Ring Oxygen In The Additional Hetero Ring Patents (Class 549/60)
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Patent number: 7056946Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: June 6, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7045535Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.Type: GrantFiled: March 8, 2002Date of Patent: May 16, 2006Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
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Patent number: 7033727Abstract: A photosensitive composition of the present invention has excellent sensitivity and pattern profile, which comprises an acid generator having a specific structure.Type: GrantFiled: September 24, 2003Date of Patent: April 25, 2006Assignee: Fuji Photo Film Co., Ltd.Inventor: Kunihiko Kodama
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Patent number: 7029606Abstract: A dihydrofuran-containing nonlinear optical chromophore having a ?-electron donor group conjugated to the dihydrofuran group through a ?-electron conjugated bridge group. The nonlinear optical chromophore is a hyperpolarizable chromophore that can be used as an electro-optic modulator in electro-optic devices.Type: GrantFiled: July 24, 2001Date of Patent: April 18, 2006Assignee: University of WashingtonInventors: Larry R. Dalton, Kwan-Yue Jen, Timothy Londergan, William Brenden Carlson, Gregory Phelan, Diyun Huang, Daniel Casmier, Todd Ewy, Nicholas Buker
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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: 7014796Abstract: Nonlinear optically active compounds, methods for making nonlinear optically active compounds, compounds useful for making nonlinear optically active compounds, methods for making compounds useful for making nonlinear optically active compounds, macrostructures that include nonlinear optically active components, and devices including the nonlinear optically active compounds and the macrostructures.Type: GrantFiled: January 15, 2003Date of Patent: March 21, 2006Assignee: University of WashingtonInventors: Kwan-Yue Jen, Hong Ma, Sen Liu, Larry R. Dalton
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Patent number: 6992104Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: December 22, 2003Date of Patent: January 31, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6989446Abstract: Process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.Type: GrantFiled: June 12, 2002Date of Patent: January 24, 2006Assignee: Ciba Specialty Chemicals Corp.Inventors: Michael Tinkl, Samuel Evans, Peter Nesvadba
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Patent number: 6943182Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: May 30, 2002Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Patent number: 6927217Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: GrantFiled: October 16, 2002Date of Patent: August 9, 2005Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
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Patent number: 6906088Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: July 11, 2003Date of Patent: June 14, 2005Assignee: FSU Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Patent number: 6890928Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: September 5, 2003Date of Patent: May 10, 2005Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffrey N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Patent number: 6887869Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
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Patent number: 6881741Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: GrantFiled: June 11, 2002Date of Patent: April 19, 2005Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constanin Yannopoulos
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Patent number: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
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Patent number: 6872837Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: June 27, 2003Date of Patent: March 29, 2005Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6869696Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are —CN, —NO2 or —COOR8; X is —CH, —CR11 or N; and Y is O, —NH, —NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.Type: GrantFiled: May 10, 2002Date of Patent: March 22, 2005Assignee: Sensient Imaging Technologies GmbHInventors: Andreas Richter, Dietmar Keil, Gerhard Diener
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Patent number: 6861446Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: March 1, 2005Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6844358Abstract: This invention provides compounds of Formula I having the structure wherein: A is O, S, or N; B is —(CH2)m—, —CH(OH)—, or carbonyl; R1 is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, or trifluoromethyl; R2 is alkyl of 1-18 carbon atoms, aryl of 6-10 carbon atoms, arylalkyl of 7-15 carbon atoms, Het-alkyl wherein the alkyl moiety is 1-6 carbon atoms; Het is R2a is alkylene of 1-3 carbon atoms; G is oxygen, sulfur, or nitrogen; R3, R4 are each, independently, hydrogen, halogen, alkyl of 1-3 carbon atoms, aryl of 6-10 carbon atoms or a heterocyclic ring of 5 to 7 ring atom containing 1 to 3 heteroatoms selected from oxygen, nitrogen, sulfur; R5 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R7)R8, —C(CH2)nCO2R9, —C(CH3)2CO2R9, —CH(R7)(CH2)nCO2R9, or CH(R7)C6H4CO2R9; R6 is hydrogen, halogen, alkyl of 1-6 carbon atoms, or —OR5; m=1-6; n=1-6; R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; R8 is —CO2R10, —CONHR10, tetrazolType: GrantFiled: November 21, 2002Date of Patent: January 18, 2005Assignee: WyethInventors: Michael S. Malamas, Jay E. Wrobel, Arlene J. Dietrich, Zenan Li, Iwan Gunawan
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Patent number: 6833453Abstract: 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: GrantFiled: October 17, 2001Date of Patent: December 21, 2004Assignee: Pharmacia & Upjohn CompanyInventors: William R. Perrault, Robert C. Gadwood
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Publication number: 20040242593Abstract: 1′-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type-2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.Type: ApplicationFiled: May 20, 2004Publication date: December 2, 2004Inventors: Bob M. Moore, Antonio M. Ferreira, Mathangi Krishnamurthy
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Patent number: 6822106Abstract: Ethylene based polymers having high molecular weights can be obtained in high yields at temperatures of industrial interest, by carrying out the polymerization reaction in the presence of catalysts comprising silicon bridged metallocenes having a particular ligand system containing a heteroatom.Type: GrantFiled: November 3, 2003Date of Patent: November 23, 2004Assignee: Basell Poliolefine Italia S.p.A.Inventors: Tiziano Dall'Occo, Ofelia Fusco, Maurizio Galimberti, Ilya Nifant'ev, Ilya Laishevtsev
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Publication number: 20040214880Abstract: The present invention relates to compounds of formula I, 1Type: ApplicationFiled: March 31, 2004Publication date: October 28, 2004Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 6809113Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: February 27, 2002Date of Patent: October 26, 2004Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6803378Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.Type: GrantFiled: September 25, 2002Date of Patent: October 12, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
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Publication number: 20040181068Abstract: The present invention discloses the identification of the novel inhibitors of farnesyl protein transferase and ras protein farnesylation. The compounds and pharmaceutical compositions disclosed herein are useful in treating diseases associated with farnesyl protein transferase, such as cancer.Type: ApplicationFiled: February 10, 2004Publication date: September 16, 2004Inventor: Rajeev S. Bhide
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Patent number: 6784173Abstract: Compounds of formula I wherein A, R1 and R2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.Type: GrantFiled: June 11, 2002Date of Patent: August 31, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Ulrike Leser-Reiff, Tim Sattelkau, Gerd Zimmermann
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Patent number: 6780879Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 2, 2001Date of Patent: August 24, 2004Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6753432Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.Type: GrantFiled: August 5, 2003Date of Patent: June 22, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Michelangelo Scalone
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Patent number: 6750245Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 6, 2002Date of Patent: June 15, 2004Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6750354Abstract: The invention relates to a process for the alkylation of 3,4-dihydroxythiophene-2,5-dicarboxylic esters or their alkali metal or alkaline earth metal salts with alkylating agents in a polar diluent in the presence of quaternary onium salts.Type: GrantFiled: September 27, 2002Date of Patent: June 15, 2004Assignee: Bayer AktiengesellschaftInventors: Günter Rauchschwalbe, Alexander Klausener, Josef Bremen, Ralf-Ingo Schenkel, Adolf Winkler
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Patent number: 6747154Abstract: A process for preparing a compound of formula 1 from a compound of formula 2 the process comprising reacting in one step the compound of formula 2 with a compound of formula 3 wherein: X− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; R1 is hydroxy, C1-C4-alkyl, C1-C4-alkoxy, CF3, or fluorine; Ar is phenyl, naphthyl, thienyl, and furyl, each optionally mono- or disubstituted with one or two groups selected from C1-C4-alkyl, C1-C4-alkoxy, hydroxy, fluorine, chlorine, bromine, or CF3; Y− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; and R is hydroxy, methoxy, ethoxy, O—N-succinimide, O—N-phthalimide, phenyloxy, nitrophenyloxy, fluorophenyloxy, pentafluorophenyloxy, vinyloxy, 2-allyloxy, —S-methyl, —S-ethyl, or —S-phenyl.Type: GrantFiled: January 9, 2003Date of Patent: June 8, 2004Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Joerg Brandenburg, Waldemar Franz-Augustin Pfrengle, Werner Rall
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Publication number: 20040068120Abstract: Compounds of the formulae Ia and Ib 1Type: ApplicationFiled: December 12, 2001Publication date: April 8, 2004Inventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Patent number: 6716995Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.Type: GrantFiled: August 17, 2001Date of Patent: April 6, 2004Assignee: Lumera CorporationInventors: Diyun Huang, Tim Londergan, Galina K. Todorova, Jingsong Zhu
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Patent number: 6710078Abstract: Compounds of Formula (I): wherein R1, R2, R3, X, Y, Z and Q are as defined in the specification which compounds are inhibitors of Ras farnesyl-protein transferase enzyme (FPTase), and useful in treating ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid and processes for the preparation of said compounds of Formula (I).Type: GrantFiled: August 23, 2002Date of Patent: March 23, 2004Assignee: Wyeth Holdings CorporationInventors: Semiramis Ayral-Kaloustian, Irwin Hollander, Ann Aulabaugh
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Patent number: 6706757Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: October 2, 2002Date of Patent: March 16, 2004Assignee: WyethInventors: Lynne Padilla Greenblatt, Michael Gerard Kelly
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Publication number: 20040034230Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: ApplicationFiled: July 11, 2003Publication date: February 19, 2004Applicant: FSU Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Publication number: 20040034223Abstract: The present invention relates to the preparation of synthons that are used to form modules that, in turn, are used to form two-dimensional close-packed planar arrays, referred to as nanomembranes. In a presently preferred embodiment, a nanomembrane herein constitutes a filter.Type: ApplicationFiled: February 7, 2002Publication date: February 19, 2004Applicant: CoValent Partners, LLC.Inventors: Timothy B. Karpishin, Josh Kriesel, Grant Merrill, Donald B. Bivin, Thomas H. Smith, Martin Stuart Edelstein
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Patent number: 6689794Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: May 10, 2002Date of Patent: February 10, 2004Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Publication number: 20040023999Abstract: Compounds of Formula (IA) and Formula (IB) 1Type: ApplicationFiled: March 21, 2003Publication date: February 5, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Rajashehar Betageri, Mario G. Cardozo, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell, Hossein Razavi
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Patent number: 6683709Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.Type: GrantFiled: February 7, 2002Date of Patent: January 27, 2004Assignee: Rodenstock GmbHInventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Publication number: 20040014979Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: ApplicationFiled: June 25, 2003Publication date: January 22, 2004Applicant: Florida State UniversityInventor: Robert A. Holton
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Publication number: 20040009995Abstract: Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I 1Type: ApplicationFiled: May 28, 2003Publication date: January 15, 2004Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Nalin Subasinghe, Ehab Khalil, Kristi Leonard, Farah Ali, Heather Rae Hufnagel, Jeremy M. Travins, Shelley K. Ballentine, Kenneth T. Wilson, Maxwell D. Cummings, Wenxi Pan, Joan Gushue, Sanath Meegalla, Mark Wall, Jinsheng Chen, M. Jonathan Rudolph, Hui Huang
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6673833Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 2, 2001Date of Patent: January 6, 2004Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6664275Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 2, 2001Date of Patent: December 16, 2003Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6660866Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 2, 2001Date of Patent: December 9, 2003Assignee: PSU Research Foundation, Inc.Inventor: Robert A. Holton
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Publication number: 20030225133Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: ApplicationFiled: March 28, 2003Publication date: December 4, 2003Inventor: Aloke A Dutta
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Publication number: 20030225091Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1Type: ApplicationFiled: November 15, 2002Publication date: December 4, 2003Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Publication number: 20030225282Abstract: This invention provides a process for the arylation of lactones to form to chiral and achiral aryllactones having high enantioselectivity where applicable.Type: ApplicationFiled: March 18, 2003Publication date: December 4, 2003Inventors: Tony Yantao Zhang, Hongbin Zhang, Christophor Scott Proctor