Discovery of 1-{4-[3-Fluoro-4-((3S,6R)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist

Benjamin P. Fauber; Olivier René; Yuzhong Deng; Jason DeVoss; Céline Eidenschenk; Christine Everett; Arunima Ganguli; Alberto Gobbi; Julie Hawkins; Adam R. Johnson; Hank La; Justin Lesch; Peter Lockey; Maxine Norman; Wenjun Ouyang; Susan Summerhill; Harvey Wong

doi:10.1021/acs.jmedchem.5b00597

Discovery of 1-{4-[3-Fluoro-4-((3S,6R)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.5b00597 ◽

2015 ◽

Vol 58 (13) ◽

pp. 5308-5322 ◽

Cited By ~ 40

Author(s):

Benjamin P. Fauber ◽

Olivier René ◽

Yuzhong Deng ◽

Jason DeVoss ◽

Céline Eidenschenk ◽

...

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Orally Bioavailable

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Faculty Opinions recommendation of Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.725547435.793507709 ◽

2015 ◽

Author(s):

Jefferson Tilley

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Orally Bioavailable

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A Drug with Lipophilicity-Dependent Potency Can Be Metabolically Stable: Discovery of a Potent and Selective Retinoic Acid Receptor-Related Orphan Receptor C2 (RORC2) Inverse Agonist as an Orally Bioavailable Anti-Inflammatory Agent

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b01545 ◽

2018 ◽

Vol 61 (23) ◽

pp. 10412-10414

Author(s):

Yibing Wang ◽

Hong Liu

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Inflammatory Agent ◽

Anti Inflammatory ◽

Orally Bioavailable

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AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c01197 ◽

2021 ◽

Vol 64 (18) ◽

pp. 13807-13829

Author(s):

Frank Narjes ◽

Antonio Llinas ◽

Stefan von Berg ◽

Johan Jirholt ◽

Sarah Lever ◽

...

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Orally Bioavailable

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Discovery of 3-Cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b00392 ◽

2018 ◽

Vol 61 (23) ◽

pp. 10415-10439 ◽

Cited By ~ 10

Author(s):

Mark E. Schnute ◽

Mattias Wennerstål ◽

Jennifer Alley ◽

Martin Bengtsson ◽

James R. Blinn ◽

...

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Orally Bioavailable

Download Full-text

Faculty Opinions recommendation of Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.725547435.793507346 ◽

2015 ◽

Author(s):

John Lowe

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Orally Bioavailable

Download Full-text

Faculty Opinions recommendation of Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.733846748.793550457 ◽

2018 ◽

Author(s):

John Lowe

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Orally Bioavailable

Download Full-text

Discovery of Chromane-6-Sulfonamide Derivative as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c01436 ◽

2021 ◽

Author(s):

Lei Chen ◽

Mei Su ◽

Qiu Jin ◽

Wei Wang ◽

Chun-Gu Wang ◽

...

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Sulfonamide Derivative

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OP0137 Complete Survival and Disease Amelioration in MRL/LPR Mice Following Therapeutic Administration of an Oral Retinoic Acid Receptor-Related Orphan Receptor Gamma T [RORGT] Inverse Agonist INV-17: A Promising Safe & Efficacious Novel Lupus Treatment

Annals of the Rheumatic Diseases ◽

10.1136/annrheumdis-2015-eular.2002 ◽

2015 ◽

Vol 74 (Suppl 2) ◽

pp. 120.2-120

Author(s):

A. Gaweco ◽

K. Matthews ◽

S. Palmer ◽

R. Shamilov ◽

K. Adam ◽

...

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor ◽

Therapeutic Administration

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Discovery of N-(2-benzyl-4-oxochroman-7-yl)-2-(5-(ethylsulfonyl) pyridin-2-yl) acetamide (b12) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist

Bioorganic Chemistry ◽

10.1016/j.bioorg.2021.105483 ◽

2021 ◽

pp. 105483

Author(s):

Lei Chen ◽

Mei Su ◽

Qiu Jin ◽

Chun-Gu Wang ◽

Israa Assani ◽

...

Keyword(s):

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor

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Discovery of [cis-3-({(5R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b00061 ◽

2018 ◽

Vol 61 (7) ◽

pp. 2973-2988 ◽

Cited By ~ 21

Author(s):

Mitsunori Kono ◽

Atsuko Ochida ◽

Tsuneo Oda ◽

Takashi Imada ◽

Yoshihiro Banno ◽

...

Keyword(s):

Acetic Acid ◽

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Inverse Agonist ◽

Orphan Receptor ◽

Acid Receptor

Download Full-text