Nitrogen In Aglycone Moiety Patents (Class 536/17.9)
-
Patent number: 7534434Abstract: This invention relates to immunogenic compounds which may serve as ligands for NKT (natural killer T) cells and to methods of use thereof in modulating immune responses.Type: GrantFiled: December 27, 2005Date of Patent: May 19, 2009Assignees: The Rockefeller University, The Scripps Research InsitituteInventors: Moriya Tsuji, David D. Ho, Chi-Huey Wong, Doug Wu, Masakazu Fujio
-
Patent number: 7517891Abstract: The present invention relates to compositions and methods for preparing pharmaceutical compositions. In some embodiments, the invention includes compounds and methods of resolving chiral compounds. In some embodiments, the invention includes chiral and crystalline compositions and hydrates. In some embodiments, the invention contemplates compositions comprising camptothecin derivatives and synthetic intermediates thereof. In some embodiments, the invention includes methods of protecting, inserting, modifying, separating isomers, and removing chemical groups.Type: GrantFiled: October 26, 2006Date of Patent: April 14, 2009Assignee: Glyconix CorporationInventor: Brian Keith Shull
-
Publication number: 20090093418Abstract: A new class of paromomycin-derived aminoglycosides, which exhibit efficient stop-codon mutation suppression activity, low toxicity and high selectivity towards eukaryotic cells are provided. Also provided are chemical and chemo-enzymatic processes of preparing these paromomycin-derived aminoglycosides and intermediates thereof, as well as pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders.Type: ApplicationFiled: October 1, 2008Publication date: April 9, 2009Applicant: Technion Research & Development Foundation Ltd.Inventors: Timor Bassov, Tamar Ben-Yosef, Igor Nudelman, Annie Rebibo-Sabbah, Dalia Shallom-Shezifi, Mariana Hainrichson
-
Publication number: 20090075909Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds of this invention can be useful for inhibition and prevention of inflammation and associated pathologies, including inflammatory and autoimmune diseases, for example, bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection or psoriasis. The present invention also relates to pharmacological compositions containing these monosaccharide derivatives, as well as methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, and other inflammatory and/or auto immune disorders.Type: ApplicationFiled: December 22, 2005Publication date: March 19, 2009Applicant: RANBAXY LABORATORIES LIMITED INC.Inventors: Viswajanani Jitendra Sattigeri, Sudershan K. Arora, Mohammad Salman, Venkata P. Palle, Muthukaman Nagarajan, Rajkumar Shirumalla, Gurpreet Kaur Aulakh, Abhijit Ray
-
Publication number: 20090048185Abstract: A therapeutic drug for diseases, in which NKT cells or stimulus of NKT cells is involved in deterioration of disease conditions, containing, as an active ingredient, a glycolipid derivative having the formula (I): wherein R1 indicates an aldopyranose residue, R2 indicates a hydrogen atom or a hydroxy group, A indicates —CH2—, —CH(OH)—CH2— or —CH?CHCH2—, x indicates an integer of 13 to 16 and y indicates an integer of 0 to 25 or its pharmacologically acceptable hydrate or solvate.Type: ApplicationFiled: October 27, 2006Publication date: February 19, 2009Inventors: Sachiko Miyake, Takashi Yamamura, Hirokazu Annoura
-
Publication number: 20090047299Abstract: Modified glycolipid compounds are provided. Also disclosed are methods for activating an NKT cell, methods of stimulating an immune response in a subject, and methods suitable for labeling NKT cells.Type: ApplicationFiled: April 9, 2007Publication date: February 19, 2009Inventors: Paul B. Savage, Luc Teyton, Albert Bendelac
-
Patent number: 7491805Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including galactosamine and N-acetyl galactosamine derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.Type: GrantFiled: February 13, 2004Date of Patent: February 17, 2009Assignee: Sirna Therapeutics, Inc.Inventors: Chandra Vargeese, Peter Haeberli, Weimin Wang, Tongqian Chen
-
Publication number: 20090042819Abstract: The invention describes novel organic nitric oxide donor salts of a antimicrobial compounds, and novel compositions and kits comprising at least one organic nitric oxide donor salt of an antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. In one embodiment the antimicrobial compounds of the invention are aztreonam, ciprofloxacin, doripenam, duramycin and tobramycin. The organic nitric oxide donors that form salts are preferably organic nitrates, organic nitrites, nitrosothiols, thionitrites and heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.Type: ApplicationFiled: February 16, 2006Publication date: February 12, 2009Applicant: NitroMed, Inc.Inventors: James L. Ellis, David S. Garvey, Chia-En Lin
-
Publication number: 20090042811Abstract: The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.Type: ApplicationFiled: June 12, 2006Publication date: February 12, 2009Inventors: Robert Bittman, Hoe-Sup Byun, Gilbert Arthur
-
Publication number: 20090036658Abstract: A method for the production of a-O-galactosyl ceramide precursor is demonstrated. The method involves the reaction of galactosyl iodide with a sphingosine derivative or phytosphingosine derivative in the presence of a quaternary ammonium iodide salt to prepare the a-O-galactosyl ceramide precursor in the a-anomer form. The a-O-galactosyl ceramide is then prepared by reaction with a suitable fatty acid or fatty acid derivative.Type: ApplicationFiled: March 3, 2006Publication date: February 5, 2009Applicant: The Regents of the University of CaliforniaInventors: Jacquelyn Gervay-Hague, Wenjun Du
-
Publication number: 20090029006Abstract: A novel compound causing an oral cavity stimulus such as acridness, which is expressed by the following structural formula (I):Type: ApplicationFiled: November 29, 2005Publication date: January 29, 2009Inventors: Norihiko Kageyama, Takako Inui, Koichi Nakahara, Hajime Komura
-
Publication number: 20090018091Abstract: The invention describes compositions and kits comprising at least one nitric oxide enhancing group antimicrobial compound, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitric oxide enhancing antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. The antimicrobial compounds of the invention are preferably tobramycin, aztreonam, ciprofloxacin and doripenam. The nitric oxide enhancing antimicrobial compounds are substituted with at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group. The nitric oxide enhancing groups are nitroxides and/or heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.Type: ApplicationFiled: August 2, 2006Publication date: January 15, 2009Applicant: NITROMED, INC.Inventors: James L. Ellis, David S. Garvey
-
Patent number: 7470671Abstract: The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the method for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thromboses or cardiac insufficiency.Type: GrantFiled: September 24, 2004Date of Patent: December 30, 2008Assignee: Laboratoire FournierInventors: Véronique Barberousse, Soth Samreth, Benaïssa Boubia, François Bellamy, Vincent Peyrou
-
Publication number: 20080300389Abstract: The current disclosure, in one embodiment, includes a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid. According to another embodiment, the disclosure provides a method of synthesizing a polysaccharide conjugate by covalently bonding a monomeric amino acid having an O-group to a polysaccharide and by conjugating a metal to the O-group to form a polysaccharide conjugate. According to a third embodiment, the disclosure relates to a method of killing a cancer cell by administering to the cell an effective amount of a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid.Type: ApplicationFiled: January 18, 2008Publication date: December 4, 2008Inventors: David J. Yang, Dong-Fang Yu, I-Chien Wei
-
Publication number: 20080300390Abstract: The present invention relates to reducing carbohydrate derivatives of adamantane amines of Formula A or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R1, R2, R3, and R4 are together or separately H, F, methyl or lower alkyl, alkenyl, or alkynyl groups, and Z is derived from a mono-, di-, oligo-, or poly-saccharide that originally had an aldehyde carbonyl group. The present invention also relates to processes for the preparation of such adamantane amine derivatives, and uses of such derivatives. The compounds of the present invention are useful in the treatment of infections caused by Gram positive or Gram negative bacteria.Type: ApplicationFiled: June 24, 2008Publication date: December 4, 2008Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Sebastian P. Assenza, Nanzhu Shen, Salvatore Iacono, Yuriy B. Kalyan, Peter Viski, Matthew Ronsheim
-
Publication number: 20080261895Abstract: The present invention provides novel isolated compounds characterized as metabolites or derivatives of desmethylvenlafaxine including hydroxy-DV metabolites, hydroxy-DV-glucuronide metabolites, N-oxide-DV metabolites, and benzyl-hydroxy-DV metabolites. The invention includes pharmaceutical compositions comprising any of the metabolites or derivatives of the invention in combination with a pharmaceutically acceptable carrier or excipient. The invention also includes a method of treating at least one central nervous system disorder in a mammal comprising providing to a mammal in need thereof an effective amount of the compounds of the invention.Type: ApplicationFiled: October 24, 2007Publication date: October 23, 2008Inventors: Matthew J. Hoffmann, William DeMaio, Jim Wang, John W. Ullrich
-
Patent number: 7439343Abstract: Aminoglycoside-polyamines are disclosed along with methods of use thereof in displacement chromatography and as DNA-binding ligands. The aminoglycoside-polyamines are derivatives of carbohydrates, such as sugars, amino sugars, deoxysugars, glycosides, nucleosides and their substituted counterparts. The subject polyamines possess a group in place of at least one hydrogen atom of at least one hydroxyl group of the carbohydrate compound. In these compounds R1 is an alkyl group or an azaalkyl group, and R2 is a primary or secondary amino group.Type: GrantFiled: September 1, 2005Date of Patent: October 21, 2008Assignee: Rensselaer Polytechnic InstituteInventors: Kaushal Rege, Shanghui Hu, Jonathan S. Dordick, Steven M. Cramer
-
Publication number: 20080241128Abstract: Ligand Drug conjugate compounds comprising a ?-glucuronide-based linker and methods of using such compounds are provided.Type: ApplicationFiled: July 18, 2006Publication date: October 2, 2008Applicant: Seattle Genetics, Inc.Inventor: Scott Jeffrey
-
Publication number: 20080206319Abstract: The present invention relates to new adjuvants and the uses in pharmaceutical compositions, like in vaccines. In particular, the present invention provides new compounds useful as adjuvants for prophylactic and/or therapeutic vaccination in the treatment of infectious diseases, inflammatory diseases, autoimmune diseases, tumours, allergies as well as for the control of fertility in human or animal populations. The compounds are particularly useful not only as systemic, but preferably as mucosal adjuvants. In addition, the invention relates to its uses as active ingredients in pharmaceutical compositions.Type: ApplicationFiled: October 19, 2006Publication date: August 28, 2008Inventors: Thomas Ebensen, Michael Morr, Carlos A. Guzman
-
Publication number: 20080177050Abstract: Alpha, omega-difunctional aldaramides, in particular diaminoaldaramides, dihydroxyaldaramides, bis(alkoxycarbonylalkyl)aldaramides, and bis(carboxyalkyl)aldaramides, and processes for preparing the aldaramides are provided.Type: ApplicationFiled: January 31, 2008Publication date: July 24, 2008Inventors: Mark Allen Andrews, Henry Keith Chenault, Garret D. Figuly
-
Publication number: 20080161546Abstract: Compounds and methods are provided for obtaining oligosaccharide mimics. More specifically, compounds and methods are described wherein oligosaccharide mimics are obtained by incorporating or substituting in a cyclohexane derivative.Type: ApplicationFiled: October 9, 2007Publication date: July 3, 2008Applicant: GlycoMimetics, Inc.Inventors: Beat Ernst, Daniel Schwizer, Arun K. Sarkar, John L. Magnani
-
Publication number: 20080125350Abstract: The present invention provides a branched polyalkylene glycol wherein three or more single-chain polyalkylene glycols and a group having reactivity with an amino acid side chain, the N-terminal amino group or the C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity are bound; and a physiologically active polypeptide modified with the branched polyalkylene glycol.Type: ApplicationFiled: October 23, 2007Publication date: May 29, 2008Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Motoo Yamasaki, Toshiyuki Suzawa, Tatsuya Murakami, Noriko Sukurai, Kinya Yamashita, Mayumi Mukai, Takashi Kuwabara
-
Publication number: 20080119414Abstract: The invention relates to a composition containing an alkyl and/or alkenyl oligoglycoside and a cationic alkyl and/or alkenyl oligoglycoside of the formula: R2—O-[G]x-Zy ??(II) wherein, R2 is a linear or branched alkyl and/or alkenyl group containing 4 to 22 carbon atoms, G is a sugar unit containing 5 or 6 carbon atoms, x is a number of 1 to 10, y is a number of 1 to 4 and Z is an —OCH2—(CH(B))v—(CH(A))w-N+(R3R4R5)X? group, where A and B independently of one another represent hydrogen or a hydroxyl group, v and w independently of one another are numbers of 1 to 18, X is an anion selected from the group consisting of chloride, bromide, iodine, fluoride, NO3?, SO42? and PO43?, and R3, R4 and R5 independently of one another represent hydrogen or alkyl and/or alkenyl groups containing 1 to 22 carbon atoms and at least two of the substituents R3 to R5 are alkyl and/or alkenyl groups.Type: ApplicationFiled: October 27, 2005Publication date: May 22, 2008Inventors: Ansgar Behler, Frank Clasen
-
Patent number: 7375088Abstract: This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.Type: GrantFiled: January 21, 2004Date of Patent: May 20, 2008Assignee: Thallion Pharmaceuticals Inc.Inventors: Brian O. Bachmann, James B. McAlpine, Emmanuel Zazopoulos, Chris M. Farnet
-
Patent number: 7365055Abstract: The invention relates to novel derivatives of morphine-6-glucuronide, the preparation method thereof and the uses of same in therapy, for example, as analgesics.Type: GrantFiled: December 22, 2004Date of Patent: April 29, 2008Assignee: BTG International LimitedInventors: Jamal Temsamani, Roger Lahana, Patrick Mouchet
-
Patent number: 7244712Abstract: The present invention relates to aminoglycoside compounds having antibiotic activity. Moreover, the present invention relates to L-aminoglycoside compounds and diastereomers thereof which posses antibiotic activity and are not susceptible to development of resistant bacterial strains. The present invention also relates to methods of treatment and pharmaceutical compositions that utilize or comprise one or more of aminoglycoside compounds provided by the invention.Type: GrantFiled: September 14, 2004Date of Patent: July 17, 2007Assignee: President and Fellows of Harvard CollegeInventor: Robert R. Rando
-
Patent number: 7220727Abstract: The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminogylcosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).Type: GrantFiled: November 1, 2001Date of Patent: May 22, 2007Assignee: Wayne State UniversityInventors: Jalal Haddad, Lakshmi Kotra, Shahriar Mobashery
-
Patent number: 7211663Abstract: One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.Type: GrantFiled: November 1, 2001Date of Patent: May 1, 2007Assignee: Massachusetts Institute of TechnologyInventors: Peter H. Seeberger, Obadiah J. Plante
-
Patent number: 7115721Abstract: There are provided a novel microorganism Enterobacter sp. B20 strain which produces (E)-4-(2-isocyanovinyl)phenyl ?-rhamnopyranoside having a favorable effect of inhibiting melanogenesis and ?-L-rhamnopyranoside produced thereby. This novel microorganism is a gram-negative bacillus isolated from soil and shows motility owing to polar flagellum. The ?-L-rhamnopyranoside, which is produced by culturing the microorganism under aerobic conditions at a culture temperature of 10 to 37° C. and at a medium pH of about 5 to 9 usually for about 1 to 7 days, is useful as a highly safe and stable whitening agent.Type: GrantFiled: January 29, 2003Date of Patent: October 3, 2006Assignees: Astellas Pharma Inc., Nagase & Co., Ltd,Inventors: Akira Nakagawa, Senji Takahashi, Toshitsugu Miyazaki, Yuuko Osanai, Kunio Kosaka, Koji Nagai, Nakako Arao, Kouichi Tanaka
-
Patent number: 7105491Abstract: This invention provides nucleic acid sequences and characterization of the gene cluster responsible for the biosynthesis of the enediyne C-1027 (produced by Streptomyces globisporus). Methods are provided for the biosynthesis of enediynes, enediyne analogs and other biological molecules. This invention also provides enediyne and enediyne analogs biosynthesized by manipulation of the C-1027 gene pathway.Type: GrantFiled: November 12, 2002Date of Patent: September 12, 2006Assignee: Wisconsin Alumni Research Foundation (WARF)Inventors: Ben Shen, Wen Liu
-
Patent number: 7019131Abstract: The reactivity of a number of p-methylphenyl thioglycoside (STol) donors which are either fully protected or have one hydroxyl group exposed has been quantitatively determined by HPLC in conjunction with the development of a broadly applicable approach for a facile one-pot synthesis of oligosaccharides. The influence on reactivity of the structural effects of different monosaccharide cores and different protecting groups on each glycoside donor is characterized and quantified. In addition, a correlation between glycosyl donor reactivity and the chemical shift of the anomeric proton by 1 H NMR has been established. A database of thioglycosides as glycosyl donors has been created using this reactivity data. The utility is demonstrated by the easy and rapid one-pot assembly of various linear and branched oligosaccharide structures.Type: GrantFiled: March 25, 2003Date of Patent: March 28, 2006Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Zhiyuan Zhang, Ian Ollmann, Timor Baasov, Xin-Shan Ye
-
Patent number: 6921810Abstract: Bifunctional antibiotics that target both bacterial RNA and resistance-causing enzymes are disclosed. The A-site of bacterial 16S rRNA serves as the target site for most aminoglycoside antibiotics. Resistance to this class of antibiotics is frequently developed by microbial enzymatic acetylation, phosphorylation or ribosylation of aminoglycosides, modifications that weaken their interactions with the target RNA. Using surface plasmon resonance (SPR), the binding affinity and stoichiometry of various amino-glycosides have been investigated and it was found that neamine, the key pharmacophore of the deoxystreptamine class of amino-glycosides, binds to the A-site in a two to one stoichiometry with a Kd of 10 ?M for each binding site. A library of neamine dimers was prepared and their affinities to 16S rRNA A-site were determined by SPR, with Kd=40 nM for the best dimer (an ˜103-fold increase in affinity). Antibiotic activities of the dimers were determined for several bacterial strains by the Kirby-Bauer method.Type: GrantFiled: April 27, 2001Date of Patent: July 26, 2005Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Steven Sucheck
-
Patent number: 6916920Abstract: A process for producing hydrazinomonosaccharide derivatives and use of hydrazines in determining the structures of aldose and ketose monosaccharides located at the reducing ends of saccharides.Type: GrantFiled: July 30, 2001Date of Patent: July 12, 2005Assignee: Takara Bio Inc.Inventors: Tsuyoshi Miyamura, Tomoe Egashira, Mutsumi Sano, Brad K. Bendiak, Ikunoshin Kato
-
Patent number: 6887854Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: GrantFiled: May 13, 2003Date of Patent: May 3, 2005Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Hermo N. Jimenez, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugai
-
Patent number: 6872820Abstract: Finely divided polysacharide derivatives are described. The finely divided polysacharide derivatives are prepared by a process comprising: a) forming an aqueous composition comprising a polysaccharide derivative and water, in which the polysaccharide derivative is soaked or dissolved; b) converting the polysaccharide derivative of the aqueous composition into finely divided solid particles by, (i) contacting the aqueous composition with superheated water vapor in a dryer-pulverizer; or (ii) causing the polysaccharide derivative of the aqueous composition to flocculate; and c) optionally drying the finely divided solid particles of step b). The primary structures of the polysaccharide starting material are largely removed, and the product has a shape factor of less than 5 and greater than or equal to 1.Type: GrantFiled: October 1, 2001Date of Patent: March 29, 2005Assignee: Wolff Walsrode AGInventors: Gunter Weber, Detmar Redeker, Bernd Klinksiek, Jürgen Hinderer, Benno Ulfik
-
Patent number: 6867230Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: June 1, 2001Date of Patent: March 15, 2005Assignee: Pfizer, Inc.Inventors: Matthew Merrill Hayward, Michael S. Visser, Robert G. Linde, II, Takushi Kaneko
-
Patent number: 6858233Abstract: The invention provides a process for reducing odour, bitterness, astringency and pungency of a Simmondsins extract by dissolving the Simmondsins extract in a solvent if the Simmondsins extract is in a dry form, reacting the liquid Simmondsins extract with a carbonaceous adsorbent, such as activated carbon, to obtain a mixture, separating the adsorbent from the mixture to obtain a purified liquid extract, and drying the purified liquid extract.Type: GrantFiled: July 3, 2003Date of Patent: February 22, 2005Assignee: International Flora Technologies, Ltd.Inventors: Qingnong Tang, James Howard Brown, Wenhui Fu
-
Patent number: 6844346Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: December 24, 2002Date of Patent: January 18, 2005Assignees: IBBEX, Inc., Univ. of Alabama at BirminghamInventors: Stephen C. Johnson, Ashraf Saeed, Ming Luo
-
Patent number: 6841536Abstract: Disclosed is a prodrug of the formula: where A is a sulfur or a selenium, and R is derived from a mono- di- or oligo- saccharide. Also disclosed is a prodrug of the formula: where A is sulfur or selenium, R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O, and the R? groups may be the same or different and may be hydrogen, alkyl, alkoxy, carboxy. Also disclosed is a conjugate of an antioxidant vitamin and a thiolamine or selenolamine. Also disclosed is a prodrug of the formula; where A is sulfur or selenium, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is also be an alkyl or aryl group, or R? is ?O, and R‡ is an alkoxy, or an amine group. Also disclosed is a prodrug of the formula: where R is COOH or H, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH,where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O.Type: GrantFiled: January 18, 2002Date of Patent: January 11, 2005Assignee: University of Utah Research FoundationInventors: Jeannette C. Roberts, Britta H. Wilmore, Pamela B. Cassidy, Pamela K. Dominick, Megan D. Short
-
Patent number: 6812332Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: January 21, 2003Date of Patent: November 2, 2004Assignees: IBBEX, Inc., UAB Research FoundationInventors: Stephen C. Johnson, Ashraf Saeed, Ming Luo
-
Patent number: 6794497Abstract: The present invention provides compounds and methods of synthesizing furanose and aminofuranose compounds of Formula I which are useful fro treating rheumatoid arthritis, immunomodulatory diseases and disorders, inflammation, and diseases and disorders characterized by exhibiting tissue proliferation.Type: GrantFiled: January 22, 2002Date of Patent: September 21, 2004Assignee: Warner-Lambert CompanyInventors: Armen M. Boldi, Elaine B. Krueger, Michael A. Walters, Thutam P. Hopkins, Meghan T. Keaney
-
Patent number: 6759523Abstract: The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.Type: GrantFiled: November 30, 2000Date of Patent: July 6, 2004Assignee: ISIS Pharmaceuticals, Inc.Inventors: Eric Swayze, Richard H. Griffey, Yili Ding, Venkatraman Mohan
-
Patent number: 6756208Abstract: The present invention has determined that exogenously added glycosylceramide (GlcCer) and other neutral glycolipids such as the homologous Glc-containing globotriaosylceramide (Gb3Cer), dose-dependently prolonged clotting times of normal plasma in the presence but not absence of APC:protein S, indicating GlcCer or Gb3Cer can enhance protein C pathway anticoagulant activity. In studies using purified proteins, inactivation of factor Va by APC:protein S was enhanced by GlcCer alone and by GlcCer, globotriaosylceramide, lactosylceramide, and galactosylceramide in multicomponent vesicles containing phosphatidylserine and phosphatidylcholine. Thus, the present invention provides neutral glycolipids such as GlcCer and Gb3Cer, as anticoagulant cofactors that contribute to the antithrombotic activity of the protein C pathway. The present invention has also determined that a deficiency of plasma GlcCer is a risk factor for thrombosis.Type: GrantFiled: February 28, 2002Date of Patent: June 29, 2004Inventors: John H. Griffin, Hiroshi Deguchi, Jose Fernandez
-
Patent number: 6747010Abstract: An objective of the present invention is to provide NKT cell-activating agents, therapeutic agents for autoimmune diseases (for example, systemic lupus erythematosus, systemic sclerosis, ulcerative colitis, encephalomyelitis, multiple sclerosis and human type I diabetes), and abortifacients. The medicinal compositions according to the present invention comprise &agr;-glycosylceramides of the following formula (I), or a salt or a solvate thereof as an active ingredient.Type: GrantFiled: January 2, 2003Date of Patent: June 8, 2004Assignee: Kirin Beer Kabushiki KaishaInventors: Masaru Taniguchi, Tetsu Kawano, Yasuhiko Koezuka
-
Patent number: 6737063Abstract: The present invention provides bacterial immunogenic agents for administration to humans and non-human animals to stimulate an immune response. Also provided are methods for vaccination of mammalian species, especially human patients, with variants of the E. coli FimH protein, said variants being derived from different strains of E. coli, and to production of antibodies that protect the vaccine recipient against infection by pathogenic bacterial species. In another aspect the invention provides antibodies against such proteins and protein complexes that may be used as diagnostics and/or as protective/treatment agents for pathogenic bacterial species. A plasmid-based method of producing polypeptides, especially fused polypeptides, such as the complex of a bacterial chaperone and a bacterial adhesin, is also disclosed.Type: GrantFiled: July 6, 2001Date of Patent: May 18, 2004Assignee: MedImmune, Inc.Inventors: Solomon Langermann, Andrew Revel, Christine Auguste, Jeanne Burlein
-
Patent number: 6683063Abstract: The invention provides methods of preventing and treating pulmonary bacterial infection or symptomatic pulmonary exposure to endotoxin and related conditions in a patient by administering to the patient antiendotoxin compounds by inhalation.Type: GrantFiled: June 11, 2002Date of Patent: January 27, 2004Assignee: Eisai Co., Ltd.Inventors: Daniel P. Rossignol, Mary W. Vermeulen
-
Patent number: 6683056Abstract: wherein when Y is or heteroaryl; A is —O(CH2)m, S, —NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.Type: GrantFiled: February 23, 2001Date of Patent: January 27, 2004Assignee: Bristol-Myers Squibb CompanyInventors: William N. Washburn, Philip M. Sher, Gang Wu
-
Patent number: 6664243Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1-R13 are as defined herein.Type: GrantFiled: November 22, 1999Date of Patent: December 16, 2003Assignee: WyethInventor: Scott C. Mayer
-
Patent number: RE38723Abstract: The subject invention provides substrates useful for analyzing the metabolic activity in cells by improving the retention of a detectable reporter molecule only in intact cells where a particular enzyme is present. In particular, improved retention results from a two part process involving conjugation of haloalkyl-substituted derivatives of a reporter molecule with intracellular cysteine-containing peptides while unblocking the reporter molecule. The substrates have the form XR-SPACER-REPORTER-BLOCK wherein -BLOCK is a group selected to be removable by action of a specific analyte, to give REPORTER spectral properties different from those of the substrate, -REPORTER- is a molecule that, when no longer bound to BLOCK by a BLOCK-REPORTER bond, has spectral properties different from those of the substrate, -SPACER- is a covalent linkage, and XR- is a haloalkyl moiety that can covalently react with an intracellular thiol (Z-S-H) to form a thioether conjugate (Z-S-R).Type: GrantFiled: August 12, 1997Date of Patent: April 12, 2005Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Ram Sabnis, John Naleway, Nels Olson, Richard P. Haugland
-
Patent number: RE39245Abstract: The present invention relates to simplified synthesis, new carbohydrate-based products and practical use of different carbohydrate-based products. Examples of these are (Gal?1-3Gal), GlcNAc?1-3Gal, ?- or ?-glycosides thereof, Gal?1-3Gal- containing tri-, or higher oligosaccharides, ?- or ?-glycosides thereof, GlcNAc?1-3Gal containing tri-, tetra-, or higher oligosaccharides, and derivatives and/or ?- or ?-glycosides thereof, Gal?1-3GalGlcNAc?1-3Gal, ?- or ?-glycosides thereof, Gal?1-3Gal?1-4GlcNAc?1-3Gal?1-4Glc, or other higher oligosaccharides containing the Gal?1-3Gal-structure, ?- or ?-glycosides thereof, modified carbohydrates, di-, tri-, oligo-, or polyfunctional products containing carbohydrate structures, and the use of the products for synthesis, affinity purification, diagnostic applications and therapy.Type: GrantFiled: December 23, 1996Date of Patent: August 22, 2006Assignee: Procur ABInventor: Kurt Nilsson