PATENT CLAIM ANALYSIS

Application Number: 15763807
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-11
Patent Classification: ["544", "238000"]

Abstract:
The present invention relates to a benzamide derivative of general formula I, a drug composition containing same and a use thereof as a drug, wherein the definitions of R 1 , Z and Q are as described in the description.

Claim (Index 1):
A compound of formula I, or a tautomer, an optical isomer and a pharmaceutically acceptable salt thereof: wherein: Q is selected from the group consisting of R a-f  is independently selected from the group consisting of H, halogen, hydroxyl, amino, C 1-6  alkyl and C 1-6 alkoxy, wherein the alkyl and the alkoxy may be optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxyl and amino, the amino may be optionally substituted by one or two C 1-6 alkyl; R 1  is: R 2  and R 3  are independently selected from the group consisting of H, C 1-6 alkyl, (CH 2 ) 0-3 -3\u02dc7-membered cycloalkyl and heterocycloalkyl containing 1 or 2 heteroatoms, and R 2  and R 3  are not hydrogen at the same time; wherein the C 1-6 alkyl may be optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxyl, amino, cyano, C 1-6 alkoxy, (C 0-6  alkyl) (C 0-6  alkyl) amino, (C 0-6  alkyl) thio, (C 1-6  alkyl)carbonyl and (C 1-6  alkyl) sulfonyl; the 3\u02dc7-membered cycloalkyl or heterocycloalkyl is substituted by one R m , wherein the R m  is selected from the group consisting of hydrogen, C 1-6 alkyl, hydroxyl, halogen and amino, the heteroatom of the heterocycloalkyl is selected from O, N and S; or R 2  and R 3 , together with the atoms attached thereto, form a 5, 6 or 7-membered ring, wherein, the 5, 6 or 7-membered ring is substituted by one R n , wherein the R n  is selected from hydrogen, C 1-6 alkyl, hydroxyl, halogen and amino; the 5, 6 or 7-membered ring, in addition to the N atom attaching to R 2  and R 3 , further contains 0, 1 or 2 heteroatoms selected from O, N, and S; R 4  is selected from the group consisting of C 1-6 alkyl, \u2014(CH 2 ) 0-1 -5\u02dc7-membered cycloalkyl, \u2014CO(CH 2 ) 0-1 \u2014R 5  and \u2014CONH\u2014R 6 , R 5  and R 6  are independently selected from C 1-6 alkyl and (CH 2 ) 0-1 -5\u02dc7-membered cycloalkyl; Z is (CH 2 ) 0-3 \u2014Y; Y is selected from the group consisting of 3\u02dc7-membered cycloalkyl, heterocycloalkyl containing 1 or 2 heteroatoms, hydroxyl, C 1-6 alkoxy, halogen, amino, cyano, nitro, alkenyl and alkynyl; wherein, the cycloalkyl, heterocycloalkyl, amino, alkenyl and alkynyl are optionally substituted by the substituents selected from the group consisting of C 1-6  alkyl, C 1-6 alkoxy, halogen, hydroxyl, amino, cyano and nitro; the heteroatom of the heterocycloalkyl is selected from N, S and O; with the proviso that the compound of formula I does not contain the following compounds: 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(1-methylbutyl) nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-isobutyl-N-methyl nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(1,3-dimethylbutyl) nicotinamide, N-cyclopentyl-6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-methyl nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(3,3-dimethylbutyl) nicotinamide, 6-{5-[(cyclopropylamino) carbonyl]-3-fluoro-2-methylphenyl}-N-ethyl-N-isopropyl nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(tertpentyl) nicotinamide, 6-{(5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(3,3,3-trifluoropropyl) nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(1,1-dimethyl butyl) nicotinamide, N-cyclohexyl-6-{5-[(cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl}-N-ethyl nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-methyl-N-(1-methylcyclopentyl) nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-isopropyl-N-methyl nicotinamide, 6-({5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(3,3,3-trifluoro-2-methylpropyl) nicotinamide, 6-{5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl}-N-(1-ethyl-1-methylpropyl) nicotinamide, 6-{5-[(cyclopropylamino) carbonyl]-3-fluoro-2-methylphenyl}-N-ethyl nicotinamide, N-cyclopropyl-3-fluoro-4-methyl-5-{5-[(4-methylpiperidin-1-yl)carbonyl]pyridine-2-yl}benzamide, N-cyclopropyl-3-{5-[(2-ethylpiperidin-1-yl)carbonyl]pyridine-2-yl}-5-fluoro-4-methyl benzamide, N-cyclopropyl-3-{5-[(2-ethyl-2-methylpiperidin-1-yl)carbonyl]pyridine-2-yl}-5-fluoro-4-methyl benzamide, N-cyclopropyl-3-fluoro-4-methyl-5-{5-[(2-propylpiperidin-1-yl)carbonyl]pyridine-2-yl}benzamide, N-cyclopropyl-3-{5-[(2,4-dimethylpiperidin-1-yl)carbonyl]pyridine-2-yl}-5-fluoro-4-methyl benzamide, N-cyclopropyl-3-{5-[(2,3-dimethylpiperidin-1-yl)carbonyl]pyridine-2-yl}-5-fluoro-4-methyl benzamide, N-cyclopropyl-3-fluoro-4-methyl-5-{5-[(2,2,3-trimethylpyrrolidine-1-yl)carbonyl]pyridine-2-yl}benzamide, N-cyclopropyl-3-{5-[(3-ethylpiperidin-1-yl)carbonyl]pyridine-2-yl}-5-fluoro-4-methyl benzamide, N-cyclopropyl-3-fluoro-4-methyl-5-{5-[(2-methylpiperidin-1-yl)carbonyl]pyridine-2-yl}benzamide, N-cyclopropyl-3-{5-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine-2-yl}-5-fluoro-4-methyl benzamide, N-cyclopropyl-3-fluoro-4-methyl-5-{5-[(3-methylpiperidin-1-yl)carbonyl]pyridine-2-yl}benzamide.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 90.0
- Lexical Diversity: 1.30303
- Patent Class: 544.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['10522955', '10581305', '12713448', '12875218', '12936784']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8422332725491402
- 35 USC 102 Novelty (BERT): 0.5290602884107665
- Combined Prediction Score: 0.8109159741353028
- Mean Citation Score: 363.297944
- Max Citation Score: 374.7806
- Similarity Product: 314.5627758111596

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