PATENT CLAIM ANALYSIS

Application Number: 15963352
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["514", "255050"]

Abstract:
This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a 1 =a 2 -a 3 =a 4 - and -b 1 =b 2 -b 3 =b 4 - represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R 1  is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl; substituted C 1-6 alkyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyloxy; substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; R 2  is hydroxy, halo, optionally substituted C 1-6 alkyl, C 3-7 cycloalkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O) p R 6 , —NH—S(═O) p R 6 , —C(═O)R 6 , —NHC(═O)H, —C(═O)NHNH 2 , —NHC(═O)R 6 , —C(═NH)R 6  or a 5-membered heterocycle; X 1  is —NR 5 —, —NH—NH—, —N═N—, —O—, —C(═O)—, C 1-4 alkanediyl, —CHOH—, —S—, —S(═O) p —, —X 2 —C 1-4 alkanediyl- or —C 1-4 alkanediyl-X 2 —; R 3  is NHR 13 ; NR 13 R 14 ; —C(═O)—NHR 13 ; —C(═O)—NR 13 R 14 ; —C(═O)—R 15 ; —CH═N—NH—C(═O)—R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl; substituted C 2-6 alkynyl; C 1-6 alkyl substituted with hydroxy and a second substituent; —C(═N—O—R 8 )—C 1-4 alkyl; R 7 ; or —X 3 —R 7 ; R 4  is halo, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, cyano, nitro, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkyloxy, aminocarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyl, formyl, amino, mono- or di(C 1-4 alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

Claim (Index 16):
A combination containing (a) a compound of formula (I) an N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein -a 1 =a 2 -a 3 =a 4 - represents a bivalent radical of formula:\n \u2014CH\u2550CH\u2014CH\u2550CH\u2014\u2003\u2003(a-1); \n -b 1 =b 2 -b 3 =b 4 - represents a bivalent radical of formula:\n \u2014CH\u2550CH\u2014CH\u2550CH\u2014\u2003\u2003(b-1); \n n is 0, 1, 2, 3, 4, or 5; m is 1, 2, 3, or 4; R 1  is selected from the group consisting of: hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl, wherein said C 1-6 alkyl is substituted with a member selected from the group consisting of: formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, and C 1-6 alkylcarbonyloxy; and C 1-6 alkyloxyC 1-6 alkylcarbonyl, wherein said C 1-6 alkyloxyC 1-6 alkylcarbonyl is substituted with C 1-6 alkyloxycarbonyl; each R 2  independently is selected from the group consisting of: hydroxy, halo, C 1-6 alkyl optionally substituted with cyano or \u2014C(\u2550O)R 6 , C 3-7 cycloalkyl, C 2-6 alkenyl optionally substituted with one or more halogen atoms or cyano, C 2-6 alkynyl optionally substituted with one or more halogen atoms or cyano, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethylthio, \u2014S(\u2550O) p R 6 , \u2014NH\u2014S(\u2550O) p R 6 , \u2014C(\u2550O)R 6 , \u2014NHC(\u2550O)H, \u2014C(\u2550O)NHNH 2 , \u2014NHC(\u2550O)R 6 , \u2014C(\u2550NH)R 6  and a radical of formula wherein each A 1  independently is N, CH or CR 6 ; and\n A 2  is NH, O, S or NR 6 ; \n X 1  is selected from the group consisting of: \u2014NR 5 \u2014, \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014O\u2014, \u2014C(\u2550O)\u2014, C 1-4 alkanediyl, \u2014CHOH\u2014, \u2014S\u2014, \u2014S(\u2550O) p \u2014, \u2014X 2 \u2014C 1-4 alkanediyl- and \u2014C 1-4 alkanediyl-X 2 \u2014; X 2  is selected from the group consisting of: \u2014NR 5 \u2014, \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014O\u2014, \u2014C(\u2550O)\u2014, \u2014CHOH\u2014, \u2014S\u2014, and \u2014S(\u2550O) p \u2014; R 3  is R 7 ; X 3  is selected from the group consisting of: \u2014NR 5 \u2014, \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014O\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, \u2014S(\u2550O) p \u2014, \u2014X 2 \u2014C 1-4 alkanediyl-, \u2014C 1-4 alkanediyl-X 2a \u2014, \u2014C 1-4 alkanediyl-X 2b \u2014C 1-4 alkanediyl, and \u2014C(\u2550N\u2014OR 8 )\u2014C 1-4 alkanediyl-;\n with X 2a  being selected from the group consisting of: \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014O\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, and \u2014S(\u2550O) p \u2014; and \n with X 2b  being selected from the group consisting of: \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, and \u2014S(\u2550O) p \u2014; \n R 4  is selected from the group consisting of: halo, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, cyano, nitro, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkyloxy, aminocarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyl, formyl, amino, mono- or di(C 1-4 alkyl)amino and R 7 ; R 5  is selected from the group consisting of: hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl, wherein said C 1-6 alkyl is substituted with a member selected from the group consisting of: formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl and C 1-6 alkylcarbonyloxy; and C 1-6 alkyloxyC 1-6 alkylcarbonyl, wherein said C 1-6 alkyloxyC 1-6 alkylcarbonyl is substituted with C 1-6 alkyloxycarbonyl; R 6  is C 1-4 alkyl, amino, mono- or di(C 1-4 alkyl)amino or polyhaloC 1-4 alkyl; R 7  is a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic carbocycle or a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic heterocycle, wherein each of said carbocyclic or heterocyclic ring systems may optionally be substituted with one, two, three, four or five substituents each independently selected from the group consisting of: halo, hydroxy, mercapto, C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, mono or di(C 1-6 alkyl)aminoC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, C 1-6 alkylthio, cyano, nitro, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkyloxy, aminocarbonyl, \u2014CH(\u2550N\u2014O\u2014R 8 ), R 7a , \u2014X 3 \u2014R 7a  and R 7a \u2014C 1-4 alkyl; R 7a  is a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic carbocycle or a monocyclic, bicyclic or tricyclic saturated, partially saturated or aromatic heterocycle, wherein each of said carbocyclic or heterocyclic ring systems may optionally be substituted with one, two, three, four or five substituents each independently selected from the group consisting of: halo, hydroxy, mercapto, C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, mono or di(C 1-6 alkyl)aminoC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, C 1-6 alkylthio, cyano, nitro, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkyloxy, aminocarbonyl, and \u2014CH(\u2550N\u2014O\u2014R 8 ); R 8  is selected from the group consisting of: hydrogen, C 1-4 alkyl, aryl and arylC 1-4 alkyl; p is 1 or 2; aryl is phenyl or phenyl substituted with one, two, three, four or five substituents each independently selected from the group consisting of: halo, hydroxy, mercapto, C 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, mono or di(C 1-6 alkyl)aminoC 1-6 alkyl, C 1-6 alkylcarbonyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, C 1-6 alkylthio, cyano, nitro, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkyloxy, aminocarbonyl, R 7  and \u2014X 3 \u2014R 7 ; and (b) one or more immunomodulating agents.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 91.0
- Lexical Diversity: 3.28148
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14451761', '15655570', '11573224', '15713452', '15241615']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8525056583046488
- 35 USC 102 Novelty (BERT): 0.6777470362746048
- Combined Prediction Score: 0.8350297961016444
- Mean Citation Score: 590.84501
- Max Citation Score: 673.1336
- Similarity Product: 665.8362709297658

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