Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Journal of Medicinal Chemistry

Volumn 61, Issue 3, 2018, Pages 1130-1152

  Vazquez, Michael L ^a   Kaila, Neelu ^a   Strohbach, Joseph W ^a   Trzupek, John D ^a   Brown, Matthew F ^a   Flanagan, Mark E ^a   Mitton Fry, Mark J ^a   Johnson, Timothy A ^a   Tenbrink, Ruth E ^a   Arnold, Eric P ^a   Basak, Arindrajit ^a   Heasley, Steven E ^a   Kwon, Soojin ^a   Langille, Jonathan ^a   Parikh, Mihir D ^a   Griffin, Sarah H ^a   Casavant, Jeffrey M ^a   Duclos, Brian A ^a   Fenwick, Ashley E ^a   Harris, Thomas M ^a   Han, Seungil ^a   Caspers, Nicole ^a   Dowty, Martin E ^a   Yang, Xin ^a   Banker, Mary Ellen ^a   Hegen, Martin ^a   Symanowicz, Peter T ^a   Li, Li ^a   Wang, Lu ^a   Lin, Tsung H ^a   Jussif, Jason ^a   Clark, James D ^a   Telliez, Jean Baptiste ^a   Robinson, Ralph P ^a   Unwalla, Ray ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL] N PROPYLMETHANESULFONAMIDE; 2 METHYL N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL] 1 OXETAN 3 YLMETHANESULFONAMIDE; 2,2,2 TRIFLUORO N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]ETHANESULFONAMIDE; 3 CYANO N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]PROPANE 1 SULFONAMIDE; 4 FLUORO N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]BENZENESULFONAMIDE; ANTIRHEUMATIC AGENT; JANUS KINASE 1; JANUS KINASE INHIBITOR; N (3 CYANOPROP 1 YL) N' [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]SULFAMIDE; N (CYCLOPROPYL) N' [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]SULFAMIDE; N (CYCLOPROPYLMETHYL) 1 [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]METHANESULFONAMIDE; N BUTYL 1 [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]METHANESULFONAMIDE; N CYCLOPROPYL N' [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]SULFAMIDE; N ETHYL 1 [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]METHANESULFONAMIDE; N ETHYL N' [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]SULFAMIDE; N METHYL N [CIS 3 [(CYCLOPROPYLSULFONYL)METHYL]CYCLOBUTYL] 7H PYRROLO[2,3 D]PYRIMIDIN 4 AMINE; N METHYL N [CIS 3 [(ETHYLSULFONYL)METHYL]CYCLOBUTYL] 7H PYRROLO[2,3 D]PYRIMIDIN 4 AMINE; N METHYL N [CIS 3 [(PROPYLSULFONYL)METHYL]CYCLOBUTYL] 7H PYRROLO[2,3 D]PYRIMIDIN 4 AMINE; N PROP 1 YL N' [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]SULFAMIDE; N [CIS 3 [(BUTYLSULFONYL)METHYL]CYCLOBUTYL] N METHYL 7H PYRROLO[2,3 D]PYRIMIDIN 4 AMINE; N [CIS 3 [(PHENYLSULFONYL)METHYL]CYCLOBUTYL] N METHYL 7H PYRROLO[2,3 D]PYRIMIDIN 4 AMINE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL] 1 OXETAN 3 YLMETHANESULFONAMIDE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL] 1 PHENYLMTHANESULFONAMIDE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]BENZENESULFONAMIDE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]BUTANE 1 SULFONAMIDE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]CYCLOPROPANESULFONAMIDE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]ETHANESULFONAMIDE; N [CIS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]PROPANE 1 SULFONAMIDE; N [TRANS 3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]CYCLOBUTYL]PROPANE 1 SULFONAMIDE; PF 04965842; UNCLASSIFIED DRUG; UNINDEXED DRUG; CYCLOBUTANE DERIVATIVE; JANUS KINASE 2; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE; SULFONAMIDE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; AUTOIMMUNE DISEASE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; FEMALE; IC50; IN VIVO STUDY; LIGAND BINDING; LIVER CELL; LIVER MICROSOME; NONHUMAN; PLASMA CLEARANCE; PLASMA PROTEIN BINDING; RAT; VOLUME OF DISTRIBUTION AT STEADY-STATE; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DOG; ENZYME SPECIFICITY; EXPERIMENTAL ARTHRITIS; HUMAN; MOLECULAR MODEL; PRECLINICAL STUDY; PROTEIN CONFORMATION; TISSUE DISTRIBUTION;

ANIMALS; ARTHRITIS, EXPERIMENTAL; AUTOIMMUNE DISEASES; CYCLOBUTANES; DOGS; DRUG EVALUATION, PRECLINICAL; HUMANS; INHIBITORY CONCENTRATION 50; JANUS KINASE 1; JANUS KINASE 2; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PYRIMIDINES; PYRROLES; RATS; SUBSTRATE SPECIFICITY; SULFONAMIDES; TISSUE DISTRIBUTION;

EID: 85041902067     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.7b01598     Document Type: Article

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