Delving into the Latest Updates on BAY-38-1315 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CETP

Mechanism

CETP inhibitors(Cholesteryl ester transfer protein inhibitors)

Therapeutic Areas

Cardiovascular DiseasesEndocrinology and Metabolic Disease

Active Indication-

Inactive Indication

AtherosclerosisHyperlipidemias

Originator Organization

Bayer AG

Active Organization-

Inactive Organization

Bayer AG

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

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Based on our former development candidate BAY 38-1315, optimization efforts led to the discovery of a novel chemical class of orally active cholesteryl ester transfer protein (CETP) inhibitors. The chromanol derivative 19b is a highly potent CETP inhibitor with favorable pharmacokinetic properties suitable for clinical studies. Chemical process optimization furnished a robust synthesis for a kilogram-scale process.

01 Mar 2010·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Novel tetrahydrochinoline derived CETP inhibitors

Q4 · MEDICINE

Article

Author: Carsten Schmeck ; Heike Gielen-Haertwig ; Gabriele Wirtz ; Olaf Weber ; Hilmar Bischoff ; Alexandros Vakalopoulos ; Volkhart Li

In the course of our efforts to identify orally active cholesteryl ester transfer protein (CETP) inhibitors, we have continued to explore tetrahydrochinoline derivatives. Based on BAY 19-4789 structural modifications led to the discovery of novel cycloalkyl substituted compounds. Thus, example 11b is a highly potent CETP inhibitor both in vitro and in vivo in transgenic mice with favourable pharmacokinetic properties for clinical development.

100 Deals associated with BAY-38-1315

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