1,2,4-triazoles (including Hydrogenated) Patents (Class 548/262.2)
  • Patent number: 7081467
    Abstract: The present invention is directed C2-disubstituted indan-1-ones of the Formula I, physiologically acceptable salts, and physiologically functional derivatives thereof, and pharmaceutical compositions comprising such compounds, salts and derivatives, which are useful for reducing weight, for the prophylaxis or treatment of obesity, and for the prophylaxis or treatment of type II diabetes in mammals. The invention is directed also to methods for reducing weight and such treatments and prophylaxis. The invention is directed also to processes for the preparation of such compounds.
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: July 25, 2006
    Assignee: Sanofi-aventis Deutschland GmbH
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Patent number: 7078424
    Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.
    Type: Grant
    Filed: June 24, 2003
    Date of Patent: July 18, 2006
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
  • Patent number: 7074816
    Abstract: A novel 1,2,4-triazole compound which is useful as a therapeutic agent for hyperuricemia and gout due to hyperuricemia is provided. A compound is represented by the following general formula (1): wherein R2 represents an unsubstituted or substituted pyridyl group, R1 represents a similar pyridyl group, a pyridine-N-oxide group corresponding to these pyridyl groups, or a phenyl group, and R3 represents hydrogen or a lower alkyl group substituted with pivaloyloxy group and R3 bonds to a nitrogen atom in the ring. A process for production of a compound by reacting a nitrile and a hydrazide, and a therapeutic agent, particularly a xanthine oxidase inhibitor are also provided.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: July 11, 2006
    Assignee: Fuji Yakuhin Co., Ltd.
    Inventors: Hiroshi Nakamura, Soichi Kaneda, Takahiro Sato, Naoki Ashizawa, Koji Matsumoto, Takashi Iwanaga, Tsutomu Inoue
  • Patent number: 7049324
    Abstract: a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ?Z1—Z2?Z3— represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalky
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: May 23, 2006
    Inventors: Ashis Kumar Saha, David William End, Bart Lieven Daniel De Corte, Henry Joseph Breslin, Li Liu
  • Patent number: 7045520
    Abstract: The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.
    Type: Grant
    Filed: February 7, 2003
    Date of Patent: May 16, 2006
    Assignee: The Curators of the University of Missouri
    Inventors: William J. Welsh, Seong Jae Yu, Anil Nair
  • Patent number: 7045533
    Abstract: The present invention relates to novel naphthalene derivatives of formula (I), wherein R1, R2, R3 and X are as defined in the description, and preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
    Type: Grant
    Filed: November 22, 2001
    Date of Patent: May 16, 2006
    Assignee: Novartis AG
    Inventors: Christopher T Brain, Andrew J Culshaw, Edward K Dziadulewicz, Ulrich Schopfer
  • Patent number: 7034161
    Abstract: A method of converting pure ?-anomer or ?/?-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5-tri-O-acetyl-?-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure ?-anomer, alpha 1,2,3,5-tetra-O-acetyl-L-ribofuiranose, are useful in manufacturing levovirin.
    Type: Grant
    Filed: August 11, 2003
    Date of Patent: April 25, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Zhiming Dong, Pingsheng Zhang
  • Patent number: 6995182
    Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: February 7, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Vincent Mutel, Juergen Wichmann
  • Patent number: 6995273
    Abstract: A compound represented by the following formula (I): and a silver halide color photographic light-sensitive material containing the compound as a coupler. In formula (I), R represents an alkyl, alkenyl, alkynyl, aryl or heterocyclic group; L is —CO— or —SO2—; and X is a hydrogen atom or a group capable of being split-off upon coupling with an oxidized product of a developing agent selected from the group consisting of a halogen atom, an aryloxy group, an alkoxy group, an arylthio group, an alkylthio group, an acyloxy group, a sulfonamide group, and an acylamino group whose bonding site is the nitrogen atom.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: February 7, 2006
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hideaki Satoh, Takeshi Nakamine, Nobuo Seto, Hiroyuki Yoneyama, Yasuhiro Shimada
  • Patent number: 6987104
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6987122
    Abstract: 2-(1H-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: January 17, 2006
    Assignee: Novuspharma S.p.A.
    Inventors: Ernesto Menta, Nicoletta Pescalli
  • Patent number: 6969727
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: November 29, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
  • Patent number: 6933390
    Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.
    Type: Grant
    Filed: July 15, 2004
    Date of Patent: August 23, 2005
    Assignee: Warner-Lambert Company
    Inventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
  • Patent number: 6919363
    Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R8 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: July 19, 2005
    Assignee: Euro-Celtique S.A.
    Inventors: Derk J. Hogenkamp, Phong Nguyen, Ji Yang
  • Patent number: 6867208
    Abstract: The present invention relates to compounds of the formula I A—B—D—E—F—G??(I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: May 13, 2002
    Date of Patent: March 15, 2005
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 6867303
    Abstract: The invention relates to new (pre)catalysts of ruthenium complexes of formula 1, wherein L1, X, X?, R1, R2, R3 and n are defined herein. The novel ruthenium complexes of formula 1 are convenient (pre)catalysts for metathesis reactions and can be applied, e.g., for ring-closing metathesis, cross metathesis or ene-ine metathesis reactions. Another aspect of the invention are the novel intermediates of formula 2.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: March 15, 2005
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Karol Grela
  • Patent number: 6849618
    Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form a 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.
    Type: Grant
    Filed: October 15, 2003
    Date of Patent: February 1, 2005
    Assignee: BASF Aktiengesellschaft
    Inventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
  • Patent number: 6833453
    Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.
    Type: Grant
    Filed: October 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: William R. Perrault, Robert C. Gadwood
  • Patent number: 6833375
    Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: December 21, 2004
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
  • Patent number: 6822094
    Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: November 23, 2004
    Assignee: Aventis Research & Technologies, GmbH & Co. KG
    Inventors: Josef Salbeck, Donald Lupo
  • Publication number: 20040229869
    Abstract: Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
    Type: Application
    Filed: March 26, 2004
    Publication date: November 18, 2004
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Sangita, Atul Kumar, Man Mohan Singh, Girish Kumar Jain, Puvvada Sri Ramanchandra Murthy, Suprabhat Ray
  • Publication number: 20040214037
    Abstract: Compounds, compositions, organic electronic devices, and methods for preparing organic electronic devices are described. The compounds of the invention contain at least two carbon-carbon triple bonds and a heteroaromatic ring having at least one —C═N— unit. The compounds can be used as electron transport agents in organic electronic devices such as organic electroluminescent devices.
    Type: Application
    Filed: April 15, 2003
    Publication date: October 28, 2004
    Inventors: Ralph R. Roberts, Yingbo Li, Sergey A. Lamansky
  • Publication number: 20040214870
    Abstract: The present invention is directed to compounds of formula (I), 1
    Type: Application
    Filed: February 4, 2004
    Publication date: October 28, 2004
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Publication number: 20040214827
    Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Application
    Filed: June 5, 2003
    Publication date: October 28, 2004
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Publication number: 20040214036
    Abstract: Compounds and compositions are provided that can be used as electron transport agents in organic electronic devices such as organic electroluminescent devices. The compounds are non-polymeric and have an aromatic core conjugated to end capping groups. The aromatic core contains a phenylene group arylene or naphthalene group arylene having a pendant heteroaryl group that includes a —C═N— unit.
    Type: Application
    Filed: April 15, 2003
    Publication date: October 28, 2004
    Applicant: 3M Innovative Properties Company
    Inventors: James G. Bentsen, Nicholas P. Goplen, Yingbo Li, Ralph R. Roberts
  • Patent number: 6759537
    Abstract: The present invention relates to novel hexacoordinated metathesis catalysts and to methods for making and using the same. The inventive catalysts are of the formula wherein: M is ruthenium or osmium; X and X1 are the same or different and are each independently an anionic ligand; L, L1′ and L2 are the same or different and are each independently a neutral electron donor ligand, wherein at least one L, L1′ and L2 is an N-heterocyclic carbene ligand; and, R and R1 are each independently hydrogen or a substituent selected from the group consisting of C1-C20 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, aryl, C1-C20 carboxylate, C1-C20 alkoxy, C2-C20 alkenyloxy, C2-C20 alkynyloxy, aryloxy, C2-C20 alkoxycarbonyl, C1-C20 alkylthio, C1-C20 alkylsulfonyl and C1-C20 alkylsulfinyl.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: July 6, 2004
    Assignees: California Institute of Technology, Cymetech, LLP
    Inventors: Robert H. Grubbs, Jennifer A. Love, Melanie S. Sanford, Tina M. Trnka, Jason L. Moore
  • Publication number: 20040122072
    Abstract: Disclosed are thermally-stable, anthraquinone colorant compounds (dyes) which contain one or more vinyl groups which render the compounds copolymerizable with reactive vinyl monomers to produce colored, polymeric compositions such as acrylate and methacrylate polymeric materials. The compounds possess good fastness (stability) to ultraviolet (UV) light, good solubility in vinyl monomers, good color strength and excellent thermal stability. Also disclosed are (1) coating composition comprising (i) one or more polymerizable vinyl compounds, (ii) one or more of the dye compounds described above, and (iii) a photoinitiator and (2) polymeric materials, i.e., polymers derived from one or more acrylic acid esters, one or more methacrylic acid esters, one or more other polymerizable vinyl compounds or mixtures of any two or more thereof, having copolymerized therein one or more of the anthraquinone colorant compounds.
    Type: Application
    Filed: November 21, 2003
    Publication date: June 24, 2004
    Inventors: Michael John Cyr, Max Allen Weaver, Gerry Foust Rhodes, Jason Clay Pearson, Phillip Michael Cook, Jos Simon De Wit, Larry Keith Johnson
  • Publication number: 20040121989
    Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.
    Type: Application
    Filed: December 19, 2002
    Publication date: June 24, 2004
    Applicant: G.D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning
  • Publication number: 20040092747
    Abstract: Amide compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Application
    Filed: July 17, 2003
    Publication date: May 13, 2004
    Inventors: Steven Lee Bender, Dilip Bhumaralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
  • Patent number: 6730690
    Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: May 4, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu
  • Patent number: 6689773
    Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form a 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.
    Type: Grant
    Filed: January 22, 2003
    Date of Patent: February 10, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
  • Patent number: 6686065
    Abstract: Organic materials based on [5] helicenes or dibenzofluorenes are shown to have excellent properties for use in electroluminescent devices, including high stability and efficiency and low excimer formation. The materials may advantageously be adapted to have hole transport or electron transport capabilities in addition to emissive properties.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: February 3, 2004
    Assignee: Canon Kabushiki Kaisha
    Inventor: Jian Ping Chen
  • Publication number: 20030232786
    Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    Type: Application
    Filed: January 15, 2003
    Publication date: December 18, 2003
    Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Patent number: 6620955
    Abstract: Chelating ligand precursors for the preparation of olefin metathesis catalysts are disclosed. The resulting catalysts are air stable monomeric species capable of promoting various metathesis reactions efficiently, which can be recovered from the reaction mixture and reused. Internal olefin compounds, specifically beta-substituted styrenes, are used as ligand precursors. Compared to terminal olefin compounds such as unsubstituted styrenes, the beta-substituted styrenes are easier and less costly to prepare, and more stable since they are less prone to spontaneous polymerization. Methods of preparing chelating-carbene metathesis catalysts without the use of CuCl are disclosed. This eliminates the need for CuCl by replacing it with organic acids, mineral acids, mild oxidants or even water, resulting in high yields of Hoveyda-type metathesis catalysts.
    Type: Grant
    Filed: November 15, 2002
    Date of Patent: September 16, 2003
    Inventors: Richard L. Pederson, Jason K. Woertink, Christopher M. Haar, David E. Gindelberger, Yann Schrodi
  • Patent number: 6610723
    Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: August 26, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Patent number: 6608175
    Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: August 19, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 6605630
    Abstract: The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: August 12, 2003
    Assignee: Syngenta Limited
    Inventor: Michael Barry Gravestock
  • Publication number: 20030143422
    Abstract: Organic materials based on [5] helicenes or dibenzofluorenes are shown to have excellent properties for use in electroluminescent devices, including high stability and efficiency and low excimer formation. The materials may advantageously be adapted to have hole transport or electron transport capabilities in addition to emissive properties.
    Type: Application
    Filed: December 12, 2001
    Publication date: July 31, 2003
    Inventor: Jian Ping Chen
  • Patent number: 6589914
    Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: July 8, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
  • Publication number: 20030105331
    Abstract: Derivatives of C2-substituted indan-1-ol compounds, processes for their preparation and their use are disclosed.
    Type: Application
    Filed: August 30, 2002
    Publication date: June 5, 2003
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Patent number: 6566383
    Abstract: Sulphonyltriazoles of the formula wherein Hal, R1, R2 are as defined in the specification are provided along with a process for preparing these compounds and a process using these compounds to control the growth of microorganisms.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: May 20, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Stefan Hillebrand, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Patent number: 6548504
    Abstract: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms o
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: April 15, 2003
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Steven Mark Bromidge, Stephen Frederick Moss
  • Patent number: 6524552
    Abstract: The invention provides a composition of matter of the formula (I): V—L—R where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body, with the provisos that where V is angiotensin or a peptidic angiotensin derivative or analog then V—L—R is other than a non-metal radionuclide substituted peptide (e.g. 125I substituted angiotensin II) and L—V is other than simply a peptide with a chelating agent amide bonded to a side chain thereof. This composition of matter may be used to image cardiovascular diseases and disorders.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: February 25, 2003
    Inventors: Jo Klaveness, Anne Naevestad, Alan Cuthbertson
  • Patent number: 6525086
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: February 25, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6518292
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably,  and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: February 11, 2003
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, James J. Li, Jun Li, Stephen G. Swartz
  • Patent number: 6509473
    Abstract: New energetic salts of 1,2,4-triazole; 3,4,5-triamino-1,2,4-triazole and of 4-amino 1,2,4-triazole were synthesized, characterized and their thermal and safety properties evaluated as possible new propellant ingredients. Energetic anions, including the nitrate anion, NO3, the perchlorate anion, ClO4, & the dinitramide anion, N(NO2)2, were paired with the protonated heterocycles through facile, high yield synthetic routes to give crystalline, energetic salts. Using such a heterocycle system, either 1,2,4-triazole; 3,4,5-triamino-1,2,4-triazole or 4-amino 1,2,4-triazole, a new family of salts were synthesized through the direct reaction of the heterocycle with the corresponding acid form of the desired anion. These reactions were carried out in commonly available polar solvents, and at ambient temperatures, to give high purity, high yield products.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: January 21, 2003
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventor: Greg W. Drake
  • Patent number: 6492525
    Abstract: The invention concerns novel organometallic complexes comprising cationic heterocyclic carbenes. It also concerns a method for preparing said complexes from dicationic heterocyclic precursor compounds. It further concerns the use as catalysts of said organometallic complexes for a certain number of chemical reactions.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: December 10, 2002
    Assignee: Rhodia Fiber & Resin Intermediates
    Inventors: Guy Bertrand, Lutz Stelzig, Olivier Guerret, Christophe Buron, Heinz Gornitzka, Paolo Burattin
  • Patent number: 6426419
    Abstract: The invention discloses ruthenium alkylidene complexes of the type (PCy3)(L)Cl2Ru(CHPh), where L is a triazolylidene ligand of the general formula: These catalysts have been found to be considerably more active for olefin metathesis at elevated temperatures than the parent catalyst (PCy3)2Cl2Ru(CHPh)(2). For example, complex 14 (L=1,3,4-triphenyl-4.5-dihydro-1H-triazol-5-ylidene) is able to catalyze the ring-closing metathesis of substituted dienes to give tetra-substituted cyclic olefins in good yield. In addition, this complex demonstrates the analogous stability towards oxygen and moisture exhibited by ruthenium alkylidene 2.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: July 30, 2002
    Assignee: California Institute of Technology
    Inventors: Robert H. Grubbs, Tina M. Trinka
  • Patent number: 6420375
    Abstract: To provide a novel compound of the formula: [wherein A1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A2 is an aromatic ring which may be substituted, X is a divalent group, Y is a nitrogen atom or a methine group, Z is an ethenylene which may be substituted or ethynylene, R is a heterocyclic group which may be substituted, provided that 3,4-dihydro-6-[3-(1H-imidazol-1-yl)-1-propenyl]-2(1H)-quinolone and 2-[3-[5-ethyl-6-methyl-2-(benzyloxy)-3-pyridyl]-1-propenyl]benzoxazole are excluded.], or a salt thereof which has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating mammals suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: July 16, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuya Aono, Fumio Itoh, Tomohiro Kaku, Masuo Yamaoka
  • Patent number: 6410539
    Abstract: The present invention relates to a compound of Formula (1) wherein Ar1 represent (A) or (B) or (C); R1 is hydrogen, C1-4alkyl or C1-4alkanoyl; R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R2 and —(CH2)nR3 are attached to ring carbon atoms; R2 is a group of Formula (II) or R2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; provided that: when n is 0, Ar3 is substituted by R2 in the 4-position and —(CH2)nR3 in the 3- or 5-position; and when n is 1 or 2, Ar3 is substituted by R2 in the 3- or 5-position and —(CH2)nR3 in the 4-position; and R5-R9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: June 25, 2002
    Assignees: Astrazenca UK Limited, Zeneca Pharma SA
    Inventor: Jean-Claude Arnould