Other

Queen's University at Kingston

Clariant Corporation

The Hong Kong Polytechnic University

Archimica Gmbh

Victor Snieckus

Stefan Scherer

David B Reitz

Horng-Chih Huang

Martin Petkovich

Donald Andrew Cameron

Ching-Cheng Wang

Andrew James Carpenter

Toni Kristian Rantanen

Johnathan Board

Suneel Singh

Ashishkumar Jayantilal Maheta

Jinglin (James T) Li

Andreas Meudt

Kwok-yin Wong

Sven Nerdinger

Bernd Lehnemann

Cheuk-Sang Kwok

Chi Huang

Yigang Zhao

Jörg Jung

Till Vogel

Compounds described herein are inhibitors of retinoic add inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids.

Compounds and methods for inhibiting CPY26 enzymes

Compounds described herein are inhibitors of retinoic acid inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids.

Compounds and methods for inhibiting CYP26 enzymes

Embodiments of the invention provide a method of using Schwartz Reagent, CpZr(H)Cl, without accumulating or isolating it. Methods provide mixtures of CpZrCl, reductants that selectively reduce CpZrCl, and substrates. After reaction of CpZrCland the reductant, an intermediate reduction product is formed, apparently Schwartz Reagent. The in situ Schwartz Reagent then selectively reduces certain functional groups on the substrate. Substrates include tertiary amides, tertiary benzamides, aryl O-carbamates, and heteroaryl N-carbamates, which are reduced to aldehydes, benzaldehydes, aromatic alcohols, and heteroaromatics, respectively. Compared to prior methods, reagents are inexpensive and stable, reaction times are short, and reaction temperature in certain cases is conveniently room temperature. It has been estimated that using the in situ method described herein instead of synthesized or commercially obtained Schwartz Reagent provides a 50% reduction in cost.

Schwartz reagents: methods of in situ generation and use

Metal chelates are useful for improving the contrast of X-ray, ultrasound, radionuclide and magnetic resonance (MR) images. However, the metal complexes must be stable and inert so that toxicity resulting from dissociation in the body can be minimized. This invention provides 16-member ring metal chelates that can provide a charge balanced metal complex having improved stability, especially for gadolinium(III) and samarium (III).

16-member ring metal chelate

A process for preparing anilineboronic acid derivative of the formula I, by converting an aniline to a diprotected aniline by introducing two protecting groups, metalating the diprotected aniline with a metalating agent and simultaneously or subsequently reacting with a boronic ester B(OR)to form a protected anilineboronic ester, which is converted, by detaching the protecting groups, to the anilineboronic esters of the formula (I).

Preparation of Anilineboronic acids and derivatives thereof

A process for preparing enantiomerically enriched tetrahydrobenzothipeine oxides comprises cyclizing an enantiomerically enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.

Method of preparing enantiomerically-enriched tetrahydrobenzothiepine oxides

A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant:in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents Rto Rhaving the following meanings: As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R, R, R, R=methyl, R, R=H).

Process for preparing bisallylboranes and nonaromatic boronic acids

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Kingston, Canada

Victor Snieckus