PATENT CLAIM ANALYSIS

Application Number: 15923895
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2019-02
Patent Classification: ["514", "338000"]

Abstract:
The present invention relates to benzimidazol-2-amines of general formula (I), in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11  and R 12  are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.

Claim (Index 27):
A method of treatment or prophylaxis of a disease comprising administering to a patient in need thereof a therapeutically effect amount of a compound of formula (I): wherein: R 1  is a halogen atom or a group selected from the group consisting of:\n C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, C 1 -C 6 -alkoxy, C 3 -C 6 -cycloalkyloxy, C 1 -C 6 -haloalkyl, C 1 -C 6 -haloalkoxy, (C 1 -C 3 -alkoxy)-(C 1 -C 6 -alkyl)-, cyano, nitro, (C 1 -C 6 -alkyl)-S\u2014, (C 1 -C 6 -alkyl)-S(\u2550O)\u2014, (C 1 -C 6 -alkyl)-S(\u2550O) 2 \u2014, (C 1 -C 6 -haloalkyl)-S\u2014, (C 1 -C 6 -haloalkyl)-S(\u2550O)\u2014, (C 1 -C 6 -haloalkyl)-S(\u2550O) 2 \u2014, \u2014C(\u2550O)OR 13 , \u2014C(\u2550O)N(R 14 )R 15 , \u2014N(R 14 )R 15 , \u2014N(R 14 )C(\u2550O)R 16 , aryl-O\u2014, aryl-(C 1 -C 3 -alkyl)-, heteroaryl-O\u2014, and heteroaryl-(C 1 -C 3 -alkyl)-, \n wherein said aryl and heteroaryl groups are optionally substituted with one or two substituents, which are independently selected from the group consisting of: \n C 1 -C 3 -alkyl, C 1 -C 3 -alkoxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, C 1 -C 3 -haloalkyl, C 1 -C 3 -haloalkoxy, halogen, cyano, \u2014C(\u2550O)OR 13 , and \u2014C(\u2550O)N(R 14 )R 5 ; \n R 2  is a hydrogen atom; R 3  is a hydrogen atom; R 4  is a hydrogen atom or a halogen atom; R 5  is a group selected from the group consisting of:\n R 13 OC(\u2550O)\u2014(C 1 -C 6 -alkyl)-, R 13 OC(\u2550O)\u2014(C 2 -C 6 -alkenyl)-, R 13 OC(\u2550O)\u2014(C 1 -C 6 -alkoxy)-, R 14 (R 15 )NC(\u2550O)\u2014(C 1 -C 6 -alkyl)-, R 14 (R 15 )NC(\u2550O)\u2014(C 2 -C 6 -alkenyl)-, and R 14 (R 15 )NC(\u2550O)\u2014(C 1 -C 6 -alkoxy)-; \n R 6  is a hydrogen atom, a halogen atom, or a group selected from the group consisting of:\n C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, (C 1 -C 3 -alkoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, C 1 -C 6 -haloalkyl, C 1 -C 6 -haloalkoxy, cyano, nitro, (C 1 -C 6 -alkyl)-S\u2014, (C 1 -C 6 -alkyl)-S(\u2550O)\u2014, (C 1 -C 6 -alkyl)-S(\u2550O) 2 \u2014, (C 1 -C 6 -haloalkyl)-S\u2014, \u2014N(R 14 )R 15 , and \u2014N(R 14 )C(\u2550O)R 16 ; \n R 7  is a hydrogen atom; R 8  is a C 1 -C 3 -alkyl group; R 9 , R 10 , and R 11  \n are independently selected from the group consisting of a hydrogen atom and C 1 -C 3 -alkyl; \n R 12  is a hydrogen atom; R 13  is a hydrogen atom or a group selected from the group consisting of:\n C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, HO\u2014(C 2 -C 6 -alkyl)-, and (C 1 -C 3 -alkoxy)-(C 1 -C 6 -alkyl)-; \n R 14  and R 15  \n are independently selected from the group consisting of: \n a hydrogen atom, C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, HO\u2014(C 2 -C 6 -alkyl)-, (C 1 -C 3 -alkoxy)-(C 2 -C 6 -alkyl)-, C 1 -C 6 -haloalkyl, H 2 N\u2014(C 2 -C 6 -alkyl)-, (C 1 -C 3 -alkyl)N(H)(C 2 -C 6 -alkyl)-, (C 1 -C 3 -alkyl) 2 N(C 2 -C 6 -alkyl)-, R 13 OC(\u2550O)\u2014(C 1 -C 6 -alkyl)-, 4- to 6-membered heterocycloalkyl, aryl, heteroaryl, aryl-(C 1 -C 6 -alkyl)-, and heteroaryl-(C 1 -C 6 -alkyl)-, \n wherein said aryl and heteroaryl groups are optionally substituted with one or two substituents, which are independently selected from the group consisting of: \n C 1 -C 3 -alkyl, C 3 -C 6 -cycloalkyl, C 1 -C 3 -alkoxy, C 3 -C 6 -cycloalkyloxy, C 1 -C 3 -haloalkyl, C 1 -C 3 -haloalkoxy, halogen, cyano, \u2014C(\u2550O)OR 13 , and \u2014C(\u2550O)NH 2 ; \n or R 14  and R 15  \n are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocycloalkyl, \n wherein said 4-6-membered heterocycloalkyl is optionally substituted with one substituent selected from the group consisting of: \n C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 1 -C 3 -alkoxy, C 1 -C 3 -haloalkoxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, amino, hydroxy, halogen, and cyano; \n or \n wherein said 4-6-membered heterocycloalkyl is optionally substituted with two halogen atoms; and \n R 16  is a hydrogen atom or a group selected from the group consisting of:\n C 1 -C 6 -alkyl, HO\u2014(C 1 -C 6 -alkyl)-, C 3 -C 6 -cycloalkyl, HO\u2014(C 3 -C 6 -cycloalkyl)-, C 1 -C 6 -haloalkyl, (C 1 -C 3 -alkoxy)-(C 1 -C 6 -alkyl)-, aryl, heteroaryl, and 4- to 6-membered heterocycloalkyl, \n wherein said aryl and heteroaryl groups are optionally substituted with one or two substituents, which are independently selected from the group consisting of: \n C 1 -C 3 -alkyl, C 3 -C 6 -cycloalkyl, C 1 -C 3 -alkoxy, C 3 -C 6 -cycloalkyloxy, C 1 -C 3 -haloalkyl, C 1 -C 3 -haloalkoxy, halogen, cyano, \u2014C(\u2550O)OR 13 , and \u2014C(\u2550O)N(R 14 )R 15 , \n or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of any of the foregoing.

Metadata:
- Claim Count in Document: 59.0
- Percentile: 90.0
- Lexical Diversity: 1.85714
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15118154', '15118157', '15742363', '15520384', '15744641']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8436864259198821
- 35 USC 102 Novelty (BERT): 0.6080606608398311
- Combined Prediction Score: 0.820123849411877
- Mean Citation Score: 539.6025579999998
- Max Citation Score: 631.552
- Similarity Product: 470.3866874694824

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