Acyclic Nitrogen Bonded Directly To Chalcogen Patents (Class 546/338)
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Publication number: 20110015396Abstract: Disclosed herein is a class of tunable phenylacetylene compounds as well as compositions and methods for their use as host compounds for ligand binding. In certain examples the hosts report binding events by exhibiting altered spectroscopic properties, such as different fluorescent emission spectra.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: The State of Oregon on behalf of the University of OregonInventors: Michael M. HALEY, Darren W. JOHNSON, Orion B. BERRYMAN, Charles A. JOHNSON, Calden N. STIMPSON
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Publication number: 20110003827Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: December 10, 2004Publication date: January 6, 2011Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20100331321Abstract: The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: December 18, 2008Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria E. Ek, Ylva Gravenfors, Jorg Holenz, Alexander Minidis, Gunnar Nordvall, Daniel Sohn, Karl S.A. Vallin, Jenny Viklund, Stefan Von Berg
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Patent number: 7816352Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.Type: GrantFiled: March 10, 2006Date of Patent: October 19, 2010Assignee: The Regents of The University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, Sylvie Barchéchath, Mary Patricia Corr
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Publication number: 20100234364Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 10, 2007Publication date: September 16, 2010Inventors: Arindrajit Basak, Jeff Jin, Jimmie Moore, Andrew M.K. Pennell, Sreenlvas Punna, Solomon Ungashe, Zheng Wei
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Patent number: 7790758Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.Type: GrantFiled: February 13, 2006Date of Patent: September 7, 2010Assignee: Glaxo Group LimitedInventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
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Patent number: 7754888Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: GrantFiled: February 9, 2007Date of Patent: July 13, 2010Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Publication number: 20100144803Abstract: N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: February 16, 2010Publication date: June 10, 2010Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers, Yuanming Zhu, James M. Renga, Vidyadhar B. Hegde, Joseph J. DeMark
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Publication number: 20100113449Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 28, 2009Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
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Patent number: 7709649Abstract: Multi-substituted pyridyl sulfoximines are useful as insecticides.Type: GrantFiled: February 9, 2007Date of Patent: May 4, 2010Assignee: Dow AgroSciences LLCInventors: Yuanming Zhu, Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers
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Patent number: 7705156Abstract: N-Substituted heteroaryl (substituted)alkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 9, 2007Date of Patent: April 27, 2010Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Gregory T. Whiteker, Nneka T. Breaux, John F. Daeuble
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Publication number: 20100056579Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 11, 2009Publication date: March 4, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
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Publication number: 20090318511Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: March 27, 2007Publication date: December 24, 2009Inventors: Thomas Leutert, Jonathan E. Grob, Ruben Alberto Tommasi, Erin E. Pusateri, Ayako Honda
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Publication number: 20090264480Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: January 2, 2009Publication date: October 22, 2009Applicant: Abbott LaboratoriesInventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
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Patent number: 7604815Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 9, 2007Date of Patent: October 20, 2009Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
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Patent number: 7572819Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consistingType: GrantFiled: February 9, 2007Date of Patent: August 11, 2009Assignee: Glaxo Group LimitedInventors: Daniel Marcus Bradley, Kevin Michael Thewlis, Simon Edward Ward
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Patent number: 7547716Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: wherein R represents an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, a cycloalkyl-substituted alkyl group, or a cyclic hydrocarbon group wherein said cyclic hydrocarbon group may be saturated, partly saturated, or aromatic; or Z may bind to R to form a cyclic structure, Z represents a hydrogen atom or a C1 to C6 alkyl group. The medicament enhanced the effect of the cancer therapy and decreases a dose of an anticancer agent and/or radiation, and therefore, can reduce side effects resulting from the cancer therapy.Type: GrantFiled: June 7, 2002Date of Patent: June 16, 2009Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Masayuki Komukai, Akiko Itai
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Publication number: 20090088459Abstract: The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: ApplicationFiled: September 17, 2008Publication date: April 2, 2009Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
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Publication number: 20090024096Abstract: A method for immobilizing dyes and antimicrobial agents on a porous surface is disclosed and described. The surface may be that of a medical device, such as a catheter, a connector, a drug vial spike, a bag spike, a prosthetic device, an endoscope, and surfaces of an infusion pump. The surfaces may also be one or more of those associated with a dialysis treatment, such as peritoneal dialysis or hemodialysis, where it is important that working surface for the dialysis fluid be sterile. These surfaces include connectors for peritoneal dialysis sets or for hemodialysis sets, bag spikes, dialysis catheters, and so forth. A method for determining whether a surface has been sterilized, and a dye useful in so indicating, is also disclosed.Type: ApplicationFiled: July 20, 2007Publication date: January 22, 2009Applicants: BAXTER INTERNATIONAL INC., BAXTER HEALTHCARE S.A.Inventors: TON THAT HAI, Mark A. Nordhaus, Vadim V. Krongauz, Kent L. Lurvey
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Publication number: 20080312298Abstract: This invention relates to CARM1, CARM1 binding pockets, or CARM1-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to CARM1 protein, complexes of CARM1 protein, homologs thereof, or CARM1-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising a CARM1 protein or homologs thereof. The invention also relates to methods of identifying binders of CARM1 proteins. The invention also relates to methods for determining the intracellular activity of CARM1 methyltransferase and methods for identifying an agent that inhibits the intracellular activity of CARM1 methyltransferase.Type: ApplicationFiled: April 11, 2008Publication date: December 18, 2008Inventors: Kenneth William Foreman, Salam Shaaban, Frances E. Park, Michael Sauder
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Publication number: 20080280915Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: November 13, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Publication number: 20080167351Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.Type: ApplicationFiled: February 13, 2006Publication date: July 10, 2008Inventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
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Publication number: 20080167472Abstract: Disclosed herein is a class of tunable phenylacetylene compounds as well as compositions and methods for their use as host compounds for ligand binding. In certain examples the hosts report binding events by exhibiting altered spectroscopic properties, such as different fluorescent emission spectra.Type: ApplicationFiled: December 14, 2007Publication date: July 10, 2008Inventors: Michael M. Haley, Darren W. Johnson, Orion B. Berryman, Charles A. Johnson, Calden N. Stimpson
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Publication number: 20080161187Abstract: Biphenylsulfonamides of the formula (I) and the N-oxides and the agriculturally acceptable salts and the veterinarily acceptable salts of the compounds I, a process for preparing these compounds, compositions comprising them, their use for controlling phytopathogenic harmful fungi and harmful arthropodes, a method for combating arthropodal pests, a method for protecting crops from attack or infestation of arthropodal pests, a method for protecting seed and non-living materials from infestation by arthropodal pests, a method for protecting non-living materials from attack or infestation by arthropodal pests and seed comprising the compounds I.Type: ApplicationFiled: March 15, 2006Publication date: July 3, 2008Applicant: BASF AktiengesellschaftInventors: Wassilios Grammenos, Joachim Rheinheimer, Jan Klaas Lohmann, Thomas Grote, Michael Puhl, Christopher Koradin, Ernst Baumann, Wolfgang Von Deyn, Jurgen Langewald, Norbert Gotz, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Henry Van Tuyl Cotter, David G. Kuhn
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Publication number: 20080108667Abstract: Multi-substituted pyridyl sulfoximines are useful as insecticides.Type: ApplicationFiled: February 9, 2007Publication date: May 8, 2008Inventors: Yuanming Zhu, Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers
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Patent number: 7148239Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.Type: GrantFiled: July 10, 2003Date of Patent: December 12, 2006Assignee: CytRx CorporationInventors: László Vígh, Péter Literáti Nagy, Jenó Szilbereky, László Ürögdi, Andrea Jednákovits, László Jaszlits, Katalin Bíró, Ede Márványos, Mihály Barabás, Erzsébet Hegedüs, László Korányi, Mária Kürthy, Gábor Balogh, Ibolya Horváth, Zsolt Török, Éva Udvardy, György Dormán, Dénes Medzihradszky, Bea Mézes, Eszter Kovács, Ernó Duda, Beatrix Farkas, Attila Glatz
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Patent number: 7109203Abstract: Sulfonamide derivitives of the formula I wherein R1-R6 are as defined in the description, processes for their production, their use as pharmaceuticals, particularly for use in the treatment or prevention of diseases in which bradykinin B1 receptor activation plays a role or is implicated, and pharmaceutical compositions comprising themType: GrantFiled: May 13, 2002Date of Patent: September 19, 2006Assignee: Novartis AGInventors: Terance W Hart, Timothy J Ritchie
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Patent number: 6936597Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.Type: GrantFiled: March 21, 2002Date of Patent: August 30, 2005Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6916934Abstract: The present invention relates to an efficient process for preparing derivatives of 1-(pyridinyl)-1,1-dialkoxy-2-aminoethane of the formula (I), with which compounds of the formula (I) can be prepared in high purity and yield and in the form of the free base without isolating the acetylpyridine oxime of the formula (XI) which is a critical product from a safety point of view as a solid.Type: GrantFiled: January 26, 2004Date of Patent: July 12, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Hans-Wolfram Flemming, Gerhard Korb, Juergen Mueller-Lehar, Walter Weber
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Patent number: 6900353Abstract: The present invention provides compounds of formula (I): useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: September 28, 2001Date of Patent: May 31, 2005Assignee: Eli Lilly and CompanyInventors: Buddy Eugene Cantrell, Winton Dennis Jones, Jr., Timothy Alan Shepherd, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6800651Abstract: The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same.Type: GrantFiled: November 20, 2002Date of Patent: October 5, 2004Assignee: Eli Lilly and CompanyInventors: Darrell Stephen Coleman, Gunnar Erik Jagdmann, Kirk Willis Johnson, Michael Parvin Johnson, Thomas Hallett Large, James Allen Monn, Darryle Darwin Schoepp, Thomas Charles Britton, Steven Scott Henry, Joseph Patrick Tizzano
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Patent number: 6747027Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: June 8, 2004Assignee: Pharmacia CorporationInventors: Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
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Patent number: 6703425Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disordersType: GrantFiled: November 15, 2002Date of Patent: March 9, 2004Assignee: Eli Lilly and CompanyInventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6653326Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively; an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxyl amine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.Type: GrantFiled: December 7, 1999Date of Patent: November 25, 2003Assignee: Biorex Research & Development Co.Inventors: László Vígh, Péter Literáti Nagy, Jenó Szilbereky, László Ürögdi, Andrea Jednákovits, László Jaszlits, Katalin Bíró, Ede Màrvànyos, Mihály Barabás, Erzsébet Hegedüs, László Korányi, Mária Kürthy, Gábor Balogh, Ibolya Horváth, Zsolt Török, Éva Udvardy, György Dormán, Dénes Medzihradszky, Bea Mézes, Eszter Kovács, Ernö Duda, Beatrix Farkas, Attila Glatz
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Patent number: 6589967Abstract: The present invention relates to novel oxime O-ether compounds represented by a general formula [I]; wherein R1 represents C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, etc., m represents an integer of 1 to 4, R2 represents hydrogen atom, C1-6 alkyl, etc., R3 and R4 each independently represents hydrogen atom or C1-6 alkyl, etc., R5 represents hydrogen atom, C1-6 alkyl, etc., R6 represents C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, Halogen atom, etc. and n represents an integer of 1 to 4, and a fungicide for agricultural and horticultural use comprising the compound as the active ingredient.Type: GrantFiled: May 6, 2002Date of Patent: July 8, 2003Assignee: Nippon Soda Co. Ltd.Inventors: Hiroshi Sano, Tadashi Sugiura, Yuuki Nakagawa, Hiroshi Hamamura, Akira Mitani, Takahiro Ando
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Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6479550Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.Type: GrantFiled: July 16, 2001Date of Patent: November 12, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller, Hugo Ziegler
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
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Patent number: 6387954Abstract: The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: May 14, 2002Assignee: Eli Lilly and CompanyInventors: Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6297282Abstract: The present application relates to compounds of formula (I) wherein A represents oxygen, sulfur or —NH—, m is 0-2, and R1, R2, R3, R6 and R7 have the meanings given in the specification, to a process for their preparation, as well as to their use in the inhibition of cyclooxygenase II.Type: GrantFiled: October 26, 1999Date of Patent: October 2, 2001Assignee: Nycomed Austria GmbHInventors: Michael Hartmann, Peter Kremminger, Heinz Blaschke, Dagmar Stimmeder, Harald Fellier, Franz Rovenszky
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Patent number: 6180787Abstract: The present invention relates to a novel process for preparing O-(3-amino-2-hydroxy-propyl)-hydroxymic acid halides of formula (I) by reacting a carboxamide oxime of formula (II) wherein R1 is as specified above with reactive 3-amino-2-hydroxy-propane derivative diazotizing the O-substituted carboxamide oxime thus obtained with sodium nitrite in the presence of hydrogen halide, decomposing the diazonium salt and if desired, separating the optically active enantiomers and/or reacting the resulting base with an organic or mineral acid wherein the carboxamide oxime of formula (II) is reacted with a 3-hydroxy azetidinium salt of formula (III) wherein R2 and R3 are a defined above and Y− is a salt forming anion, in a lower alcoholic, preferably ethanolic medium optionally containing water and made alkaline with an alkali hydroxide, and before diazotizing the O-substituted carboxamide oxime intermediate obtained, the reaction mixture is neutralised and the organic solvent is removed.Type: GrantFiled: December 15, 1999Date of Patent: January 30, 2001Assignee: Biorex Kutato es Fejleszto Rt.Inventors: L{acute over (a)}szl{acute over (o)} {umlaut over (U)}rögdi, Mih{acute over (a)}ly Barab{acute over (a)}s, Ede M{acute over (a)}rv{acute over (a)}nyos, Magdolna Török, Zita Cs{acute over (a)}kai
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Patent number: 6127372Abstract: This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: ##STR1## This invention also provides 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 provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.Type: GrantFiled: April 1, 1996Date of Patent: October 3, 2000Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Mark Andrew Murcko, Perry Michael Novak, Govinda Rao Bhisetti
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Patent number: 6075166Abstract: The present invention is to novel photochemically cleavable aryl sulfonamides of the formulaP--A.sub.3 --A.sub.2 --A.sub.1 --S(O).sub.2 NR.sub.1 R.sub.2whereinR.sub.1 and R.sub.2 are independently selected from optionally substituted alkyl, arylalkyl or heteroarylalkyl;A.sub.1 is an aryl or heteroaryl moiety;A.sub.2 is a linking agent is an aryl, heteroaryl, arylalkyl, heteroaryl alkyl, or an alkyl, wherein the alkyl moiety in the arylalkyl, heteroaryl alkyl, or alkyl group is optionally interrupted one or more times independently by oxygen, NR.sub.3, sulfur or an amide group;R.sub.3 is alkyl;A.sub.3 is an electron rich aryl or heteroaryl moiety having an E.sub.1/2 potential of 0.5 to 2.0 and which moiety is capable of forming an exciplex;P is a solid support.Another aspect of the present invention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, for use in non-sequential encoding, as a tagging agent.Type: GrantFiled: March 31, 1995Date of Patent: June 13, 2000Assignee: SmithKline Beecham CorporationInventors: Ravi Shunker Garigipati, Jerry Leroy Adams
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Patent number: 6015822Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastro-intestinal region or for the treatment of diarrheal illnesses.Type: GrantFiled: November 9, 1998Date of Patent: January 18, 2000Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
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Patent number: 5972976Abstract: The invention relates to an aminostilbazole derivative of the following formula or a hydrate thereof, and a salt thereof. ##STR1## wherein R.sup.1 and R.sup.2 each represents hydrogen etc.; R.sup.3, R.sup.4, R.sup.13, and R.sup.14 each represents hydrogen, C.sub.1-3 acyl, halogen, hydroxy etc.; R.sup.5 represents hydrogen or hydroxy-substituted C.sub.1-3 alkyl etc.; R.sup.6 represents benzenesulfonyl substituted by C.sub.1-3 alkoxy etc.; ring Y represents phenyl etc.; ring Z represents 4-pyridyl, its oxide etc. The compound is useful or the treatment of various malignant tumors.Type: GrantFiled: October 2, 1996Date of Patent: October 26, 1999Assignee: Nippon Shinyaku Company, LimitedInventors: Hiroyoshi Hidaka, Akira Matsuura, Masato Matsuda
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Patent number: 5919796Abstract: Hydroximic acid derivatives possess anti-ischemic effects, and therefore, they are useful for treating ischemic states and diseases, such as myocardial ischemia (which may be induced by occlusion of coronary arteries). These derivatives include compounds of formula (I): ##STR1## wherein: X represents a halogen; Z represents an aromatic group, a pyridinyl group, a picolyl group, or a lutidyl group; and R represents an --A--N(R.sub.1)R.sub.2 group, wherein:R.sub.1 and R.sub.2 represent, independently from each other, hydrogen or an alkyl group;or R.sub.1 and R.sub.2, together with the adjacent nitrogen atom, form a 5- to 7-membered,saturated heterocyclic group optionally containing an additional nitrogen, oxygen,or sulfur atom, the heterocyclic group optionally being substituted by at least one alkyl group; andA represents a straight or branched chain alkylene group, as well as pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: November 5, 1996Date of Patent: July 6, 1999Assignee: BIOREX Kutato es Fejleszto Rt.Inventors: Mihaly Barabas, Ede Marvanyos, Laszlo Urogdi, Laszlo Vereczkey, Laszlo Jaszlits, Katalin Biro, Andrea Jednakovits, Erzsebet Radvanyi nee Hegedus, Istvanne Udvardy-Nagy
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Patent number: 5808082Abstract: A process for the preparation of Phosphodiesterase IV inhibitors is described. The process consists of eight chemical steps involving five isolations to prepare the title compound from readily available isovanillin in 35% overall yield (Scheme 1). The process is highlighted by: a) a highly diastereoselective Michael addition of phenyllithium using (1R, 2S) cis-aminoindanol as a chiral auxiliary, b) highly crystalline intermediates providing for efficient purifications, c) crystallization of the final compound as its CSA salt for excellent enantiomeric purity.Type: GrantFiled: April 22, 1997Date of Patent: September 15, 1998Assignee: Merck & Co., Inc.Inventors: Woo-Baeg Choi, Hywyn R. D. Churchill, Joseph E. Lynch, Paul J. Reider, Ralph P. Volante
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Patent number: 5780488Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: March 26, 1997Date of Patent: July 14, 1998Assignee: Merck & Co., Inc.Inventors: Jeffrey Bergman, Christopher Dinsmore
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Patent number: 5756426Abstract: Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom andY is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH andY is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.Type: GrantFiled: September 11, 1995Date of Patent: May 26, 1998Assignee: Novartis CorporationInventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, Rene Zurfluh