Nitrogen In Aglycone Moiety Patents (Class 536/17.4)
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Publication number: 20110251148Abstract: Compounds, compositions and methods are provided for use to inhibit infection by human immunodeficiency virus (HIV). More specifically, the present invention relates to glycomimetic compounds that inhibit HIV infection, and uses thereof.Type: ApplicationFiled: April 6, 2011Publication date: October 13, 2011Applicant: GlycoMimetics, Inc.Inventors: John L. MAGNANI, Arun K. Sarkar
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Patent number: 8030459Abstract: The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for creating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. The present invention also relates to chiral polyketals, methods for their preparation, and methods for use in chromatographic applications, specifically in chiral separations.Type: GrantFiled: July 18, 2003Date of Patent: October 4, 2011Assignee: The General Hospital CorporationInventors: Mikhail I. Papisov, Alexander Yurkovetskiy
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Patent number: 8022192Abstract: The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R1, R2, R3, R4 and R5 may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R6 is an alkyl group, for example R7 is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PG1 is a pivaloyl group or the like, as an example, X1 is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.Type: GrantFiled: March 16, 2006Date of Patent: September 20, 2011Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kiyoshi Kasai, Tetsuji Ozawa, Nobuhiko Fushimi, Hidetoshi Isawa, Ken Kikuchi, Masahiro Kobayashi, Junichi Sonehara, Minoru Kubota
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Publication number: 20110224413Abstract: Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives and pyrazole intermediates of the same. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes and intermediates for preparing the same.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Michael Tolar Martin, Michael S. McClure, Vassil Elitzin
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Publication number: 20110218160Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20110206613Abstract: Biologically active compounds are provided that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, ophthalmological or urological disorders as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso-substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed.Type: ApplicationFiled: September 17, 2009Publication date: August 25, 2011Inventors: Arno Wiehe, Daniel Aicher, Christian B .W. Stark, Volker Albrechi, Susanna Gräfe
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Patent number: 8003615Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R1 represents a glycosyl group, a phosphate group, or a cyclic phosphate group bound to R2; R2 represents —CH2OH, —CHO, —CH2NH2, —CH2-amino acid residue, or —CH2—OPO2H; and R3 represents hydrogen atom, or —PO3H2, and a composition for cosmetics, medicaments, foodstuffs, and/or feeds containing the aforementioned compound or a salt thereof.Type: GrantFiled: September 30, 2004Date of Patent: August 23, 2011Assignee: Daiichi Fine Chemical Co., Ltd.Inventors: Keiji Sakamoto, Koichi Wada, Hajime Ito, Nobuhiro Take, Hiroshi Morimoto, Fumio Maniwa, Yukiko Shimmoto
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Publication number: 20110201793Abstract: The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R1, R2, R3, R4 and R5 may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R6 is an alkyl group, for example R7 is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PG1 is a pivaloyl group or the like, as an example, X1 is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.Type: ApplicationFiled: April 25, 2011Publication date: August 18, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kiyoshi KASAI, Tetsuji OZAWA, Nobuhiko FUSHIMI, Hidetoshi ISAWA, Ken KIKUCHI, Masahiro KOBAYASHI, Junichi SONEHARA, Minoru KUBOTA
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Patent number: 7998935Abstract: The present invention provides quinaldine-based semisquaraines, symmetrical and unsymmetrical squaraine dyes represented by the general formulae 1, 2 and 3 and/or pharmaceutically acceptable derivatives thereof as sensitizers for photodynamic therapeutical and industrial applications. These symmetrical and unsymmetrical squaraine dyes posses absorption which extends well into the photodynamic window (650-800 nm) and hence are useful for the treatment of deep seated tumors. The absorption of these dyes can be tuned by changing the substituents on the quinaldine moiety thereby enabling the development of a library of dyes which have absorption ranging from 650 to 800 nm. They also exhibited fluorescence emission in the long wavelength region making them useful as near infrared fluorescence sensors for the detection of tumors. These dyes are non-toxic in the dark and exhibit good photocytotoxicity.Type: GrantFiled: January 8, 2007Date of Patent: August 16, 2011Assignee: Council of Scientific and Industrial ResearchInventors: Danaboyina Ramaiah, Jyothish Kuthanapillil, Kalliat Thazhathveetil Arun
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Publication number: 20110189655Abstract: The present invention relates to reagents and methods for influenza virus detection. These reagents and methods disclosed in the present invention enable simple, rapid, specific and sensitive detection of influenza virus types A and B. These reagents are N-acetylneuraminic acid-firefly luciferin conjugates which can be cleaved by influenza virus neuraminidase.Type: ApplicationFiled: February 2, 2011Publication date: August 4, 2011Inventors: Xing Xiang Li, Tianxin Wang
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Publication number: 20110190226Abstract: The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4?-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.Type: ApplicationFiled: November 10, 2008Publication date: August 4, 2011Inventors: Bao-Han C. Vu, Maqbool A. Siddiqui, Victor E. Marquez, Stephen H. Hughes
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Publication number: 20110166088Abstract: The present invention provides Gyrase B and/or Topoisomerase IV par E inhibitors, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonas spp., Acenetobacter spp., Moraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Ktycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Corynebacterium, Bacillus spp., Enterobactericeae,’ (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: June 25, 2009Publication date: July 7, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Jitendra A. Sattigeri, Naresh Kumar, Ajay Yadav, Lalima Sharma, Ian A. Cliffe, Shibu B. Varughese, Shaikh Rizwan Shabbir, V. Samuel Raj, Dilip J. Upadhyay, Pradip K. Bhatnager
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Publication number: 20110135713Abstract: The present invention provides protonated compounds having antiviral and antimicrobial activity. The invention also provides antimicrobial compositions comprising protonated compounds of the invention. The protonated compounds of the invention provide efficacious antimicrobial activity against resistant strains of bacteria and opportunistic fungi. The invention also provides antiviral compositions comprising compounds of the invention. Viruses that may be treated by compositions of the invention include, but are not limited to, HIV, HSV, CMV, HBV, HCV and influenza virus.Type: ApplicationFiled: January 6, 2011Publication date: June 9, 2011Applicant: Lakewood-Amedex, Inc.Inventor: Roderic M.K. Dale
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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: 20110117009Abstract: The present invention relates to a drug polymer conjugate comprising a pharmaceutically active compound and a dendritic polyglycerol, as well as to a drug polymer conjugate comprising a pharmaceutically and/or diagnostically active compound bound to a dendritic polyglycerol core having a polyethylene glycol shell.Type: ApplicationFiled: March 31, 2009Publication date: May 19, 2011Applicants: FREIE UNIVERSITÄT BERLIN, KTB TUMORFORSCHUNGSGESELLSCHAFT MBHInventors: Felix Kratz, Rainer Haag, Marcelo Calderon
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Publication number: 20110097753Abstract: The present invention relates to chemiluminescent method and regent to detect analyte. One aspect of the current invention relates to using enzyme substrate that can be cleaved by target enzyme to release chemiluminescent compound giving light signal for the detection of varieties of target enzymes. Another aspect of the current invention relates to use chemiluminescent enzyme coupled with analyte binding molecules to detect specific analyte molecules in a homogenous phase.Type: ApplicationFiled: October 15, 2008Publication date: April 28, 2011Inventors: Tianxin Wang, Xing Xiang Li
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Patent number: 7932236Abstract: Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection is also described.Type: GrantFiled: November 3, 2005Date of Patent: April 26, 2011Assignee: Seneb Biosciences, Inc.Inventors: Shawn DeFrees, Zhi-Guang Wang
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Publication number: 20110086810Abstract: The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.Type: ApplicationFiled: October 8, 2010Publication date: April 14, 2011Applicant: INCYTE CORPORATIONInventors: James D. RODGERS, Adam SHILLING, Argyrios G. ARVANITIS, Stacey SHEPARD, Laurine G. GALYA, Mei LI, Frank M. NEDZA
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Publication number: 20110086053Abstract: This invention relates to immunogenic compounds which serve as ligands for NKT (natural killer T) cells and to methods of use thereof in modulating immune responses.Type: ApplicationFiled: December 2, 2010Publication date: April 14, 2011Applicants: THE ROCKEFELLER UNIVERSITY, THE SCRIPPS RESEARCH INSTITUTEInventors: Moriya Tsuji, David D. Ho, Chi-Huey Wong, Douglass Wu, Masakazu Fujio, Xiangming Li
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Publication number: 20110071097Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.Type: ApplicationFiled: March 3, 2009Publication date: March 24, 2011Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: David Gin, Jeremy Wilmot, Hakim Djaballah
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Publication number: 20110059022Abstract: Disclosed herein are compounds useful as two-photon tracers. Also, methods are provided for visualizing intracellular glucose uptake, screening anticancer agents, and diagnosing cancer using the compounds. They exhibit preferential uptake by cancer cells, penetrability sufficient to allow bright section images, high water solubility, high pH resistance and low toxicity in addition to applicability to living cells in deep tissues over a long period of time.Type: ApplicationFiled: September 7, 2010Publication date: March 10, 2011Applicant: SNU R&DB FOUNDATIONInventors: Seung Bum PARK, Bong Rae CHO, Hyang Yeon LEE, Jong Min PARK
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Publication number: 20110059477Abstract: Disclosed are a novel fluorescent glucose analogue, a method for the synthesis thereof and the use thereof. The novel fluorescent glucose analogue is labeled with fluorescent dye by O-1-glycosylation and via various linkers. The fluorescent glucose analogue can be applied to molecular bioimaging and a method for screening curative or preventive drugs for glucose metabolism-related diseases.Type: ApplicationFiled: September 7, 2010Publication date: March 10, 2011Applicant: SNU R&DB FOUNDATIONInventors: Seung Bum PARK, Hyang Yeon LEE, Jong Min PARK
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Publication number: 20110053873Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: January 30, 2009Publication date: March 3, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Young K. Chen, Eric Wang Co, Prasuna Guntupalli, John David Lawson, Wolfgang Reinhard Ludwig Notz, Jeffrey A. Stafford, Huong-Thu Ton-Nu
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Publication number: 20110046003Abstract: A novel N-acetyl-5-N,4-O-carbonyl-protected dibutyl sialyl phosphate donor for sialylation of both primary and sterically hindered secondary acceptors to prepare sialosides with high yield and ?-selectivity is disclosed. Methods for making disaccharide building blocks comprising ?(2?3), ?(2?6), ?(2?8), ?(2?8)/?(2?9) alternate, and ?(2?9) sialosides are provided. methods for one-pot synthesis of complex sialosides are disclosed. Libraries of sialosides and methods for using the libraries for detection and receptor binding analysis of surface glycoproteins or pathogens and cancer cells are disclosed. Methods for distinguishing between hemagglutinin (HA) from various strains of influenza are provided.Type: ApplicationFiled: March 29, 2010Publication date: February 24, 2011Applicant: ACADEMIA SINICAInventors: Chi-Huey Wong, Chung-Yi Wu, Ting-Jen R. Cheng
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Publication number: 20110038952Abstract: This invention relates with the gambogic acid glycoside derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: X1, X2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted glycosyl, optionally substituted multi-hydroxyl, optional substituent oxy, optional substituent containing carbon, oxygen, sulfur, nitrogen or phosphorus element. Compounds of the present invention are useful as therapeutically effective agents of anti-cancer, anti-virus and anti-bacterial. This invention also relates with their preparative methods and applications.Type: ApplicationFiled: September 26, 2008Publication date: February 17, 2011Inventor: Lifeng Xu
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Publication number: 20110034404Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:Type: ApplicationFiled: October 13, 2010Publication date: February 10, 2011Inventors: Kimihiko GOTO, Ryo Horikoshi, Mariko Tsuchida, Kazuhiko Oyama, Satoshi Omura, Hiroshi Tomoda, Toshiaki Sunazuka
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Publication number: 20110034679Abstract: The present invention provides a novel form of 3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.Type: ApplicationFiled: April 13, 2009Publication date: February 10, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Hideki Takeuchi, Eiji Tsuru
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Publication number: 20110021765Abstract: The invention provides a paramagnetic lanthanide (III) complex comprising a lanthanide (III) ion and a polydentate ligand wherein the polydentate ligand comprises one or more fluorine atoms in which the distance of at least. one of the fluorine atoms to the lanthanide ion is less than 7, said polydentate ligand not being a DPTA bisamide of p-CF3-aniline.Type: ApplicationFiled: April 11, 2008Publication date: January 27, 2011Inventors: David Parker, Padma Kanthi Senanayake
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Patent number: 7863428Abstract: This invention relates to hydrolase fluorogenic substrates with improved cell permeability, methods for the preparation thereof, and methods of measuring activities of hydrolases, particularly in cell-based assays. The substrates easily diffuse into the cells, where they are enzymatically processed to yield photostable fluorescent products, and are particularly fitted for visualising enzyme-derived activities in cell-based assays.Type: GrantFiled: December 26, 2003Date of Patent: January 4, 2011Assignee: Tibotec BVBAInventors: Inge Dierynck, Jan Ludwig Goeman, Koenraad Lodewijk August Van Acker, Johan Theo André Van Der Eycken
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Publication number: 20100324274Abstract: Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described.Type: ApplicationFiled: July 6, 2010Publication date: December 23, 2010Inventors: Shawn DeFrees, Zhi-Guang Wang
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Patent number: 7842677Abstract: Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described.Type: GrantFiled: August 29, 2002Date of Patent: November 30, 2010Assignee: Seneb Biosciences, Inc.Inventors: Shawn DeFrees, Zhi Guang Wang
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Patent number: 7829542Abstract: Methods and compositions for treating or ameliorating diseases and other conditions, such as infectious diseases, autoimmune diseases and allergies are provided. The methods employ cyclic AGPs for selectively stimulating immune responses in animals and plants.Type: GrantFiled: May 30, 2008Date of Patent: November 9, 2010Assignee: Corixa CorporationInventors: Jory R. Baldridge, David A. Johnson, Christopher W. Cluff
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Publication number: 20100279965Abstract: Compounds, compositions and methods are provided for treating cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood. More specifically, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described.Type: ApplicationFiled: April 27, 2010Publication date: November 4, 2010Applicant: GlycoMimetics, Inc.Inventors: John L. Magnani, Arun K. Sarkar
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Publication number: 20100279962Abstract: The present invention provides a novel form of 3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since bis[3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide] monosebacate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.Type: ApplicationFiled: December 24, 2008Publication date: November 4, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Hideki Takeuchi, Eiji Tsuru
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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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Patent number: 7820627Abstract: The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.Type: GrantFiled: May 9, 2003Date of Patent: October 26, 2010Assignee: Oncothyreon Inc.Inventors: Zi-Hua Jiang, R. Rao Koganty, Wladyslaw Budzynski
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Patent number: 7820804Abstract: The invention relates to substituted fluoroglycoside derivatives of pyrazoles of formula (I) as further defined in the specification, to the physiologically compatible salts thereof, to a method for their production, and to their use as antidiabetics.Type: GrantFiled: December 6, 2006Date of Patent: October 26, 2010Assignee: Sanofi-Aventia Deutschland GmbHInventors: Harm Brummerhop, Wendeline Frick, Heiner Glombik, Oliver Plettenburg, Martin Bickel, Hubert Heuer, Stefan Theis
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Publication number: 20100261664Abstract: Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof The invention relates to substituted heterocyclic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation. The compounds are suitable for example as antidiabetics.Type: ApplicationFiled: May 25, 2010Publication date: October 14, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Wendelin FRICK, Heiner GLOMBIK, Werner KRAMER, Hubert HEUER, Harm BRUMMERHOP, Oliver PLETTENBURG
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Publication number: 20100256080Abstract: The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B), wherein R? represents and R? represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N—CO—O—, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene; in free form or in form of a pharmaceutically acceptable acid addition salt. Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.Type: ApplicationFiled: November 25, 2008Publication date: October 7, 2010Inventors: Ulrich Hassiepen, Matthias Kittelmann
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Publication number: 20100249049Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 7, 2010Publication date: September 30, 2010Inventors: Hiroshi MIYAZAKI, Junko TSUBAKIMOTO, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAL, Tetsuya YANAGIDA, Yataka HISADA
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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: 20100215574Abstract: The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.Type: ApplicationFiled: October 22, 2009Publication date: August 26, 2010Inventor: FELIX KRATZ
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Publication number: 20100204170Abstract: 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 particular glycomimetics alone or linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).Type: ApplicationFiled: April 20, 2010Publication date: August 12, 2010Applicant: GlycoMimetics, Inc.Inventors: John L. MAGNANI, John T. PATTON, JR., Arun K. SARKAR, Sergei A. SVAROVSKY, Beat ERNST
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Publication number: 20100204163Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is —H or —OCH3; R2 is —H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently —CH3, —C(O)H or —CH2OR6, wherein R6 is —H or a hydrocarbyl group having 1 to 20 carbon atoms. In some embodiments, compounds of Formula (I) exhibit selective affinity for ETA receptors and serve as endothelin receptor antagonists. In some embodiments, the compounds correspond to metabolites of ambrisentan produced by the enzymatic action of cytochrome P450 or uridine diphosphate glucuronosyl transferase enzymes, for example as elucidated in pre-clinical or clinical studies.Type: ApplicationFiled: July 31, 2008Publication date: August 12, 2010Applicant: Gilead Colorado, Inc.Inventors: Lawrence S. Melvin, JR., Martina Ullrich, Hans-Guenther Hege, Jürgen Weymann
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Publication number: 20100204164Abstract: 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: ApplicationFiled: February 11, 2010Publication date: August 12, 2010Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, David A. Demeter, Zoltan L. Benko, Debra L. Camper
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Publication number: 20100190158Abstract: The present invention relates to an in vitro method for detecting a target DNA sequence in cells using an oligonucleotide which is labelled with a beta-D-galactopyranoside which, on hydrolysis of the glycosidic linkage, forms a water-insoluble dye. The invention relates in particular to an in vitro method for detecting a target DNA sequence from a group of DNA sequences whose members differ from one another in exactly one predetermined nucleotide position, by using an oligonucleotide which is labelled with a beta-D-galactopyranoside which, on hydrolysis of the glycosidic linkage, forms a water-insoluble dye. The invention additionally relates to the use of such an oligonucleotide in DNA hybridization methods. The invention finally relates to kits for carrying out the above methods.Type: ApplicationFiled: December 12, 2007Publication date: July 29, 2010Inventors: Dieter Peitz, Martin Zentgraf
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Publication number: 20100190728Abstract: Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.Type: ApplicationFiled: May 31, 2005Publication date: July 29, 2010Applicant: Human Biomolecular Research InstituteInventors: John R. Cashman, James M. MacDougall
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Patent number: 7754694Abstract: The present invention provides pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrug of general formula 1a-b, useful as selective anticancer agents. The present invention also provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrugs of general formula 1a-b. This invention also provides activation of these prodrugs by E.coli ? galactosidase and envisaged that these molecules are toxic to human cancer cell lines in the presence of the enzyme E.coli ?-galactosidase. The prodrugs 1a and 1b were also found to be toxic to human cancer HepG2 cells even in the absence of the E.coli ?-galactosidase. The toxic effect of the molecules when activated was similar to that of the parent molecules 6a and 6b, respectively.Type: GrantFiled: January 16, 2008Date of Patent: July 13, 2010Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Venkatesh Tekumalla
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Patent number: 7749972Abstract: The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like. It is a 1-substituted-7-(?-D-glycopyranosyloxy)(aza)-indole compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof: wherein R1 represents a halogen atom or the like; n represents j an integer number from 0 to 3; R2 represents a hydrogen atom or the like; X represents a carbon atom which a hydrogen atom or the like binds to, or a nitrogen atom; Q represents an alkylene group or an alkenylene group each of which may have an oxygen atom or a sulfur atom in the chain; and A represents an aryl or heteroaryl group which may have a substituent.Type: GrantFiled: February 14, 2006Date of Patent: July 6, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Kohsuke Ohno
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Publication number: 20100167989Abstract: The present invention relates to new isopropoxyphenylmethyl inhibitors of SGLT2, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: October 23, 2009Publication date: July 1, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant