Hetero Ring Is Five-membered Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen (e.g., Selenazoles, Etc.) Patents (Class 548/100)
  • Patent number: 6525026
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: February 25, 2003
    Assignees: Elan Pharmaceuticals, Inc., American Home Products Corporation
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Susan Ashwell, Reinhardt Bernhard Baudy, Louis John Lombardo
  • Publication number: 20020169239
    Abstract: 2H-Benzotriazole UV absorbers substituted at the 3-position or at the 5-position of the phenyl ring by a 1,1-diphenylalkyl moiety, particularly a 1,1-diphenylethyl group, are particularly photostable in automotive coatings, and are of low color and exhibit low volatility in thermoplastic compositions.
    Type: Application
    Filed: February 7, 2002
    Publication date: November 14, 2002
    Inventors: Mervin G. Wood, Ramanathan Ravichandran, Joseph Suhadolnik, David Bramer, Jacqueline Lau, Anthony DeBellis
  • Patent number: 6475730
    Abstract: The present invention relates to a method of detecting nucleic acids and particularly to a method of analyzing for the presence and/or amount of a nucleic acid.
    Type: Grant
    Filed: December 20, 1999
    Date of Patent: November 5, 2002
    Assignee: The Victoria University of Manchester
    Inventors: Kenneth T Douglas, Elena V Bichenkova
  • Patent number: 6465421
    Abstract: The growth of body and/or head/cranial hair on mammalian organisms, for example humans, is modulated by administering thereto, whether topically and/or systemically, therapeutically effective amounts of at least one lipoxygenase or cyclooxygenase inhibitor, or at least one lipoxygenase or cyclooxygenase stimulator, preferably in the presence of at least one lipoxygenase/cyclooxygenase substrate or precursor thereof; when a hair-growth or hair loss-limiting response is sought to be elicited, a lipoxygenase inhibitor and/or cyclooxygenase stimulator is administered (conversely, to reduce or prevent hair growth, a lipoxygenase stimulator and/or cyclooxygenase inhibitor is administered).
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: October 15, 2002
    Assignee: Societe l'Oreal S.A.
    Inventors: Albert Duranton, Olivier De Lacharriere
  • Publication number: 20020127179
    Abstract: A method for purifying various nitrogen containing flavor and fragrance compounds is described. The method comprises at least one step of reverse crystallization for liquid compounds and may be followed by at least one step of forward crystallization for compounds that are solid at room temperature.
    Type: Application
    Filed: February 26, 2001
    Publication date: September 12, 2002
    Inventor: Morris Mann
  • Publication number: 20020111404
    Abstract: Benzotriazole UV absorbers substituted with a ultra long ester or amide moiety wherein the ester or amide group is a hydrocarbyl group of 25 to 100 carbon atoms or is a group of alkyl of 25 to 100 carbon atoms interrupted by 5 to 39 oxygen atoms and terminated with an omega-OH or an omega-OR group exhibit excellent stabilization efficacy while they concomitantly do not bloom when incorporated into polyolefin films. These benzotriazole UV absorbers also provide excellent protection to white, dyed, dipped, unscented and/or scented candle wax from discoloration and degradation.
    Type: Application
    Filed: February 11, 2002
    Publication date: August 15, 2002
    Inventors: Mervin Wood, Ramanathan Ravichandran, Douglas Wayne Horsey, Anunay Gupta, Deborah DeHessa, Luther A. R. Hall, Andrea Smith, Stephen Mark Andrews
  • Publication number: 20020111496
    Abstract: The subject invention provides compounds and methods of producing compounds, which are useful inhibitors of glycosyltransferase enzymes. These compounds represent a new class of glycosyltransferase inhibitors and are potent inhibitors of sialyltransferase. The subject invention also provides methods of treating diseases or conditions associated with glycosytransferases. Methods of modulating the activity of glycosytransferases are also provided.
    Type: Application
    Filed: February 4, 2002
    Publication date: August 15, 2002
    Inventors: Benjamin A. Horenstein, Hongbin Sun
  • Patent number: 6420522
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: July 16, 2002
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
  • Publication number: 20020091267
    Abstract: A method for producing camphorsultam, which includes the following steps 1 to 4:
    Type: Application
    Filed: July 9, 2001
    Publication date: July 11, 2002
    Inventors: Hiroshi Shiratani, Shigeya Yamasaki
  • Patent number: 6416762
    Abstract: The present invention provides structure-based combinatorial libraries of compounds containing the functional group minima of picornaviruses including poliovirus and rhinovirus. The libraries can be used to screen for therapeutical antiviral compounds, e.g., anti-picornaviral capsid-binding compounds.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: July 9, 2002
    Assignee: President and Fellows of Harvard College
    Inventors: Diane M. Joseph-McCarthy, Lyle D. Isaacs, George M. Whitesides, Martin Karplus, James M. Hogle, James Li-wen Cheh
  • Patent number: 6403807
    Abstract: Bridged fluorescent dyes of the cyanine and squaraine families are disclosed. The dyes are useful as markers in assay techniques and offer advantages of undergoing excitation at a common wavelength but emitting at structure dependent different wavelengths.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: June 11, 2002
    Assignee: SurroMed, Inc.
    Inventors: Rajendra Singh, Gregory Gorski, Gary Frenzel
  • Patent number: 6383521
    Abstract: The present invention provides Wondonin A of general formula (I), which is extracted from a two-sponge association of phylum Porifera (sponge) and has antiangiogenic activity, and a process for preparing the same. Wondonin A has no cytotoxicity, but has an inhibitory activity against angiogenesis which is one of the crucial mechanisms of cancer cell metastasis, thus, it can be applied not only as an anticancer drug but also as a therapeutic agent of angiogenesis-associated diseases such as cardiac ischemia, rheumatoid arthritis, and diabetes mellitus.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: May 7, 2002
    Assignee: Korea Ocean Research and Development
    Inventors: Jong-Heon Shin, Ki-Woong Cho, Young-Wan Seo, Jung-Rae Rho, Hyi-Seung Lee, Ho-Jeong Kwon
  • Patent number: 6372895
    Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.
    Type: Grant
    Filed: July 7, 2000
    Date of Patent: April 16, 2002
    Assignee: 3M Innovative Properties Company
    Inventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
  • Publication number: 20020006378
    Abstract: Compositions having a texaphyrin-lipophilic molecule conjugate loaded into a biological vesicle and methods for imaging, diagnosis and treatment using the loaded vesicle are provided. For example, liposomes or red blood cells loaded with a paramagnetic texaphyrin-lipophilic molecule conjugate have utility as a blood pool contrast agent, facilitating the enhancement of normal tissues, magnetic resonance angiography, and marking areas of damaged endothelium by their egress through fenestrations or damaged portions of the blood vascular system. Liposomes or cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate can be photolysed, allowing for a photodynamic therapy effect at the site of lysis. Availability of red blood cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate provides a method for delivering a photodynamic therapeutic agent to a desired site with a high concentration of oxygen.
    Type: Application
    Filed: November 20, 1997
    Publication date: January 17, 2002
    Inventors: STUART W. YOUNG, MEREDITH WRIGHT, JONATHAN L. SESSLER, TARAK D. MODY, DARREN MAGDA
  • Patent number: 6319488
    Abstract: This invention relates to colloidal systems charged with polymethine dyes and having suitable photophysical and pharmacological properties, their use as a contrast medium in fluorescence and transillumination diagnostics in the near infrared spectral range, as well as methods for their production.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: November 20, 2001
    Assignee: Institut für Diagnostikforschung GmbH an der Freien Universität Berlin
    Inventors: Kai Licha, Björn Riefke, Werner Weitschiess, Dieter Heldmann, Violetta Sudmann
  • Patent number: 6277877
    Abstract: Compounds of Formula (I) wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR8R9 or C(O)R12 as glycogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat diabetes, hyperglycemia, hypercholesterolemia, hypertension, hyperisulinemia, hyperlipidemia, atherosclerosis and myocardial ischemia in mammals.
    Type: Grant
    Filed: August 15, 2000
    Date of Patent: August 21, 2001
    Assignee: Pfizer, Inc.
    Inventors: Dennis J. Hoover, Bernard Hulin, William H. Martin, Douglas Phillips, Judith L. Treadway
  • Publication number: 20010014646
    Abstract: Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.
    Type: Application
    Filed: March 2, 2001
    Publication date: August 16, 2001
    Inventors: Peter Borden Mackenzie, Christopher Moore Killian, Leslie Shane Moody, Jason Patrick McDevitt
  • Patent number: 6274738
    Abstract: The invention provides DNA primase assays suitable for identifying DN primase modulating agents, methods of modulating DNA primase activity, compounds for modulating DNA primase activity, and compositions which modulate DNA primase.
    Type: Grant
    Filed: November 24, 1997
    Date of Patent: August 14, 2001
    Assignee: Geron Corporation
    Inventors: Michael R. Kozlowski, Junko Aimi, Ryan Holcomb
  • Patent number: 6218137
    Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: April 17, 2001
    Assignee: Lumigen, Inc.
    Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
  • Patent number: 6218359
    Abstract: The current invention concerns the use of a receptor from the RZR/ROR receptor family or of a functional fragment thereof in a test of a compound for anti-autoimmune, anti-arthritic, anti-tumor, melatonin-like and/or melatonin-antagonistic activity and the production of a receptor ligand complex comprising said receptor or a functional fragment thereof and a ligand of said receptor. Described is also a method for testing compounds for said activity (screening for ligands) and the active compounds identified therewith.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: April 17, 2001
    Assignee: Novartis Corporation
    Inventors: Irmgard Wiesenberg, Martin Missbach
  • Patent number: 6187928
    Abstract: Novel imidazolium compounds of the formula wherein A represents the atomic group necessary to form a heteroaromatic ring, which may be optionally substituted by one or more R substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; B is an optional substituent which represents the atomic group necessary to form a heteroaromatic ring or a double or triple carbon-nitrogen bond, which may optionally be substituted by one or more R′ substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; C is an optional substituent which represents the atomic group necessary to form an aromatic or heteroaromatic ring, which may optionally be substituted by one or more R″″ substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substituents; R″ and R′″ are each independently a lower alk
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: February 13, 2001
    Assignee: The Rockefeller University
    Inventors: Robert J. Donovan, Robert J. Morgan
  • Patent number: 6179906
    Abstract: This invention provides water-based compositions, particularly coating, ink, and agricultural compositions, manifesting reduced equilibrium and dynamic surface tension by the incorporation of a surface tension reducing amount of certain cyclic urea compounds of the structure where R is a C6 to C12 alkyl group or R″O—(CH2)m—, R′ is hydrogen or methyl, R″ is a C4 to C12 alkyl group, m is 2-4 and n is 1 or 2.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: January 30, 2001
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Anthony Marsella, Kevin Rodney Lassila
  • Patent number: 6162915
    Abstract: Chlorosulfonyl substituted aromatic heterocyclic compounds, such as 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compounds, were prepared in good yield by chloroxidation of di(aromatic heterocyclyl) disulfide compounds in a medium containing water, a water-immiscible organic solvent, and a phase transfer catalyst, such at tetrabutylammonium chloride.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: December 19, 2000
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas L. Pearson, Jimmy J. Tai, Timothy J. Adaway
  • Patent number: 6140051
    Abstract: Dibenzazole compounds having the general structure: ##STR1## wherein; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are independently H or a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety; Y is H or a cleavable moiety; X is a hydrogen, halogen, CF.sub.3, or SO.sub.3 H; V and W are oxygen or sulfur; Z is --C.dbd.C--, --C.tbd.C-- or an aromatic ring moiety; and n is 0, 1, or 2. When n=0 at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 is a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety or X is a halogen, CF.sub.3 or SO.sub.3 H. These compounds are highly fluorescent and can be easily detected using a fluorometer. Derivatives in which the Y group is a substituent other than H contain a fluorescence inhibiting chemical moiety that upon removal restores the fluorescence of the compound.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: October 31, 2000
    Assignee: Promega Biosciences, Inc.
    Inventors: Lauren R. Brown, Cheng Xu
  • Patent number: 6107329
    Abstract: Compounds of Formula (1) wherein R.sub.6 is carboxy, (C.sub.1 -C.sub.8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR.sub.8 R.sub.9 or C(O)R.sub.12 as glucogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat diabetes, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis and myocardial ischemia in mammals.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: August 22, 2000
    Assignee: Pfizer, Inc.
    Inventors: Dennis J. Hoover, Bernard Hulin, William H. Martin, Douglas Phillips, Judith L. Treadway
  • Patent number: 6087510
    Abstract: Methods of preparation of dyed textiles, fluorescent polymer matrices, fluorescent clonal markers, non-lineal optical polymers and diagnostic imaging agents are described using compounds with the general formula ##STR1## wherein A represents the atomic group necessary to form a heteroaromatic ring, wherein R may be a variety of;wherein P or Q are optional substituents, each independently a substituent selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halo, lower alkylamino, amino, nitro, or carboxy, or P and Q together represent the atomic group necessary to form a heteroaromatic ring, wherein R' may be a variety of substituents;C is an optional substituent which represents the atomic group necessary to form an aromatic or heteroaromatic ring, wherein R"" may be a variety of substituents;R" is hydrogen, a lower alkyl or aryl group, or together with R'" and the nitrogen atom to which it is attached, form a heterocyclic ring having from 5 to 7 members, which may optionally contain a
    Type: Grant
    Filed: February 8, 1999
    Date of Patent: July 11, 2000
    Assignee: The Rockefeller University
    Inventors: Robert J. Donovan, Robert J. Morgan
  • Patent number: 6084102
    Abstract: Minor groove binding molecules are covalently bound to oligonucleotides which in their base sequence are complementary to a target sequence of single stranded or double stranded DNA, RNA or hybrids thereof. The covalently bound oligonucleotide minor groove binder conjugates strongly bind to the target sequence of the complementary strand.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: July 4, 2000
    Assignee: Epoch Pharmaceuticals, Inc.
    Inventors: Igor V. Kutyavin, Eugeny A. Lukhtanov, Howard B. Gamper, Rich B. Meyer, Jr.
  • Patent number: 6083505
    Abstract: An immunogen/vaccine adjuvant composition containing an immunogen in an amount effective to stimulate an immune response and as a vaccine adjuvant a 1H-imidazo[4,5-c]quinolin-4-amine in an amount effective to increase the immune response to the immunogen.
    Type: Grant
    Filed: March 24, 1994
    Date of Patent: July 4, 2000
    Assignee: 3M Innovative Properties Company
    Inventors: Richard L. Miller, Mark A. Tomai, David I. Bernstein, Christopher J. Harrison
  • Patent number: 6083485
    Abstract: This invention relates to an in-vivo diagnostic method based on near infrared radiation (NIR radiation) that uses water-soluble dyes and their biomolecule adducts, each having specific photophysical and pharmaco-chemical properties, as a contrast medium for fluorescence and transillumination diagnostics in the NIR range, to new dyes and pharmaceuticals containing such dyes.
    Type: Grant
    Filed: November 7, 1997
    Date of Patent: July 4, 2000
    Assignees: Institut fur Diagnostikforschung GmbH, der Freien Universitat Berlin
    Inventors: Kai Licha, Bjorn Riefke, Wolfhard Semmler, Ulrich Speck, Christoph-Stephan Hilger
  • Patent number: 6080868
    Abstract: The invention provides an asymmetric cyanine dye compound having the structure ##STR1## including substituted forms thereof, wherein, at least one of R.sub.1 and R.sub.2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labeled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labeled polynucleotides.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: June 27, 2000
    Assignee: The Perkin-Elmer Corporation
    Inventors: Linda G. Lee, Ronald J. Graham, Khairuzzaman B. Mullah, Francis T. Haxo
  • Patent number: 6028088
    Abstract: The present invention provides thiazolidinediones which are useful as antiproliferative, antiinflammatory and antiinfective agents. These compounds are useful for the treatment of certain endocrine diseases including diabetes, certain malignant and non-malignant proliferative diseases including prostate cancer, breast cancer, psoriasis, and acne, certain cardiovascular disorders including hypertension and occlusive vascular diseases.
    Type: Grant
    Filed: October 30, 1998
    Date of Patent: February 22, 2000
    Assignee: The University of Mississippi
    Inventors: Harrihar A. Pershadsingh, Mitchell A. Avery
  • Patent number: 6015544
    Abstract: A process for producing a carrier free radio halogenated 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5,6-dihydro-5-methyl-6-oxo-4H-imida zo[1,5-a][1,4]-benzodiazepine of formula (II) where R.sup.1 is a radioactive halogen and R.sup.1 may be at 7, 8, 9 or 10 substituent. The above compound is used in a pharmaceutical composition for nuclear medicine examination.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: January 18, 2000
    Assignee: Map Medical Technologies Oy
    Inventors: Christian Foged, Christer Halldin, Jukka Hiltunen, Lars Farde
  • Patent number: 6001829
    Abstract: The present invention relates to novel fluoropropenyl heterocycles of the formula (I) foundCF.sub.2 .dbd.CX--CH.sub.2 -Het (1),in whichHet, X and R are each as defined in the description, to processes for their preparation and to their use for controlling animal pests.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: December 14, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Udo Kraatz, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Norbert Mencke
  • Patent number: 5994143
    Abstract: Fluorescent conjugates suitable for use in flow cytometry and other biological applications. The fluorescent conjugates comprise an antibody having a polymeric dye bound thereto. The polymeric dye is preferably enhanced by a hydrophobic and conformationally restrictive moiety either bound thereto or in close association therewith. The hydrophobic and conformationally restrictive moiety is preferably derived from a cyclodextrin. The polymeric dye comprises a polymeric entity having signal-generating groups, such as aminostyryl pyridinium dye residues attached thereto. The fluorescent conjugates exhibit exceptional stability characteristics and avoid many of the problems of energy transfer, bio-conjugability, and solubility.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: November 30, 1999
    Assignee: Abbott Laboratories
    Inventors: Christopher Bieniarz, Jeffrey B. Huff, Michael J. Cornwell, Seshagiri R. Tata Venkata
  • Patent number: 5935927
    Abstract: The present invention relates generally to methods and compositions for treating amyloidogenic diseases such as Alzheimer's disease and the development of type II diabetes, in which deposition of amyloid in organs such as the brain and pancreas interfere with neurological function and insulin release, respectively. The methods and compositions are directed toward increasing the activity of scavenger cells within the body at recognizing and removing amyloid deposits from affected tissues and organs. Scavenger cells may be targeted to amyloid deposits by means of spontaneously-occurring chemical modifications called advanced glycosylation endproducts (AGEs). Compositions are described which increase scavenger cell activity towards AGE-modified amyloid.
    Type: Grant
    Filed: August 10, 1996
    Date of Patent: August 10, 1999
    Assignee: The Picower Institute For Medical Research
    Inventors: Michael P. Vitek, Anthony Cerami, Richard J. Bucala, Peter C. Ulrich, Helen Vlassara, Xini Zhang
  • Patent number: 5932363
    Abstract: A luminescent composition containing a mixture of a fluorescent material and a metal chelate compound of the formulaL.sub.n --M.sup.+n (I)wherein M represents a metal; n is a number of from 1 to 3, and L is a ligand of the formula ##STR1## wherein Ar is an aryl; X is selected from the group consisting of oxygen, sulfur, and selenium; N is nitrogen; O is oxygen, and Z is a suitable aromatic component.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: August 3, 1999
    Assignee: Xerox Corporation
    Inventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
  • Patent number: 5919809
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: July 6, 1999
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 5874587
    Abstract: Novel imidazolium compounds of the formula ##STR1## wherein A represents the atomic group necessary to form a heteroaromatic ring, which may be optionally substituted by one or more R substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; B is an optional substituent which represents the atomic group necessary to form a heteroaromatic ring or a double or triple carbon-nitrogen bond, which may optionally be substituted by one or more R' substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; C is an optional substituent which represents the atomic group necessary to form an aromatic or heteroaromatic ring, which may optionally be substituted by one or more R"" substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substituents; R" and R'" are each independently a lower alkyl or aryl group, or together with the nitrogen
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: February 23, 1999
    Assignee: The Rockefeller University
    Inventors: Robert J. Donovan, Robert J. Morgan
  • Patent number: 5849921
    Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo?1,2-a!pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-?(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo?1,2-a!pyridin-2-yl)-ben zimidazol-1-yl)-methyl!-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 15, 1998
    Assignee: Astra Aktiebolag
    Inventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
  • Patent number: 5804389
    Abstract: A method for detecting abnormal cell shedding rates of mature epithelial cells of a warm-blooded animal, such as the epithelial cells of the gastric or colonic glands. A labeling composition containing, e.g., a cyanine dye is applied to epithelial cells, following which the site is observed over time. Abnormal cell shedding rates are indicative of disease states such as carcinoma.
    Type: Grant
    Filed: December 29, 1995
    Date of Patent: September 8, 1998
    Assignee: Phanos Technologies, Inc.
    Inventor: Masahiro Tada
  • Patent number: 5747515
    Abstract: Novel heterocyclic compounds having a structure according to general formula (1), pharmaceutically acceptable acid addition salts and solvates thereof are described as having a pharmacological profile showing potential for treatment of acute and chronic neuropsychiatric disorders which are known as progressively deteriorating conditions leading to neuronal cell death and dysfunction. Pharmaceutical formulations are described as containing said therapeutic compounds.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: May 5, 1998
    Assignee: Astra Aktiebolag
    Inventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
  • Patent number: 5741912
    Abstract: Novel compounds containing a heteroatom-bearing bridge and novel complexes of these compounds with metals. The novel compounds and complexes are useful in diagnostic and therapeutic methods.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 21, 1998
    Assignee: Bracco International B.V.
    Inventors: Kondareddiar Ramalingam, Natarajan Raju
  • Patent number: 5712299
    Abstract: The present invention relates to novel heterocyclic compounds having the general formula (1) ##STR1## wherein: X is O, S or Se;R.sub.1 is H, lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkyl or CF.sub.3 ;R.sub.2 is H, lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkyl or CF.sub.3 ;W is O, S, NH or N-lower alkyl;R.sub.3 is H, lower alkyl or lower acyl;Ar is phenyl, furyl, thienyl, naphthyl, pyridyl or pyrrolyl, optionally substituted by R.sub.6 ;R.sub.6 is one or more groups selected from lower alkyl, lower acyl, halogen, lower alkoxy, CF.sub.3, OH, NO.sub.2 or NR.sub.4 R.sub.5, wherein R.sub.4 and R.sub.5 independently are H, lower alkyl or lower acyl;geometrical and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition salts thereof and solvates thereof having therapeutic activity, processes and intermediates for their preparation, pharmaceutical formulations containing said compounds and the medicinal use of said compounds.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: January 27, 1998
    Assignee: Astra Aktiebolag
    Inventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
  • Patent number: 5691381
    Abstract: The present invention provides novel hydroxamic acids and carbocyclic acids and derivatives thereof and to pharmaceutical compositions and methods of use of these novel compounds for the inhibition of matrix metalloproteinases, such as stromelysin, and inhibit the production of tumor necrosis factor alpha, and for the treatment of arthritis and other related inflammatory diseases.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: November 25, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Irina Cipora Jacobson, Carl Peter Decicco, Robert Joseph Cherney
  • Patent number: 5672332
    Abstract: This invention provides functional dyes of the general formula: ##STR1## wherein R.sup.1, R.sup.2, and R.sup.5 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 allkyl, C.sub.1 -C.sub.10 alkoxyl, hydroxyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, carboxyl, C.sub.1 -C.sub.10 carboxylalkyl, halogen, nitro, C.sub.1 -C.sub.10 alkoxycarbonyl, mercapto, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.1 -C.sub.10 alkylthio, sulfonate, and --(CH.sub.2).sub.m --N(R.sup.6)(R.sup.7) wherein R.sup.6 and R.sup.7 are independently hydrogen or C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 acyl, and R.sup.6 and R.sup.7 are capable of forming 5, 6, or 7 membered rings which may optionally be substituted with --O--, --NR.sup.8, or --S--; R.sup.3 and R.sup.4 may be the same or different and are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: May 13, 1996
    Date of Patent: September 30, 1997
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: Ella Y. Fung, Raghavan Rajagopalan
  • Patent number: 5672333
    Abstract: This invention provides functional dyes of the general formula: ##STR1## wherein R1, R2, and R.sup.5 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyl, hydroxyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, carboxyl, C.sub.1 -C.sub.10 carboxylalkyl, halogen, nitro, C.sub.1 -C.sub.10 alkoxycarbonyl, mercapto, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.1 -C.sub.10 alkylthio, sulfonate, and --(CH.sub.2).sub.m --N(R.sup.6)(R.sup.7) wherein R.sup.6 and R.sup.7 are independently hydrogen or C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 acyl, and R.sup.6 and R.sup.7 are capable of forming 5, 6, or 7 membered rings which may optionally be substituted with --O--, --NR.sup.8, or --S--; R.sup.3 and R.sup.4 may be the same or different and are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, C.sub.1 -C.
    Type: Grant
    Filed: May 13, 1996
    Date of Patent: September 30, 1997
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: Raghavan Rajagopalan, Ella Y. Fung
  • Patent number: 5627286
    Abstract: Novel compounds containing a heteroatom-bearing bridge and novel complexes of these compounds with metals. The novel compounds and complexes are useful in diagnostic and therapeutic methods.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 6, 1997
    Assignee: Bracco International B.V.
    Inventors: Kondareddiar Ramalingam, Natarajan Raju
  • Patent number: 5563168
    Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.
    Type: Grant
    Filed: June 16, 1995
    Date of Patent: October 8, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5532228
    Abstract: The invention discloses side-chain homologous vitamin D derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, B, and D have the meanings defined in the specification and either (1) A is a direct bond between carbon atoms 20 and 22 and X is an oxy alkylene radical, --(CH.sub.2).sub.n O-- where n is 1 to 3; (2) A is a methylene bridge, --CH.sub.2 --, between carbon atoms 20 and 22 and X is either an alkylene radical, --(CH.sub.2).sub.n -- or an oxy alkylene radical, --(CH.sub.2).sub.n O--, where n is 1 to 3; or (3) if A is a direct bond and B and D together form a second bond, then X(R.sup.5) (R.sup.6) is ##STR2## The compounds possess proliferation-inhibiting and cell-differentiating activity.
    Type: Grant
    Filed: June 1, 1993
    Date of Patent: July 2, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Gunter Neef, Gerald Kirsch, Andreas Stein-Eyer, Katica Schwarz, Matthias Brautigam, Ruth Thieroff-Ekerdt, Petra Rach
  • Patent number: RE35811
    Abstract: Insecticidal novel nitro compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkyl, R.sup.3 is --S--R.sup.4 or ##STR2## in which R.sup.4 is C.sub.1-4 alkyl, R.sup.5 and R.sup.6 are hydrogen or C.sub.1-4 alkyl,Y is CH or N, andZ is a five- or six-membered heterocyclic group having at least one nitrogen atom which may be substituted by halogen or C.sub.1-4 alkyl, provided that where Y is CH,then R.sup.1 is C.sub.1-4 alkyl.
    Type: Grant
    Filed: October 3, 1995
    Date of Patent: May 26, 1998
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya