- A New N-Trityl-Substituted Aminopyridinato Titanium Catalyst for Hydroamination and Hydroaminoalkylation Reactions - Unexpected Intramolecular C-H Bond Activation
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Sterically demanding 2,6-bis(tritylamino)pyridine is used for the synthesis of a mono(2,6-diaminopyridinato) titanium complex that undergoes unexpected intramolecular C-H bond activation to give access to an unusual 1-titanaisoindoline derivative. Both titanium complexes do not show high catalytic activity for hydroaminoalkylation reactions of alkenes but exceptional results are obtained in the field of alkene, alkyne, and allene hydroamination including room temperature activity for intramolecular alkene hydroamination, excellent regioselectivity of intermolecular alkyne and allene hydroamination as well as selectivity for hydroamination over hydroaminoalkylation during cyclization reactions of primary aminoalkenes.
- Lühning, Lars H.,Brahms, Christian,Nimoth, Jelte P.,Schmidtmann, Marc,Doye, Sven
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p. 2071 - 2082
(2015/10/19)
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- THERAPY FOR COMPLICATIONS OF DIABETES
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A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
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- ANTIHYPERTENSIVE THERAPY
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A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.
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- Method for treating resistant hypertension
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A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.
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- Synthesis and biological activity of allosteric modulators of GABA B receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines
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A series of 15 analogues of fendiline, and 34 derivatives of N-(3-phenylpropyl)-1-arylethylamine have been prepared for evaluation as positive allosteric modulators of GABAB receptors. The most active (EC50, 10 nM) was N-(3,3-diphenylpropyl)-1-(3-chloro-4-methoxyphenyl) ethylamine 6g. CSIRO 2006.
- Kerr, David I. B.,Ong, Jennifer,Perkins, Michael V.,Prager, Rolf H.,Puspawati, Ni Made
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p. 445 - 456
(2007/10/03)
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- ISOPRENOID DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME
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Isoprenoid derivatives represented by the general formula (I) wherein R represents a hydrogen atom or a lower alkyl group, X represents -CH2-, -O- or -NH-, n represents number of the double bond in trans-configuration and is 1 or 2, and m is an integer from 0 to 3. The compounds have a 5-lipoxygenase-inhibiting activity and are useful as a therapeutic agent for such diseases as allergy, nephritis, hepatitis, rheumatism and gastric ulcer.
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