PATENT CLAIM ANALYSIS

Application Number: 16063370
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2019-02
Patent Classification: ["514", "339000"]

Abstract:
The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R 1 , R 2 , R 3 , R 4  and R 5  are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.

Claim (Index 1):
A compound of general formula (I): in which: R 1  represents a group selected from pyrazolyl, imidazolyl, oxadiazolyl, triazolyl, isoxazolyl, thienyl, pyridin-2-yl, pyridin-4-yl, pyrimidinyl, triazinyl and pyrazinyl, said group being optionally substituted with one R 6  group, and said group being, additionally, optionally substituted one or two times, differently or identically, with a R 7  group, or R 1  represents a group selected from the ring of said group being, besides R 6 , optionally substituted further one or two times, differently or identically, with a R 7  group, in which \u201c*\u201d represents the point of attachment to the rest of the molecule, or R 1  represents a group selected from pyridine-3-yl or pyridazin-3-yl, optionally substituted with one R 8  group; R 2  represents a group selected from in which \u201c*\u201d represents the point of attachment to the rest of the molecule; R 3  represents a hydrogen atom or a halogen atom or a group selected from C 1 -C 4 -alkyl and C 1 -C 6 -alkoxy; R 4  represents a hydrogen atom or a halogen atom or a group selected from C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy and C 1 -C 4 -haloalkoxy; R 5  represents a hydrogen atom or a halogen atom or a group selected from C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl and C 3 -C 6 -cycloalkyl; R 6  represents a hydrogen atom or a group selected from C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -hydroxyalkyl, (C 1 -C 3 -alkoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 6 -cycloalkyl and (C 3 -C 6 -cycloalkyl)-(C 1 -C 3 -alkyl)-,\n said C 3 -C 6 -cycloalkyl and said (C 3 -C 6 -cycloalkyl)-(C 1 -C 3 -alkyl)- group being optionally substituted one, two or three times, identically or differently, with a fluorine atom, a chlorine atom or with a group selected from C 1 -C 3 -alkyl and C 1 -C 3 -haloalkyl; \n R 7  represents a halogen atom or a group selected from hydroxy, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -hydroxyalkyl, (C 1 -C 3 -alkoxy)-(C 1 -C 3 -alkyl)-, (C 1 -C 3 -haloalkoxy)-(C 1 -C 3 -alkyl)-, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, C 4 -C 8 -cycloalkenyl, (C 3 -C 8 -cycloalkyl)-(C 1 -C 3 -alkyl)-, (phenyl)-C 1 -C 3 -alkyl-, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, heterospirocycloalkyl, phenyl, heteroaryl, \u2014CN, \u2014(CH 2 ) x \u2014N(R 11 )R 11a , \u2014C(\u2550O)R 13 , \u2014C(\u2550O)\u2014OR 13 , \u2014C(\u2550O)\u2014N(R 11 )R 11a ,\n \u2014N(R 11 )R 11a , \u2014N(R 16 )\u2014C(\u2550O)\u2014R 13 , \u2014N(R 16 )\u2014S(\u2550O) 2 \u2014R 13 , \u2014N(R 16 )\u2014C(\u2550O)\u2014N(R 11 )R 11a , \u2014N(R 16 )\u2014C(\u2550O)\u2014OR 13 , C 1 -C 6 -alkoxy, C 1 -C 6 -haloalkoxy, C 3 -C 8 -cycloalkoxy-, (C 3 -C 8 -cycloalkyl)-(C 1 -C 3 -alkoxy)-, phenyloxy-, heteroaryloxy-, \u2014O\u2014(CH 2 ) x -phenyl, \u2014O\u2014(CH 2 ) x -heteroaryl, \n \u2014O\u2014C(\u2550O)\u2014R 13 , \u2014O\u2014C(\u2550O)\u2014N(R 11 )R 11a , C 1 -C 6 -alkylsulfanyl, C 1 -C 6 -haloalkylsulfanyl, \u2014S(\u2550O)\u2014R 13 , \u2014S(\u2550O) 2 \u2014R 13 , \u2014S(\u2550O) 2 \u2014N(R 11 )R 11a  and \u2014S(\u2550O)(\u2550NR 17 )R 13 ,\n said C 3 -C 8 -cycloalkyl, said (C 3 -C 8 -cycloalkyl)-(C 1 -C 3 -alkyl)- and said (C 3 -C 8 -cycloalkyl)-(C 1 -C 3 -alkoxy)- group being optionally substituted one, two or three times, identically or differently, with a fluorine atom, a chlorine atom or with a group selected from C 1 -C 3 -alkyl and C 1 -C 3 -haloalkyl, \n said 4- to 7-membered heterocycloalkyl, said 5- to 7-membered heterocycloalkenyl and said heterospirocycloalkyl group being optionally substituted one, two or three times, identically or differently, with a fluorine atom, a chlorine atom or with a group selected from oxo, C 1 -C 3 -alkyl and C 1 -C 3 -haloalkyl, and \n said heteroaryl group and said phenyl group being optionally substituted one, two or three times, identically or differently, with a halogen atom or a group selected from \u2014CN, C 1 -C 3 -alkyl, trifluoromethyl, C 1 -C 3 -alkoxy and trifluoromethoxy; or \n \n R 6  and R 7 , or two R 7  groups, when being attached to adjacent ring atoms of the group R 1 , together form a group selected from:\n \u2014(O\u2014CH 2 \u2014O)\u2014, \u2014(O\u2014(CH 2 ) 2 \u2014O)\u2014, \u2014(O\u2014(CH 2 ) 2 )\u2014, \u2014(CH 2 \u2014O\u2014CH 2 )\u2014, \u2014(NR 16 \u2014(CH 2 ) 2 \u2014O)\u2014, \u2014(NR 16 \u2014(CH 2 ) 3 \u2014O)\u2014, \u2014(S\u2014(CH 2 ) 2 )\u2014, \u2014(O\u2014(CH 2 ) 3 )\u2014, \u2014((CH 2 ) 3 )\u2014, \u2014((CH 2 ) 4 )\u2014, \u2014(O\u2014CH\u2550CH)\u2014, \u2014(S\u2014CH\u2550CH)\u2014; \n R 8  represents a hydrogen atom or a group selected from methyl, ethyl, methoxy, ethoxy and dimethylamino; R 9  represents a hydrogen atom or a \u2014CN or C 1 -C 3 -alkyl group; R 10  represents a group selected from \u2014C(\u2550O)R 12 , \u2014C(\u2550O)OR 13 , \u2014C(\u2550O)N(R 14 )R 14a , \u2014S(\u2550O) 2 R 15 , \u2014S(\u2550O) 2 N(R 14 )R 14a , 5- to 6-membered heteroaryl and phenyl,\n said 5- to 6-membered heteroaryl group and said phenyl group being optionally substituted one, two or three times, identically or differently, with a halogen atom or a group selected from \u2014CN, C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 1 -C 3 -alkoxy and C 1 -C 3 -haloalkoxy; \n R 11  and R 11a , independently from each other, represent a hydrogen atom or a group selected from C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 1 -C 6 -hydroxyalkyl, (C 1 -C 3 -alkoxy)-(C 1 -C 3 -alkyl)-, (C 3 -C 6 -cycloalkyl)-(C 1 -C 3 -alkyl)- and benzyl, or R 11  and R 11a , together with the nitrogen atom they are attached to, represent a 4- to 7-membered heterocycloalkyl group, said group being optionally substituted one or two times, identically or differently, with a halogen atom, or a group selected from hydroxy, oxo, \u2014CN, C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 1 -C 3 -alkoxy, \u2014C(\u2550O)R 8 , \u2014C(\u2550O)OR 8  and \u2014S(\u2550O) 2 R 18 ; R 12  represents a hydrogen atom or a group selected from C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -hydroxyalkyl, (C 1 -C 3 -alkoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 6 -cycloalkyl, (C 3 -C 6 -cycloalkyl)-(C 1 -C 3 -alkyl)-, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, 5- to 6-membered heteroaryl and phenyl,\n said 5- to 6-membered heteroaryl group and said phenyl group being optionally substituted one, two or three times, identically or differently, with a halogen atom or a group selected from \u2014CN, C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 1 -C 3 -alkoxy and C 1 -C 3 -haloalkoxy, \n said C 3 -C 6 -cycloalkyl group being optionally substituted one, two or three times, identically or differently, with a halogen atom or a group selected from \u2014CN, C 1 -C 3 -alkyl and C 1 -C 3 -haloalkyl; \n R 13  represents a group selected from C 1 -C 4 -alkyl and benzyl; R 14  and R 14a , independently from each other, represent a hydrogen atom or a group selected from C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl and benzyl, or R 14  and R 14a , together with the nitrogen atom they are attached to, represent a 4- to 7-membered heterocycloalkyl group, said group being optionally substituted one or two times, identically or differently, with a halogen atom or a group selected from hydroxyl, \u2014CN, C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 1 -C 3 -alkoxy, C 1 -C 3 -haloalkoxy and (C 1 -C 3 -alkoxy)-(C 1 -C 3 -alkyl)-; R 15  represents a group selected from C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -hydroxyalkyl, (C 1 -C 3 -alkoxy)-(C 1 -C 6 -alkyl)-, (C 1 -C 3 -alkoxy)-(C 2 -C 3 -alkoxy)-(C 1 -C 6 -alkyl)-, C 3 -C 6 -cycloalkyl, (C 3 -C 6 -cycloalkyl)-(C 1 -C 3 -alkyl)-, 4- to 7-membered heterocycloalkyl, 5- to 6-membered heteroaryl and phenyl,\n said 5- to 6-membered heteroaryl group and said phenyl group being optionally substituted one, two or three times, identically or differently, with a halogen atom or a group selected from \u2014CN, C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 1 -C 3 -alkoxy and C 1 -C 3 -haloalkoxy; \n R 16  represents a hydrogen atom or a group selected from C 1 -C 4 -alkyl and benzyl; R 17  represents a hydrogen atom or a group selected from \u2014CN, \u2014C(\u2550O)OR 13 , C 1 -C 4 -alkyl and benzyl; R 18  represents a C 1 -C 3 -alkyl group; x represents an integer selected from 1, 2, 3 and 4, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

Metadata:
- Claim Count in Document: 16.0
- Percentile: 94.0
- Lexical Diversity: 1.61404
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15080068', '14772865', '14403151', '13078192', '15083503']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7983062012921639
- 35 USC 102 Novelty (BERT): 0.5206813186148855
- Combined Prediction Score: 0.770543713024436
- Mean Citation Score: 306.67584
- Max Citation Score: 309.4958200000001
- Similarity Product: 217.455637791946

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