A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity

Masanori Baba, Osamu Nishimura, Naoyuki Kanzaki, +9

Proceedings of the National Academy of Sciences

A Novel Cyclohexene Derivative, Ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), Selectively Inhibits Toll-Like Receptor 4-Mediated Cytokine Production through Suppression of Intracellular Signaling

Masayuki Ii, Naoko Matsunaga, Kaoru Hazeki, +6

Molecular Pharmacology

TAK-242 selectively suppresses Toll-like receptor 4-signaling mediated by the intracellular domain

Tomohiro Kawamoto, Masayuki Ii, Tomoyuki Kitazaki, +2

European Journal of Pharmacology

InflammationToll-like ReceptorsIntracellular DomainCytokineSignal Transduction +11

Analysis of binding site for the novel small‐molecule TLR4 signal transduction inhibitor TAK‐242 and its therapeutic effect on mouse sepsis model

Katsunori Takashima, Naoko Matsunaga, Mitsuhiro Yoshimatsu, +6

British Journal of Pharmacology

Role of tumor necrosis factor alpha in pathogenesis of pneumococcal pneumonia in mice

Koji Takashima, Kazuhiro Tateda, Tetsuya Matsumoto, +3

Infection and Immunity

Inflammatory Lung DiseaseLung InflammationHumoral ResponseImmunologyKlebsiella Pneumoniae +16

Therapeutic effects of TAK-242, a novel selective Toll-like receptor 4 signal transduction inhibitor, in mouse endotoxin shock model

Takukyu Sha, Mie Sunamoto, Tomoyuki Kitazaki, +3

European Journal of Pharmacology

InflammationToll-like ReceptorsCytokineSignal TransductionMedicine +9

TAK-599, a novel N-Phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties

Tomoyasu Ishikawa, Nobuyuki Matsunaga, H. TAWADA, +7

Bioorganic & Medicinal Chemistry

Medicinal ChemistryPharmaceutical ScienceAnti-mrsa Cephalosporin T-91825BiochemistryMedicine +6

TAK-652 Inhibits CCR5-Mediated Human Immunodeficiency Virus Type 1 Infection In Vitro and Has Favorable Pharmacokinetics in Humans

Masanori Baba, Katsunori Takashima, Hiroshi Miyake, +5

Antimicrobial Agents and Chemotherapy

MedicineHuman RetrovirusImmunologyAntiviral ResponseAntiviral Therapy +12

Orally active CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological activities of 1-benzazepine derivatives containing a sulfoxide moiety

Masaki Seto, Naoki Miyamoto, Katsuji Aikawa, +5

Bioorganic & Medicinal Chemistry

MedicineActive Ccr5 Antagonists1-Benzazepine DerivativesAntiviral Drug DevelopmentAntiviral Drug +5

Therapeutic effect of cefozopran (SCE-2787), a new parenteral cephalosporin, against experimental infections in mice

Yuji Iizawa, Kenji Okonogi, Rina Hayashi, +3

Antimicrobial Agents and Chemotherapy

Experimental InfectionsTherapeutic EffectHealth SciencesAntibioticsAntiparasitic Agent +12