Discovery and Development of Aliskiren, the First‐in‐Class Direct Renin Inhibitor for the Treatment of Hypertension

Wood, Jeanette M.; Maibaum, Jürgen

doi:10.1002/9783527630943.ch10

Cited by 3 publications

(3 citation statements)

References 81 publications

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“…221 The discovery and development of aliskiren is a major achievement considering the challenges involved after the merger of two pharmaceutical company giants such as Ciba-Geigy and Sandoz to form Novartis. The article by Wood and Maibaum 202 on the history of the discovery and development of aliskiren is a testimony of how events unfolded leading to its launching as a first-in-class antihypertensive drug. Credit also goes to Speedel, who against many odds, achieved a large-scale synthesis of aliskiren at a cost that allowed Novartis to continue its development.…”

Section: Podolactones (Syngenta Crop Protection Basel Switzerland)mentioning

confidence: 99%

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My 50-Plus Years of Academic Research Collaborations with Industry. A Retrospective

Hanessian

2024

J. Org. Chem.

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Section: Podolactones (Syngenta Crop Protection Basel Switzerland)mentioning

confidence: 99%

“…The first ‘’Swiss Connection”. The development of aliskiren as a drug to control hypertension has a fascinating history dating back some 30 years . A brief synopsis is given below leading to our efforts in devising synthetic routes to aliskiren and its prototypes.…”

Section: Medicinal Chemistry-inspired Collaborations With Industry Ma...mentioning

confidence: 99%

My 50-Plus Years of Academic Research Collaborations with Industry. A Retrospective

Hanessian

2024

J. Org. Chem.

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“…In 1999, former Ciba employees founded Speedel to continue developing aliskiren. In 2003, after successful phase I clinical trials and improved process chemistry, aliskiren was licensed back to Novartis . Aldoril (methyldopa + hydrochlorothiazide), approved in 1962 but later discontinued, was the first hydrochlorothiazide combination to be approved.…”

Section: Hydrochlorothiazide Combinationsmentioning

confidence: 99%

A Survey of the Structures of US FDA Approved Combination Drugs

et al. 2018

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Combination drugs are an important class of US FDA approved pharmaceuticals. These drugs have been on a continuous growth trajectory since the first combination drugs were approved in the 1940s. In this Perspective, we report the first comprehensive compilation and analysis of US FDA approved combination drugs, from the first approval in 1943 through 2018. Our database contains 419 combination drugs, which are represented by 328 unique small molecule structures. Breakdown of these drugs according to disease category, structure, combination composition, and year of approval is presented as well as the top 24 most commonly used small molecule combination drug components. For frequently used small molecule components, we present “relationship diagrams” to aid in the visualization of the many drug combinations these structures are part of. The main body contains 10 disease-focused sections wherein every small molecule component utilized as part of a combination for each disease category is displayed.

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Catalytic asymmetric Friedel–Crafts synthesis of 1,1′-diaryl-2-substituted 4-pentenes enables stereoselective access to functionalized tetrahydronaphthalenes

2017

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A series of electron-rich arenes were reacted with 1-alkyl or 1-aryl 1′-allyl benzylic alcohols to give the corresponding 1,1′-diarylalkanes, in the presence of Lewis and Brønsted acids as catalysts. In the presence of HBF4, 1,1′-diarylalkanes containing an allylic chain were shown to form tetrahydronaphthalenes through a rearrangement involving spirocyclic intermediates. The mechanism of the cyclization is discussed.

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Discovery and Development of Aliskiren, the First‐in‐Class Direct Renin Inhibitor for the Treatment of Hypertension

Cited by 3 publications

References 81 publications

My 50-Plus Years of Academic Research Collaborations with Industry. A Retrospective

My 50-Plus Years of Academic Research Collaborations with Industry. A Retrospective

A Survey of the Structures of US FDA Approved Combination Drugs

Catalytic asymmetric Friedel–Crafts synthesis of 1,1′-diaryl-2-substituted 4-pentenes enables stereoselective access to functionalized tetrahydronaphthalenes

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