Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/113)
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Publication number: 20100279983Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2007Publication date: November 4, 2010Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
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Publication number: 20100261677Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: September 4, 2008Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20100221215Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100210595Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: ApplicationFiled: July 25, 2008Publication date: August 19, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Publication number: 20100204183Abstract: The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.Type: ApplicationFiled: May 2, 2008Publication date: August 12, 2010Applicant: QUEEN MARY & WESTFIELD COLLEGEInventors: Alice Sullivan, Adina Michael-Titus, Lesley Robson
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Publication number: 20100183517Abstract: Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.Type: ApplicationFiled: January 22, 2010Publication date: July 22, 2010Applicant: CANCER TARGETED TECHNOLOGY LLCInventor: Cliff Berkman
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Patent number: 7759491Abstract: The present invention provides a method for producing an indazol-3-ylmethyl phosphonium salt represented by Formula (IV): [wherein X represents halogen, OSO2Ra (wherein Ra represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or OC(?O)Rb (wherein Rb has the same meaning as the above Ra), or the like, and R1, R2 and R3 may be the same or different and each represents substituted or unsubstituted aryl or the like] or a salt thereof, which comprises reacting a compound represented by Formula (I): a compound represented by Formula (II): H—X??(II) (wherein X has the same meaning as defined above), and a compound represented by Formula (III): (wherein R1, R2 and R3 have the same meanings as defined above, respectively), and the like.Type: GrantFiled: April 28, 2006Date of Patent: July 20, 2010Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Koji Hagihara, Tsutomu Matsumura, Masahiro Hoshikawa, Iwao Chujo
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Publication number: 20100168359Abstract: Described herein are tri-functional compounds useful in the production of ophthalmic lenses. The compounds are composed of UV absorber having a polymerization initiator directly or indirectly bonded to the ultraviolet absorber, and an olefinic group directly or indirectly bonded to the ultraviolet absorber. Also described herein are polymers and ophthalmic lenses produced from the tri-functional compounds described herein.Type: ApplicationFiled: December 17, 2009Publication date: July 1, 2010Inventors: Angelika Maria Domschke, Lynn Cook Winterton, Troy Vernon Holland, Richard Charles Turek
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Patent number: 7709652Abstract: Disclosed are UV absorbers that contain a labile functional group capable of initiating free radical polymerization.Type: GrantFiled: May 22, 2008Date of Patent: May 4, 2010Assignee: Alcon, Inc.Inventor: Douglas C. Schlueter
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Publication number: 20100087634Abstract: Fluorous-tagged oligonucleotide reagents and an oligonucleotide purification methodology making use thereof, the method comprising: Synthesizing oligonucleotides using oligonucleotide reagents each bearing at least one fluorous group to yield a mixture of synthesis products and reagents, the mixture including at least one target synthesized oligonucleotide bearing at least one fluorous group; passing the mixture through a separation medium having an affinity for the at least one fluorous group so that the target synthesized oligonucleotide bearing at least one fluorous group is adsorbed by the separation medium; washing the separation medium with at least a first solvent to selectively dissociate therefrom substantially all synthesis products and reagents of the heterogenous mixture other than the at least one target synthesized oligonucleotide bearing at least one fluorous group; and subsequently dissociating the at least one synthesized oligonucleotide from the separation medium, with or without the fluorouType: ApplicationFiled: October 20, 2009Publication date: April 8, 2010Applicant: BERRY & ASSOCIATES, INC.Inventors: David A. Berry, William H. Pearson
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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: 20090192121Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: ApplicationFiled: March 26, 2009Publication date: July 30, 2009Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
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Publication number: 20090170812Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: June 25, 2007Publication date: July 2, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Victoria Bartlett, Lynne Garrity-Ryan, Mark Grier, Oak K. Kim, Atul K. Verma
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Publication number: 20090131369Abstract: This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: Here, X1 and X2 are independently O or S, wherein at least one of X1 and X2 is O; Y1 and Y2 are independently O or S, wherein at least one of Y1 and Y2 is O; R1 is alkyl having from 1-4 carbon atoms; R2, R3, and R4 are independently hydrogen or a cation; R5 and R6 are independently hydrogen, halogen, alkyl (having from 1-8 carbon atoms), —OR7, —SR8, —CO—R9, —OSO2—Ar, or —S(O)R10; R7 is alkyl having from 1-8 carbon atoms; R8 is alkyl (having from 1-8 carbon atoms) or aryl; R9 is alkyl (having from 1-8 carbon atoms), cycloalkyl (having from 3-6 carbon atoms), or aryl; Ar is aryl; and R10 is alkyl (having from 1-8 carbon atoms) or aryl. The compounds generally are soluble and stable in water, and have antiparasitic (particularly anthelmintic) activity in vivo that is comparable to known water-insoluble benzimidazole carbamates (e.g., albendazole and fenbendazole).Type: ApplicationFiled: July 18, 2006Publication date: May 21, 2009Applicant: Intervet International B.V.Inventor: Christophe Pierre Alain Chassaing
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Publication number: 20090069568Abstract: The present invention provides a method for producing an indazol-3-ylmethyl phosphonium salt represented by Formula (IV): [wherein X represents halogen, OSO2Ra (wherein Ra represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or OC(?O)Rb (wherein Rb has the same meaning as the above Ra), or the like, and R1, R2 and R3 may be the same or different and each represents substituted or unsubstituted aryl or the like] or a salt thereof, which comprises reacting a compound represented by Formula (I): a compound represented by Formula (II): H—X??(II) (wherein X has the same meaning as defined above), and a compound represented by Formula (III): (wherein R1, R2 and R3 have the same meanings as defined above, respectively), and the like.Type: ApplicationFiled: April 28, 2006Publication date: March 12, 2009Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Koji Hagihara, Tsutomu Matsumura, Masahiro Hoshikawa, Iwao Chujo
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Patent number: 7494983Abstract: This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: August 31, 2004Date of Patent: February 24, 2009Assignee: Merck & Co. Inc.Inventors: Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
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Publication number: 20090036409Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.Type: ApplicationFiled: August 20, 2008Publication date: February 5, 2009Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence De Garavilla, Bruce E. Maryanoff
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Publication number: 20090011975Abstract: The invention provides a method of inhibiting cell death in a mammal. The method comprises administering to a mammal an effective amount of a composition comprising a cell protection factor covalently linked to a bone targeting agent via a linkage that is cleaved under physiological conditions, whereby the cell protection factor is released from the bone targeting agent in vivo to inhibit cell death. The invention further provides a compound comprising a cell protection factor covalently attached to a bone targeting agent via a linker that is cleaved under physiological conditions.Type: ApplicationFiled: July 31, 2008Publication date: January 8, 2009Applicant: Semafore Pharmaceuticals Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Tim C. Smith
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Publication number: 20080318255Abstract: The present invention relates to a method (assay) for determining the activity of an enzyme selected from the group consisting of a sphingosine kinase and a phosphatase involved in the sphingolipid pathway by use of a labeled sphingosine.Type: ApplicationFiled: September 28, 2004Publication date: December 25, 2008Inventors: Andreas Billich, Peter Ettmayer, Diana Mechtcheriakova, Peter Nussbaumer, Alexander Wlachos
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Publication number: 20080312188Abstract: Novel compounds designed to allow interactions with binding sites of GSK-3 and hence are capable of inhibiting GSK-3 activity, via inhibition of substrate binding are disclosed. Further disclosed are pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions.Type: ApplicationFiled: April 30, 2008Publication date: December 18, 2008Applicant: Tel Aviv University Future Technology Development L.P.Inventors: Hagit Eldar-Finkelman, Moshe Portnoy
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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: 7439385Abstract: The present invention provides a novel process for preparation of bisphosphonic acid derivatives or pharmaceutical acceptable salt thereof, by reacting carboxylic acid having structural formula (II) with phosphorous acid and a halophosphorous compound, wherein halophosphorous compound is selected from the group comprising of PCl3, PCl5, POCl3, PBr3, POBr3, and PBr5 in presence of diphenyl ether.Type: GrantFiled: July 24, 2006Date of Patent: October 21, 2008Assignee: Alembic LimitedInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra
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Publication number: 20080249290Abstract: Disclosed is a compound of the formula and dimers thereof, wherein R, R?, X, (Y)m, and (Z)n are as defined herein. The compounds are useful as colorants, particularly in applications such as phase change inks.Type: ApplicationFiled: April 4, 2007Publication date: October 9, 2008Inventors: Jeffrey H. Banning, James D. Mayo, Rina Carlini
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Publication number: 20080193700Abstract: The invention relates to novel optical recording media, which comprise particular novel metal chelates and have an excellent recording and playback quality, especially at a wavelength of from 300 to 500 nm.Type: ApplicationFiled: April 25, 2005Publication date: August 14, 2008Applicant: CIBA SPECIALTY CHEMICALS HOLDING INC.Inventors: Heinz Wolleb, Annemarie Wolleb, Frank Bienewald, Beat Schmidhalter, Jean-Luc Budry
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Patent number: 7410956Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.Type: GrantFiled: February 11, 2003Date of Patent: August 12, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Patent number: 7312219Abstract: Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: August 6, 2003Date of Patent: December 25, 2007Assignee: Metabasis Therapeutics, Inc.Inventors: Qun Dang, Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, M. Rami Reddy, Atul Agurwal
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Patent number: 7235537Abstract: Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: August 29, 2003Date of Patent: June 26, 2007Assignee: Array BioPharma, Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley, Kevin Koch
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Patent number: 7208606Abstract: The invention pertains to a hydroformylation process for the conversion of an ethylenically unsaturated compound to an alcohol comprising a first step of reacting at an elevated temperature in a reactor the ethylenically unsaturated compound, carbon monoxide, hydrogen, and a phosphine-containing cobalt hydroformylation catalyst, which are dissolved in a solvent, followed by a second step of separating a mixture comprising the alcohol and heavy ends from a solution comprising the catalyst and the solvent, followed by a third step of recycling the solution to the reactor.Type: GrantFiled: October 10, 2006Date of Patent: April 24, 2007Assignee: Shell Oil CompanyInventors: Eit Drent, Jacoba Catherina Lucia Johanna Suykerbuyk
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Patent number: 7205412Abstract: An antibiotic additive and an ink composition including the antibiotic additive include a compound produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction. The ink composition includes a colorant, a solvent and an antibiotic additive produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction.Type: GrantFiled: July 2, 2003Date of Patent: April 17, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Seung-min Ryu, Jae-hwan Kim, Jong In Lee, Dae hee Lee
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Patent number: 7192968Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.Type: GrantFiled: April 5, 2001Date of Patent: March 20, 2007Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
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Patent number: 7183276Abstract: The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W—D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.Type: GrantFiled: February 27, 2003Date of Patent: February 27, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Nozomu Sakai, Yu Momose, Katsuhito Murase, Masatoshi Hazama
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Patent number: 7060290Abstract: Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.Type: GrantFiled: February 16, 2000Date of Patent: June 13, 2006Assignee: Supergen, Inc.Inventors: Bruce H. Morimoto, Peter L. Barker
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Patent number: 7030103Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: October 8, 2002Date of Patent: April 18, 2006Assignee: Methylgene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6960572Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC, RD, RE, p, q and X are as defined herein, and to their preparation and use.Type: GrantFiled: June 21, 2002Date of Patent: November 1, 2005Assignee: Ariad Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III, Yihan Wang, Regine Bohacek
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Patent number: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6777433Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.Type: GrantFiled: June 28, 2002Date of Patent: August 17, 2004Assignee: Merck Frosst Canada & Co.Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Robert Young
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Publication number: 20040116387Abstract: 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, subcllinical hyperthyrodism and liver diseases.Type: ApplicationFiled: January 12, 2004Publication date: June 17, 2004Inventors: Johan Malm, Erik Floistrup, Spiros Grivas, Yi-Lin Li
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Publication number: 20040116710Abstract: Disclosed are compounds of the formula I 1Type: ApplicationFiled: August 29, 2003Publication date: June 17, 2004Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley, Kevin Koch
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Publication number: 20040058892Abstract: Novel FBPase inhibitors of the formula I and X 1Type: ApplicationFiled: August 6, 2003Publication date: March 25, 2004Inventors: Qun Dang, Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, N. Rami Reddy, Atul Agarwal
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Patent number: 6706698Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.Type: GrantFiled: September 26, 2001Date of Patent: March 16, 2004Assignee: Ilex Products, Inc.Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
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Publication number: 20040038943Abstract: This invention provides indole and benzimidazole 15-lipoxygenase (15-LO) inhibitors of the formula where one of Y1 and Y2 is CH, N, or NH, and the other is R3 includes H, halo. HN2, COOH, alkyl; R4 includes halo, alkyl, and alkoxy; Z is C, CH, or NR5; R5 is H or oxycabonyl; and each X is independently H, alkyl, alkoxy, or halo.Type: ApplicationFiled: February 21, 2003Publication date: February 26, 2004Inventors: David Thomas Connor, William Howard Roark, Roderick Joseph Sorenson
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Publication number: 20040024037Abstract: An antibiotic additive and an ink composition including the antibiotic additive include a compound produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction. The ink composition includes a colorant, a solvent and an antibiotic additive produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction. The antibiotic additive prevents surface dry, improves storage stability and inhibits propagation and growth of bacteria in an ink and has excellent compatibility with a general dye or pigment.Type: ApplicationFiled: July 2, 2003Publication date: February 5, 2004Applicant: SAMSUNG Electronics Co., Ltd.Inventors: Seung-Min Ryu, Jae-Hwan Kim, Jong In Lee, Dae Hee Lee
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Publication number: 20030213164Abstract: Compounds of formula I or II 1Type: ApplicationFiled: April 17, 2003Publication date: November 20, 2003Inventors: Stephen D. Pastor, Andrew B. Naughton, Robert Detlefsen, Mervin G. Wood, Joseph Suhadolnik, Anthony DeBellis, Deborah DeHessa
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Patent number: 6645950Abstract: Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis. Embodiments include a 5(6)-substituted benzimidazole-2-carbamate of formula I wherein A represents a multi-substituted alkyl group or aromatic ring.Type: GrantFiled: October 22, 2001Date of Patent: November 11, 2003Assignee: Angiogene Pharmaceuticals Ltd.Inventor: Peter David Davis
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Patent number: 6613945Abstract: The invention concerns a resolution method for a racemic mixture of aldehyde of formula (I). The aldehydes of formula I are useful in their enantiomeric form or their racemic form for preparing transition metal complexes useful as catalysts in hydroformylation reactions of olefins.Type: GrantFiled: August 7, 2001Date of Patent: September 2, 2003Assignee: Rhodia ChimieInventors: François Mercier, Stéphane Lelievre, François Mathey, Michel Spagnol
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Publication number: 20030130524Abstract: Provided is a process for preparing 2H-benzotriazole UV absorbers containing a perfluoroalkyl moiety at the 5-position of the benzo ring, for example a trifluoromethyl group, which involves diazotizing the perfluoroalkyl substituted o-nitroaniline using concentrated sulfuric acid plus sodium nitrite or nitrosylsulfuric acid to form the corresponding monoazobenzene intermediate via the diazonium salt intermediate which is reduced to the corresponding 5-perfluoroalkyl substituted 2H-benzotriazole UV absorber compound by conventional reduction means. Also provided is a novel one-pot, multiphase reaction for the preparation of 2(2-nitrophenylazo) substituted phenols, which are precursors for 2H-benzotriazole UV absorbers.Type: ApplicationFiled: December 10, 2002Publication date: July 10, 2003Inventors: Mervin G. Wood, Deborah DeHessa, Joseph Suhadolnik, Andrew B. Naughton, Jerome Sanders, Jacqueline Lau, Rong Xiong, Joseph Babiarz
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Publication number: 20030120083Abstract: Provided is a process for preparing 2H-benzotriazole UV absorbers containing a perfluoroalkyl moiety at the 5-position of the benzo ring, for example a trifluoromethyl group, which involves diazotizing the perfluoroalkyl substituted o-nitroaniline using concentrated sulfuric acid plus sodium nitrite or nitrosylsulfuric acid to form the corresponding monoazobenzene intermediate via the diazonium salt intermediate which is reduced to the corresponding 5-perfluoroalkyl substituted 2H-benzotriazole UV absorber compound by conventional reduction means. Also provided is a novel one-pot, multiphase reaction for the preparation of 2(2-nitrophenylazo) substituted phenols, which are precursors for 2H-benzotriazole UV absorbers.Type: ApplicationFiled: December 10, 2002Publication date: June 26, 2003Inventors: Mervin G. Wood, Deborah DeHessa, Joseph Suhadolnik, Andrew B. Naughton, Jerome Sanders, Jacqueline Lau, Rong Xiong, Joseph Babiarz
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Patent number: 6576760Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.Type: GrantFiled: January 11, 2001Date of Patent: June 10, 2003Assignee: Chelator LLCInventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
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Publication number: 20030104473Abstract: The present invention provides common ligand mimics that act as common ligands for a receptor family. The present invention also provides bi-ligands containing these common ligand mimics. Bi-ligands of the invention provide enhanced affinity and/or selectivity of ligand binding to a receptor or receptor family through the synergistic action of the common ligand mimic and specificity ligand that compose the bi-ligand. The present invention also provides combinatorial libraries containing the common ligand mimics and bi-ligands of the invention. Further, the present invention provides methods for manufacturing the common ligand mimics and bi-ligands of the invention and methods for assaying the combinatorial libraries of the invention.Type: ApplicationFiled: March 12, 2002Publication date: June 5, 2003Inventors: Qing Dong, Hengyuan Lang, Lan Xie, Lin Yu