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Dive into the research topics where Donatella Chianelli is active.

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Featured researches published by Donatella Chianelli.


Journal of Medicinal Chemistry | 2017

Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)

David C. Tully; Paul Vincent Rucker; Donatella Chianelli; Jennifer A. Williams; Agnes Vidal; Phil B. Alper; Daniel Mutnick; Badry Bursulaya; James Schmeits; Xiangdong Wu; Dingjiu Bao; Jocelyn Zoll; Young Chul Kim; Todd Groessl; Peter McNamara; H. Martin Seidel; Valentina Molteni; Bo Liu; Andrew Phimister; Sean B. Joseph; Bryan A. Laffitte

The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases bile acid conjugation, transport, and excretion, thereby protecting the liver from the harmful effects of bile accumulation, leading to considerable interest in FXR as a therapeutic target for the treatment of cholestasis and nonalcoholic steatohepatitis. We identified a novel series of highly potent non-bile acid FXR agonists that introduce a bicyclic nortropine-substituted benzothiazole carboxylic acid moiety onto a trisubstituted isoxazole scaffold. Herein, we report the discovery of 1 (tropifexor, LJN452), a novel and highly potent agonist of FXR. Potent in vivo activity was demonstrated in rodent PD models by measuring the induction of FXR target genes in various tissues. Tropifexor has advanced into phase 2 human clinical trials in patients with NASH and PBC.


Archive | 2008

COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS

Xiaolin Li; Xiaodong Liu; Donatella Chianelli; Jon Loren; Juliet Nabakka; Timothy Michael Ramsey; Werner Breitenstein


Archive | 2007

Spiro imidazole derivatives as ppar modulators

Robert Epple; Ross Russo; Mihai Azimioara; Christopher Cow; Valentina Molteni; Xiaolin Li; Donatella Chianelli


Archive | 2007

Compositions and methods for modulating c-kit and pdgfr receptors

Donatella Chianelli; Christopher Cow; Yun He; Songchun Jiang; Xiaolin Li; Xiaodong Liu; Zuosheng Liu; Jon Loren; Valentina Molteni; Juliet Nabakka; Pingda Ren; Taebo Sim; Xiaodong Wang; Shuli You


Archive | 2007

Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors

Xiaolin Li; Donatella Chianelli; Jon Loren; Juliet Nabakka; Xiaodong Liu; Shifeng Pan; Yi Liu; Donald S. Karanewsky; Pascal Furet; Vito Guagnano; Shuli You


Archive | 2008

2-heteroarylamino-pyrimidine derivatives as kinase inhibitors

Donatella Chianelli; Valentina Molteni; Xiaolin Li; Xiaodong Liu; Juliet Nabakka; Jon Loren


Archive | 2009

HETEROCYCLIC COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS

Xiaolin Li; Xiaodong Liu; Jon Loren; Valentina Molteni; Juliet Nabakka; Vince Yeh; Donatella Chianelli


Archive | 2011

COMPOSITIONS AND METHODS FOR MODULATING FXR

David C. Tully; Paul Vincent Rucker; Phillip B. Alper; Daniel Mutnick; Donatella Chianelli


Archive | 2010

Compounds and compositions as microsomal prostaglandin e synthase-1 inhibitors

Donatella Chianelli; Valentina Molteni; Pamela A. Albaugh; Ha-Soon Choi; Jon Loren; Zhicheng Wang; Pranab Mishra


Archive | 2008

5- (4- (haloalkoxy) phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors

Valentina Molteni; Xiaolin Li; Xiaodong Liu; Donatella Chianelli; Juliet Nabakka; Jon Loren; Shuli You

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Valentina Molteni

Genomics Institute of the Novartis Research Foundation

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Jon Loren

Genomics Institute of the Novartis Research Foundation

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Juliet Nabakka

Genomics Institute of the Novartis Research Foundation

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David C. Tully

Genomics Institute of the Novartis Research Foundation

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Christopher Cow

Genomics Institute of the Novartis Research Foundation

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