- Synthesis of the CETP inhibitor torcetrapib: The resolution route and origin of stereoselectivity in the iminium ion cyclization
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A practical, efficient synthesis of (-)-(2R,4S)-4-[(3,5-bis- trifluoromethyl-benzyl)methoxycarbonylamino]-2-ethyl-6-trifluoromethyl-3, 4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (1), a cholesteryl ester transfer protein (CETP) inhibitor, is desc
- Damon, David B.,Dugger, Robert W.,Magnus-Aryitey, George,Ruggeri, Roger B.,Wester, Ronald T.,Tu, Meihua,Abramov, Yuriy
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- A concise asymmetric synthesis of torcetrapib
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(Chemical Equation Presented) Optically active torcetrapib was synthesized in seven steps from achiral precursors without the need for protecting groups, utilizing an enantioselective aza-Michael reaction to achieve asymmetry.
- Guino, Meritxell,Pim, Huat Phua,Caille, Jean-Claude,King, Kuok Hii
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p. 6290 - 6293
(2008/02/10)
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- Asymmetric synthesis of the cholesteryl ester transfer protein inhibitor torcetrapib
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Previously our group reported synthetic efforts used to synthesize kilogram quantities of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, 1, via a mid-stage resolution. This account describes research conducted to develop an asymmetri
- Damon, David B.,Dugger, Robert W.,Hubbs, Stephen E.,Scott, Jill M.,Scott, Robert W.
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p. 472 - 480
(2012/12/22)
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- CETP inhibitors in combination with antihypertensive agents and uses thereof
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This invention relates to pharmaceutical combinations of a cholesteryl ester transfer protein (CETP) inhibitor or a pharmaceutically acceptable salt thereof; and an antihypertensive agent or a pharmaceutically acceptable salt thereof, optionally in combination with an HMG CoA reductase inhibitor or a pharmaceutically acceptable salt thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from atherosclerosis, peripheral vascular disease, dyslipidemia, hyperbetaliproteinemia, hypoalphalipoproteinemia, hypercholesterolemia, hypertriglyceridemia, familial-hypercholesterolemia, cardiovascular disorders, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, angioplastic restenosis, hypertension, vascular complications of diabetes, obesity or endotoxemia in a mammal (including a human being either male or female).
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- Methods of treatment with CETP inhibitors and antihypertensive agents
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This invention relates to cholesterol ester transfer protein (CETP) inhibitors, pharmaceutical compositions containing such inhibitors, and the use of such inhibitors to treat certain disease/conditions optionally in combination with certain therapeutic agents e.g., antihypertensive agents.
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- Method for making 4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinoline
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Methods of preparing CETP inhibitors are disclosed.
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- 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines
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Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma l
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