Katalin T Prokai

7186707, Mar 6, 2007

Dec 9, 2003

10/731528

Laszlo Prokai - Gainesville FL, US
Katalin Prokai - Gainesville FL, US
James Simpkins - Fort Worth TX, US
Neeraj Agarwal - Fort Worth TX, US

University of Florida - Gainesville FL
University of North Texas Health Science Center - Fort Worth TX

A61K 31/56
C07J 1/00

514178, 552612

The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

7300926, Nov 27, 2007

Sep 17, 2003

10/666191

Laszlo Prokai - Gainesville FL, US
Katalin Prokai - Gainesville FL, US
James Simpkins - Fort Worth TX, US

University of Florida Research Foundation, Inc. - Gainesville FL
University of North Texas Health Science Center at Fort Worth - Fort Worth TX

A61K 31/56
C07J 1/00

514178, 552612

The present invention relates to novel estrogen-related steroidal quinols and their use as drugs for estrogen replacement therapy. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues, bone, in the cardiovascular system, and in the CNS (central nervous system) with only a slight estrogenic action or no estrogenic action in the uterus. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example, estrogen replacement therapy, prevention and treatment of osteoporosis).

7534779, May 19, 2009

Aug 14, 2007

11/838676

Laszlo Prokai - Mansfield TX, US
Katalin Prokai - Mansfield TX, US

University of Florida - Gainesville FL
University of North Texas Health Science Center - Fort Worth TX

A61K 31/56
C07J 1/00

514178, 562612, 562627

The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transcorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

7572781, Aug 11, 2009

Feb 15, 2007

11/706617

Laszlo Prokai - Gainesville FL, US
Katalin Prokai - Gainesville FL, US
James Simpkins - Fort Worth TX, US
Neeraj Agarwal - Fort Worth TX, US

University of Florida - Gainesville FL
University of North Texas Health Science Center - Fort Worth TX

A61K 31/56
C07J 1/00

514179, 514178, 514182, 552612

The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

20030229060, Dec 11, 2003

Apr 1, 2003

10/405413

Laszlo Prokai - Gainesville FL, US
Katalin Prokai - Gainesville FL, US
James Simpkins - Fort Worth TX, US

A61K031/58
A61K031/56

514/176000, 514/178000

The present invention relates to novel estrogen-related steroidal quinols and their use as prodrugs for phenolic estrogens and estrogen analogs. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues and penetration across the blood-brain barrier when compared to phenolic estrogens and estrogen analogs.

20070213310, Sep 13, 2007

Mar 5, 2007

11/682072

Laszlo Prokai - Mansfield TX, US
Katalin Prokai - Mansfield TX, US

A61K 31/56
C07J 51/00

514178000, 514182000, 552612000

The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).