Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
Type:
Grant
Filed:
October 31, 2003
Date of Patent:
December 12, 2006
Assignees:
North Carolina State University, ZettaCore, Inc.
Inventors:
Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
Abstract: Perfluoropolyether benzotriazole compounds and compositions containing perfluoropolyether benzotriazole compounds are provided. The perfluoropolyether benzotriazole compounds can be attached to a substrate having a metal or metal oxide-containing surface to provide at least one of the following characteristics: anti-soiling, anti-staining, ease of cleaning, repellency, hydrophobicity, or oleophobicity.
Type:
Grant
Filed:
January 30, 2004
Date of Patent:
December 12, 2006
Assignee:
3M Innovative Properties Company
Inventors:
Richard M. Flynn, Naiyong Jing, Mark J. Pellerite
Abstract: Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals The invention relates to cycloalkyl derivatives having bioisosteric carboxylic acid groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.
Type:
Grant
Filed:
February 27, 2004
Date of Patent:
December 12, 2006
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Dirk Gretzke, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
December 18, 2003
Date of Patent:
December 5, 2006
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, Jared D Kuemmerle, Hong Zhang, William E Kemnitzer
Abstract: This invention relates to agents and conjugates that can be used to detect and isolate target components from complex mixtures such as proteins and protein fragments from biological samples from in vivo and in vitro sources. Agents comprise a detectable group bound to a photoreactive group. Conjugates comprise agents coupled to substrates by covalent bounds which can be selectively cleaved with the administration of electromagnetic radiation. Targets substances labeled with detectable molecules can be easily identified and separated from a heterologous mixture of substances. Exposure of the conjugate to radiation releases the target in a functional form and completely unaltered. Using photocleavable molecular precursors as the conjugates, label can be incorporated into macromolecules, the nascent macromolecules isolated and the label completely removed.
Abstract: A process for making N-vinyl-2-pyrrolidone (NVP) is disclosed. The process comprises dehydrating N-(2-hydroxyethyl)-2-pyrrolidone (HEP) in the presence of a catalyst and added water. Adding an effective amount of water into the dehydration process reduces the amount of N-ethyl-2-pyrrolidone (NEP) formed compared with the amount produced in the absence of the added water. Adding water can also sustain high conversions of HEP, minimize heavies formation, and improve selectivity to NVP. The process provides high-purity NVP and avoids a costly crystallization step.
Abstract: An unstable, methyl-substituted (1,1 oxaly diimidazole) molecule capable of accelerating the rate at which a material attains maximum chemiluminescence when reacted hydrogen peroxide in the presence of a fluorophore and a method to synthesize such molecules.
Type:
Grant
Filed:
November 10, 2003
Date of Patent:
November 28, 2006
Assignee:
Clemson University
Inventors:
Ji Hoon Lee, Mark A. Schlautman, Elizabeth A. Carraway
Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N—S(?O)2—; mono- or di(C1-6alkyl)amino-S(?O)2; —C(?N—Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-? and/or I
Type:
Grant
Filed:
August 9, 2002
Date of Patent:
November 21, 2006
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Christopher John Love, Jean Pierre Frans Van Wauwe, Marc J. De Brabander, Roger Clive Moses, Mykhalyo Goncharenko, Ludwig Paul Cooymans, Nele Vandermaesen, Gaston Stanislas Marcella Diels, Anthony William Sibley, Caterina Noula
Abstract: A novel process for preparation of alkenylphosphine oxides or alkenylphosphinic acid esters provided by which the objective compounds can be easily, safely and efficiently synthesized and easily separated and purified with little formation of by-products. Specifically, a process of conducting the addition reaction of an easily available secondary phosphine oxide or hydrogen phosphinic acid ester with an acetylene compound with a catalyst containing a Group 9 or 10 metal of the periodic table to thereby obtain the corresponding alkenylphosphine oxide or alkenylphosphinic acid ester.
Type:
Grant
Filed:
February 12, 2002
Date of Patent:
November 14, 2006
Assignees:
Japan Science and Technology Corporation, National Institute of Advanced Industrial Science & Technology
Abstract: Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification. and salts thereof. Since the compound represented by the formula (I) binds and antagonizes to DP receptor, it is useful for the prevention or treatment against the disease such as allergic disorder, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, pleuritis complicated by rheumatoid arthritis, cerebrovascular disease, and ulcerative colitis.
Abstract: The present invention provides a novel process for preparation of trans-3-ethyl 2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide via the novel intermediate compounds of formula 3.
Abstract: There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
October 31, 2006
Assignee:
AstraZeneca AB
Inventors:
Tord Inghardt, Anders Johansson, Arne Svensson
Abstract: Novel compounds of the general formula (I), wherein Ar, R1, R2, X1, X2, Y1, Y, and Z are as defined in the specification, the use of these compounds as pharmaceutical compositions, pharmaceutical 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 Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.
Type:
Grant
Filed:
October 24, 2003
Date of Patent:
October 31, 2006
Assignee:
Novo Nordisk A/S
Inventors:
Lone Jeppesen, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg, Pavel Pihera, Miroslav Havranek
Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having at least one halogenated hydrocarbon moiety, a biaryl moiety, and at least one heterocyclic moiety, that are useful as such agents.
Type:
Grant
Filed:
December 1, 2004
Date of Patent:
October 31, 2006
Assignee:
Rib-X Pharmaceuticals, Inc.
Inventors:
Shili Chen, Jiacheng Zhou, Yusheng Wu, Deping Wang, Joseph M. Salvino, Adegboyega K. Oyelere, Rongliang Lou
Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
June 2, 2004
Date of Patent:
October 31, 2006
Assignee:
Abbott Laboratories
Inventors:
Michael L. Curtin, Steven K. Davidsen, Robin R. Frey, Howard R. Heyman, James H. Holms, Michael Michaelides, Douglas H. Steinman
Abstract: The present invention relates to a process for the preparation of activated polyethylene glycols, or PEG(NPC)2s, comprising reacting polyethylene glycol with an activator while in the presence of an aromatic nitrogen containing heterocyclic base. The process is carried out at temperatures ranging from about 20 to about 30° C., more preferably at room temperature, and under stoichiometric conditions.
Abstract: This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-? activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.
Abstract: Heterocyclic amides of formula (1) wherein: Z is CH or nitrogen; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are selected from for example hydrogen, halo, C1-4alkyl, and C1-4alkanoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR2R3 or —OR3; R2 and R3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have va
Type:
Grant
Filed:
March 4, 2003
Date of Patent:
October 17, 2006
Assignee:
AstraZeneca AB
Inventors:
Paul Whittamore, Stuart Norman Lile Bennett, Iain Simpson
Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.
Type:
Grant
Filed:
January 26, 2005
Date of Patent:
October 17, 2006
Assignee:
Galderma Research & Development
Inventors:
Jean-Michel Bernardon, Laurence Clary, Eric Terranova