The Discovery of Macitentan—A Standard Medicinal Chemistry Program?

Bolli, M.H.; Boss, C.; Gatfield, J.; Iglarz, M.; Treiber, A.

doi:10.1016/b978-0-12-409547-2.12455-2

Comprehensive Medicinal Chemistry III 2017

DOI: 10.1016/b978-0-12-409547-2.12455-2

|View full text |Cite

The Discovery of Macitentan—A Standard Medicinal Chemistry Program?

M.H. Bolli¹,

C. Boss²,

J. Gatfield³

et al.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2020

Publication Types

Select...

Article1

Relationship

Self Cite0

Independent1

Authors

Journals

Cited by 1 publication

(1 citation statement)

References 167 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…1 our medicinal chemistry program from the starting point bosentan (1) to the discovery of macitentan (10) is summarized. [1,17,21] Over the course of our medicinal chemistry program, we modified structure 1, including by adding specifically designed new structural features. We worked on the sulfonamide moiety, increasing the distance between the phenyl ring and the sulfur by putting a double bond in between.…”

mentioning

confidence: 99%

20 Years of Medicinal Chemistry – Always Look at the Bright Side (of Life)

Boss

2020

Chimia

View full text Add to dashboard Cite

This paper summarizes a personal perspective on key learnings from projects the author was involved in over the last 20 years. For example, the discovery of macitentan, the most successful molecule to date from this personal collection, marketed by J&J for the treatment of pulmonary arterial hypertension (PAH). [1] Then the discovery of ACT-462206, a dual orexin receptor antagonist for the treatment of insomnia disorder with a serendipitously short story from the screening hit to the drug [2] followed by the identification of daridorexant, another dual orexin receptor antagonist. Daridorexant successfully passed first pivotal phase 3 clinical trial in April 2020 for the treatment of insomnia disorder [3] ("Good things come to those who wait"). Finally, ACT-451840, an antimalarial drug with a novel mechanism of action, identified in the perfect collaboration between academia and industry. The compound is in phase 2 clinical development. [4] In addition, the importance of the screening compound collection is briefly discussed, as a key asset for drug discovery. The measures Idorsia implemented to obtain valuable hits from high-throughput screening (HTS) campaigns are elaborated. [5] Drug discovery is a multi-disciplinary business with unlimited exciting challenges asking for excessive optimism when tackling them in a playful manner.

show abstract

mentioning

confidence: 99%

20 Years of Medicinal Chemistry – Always Look at the Bright Side (of Life)

Boss

2020

Chimia

View full text Add to dashboard Cite

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

The Discovery of Macitentan—A Standard Medicinal Chemistry Program?

Cited by 1 publication

References 167 publications

20 Years of Medicinal Chemistry – Always Look at the Bright Side (of Life)

20 Years of Medicinal Chemistry – Always Look at the Bright Side (of Life)

Contact Info

Product

Resources

About