1027346-21-9

Usage

Uses

Used in Pharmaceutical Industry:
Tert-butyl (3S)-3-[(2-methylpropyl)amino]piperidine-1-carboxylate is used as a key intermediate in the synthesis of various pharmaceuticals for its ability to contribute to the development of new drugs with potential therapeutic applications.
Used in Drug Discovery and Development:
In the field of drug discovery and development, tert-butyl (3S)-3-[(2-methylpropyl)amino]piperidine-1-carboxylate serves as a valuable building block, facilitating the creation of novel compounds with diverse pharmacological properties, which can be further optimized for specific therapeutic targets.
Used in Organic Chemistry:
As an organic chemistry building block, tert-butyl (3S)-3-[(2-methylpropyl)amino]piperidine-1-carboxylate is utilized for the synthesis of a wide range of biologically active molecules, including potential lead compounds for drug development, due to its unique structural features and reactivity.

Upstream product

• 78-84-2 isobutyraldehyde 
• 625471-18-3 tert-butyl (3S)-3-aminopiperidine-1-carboxylate 

Downstream Products

• 1009633-79-7 C₂₂H₃₂ClN₃O₂ 

Relevant academic research and scientific papers

Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors

The action of the aspartyl protease renin is the rate-limiting initial step of the renin-angiotensin-aldosterone system. Therefore, renin is a particularly promising target for blood pressure as well as onset and progression of cardiovascular and renal diseases. New pyrimidine derivatives 5–14 were designed in an attempt to enhance the renin inhibitory activity of compound 3 identified by our previous fragment-based drug design approach. Introduction of a basic amine essential for interaction with the two aspartic acids in the catalytic site and optimization of the S1/S3 binding elements including an induced-fit structural change of Leu114 (‘Leu-in’ to ‘Leu-out’) by a rational structure-based drug design approach led to the discovery of N-(piperidin-3-yl)pyrimidine-5-carboxamide 14, a 65,000-fold more potent renin inhibitor than compound 3. Surprisingly, this remarkable enhancement in the inhibitory activity of compound 14 has been achieved by the overall addition of only seven heavy atoms to compound 3. Compound 14 demonstrated excellent selectivity over other aspartyl proteases and moderate oral bioavailability in rats.

Heterocyclic compound and use thereof

Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.

AMIDE COMPOUNDS AND USE OF THE SAME

A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like