Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/220)
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Publication number: 20080207887Abstract: Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.Type: ApplicationFiled: November 8, 2007Publication date: August 28, 2008Applicant: EPOCH BIOSCIENCES, INC.Inventors: Eugeny Lukhtanov, Alexei Vorobiev
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Patent number: 7417156Abstract: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities.Type: GrantFiled: September 26, 2003Date of Patent: August 26, 2008Assignee: Johns Hopkins UniversityInventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
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Publication number: 20080188645Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).Type: ApplicationFiled: April 12, 2006Publication date: August 7, 2008Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Graham Ellis-Davies, Atsuya Momotake
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Publication number: 20080171724Abstract: Phosphorus substituted mycophenolate oxime derivatives with anti-cancer, anti-viral, anti-inflammatory anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as in assays for the detection of cancer, viral infection, inflammation and tissue/organ transplant rejection.Type: ApplicationFiled: October 26, 2005Publication date: July 17, 2008Applicant: GILEAD SCIENCES, INC.Inventors: William J. Watkins, Aesop Cho
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Publication number: 20080139822Abstract: The invention provides a novel optically active biaryl phosphorus compound that can be produced easily without the step of optical resolution, which is almost indispensable step in a conventional method.Type: ApplicationFiled: December 7, 2007Publication date: June 12, 2008Inventors: Ken Tanaka, Wataru Kuriyama
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Publication number: 20080132713Abstract: A myo-inositol derivative: R1, R2, R3 and R4 are identical, being selected from PO3H2, PO3Na2, PO3K2, PO3Li2, PO3Ca, PO3Mg, PO3(NH4)2, PO3(RNH3)2, PO3(R2NH2)2, PO3(R4N)2, PO(OR)2, H, COZ and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; R5 is one of H, benzyl, 4-methoxybenzyl, COZ, PO3H2, PO3Na2, PO3K2, PO3Li2, PO3Ca, PO3Mg, PO3(NH4)2, PO3(RNH3)2, PO3(R2NH2)2, PO3(R4N)2, PO(OR)2, and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; X is one of CH2, CH2CH2O, and CH2CH2CH2O; n is an integer from 1 to 8; L1 is a single bond or CH2; L2 is one of a single bond, CONH, CH2CONH, CH2CH2CONH, CH2CH2NHCO, CH2CH2NHCONH, CH2CH2NHCSNH, CH2CH2NHSO2, CH2CH2CH2NHCO, CH2CH2CH2NHCONH, CH2CH2CH2NHCSNH, CH2CH2CH2NHSO2, NHCO, NHCONH, NHCSNH, OCONH, CH2, CH2CH2, CH2CH2O, CH2CH2S, CH2CH2NH, CH2CH2CH2, CH2CH2CH2O, CH2CH2CH2S, CH2CH2CH2NH, and NH—SO2; and R6 is a UType: ApplicationFiled: November 5, 2007Publication date: June 5, 2008Inventor: David A. Berry
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Patent number: 7374900Abstract: Disclosed are compounds of the formula (I): wherein R3, R4, R5, R9, and R10 are selected from the group consisting of H and groups or atoms other than H, and R6 and R8 are halo or hydrogen; X1, X2, and X3 are independently O or S; provided that R9 and R10 are not simultaneously H, when all of X1, X2, and X3 are O; and of the formula (II) wherein R11-R14 are selected from the group consisting of H and groups or atoms other than H; X4-X9 are independently O or S; n and m are 0 or 1 but m and n cannot be 0 simultaneously; R15-R24 can be H or any substituent so long as the compound of formula II upon hydrolysis provides a fluorescent compound. These compounds are useful as substrates with high specificity for organophosphatase particularly human paraoxonase and bacterial organophosphorus hydrolase.Type: GrantFiled: March 16, 2004Date of Patent: May 20, 2008Assignee: The American National Red CrossInventors: Serguei Soukharev, David Hammond
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Patent number: 7358377Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.Type: GrantFiled: March 29, 2005Date of Patent: April 15, 2008Assignees: University of Iowa Research Foundation, The United States of AmericaInventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
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Publication number: 20080076833Abstract: The present invention relates to phosphorylated polyphenols, preferably tannins that, unlike their unphosphorylated counterparts, do not suffer from relatively low stability, resulting in an activity that is relatively short in time, and/or that do not result in yellowing of materials therewith such as textiles or polymers. The present invention further relates to a simple, cheap and environmentally friendly way of preparing these compounds. The phosphorylation process of the invention can be extended to simple phenolic compounds as well, as long as these have at least one accessible hydroxyl group. The phosphorylated compounds according to the invention can be used as antioxidants, as radical scavengers, as complexating agents for metals and proteins, as antibacterials or antiallergenic compounds, and as agents to flock textile.Type: ApplicationFiled: September 14, 2004Publication date: March 27, 2008Applicant: AJINOMOTO OMNICHEM S.A.Inventors: Willy Van Brussel, Geert Schelkens, Patrick Ricquier
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Preparation of oseltamivir phosphate (Tamiflu) and intermediates starting from D-glucose or D-xylose
Publication number: 20080009639Abstract: Novel processes for the preparation of the anti-viral agent, Oseltamivir Phosphate and novel intermediates prepared in such processes. The novel processes use as starting materials D-glucose or D-xylose in the preparation of Oseltamivir Phosphate.Type: ApplicationFiled: February 23, 2007Publication date: January 10, 2008Inventors: Bruno Konrad Radatus, K.S. Keshava Murthy, Gamini Weeratunga, Stephen E. Horne, Kiran Kumar Kothakonda, Eckardt C.G. Wolf, Zhongyi Wang -
Patent number: 7300766Abstract: A compound for enhancing the light output of a chemiluminescent system and, in particular, a stabilized, triggerable 1,2-dioxetane, is obtained by reacting a polyvinylbenzyl halide and a bilinker with either a trisubstituted amine or trisubstituted phosphine. A fluorescent molecule may be attached to polymer along with the trisubstituted amine or trisubstituted phosphine. Also, the benzyl halide may be reacted with a ?-electron donor, such as a vinyl naphthalene or vinylanthracene to form a co-polymer which is polymerizable with the trisubstituted amine and/or trisubstituted phosphine. By controlling the reaction parameters it is possible to obtain either a water-soluble or partial water soluble or insoluble compound crosslink polymer.Type: GrantFiled: May 23, 2003Date of Patent: November 27, 2007Inventor: Brij P. Giri
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Patent number: 7253298Abstract: The present invention concerns a process for hydrocyanating ethylenically unsaturated organic compounds to compounds containing at least one nitrile function. It relates more particularly to the hydrocyanation of diolefins such as butadiene or of substituted olefins such as alkenenitriles, for instance pentenenitriles. According to the process of the invention the reaction is implemented in the presence of a metal complex catalyst comprising a transition metal such as nickel and an organic ligand.Type: GrantFiled: June 24, 2005Date of Patent: August 7, 2007Assignee: Rhodia Polyamide IntermediatesInventors: Jean-Christophe Galland, Blaise Didillon, Philippe Marion, Damien Bourgeois
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Patent number: 7112684Abstract: Dye reagents useful in labeling biological materials are provided along with methods for their use.Type: GrantFiled: December 22, 2004Date of Patent: September 26, 2006Assignee: Epoch Biosciences, Inc.Inventors: Eugeny A. Lukhtanov, Alexei V. Vorobiev, Michael W. Reed, Nicolaas M. J. Vermeulen
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Patent number: 7087416Abstract: Methods and compositions are provided for detecting changes in membrane potential in membranes biological systems. In one aspect, the method comprises; a) providing a living cell with a first reagent comprising a charged hydrophobic molecule which is typically a fluorescence resonance energy transfer (FRET) acceptor or donor, or is a quencher and is capable of redistributing within the membrane of a biological membrane in response to changes in the potential across the membrane; b) providing the cell with a second reagent that can label the first face or the second face of a biological membrane within the cell; c) detecting light emission from the first reagent or the second reagent. One aspect of this method involves monitoring membrane potential changes in subcellular organelle membranes in a living cells. Another aspect of the invention is the use of certain embodiments of the method for the screening of test chemicals for activity to modulate the activity of a target ion channel.Type: GrantFiled: December 31, 2002Date of Patent: August 8, 2006Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Jesus E. Gonzalez, III
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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: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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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: 6921774Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.Type: GrantFiled: January 17, 2003Date of Patent: July 26, 2005Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
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Patent number: 6878665Abstract: The invention relates to novel diphosphines, in optically pure or racemic form, of formula (I): in which: R1 and R2 are a (C5-C7)cycloalkyl group, an optionally substituted phenyl group or a 5-membered heteroaryl group; and A is (CH2—CH2) or CF2. The invention further relates to the use of a compound of formula (I) as a ligand for the preparation of a metal complex useful as a chiral catalyst in asymmetric catalysis, and to the chiral metal catalysts comprising at least one ligand of formula (I).Type: GrantFiled: September 16, 2002Date of Patent: April 12, 2005Assignee: SynkemInventors: Sébastien Duprat de Paule, Nicolas Champion, Virginie Vidal, Jean-Pierre Genet, Philippe Dellis
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Patent number: 6872838Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.Type: GrantFiled: July 29, 2002Date of Patent: March 29, 2005Assignee: University of KansasInventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
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Publication number: 20040260101Abstract: The invention relates to novel diphosphines, in optically pure or racemic form, of formula (I): 1Type: ApplicationFiled: March 23, 2004Publication date: December 23, 2004Inventors: Sebastien Duprat De Paule, Nicolas Champion, Virginie Vidal, Jean-Pierre Genet, Philippe Dellis
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Patent number: 6831098Abstract: A hesperitin pro-form is provided. The invention provides both a hydrophilic and lipophilic hesperetin pro-form. A pharmaceutical composition is provided which is suitable for topical or oral administration in an individual, the composition comprising a hydrophilic hesperetin pro-form and a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which is suitable for topical or oral administration in an individual, the composition including a lipophilic hesperetin pro-form and a pharmaceutically acceptable carrier. A method is provided for treating a subject having or at risk of having a cell proliferative disorder, including administering to the subject a therapeutically effective amount of a hesperetin pro-form.Type: GrantFiled: February 8, 2002Date of Patent: December 14, 2004Assignee: Zielinski LaboratoryInventor: Jan E. Zielinski
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Patent number: 6774142Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).Type: GrantFiled: September 6, 2002Date of Patent: August 10, 2004Inventors: Thomas P. Lahey, Vithal J. Rajadhyasksha
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Patent number: 6767716Abstract: A chemiluminescent 1,2-dioxetane includes an alkaline phosphatase triggerable stable 1,2-dioxetane; a polymeric enhancer which is either an ammonium or phosphonium salt of a polyvinylbenzyl chloride and an aqueous enzyme diluent or stabilizer which corresponds to blood component including blood protein. The system is efficacious for single molecule detection of alkaline phosphatase and other enzymes.Type: GrantFiled: June 18, 2001Date of Patent: July 27, 2004Inventor: Brij P. Giri
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Publication number: 20040138477Abstract: A derivative of phosphoric acid ester salt or adduct or a mixture thereof is obtained from a reaction product, polycondensed with at least one aldehyde, of at least one polyol phosphoric acid ester with at least one organic nitrogen base. The derivative is advantageously used as a flame-inhibiting and/or intumescent treatment in plastic mouldings, on porous carriers or in paint or coating systems. The production of the derivative or a mixture thereof by reacting at least one polyol with phosphorus pentoxide and reacting the polyol phosphoric acid ester obtained in that way with at least one organic nitrogen base forming a phosphoric acid ester salt or adduct, is characterised in that the amount of phosphorus pentoxide required for the esterification operation is suspended in an amount of the ester or ester mixture to be produced, then at a temperature in the range of 20-180° C.Type: ApplicationFiled: March 1, 2004Publication date: July 15, 2004Inventors: Karl Gotzmann, Thomas Futterer, Hans-Dieter Nagerl, Vincent Mans
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Publication number: 20040059136Abstract: The invention concerns novel flavone and isoflavone derivatives of formulae (Ia) and (Ib) wherein: X represents a group of formula —COOR, or —PO(OR)2; R represents a hydrogen atom or an alkaline or alkaline-earth metal, or a lower alkyl group; R1 represents a hydroxy group, a lower alkoxy group or an acyloxy group; R2 and R3, identical or different, represent a hydrogen or halogen atom, or a trifluoromethyl group, a trichloromethyl group, a hydroxy group, an alkoxy group or an acyloxy group comprising 1 to 5 carbon atoms, or R2 and R3 can combine to form an alkylene dioxy group. The invention is useful for rheumatic diseases.Type: ApplicationFiled: October 3, 2003Publication date: March 25, 2004Inventors: Jean-Pierre Gesson, Nadia Fonteneau, Martine Mondon, Suzy Charbit, Herve Ficheux, Francois Schutze
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Patent number: 6664380Abstract: Free perfluorosulfonylmethide compounds and metal salts thereof show strong catalytic activity in carbon-carbon bond formation reactions, in amounts as low as 0.1 mole %. Fluorous media may be used, especially biphasic fluorous media enabling ready recycling of the catalyst. The formula thereof is: M[C(SO2R1)3−(m+q)(SO2R2)m(SO2R3)q]x where M is H, Sc, Y, La, Ce, Pr, Nd, Sm Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Zr, Hf, Th, Nb, Ta, U, Bi, Al, Ga, In or Tl, x is the common oxidation state of a said metal M, R1, R2 and R3 are perfluorinated or polyfluoronated hydrocarbon, ether or amine moieties or mixtures thereof and m+q=0, 1, 2 or 3 (m and q being zero or integers).Type: GrantFiled: February 19, 2002Date of Patent: December 16, 2003Assignee: The Institute of Applied CatalysisInventors: Anthony Gerard Martin Barrett, David Christopher Braddock, David Chadwick
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Patent number: 6656927Abstract: A compound represented by the general formula (I) or a salt thereof, wherein R represents a group represented by the following formula (A), (B) or (C) wherein R1 and R2 independently represent a C1-6 alkyl group, R3 represents an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group or a C1-6 alkoxy group and X-represents an anion, and n represents an integer of 2 to 5. The compound or a salt is useful as a ligand of inositol-1,4,5-trisphosphate (IP3) receptor.Type: GrantFiled: November 30, 2001Date of Patent: December 2, 2003Assignees: Daiichi Pharmaceutical., Ltd.Inventors: Tetsuo Nagano, Kazuya Kikuchi, Takanari Inoue, Masamitsu Iino, Kenzo Hirose
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Patent number: 6645951Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.Type: GrantFiled: July 16, 2001Date of Patent: November 11, 2003Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
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Patent number: 6630114Abstract: The invention relates to new calixarenes according to the formula: wherein R1 and R2, which may be identical or different, are alkyl, alkoxy or aryl groups, and n is an integer equal to 2, 3 or 4. Said calixarenes may be used to extract actinides and lanthanides from aqueous solutions.Type: GrantFiled: July 10, 2001Date of Patent: October 7, 2003Assignee: Commissariat a l'Energie AtomiqueInventors: Jean-François Dozol, Hélène Rouquette, Alejandro Garcia Carrera, Laetitia Delmau, Volker Böhmer, Alexander Shivanyuk, Christian Muzigmann
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Patent number: 6613743Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.Type: GrantFiled: December 6, 2000Date of Patent: September 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Robin Hale, Clarence Webster Andrews, III, Eric Steven Furfine, Ronald George Sherrill, Andrew Spaltenstein, Gregory Thomas Lowen
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Patent number: 6541613Abstract: Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hyrolyzable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs.Type: GrantFiled: December 15, 2000Date of Patent: April 1, 2003Assignee: Uyrex CorporationInventors: Sheldon S. Hendler, Jan Zielinski
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Patent number: 6515151Abstract: Methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Compounds prepared by the methods of the present invention are also disclosed.Type: GrantFiled: June 13, 2000Date of Patent: February 4, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Poss, Jerome L. Moniot, Ivan D. Trifunovich, David J. Kucera, John K. Thottahil, Shu-Hui Chen, Jianmei Wei
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Patent number: 6472539Abstract: A process for producing a diphosphine oxide or diphosphonate represented by formula (1) as defined, which comprises treating, with a base, a phosphine compound represented by formula (2) as defined and adding the thus-treated phosphine compound to a nonpolar solvent having an oxidative metal compound suspended therein so as to effect dimerization. The present invention makes it possible to produce, conveniently, in a high yield and safely, a diphosphine oxide or diphosphonate which is an intermediate for producing a diphosphine compound useful as a ligand of a metal complex serving as a catalyst for asymmetric synthesis reaction.Type: GrantFiled: July 6, 2001Date of Patent: October 29, 2002Assignee: Takasago International CorporationInventors: Tohru Yokozawa, Takao Saito, Noboru Sayo, Takero Ishizaki
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Patent number: 6472406Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 5, 2000Date of Patent: October 29, 2002Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6429202Abstract: The present invention relates to complexes of proanthocyanidin A2 and one or more phospholipids, pharmaceutical compositions containing the complex of proanthocyanidin A2 and one or more phospholipids, and methods of treating or preventing atherosclerosis and myocardial and cerebral infarction in a patient by administering the complex of proanthocyanidin A2 and one or more phospholipids, as well as methods of forming such complexesType: GrantFiled: June 11, 2001Date of Patent: August 6, 2002Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Paolo Morazzoni
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Patent number: 6417176Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: February 7, 2001Date of Patent: July 9, 2002Assignee: Tularik, Inc.Inventor: Jonathan B. Houze
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Publication number: 20020086333Abstract: A novel cartilage-specific compound and methods of diagnosis in medical and veterinary contexts using the compound. Screening methods for therapeutic substances and methods of treatment are also provided.Type: ApplicationFiled: September 28, 2001Publication date: July 4, 2002Inventors: Harpal Kaur Gahunia, Kenneth Pritzker, Reinhold Vieth
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Patent number: 6410752Abstract: An object of the present invention is to provide the tocopherol derivatives represented by the following formula (I), and their salts: Wherein, R1, R2 and R3 are H or methyl group, and at least one positions selected from group consisting of the R1, R2 and R3 positions are methyl group; and, A is CH2—CH(CH3)— or CH═C(CH3)— The other object of the present invention is to provide a method for preparing the above tocopherol derivatives. The tocopherol derivatives is prepared by reacting tocopherol with phosphorous oxychloride in an equivalent ratio of 1:1˜1.3, in presence of an organic base, in an organic solvent; reacting the tocopherol dichlorophosphate produced by the above reaction with 3-aminopropanol in presence of an organic base, in an organic solvent; and, hydrolyzing the above products.Type: GrantFiled: January 9, 2001Date of Patent: June 25, 2002Assignee: Pacific CorporationInventors: Kil Joong Kim, Duck Hee Kim, Ho Sik Rho, Jae Won You, Chun Ja Nam, Jong Eoun Hong, Hak Hee Kang, Ih Seob Chang
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Patent number: 6403811Abstract: A process for recovering a concentrate of chromans from a distillate containing chromans is provided comprising the steps of: (1) forming chroman phosphates in the distillate; (2) subjecting the distillate to shearing forces, in the presence of a gas of flotation to form a froth; and (3) recovering the froth containing the concentrate of chroman phosphates.Type: GrantFiled: July 25, 2001Date of Patent: June 11, 2002Assignee: Swig Pty LtdInventor: Simon Michael West
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Patent number: 6380175Abstract: The present invention is directed to a method for enhancing the delivery of delta-9-tetrahydrocannabinol (“THC”) to the brain of a mammal in need of treatment with this drug, by administering water-soluble prodrugs of THC intranasally.Type: GrantFiled: August 2, 2001Date of Patent: April 30, 2002Assignee: New Millennium Pharmaceutical Research, Inc.Inventors: Anwar A. Hussain, Lewis W. Dittert, Ali M. Qaisi, Ashraf Traboulsi
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Publication number: 20020045765Abstract: An object of the present invention is to provide the tocopherol derivatives represented by the following formula (I), and their salts: 1Type: ApplicationFiled: January 9, 2001Publication date: April 18, 2002Inventors: Kil Joong Kim, Duck Hee Kim, Ho Sik Rho, Jae Won You, Chun Ja Nam, Jong Eoun Hong, Hak Hee Kang, Ih Seop Chang
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Publication number: 20020028791Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1Type: ApplicationFiled: July 18, 2001Publication date: March 7, 2002Inventors: Robert F. Kaltenbach, George L. Trainor
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Patent number: 6346615Abstract: Spiroadamantyl dioxetanes bearing an alkoxy substituent, and an aromatic substituent of phenyl or naphthyl on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears a moiety designated OX, wherein the X is cleaved by an enzyme with which the dioxetane is permitted to come in contact with. The T½ kinetics of the chemiluminescent reaction, as well as the signal intensity, or quantum yield of the chemiluminescent reaction, can be altered by selection of an electron-withdrawing or an electron-donating group Z, at positions on the aromatic substituent other than those adjacent the point of attachment to the dioxetane. Signal strength can further be enhanced by recognized chemiluminescent enhancers.Type: GrantFiled: September 6, 2000Date of Patent: February 12, 2002
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Patent number: 6337406Abstract: Chiral phosphine ligands derived from chiral natural products including D-mannitol and tartaric acid. The ligands contain one or more 5-membered phospholane rings with multiple chiral centers, and provide high stereoselectivity in asymmetric reactions.Type: GrantFiled: August 19, 1999Date of Patent: January 8, 2002Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Patent number: 6329421Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: February 25, 1997Date of Patent: December 11, 2001Assignee: Merck Frosst Canada & Co.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 6313317Abstract: Disclosed is a ruthenium-phosphine complex usable as the catalyst giving a high enantiomer excess in an asymmetric reaction and a method for producing the complex. The ruthenium-phosphine complex is represented by formula (1): [{(RuX(L)}2(&mgr;-X)3]−[R22NH2]+ (1) wherein R2 represents hydrogen, alkyl, cycloalkyl or benzyl and L represents a diphosphine ligand represented by formula (2): wherein R1 represents an optionally substituted phenyl group and X represents a halogen atom. The method for preparing a ruthenium-phosphine complex represented by formula (1) is characterized in that a ruthenium complex represented by the formula [RuX(arene)(L)]X and an ammonium salt represented by the formula R22NH.HX are reacted with each other.Type: GrantFiled: March 22, 1999Date of Patent: November 6, 2001Assignee: Takasago International CorporationInventors: Noboru Sayo, Takao Saito, Tohru Yokozawa
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Patent number: 6281390Abstract: Compounds of formula III, wherein R6 und R7 signify identical or different secondary phosphino; R8 is —CH2—OH, —CH2—NH2—, —CH2O——B—FU, —CH2—NH2—B—FU, or —O—B—FU; R9 has the same significance as R8 or is C1-C4-alkyl or C1-C4-alkoxy; or R8 and R9 together signify HOCH(CH2—O—)2, H2NCH—(CH2—O—)2, FU—B—OCH(CH2—O—)2 or FU—B—HNCH(CH2—O—)2; B is a bridging group; and FU is a functional group. The compounds may be bonded to inorganic or organic carriers. Their d-8 metal complexes are valuable catalysts for the enantioselective hydrogenation of prochiral organic compounds with carbon multiple bonds or carbon/hetero atom multiple bonds.Type: GrantFiled: November 17, 1999Date of Patent: August 28, 2001Assignee: Solvias AGInventors: Benoît Pugin, Ivo Steiner, Rhony Niklaus Aufdenblatten, Antonio Togni
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Publication number: 20010014688Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: ApplicationFiled: November 13, 1998Publication date: August 16, 2001Inventors: THOMAS E. BARTA, DANIEL P. BECKER, TERRI L. BOEHM, GARY A. DECRESCENZO, CLARA I. WILLAMIL, JOSEPH J. MCDONALD, JOHN N. FRESKOS, DANIEL P. GETMAN, GUNNAR J. HANSON
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Patent number: RE38117Abstract: Described herein are novel trioxane dimers of structure which possess antiproliferative and antitumor activities.Type: GrantFiled: November 21, 2000Date of Patent: May 6, 2003Assignees: Hauser, Inc., Johns HopkinsInventors: Qun Y. Zheng, Christopher Murray, Randall J. Daughenbaugh, Poonsakdi Ploypradith, Gary H. Posner