PATENT CLAIM ANALYSIS

Application Number: 16460898
Application Type: Utility
Filing Date: 2019-07
Publication Date: 2019-10
Patent Classification: ["514", "218000"]

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 17):
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredients (a) a compound of formula (I) an N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or 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, or 4; 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 alkyloxycarbonyl; C 1-6 alkyl; C 1-6 alkyl 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 substituted with C 1-6 alkyloxycarbonyl; each R 2  is independently selected from: 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  is independently selected from the group consisting of: N, CH and CR 6 ; and A 2  is selected from the group consisting of: NH, O, S and NR 6 ; 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 C 1-6 alkyl substituted with R 7 ; 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 hydrogen; R 6  is selected from the group consisting of: C 1-4 alkyl; amino; mono- or di(C 1-4 alkyl)amino; and 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 and 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; 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 \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014O\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, \u2014S(\u2550O) p \u2014; and \n with X 2b  being \u2014NH\u2014NH\u2014, \u2014N\u2550N\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, \u2014S(\u2550O) p \u2014; \n p is 1 or 2; and 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: 100.0
- Lexical Diversity: 3.28148
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15963352', '14451761', '15655570', '11573224', '15713452']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8496532600215088
- 35 USC 102 Novelty (BERT): 0.6788378813846273
- Combined Prediction Score: 0.8325717221578206
- Mean Citation Score: 617.73722
- Max Citation Score: 675.7882
- Similarity Product: 667.4660864354372

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