Cytochroma Inc.

Johns Hopkins University

Queen's University at Kingston

Opko Ireland Global Holdings, Limited

Ecosynthetix Inc.

Eirgen Pharma Ltd.

Cyctochroma Inc.

Opko IP Holdings Ii, Inc.

Uttam Saha

Gary H Posner

Mehmet Kahraman

Martin Petkovich

Donald Andrew Cameron

P Martin Petkovich

Qiang Wang

Jay A White

Steven Bloembergen

Byung-Chul Suh

Glenville Jones

Hong Woon Yang

Christian F Helvig

Kenneth R Crawford

Rachel D Slack

Heung Bae Jeon

Lindsey C Hess

Steven M Silverman

Alvin S Kalinda

Jae Kyoo Lee

Compounds that are inhibitors of retinoic acid inducible P450 (CYP26) enzymes. The compounds have retinoid activity, are resistant to CYP26-mediated catabolism, act as inhibitors of CYP26B1, and are used for treating diseases that are responsive to retinoids.

Compounds and methods for inhibiting CYP26 enzymes

A stabilized 1,25-dihydroxyvitamin Dcomposition which is particularly well suited for pharmaceutical formulations, pharmaceutical formulations of the 1,25-dihydroxyvitamin Dcomposition, and a method of making the purified composition by purifying a crude 1,25-dihydroxyvitamin Dfrom acetone/water, are disclosed.

Stabilized 1, 25-dihydroxyvitamin D2 and method of making same

This patent describes formaldehyde free or formaldehyde reduced binders useful, for example, in a fiber based composite material such as glass or other mineral fiber insulation, non-woven fabric or wood-based board. In one example, melamine is used as an acidic solution or a salt. The salt or solution is used to create an aqueous binder with other components such as a polyol and a crosslinker. A preferred polyol is a nanoparticle comprising high molecular weight starch. In other examples, binders include mixtures of a polyol with urea and a crosslinker. In other examples, a multi-component nanoparticle is made by reacting a polyol such as starch in an extruder with an insolubilizer such as melamine or urea. The resulting particles are mixed with water, optionally with other components such as an additional crosslinker, to create an aqueous binder.

Formaldehyde free binder and multi-component nanoparticle

This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

1-deoxy analogs of 1,25-dihydroxyvitamin D3 compounds

This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.

Phosphate management with small molecules

The present invention provides novel 16,23-diene 25-oxime ether analogs of 1,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the novel compound of the invention are useful for treating diseases which benefit from a modulation of the levels of 1,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.

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The present invention provides novel D-ring and side-chain analogs of 1&#x3b1;,25-dihydroxyvitamin D, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1&#x3b1;,25-dihydroxyvitamin D, for example, cell-proliferative disorders.

A process for producing a compound of the formula: including reacting of a compound of the formula: with diphenyl phosphine oxide using a binary phase reaction mixture including diphenyl phosphine oxide in an organic solvent, a basic aqueous solution, and a phase transfer catalyst, to obtain the compound of formula 1,wherein Ph is phenyl, Xand Xare both hydrogen or Xand Xtaken together are CH, Ris a protecting group, Ris fluorine, hydrogen, or OR, wherein Ris a protecting group, and the squiggly line represents a bond that results in the adjacent double bond being in either the E or Z configuration, is disclosed.

Process for producing phosphine oxide vitamin D precursors

The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1&#x3b1;,25-dihydroxy vitamin D, for example, cell-proliferative disorders.

24-sulfoximine vitamin D3 compounds

Growing community of inventors

Thornhill, Canada

Uttam Saha