Nitrogen Or Sulfur In Aglycone Moiety Patents (Class 536/17.6)
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Patent number: 11993625Abstract: The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the same and to methods for using the same to treat pathological conditions such as cancer.Type: GrantFiled: January 10, 2018Date of Patent: May 28, 2024Assignee: Pfizer, Inc.Inventors: Omar Khaled Ahmad, Stephen Paul Brown, Kenneth John Dirico, Russell Dushin, Gary Frederick Filzen, Sujiet Puthenveetil, Pavel Strop, Chakrapani Subramanyam, Lawrence N. Tumey
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Patent number: 11925680Abstract: Neoglycoconjugates as immunogens and therapeutic/diagnostic tools are described herein. The neoglycoconjugates are produced by conjugating a carbohydrate antigen intermediate to a free amine group of a carrier material (e.g., carrier protein). The intermediate comprises a linker having a first end and a second end, the first end being conjugated to a carbohydrate antigen via a thio ether bond and the second end comprising a functional group reactable with a free amine group. Following coupling, the carbohydrate antigen becomes covalently bound to the carrier material via an amide, a carbamate, a sulfonamide, a urea, or a thiourea bond, thereby producing the neoglycoconjugate. Applications of the neoglycoconjugates as antigens, immunogens, vaccines, and in diagnostics are also described.Type: GrantFiled: September 18, 2020Date of Patent: March 12, 2024Assignee: Koranex CapitalInventors: Tze Chieh Shiao, Serge Moffett, Serge Mignani, Rene Roy
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Publication number: 20150148527Abstract: A sugar chain-containing polymer that enables targeting to the lesion area of liver fibrosis and is useful for imaging, diagnosis and therapy of liver fibrosis; and a sugar chain-containing polymer complex comprising the polymer as a carrier for an anionic substance useful fix therapy and the like; are provided. The polymer is a sugar chain-containing polymer which is a cationic polymer comprising an amine, which polymer comprises N-acetylglucosamine bound thereto. The polymer preferably has a disulfide bond. The polymer preferably has a structure in which polyethyleneimine is linked via a disulfide bond.Type: ApplicationFiled: May 27, 2014Publication date: May 28, 2015Applicants: SOMAR Corp., KOREAN RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Bong Hyun CHUNG, Hirohiko ISE, Toshihiro AKAIKE, Sun-Jung KIM
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Patent number: 9006468Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.Type: GrantFiled: January 25, 2012Date of Patent: April 14, 2015Assignee: Dow AgroSciences, LLC.Inventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, David A. Demeter, Kristy Bryan, Annette V. Brown, William H. Dent, III, Denise P. Cudworth, Jaime S. Nugent, Ricky Hunter, Jack G. Samaritoni
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Publication number: 20150045545Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbent according to the invention for the purification of organic molecules, in particular pharmaceutically active compounds, preferably in chromatographic applications.Type: ApplicationFiled: September 17, 2012Publication date: February 12, 2015Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
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Publication number: 20150005245Abstract: Sialic acid derivatives of the formula (I) in which the symbols have the definitions stated in the description are suitable as medicaments, more particularly for diseases whose course is influenced by Siglec ligands.Type: ApplicationFiled: December 21, 2012Publication date: January 1, 2015Inventors: Reinhard Brossmer, Horst Prescher
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Patent number: 8871726Abstract: The present invention relates to a C-aryl glucoside derivative of Formula (I) below, a preparation method therefor and a use thereof, wherein X, R1, R2, R3, R4, m and n are as defined in specification. The derivative of the present invention is a sodium-glucose co-transporter 2 (SGLT-2) inhibitor associated with glucose reabsorption of bowel or kidney, and has a good urine glucose excreting effect, thus being useful as a therapeutic agent for treating diabetes and related diseases.Type: GrantFiled: October 27, 2011Date of Patent: October 28, 2014Assignee: Shanghai Allist Pharmaceuticals, Inc.Inventor: Huibing Luo
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Publication number: 20140309178Abstract: Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula: the various substituents of which are defined herein.Type: ApplicationFiled: November 18, 2013Publication date: October 16, 2014Applicant: LEXICON PHARMACEUTICALS, INC.Inventors: Kenneth Gordon CARSON, Nicole Cathleen GOODWIN, Bryce Alden HARRISON, David Brent RAWLINS, Eric STROBEL, Brian ZAMBROWICZ
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Publication number: 20140295566Abstract: A novel ligand conjugate which is effectively utilizable for analyzing a function of a protein; a ligand-supporting object; and a method of analyzing a protein. The ligand conjugate has a structure which comprises: a linker compound having a structure represented by the following General Formula (1): (wherein n and p each is an integer of 0 to 6) in which X is a structure comprising one, two, or three hydrocarbon derivative chains which have an aromatic amino group at the end and may have a carbon-nitrogen bond in the main chain, Y is a hydro-carbon structure containing one or more sulfur atoms, and Z is a straight-chain structure comprising a carbon-carbon bond or carbon-oxygen bond; and a sugar which has a reducing end and is bonded to the linker compound through the aromatic amino group.Type: ApplicationFiled: May 9, 2014Publication date: October 2, 2014Applicants: Japan Science and Technology Agency, National University Corporation Kagoshima UniversityInventor: Yasuo SUDA
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Publication number: 20140255374Abstract: Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of autoimmune disease, inflammatory disease, or cancer. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.Type: ApplicationFiled: November 6, 2013Publication date: September 11, 2014Applicant: CERULEAN PHARMA INC.Inventor: Scott Eliasof
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Patent number: 8828952Abstract: The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.Type: GrantFiled: October 16, 2008Date of Patent: September 9, 2014Assignee: Progen Pharmaceuticals LimitedInventors: Vito Ferro, Tomislav Karoli, Ligong Liu, Paul Newton Handley, Kenneth David Johnstone, Norbert Wimmer, Edward Timothy Hammond
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Patent number: 8796229Abstract: Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.Type: GrantFiled: August 31, 2011Date of Patent: August 5, 2014Assignee: University of Georgia Research Foundation, Inc.Inventors: Geert-Jan Boons, Jun Guo
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Publication number: 20140171630Abstract: Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3?-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.Type: ApplicationFiled: February 20, 2014Publication date: June 19, 2014Applicant: GALECTO BIOTECH ABInventor: Ulf NILSSON
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Patent number: 8742080Abstract: A process for the preparation of compounds having formula (I) is disclosed, wherein: —R1 is a methoxy or methylthio group; —R2 is a O-glycosyloxy residue. Compounds having formula (I) are prepared by reacting the corresponding precursor having R2?OH and the suitably protected 1-acetyl-glycose.Type: GrantFiled: April 9, 2009Date of Patent: June 3, 2014Assignee: Indena S.p.A.Inventors: Stephen Beszant, Bruno Gabetta
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Patent number: 8709747Abstract: The invention relates to compounds of formula (I) wherein the groups A and B represent independently from each other —CH?CH—, or —C?C—, the terms t, u, v, w represent, independently from each other, values ranging from 0 to 9, the groups Y1 and Y2 can represent independently from each other an alkyl group (linear, branched or substituted) carrying from 1 to 9 carbon atoms, the groups Z1, Z2, Z3, and Z4 can represent independently from each other a chemically reactive group W, such as OH, NH2, SH, the groups Z5 and Z6 represent independently from each other a hydrogen atom, silica nanoparticles functionalized by these compounds, and their use as drugs.Type: GrantFiled: December 7, 2010Date of Patent: April 29, 2014Assignees: Centre National de la Recherche Scientifique, Universite de Rennes 1, I.N.S.E.R.M. (Institut National de la Sante et de la Recherche Medicale), Universite Montpellier 2 Sciences et TechniquesInventors: David Brevet, Laurence Raehm, Mireille Blanchard-Desce, Olivier Mongin, Magali Gary-Bobo-Sable-Teychene, Marcel Garcia, Alain Morere, Jean-Olivier Durand
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Publication number: 20140031533Abstract: A precursor used for labeling hepatocyte receptors and applied to radiotracers for imaging or pharmaceutical compositions for liver cancers is revealed. The precursor is a bifunctional compound. The bifunctional group includes a trisaccharide structure and a diamide dimercaptide (N2S2) ligand. The trisaccharide has high affinity to asialoglycoprotein receptors (ASGPR) on surfaces of hepatocytes while N2S2 ligand reacts with radioisotopes to form neutral complexes. Thus the precursor stays on surfaces of hepatocytes to provide radioisotope labeling or treatment effect of liver cancers.Type: ApplicationFiled: July 24, 2012Publication date: January 30, 2014Applicant: ATOMIC ENERGY COUNCIL, INSTITUTE OF NUCLEAR ENERGY RESEARCHInventors: SHOW-WEN LIU, YU CHANG, CHENG-FANG HSU, MING-CHE TSAI, TSUNG-HSIEN CHIANG, YUEH-FENG DENG, KUEI-LIN LU, CHIH-YUAN LIN, DA-MING WANG, CHING-YUN LI
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Publication number: 20140024608Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: March 14, 2013Publication date: January 23, 2014Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Publication number: 20130288986Abstract: Described herein is a cyclodextrin containing polymer conjugate.Type: ApplicationFiled: June 20, 2013Publication date: October 31, 2013Inventors: Mark E. Davis, Jungyeon Hwang, Tianyi Ke, Ching-jou Lim, Thomas Schluep
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Patent number: 8536153Abstract: The efficient synthesis of phosphatidylinositol mono- to hexa-mannoside (PIM1 to PIM6) is reported. The invention relates to these phosphatidylinositol mono- to hexa-mannosides carrying a linker and a reactive functional group, e.g. the sulfhydryl group, a protein, a fluorescent probe, or a solid phase. The invention further relates to vaccines comprising the PIMs linked to a carrier protein or an antigen.Type: GrantFiled: November 3, 2009Date of Patent: September 17, 2013Assignee: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.Inventors: Peter H. Seeberger, Siwarutt Boonyarattanakalin, Bernd Lepenies
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Patent number: 8530448Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids, which include a portion or analogue thereof) linked to a carbohydrate or glycomimetic.Type: GrantFiled: April 2, 2010Date of Patent: September 10, 2013Assignee: Glycomimetics, Inc.Inventors: John L. Magnani, John T. Patton, Jr., Leonard M. Williams
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Patent number: 8476413Abstract: Sulfanyl-tetrahydropyran-based compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment of diseases and disorders such as diabetes and obesity are disclosed.Type: GrantFiled: August 18, 2010Date of Patent: July 2, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
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Patent number: 8450466Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: GrantFiled: March 23, 2009Date of Patent: May 28, 2013Assignees: The General Hosptial Corporation, Fluoropharma, Inc.Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Publication number: 20130116203Abstract: The present invention provides glucosinolate and isothiocyanate compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents.Type: ApplicationFiled: November 7, 2011Publication date: May 9, 2013Inventors: Scott R. Rajski, Jared Rae Mays
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Publication number: 20130065849Abstract: The invention relates to compounds of formula (I) wherein the groups A and B represent independently from each other —CH?CH—, or —C?C—, the terms t, u, v, w represent, independently from each other, values ranging from 0 to 9, the groups Y1 and Y2 can represent independently from each other an alkyl group (linear, branched or substituted) carrying from 1 to 9 carbon atoms, the groups Z1, Z2, Z3, and Z4 can represent independently from each other a chemically reactive group W, such as OH, NH2, SH, the groups Z5 and Z6 represent independently from each other a hydrogen atom, silica nanoparticles functionalized by these compounds, and their use as drugs.Type: ApplicationFiled: December 7, 2010Publication date: March 14, 2013Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, UNIVERSITE DE RENNES 1Inventors: David Brevet, Laurence Raehm, Mireille Blanchard-Desce, Olivier Mongin, Magali Gary-Bobo-Sable-Teychene, Marcel Garcia, Alain Morere, Jean-Olivier Durand
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Patent number: 8394774Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.Type: GrantFiled: February 11, 2010Date of Patent: March 12, 2013Assignee: Dow AgroSciences, LLC.Inventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Annette V. Brown, Thomas L. Siddall
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Publication number: 20130035479Abstract: The present invention relates to a novel process for the chemical synthesis of ?-(1->6)-linked glucosamine disaccharides of the formula (1) and (intermediate) compounds relating to the process. According to further aspects the invention relates to compositions comprising the compounds and the use of the compounds in the synthesis of disaccharides and medicine.Type: ApplicationFiled: October 1, 2012Publication date: February 7, 2013Applicant: OM PHARMAInventor: OM PHARMA
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Publication number: 20130030162Abstract: A new process for extracting and purifying glucosinolates from plant material, preferably broccoli sprouts or seeds is described. An alcoholic extract is adsorbed onto a basic resin and eluted with ammonia. Optionally, the alcoholic extract is passed through an ion-exchange column containing acidic resin prior to the adsorption/elution step.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: DSM IP ASSETS B.V.Inventors: Christof WEHRLI, Jan SCHUTZ
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Publication number: 20120263735Abstract: The present invention refers to compounds of formula (I) as useful melanoma vaccines' active ingredients. As a matter of fact, compounds of formula (I) are immunogenic artificial antigens, mimetics of GM3 and GM3 lactone, well known tumor associated antigens (TAAs). In addition, the present invention refers to specific antibodies for compounds of formula (I) which are able to bind to the TAAs. The hereinabove reported compounds and antibodies are therefore potentially useful respectively for the active and passive immunization against tumors overexpressing GM3 ganglioside, in a preferred embodiment melanoma and colon cancer, and for their diagnosis and prognosis.Type: ApplicationFiled: November 4, 2010Publication date: October 18, 2012Applicant: AZIENDA OSPEDALIERO-UNIVERSITARIA CAREGGI (Italian Hospital)Inventors: Cristina Nativi, Lucio Toma, Barbara Richichi, Carlotta Lunghi
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Publication number: 20120258043Abstract: Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.Type: ApplicationFiled: April 26, 2012Publication date: October 11, 2012Applicant: BRACCO SUISSE S.A.Inventors: Ramachandran RANGANATHAN, Kondareddiar RAMALINGAM, Radhakrishna PILLAI, Edmund R. MARINELLI, Rolf E. SWENSON
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Patent number: 8222381Abstract: New compounds and methods for the preparation of combinatorial libraries of potentially biologically active compounds are based on monosaccharides of formula I being a derivative of a furanose or pyranose form of a monosaccharide, .Type: GrantFiled: August 8, 2003Date of Patent: July 17, 2012Assignee: Alchemia LimitedInventors: Michael West, Peter Andrews, Tracie Elizabeth Ramsdale, Wim Meutermans, Giang Thanh Le, Chris Clark, Giovanni Abbenante, Ligong Liu
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Publication number: 20120165277Abstract: Compounds having an effect as i.a. galectin inhibitors, to the use of said compounds as a medicament, as well as for the manufacture of a medicament for treatment of disorders relating to the binding of galectin to receptors in a mammal, where in the galectin is preferably a galectin-3.Type: ApplicationFiled: April 26, 2010Publication date: June 28, 2012Applicant: FORSKARPATENT I SYD ABInventors: Hakon Leffler, Ulf J. Nilsson, Henrik Von Wachenfeldt
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Publication number: 20120165283Abstract: This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.Type: ApplicationFiled: March 7, 2012Publication date: June 28, 2012Inventors: Yoshihiko Kobayashi, Yoshihisa Akiyama, Takeshi Murakami, Nobuto Minowa, Masaki Tsushima, Yukiko Hiraiwa, Shoichi Murakami, Mitsuhiro Abe, Kazushige Sasaki, Shigeru Hoshiko, Toshiaki Miyake, Yoshiaki Takahashi, Daishiro Ikeda
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Publication number: 20120137929Abstract: There is provided a gallotannic compound, a method of producing a gallotannic compound, a lithographic printing plate coating composition, a lithographic printing plate, a method of producing a lithographic printing plate and a method of printing.Type: ApplicationFiled: June 11, 2010Publication date: June 7, 2012Applicant: MYLAN GROUPInventors: My T Nguyen, A. Kha Phan, Quoc Khoi Nguyen, Marc-André Locas
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Patent number: 8173606Abstract: The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.Type: GrantFiled: December 3, 2010Date of Patent: May 8, 2012Assignee: Progen Pharmaceuticals LimitedInventors: Vito Ferro, Jon Krueger Fairweather, Tomislav Karoli, Ligong Liu
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Patent number: 8173797Abstract: The present invention is directed to new therapeutic compounds isolated from spider venom and methods of using these new compounds. The compounds are sulfated nucleoside derivatives including ribonucleoside mono- and disulfates derived from guanine, adenosine, and cytidine. Some of these compounds are glycosylated or fucosylated bearing one or more sugar residues.Type: GrantFiled: July 21, 2005Date of Patent: May 8, 2012Assignee: Cornell Research Foundation, Inc.Inventors: Jerrold Meinwald, Andrew Edmund Taggi, Frank Clemens Schroeder
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Publication number: 20120058960Abstract: Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.Type: ApplicationFiled: August 31, 2011Publication date: March 8, 2012Applicant: University of Georgia Research Foundation, Inc.Inventors: Geert-Jan BOONS, Jun Guo
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Publication number: 20120045390Abstract: The present invention is directed to compositions of matter useful for the diagnosis and treatment of tumor in mammals and to methods of using those compositions of matter for the same.Type: ApplicationFiled: September 5, 2003Publication date: February 23, 2012Applicant: Genentech, Inc.Inventors: Frederic J. DeSauvage, William I. Wood, Zemin Zhang
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Publication number: 20120009669Abstract: A bifunctional compound with a monosaccharide and a N2S2 ligand, and more particularly, a bifunctional compound with a N2S2 ligand and aminohexylacetyl galactosamine (ah-GalNAc4) is provided. A method for preparing the bifunctional compound with a monosaccharide and a N2S2 ligand is also provided, including activating a carboxyl group in an organic ligand, reacting the activated carboxyl group with a galactopyranoside through amidation, and then hydrolyzing. The bifunctional compound of the present invention is widely useful in nuclear medicine for preparation of liver imaging agents for assisting in correct diagnosis of diseases.Type: ApplicationFiled: April 15, 2011Publication date: January 12, 2012Applicant: Institute of Nuclear Energy Research Atomic Energy Council, Executive YuanInventors: SHOW-WEN LIU, CHENG-HSIEN LIN, YU CHANG, CHENG-FANG HSU, TSYH-LANG LIN
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Patent number: 8044029Abstract: Disclosed herein are methods for the treatment of autoimmune or immune related diseases or disorders. Also disclosed are methods for treating such autoimmune or immune related diseases or disorders with the administration of sulfatides. Also disclosed herein are methods of treating autoimmune or immune related diseases or disorders by administering an amount of a sulfatide to the body of a patient effective to reduce or prevent the symptoms of the autoimmune or immune related disease or disorder.Type: GrantFiled: September 28, 2006Date of Patent: October 25, 2011Assignee: Torrey Pines Institute for Molecular StudiesInventor: Vipin Kumar Chaturvedi
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Publication number: 20110224156Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: March 8, 2011Publication date: September 15, 2011Inventors: Mark A. Wolf, Keith D. Barnes
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Publication number: 20110190227Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists Of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: July 2, 2009Publication date: August 4, 2011Applicant: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns, Jeffrey Roger Roppe
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Publication number: 20110130354Abstract: The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.Type: ApplicationFiled: December 3, 2010Publication date: June 2, 2011Applicant: Progen Pharmaceuticals LimitedInventors: Vito Ferro, Jon Krueger Fairweather, Tomislav Karoli, Ligong Liu
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Publication number: 20110130554Abstract: A process for the preparation of compounds having formula (I) is disclosed, wherein: —R1 is a methoxy or methylthio group; —R2 is a O-glycosyloxy residue. Compounds having formula (I) are prepared by reacting the corresponding precursor having R2=OH and the suitably protected 1-acetyl-glycose.Type: ApplicationFiled: April 9, 2009Publication date: June 2, 2011Applicant: INDENA S.P.A.Inventors: Stephen Beszant, Bruno Gabetta
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Publication number: 20110130553Abstract: Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3?-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.Type: ApplicationFiled: May 18, 2009Publication date: June 2, 2011Inventor: Ulf Nilsson
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Publication number: 20110028702Abstract: 13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthrcyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines to 13-deoxyanthrcyclines wherein the reduction reaction is maintained at temperatures of about 55° C. to 64° C. without stirring or agitation. The reaction is completed with the addition of aqueous bicarbonate which forms the 13-deoxyanthracycline and precipitates. The precipitates are filtered and the precipitate and filtrate are extracted separately with organic solvents. The crude 13-deoxy anthracycline can be converted to 5-imino-13-deoxy anthracycline by reaction with methanolic ammonia. The reaction can also be performed with an acidic pyridinium salt instead of a strong acid so that neutralization of the reaction or extraction of the product is not necessary, thereby facilitating purification.Type: ApplicationFiled: August 5, 2010Publication date: February 3, 2011Applicant: Gem Pharmaceuticals, LLCInventors: Gerald M. Walsh, Richard D. Olson
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Publication number: 20100279958Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids, which include a portion or analogue thereof) linked to a carbohydrate or glycomimetic.Type: ApplicationFiled: April 2, 2010Publication date: November 4, 2010Applicant: GlycoMimetics, Inc.Inventors: John L. MAGNANI, John T. Patton, JR., Leonard M. Williams
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Publication number: 20100240878Abstract: The present invention relates to improved fluorescently labeled monosaccharide and low molecular weight oligosaccharide conjugates for immunofluorescent staining, confocal microscopic imaging and flow cytometry/fluorescence activated cell sorting (FACS). These fluorophore conjugates target cells, components of cell surfaces and extracellular components; and are useful as probes for tumor targeting and cellular uptake.Type: ApplicationFiled: March 20, 2009Publication date: September 23, 2010Inventor: Donald L. Barbeau
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Publication number: 20100221358Abstract: The invention relates to novel synthetic derivatives of ?-glycolipids and uses thereof as immunomodulators. More particularly, the invention relates to synthetic derivatives of ?-glycolipids, specifically, the compounds of any one of Formula I, II III and IV or any mixture or combination thereof, and particularly the ALIB-97 (Formula II) derivative and uses thereof for the treatment of different pathologic disorders, particularly, immune-related hepatic disorders and pathologies associated with the metabolic syndrome.Type: ApplicationFiled: October 13, 2009Publication date: September 2, 2010Inventors: Yaron Ilan, Arie Dagan
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Patent number: 7772430Abstract: Described herein are derivatives of arylsulfonamido-substituted hydroxamic acid of formula (I) having good solubility in water and inhibitory activity of matrix metalloproteinases, useful for the preparation of pharmaceutical compositions for the treatment of diseases associated to a pathologic activity and/or an over-expression of metalloproteinases, and of cosmetic preparations having anti-ageing properties in particular for hair and skin.Type: GrantFiled: July 29, 2005Date of Patent: August 10, 2010Assignee: Protera S.R.L.Inventors: Ivano Bertini, Marco Fragai, Mauro Lo Conte, Claudio Luchinat, Cristina Nativi, Chiara Venturi
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Publication number: 20100184607Abstract: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.Type: ApplicationFiled: August 1, 2008Publication date: July 22, 2010Applicant: Alchemia Pty Ltd.Inventors: Michael Leo West, Wim Meutermans, George Adamson, Karl Schafer, Darren Schliers