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 6):
The compound according to  claim 1 , wherein\n X is C(\u2550O) or CHR 8  and R 8  is hydrogen; \u2014C(\u2550O)\u2014NR 17 R 18 ; arylC 1-6 alkyloxycarbonyl; C 1-6alkyl substituted with hydroxyl; piperazinylcarbonyl substituted with hydroxyl; hydroxyC 1-6 alkyl; hydroxyC 1-6 alkyloxyC 1-6 alkyl; pyrrolidinyl substituted with hydroxyl-C 1-6 alkyl; or piperidinylcarbonyl substituted with one or two substituents selected from hydroxy, C 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkyl(dihydroxy)C 1-6alkyl or C 1-6 alkyloxy(hydroxy)C 1-6 alkyl; R 17  and R 18  are each independently selected from hydrogen, C 1-6 alkyl, di(C 1-6 alkyl)aminoC 1-6 alkyl, arylC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl or hydroxyC 1-6 alkyl; is \u2014CR 9 \u2550C<, \u2014CHR 9 \u2014CH< or \u2014CHR 9 \u2014N<;\n R 1  is hydrogen, heteroaryl, C 1-6 alkyloxycarbonyl, C 1-12 alkyl or C 1-12 alkyl substituted with heteroaryl; \n R 3  is hydrogen, C 1-6 alkyl or heteroaryl; \n R 4  and R 5  are each independently hydrogen, halo, C 1-6 alkyl, cyano, cyanoC 1-6 alkyl, hydroxy or C 1-6 alkyloxy; \n when p is 1 then R 7  is arylC 1-6 alkyl or hydroxy; \n Z is a radical selected from (a-1), (a-2), (a-3), (a-4), (a-5), (a-6), (a-7), (a-8) and (a-9); \n R 10  or R 11  are each independently selected from hydrogen, halo, hydroxy, amino, C 1-6 alkyl, nitro, polyhaloC 1-6 alkyl, cyano, cyanoC 1-6 alkyl, tetrazoloC 1-6 alkyl, aryl, heteroaryl, heteroarylC 1-6 alkyl, aryl(hydroxy)C 1-6 alkyl, arylcarbonyl, C 1-6 alkylcarbonyl, C 3-7 cycloalkylcarbonyl, C 3-7 cycloalkyl(hydroxy)C 1-6 alkyl, arylC 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylcarbonyloxyC 1-6  alkyl, C 1-6 alkyloxycarbonylC 1-6 alkyloxyC 1-6 alkyl, hydroxyC 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkyloxycarbonylC 2-6 alkenyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkyloxycarbonyl, aminocarbonyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, hydroxycarbonyl, hydroxycarbonylC 1-6 alkyl and \u2014(CH 2 ) v \u2014(C(\u2550O)) r \u2014(CHR 19 ) u \u2014NR 13 R 14 ; \n v is 0 or 1; \n u is 0 or 1; \n R 12  is hydrogen or C 1-6 alkyl; \n R 13  and R 14  are each independently selected from hydrogen; C 1-12 alkyl; C 1-6 alkylcarbonyl; C 1-6 alkylsulfonyl; arylC 1-6 alkylcarbonyl; C 3-7 cycloalkylcarbonyl; \u2014(CH 2 ) k \u2014NR 15 R 16 ; C 1-12 alkyl substituted with a substituent selected from hydroxy, hydroxycarbonyl, cyano, C 1-6 alkyloxycarbonyl or aryl; or \n R 13  and R 14  together with the nitrogen to which they are attached form morpholinyl, pyrrolidinyl, piperazinyl or piperazinyl substituted with a substituent selected from C 1-6 alkyl or arylC 1-6 alkyloxycarbonyl; \n k is 2; \n R 15  and R 16  are each independently selected from hydrogen, C 1-6 alkyl or arylC 1-6 alkyloxycarbonyl; or \n R 15  and R 16  together with the nitrogen to which they are attached form morpholinyl or piperazinyl, or piperazinyl substituted with C 1-6 alkyloxycarbonyl; \n aryl is phenyl or phenyl substituted with halo; and \n heteroaryl is pyridinyl, indolyl, oxadiazolyl or tetrazolyl; and each pyridinyl, indolyl, oxadiazolyl or tetrazolyl can optionally be substituted with one substituent selected from C 1-6 alkyl, aryl or arylC 1-6 alkyl.

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): 0.8167364640931265
- 35 USC 102 Novelty (BERT): 0.5974327270970485
- Combined Prediction Score: 0.7948060903935187
- Mean Citation Score: 491.280192
- Max Citation Score: 504.37778
- Similarity Product: 489.7156282411026

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