Abstract: The present invention relates to methods of use of aminodiphosphonate to modulate apolipoprotein E levels and the use of such compounds in therapy, including cardiovascular and neurological disease states.
Type:
Grant
Filed:
February 14, 2003
Date of Patent:
April 24, 2007
Assignee:
ILEX Products, Inc.
Inventors:
Hieu Trung Phan, Lân Mong Nguyen, Raymond Azoulay, Vinh Van Diep, Eric Joseph Niesor, Craig Leigh Bentzen, Yves Gyon Gellin, Anne Perez, Jean-Luc Thulliard
Abstract: A method for enhancing the efficacy of chemotherapy in the treatment of cancer in animals, particularly humans, is provided wherein isocoumarin derivatives that exhibit unique chemopotentiation properties are employed in a combination treatment with chemotherapy.
Abstract: The present invention provides a process for the preparation of homophthlate esters useful in the preparation of homophthalic anhydride reactants.
Type:
Grant
Filed:
July 28, 2003
Date of Patent:
September 28, 2004
Assignee:
Ilex Products, Inc.
Inventors:
William E. Bauta, William R. Cantrell, Jr., Dennis P. Lovett
Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
Type:
Grant
Filed:
September 26, 2001
Date of Patent:
March 16, 2004
Assignee:
Ilex Products, Inc.
Inventors:
Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
Abstract: The present invention provides for the preparation &bgr;-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-&bgr;-D-adenine nucleosides wherein a blocked 2-deoxy-&agr;-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of &bgr; to &agr;-anomer is at least 99:1.
Type:
Grant
Filed:
August 1, 2002
Date of Patent:
January 20, 2004
Assignee:
Ilex Products, Inc.
Inventors:
William E. Bauta, Brian D. Burke, Brian E. Schulmeier, William R. Cantrell, Jr., Dennis P. Lovett, Jose Puente
Abstract: The present invention provides a process from preparing isocoumarin-3-yl derivatives comprising reacting a homophthalic anhydride derivative with a carbonyl compound, wherein the carbonyl group is substituted with an acyl activating group, in the presence of a reaction medium comprising a solvent and a base. The invention also encompasses a process for the preparation of homophthalate esters useful in the preparation of homophthalic anhydride reactants as well as an integrated process wherein the twp reactions are carried out sequentially to afford the desired isocoumarin derivative.
Type:
Grant
Filed:
July 2, 2002
Date of Patent:
December 16, 2003
Assignee:
ILEX Products, Inc.
Inventors:
William E. Bauta, William R. Cantrell, Jr., Dennis P. Lovett
Abstract: Aminophosphonates alpha substituted by phenol groups of formula (I) have lipoprotein(a) lowering activity.
Type:
Grant
Filed:
April 3, 2000
Date of Patent:
December 9, 2003
Assignee:
Ilex Products, Inc.
Inventors:
Lan Mong Nguyen, Eric Niesor, Craig Leigh Bentzen, Hieu Trung Phan, Vinh Van Diep, Simon Floret, Raymond Azoulay, Alexandre Bulla, Yves Guyon-Gellin, Robert John Ife