Nitrogen Attached Indirectly To The Phosphorus By Nonionic Bonding Patents (Class 558/190)
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Publication number: 20150133405Abstract: The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g.Type: ApplicationFiled: May 8, 2013Publication date: May 14, 2015Inventors: Marc F. Pelletier, George William Farr, Paul Robert Mcguirk, Christopher H. Hall, Walter F. Boron
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Patent number: 8999960Abstract: Novel oxidized thiophospholipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions. Exemplary oxidized thiophospholipid according to embodiments described herein have the formula: wherein X1, X2, A1, A2, B?, B?, D? and D? are as described herein.Type: GrantFiled: October 1, 2009Date of Patent: April 7, 2015Assignee: Vascular Biogenics Ltd.Inventors: Eyal Breitbart, Eti Kovalevski-Ishai, Erez Feige, Itzhak Mendel, Zeev Ziniuk, Gideon Halperin
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Publication number: 20150038466Abstract: The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.Type: ApplicationFiled: December 31, 2012Publication date: February 5, 2015Inventors: Sylvie Ducki, Khalil Bennis, Alain Eschalier, Jérôme Busserolles, Florian Lesage, Nuno Rodriguez, Delphine Vivier
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Publication number: 20140364398Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: PFIZER INC.Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
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Publication number: 20140303122Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: March 28, 2014Publication date: October 9, 2014Applicant: AJINOMOTO CO., INC.Inventors: Masayuki SUGIKI, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
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Patent number: 8796485Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 4, 2011Date of Patent: August 5, 2014Assignee: Ajinomoto Co., Inc.Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
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Patent number: 8518913Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: GrantFiled: December 9, 2011Date of Patent: August 27, 2013Assignee: Allergan, Inc.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8507710Abstract: The invention relates to pharmaceutical compositions comprising alkylphosphocholines and antimetabolite antitumor substances. The pharmaceutical compositions of the invention are useful for the treatment of benign and malignant oncoses in humans and animals. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.Type: GrantFiled: March 31, 2010Date of Patent: August 13, 2013Assignee: AEterna Zentaris GmbHInventors: Jurgen Engel, Eckhard Gunther, Herbert Sindermann
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Publication number: 20130102570Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.Type: ApplicationFiled: September 28, 2012Publication date: April 25, 2013Applicant: AJINOMOTO CO., INC.Inventor: AJINOMOTO CO., INC
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Publication number: 20130096092Abstract: Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.Type: ApplicationFiled: June 10, 2011Publication date: April 18, 2013Applicants: Health and Human ServicesInventors: Daniel Appella, Ettore Appella, John K. Inman, Lisa M. Miller Jenkins, Ryo Hayashi, Deyun Wang
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Patent number: 8383605Abstract: The invention relates to the use of alkylphosphocholines in combination with antimetabolites for the treatment of multiple myeloma, colon cancer or renal cancer. Preferred alkylphosphocholines are described by the Formula II. A particularly effective treatment includes administering a combination of perifosine and capecitabine.Type: GrantFiled: March 31, 2010Date of Patent: February 26, 2013Assignee: AEterna Zentaris GmbHInventors: Jürgen Engel, Eckhard Günther, Herbert Sindermann, Babette Aicher
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Publication number: 20120270842Abstract: The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.Type: ApplicationFiled: April 27, 2012Publication date: October 25, 2012Applicant: Metabasis Therapeutics, Inc.Inventors: K. RAJA REDDY, Jeff Stebbins, Serge H. Boyer, Mark D. Erion, Scott J. Hecker, Nicholas Brian Raffaele, Brett C. Bookser, Venkat Reddy Mali
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Patent number: 8283453Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.Type: GrantFiled: August 14, 2009Date of Patent: October 9, 2012Assignee: International Business Machines CorporationInventors: Ali Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Publication number: 20120190648Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C1-C6)alkyl or (C1-C6)alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, ORa, SRb, NRcRd, PO(ORe)(ORf), CO2Rg, SO2Rh SO3R1, P0(0H)(CH(0H)Rk), CN, N3 and NH—C(?NH)NH2, with Ra, Rb, Rc and Rd, representing, independently of each other, an hydrogen atom, a (C1-C6)alkyl group or a —CO—(C1-C6)alkyl group, Re, Rf, Rg, Rh and R1 representing, independently of each other, an hydrogen atom or a (C1-C6)alkyl group, and Rk representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO2, as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.Type: ApplicationFiled: July 23, 2010Publication date: July 26, 2012Inventors: Philippe Jubault, Jean-Charles Quirion, Gerald Lemonnier, Cedric Lion
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Publication number: 20120157413Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8119617Abstract: The present invention relates to compounds of formula wherein the residues have various meanings and their use as pharmaceuticals.Type: GrantFiled: August 21, 2007Date of Patent: February 21, 2012Assignee: Novartis AGInventors: Karl Baumann, Andreas Billich, Berndt Oberhauser
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Publication number: 20110251418Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 4, 2011Publication date: October 13, 2011Applicant: AJINOMOTO CO., INC.Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
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Publication number: 20110236931Abstract: Provided is a method to identify OP-adducted biomarkers of OP exposure as well as compounds containing OPs that can provide OP adducts.Type: ApplicationFiled: April 14, 2009Publication date: September 29, 2011Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventors: John R. Cashman, Mary T. MacDonald
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Patent number: 7998933Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.Type: GrantFiled: July 26, 2010Date of Patent: August 16, 2011Assignee: L'Oreal S.A.Inventors: Maria Dalko, Yann Mahe, Lionel Breton
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Publication number: 20110195937Abstract: Novel oxidized thiophospholipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions. Exemplary oxidized thiophospholipid according to embodiments described herein have the formula: wherein X1, X2, A1, A2, B?, B?, D? and D? are as described herein.Type: ApplicationFiled: October 1, 2009Publication date: August 11, 2011Applicant: Vascular Biogenics Ltd.Inventors: Eyal Breitbar, Eti Kovalevski-Ishai, Erez Feige, Itzhak Mendel, Zeev Ziniuk, Gideon Halperin
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Publication number: 20110059923Abstract: The present invention relates to a novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof, a production method therefor and a pharmaceutical composition for preventing and treating central nervous system disorders which contains the same as an active component. The novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof according to the present invention can beneficially be used to prevent and treat central nervous system disorders since it exhibits an equivalent biological and pharmacological activity to venlafaxine and salts thereof which are known in the field, it has very little toxicity, and, in particular, it is outstandingly soluble in water as compared with prior-art venlafaxine derivatives.Type: ApplicationFiled: May 8, 2009Publication date: March 10, 2011Applicant: JE IL PHARMACEUTICAL CO., LTD.Inventors: Seok Won Kang, Jong Soo Chun, Heung Mo Kang, Eui Seok Hong, Kwang-Woo Chun, Young Seok Byun, Myung-Hwa Kim, Young II Moon, Jei Man Ryu
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Publication number: 20110028421Abstract: The invention relates to the use of alkylphosphocholines in combination with antimetabolites for the treatment of multiple myeloma, colon cancer or renal cancer. Preferred alkylphosphocholines are described by the Formula II. A particularly effective treatment includes administering a combination of perifosine and capecitabine.Type: ApplicationFiled: March 31, 2010Publication date: February 3, 2011Applicant: AEterna Zentaris GmbHInventors: Jürgen Engel, Eckhard Günther, Herbert Sindermann, Babette Aicher
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Publication number: 20100317831Abstract: A probe compound for protein tyrosine phosphatases (PTPs), as shown in Formula (I) is provided. In Formula (I), A1 and A2 represent amino acids. The amino acids include leucine, phenylalanine, glutamic acid, lysine, alanine, arginine, aspartic acid, asparagine, citrulline, cysteine, cystine, glutamine, glycine, histidine, hydroxyproline, isoleucine, methionine, proline, serine, threonine, tryptophan, valine or a combination thereof. The invention also provides probe compound precursors for protein tyrosine phosphatases (PTPs).Type: ApplicationFiled: June 13, 2010Publication date: December 16, 2010Applicant: NATIONAL TAIWAN UNIVERSITYInventor: Lee-Chiang Lo
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Patent number: 7829737Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.Type: GrantFiled: March 6, 2008Date of Patent: November 9, 2010Assignee: Ceptyr, Inc.Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, Maher Qabar, Lauri Marie Schultz, Feng Hong, William Patt, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffry Howbert
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Publication number: 20100249074Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: ApplicationFiled: March 29, 2010Publication date: September 30, 2010Inventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20100112061Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.Type: ApplicationFiled: December 12, 2007Publication date: May 6, 2010Inventors: William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
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Publication number: 20100113770Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group rType: ApplicationFiled: October 14, 2009Publication date: May 6, 2010Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Susumu MUTO, Akiko ITAI
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Publication number: 20100086860Abstract: The invention relates to novel photopolymers based on specific urethane acrylates as writing monomers, which are suitable for producing holographic media, in particular for visual display of images.Type: ApplicationFiled: September 29, 2009Publication date: April 8, 2010Applicant: Bayer MaterialScience AGInventors: Thomas Roelle, Friedrich-Karl Bruder, Thomas Faecke, Marc-Stephan Weiser, Dennis Hoenel, Nicolas Stoeckel
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Publication number: 20100024683Abstract: The invention provides a phosphate compound having an unsaturated double bond and a metal salt thereof; a dental material containing a phosphate compound having an unsaturated double bond and/or a metal salt thereof; and a dental composition containing a phosphate compound having an unsaturated double bond and/or a metal salt thereof. The phosphate compound of the invention provides a dental material and a dental composition such as a bonding material, adhesive material and a dental luting agent that are highly stable during storage, convenient for handling, and that exhibit higher adhesiveness and bond durability.Type: ApplicationFiled: September 26, 2007Publication date: February 4, 2010Applicant: MITSUI CHEMICALS, INC.Inventors: Masatoshi Takagi, Atsuo Otsuji, Akinori Nagatomo, Kouji Suesugi
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Publication number: 20100027192Abstract: Disclosed are coated metal oxide nanoparticles comprising a metal oxide nanoparticle having a surface; and ligands attached to the metal oxide nanoparticle surface. Also disclosed are phosphonic acid compounds comprising the structure Gn-R-Xn, wherein G is a terminal group; wherein R is a bridging group; wherein X is a phosphonic acid group; and wherein each n is, independently, 1, 2, or 3. Also disclosed are methods for preparing and using coated metal oxide nanoparticles. Also disclosed are nanocomposite compositions comprising a polymer; and a coated metal oxide nanoparticle dispersed within the polymer. Also disclosed are articles, films, and capacitors comprising a coated metal oxide nanoparticle or a nanocomposite composition. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 12, 2006Publication date: February 4, 2010Inventors: Joseph Perry, Simon Jones, Joshua N. Haddock, Peter Hotchkiss
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Patent number: 7632652Abstract: The invention is directed to novel compositions of matter and methods of detecting in situ an immunohistochemical epitope or nucleic acid sequence of interest in a biological sample comprising binding an enzyme-labeled conjugate molecule to the epitope or sequence of interest in the presence of a redox-inactive reductive species and a soluble metal ion, thereby facilitating the reduction of the metal ion to a metal atom at or about the point where the enzyme is anchored. Novel phosphate derivatives of reducing agents are described that when exposed to a phosphatase are activated to their reducing form, thereby reducing metal ions to insoluble metal.Type: GrantFiled: June 24, 2004Date of Patent: December 15, 2009Assignee: Ventana Medical Systems, Inc.Inventors: Christopher Bieniarz, Casey A. Kernag, Jerome W. Kosmeder, Paula Rodgers, Jennifer Wong
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Patent number: 7598232Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula (I); wherein: X, X1, X2, Ra, R1, R2,R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.Type: GrantFiled: February 28, 2003Date of Patent: October 6, 2009Assignees: Temple University - Of the Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
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Publication number: 20090231663Abstract: An electrochromic compound having in the molecule at least an adsorbable group, a redox chromophore and a spacer portion, and represented by the following General Formula (1): wherein A represents the adsorbable group, C represents the redox chromophore, and X represents the spacer portion represented by the following formula; wherein R1 and R3 each represent an aliphatic hydrocarbon group or an aromatic derivative group, R2 represents a hydrogen atom or a monovalent group.Type: ApplicationFiled: March 10, 2009Publication date: September 17, 2009Inventors: Shigenobu HIRANO, Takeshi Shibuya, Hiroshi Kondo, Yuki Nakamura, Yukiko Abe, Tohru Yashiro
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Publication number: 20090226954Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.Type: ApplicationFiled: December 4, 2008Publication date: September 10, 2009Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne F. Patton
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Publication number: 20090176745Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.Type: ApplicationFiled: December 29, 2008Publication date: July 9, 2009Applicant: Emory UniversityInventor: Jack L. Arbiser
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Patent number: 7504389Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.Type: GrantFiled: November 15, 2005Date of Patent: March 17, 2009Assignee: Ceptyr, Inc.Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, William Patt, Maher Qabar, Lauri Mario Schultz, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffry Howbert
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Publication number: 20080312403Abstract: The invention relates to novel aromatic urethane (meth)acrylates having a high refractive index, a process for the preparation thereof and a process for the production of holographic media.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Bayer MaterialScience AGInventors: Nicolas Stockel, Friedrich-Karl Bruder, Jan Weikard
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Publication number: 20080261237Abstract: The present invention relates to inositol phosphate derivatives, in which the inositol phosphate is substituted with one or two reactive groups G or one or two conjugated substances or molecules M, said reactive group(s) G or said substance(s) or molecule(s) M being linked to IP1 via a linkage group L, M being chosen from the following group: a tracer, an immunogen, a member of a binding partner pair, a solid support. Application: tools allowing the study of the inositol phosphate cycle and therefore, indirectly, the study of seven transmembrane domain receptors coupled to phospholipase C, receptors having a tyrosine kinase activity, and in general enzymes involved in the variations of the intracellular concentration of IP1.Type: ApplicationFiled: December 2, 2005Publication date: October 23, 2008Inventors: Herve Bazin, Herve Ansanay, Eric Trinquet, Gerard Mathis
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Patent number: 7419970Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.Type: GrantFiled: April 11, 2005Date of Patent: September 2, 2008Assignee: L'OrealInventors: Maria Dalko, Yann Mahe, Lionel Breton
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Patent number: 7410965Abstract: A delayed release pharmaceutical formulation containing 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol or a pharmaceutically acceptable salt thereof in a matrix; said matrix containing from 1 to 80 wt. % of at least one pharmaceutically acceptable, matrix-forming, hydrophilic or hydrophobic polymer and having the following in vitro dissolution rate relative to 100 wt. % of the 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol contained in the formulation: 3-35 wt. % released after 0.5 hour, 5-50 wt. % released after 1 hour, 10-75 wt. % released after 2 hours, 15-82 wt. % released after 3 hours, 30-97 wt. % released after 6 hours, more than 50 wt. % released after 12 hours, more than 70 wt. % released after 18 hours, and more than 80 wt. % released after 24 hours.Type: GrantFiled: November 29, 2004Date of Patent: August 12, 2008Assignee: Gruenenthal GmbHInventors: Johannes Bartholomaeus, Iris Ziegler
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Patent number: 7405317Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C1-C10 alkyl or haloalkyl; R? and R? are each independently C1-C10 alkyl; R1 is CH3; and X is O; or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.Type: GrantFiled: September 21, 2005Date of Patent: July 29, 2008Assignee: Vion Pharmaceuticals Inc.Inventors: Xu Lin, Ivan King, Michael F. Belcourt, Terrence W. Doyle
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Publication number: 20080161592Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.Type: ApplicationFiled: March 6, 2008Publication date: July 3, 2008Applicant: CEPTYR, INC.Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, William Patt, Maher Qabar, Lauri Marie Schultz, Feng Hong, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffrey Howbert
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Patent number: 7378539Abstract: Classes of molecules are disclosed which can, for example, be used in molecular switches. The classes of molecules include at least three segments—an electronic donor (“D”), a switchable bridge (“B”), and an electronic acceptor (“A”)—chemically connected and linearly arranged (e.g., D-B-A). The electronic donor can be an aromatic ring system with at least one electron donating group covalently attached; an aromatic ring system with an electron withdrawing group covalently attached is usually employed as the electronic acceptor; and the switchable bridge can be a pi system that can be switched on or off using an external electric field.Type: GrantFiled: September 22, 2004Date of Patent: May 27, 2008Assignee: Hewlett-Packard Development Company, L.P.Inventors: Sean X. Zhang, Zhang-Lin Zhou, Kent Vincent, R. Stanley Williams
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Patent number: 7371747Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.Type: GrantFiled: November 13, 2002Date of Patent: May 13, 2008Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
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Patent number: 7199214Abstract: The present invention is directed to a process for the preparation of polyalkoxyaminies from monoalkoxyamine(s) of formula (I) and of at least one polyunsaturated compound of formula (II): and the preparation of polyfunctional living (co)polymers by polymerization by the radical route of one or more vinyl monomers in the presence of the polyalkoxyamines thus prepared.Type: GrantFiled: October 20, 2004Date of Patent: April 3, 2007Assignee: Arkema FranceInventors: Jean-Luc Couturier, Olivier Guerret, Stéphanie Magnet
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Patent number: 7078552Abstract: The present invention relates to the syntheses and structural elucidation of Combretastatin A1-Phosphate Prodrugs and Combretastatin B1-Phosphate Prodrugs and the utilization of those prodrugs in the treatment of neoplastic diseases. The prodrugs described herein have the structure: Combretastin A-1 Phosphate Prodrug (I) and Combretastin B-1 Phosphate Prodrug (II).Type: GrantFiled: April 27, 2001Date of Patent: July 18, 2006Assignee: Arizona Board of RegentsInventors: George R. Pettit, John W. Lippert, III
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Publication number: 20040229845Abstract: The instant invention provides reagents and methods for diagnosis, detection and treatment of cancers (for example, prostate cancers). In particular, the invention provides methods to generate various functionalized PSMA ligands, and their uses in diagnosis, detection, imaging, and treatment of prostate cancers, especially those overexpressing PSMA.Type: ApplicationFiled: June 16, 2004Publication date: November 18, 2004Applicant: Beth Israel Deaconess Medical CenterInventor: John V. Frangioni
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Publication number: 20040220147Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.Type: ApplicationFiled: June 10, 2004Publication date: November 4, 2004Inventors: Johan Malm, Peter Brandt, Karin Edvinsson, Thomas Ericsson, Sandra Gordon
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Publication number: 20040215022Abstract: Disclosed are colorant compounds of the formula 1Type: ApplicationFiled: May 25, 2004Publication date: October 28, 2004Applicant: Xerox CorporationInventors: Jeffery H. Banning, Donald R. Titterington, Clifford R. King
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Patent number: RE39593Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 17, 2003Date of Patent: April 24, 2007Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs