Abstract: This invention relates to synthetic excitatory amino acid prodrugs of formula (I) wherein the residues R11, R12 and R13 are as defined in claim 1. The invention further relates to processes for the preparation of the compounds of formula (I), and to pharmaceutical compositions for the treatment of neurological and psychiatric disorders comprising said compounds.
Type:
Application
Filed:
April 30, 2004
Publication date:
December 9, 2004
Inventors:
Ana Belen Bueno Melendo, Alfonso De Dios, Carmen Dominguez-Fernandez, Mark Francis Herin, Luisa Maria Martin-Cabrejas, Jose Alfredo Martin, Maria Angeles Martinez-Grau, Steven Marc Massey, James Allen Monn, Carlos Montero Salgado, Concepcion Pedregal-Tercero, Matthew John Valli
Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9′ have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-IR dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.
Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.
Abstract: The present invention relates to a method for the regulation and control of biofilm layers. In particular, the present invention is concerned with methods for degrading or causing sloughing of biofilms from surfaces. The invention is also related to compositions suitable for use in carrying out these methods.
Type:
Application
Filed:
March 31, 2004
Publication date:
July 29, 2004
Inventors:
Steffan Kjelleberg, Michael Givskov, Mortan Hentzer
Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.
Type:
Grant
Filed:
October 7, 2002
Date of Patent:
July 13, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
Abstract: A new inhibitor of microtubule assembly (IC50 0.59 &mgr;M); with antineoplastic properties, denominated “dioxostatin”, has been synthesized and its effectiveness against human cancer and murine P388 lymphocytic leukemia cell lines demonstrated. Dioxostatin hs the following structure (I).
Abstract: Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4&bgr;-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4&bgr;-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
Type:
Application
Filed:
November 13, 2003
Publication date:
June 3, 2004
Inventors:
Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
Abstract: The present invention provides a stable, low free formaldehyde, synergistic antimicrobial composition, and a method of inhibiting the growth of or reducing microorganisms by applying the composition. Preferably, the constituents are dimethylol dimethylhydantoin, monomethylol dimethylhydantoin, dimethyl hydantoin, and dehydroacetic acid or its salts thereof. The composition has a free formaldehyde content of less than 0.2% and is beneficial for controlling microbiological and fungal contamination in personal care products, household products and industrial products and systems.
Abstract: The present invention provides a novel 4′-demethyl-4′-O-substituted-1-deoxypodophyllotoxin derivative, a geometric isomer thereof, a process for the preparation thereof, and an anticancer composition comprising the same.
Type:
Application
Filed:
April 28, 2003
Publication date:
March 4, 2004
Inventors:
Song-Bae Kim, Byung-Zun Ahn, Yong Kim, Young-Jae You
Abstract: This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administered
Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
Type:
Application
Filed:
January 22, 2003
Publication date:
January 8, 2004
Inventors:
Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
Abstract: New triterpenoid derivatives with various substituents at the C-17 position of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) were synthesized. Among them, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-2-methylimidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-4-methylimidazole show extremely high inhibitory activity (IC50=0.01-1 pM level) against production of nitric oxide induced by interferon-&ggr; in mouse macrophages. These compounds can be used in the prevention or treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, rheumatoid arthritis, and other inflammatory diseases. All the new triterpenoid derivatives are more potent than previously known CDDO.
Type:
Application
Filed:
May 12, 2003
Publication date:
January 1, 2004
Applicant:
The Trustees of Dartmouth College
Inventors:
Tadashi Honda, Yukiko Honda, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
Abstract:
The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Type:
Grant
Filed:
November 14, 2002
Date of Patent:
December 9, 2003
Assignees:
Aventis Pharma Deutschland GmbH, Genentech, Inc.
Inventors:
Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
Abstract: The present invention relates to the use of a dibenzocyclooctane lignan derivative of the following general formula (I) for treatment of neurodegenerative disorders:
wherein R1 is H or C1-4 lower alkyl; R2, R3, R4 and R5 are respectively H, OH, C1-4 lower alkyl, C1-4 lower alkoxy, or R2 and R3 or R4 and R5 are respectively combined to form the group of —OCH2O—. Pharmaceutical preparations containing the dibenzocyclooctane lignan derivative as the active ingredient also are disclosed.
Type:
Grant
Filed:
June 19, 2002
Date of Patent:
November 25, 2003
Assignee:
Elcom Bio Technology Co., Ltd.
Inventors:
Young-Joong Kim, Sang-Hyun Sung, Mi-Gyeong Lee, So-Ra Kim, Gyeong-A Gu, Won-Ju Jeong
Abstract: The present invention provides compositions and methods for treating an animal, preferably a human, suffering from or predisposed to a physical disorder by administering an effective amount of a composition comprising at least one RAR antagonist, preferably an RAR&agr; antagonist, and at least one RXR agonist. The combination of an RXR agonist, which has no therapeutic effects alone, with an RAR antagonist allows the use of lower doses of the RAR antagonist than were previously thought to be efficacious; this approach obviates many of the undesirable physiological side-effects of treatment with RAR antagonists.
Type:
Grant
Filed:
July 19, 2000
Date of Patent:
November 25, 2003
Assignees:
Bristol-Myers Squibb Company, Institut National de la Sante et de la Recherche
Medicale, Centre National de la Recherche Scientifique, Universite Louis Pasteur
Inventors:
Pierre Chambon, Hinrich Gronemeyer, Peter R. Reczek, Jacek Ostrowski
Abstract: The present invention is directed to a sensate composition including at least one cooling sensate, warming sensate and tingling sensate. The tingling sensate is at least one of Jambu Oleoresin and Spilanthol. The present invention is further directed to a method of using the sensate composition in a food, pharmaceutical or personal care product.
Type:
Application
Filed:
June 17, 2003
Publication date:
November 20, 2003
Applicant:
Takasago International Corporation
Inventors:
Tetsuo Nakatsu, Peter J. Mazeiko, Andrew T. Lupo, Carter B. Green, Charles H. Manley, David J. Spence, Hideaki Ohta
Abstract: This invention relates to a method of treating human immunodeficiency virus (HIV) infection in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cytotoxic agent and (ii) at least one non-nucleoside reverse transcriptase HIV inhibitor (NNRTI). This invention also relates to a method of treating chronic viral infections comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cytotoxic agent and (ii) at least one antiviral agent.
Abstract: N-Substituted glucamine compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agent selected from among nucleosides, nucleotides, immunomodulators, immunostimulants or various combinations of such other agents.
Type:
Application
Filed:
December 17, 2002
Publication date:
October 16, 2003
Applicant:
Pharmacia Corporation
Inventors:
Richard A. Mueller, Martin L. Bryant, Richard A. Partis
Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof: 1
Type:
Application
Filed:
December 6, 2002
Publication date:
September 18, 2003
Inventors:
Michael A. Walker, Jacques Banville, Roger Remillard, Serge Plamondon
Abstract: A method of treating ocular hypotension, hypertension, hemorrhage, myocardial ischemia, angina pectoris, coronary contraction, cerebrovascular contraction after subarachnoidal hemorrhage, cerebral hemorrhage and asthma which comprises administering to a mammal suffering therefrom a therapeutically effective amount of a thromboxane ligand which is a compound formula I, 1
Type:
Application
Filed:
August 5, 2002
Publication date:
June 12, 2003
Applicant:
ALLERGAN SALES, INC.
Inventors:
Robert M. Burk, Achim H-P Krauss, David F. Woodward
Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
Type:
Grant
Filed:
June 21, 2002
Date of Patent:
May 20, 2003
Assignee:
The University of North Carolina at Chapel Hill
Inventors:
Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
Abstract: Disclosed is a method for promoting bile secretion, which comprises administering and effective amount of a certain 15-keto-prostaglandin compound to a subject having a disease or condition associated with bile secretion deficient. Also disclosed is a method for treatment of a liver to be transplanted in a liver transplantation process, which comprises contacting the liver with a liquid composition comprising the 15-keto-prostaglandin compound as above.
Abstract: The invention relates to pharmaceutical preparations containing a dibenzocyclooctane lignan derivative for prevention and treatment of neurodegenerative disease.
Type:
Application
Filed:
June 19, 2002
Publication date:
March 13, 2003
Inventors:
Young-Joong Kim, Sang-Hyun Sung, Mi-Gyeong Lee, So-Ra Kim, Gyeong-A Gu, Won-Ju Jeong
Abstract: An absorbent article having a bodyside liner includes a hydrophilic lotion formulation on the outer bodyfacing surface thereof. The hydrophilic lotion formulation comprises from about 10 to about 90 weight percent of a hydrophilic solvent, from about 5 to about 90 weight percent of a high molecular weight polyethylene glycol, and from about 0 to about 60 weight percent of a fatty alcohol. The hydrophilic lotion formulation has a reduced adverse effect on the absorbent and liquid uptake properties of the liner and the absorbent body when compared to conventional lipophilic or hydrophobic lotion formulations. The hydrophilic lotion formulation acts as a lubricant to reduce the abrasion of the skin caused by the liner and also transfers to the skin to provide improved skin health.
Type:
Grant
Filed:
April 23, 1999
Date of Patent:
February 4, 2003
Assignee:
Kimberly-Clark Worldwide, Inc.
Inventors:
Duane Gerard Krzysik, David Charles Musil, Frank Andrew Rosch, III, Gordon Allen Shaw, Diane Michele Underhill, Jeffrey Michael Hockersmith
Abstract: The preparation and use of a protected organic aldehyde is described wherein bioavailability of the orally administered therapeutic aldehyde is improved. The protected aldehyde is prepared by reacting the aldehyde with a protecting group, for example, condensing the aldehyde chemically with a thiazolidine-4-carboxylic acid. The improved bioavailability of such orally administered drugs increases the feasibility of delivering sufficient amounts of vanillin or other therapeutic organic aldehydes in vivo to prevent sickling in sickle cell anemia. Combination therapy is also described wherein a protected organic aldehyde is administered to a subject in treatment of sickle cell anemia in conjunction with one or more other drugs, such as pain killers, used in treatment of the symptoms of sickle cell anemia or sickle cell disease.
Type:
Application
Filed:
March 12, 2002
Publication date:
January 30, 2003
Applicant:
Medinox, Inc.
Inventors:
Ching-San Lai, Vassil P. Vassilev, Long-Shiuh Chen
Abstract: A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.
Type:
Grant
Filed:
June 21, 2001
Date of Patent:
January 28, 2003
Assignee:
R.P. Scherer Technologies, Inc.
Inventors:
Ronald S. Vladyka, Jr., David F. Erkoboni, Pamela R. Stergios
Abstract: The present invention provides a citral acetal capable of sustaining a lemon aroma unique to citral and a perfume composition comprising the citral acetal, as well as an LDH inhibitor and a deodorant, cosmetics and a skin agent for external application, comprising the LDH inhibitor. The citral acetal of the present invention is represented by formula (1):
wherein the wavy line represents a cis and/or trans form, and R represents a C1, to C9, linear or branched alkyl group.
Abstract: Anticonvulsant compounds of the general formula I:
where X, R1, R2, R3, R4, R5, and R6 are as herein defined; are useful in treating acute ischemia-induced neurodegeneration, such as occurs during and after stroke, head trauma, spinal injury, non-fatal cardiac arrest, or major surgical procedures. Furthermore, pharmaceutical compositions containing a compound of formula I as well as methods for their use are disclosed.
Type:
Grant
Filed:
July 20, 2000
Date of Patent:
December 17, 2002
Assignee:
Ortho McNeil-Pharmaceutical, Inc.
Inventors:
Michael J. Costanzo, Bruce E. Maryanoff, Richard P. Shank
Abstract: Compositions having broad effectiveness against bacterial and fungi, which comprise (a) an iodopropynylbutyl compound and (b) one or more formaldehyde donor compounds, the formaldehyde donor compounds being N-formals, O-formals and/or a combination thereof. The compositions are also stable and effective in the form of liquid concentrates. The present invention also relates to the use of such compositions in industrial products and to industrial products which comprise these compositions.
Type:
Grant
Filed:
May 22, 2001
Date of Patent:
October 22, 2002
Assignee:
Air Liquide Sante (International)
Inventors:
Wolfgang Beilfuss, Wolfgang Siegert, Klaus Weber
Abstract: Provided are, among other things, lipid-lowering or glucose-lowering methods and compounds, particularly lipid-lowering or glucose-lowering compounds, with an A-B ring structure as follows: 1
Type:
Application
Filed:
October 23, 2001
Publication date:
October 17, 2002
Inventors:
Dilip R. Wagle, Sheng Ding Fang, Ihor Terleckyj, John Resek, John J. Egan
Abstract: The present invention relates to a method for opening potassium channels in mammalian cells by administering to a mammal effective amounts of potassium channel-opening keto compounds as described herein.
Type:
Application
Filed:
March 4, 2002
Publication date:
September 19, 2002
Inventors:
George N. Lambrou, Anna Ottlecz, Christine Percicot, Michael Wiederholt
Abstract: A new family of compounds, particularly aryl-indane compounds, is disclosed. The compounds may be used as inhibitors of P-glycoprotein-mediated transport. Use of the compounds to enhance bioavailability and to modulate multi-drug resistance to chemotherapeutic agents is disclosed.
Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.
Type:
Grant
Filed:
July 14, 2000
Date of Patent:
July 23, 2002
Assignee:
Les Laboratoires Servier
Inventors:
Michel Langlois, Monique Mathe-Allainmat, Carole Jellimann, Jean Andrieux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
Abstract: An anti-inflammatory, either a NSAID or glucocorticoid steroid in the form of an ointment, cream, lotion, gel, powder, tablet, paste, film, tape or adhesive bandage, provided with appropriate vehicle to allow specific adherence to specific gingival areas, for topical treatment of inflammation. This composition and the method of using same is used to prevent or relieve migraine, tension-type headache, post-traumatic headache, facial pain and cervical muscle spasm.
Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I:
TI—L—TII (I)
wherein:
TI is a topoisomerase I inhibitor such as a camptothecin group;
TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and
L is a linking group.
The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
July 16, 2002
Assignees:
The University of North Carolina at Chapel Hill, Yale University
Inventors:
Kuo-Hsiung Lee, Yung-Chi Cheng, Xin Guo, Kenneth F. Bastow, Hui-Kang Wang
Abstract: A method for treating a fungal infection is disclosed. The method includes contacting a fungus with a substituted aurone derivative.
Type:
Application
Filed:
September 20, 2001
Publication date:
July 4, 2002
Inventors:
Wai-Lam Alex Chu, Flemming R. Jensen, Thomas B. Jensen, James B. McAlpine, Brigitte Sokilde, Alexandra M. SantAna-Sorensen, Sunil Ratnayake, Jack B. Jiang, Catharine Noble, Angela M. Stafford
Abstract: The present invention relates to a new pesticide which is based on a photosensitizer or combination of photosensitizers of the tetrapyrrole and/or tetraazapyrrole series which may comprise a biological and/or chemical attractant for pests and to a method of controlling pests using the new pesticide.
Abstract: The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide selected from the compounds having a fungicidal activity against plant diseases, and to a method for using the same:
wherein R1 is hydrogen, alkyl or cycloalkyl and R2 is CO—Y—R3, wherein Y is O, S, NR4 or the like and R3 is hydrogen, alkyl, phenyl, 5- or 6-membered heterocycle or the like.
Abstract: A method for blocking the attachment of leukocytes to endothelial cells/lining of the blood vessels using a plant derived protoberberine alkaloid, berberine or its pharmaceutically acceptable salts. This prevents tissue damage to the surrounding tissue. The method also can be used to prevent and/or treat clinical manifestations that involve endothelial cell-leukocyte attachment, for example septic shock, arthritis, psoriasis, multiple sclerosis, allergic asthma, metastatic melanoma and graft rejection.
Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.
Abstract: A method of treating a disease condition intermediated by a center of stimuli which regulates autonomic activity of an internal organ involves administration of an effective amount of podophyllotoxin.
Abstract: Compositions having broad effectiveness against bacteria and fungi, which comprise (a) an iodopropynylbutyl compound and (b) one or more formaldehyde donor compounds, the formaldehyde donor compounds being N-formals, O-formals and/or a combination thereof. The compositions are also stable and effective in the form of liquid concentrates. The present invention also relates to the use of such compositions in industrial products and to industrial products which comprise these compositions.
Type:
Grant
Filed:
November 23, 1999
Date of Patent:
March 12, 2002
Assignee:
Air Liquide Sante (International)
Inventors:
Wolfgang Beilfuss, Wolfgang Siegert, Klaus Weber
Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:
Type:
Grant
Filed:
June 2, 1999
Date of Patent:
March 5, 2002
Assignee:
Alcon Laboratories, Inc.
Inventors:
Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko