PATENT CLAIM ANALYSIS

Application Number: 16059960
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2018-12
Patent Classification: ["514", "461000"]

Abstract:
Prodrugs of galiellactone, and derivatives thereof, are provided by reacting the parent compound, e.g. galiellactone, with a thiol. Such drugs may be administered orally to treat cancer and other proliferative diseases.

Claim (Index 18):
A compound according to formula (Ia), wherein R 1  is halo; R 1 \u2032 is selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO 2 C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO 2 C1-C5 alkyl, and N(C0-C5 alkyl)SO 2 C1-5 fluoroalkyl; R 2  and R 2 \u2032 are independently selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO 2 C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO 2 C1-C5 alkyl, and N(C0-C5 alkyl)SO 2 C1-5 fluoroalkyl; R 3  and R 3 \u2032 are independently selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO 2 C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO 2 C1-C5 alkyl, and N(C0-C5 alkyl)SO 2 C1-5 fluoroalkyl; and R 4  and R 4 \u2032 are independently selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl) 2  in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl) 2  in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO 2 C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO 2 C1-C5 alkyl, and N(C0-C5 alkyl)SO 2 C1-5 fluoroalkyl; as a free base, an acid in its non-charged protonated form, a pharmaceutically acceptable addition salt, solvate, solvate of a salt thereof, a pure diastereomer, a pure enantiomer, a diastereomeric mixture, a racemic mixture, a scalemic mixture, a corresponding tautomeric form resulting from a hydrogen shift between two hetero-atoms and/or the corresponding tautomeric form resulting from a keto-enol tautomerization.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 96.0
- Lexical Diversity: 1.22581
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15124096', '13811015', '15578589', '13202875', '12668599']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8432752613337675
- 35 USC 102 Novelty (BERT): 0.6772727814253712
- Combined Prediction Score: 0.8266750133429279
- Mean Citation Score: 556.556944
- Max Citation Score: 727.63806
- Similarity Product: 645.175180823071

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