Abstract: This invention provides novel arylindenopyridines of the formula: , and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing PDE activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
Type:
Grant
Filed:
April 16, 2002
Date of Patent:
October 25, 2005
Assignee:
Ortho-McNeil Pharmaceutical, Inc
Inventors:
Geoffrey R. Heintzelman, Kristin M. Averill, John H. Dodd
Abstract: The present invention relates to compounds of the formula (I): which are produced by the plant Garcinia punctata, chemical derivatives derived therefrom, a process for their preparation, and their use as pharmaceuticals, in particular for the treatment and/or prophylaxis of bacterial infectious diseases.
Type:
Grant
Filed:
July 31, 2003
Date of Patent:
October 18, 2005
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Matthias Schiell, Michael Kurz, Sabine Haag-Richter
Abstract: This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
Type:
Grant
Filed:
May 15, 2003
Date of Patent:
October 4, 2005
Assignee:
Genelabs Technologies, Inc.
Inventors:
Christoher Don Roberts, Jesse Daniel Keicher, Mikail Hakan Gezginci, Mark Douglas Velligan
Abstract: The invention provides peptide synthons having protected functional groups for attachment of desired moieties (e.g. functional molecules or probes). Also provided are peptide conjugates prepared from such synthons, and synthon and conjugate preparation methods including procedures for identifying the optimum probe attachment site. Biosensors are provided having environmentally sensitive dyes that can locate specific biomolecules within living cells and detect chemical and physiological changes in those biomolecules as the living cell is moving, metabolizing and reacting to its environment. Methods are included for detecting GTP activation of a Rho GTPase protein using polypeptide biosensors. When the biosensor binds GTP-activated Rho GTPase protein, the environmentally sensitive dye emits a signal of a different lifetime, intensity or wavelength than when not bound.
Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
Type:
Grant
Filed:
August 13, 2003
Date of Patent:
September 27, 2005
Assignee:
Pfizer Inc.
Inventors:
Peter Bertinato, Brian S. Bronk, Alan E. Blize, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
Abstract: Triazole compounds having a 2,6-disubstituted-phenyl group in the 3-position, 5?-arylthien-3-yl group in the 5-position and an alkyl group in the 1-position are effective in controlling lepidoptera, coleoptera, mites and other sucking pests.
Type:
Grant
Filed:
September 17, 2003
Date of Patent:
September 27, 2005
Assignee:
Dow AgroSciences LLC
Inventors:
Vidyadhar Babu Hegde, Scott Jerome Bis, Maurice Chee Hoong Yap, Denise Marie Perreault, Francis Eugene Tisdell, Leonard Paul Dintenfass, James Edwin Dripps, James Michael Gifford, Katherine Anne Guenthenspberger, Laura Lee Karr, Joe Raymond Schoonover
Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
Type:
Grant
Filed:
September 26, 2003
Date of Patent:
September 27, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Joseph William Epstein, Semiramis Ayral-Kaloustian
Abstract: Disclosed is a process for the preparation of a peptoid substituted azole compound comprising reacting an amino functionalized azole compound with a resin bound peptoid oligomer bearing a terminal halogen substituent followed by cleavage of the resultant product from the resin surface using a fluorinated organic acid in an inert solvent.
Type:
Grant
Filed:
December 12, 2001
Date of Patent:
September 20, 2005
Assignee:
Eastman Kodak Company
Inventors:
Donald R. Diehl, Robert J. Niger, Hans F. Schmitthenner, William J. Sonnefeld, Richard P. Dunlap
Abstract: The invention relates to a desorption process for epothilones, especially epothilone A and/or epothilone B, from resins and new production, work-up or purification processes or manufacturing methods for epothilones comprising said desorption process, as well as the use of certain solvents for the desorption of epothilones from resins.
Abstract: Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.
Type:
Grant
Filed:
December 23, 2003
Date of Patent:
September 6, 2005
Assignee:
UCB Farchim SA
Inventors:
Gregory N. Beatch, Lewis S. L. Choi, Clive P. Page, Bertrand M. C. Plouvier, Yuzhong Liu
Abstract: Hydroxy substituted fused naphthyl-azoles and fused indeno-azoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
Abstract: A novel class of benz[f]indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
Type:
Grant
Filed:
December 6, 2001
Date of Patent:
August 16, 2005
Assignee:
Eli Lilly and Company
Inventors:
Douglas Wade Beight, Michael Dean Kinnick, Ho-Shen Lin, John Michael Morin, Michael Enrico Richett, Daniel Jon Sall, Jason Scott Sawyer, Edward C R Smith
Abstract: The invention relates to novel biaromatic compounds which correspond to the general formula (I) below: and also to the method for preparing them and their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or alternatively in cosmetic compositions.
Abstract: The invention relates to a process for reducing the monomeric aziridine content in a polyaziridine forming reaction mixture by adding to the polyaziridine forming reaction mixture an excess of an organic carbonate scavenger wherein the excess is based on the equivalent ratio of scavenger to monomeric aziridine, and to a product obtained by this process and to a coating composition containing the product obtained by the process.
Type:
Grant
Filed:
October 31, 2002
Date of Patent:
August 9, 2005
Assignee:
Bayer MaterialScience LLC
Inventors:
Lanny D. Venham, Douglas A. Wicks, Karsten Danielmeier, Joseph P. Mandara
Abstract: The present invention provides substituted triazole diamine derivatives as selective kinase or dual-kinase inhibitors and a method for treating or ameliorating a selective kinase or dual-kinase mediated disorder.
Type:
Grant
Filed:
December 21, 2001
Date of Patent:
August 2, 2005
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Ronghui Lin, Peter J. Connolly, Steven K. Wetter, Shenlin Huang, Stuart L. Emanuel, Robert H. Gruninger, Steven A. Middleton
Abstract: The present invention relates to compounds of the formula Orosco wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.
Abstract: A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
Abstract: The present invention provides cystine derivatives, which may be in a free form, a salt form, a solvate form. The cystine derivatives of the present invention may be used to suppress activation of inflammatory factors. Accordingly, the present invention provides: compositions containing the cystine derivatives; a method for suppressing the activation of inflammatory factors by administering the composition; a method for preventing, ameliorating and/or therapeutically treating diseases, skin injuries or disorders involved in the activation of inflammatory factors by administering the composition; a method for preventing, delaying, ameliorating and/or therapeutically treating skin change via aging or aesthetically unfavorable skin change as induced or promoted by inflammatory factors by administering the composition; and pharmaceutical agents containing the cystine derivatives.
Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
Type:
Grant
Filed:
October 28, 2003
Date of Patent:
June 28, 2005
Assignee:
UCB, S.A.
Inventors:
Edmond Differding, Benoît Kenda, Bénédicte Lallemand, Alain Matagne, Philippe Michel, Patrick Pasau, Patrice Talaga