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 2):
The compound according to  claim 1 , wherein\n R 1  represents a group selected from in which \u201c*\u201d represents the point of attachment to the rest of the molecule, the ring of said group being, besides R 6 , optionally substituted further one or two times, differently or identically, with a R 7  group, or R 1  represents a group selected from in which \u201c*\u201d represents the point of attachment to the rest of the molecule; 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 4 -alkoxy; R 4  represents a hydrogen atom or a group selected from C 1 -C 3 -alkyl and C 1 -C 3 -fluoroalkyl; R 5  represents a hydrogen atom or a bromine atom; R 6  represents a hydrogen atom or a group selected from C 1 -C 6 -alkyl, C 1 -C 4 -fluoroalkyl, C 1 -C 4 -hydroxyalkyl, (C 1 -C 2 -alkoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 8 -cycloalkyl and (C 3 -C 8 -cycloalkyl)-(methyl)-,\n said C 3 -C 8 -cycloalkyl and said (C 3 -C 8 -cycloalkyl)-(methyl)- 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 methyl and trifluoromethyl; \n R 7  represents a halogen atom or a group selected from hydroxy, C 1 -C 6 -alkyl, C 1 -C 4 -fluoroalkyl, C 1 -C 4 -hydroxyalkyl, (C 1 -C 2 -alkoxy)-(C 1 -C 3 -alkyl)-, (C 1 -C 2 -fluoroalkoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 4 -cycloalkyl, (C 3 -C 4 -cycloalkyl)-(methyl)-, (phenyl)-(C 1 -C 3 -alkyl)-, 4- to 7-membered heterocycloalkyl, heterospirocycloalkyl, 5- to 6-membered heteroaryl, \u2014CN, \u2014(CH 2 ) x \u2014N(R 11 )R 11a , \u2014C(\u2550O)R 13 , \u2014C(\u2550O)\u2014N(R 11 )R 11a , \u2014N(R 11 )R 11a , C 1 -C 6 -alkoxy, C 1 -C 4 -fluoroalkoxy, (C 3 -C 4 -cycloalkyl)-(methoxy)-, C 1 -C 4 -alkylsulfanyl, S(\u2550O)\u2014R 13  and \u2014S(\u2550O) 2 \u2014R 13 ,\n said C 3 -C 4 -cycloalkyl, said (C 3 -C 4 -cycloalkyl)-(methyl)- and said (C 3 -C 4 -cycloalkyl)-(methoxy)- group being optionally substituted one, two or three times, identically or differently, with a fluorine atom or with a group selected from methyl and trifluoromethyl, \n said 4- to 7-membered heterocycloalkyl and said heterospirocycloalkyl group being optionally substituted one, two or three times, identically or differently, with a fluorine atom or with a group selected from oxo, methyl and trifluoromethyl, and \n said 5- to 6-membered heteroaryl group being optionally substituted one, two or three times, identically or differently, with a halogen atom or a group selected from methyl, trifluoromethyl and methoxy; or \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((CH 2 ) 3 )\u2014, \n \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 methoxy and ethoxy; R 9  represents a hydrogen atom or a methyl or ethyl 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 or two times, identically or differently, with a fluorine atom, chlorine atom or bromine atom, or a group selected from \u2014CN, methyl, trifluoromethyl and methoxy; \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 -fluoroalkyl, C 3 -C 4 -cycloalkyl, C 1 -C 4 -hydroxyalkyl, (C 1 -C 2 -alkoxy)-(C 1 -C 3 -alkyl)-, (C 3 -C 4 -cycloalkyl)-(methyl)- and benzyl, or R 11  and R 11a , together with the nitrogen atom they are attached to, represent a 4- to 6-membered heterocycloalkyl group, said group being optionally substituted one or two times, identically or differently, with a fluorine atom, or a group selected from hydroxy, oxo, \u2014CN, methyl, trifluoromethyl and methoxy; R 12  represents a hydrogen atom or a group selected from C 1 -C 4 -alkyl, C 1 -C 4 -fluoroalkyl, C 1 -C 4 -hydroxyalkyl, (C 1 -C 2 -alkoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 6 -cycloalkyl, (C 3 -C 6 -cycloalkyl)-(C 1 -C 2 -alkyl)-, C 2 -C 4 -alkenyl, 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 fluorine atom, a chlorine atom or a group selected from methyl, trifluormethyl and methoxy, \n said C 3 -C 6 -cycloalkyl group being optionally substituted one, two or three times, identically or differently, with a fluorine atom, a chlorine atom or a group selected from \u2014CN, methyl and trifluoromethyl; \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 3 -alkyl, trifluoromethyl and cyclopropyl, 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 group selected from C 1 -C 3 -alkyl, C 1 -C 3 -fluoroalkyl, C 1 -C 3 -alkoxy, trifluoromethoxy and (C 1 -C 2 -alkoxy)-(C 1 -C 2 -alkyl)-; R 15  represents a group selected from C 1 -C 4 -alkyl, C 1 -C 4 -fluoroalkyl, (C 1 -C 2 -alkoxy)-(C 1 -C 3 -alkyl)-, (C 1 -C 2 -alkoxy)-(ethoxy)-(C 1 -C 3 -alkyl)-, C 3 -C 6 -cycloalkyl, (C 3 -C 6 -cycloalkyl)-(C 1 -C 2 -alkyl)- and 4- to 7-membered heterocycloalkyl; R 16  represents a hydrogen atom or a C 1 -C 3 -alkyl group; x represents an integer selected from 1 and 2, 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): 0.7985853467498976
- 35 USC 102 Novelty (BERT): 0.5171296731405164
- Combined Prediction Score: 0.7704397793889595
- Mean Citation Score: 306.67584
- Max Citation Score: 309.4958200000001
- Similarity Product: 240.1566250222231

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