Discovery of TAK-875: A potent, selective, and orally bioavailable GPR40 agonist

ACS Medicinal Chemistry Letters

Volumn 1, Issue 6, 2010, Pages 290-294

  Negoro, Nobuyuki ^a   Sasaki, Shinobu ^a   Mikami, Satoshi ^a   Ito, Masahiro ^a   Suzuki, Masami ^a   Tsujihata, Yoshiyuki ^a   Ito, Ryo ^a   Harada, Ayako ^a   Takeuchi, Koji ^a   Suzuki, Nobuhiro ^a   Miyazaki, Junichi ^a   Santou, Takashi ^a   Odani, Tomoyuki ^a   Kanzaki, Naoyuki ^a   Funami, Miyuki ^a   Tanaka, Toshimasa ^a   Kogame, Akifumi ^a   Matsunaga, Shinichiro ^a   Yasuma, Tsuneo ^a   Momose, Yu ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

Author keywords

agonist; GPR40; GSIS; insulin secretagogue; OGTT; TAK 875

Indexed keywords

[6 [[2',6' DIMETHYL 4' [3 (METHYLSULFONYL)PROPOXY]BIPHENYL 3 YL]METHOXY] 2,3 DIHYDRO 1 BENZOFURAN 3 YL]ACETIC ACID HEMI HYDRATE; ALKANOIC ACID; ANTIDIABETIC AGENT; DIHYDROBENZOFURAN DERIVATIVE; FUSED PHENYLALKANOIC ACID DERIVATIVE; G PROTEIN COUPLED RECEPTOR 40; GLUCOSE; INSULIN; TAK 875; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DOSE RESPONSE; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STABILITY; DRUG STRUCTURE; FEMALE; GLUCOSE BLOOD LEVEL; IMPAIRED GLUCOSE TOLERANCE; IN VITRO STUDY; INSULIN BLOOD LEVEL; INSULIN LIKE ACTIVITY; INSULIN RELEASE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PRIORITY JOURNAL; RAT; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION;

RATTUS;

EID: 77956500937     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml1000855     Document Type: Article

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15. Manuscript in preparation on lead discovery process.
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