http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2764243-C2

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filingDate 2018-09-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2022-01-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e1bdaf69568a25ebf5c7b16c2d891fd
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7e266cf3b1ebdc27ef795e851534d423
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publicationDate 2022-01-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2764243-C2
titleOfInvention Heterocyclic compounds as pad inhibitors
abstract FIELD: chemistry. n SUBSTANCE: invention relates to a compound by the formula (I), stereoisomers thereof and pharmaceutically acceptable salts thereof, wherein X represents O or S; Y is selected from O or N; Z is N; A represents CR 1 ; B represents CR 2 ; n equals 0 or 1; R 1 and R 2 are independently selected from hydrogen; R 3 is absent when Y is O or N when Y is selected from the group consisting of hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C(O)C 1-6 alkyl, SO 2 C 1-6 alkyl, SO 2 C 3-6 cycloalkyl and SO 2 C 6 aryl, wherein SO 2 C 6 aryl and SO 2 C 1-6 alkyl are optionally substituted with C 1-6 alkoxy, halogen and C 6 aryl; R 10 and R 11 are taken together, forming a 5-6-membered monocyclic saturated heterocyclic ring, wherein the 5-6-membered monocyclic saturated heterocyclic ring is optionally substituted with substituents selected from the group consisting of amino, C 1 alkylamino, and -NHC(O)CH=CHCH 2 N(CH 3 ) 2 ; R 12 , R 13 , R 14 , and R 15 are independently selected from the group consisting of hydrogen and C 1-6 alkyl, R 16 is selected from a 9-membered bicyclic heteroaryl containing 1 to 2 heteroatoms selected from N or S, wherein the 9-membered bicyclic heteroaryl is optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkyl-C 6 aryl, C 2-6 alkenyl-C 6 aryl, C 1-6 alkyl-C 3-5 heterocyclyl, wherein the heterocyclyl comprises one heteroatom selected from a nitrogen or oxygen atom (oxetan, tetrahydropyran, piperidine), C 3-5 heteroaryl, and C 1-6 alkyl-C 3-5 heteroaryl, wherein heteroaryl comprises from 1 to 2 heteroatoms in the ring, selected from a nitrogen or sulpur atom (pyridine, pyrimidine, pyridazine, and thiazole), and wherein C 1-6 alkyl, C 1-6 alkyl-C 6 aryl, C 3-5 heteroaryl, C 1-6 alkyl-C 3-5 heteroaryl, and C 1-6 alkyl-C 3-5 heterocyclyl are optionally substituted with one or several groups selected from hydrogen, C 1-6 alkyl, C 1-6 alkoxy, C 3-8 cycloalkyl, halogen, hydroxyl, -CH 2 OH, and -COOH. The invention also relates to compounds by the formula (II) and compounds by the formula (III). n EFFECT: compounds represented by formulas (I), (II), (III) are intended for inhibiting the enzymatic activity of PAD4 in a cell; compound by the formula (I), formula (II), and formula (III) is intended for application for treating a PAD4-mediated condition selected from rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosus, and psoriasis. n n n n 19 cl, 1 tbl, 88 ex
priorityDate 2017-09-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID19844
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138491421
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138503069
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID423517454
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419068443
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID458396401
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138503211
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID413565356
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID23569
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418722377
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID2774502
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID450155124
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID453739895
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID4807
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138491410
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418710223
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID431049367
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID432156194
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID413374639
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID2760897
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID451525087
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418747663
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID69993
http://rdf.ncbi.nlm.nih.gov/pubchem/taxonomy/TAXID338536
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418732713
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID81138
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID122703071
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID1514172
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID8895
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID453625527
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID15512811
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418784431
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419584198
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID21900574
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418782633
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID457193212
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138491413
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418867797
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138503061
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID11240
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID165337
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID84431
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID353238
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID53427730
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418837871
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID101175
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID418390692

Total number of triples: 637.