Abstract: A system for carrying out fast perfusion for the patch clamp techniques useful in studying the effect of compounds on ion transfer channels in biological tissue is disclosed. The invention additionally includes microperfusion chamber assemblies capable of utilizing small amounts of material to be tested and small amounts of liquid carrier, thereby enabling multiple tests to be completed in a short period of time. The invention more broadly relates to an electrophysiology drug handling and application set up for screening chemicals such as drugs while providing high throughput and low volumes of solutions and samples.
Abstract: The invention provides a novel assay system for measuring the amount of active PAI-1 in a sample with sensitivity, and correlation to an active PAI-1 amount. The assay determines the amount of active PAI-1 in a sample by utilizing a novel standard curve. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims. 37 CFR 1.72(b).
Abstract: The present invention provides an anthelmintic composition including an avermectin or milbemycin, together with triclabendazole, and a predetermined quantity of rheology modifier, such as Laponite or xanthan gum, sufficient to render the anthelmintic composition suitable as an oral drench.
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
November 1, 2005
Assignee:
Wyeth
Inventors:
Michael S. Malamas, Iwan Gunawan, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
Abstract: Novel human Kv4.3 polypeptides, polynucleotides which encode these polypeptides, and methods for producing these polypeptides are provided. Diagnostic, therapeutic, and screening methods employing the polynucleotides and polypeptides of the present invention are also provided.
Type:
Grant
Filed:
January 31, 2002
Date of Patent:
November 1, 2005
Assignee:
Wyeth
Inventors:
Mark Ian Cockett, Daniel Wayne Dilks, Huai-Ping Chang Ling, Patricia Tyson Sokol
Abstract: The present invention provides a new process and intermediates for the production of antiviral compound 4?,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2?-disulfonic acid and its pharmaceutically acceptable salts.
Type:
Grant
Filed:
September 22, 2004
Date of Patent:
November 1, 2005
Assignee:
Wyeth
Inventors:
Silvio Iera, Christopher A. Demerson, Jacqueline F. Lunetta, Maria Papamichelakis, Michael F. MacEwan, Wayne G. McMahon, John R. Potoski, Arthur G. Mohan, Antonia Nikitenko
Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
May 17, 2004
Publication date:
October 27, 2005
Applicant:
Wyeth
Inventors:
Michael Malamas, Robert McDevitt, Iwan Gunawan, Eric Manas, Michael Collini, Heather Harris, James Keith, Leo Albert, C. Lyttle
Abstract: A method for rapamycin-specific labeling using rapI, rapM and/or rapQ enzymes is described. Also are methods for generating crude enzyme extracts useful in the method of the invention. Uses of the specifically labeled rapamycin as diagnostic tools are provided.
Abstract: Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl.
Abstract: A multifunctional molecular complex for the transfer of a nucleic acid composition to a target cell is provided. The complex is comprised of A) said nucleic acid composition and B) a transfer moiety comprising 1) one or more cationic polyamines bound to said nucleic acid compositions, 2) one or more endosome membrane disrupting components attached to at least one nitrogen of the polyamine and 3) one or more receptor specific binding components.
Abstract: A therapeutic composition for inhibiting the function of a target polynucleotide sequence in a mammalian cell includes an agent that provides to a mammalian cell an at least partially double-stranded RNA molecule comprising a polynucleotide sequence of at least about 200 nucleotides in length, said polynucleotide sequence being substantially homologous to a target polynucleotide sequence. This RNA molecule desirably does not produce a functional protein. The agents useful in the composition can be RNA molecules made by enzymatic synthetic methods or chemical synthetic methods in vitro; or made in recombinant cultures of microorganisms and isolated therefrom, or alternatively, can be capable of generating the desired RNA molecule in vivo after delivery to the mammalian cell.
Abstract: The present invention relates to a topical formulation for the treatment of a dermatological condition which comprises a macrocyclic lactone antibiotic, immunosuppresive macrolide or a biologically active analogue, derivative or pro-drug thereof; characterized in that it further comprises a permeation modulator and the permeation modulator and the macrocyclic lactone or macrolide or the biologically active analogue, derivative or pro-drug thereof are present in relative amounts such that when a therapeutic amount is applied to the skin a minimal systemic effect is produced. The immunosuppressive macrolide may be sirolimus.
Abstract: Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with dicarboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.
Abstract: The present invention is directed to secondary amino- and cycloamino-cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Application
Filed:
October 12, 2004
Publication date:
October 20, 2005
Applicant:
Wyeth
Inventors:
Paige Mahaney, Michael Webb, Lori Gavrin, Eugene Trybulski
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure where R1 R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification.
Abstract: A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acetylation of 42-hydroxy of rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic solvent.
Abstract: Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
Abstract: This invention is directed to Acyl Carrier Protein Synthase (ACPS) crystals and crystals of Acyl Carrier Protein Synthase-Coenzyme A (ACPS-CoA) complex, and to the use of these crystals to determine the three dimensional structure of ACPS. This invention is further directed to the use of rational drug design methods to identify agents that may interact with active sites of ACPS and ACPS-CoA complex, and to the testing of these agents to identify agents that may inhibit ACPS and/or ACPS-CoA complex activity.
Type:
Grant
Filed:
January 25, 2001
Date of Patent:
October 18, 2005
Assignees:
Wyeth, Millennium Pharmaceuticals, Inc.
Inventors:
Kevin Delos Parris, William Stuart Somers, Amy Szepui Tam, Laura Long Lin, Mark Lloyd Stahl