Discovery of A-971432, an orally bioavailable selective sphingosine-1-phosphate receptor 5 (S1P5) agonist for the potential treatment of neurodegenerative disorders

Journal of Medicinal Chemistry

Volumn 58, Issue 23, 2015, Pages 9154-9170

  Hobson, Adrian D ^a   Harris, Christopher M ^a   Van Der Kam, Elizabeth L ^a   Turner, Sean C ^a   Abibi, Ayome ^a,c   Aguirre, Ana L ^a   Bousquet, Peter ^a   Kebede, Tegest ^a   Konopacki, Donald B ^a   Gintant, Gary ^a   Kim, Youngjae ^a   Larson, Kelly ^a   Maull, John W ^a   Moore, Nigel S ^a   Shi, Dan ^a   Shrestha, Anurupa ^a   Tang, Xiubo ^b   Zhang, Peng ^b   Sarris, Kathy K ^a  

^a ABBVIE INC   (United States)

^b Shanghai ChemPartner Co Ltd   (China)

^c Firmenich Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [(3' (TRIFLUOROMETHYL) [1,1' BIPHENYL] 4 YL)METHYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [(3' ,4' DICHLORO [1,1' BIPHENYL] 4 YL)METHYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [(3' ,5' DICHLORO [1,1' BIPHENYL] 4 YL)METHYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [(4' ETHYL [1,1' BIPHENYL] 4 YL)METHYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [(4' METHYL [1,1' BIPHENYL] 4 YL)METHYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (4 CHLOROPHENOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (BENZYLOXY) 2 CHLOROBENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (BENZYLOXY) 2 METHYLBENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (BENZYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (DECYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (HEPTYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (HEXYLOXY)BENZYL] 3 METHYLPIPERIDINE 4 CARBOXYLIC ACID; 1 [4 (HEXYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (HEXYLOXY)BENZYL]PIPERIDINE 3 CARBOXYLIC ACID; 1 [4 (HEXYLOXY)BENZYL]PIPERIDINE 4 CARBOXYLIC ACID; 1 [4 (HEXYLOXY)BENZYL]PYRROLIDINE 3 CARBOXYLIC ACID; 1 [4 (NONYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (OCTYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 (PENTYLOXY)BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(2 CHLOROBENZYL)OXY] 3 METHOXYBENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(2 METHYLBENZYL)OXY]BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(2,4 DICHLOROBENZYL)OXY] 3 METHOXYBENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(2,4 DICHLOROBENZYL)OXY]BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(3 CHLOROBENZYL)OXY]BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(3,4 DICHLOROBENZYL)OXY] 3 NITROBENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [(4 FLUOROBENZYL)OXY]BENZYL]AZETIDINE 3 CARBOXYLIC ACID; 1 [4 [[3 (TRIFLUOROMETHYL)BENZYL]OXY]BENZYL]AZETIDINE 3 CARBOXYLIC ACID; A 971432; CENTRAL NERVOUS SYSTEM AGENTS; UNCLASSIFIED DRUG; UNINDEXED DRUG; AZETIDINE 2 CARBOXYLIC ACID; AZETIDINE-2,3-DICARBOXYLIC ACID; BENZENE DERIVATIVE; SPHINGOSINE 1 PHOSPHATE RECEPTOR;

ALZHEIMER DISEASE; AMINATION; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; COGNITION; COGNITIVE DEFECT; CONTROLLED STUDY; DEGENERATIVE DISEASE; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG MEGADOSE; DRUG SCREENING; DRUG SYNTHESIS; DRUG TOLERABILITY; ELECTRIC RESISTANCE; FEMALE; HALF LIFE TIME; HAPLORHINI; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; IN VIVO STUDY; LIPID STORAGE; LOW DRUG DOSE; MALE; MAXIMUM PLASMA CONCENTRATION; MITSUNOBU REACTION; MOUSE; MULTIPLE SCLEROSIS; NONHUMAN; PLASMA PROTEIN BINDING; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; STEREOCHEMISTRY; TIME TO MAXIMUM PLASMA CONCENTRATION; WORKING MEMORY; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; BAGG ALBINO MOUSE; C57BL MOUSE; CELL LINE; CHEMISTRY; COGNITIVE AGING; DRUG EFFECTS; MACACA FASCICULARIS; METABOLISM; NEURODEGENERATIVE DISEASES; ORAL DRUG ADMINISTRATION; PATHOLOGY; SPRAGUE DAWLEY RAT;

ADMINISTRATION, ORAL; ANIMALS; AZETIDINECARBOXYLIC ACID; BENZENE DERIVATIVES; BLOOD-BRAIN BARRIER; CELL LINE; COGNITIVE AGING; DOGS; FEMALE; HUMANS; MACACA FASCICULARIS; MALE; MICE; MICE, INBRED BALB C; MICE, INBRED C57BL; NEURODEGENERATIVE DISEASES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, LYSOSPHINGOLIPID;

EID: 84949766855     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00928     Document Type: Article

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