Lloyd Gary Tillman

US Patent:

6730679, May 4, 2004

Filed:

Mar 20, 1997

Appl. No.:

08/820848

Inventors:

Arup K. Roy - Greenville NC
Lloyd Gary Tillman - Carlsbad CA

Assignee:

SmithKline Beecham Corporation - Philadelphia PA

International Classification:

A61K 31495

US Classification:

514255, 5142312, 514307, 514365, 514458

Abstract:

Pharmaceutical formulations containing HIV protease inhibitors, specifically including 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester (alternatively known as VX 478 or 141W94), and a tocopherol, and their use in medical therapy are described.

US Patent:

6747014, Jun 8, 2004

Filed:

Dec 21, 2001

Appl. No.:

10/029598

Inventors:

Ching-Leou Teng - San Diego CA
Phillip Dan Cook - Fallbrook CA
Lloyd Tillman - Carlsbad CA
Gregory E. Hardee - Rancho Sante Fe CA
David J. Ecker - Encinitas CA
Muthiah Manoharan - Carlsbad CA

Assignee:

ISIS Pharmaceuticals, Inc. - Carlsbad CA

International Classification:

A61K 3170

US Classification:

514 44, 536 243, 536 2431, 536 2433, 536 245

Abstract:

The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e. g. , neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.

US Patent:

7576067, Aug 18, 2009

Filed:

Dec 1, 2004

Appl. No.:

11/000814

Inventors:

Susan Weinbach - San Diego CA, US
Lloyd G. Tillman - Oceanside CA, US
Richard S. Geary - Carlsbad CA, US
Gregory E. Hardee - Carlsbad CA, US

Assignee:

Isis Pharmaceuticals, Inc. - Carlsbad CA

International Classification:

A61K 31/70
A61K 31/20
A61K 9/22
A61K 9/52
C07H 21/04

US Classification:

514 44, 514558, 536 245, 424468, 424494

Abstract:

Delayed release oral pharmaceutical formulations and methods for enhanced intestinal drug absorption. The formulation comprises a first population of carrier particles comprising a drug and a penetration enhancer which are released at a first location in the intestine, and a second population of carrier particles comprising a penetration enhancer and a delayed release coating or matrix. This penetration enhancer is released at a second location in the intestine downstream from the first location and enhances absorption of the drug when it reaches the second location.

US Patent:

8377897, Feb 19, 2013

Filed:

Sep 28, 2005

Appl. No.:

11/237063

Inventors:

Ching-Leou Teng - San Diego CA, US
Phillip Dan Cook - Lake San Marcos CA, US
Lloyd Tillman - Carlsbad CA, US
Gregory E. Hardee - Rancho Sante Fe CA, US
David J. Ecker - Encinitas CA, US
Muthiah Manoharan - Carlsbad CA, US

Assignee:

Isis Pharmaceuticals, Inc. - Carlsbad CA

International Classification:

A61K 31/70
C07H 21/02
C07H 21/04

US Classification:

514 44A, 536 245

Abstract:

The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e. g. , neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.

US Patent:

20030027780, Feb 6, 2003

Filed:

Feb 8, 2002

Appl. No.:

10/071822

Inventors:

Gregory Hardee - Rancho Santa Fe CA, US
Lloyd Tillman - Carlsbad CA, US
Maria Gonzalez-Ferreiro - Berlin, DE
Rahul Mehta - San Marcos CA, US
Ching-Leou Teng - San Diego CA, US

International Classification:

A61K048/00
A61K009/14

US Classification:

514/044000, 424/046000

Abstract:

The present invention is related to non-parenteral multiparticulate formulations capable of transporting therapeutic, prophylactic and diagnostic agents across mucosal membranes such as gastrointestinal, buccal, nasal, rectal and vaginal. Formulations comprise a plurality of carrier particles, an agent to be delivered across a mucosal membrane, and a penetration enhancer. The drug is adhered to the surface of the carrier particle or is impregnated within by electrostatic, covalent or mechanical forces.

US Patent:

20030083286, May 1, 2003

Filed:

Aug 22, 2001

Appl. No.:

09/935316

Inventors:

Ching-Leou Teng - San Diego CA, US
Lloyd Tillman - Carlsbad CA, US
Richard Geary - Carlsbad CA, US
Gregory Hardee - Rancho Santa Fe CA, US

International Classification:

A61K048/00
A61K038/17
A61K009/48
A61K009/28

US Classification:

514/044000, 424/463000, 514/012000, 424/474000

Abstract:

Compositions and methods for enhanced intestinal drug absorption. The formulation comprises a first population of carrier particles comprising a drug and a bioadhesive compound and a second population of carrier particles comprising a penetration enhancer. The bioadhesive extends the residence time of the drug and its absorptive potential across the portion of the intestinal mucosa made permeable by the penetration enhancer.

US Patent:

20030124196, Jul 3, 2003

Filed:

Aug 22, 2001

Appl. No.:

09/944493

Inventors:

Susan Weinbach - San Diego CA, US
Lloyd Tillman - Carlsbad CA, US
Richard Geary - Carlsbad CA, US
Gregory Hardee - Rancho Santa Fe CA, US

International Classification:

A61K048/00
A61K009/50

US Classification:

424/499000, 514/044000

Abstract:

Delayed release oral pharmaceutical formulations and methods for enhanced intestinal drug absorption. The formulation comprises a first population of carrier particles comprising a drug and a penetration enhancer which are released at a first location in the intestine, and a second population of carrier particles comprising a penetration enhancer and a delayed release coating or matrix. This penetration enhancer is released at a second location in the intestine downstream from the first location and enhances absorption of the drug when it reaches the second location.

US Patent:

20040229831, Nov 18, 2004

Filed:

Mar 4, 2004

Appl. No.:

10/793497

Inventors:

Ching-Leou Teng - San Diego CA, US
Phillip Cook - Fallbrook CA, US
Lloyd Tillman - Oceanside CA, US
Gregory Hardee - Rancho Sante Fe CA, US
David Ecker - Encinitas CA, US
Muthiah Manoharan - Weston MA, US

Assignee:

ISIS Pharmaceuticals, Inc. - Carlsbad CA

International Classification:

A61K048/00
A61L009/04

US Classification:

514/044000, 424/045000

Abstract:

The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.