Abstract: The invention provides polyamides suitable for modulating cellular or viral gene expression by binding to an identified target DNA sequence adjacent to the binding site of a minor groove transcription factor protein. The polyamides of the present invention are useful for the treatment of a human infected with a virus such as HIV-1. The polyamides of the present invention are also useful for the treatment of conditions, such as cancers, that result from the expression or over-expression of cellular genes, particularly oncogenes.
Type:
Grant
Filed:
April 25, 2000
Date of Patent:
December 9, 2003
Assignees:
California Institute of Technology, The Scripps Research Institute
Inventors:
Joel M. Gottesfeld, Peter B. Dervan, Donald E. Mosier, Eldon E. Baird
Abstract: A controlled release composition for a biologically active material, which composition is liquid or liquid crystalline and comprises at least one medium or long-chain fatty acid ester of diglycerol as a carrier for said biologically active material, said biologically active material being dissolved or dispersed in said carrier. Said composition is especially useful as a medical composition.
Type:
Grant
Filed:
July 8, 1999
Date of Patent:
December 9, 2003
Assignee:
GS Development AB
Inventors:
Kåre Larsson, Helena Ljusberg-Wahren, Niels Krog
Abstract: Provided are the compound (E)-4-carboxystyryl-4-chlorobenzyl sulfone, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 27, 2002
Date of Patent:
December 2, 2003
Assignee:
Temple University - Of the Commonwealth System of Higher
Education
Inventors:
Stephen C. Cosenza, M. V. Ramana Reddy, E. Premkumar Reddy
Abstract: The treatment of an estrogen sensitive condition by the administration of a selective estrogen receptor modulator is improved by additionally administering a progestationally active compound to the recipient. The additional agent can express both progestational and androgenic activity or an androgenically active material can be employed, if desired. Additionally, clomiphene in an array of isomeric ratios (EN:ZU) can be used alone for prevention of osteoporosis, maintenance of a healthful blood lipid profile, and prevention of breast tumors, or to sustain amenorrhea.
Abstract: This invention relates to two methods treating such disease as AIDS. The first method includes administering the Trigger Factor such as TNF, which is defined as substance stimulating infected cells to increase HIV replication and hence subjecting the infected cells to death or the programmed death (apoptosis), further administering new-infection suppressor such as AZT and preferably inducer to migrate infected cells (lymphocytes) to the blood system from the lymphatic system, and then continuing extinction of the replicated HIVs by extracorporeal blood processing until all the infected cells die.
The second method includes administering electroconductive and/or magnetic microparticles on the surface whereon of which such infectiously adhesive substance to HIVs and infected cells as CD4 is coated, and killing HIVs/infected cells adhered to the microparticles by heating the microparticles with electromagnetic field (wave) applied externally to the patient.
Abstract: Disclosed and claimed are methods for oral contraception, or a hormone replacement therapy, or for treating breast cancer, in a patient in need thereof involving administering to the patient, at a dosage of no greater than 200 &mgr;g/day per 70 kg subject, a compound having Formula (I):
wherein X in combination with K form a steroidal ring and R5 is a sulphamate group that has of the formula:
wherein each of R1 and R2 is H.
Type:
Grant
Filed:
January 5, 2001
Date of Patent:
November 25, 2003
Assignees:
Sterix Limited, Schering AG
Inventors:
Barry Victor Lloyd Potter, Michael John Reed, Walter Elger, Gudrun Roddersen, Heinrich-Thomas Proske
Abstract: A method of superficial epidermal peeling in a human comprising massaging unto the horny layer of the epidermis (stratum corneum), a composition comprising vegetable-derived elements characterized by sufficient length and rigidity to enter into the horny layer, improving the constitution of the skin tint, smoothing the skin surface, removing wrinkles, blemishes, localized hyperkeratoses and reducing skin pore size by regulating seborrhea.
Type:
Grant
Filed:
July 30, 2001
Date of Patent:
November 25, 2003
Inventors:
Veronique Simon, Michel Dubourdeaux, Daniel Jean
Abstract: As a novel photochemotherapeutical method for the treatment or prevention of an auto-immune disease, there is provided a method for treating an auto-immune disease, which comprises administering to the patient mono-L-aspartyl chlorin e6 or mono-L-glutamyl chlorin e6 or a pharmacologically acceptable salt thereof, followed by subjecting the blood vessel blood of the patient containing the administered compound to exposure with an ultraviolet ray or a laser light, thereby to excite said compound photochemically. This method is effective to decrease the level of auto-antibody in the blood of the patient and is also of high safety.
Abstract: This invention relates to a dry granulation capsule formulation of the HIV protease inhibitor, indinavir sulfate, which is useful in the treatment of AIDS, ARC or HIV infection. Processes for making the oral formulation are also disclosed.
Type:
Grant
Filed:
March 4, 1998
Date of Patent:
November 11, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Chung Y. Lui, Drazen Ostovic, Ashok V. Katdare, Christine Stelmach
Abstract: A stable composition including a water-sensitive pharmacologically active agent, such as an enzyme, an antibiotic or a vitamin, a hydrophilic non-polar primary solvent, an optional hydrophilic non-polar secondary solvent and optional pharmaceutical or cosmetic adjuvants to enhance appearance for topical use. Where the water-sensitive or water-degradable component is L-Ascorbic acid and the principal solvent is N-methyl-2-pyrrolidone (“NMP”) the composition is stable for many months at a concentration of L-Ascorbic acid of up to about 40 % w/v. This composition using NMP as a solvent and enhancer of skin penetration together with appropriate adjuvants is useful for preparing dermatological topical dosage for cosmetic and therapeutic purposes.
Abstract: Delivery of metal particles to living tissue, then applying external energy that interacts with the metal particles, is found to selectively increase the energy deposition and interaction surrounding the metal particles. The method is useful to improve treatment of various conditions, since targeted cells may be selectively altered or killed. Metal particles are also loaded into cells or membrane vesicles by placing metal seed particles into the cells or vesicles, then chemically depositing additional metal on the metal seed particles. The metal particles are useful to improve imaging and therapies by their interaction with externally applied energy.
Abstract: Isosorbide mononitrate formulations and methods of treatment are disclosed. The formulations and treatments provide for subtherapeutic levels of the mononitrate in a washout period to prevent nitrate tolerance.
Type:
Grant
Filed:
February 7, 1997
Date of Patent:
November 4, 2003
Assignee:
Athpharma Limited
Inventors:
Edward James Geoghegan, Seamus Mulligan, Mary Margaret Foynes
Abstract: An estrogen-free contraceptive is provided which does not have the bleeding-related drawbacks of conventional progestogen-only pills. Thus the invention is a contraceptive kit comprising a combined means for the simultaneous daily administration of a progestogen as the sole contraceptively effective ingredient and an anti-progestogen. Said combined means preferably is in the form of tablets having a normal contraceptive dose of the progestogen and low dose of the anti-progestogen.
Abstract: The present invention discloses an antimicrobial preservative composition and methods of using the same. The antimicrobial preservative composition includes a glycerol fatty acid ester, a binary mixture of fatty acids including a first fatty acid antimicrobial agent selected from fatty acids having about six to about eighteen carbon atoms and a second fatty acid antimicrobial agent selected from fatty acids having about six to about eighteen carbon atoms where the second fatty acid is different from the first fatty acid and a food-grade carrier. Also disclosed is an antimicrobial preservative composition which includes a safe and effective amount of a ethoxylated or propoxylated glycerol fatty acid ester, a binary mixture of fatty acids including a first fatty acid antimicrobial agent selected from this C6 to C18 fatty acids and a second fatty acid antimicrobial agent selected from C6 to C18 fatty acids where the second fatty acid is different from the first fatty acid and a food-grade carrier.
Abstract: The use of an organosiloxane bearing at least one ultraviolet-absorbing group in, and for the preparation of, a cosmetic or dermatological composition as an agent for protecting the color of artificially colored keratin fibres against the effects of UV radiation, in particular solar radiation.
Type:
Grant
Filed:
October 30, 2000
Date of Patent:
October 21, 2003
Assignee:
L'Oreal S.A.
Inventors:
Hervé Richard, Alain Lagrange, Claude Dubief, Damarys Braida-Valerio
Abstract: Processes for the preparation, prepared solutions, and the use of radium-223 for the treatment of calcified tumors, bone tumors, treatment of bones, bone surfaces and soft tissues is described.
Type:
Grant
Filed:
January 3, 2000
Date of Patent:
October 21, 2003
Assignee:
Anticancer Therapeutic Inventions AS
Inventors:
Roy H. Larsen, Gjermund Henriksen, Øyvind S. Bruland
Abstract: The invention provides methods for enhancing cognitive activity and stimulating memory capacity, comprising the step of administering an effective amount of a compound with GABAC receptor antagonist activity to an animal in need of such treatment. Preferably the compound has selective GABAc receptor antagonist activity, and more preferably comprises a phosphinic acid group. The invention also provides novel compounds and compositions. The methods of the invention are useful in the treatment of dementias and conditions involving cognitive deficit, or memory impairment.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
October 14, 2003
Assignees:
The University of Sydney, Polychip Pharmaceuticals Pty. Ltd.
Inventors:
Graham A. R. Johnston, Peter M. Burden, Kenneth Noel Mewett, Mary Chebib
Abstract: The invention includes a method of treating neurogenic urinary dysfunction that comprises contacting urinary bladder mucosa of a patient afflicted with neurogenic urinary dysfunction with an effective dose of a homovanilloid compound, in particular a compound selected from the group RTX, TYX, 20-homovanillyl-mezerein or 20-homovanillyl-12-deoxyphorbol-13-phenylacetate. The invention includes treatment of urge incontinence due to detrusor hyperreflexia (DH). The invention also includes treatment of sensory hypersensitivity of the bladder resulting from prostate hypertrophy or interstial cystitis, as well as other neurogenic conditions resulting in increased micturition frequency or decreased bladder capacity, with or without frank incontinence.
Abstract: Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine from decomposing through the proposed pathway. The prodrug will be hydrolyzed in the stomach or the gut into thyroxine and the biologically inert dimethylphosphinic acid. Related products may be stabilized with the same or similar protecting groups.