Synthesis and Structure–Activity Relationships of Pyrazolo[1,5-a]pyridine Derivatives: Potent and Orally Active Antagonists of Corticotropin-Releasing Factor 1 Receptor

Yoshinori Takahashi; Shigeki Hibi; Yorihisa Hoshino; Koichi Kikuchi; Kogyoku Shin; Kaoru Murata-Tai; Masae Fujisawa; Mitsuhiro Ino; Hisashi Shibata; Masahiro Yonaga

doi:10.1021/jm300259r

Synthesis and Structure–Activity Relationships of Pyrazolo[1,5-a]pyridine Derivatives: Potent and Orally Active Antagonists of Corticotropin-Releasing Factor 1 Receptor

Journal of Medicinal Chemistry ◽

10.1021/jm300259r ◽

2012 ◽

Vol 55 (11) ◽

pp. 5255-5269 ◽

Cited By ~ 22

Author(s):

Yoshinori Takahashi ◽

Shigeki Hibi ◽

Yorihisa Hoshino ◽

Koichi Kikuchi ◽

Kogyoku Shin ◽

...

Keyword(s):

Corticotropin Releasing Factor ◽

Pyridine Derivatives ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Design of 2,5-Dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and Structure−Activity Relationships of a Series of Potent and Orally Active Corticotropin-Releasing Factor Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm040058e ◽

2004 ◽

Vol 47 (19) ◽

pp. 4787-4798 ◽

Cited By ~ 91

Author(s):

Chen ◽

Keith M. Wilcoxen ◽

Charles Q. Huang ◽

Yun-Feng Xie ◽

James R. McCarthy ◽

...

Keyword(s):

Corticotropin Releasing Factor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Synthesis and structure–activity relationships of 8-substituted-2-aryl-5-alkylaminoquinolines: Potent, orally active corticotropin-releasing factor-1 receptor antagonists

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2012.09.028 ◽

2012 ◽

Vol 20 (22) ◽

pp. 6559-6578 ◽

Cited By ~ 7

Author(s):

Kunitoshi Takeda ◽

Taro Terauchi ◽

Minako Hashizume ◽

Kohdoh Shikata ◽

Ryota Taguchi ◽

...

Keyword(s):

Corticotropin Releasing Factor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Design, Synthesis, and Structure–Activity Relationships of Novel Pyrazolo[5,1-b]thiazole Derivatives as Potent and Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm300864p ◽

2012 ◽

Vol 55 (19) ◽

pp. 8450-8463 ◽

Cited By ~ 9

Author(s):

Yoshinori Takahashi ◽

Minako Hashizume ◽

Kogyoku Shin ◽

Taro Terauchi ◽

Kunitoshi Takeda ◽

...

Keyword(s):

Corticotropin Releasing Factor ◽

Receptor Antagonists ◽

Thiazole Derivatives ◽

Design Synthesis ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2021.116019 ◽

2021 ◽

Vol 33 ◽

pp. 116019

Author(s):

Ikumi Kuriwaki ◽

Minoru Kameda ◽

Kazuhiko Iikubo ◽

Hiroyuki Hisamichi ◽

Yuichiro Kawamoto ◽

...

Keyword(s):

Systemic Exposure ◽

Pyrimidine Derivatives ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Synthesis, structure–activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2005.05.117 ◽

2005 ◽

Vol 15 (17) ◽

pp. 3870-3873 ◽

Cited By ~ 14

Author(s):

Xiaojun Han ◽

Jodi A. Michne ◽

Sokhom S. Pin ◽

Kevin D. Burris ◽

Lynn A. Balanda ◽

...

Keyword(s):

Anxiolytic Activity ◽

Corticotropin Releasing Factor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity

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Biphenylsulfonamide Endothelin Antagonists: Structure−Activity Relationships of a Series of Mono- and Disubstituted Analogues and Pharmacology of the Orally Active Endothelin Antagonist 2‘-Amino-N- (3,4-dimethyl-5-isoxazolyl)-4‘-(2-methylpropyl)[1,1‘-biphenyl]-2-sulfonamide (BMS-187308)

Journal of Medicinal Chemistry ◽

10.1021/jm970872k ◽

1998 ◽

Vol 41 (26) ◽

pp. 5198-5218 ◽

Cited By ~ 22

Author(s):

Natesan Murugesan ◽

Zhengxiang Gu ◽

Philip D. Stein ◽

Sharon Bisaha ◽

Steve Spergel ◽

...

Keyword(s):

Structure Activity Relationships ◽

Structure Activity ◽

Endothelin Antagonists ◽

Orally Active ◽

Endothelin Antagonist

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ChemInform Abstract: Orally Active Cephalosporins. Part 4. Synthesis, Structure-Activity Relationships and Oral Absorption of Novel 3-(4-Pyrazolylmethylthio)cephalosporins with Various C-7 Side Chains.

ChemInform ◽

10.1002/chin.200221193 ◽

2010 ◽

Vol 33 (21) ◽

pp. no-no

Author(s):

Hirofumi Yamamoto ◽

Yoshiteru Eikyu ◽

Shinya Okuda ◽

Kohji Kawabata ◽

Hisashi Takasugi ◽

...

Keyword(s):

Oral Absorption ◽

Side Chains ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Orally active cephalosporins. III. Synthesis and structure-activity relationships of new 3-heterocyclicthiomethylthio-7.BETA.-((Z)-2(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido)-3-cephem-4-carboxylic acids.

The Journal of Antibiotics ◽

10.7164/antibiotics.46.316 ◽

1993 ◽

Vol 46 (2) ◽

pp. 316-330 ◽

Cited By ~ 2

Author(s):

MASAHARU KUME ◽

TADATOSHI KUBOTA ◽

YASUO KIMURA ◽

HIROMU NAKASHIMIZU ◽

KIYOSHI MOTOKAWA

Keyword(s):

Carboxylic Acids ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Corrigendum to “Design, synthesis, and structure–activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists” [Bioorg. Med. Chem. 22 (2014) 6071–6088]

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2015.04.042 ◽

2015 ◽

Vol 23 (13) ◽

pp. 3870

Author(s):

Yu Yoshida ◽

Taro Terauchi ◽

Yoshimitsu Naoe ◽

Yuji Kazuta ◽

Fumihiro Ozaki ◽

...

Keyword(s):

Receptor Antagonists ◽

Design Synthesis ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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Dihydropyridopyrazinones and Dihydropteridinones as Corticotropin-Releasing Factor-1 Receptor Antagonists: Structure−Activity Relationships and Computational Modeling

Journal of Medicinal Chemistry ◽

10.1021/jm0611410 ◽

2007 ◽

Vol 50 (9) ◽

pp. 2269-2272 ◽

Cited By ~ 4

Author(s):

Carolyn D. Dzierba ◽

Andrew J. Tebben ◽

Richard G. Wilde ◽

Amy G. Takvorian ◽

Maria Rafalski ◽

...

Keyword(s):

Computational Modeling ◽

Corticotropin Releasing Factor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity

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