DR. NORMAN B JAVITT, M.D.
Osteopathic Medicine in New York, NY

5494901, Feb 27, 1996

Jan 5, 1993

8/000935

Jonathan C. Javitt - Washington DC
Norman B. Javitt - New York NY
Peter McDonnell - Los Angeles CA

A61K 31715, A61K 3170

514 58

A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of. beta. -cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.

5773431, Jun 30, 1998

Apr 4, 1997

8/809435

Norman B. Javitt - New York NY

A61K 3156

514177

A method for preventing or reducing restenosis wherein a 27-hydroxycholesterol or a 25,26 and/or 27-aminocholesterol, or a sterol 27-hydroxylase stimulant, is administered in a restenosis preventing and/or reducing amount. The invention also includes a method for treating cancer using 27-hydroxycholesterol.

5418225, May 23, 1995

Jan 5, 1993

8/000935

Jonathan C. Javitt - Washington DC
Norman B. Javitt - New York NY
Peter McDonnell - Los Angeles CA

A61K 31715, A61K 3170

514 58

A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of. beta. -cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.

4939134, Jul 3, 1990

Sep 19, 1988

7/246444

Norman B. Javitt - New York NY
Stephen R. Wilson - Chatham NJ

New York University - New York NY

A61K 3156

514177

This invention relates to cholesterol synthesis and to the accumulation and regulation of cholesterol levels in body tissue. More specifically, the invention provides that the compound 26-aminocholesterol, ##STR1## and analogs and derivatives thereof, exhibit biological activity as a potent inhibitor of cholesterol synthesis and/or cholesterol accumulation in body tissue. The compounds strongly inhibit of the enzyme HMGCoA reductase and low density lipoprotein accumulation by non-hepatic cells. Surprisingly, it has been discovered that 26-aminocholesterol is selective for fibroblast (plasma) cells, and has little or no effect on hepato (liver) cells. Therapeutic compounds according to the invention include substituted or unsubstituted sterols of the formula: ##STR2## wherein the carbon atoms at positions 5 and 6 of the sterol are one of saturated and unsaturated, R. sub. 1 is one of a 3-hydroxyl group and a 3-keto group, R. sub. 2 is one of a hydroxyl group and a keto group, and wherein at least one of R. sub. 3, R. sub. 4 and R. sub.

2006012, Jun 8, 2006

Aug 25, 2005

11/212031

Norman Javitt - New York NY, US

A61K 39/395, A61K 31/56

424133100, 514169000

This invention relates to oxysteroids and oxysteroid hormones which have been identified. These oxysteroids are C27 modified sterols, particularly derivatives of intermediates in cholesterol synthesis, including lanosterol, zymosterol and desmosterol, including C27 diol and C27 acid derivatives, as well as related compounds and analogs thereof. The oxysteroids are capable of binding to or otherwise interacting with orphan nuclear receptors to result in modulation of gene expression. The invention further relates to methods of modulating the rate of cholesterol synthesis in a mammal. More specifically, the invention relates to treatment of cholesterol-related conditions which are improved or ameliorated by modulating the rate of cholesterol synthesis or cholesterol metabolism in a human in need thereof by administration of these oxysteroids, analogs or antagonists thereof. The invention includes methods for ameliorating, treating or preventing macular degeneration in a mammal comprising administering to said mammal an agent which stimulates or enhances the expression or activity of steroid sulphotransferase (SLUT2), particularly SLUT2B1b, or which stimulates or enhances the expression or activity of CYP27A1 or sterol 27-hydroxylase or otherwise increasing the sulfonation or 27-hydroxylation of cholesterol intermediates, including 7-ketocholesterol. Assays for identification of analogs, antagonists or modulators of these oxysteroids or of sterol 27-hydroxylase are also provided.

2004012, Jun 24, 2004

Sep 10, 2003

10/659764

Norman Javitt - New York NY, US

A61K039/395, A61K031/56

514/170000, 424/130100, 424/146100

Methods of reducing the cholesterol accumulation in a subject, including methods of reducing cholesterol synthesis and methods of increasing cholesterol degradation. Cholesterol synthesis is inhibited by administering a compound capable of increasing 27-hydroxy-7-dehydrocholesterol and/or 27-hydroxy-8-dehydrocholesterol levels, wherein an increase in 27-hydroxy-7-dehydrocholesterol and/or 27-hydroxy-8-dehydrocholesterol levels results in an inhibition of cholesterol synthesis. Cholesterol degradation is increased by increasing the level of 7-hydroxylase in extrahepatic tissue and cells.

5587368, Dec 24, 1996

Oct 6, 1994

8/319225

Norman B. Javitt - New York NY

New York University - New York NY

A61K 3156

514177

A method for preventing or reducing restenosis wherein a 27-hydroxycholesterol or a 25,26 and/or 27-aminocholesterol, or a sterol 27-hydroxylase stimulant, is administered in a restenosis preventing and/or reducing amount. The invention also includes a method for treating cancer using 27-hydroxycholesterol.

4427668, Jan 24, 1984

Apr 1, 1982

6/364338

Norman B. Javitt - New York NY

New York University - New York NY

A61K 3156

424238

Use of 26-hydroxycholesterol for reducing cholesterol synthesis and/or accumulation in body tissues.