PATENT CLAIM ANALYSIS

Application Number: 16003232
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-09
Patent Classification: ["548", "301100"]

Abstract:
The present invention encompasses compounds of formula (I) wherein the groups R 1  to R 4 , R 7 , A, D, E, F, V, W, X, Y, n, r and q are defined in claim  1,  their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.

Claim (Index 1):
A compound of formula (I) wherein\n R 1  is a group, optionally substituted by one or more, identical or different R b1  and/or R c1 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl;\n each R b1  is independently selected from among \u2014OR c1 , \u2014NR c1 R c1 , halogen, \u2014CN, \u2014C(O)R c1 , \u2014C(O)OR c1 , \u2014C(O)NR c1 R c1 , \u2014S(O) 2 R c1 , \u2014S(O)2NR c1 R c1 , \n \u2014NHC(O)R c1 , \u2014N(C 1-4 alkyl)C(O)R c1  and the bivalent substituent \u2550O, while \u2550O may only be a substituent in non-aromatic ring systems; \n each R c1  independently of one another denotes hydrogen or a group, optionally substituted by one or more, identical or different R d1  and/or R e1 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n each R d1  is independently selected from among \u2014OR e1 , \u2014NR e1 R e1 , halogen, \u2014CN, \u2014C(O)R e1 , \u2014C(O)OR e1 , \u2014C(O)NR e1 R e1 , \u2014S(O) 2 R e1 , \u2014S(O) 2 NR e1  R e1 , \n \u2014NHC(O)R e1 , \u2014N(C 1-4 alkyl)C(O)R e1  and the bivalent substituent \u2550O, while \u2550O may only be a substituent in non-aromatic ring systems; \n each R e1  independently of one another denotes hydrogen or a group, optionally substituted by one or more, identical or different R f1  and/or R g1 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n each R f1  is independently selected from among \u2014OR g1 , \u2014NR g1 R g1 , halogen, \u2014CN, \u2014C(O)R g1 , \u2014C(O)OR g1 , \u2014C(O)NR g1 R g1 , \u2014S(O) 2 R g1 , \u2014S(O) 2 NR g1 R g1 , \n \u2014NHC(O)R g1 , \u2014N(C 1-4 alkyl)C(O)R g1  and the bivalent substituent \u2550O, while \u2550O may only be a substituent in non-aromatic ring systems; \n each R g1  is independently selected from among hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n \n R 2  and R 3 , each independently, is selected from among hydrogen, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl, wherein said C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl is optionally substituted by one or more, identical or different R b2  and/or R c2 ;\n each R b2  is independently selected from among \u2014OR c2 , \u2014NR c2 R c2 , halogen, \u2014CN, \u2014C(O)R c2 , \u2014C(O)OR c2 , \u2014C(O)NR c2 R c2 , \u2014S(O) 2 R c2 , \u2014S(O) 2 NR c2 R c2 , \n \u2014NHC(O)R c2 , \u2014N(C 1-4 alkyl)C(O)R c2  and the bivalent substituent \u2550O, while \u2550O may only be a substituent in non-aromatic ring systems; \n each R c2  independently of one another denotes hydrogen or a group, optionally substituted by one or more, identical or different R d2  and/or R e2 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, C 4-6 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n each R d2  is independently selected from among \u2014OR e2 , \u2014NR e2 R e2 , halogen, \u2014CN, \u2014C(O)R e2 , \u2014C(O)OR e2 , \u2014C(O)NR e2 R e2 , \u2014S(O) 2 R e2 , \u2014S(O) 2 NR e2 R e2 , \n \u2014NHC(O)R e2 , \u2014N(C 1-4 alkyl)C(O)R e2  and the bivalent substituent \u2550O, while \u2550O may only be a substituent in non-aromatic ring systems; \n each R e2  independently of one another denotes hydrogen or a group selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, C 4-6 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n \n A is selected from among phenyl and 5-6 membered heteroaryl if F is carbon or \n A is 5-6 membered, nitrogen-containing heteroaryl if F is nitrogen; \n each R a4  is independently selected from among R a4  and R b4 ;\n each R a4 independently of one another is a group, optionally substituted by one or more, identical or different R b4  and/or R c4 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n each R b4  is independently selected from among \u2014OR c4 , \u2014NR c4 R c4 , halogen, \u2014CN, \u2014C(O)R c4 , \u2014C(O)OR c4 , \u2014C(O)NR c4 R c4 , \u2014C(O)NR g4 OR c4 , \u2014S(O) 2 R c4 , \n \u2014S(O) 2 NR c4 R c4 , \u2014NHSO 2 R c4 , \u2014N(C 1-4 alkyl)SO 2 R c4 , \u2014NHC(O)R c4  and \u2014N(C 1-4 alkyl)C(O)R c4 ; \n each R c4  independently of one another denotes hydrogen or a group, optionally substituted by one or more, identical or different R d4  and/or R e4 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n each R d4  is independently selected from among \u2014OR e4 , \u2014NR e4 R e4 , halogen, \u2014CN, \u2014C(O)R e4 , \u2014C(O)OR e4 , \u2014C(O)NR e4 R e4 , \u2014C(O)NR g4 OR e4 , \u2014S(O) 2 R e4 , \n \u2014S(O) 2 NR e4 R e4 , \u2014NHC(O)R e4  and \u2014N(C 1-4 alkyl)C(O)R e4 ; \n each R e4  independently of one another denotes hydrogen or a group, optionally substituted by one or more, identical or different R f4  and/or R g4 , selected from among C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n each R f4  is independently selected from among \u2014OR g4 , \u2014NR g4 R g4 , halogen, \u2014CN, \u2014C(O)R g4 , \u2014C(O)OR g4 , \u2014C(O)NR g4 R g4 , \u2014C(O)NR g4 OR g4 , \u2014S(O) 2 R g4 , \n \u2014S(O) 2 NR g4 R g4 , \u2014NHC(O)R g4  and \u2014N(C 1-4 alkyl)C(O)R g4 ; \n each R g4  is independently selected from among hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, C 6-10 aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; \n \n r denotes the number 0, 1, 2 or 3; \n n denotes the number 1, 2 or 3; \n each R 7  is independently selected from among halogen, C 1-4 alkyl, \u2014CN, C 1-4 haloalkyl, \u2014OC 1-4 alkyl and \u2014OC 1-4 haloalkyl; \n q denotes the number 0, 1, 2 or 3; \n W, X and Y is each independently selected from \u2014N\u2550 and \u2014CH\u2550, wherein the hydrogen in each \u2014CH\u2550 may be replaced by a substituent R 7  if present and wherein at least one of W, X and Y is \u2014N\u2550 and a maximum of two of W, X and Y can be \u2014N\u2550; \n V is oxygen or sulfur; \n D is nitrogen, E is carbon and F is carbon; or \n D is carbon, E is nitrogen and F is carbon; or \n D is carbon, E is carbon and F is nitrogen; \n or a salt thereof.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 94.0
- Lexical Diversity: 1.45763
- Patent Class: 548.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15503754', '15287958', '14790032', '14683173', '13746411']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.794370716574116
- 35 USC 102 Novelty (BERT): 0.5688516772815991
- Combined Prediction Score: 0.7718188126448643
- Mean Citation Score: 386.50986600000016
- Max Citation Score: 452.09863
- Similarity Product: 424.8623624272014

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