Abstract: A method of inducing the viral resistance of plants comprises treating the plants, the soil or seeds with an effective amount of the compound of the formula I 1
Abstract: The use of an activator or ligand of a peroxisome proliferator-activated receptor, other than PPAR&ggr;, or pharmaceutically acceptable derivative of said activator or ligand, in the manufacture of a medicament for the treatment or prophylaxis of bone disease allows, for the first time, bone anabolism to enhance the deposition of bone in conditions which would benefit from increased bone deposition. The reverse, where there is inhibition and/or retardation of bone deposition is also facilitated.
Abstract: The present invention relates to a method of treating alcoholism or alcohol dependence in a mammal, including a human, by administering to the mammal a monoamine reuptake inhibitor in combination with an opioid antagonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a monoamine reuptake inhibitor and an opioid antagonist.
Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
Type:
Application
Filed:
September 17, 2002
Publication date:
July 3, 2003
Applicant:
Roche Bioscience, a division of Syntex (U.S.A.) LLC
Abstract: The invention provides substituted phenol compounds and pharmaceutical compositions containing substituted phenol compounds which are useful for inducing or maintaining anesthesia or sedation in a mammal. This invention also provides methods for inducing or maintaining anesthesia or sedation in a mammal using substituted phenol compounds.
Type:
Application
Filed:
September 26, 2002
Publication date:
June 26, 2003
Inventors:
Thomas E. Jenkins, Yu-Hua Ji, Huiwei Wu, Jennifer Bolton
Abstract: The invention relates to a pharmaceutical composition for relieving pelvic pain or infertility associated with uterine dysrhythmia. The composition includes a locally-administered anti-dysrhythmic treating agent and a bioadhesive extended-release carrier. The composition may be delivered in an extended release formulation that includes a bioadhesive, water-swellable, water-insoluble, cross-linked polycarboxylic acid polymer, such as polycarbophil. The treating agent may be a local anesthetic, such as lidocaine. The invention also relates to a method of treating or preventing pelvic pain, or treating or improving infertility, by inserting a mixture of an anti-dysrhythmic treating agent and a bioadhesive carrier into the vagina of the patient to be treated.
Type:
Application
Filed:
October 24, 2002
Publication date:
June 19, 2003
Inventors:
Howard L. Levine, William J. Bologna, Dominique De Ziegler
Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them.
Type:
Application
Filed:
June 12, 2002
Publication date:
June 19, 2003
Inventors:
Joachim Brendel, Thomas Bohme, Stefan Peukert, Heinz-Werner Kleemann
Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.
Type:
Grant
Filed:
October 3, 2000
Date of Patent:
June 10, 2003
Assignee:
Theravance, Inc.
Inventors:
Sabine M. Axt, Timothy J. Church, Witold N. Hruzewicz, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice
Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
Type:
Grant
Filed:
October 13, 2000
Date of Patent:
June 10, 2003
Assignee:
GD Searle & Company
Inventors:
Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is an
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
May 20, 2003
Assignee:
Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik
Produktionsaktieselskab)
Abstract: Microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, characterized in that
Abstract: The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
Type:
Application
Filed:
August 19, 2002
Publication date:
May 1, 2003
Inventors:
Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma
Abstract: Compounds for treating diseases by altering mitochondrial function that affects cellular processes, as well as to compositions and methods related thereto. The compounds have the structure
wherein R1, R2, R3 and A are as defined herein.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
April 22, 2003
Assignee:
MitoKor
Inventors:
Yazhong Pei, Walter H. Moos, Soumitra S. Ghosh
Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is
In another embodiment, the composition is
In yet another embodiment, the composition is
Additional alternative embodiments are R or R″ are therapeutic moieties.
Type:
Grant
Filed:
March 30, 2001
Date of Patent:
April 22, 2003
Inventors:
Nnochiri Nkem Ekwuribe, Jennifer A. Riggs-Sauthier
Abstract: Mucosal surface-coat-forming film dosage units containing a water-soluble hydrocolloid, an effective dose of an active agent and a mucosal adhesion enhancer; wherein the active agent is encapsulated within a polymer which is chemically or physically distinct from the hydocolloid; wherein the mucosal adhesion enhancer is a starch graft copolymer; wherein the film exhibits a dry tack value of less than 3.5 g, a wet tack of greater than 35 g, a gelation temperature that is greater than 70° C. for a 2% polymer solution, a dry film thickness of less than 20 mil, a water content of 0.5 to 10%, a tensile strength greater than 1500 psi, a modulus in the range of 35,000 to 300,000 psi, a % elongation of less than 20%, a tear probagation resistance of 0.001 to 1 N, and a dissolution time in the range of 1 to 600 seconds upon application to an oral mucosal surface.
Type:
Grant
Filed:
November 5, 1999
Date of Patent:
April 22, 2003
Assignee:
Lavipharm Laboratories Inc.
Inventors:
Li-Lan H. Chen, William R. Pfister, Donald W. Renn, Thitiwan Buranachokpaisan, James Osborne, Hock Seng Tan, Li Tao
Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.
Type:
Grant
Filed:
May 15, 2001
Date of Patent:
April 22, 2003
Assignee:
Eli Lilly and Company
Inventors:
Robert M. Scarborough, Mark Smyth, Ting Su, Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffry Bernard Franciskovich
Abstract: The present invention is directed to compositions that inhibit the nonenzymatic glycation of albumin, as well as methods of using compounds that inhibit albumin glycation for the treatment of glycation-related pathologies.
Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.
Abstract: This invention provides to a method for enhancement of systemic delivery of oxybutynin by administration via the nasal route, and methods of treatment comprising intranasal administration of oxybutynin. The present invention further provides pharmaceutical compositions comprising oxybutynin and/or pharmaceutically acceptable salts thereof.
Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.
Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. The present invention also provides a novel method for the synthesis of alpha-amino acids and derivatives thereof.
Abstract: Novel compounds of the general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.
Type:
Application
Filed:
July 30, 2002
Publication date:
March 20, 2003
Inventors:
Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.
Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.
Type:
Grant
Filed:
October 19, 1999
Date of Patent:
March 4, 2003
Assignees:
Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation, Ltd.
Inventors:
Sasson Cohen, Yaacov Herzig, Ruth Levy, Mitchell Shirvan, Jeff Sterling, Alex Veinberg, Moussa B. H. Youdim, John P. M. Finberg
Abstract: An objective of the present invention is to provide an agent that is clinically effective in the treatment or prevention of reperfusion injury. The agent for use in the treatment or prevention of reperfusion injury according to the present invention comprises an integrin &agr;v&bgr;3 antagonist, a pharmaceutically acceptable salt thereof, or a solvate thereof as active ingredient.
Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.
Type:
Application
Filed:
October 9, 2001
Publication date:
February 13, 2003
Inventors:
Klaus Urbahns, Michael Woltering, Susanne Nikolic, Josef Pernerstorfer, Berthold Hinzen, Elke Dittrich-Wengenroth, Hilmar Bischoff, Claudia Hirth-Dietrich, Klemens Lustig
Abstract: The invention provides a combination of of trimebutine [2-dimethylamino-2-phenylbutyl-3, 4, 5-trimethoxy-benzoate hydrogen maleate] or its corresponding stereoisomers with an opioid analgesic for the preparation of a medicament to prevent and/or treat pain or nociception.
Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.
Type:
Application
Filed:
July 31, 2001
Publication date:
February 6, 2003
Inventors:
Helmut Haning, Josef Pernerstorfer, Gunter Schmidt, Michael Woltering, Hilmar Bischoff, Verena Vohringer, Axel Kretschmer, Christiane Faeste
Abstract: Methods are disclosed for prophylactically and chronically preventing symptomatic depression, neuronal cell injury and cell death in systemic and neurological conditions, populations with cerebrovascular risk factors, and invasive vascular procedures, employing a glycine-site antagonist at the NMDA (N-methyl-D-aspartate) complex e.g., 2-phenyl-1,3-propanediol dicarbamate (felbamate).
Abstract: A novel fatty polypropoxylate ester which is an ester of an aliphatic or an aromatic monoacid formed by reacting the acid with a stoichiometric excess of a polypropoxylated fatty alcohol.
Type:
Application
Filed:
February 26, 2002
Publication date:
December 19, 2002
Inventors:
Ronald J. Smith, Maria K. Smith, Sayer B. Needelman, G. Frank DeMonico
Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I:
where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Type:
Grant
Filed:
August 28, 2000
Date of Patent:
December 17, 2002
Assignee:
Cytovia, Inc.
Inventors:
Yan Wang, Sui Xiong Cai, Eckard Weber, Gordon B. Mills, Douglas R. Green, Lufeng Guan
Abstract: Propanolamine derivatives represented by the following formula (I):
These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
Abstract: The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon administration to the eye. The present invention also discloses methods of topical ophthalmic administration of the compositions to the eye.
Type:
Grant
Filed:
November 23, 1999
Date of Patent:
November 26, 2002
Assignee:
Alcon Manufacturing, Ltd.
Inventors:
Bahram Asgharian, Gerald Cagle, Mandar V. Shah, Kerry L. Markwardt
Abstract: Compound of formula I
activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mammalian hosts, and processes for their preparation, are also described.
Type:
Grant
Filed:
May 31, 2001
Date of Patent:
November 12, 2002
Assignee:
Telik, Inc.
Inventors:
John Patterson, Sophia Park, Robert T. Lum, Wayne R. Spevak
Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.
Type:
Application
Filed:
January 25, 2002
Publication date:
November 7, 2002
Inventors:
Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
Type:
Application
Filed:
October 19, 2001
Publication date:
November 7, 2002
Inventors:
Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
Abstract: This invention provides to a method for enhancement of systemic delivery of oxybutynin by administration via the nasal route, and methods of treatment comprising intranasal administration of oxybutynin. The present invention further provides pharmaceutical compositions comprising oxybutynin and/or pharmaceutically acceptable salts thereof.
Type:
Application
Filed:
February 23, 2001
Publication date:
October 31, 2002
Inventors:
Amanda J. Sherratt, Abdulghani A. Houdi