p38\u03b2, p38\u03b3, p38\u03b4, or a combination thereof, the method comprising administering the composition to a subject in need thereof, wherein the compound is effective in treating or ameliorating at least one symptom of the disease or disorder and wherein:\n the PTM is represented by the chemical structure: \n wherein each X is independently H, OMe, or F; the linker (L) comprises a chemical structural unit represented by the formula:\n -(A) q -, wherein: \n (A) q  is a group which is connected to a ULM or PTM moiety; and \n q is an integer greater than or equal to 1; \n each A 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 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 heteocyclyl 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 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 cyclo 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, CCH, 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), NHSO 2 N(C 1-8 alkyl) 2 , NHSO 2 NH 2 ; the ULM is represented by the chemical structure: wherein\n R 1  is H, ethyl, isopropyl, tert-butyl, sec-butyl, cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; optionally substituted alkyl, optionally substituted hydroxyalkyl, optionally substituted heteroaryl, or haloalkyl; \n R 14a  is H, haloalkyl, optionally substituted alkyl, methyl, fluoromethyl, hydroxymethyl, ethyl, isopropyl, or cyclopropyl; \n R 15  is selected from the group consisting of H, halogen, CN, OH, NO 2 , optionally substituted heteroaryl, optionally substituted aryl; optionally substituted alkyl, optionally substituted haloalkyl, optionally substituted haloalkoxy, cycloalkyl, or cycloheteroalkyl (each optionally substituted); \n X is C or C\u2550O; and \n the dashed line indicates the site of attachment to the linker.

Metadata:
- Claim Count in Document: 34.0
- Percentile: 94.0
- Lexical Diversity: 1.83333
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15881318', '14822309', '15341275', '15730728', '15847628']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7838096913554208
- 35 USC 102 Novelty (BERT): 0.6255031691008807
- Combined Prediction Score: 0.7679790391299668
- Mean Citation Score: 439.84440000000006
- Max Citation Score: 695.188
- Similarity Product: 506.7374195537567

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