PATENT CLAIM ANALYSIS

Application Number: 15982043
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-09
Patent Classification: ["549", "406000"]

Abstract:
The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 20 , X, Y, Q and Z have defined meanings.

Claim (Index 16):
A process for preparing a compound as claimed in  claim 1 , characterized by\n a) reacting an intermediate of formula (IV) with an intermediate of formula (V) wherein W is an appropriate leaving group with the variables as defined in  claim 1 ; b) converting compounds of formula (I) wherein X is C(\u2550O), herein referred to as compounds of formula (I-b), to compounds of formula (I) wherein X is CH 2 , herein referred to as compounds of formula (I-a), in the presence of lithium aluminium hydride in a suitable solvent with the variables as defined in  claim 1 ; c) reacting a carboxaldehyde of formula (VI), with an intermediate of formula (VII) with the variables as defined in  claim 1 ; d) reacting an intermediate of formula (IV) with a carboxaldehyde of formula HC(\u2550O)Z to obtain compounds of formula (I) wherein t is 1, herein referred to as compounds of formula (I-c), with the variables as defined in  claim 1 ; e) reacting an intermediate of formula (VIII) with lithium aluminium hydride in a suitable solvent, to obtain compounds of formula (I) wherein s is 1, herein referred to as compounds of formula (I-d) with the variables as defined in  claim 1 ; f) reacting an intermediate of formula (XXIV) with lithium aluminium hydride in a suitable solvent, to obtain compounds of formula (I) wherein R 4  is \u2014CH 2 \u2014OH, herein referred to as compounds of formula (I-e), with the variables as defined in  claim 1 ; g) converting an intermediate of formula (XIX) in the presence of a strong acid in a suitable solvent to obtain compounds of formula (III) with the variables as defined in  claim 1 ; h) reacting an intermediate of formula (IV) wherein s is 0, R 3  is hydrogen, is \u2014CR 9 \u2550C< and R 9  together with R 20  forms a direct bond, herein referred to as intermediates of formula (IV-c), with an intermediate of formula (V) wherein W is a suitable leaving group in a reaction-inert solvent to obtain compounds of formula (III) wherein s is 0 and R 3  is hydrogen, herein referred to as compounds of formula (III-a), with the variables as defined in  claim 1 ; h) Fisher indole synthesis starting form intermediates of formula (XXII) and (XXIII) to obtain compounds of formula (III) wherein R 6  is hydrogen, herein referred to as compounds of formula (III-b), with the variables as defined in  claim 1 .

Metadata:
- Claim Count in Document: 16.0
- Percentile: 93.0
- Lexical Diversity: 1.53061
- Patent Class: 549.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['12678961', '12938633', '12678680', '11575552', '12293545']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8165701492423245
- 35 USC 102 Novelty (BERT): 0.5980685927270468
- Combined Prediction Score: 0.7947199935907968
- Mean Citation Score: 491.280192
- Max Citation Score: 504.37778
- Similarity Product: 492.955425346861

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