Richard S Stone

US Patent:

6528516, Mar 4, 2003

Filed:

May 4, 2001

Appl. No.:

09/743744

Inventors:

Mortimer M. Civan - Wynnewood PA
Richard A. Stone - Havertown PA
Claire H. Mitchell - Philadelphia PA
Kenneth A. Jacobson - Silver Springs MD

Assignee:

Trustees of the University of Pennsylvania, The Center for Technology Transfer - Philadelphia PA

International Classification:

A61K 31435

US Classification:

514277, 514913

Abstract:

This invention relates to a method of decreasing intraocular pressure by administrating an A3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen.

US Patent:

20030083227, May 1, 2003

Filed:

Aug 13, 2002

Appl. No.:

10/217755

Inventors:

Mortimer Civan - Wynnewood PA, US
Kenneth Jacobson - Silver Spring MD, US
Anthony MacKnight - Dunedin, NZ
Claire Mitchell - Philadelphia PA, US
Richard Stone - Havertown PA, US

International Classification:

A61K031/00

US Classification:

514/001000

Abstract:

Provided is a method for modulating, controlling or regulating intraocular pressure and secretion of the aqueous humor of the eye, in particular for treating or reducing elevated intraocular pressure or secretion, e.g., related to glaucomas. Selected combined drug therapy effectively and synergistically modulates intraocular pressure by either (1) double-blocking the uptake step, wherein both transporters in the first (entry step) of aqueous humor formation are blocked or inhibited; or (2) blocking the entry and exit steps, wherein the sodium-hydrogen (Na/H) exchanger underlying the entry step is blocked or inhibited, and also lowering or reducing the activity of the chloride (Cl) channels involved in the second (exit) step of aqueous humor formation. By combining the selected drugs or compounds to produce a combined or synergistic modulating effect, control of IOP is achieved at very low concentrations, with fewer adverse side-effects on the patient. Moreover, the selectivity of each component in the combination permits the fluid levels in the intraocular space to be tailored to the individual patient or circumstance.

US Patent:

20030153626, Aug 14, 2003

Filed:

Feb 25, 2003

Appl. No.:

10/374003

Inventors:

Mortimer Civan - Wynnewood PA, US
Richard Stone - Havertown PA, US
Claire Mitchell - Philadelphia PA, US
Kenneth Jacobson - Silver Springs MD, US

International Classification:

A61K031/137

US Classification:

514/651000

Abstract:

A method for decreasing intraocular pressure by administering an Asubtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen. These agents, by inhibiting influx or promoting efflux of aqueous humor, can be used to treat glaucoma.

US Patent:

20090258836, Oct 15, 2009

Filed:

Apr 6, 2009

Appl. No.:

12/419062

Inventors:

Mortimer M. Civan - Philadelphia PA, US
Kenneth A. Jacobson - Silver Spring MD, US
Marcel Y. Avila - Bogota, CO
Richard Stone - Havertown PA, US

International Classification:

A61K 31/7076
A61P 27/06

US Classification:

514 46, 514 45

Abstract:

Provided are methods for reducing intraocular pressure in an individual having an ocular disorder causing elevated intraocular pressure, such as glaucoma. The method comprises administering to the individual an effective intraocular pressure-reducing amount of a pharmaceutical composition comprising an Asubtype adenosine receptor (AAR) antagonist, including dihydropyridine, pyridine, pyridinium salt or triazoloquinazoline, and derivatives thereof expressly having AAR antagonist activity, including, e.g., the nucleoside-based AAR antagonist, MRS-3820. Further provided is a method for ensuring the delivery of a topically administered therapeutic composition for reducing intraocular pressure, wherein the method expressly requires physically opening a channel through the corneal barrier of the patient's eye by a microneedle or micropipette to permit transport of the topical composition to the anterior chamber of the eye.

US Patent:

56376049, Jun 10, 1997

Filed:

Jun 29, 1994

Appl. No.:

8/268035

Inventors:

Alan M. Laties - Philadelphia PA
Richard A. Stone - Havertown PA

Assignee:

The Trustees of the University of Pennsylvania - Philadelphia PA

International Classification:

A61K 3142

US Classification:

514374

Abstract:

A composition for the inhibition of the abnormal postnatal axial growth of the eye of a maturing animal which comprises a pharmaceutically effective amount of a muscarinic pharmacological antagonist relatively selective for blocking the cholinergic receptors in cells of the brain, neural tissue and/or neural ganglia but less selective for blocking the cholinergic receptors of the cells of smooth muscles at the front of the eye, said antagonist present in a carrier or diluent suitable for ocular administration. A suitable antagonist is pirenzepine. Other suitable antagonists are telenzepine and o-methoxy-sila-hexocyclium.

US Patent:

55677312, Oct 22, 1996

Filed:

Sep 27, 1994

Appl. No.:

8/313356

Inventors:

Alan M. Laties - Philadelphia PA
Richard A. Stone - Havertown PA

Assignee:

The Trustees of the University of Pennsylvania - Philadelphia PA

International Classification:

A61K 31195
A61K 31205

US Classification:

514554

Abstract:

A composition for the inhibition of the abnormal postnatal axial growth of the eye of a maturing animal which comprises a pharmaceutically effective amount of a gamma aminobutyric acid antagonist relatively selective for GABA. sub. B receptors in the cells of the eye, said antagonist present in a carrier or diluent suitable for ocular administration. A suitable antagonist is 2-OH saclofen.

US Patent:

53859391, Jan 31, 1995

Filed:

Apr 30, 1993

Appl. No.:

8/056056

Inventors:

Alan M. Laties - Philadelphia PA
Richard A. Stone - Havertown PA

Assignee:

The Trustees of the University of Pennsylvania - Philadelphia PA

International Classification:

A61K 31195
A61K 31205

US Classification:

514561

Abstract:

A composition for the inhibition of the abnormal postnatal axial growth of the eye of a maturing animal which comprises a pharmaceutically effective amount of a gamma aminobutyric acid antagonist relatively selective for GABA. sub. B receptors in the cells of the eye, said antagonist present in a carrier or diluent suitable for ocular administration. A suitable antagonist is 2-OH saclofen.

US Patent:

51225220, Jun 16, 1992

Filed:

May 11, 1990

Appl. No.:

7/522241

Inventors:

Alan M. Laties - Philadelphia PA
Richard A. Stone - Havertown PA

Assignee:

The Trustees of the University of Pennsylvania - Philadelphia PA

International Classification:

A61K 3155

US Classification:

514220

Abstract:

A composition for the inhibition of the abnormal postnatal axial growth of the eye of a maturing animal which comprises a pharmaceutically effective amount of a muscarinic pharmacological antagonist relatively selective for blocking the cholinergic receptors in cells of the brain, neural tissue and/or neural ganglia but less selective for blocking the cholinergic receptors of the cells of smooth muscles at the front of the eye, said antagonist present in a carrier or diluent suitable for ocular administration. A suitable antagonist is pirenzepine. Other suitable antagonists are telenzepine and o-methoxy-sila-hexocyclium.