Chalcogen Bonded Directly At 2-position Of The Oxazole Ring Patents (Class 548/229)
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Publication number: 20080119476Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: July 1, 2005Publication date: May 22, 2008Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Publication number: 20080119533Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.Type: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: UNIVERSITY OF SOUTH FLORIDAInventors: Edward Turos, Rajesh Kumar Mishra
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Patent number: 7342039Abstract: The present invention relates to substituted indole oximes and methods of using them.Type: GrantFiled: September 23, 2004Date of Patent: March 11, 2008Assignee: WyethInventors: Lisa Marie Havran, John Anthony Butera, Hassan Mahmoud Elokdah, Douglas John Jenkins, Eric Gould Gundersen
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Patent number: 7342035Abstract: In particular, zolmitriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Transesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Saponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Decarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 5, 2003Date of Patent: March 11, 2008Assignee: Inke, S.A.Inventors: Montserrat Armengol Asparo, Pere Dalmases Barjoan
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Patent number: 7332611Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.Type: GrantFiled: May 8, 2006Date of Patent: February 19, 2008Assignee: University of South FloridaInventors: Edward Turos, Rajesh Kumar Mishra
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Publication number: 20080027053Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.Type: ApplicationFiled: July 9, 2007Publication date: January 31, 2008Inventors: Mark J. Macielag, Manomi A. Tennakoon
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Publication number: 20080021079Abstract: Compounds useful for treating cellular proliferative diseases and disorders by inhibiting the activity of KSP are disclosed.Type: ApplicationFiled: May 5, 2004Publication date: January 24, 2008Inventors: Han-Jie Zhou, Gustave Bergnes
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Patent number: 7309791Abstract: The invention relates to new compounds, being 3-phenylpropionic acid derivatives of formula I wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; Z represents NH, N—C1–C10-alkyl, N-aryl, N-heteroaryl, S, or O; X represents O, S, NH, N—C1–C10-alkyl, N-aryl, NSO2—C1–C10-alkyl, N—SO2-aryl, or N—SO2-heteroaryl; R1, to R6 each independently represent hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof. The compounds are the ligands of PPAR-gamma receptor and are useful as medicaments.Type: GrantFiled: January 12, 2006Date of Patent: December 18, 2007Assignee: Adamed Sp. z.o.oInventors: Zbigniew Majka, Katarzyna Ewa Rusin, Dominik Daniel Kludkiewicz, Krzysztof Kurowski, Katarzyna Joanna Matusiewicz, Tomasz Stawinski, Daniel Sulikowski, Piotr Kowalczyk
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Publication number: 20070281978Abstract: This invention relates an inhibitory modulator of AQP4 protein regarding its transmembrane water transport properties, wherein the modulator selectively binds to the AQP4 protein, and inhibits AQP4 mediated water transport.Type: ApplicationFiled: June 1, 2007Publication date: December 6, 2007Applicant: NIIGATA UNIVERSITYInventors: Tsutomu Nakada, Vincent J. Huber
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Patent number: 7294719Abstract: A process for producing N-carboxyanhydrides is disclosed. The process produces N-carboxyanhydrides as a product and HCl as a by-product. The HCl by-product is purged from the reaction mixture by passing a purge gas through the reaction mixture as a carbonylation reagent is reacting with an amino acid or a salt thereof. The N-carboxyanhydrides produced by this process have a relatively lower chloride impurity content, relatively higher yields can be achieved, and the N-carboxyanhydrides can be produced on a larger scale.Type: GrantFiled: October 26, 2005Date of Patent: November 13, 2007Assignee: Sigma-Aldrich Co.Inventors: John Michael Carubia, Thomas Mark Weaver, Ettigounder Ponnusamy
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Patent number: 7285565Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: January 14, 2005Date of Patent: October 23, 2007Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 7279494Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of formula I or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 1, 2004Date of Patent: October 9, 2007Assignee: Pfizer Inc.Inventors: Adam Renslo, Mikhail Fedor Gordeev, Dinesh Vinoobhai Patel, Hongwu Gao, Vara Prasad Venkata Nagendra Josyula
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Patent number: 7279582Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: October 25, 2002Date of Patent: October 9, 2007Assignee: Abbott LaboratoriesInventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
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Patent number: 7273867Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disordersType: GrantFiled: December 5, 2001Date of Patent: September 25, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
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Patent number: 7265140Abstract: The present invention relates to acyloxymethylcarbamate oxazolidinones. The compounds of the present invention have potent activity with excellent oral bioavailability against Gram-positive and Gram-negative bacteria.Type: GrantFiled: September 9, 2004Date of Patent: September 4, 2007Assignee: Pfizer IncInventors: Vara Prasad Venkata Nagendra Josyula, Robert C. Gadwood, Lisa Marie Thomasco, Ji-Young Kim, Allison Laura Choy, Frederick Earl Boyer
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Patent number: 7262299Abstract: A process for performing a catalytic Diels-Alder reaction by reacting a diene with a dienophile in the presence of a heterogeneous catalyst comprising a zeolitic material exchanged or impregnated with ions of a Lewis acidic metal is described. The catalyst, for example, copper-exchanged zeolite Y, may be treated with chiral bis(imine) compounds to direct the chirality of the reaction products. The catalyst can be separated from the reaction mixture and re-used in further Diels Alder reactions.Type: GrantFiled: October 31, 2002Date of Patent: August 28, 2007Assignee: Johnson Matthey PLCInventors: Neil Aubrey Caplan, Frederick Ernest Hancock
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Patent number: 7259263Abstract: The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.Type: GrantFiled: June 29, 2005Date of Patent: August 21, 2007Assignee: Jansen Pharmaceutica N.V.Inventors: Dennis J. Hlasta, Craig A. Zificsak
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Patent number: 7238814Abstract: The invention describes compositions and kits comprising 4-aza-4-(2-methyl-2-sulfanylpropyl) tricyclo(5.2.1.0<2,6>)dec-8-ene-3,5-dione; 4-aza-4-(2-methyl-2-(nitrosothio)propyl) tricyclo(5.2.1.0<2,6>)dec-8-ene-3,5-dione; 4-{1-methyl-1-((2,4,6-trimethoxyphenyl)methylthio)ethyl}-1,3-oxazolidin-2-one; 2-aAmino-3-methyl-3-((2,4,6-trimethoxyphenyl)methylthio)butan-1-ol; 4-(1-methyl-1-(nitrosothio)ethyl)-1,3-oxazolidin-2-one; or pharmaceutically acceptable salts thereof. The compositions of the invention can further comprise at least one penetration enhancer, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.Type: GrantFiled: February 20, 2004Date of Patent: July 3, 2007Assignee: NitroMed, Inc.Inventors: Przemyslaw A. Marek, Andzrej M. Trocha, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson
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Patent number: 7223870Abstract: Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.Type: GrantFiled: August 21, 2003Date of Patent: May 29, 2007Assignee: Pfizer Inc.Inventors: Arun Ghosh, Stephane Caron, Janice E. Sieser
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Patent number: 7211668Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucType: GrantFiled: April 6, 2004Date of Patent: May 1, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
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Patent number: 7199143Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein —N-HET is, for example, (Ic) or (If) wherein R1 is, for example, halogen or a (1–4C)alkyl group which is substituted by one substituent selected from, for example, hydroxy, (1–4C)alkoxy, amino, cyano or azido; Q is selected from, for example, Q1 wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: February 25, 2003Date of Patent: April 3, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hales, Folkert Reck, Fei Zhou, Paul Robert Fleming, Daniel Robert Carcanague
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Patent number: 7192954Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: March 20, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Cory R. Theberge, Theresa M. Williams, C. Blair Zartman, Xu-Fang Zhang, Steven N. Gallicchio
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Patent number: 7186844Abstract: A method for producing a cyclic carbamate ester produces the cyclic carbamate ester by reacting an organic compound having at least two halogen atoms per molecule, an amine having at least two hydrogen atoms on a nitrogen atom, and carbon dioxide.Type: GrantFiled: January 3, 2005Date of Patent: March 6, 2007Assignee: Mitsubishi Gas Chemical Co., Inc.Inventor: Kazuto Ikemoto
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Patent number: 7186738Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.Type: GrantFiled: March 16, 2004Date of Patent: March 6, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
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Patent number: 7166607Abstract: The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disordersType: GrantFiled: May 27, 2003Date of Patent: January 23, 2007Assignee: AstraZeneca ABInventors: Roger Bonnert, Stephen Brough, Tony Cook, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
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Patent number: 7160912Abstract: The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.Type: GrantFiled: July 3, 2003Date of Patent: January 9, 2007Assignees: Dr.Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Inventors: Natesan Selvakumar, Jagattaran Das, Sanjay Trehan, Javed Iqbal, Magadi Sitaram Kumar, Ramanujam Rajagopalan, Mamidi Naga Venkata Srinivasa Rao
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Patent number: 7157482Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.Type: GrantFiled: March 16, 2004Date of Patent: January 2, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7115777Abstract: The present inventions relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, the use and manufacture of a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).Type: GrantFiled: May 28, 2003Date of Patent: October 3, 2006Assignee: Novartis AGInventors: Thomas Allmendinger, Peter Furter
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Patent number: 7091196Abstract: The invention provides a family of compounds useful as anti-infective agents and/or anti-proliferative agents, for example, chemotherapeutic agents, anti-fungal agents, anti-bacterial agents, anti-parasitic agents, anti-viral agents, and/or anti-inflammatory agents, and/or prokinetic (gastrointestinal modulatory) agents, having the formula: or pharmaceutically acceptable salts, esters, or prodrugs thereof.Type: GrantFiled: September 25, 2003Date of Patent: August 15, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Deping Wang, Joyce A. Sutcliffe, Adegboyega K. Oyelere, Timothy S. McConnell, Joseph A. Ippolito, John N. Abelson, Dane M. Springer, Joseph M. Salvino, Rongliang Lou, Joel A. Goldberg, Jay J. Farmer, Erin M. Duffy, Ashoke Bhattacharjee
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Patent number: 7087629Abstract: Compounds of formula (I) or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q3 and Q5; R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: March 6, 2003Date of Patent: August 8, 2006Assignee: AstraZeneca ABInventor: Michael Barry Gravestock
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Patent number: 7074785Abstract: Novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of processes for preparing these substances, and their use for controlling pests, and also novel intermediates and their preparation.Type: GrantFiled: September 4, 2002Date of Patent: July 11, 2006Assignee: Bayer Cropscience AGInventors: Thomas Seitz, Martin Füsslein, Johannes Rudolf Jansen, Udo Kraatz, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Christoph Erdelen, deceased
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Patent number: 7049443Abstract: The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compounds and the bioavailability of these oxazolidinone compounds is improved by improving the solubility thereof.Type: GrantFiled: July 12, 2002Date of Patent: May 23, 2006Assignee: Pharmacia & Upjohn CompanyInventor: Jackson B. Hester, Jr.
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Patent number: 7034017Abstract: This invention relates to compounds of formula (I) wherein R1 represents optionally substituted phenyl, R2 represents optionally substituted and the remaining “R” groups are as defined in the specification and claims, as well as a method for making such materials, pharmaceutical compositions containing such materials, and methods of using such materials in medical treatment.Type: GrantFiled: January 28, 2002Date of Patent: April 25, 2006Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
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Patent number: 7030148Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I) where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutical acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: December 21, 2001Date of Patent: April 18, 2006Assignee: Dr. Reddy's Research FoundationInventors: Selvakumar Natesan, Jagattaran Das, Javed Iqbal, Sitaram Kumar Magadi, Srinivasa Rao Naga Venkata Mamidi, Rajagopalan Ramanujam, Baskaran Sundarababu, Braj Bhushan Lohray
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Patent number: 7002020Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.Type: GrantFiled: August 17, 2000Date of Patent: February 21, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
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Patent number: 6992103Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.Type: GrantFiled: November 29, 2002Date of Patent: January 31, 2006Assignee: SmithKline Beecham P.L.C.Inventors: Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Steven James Stanway, Leontine Saskia Trouw
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Patent number: 6979741Abstract: Acetyl Coenzyme A Carboxylase inhibitors, pharmaceutical compositions containing such compounds and the use of such compounds to treat for example, Metabolic Syndrome including atherosclerosis, diabetes and obesity.Type: GrantFiled: February 20, 2003Date of Patent: December 27, 2005Assignee: Pfizer Inc.Inventors: David A. Perry, H. James Harwood
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Patent number: 6967196Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.Type: GrantFiled: February 22, 2000Date of Patent: November 22, 2005Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
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Patent number: 6949537Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 5, 2004Date of Patent: September 27, 2005Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 6943179Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumorsType: GrantFiled: February 27, 2002Date of Patent: September 13, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Patent number: 6939867Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseasesType: GrantFiled: February 28, 2002Date of Patent: September 6, 2005Assignee: Pfizer Inc.Inventors: Robert L. Dow, Ernest S. Paight
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Patent number: 6909005Abstract: The present invention provides an improved (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone product which is prepared by a method which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.Type: GrantFiled: September 11, 2000Date of Patent: June 21, 2005Assignee: AstraZeneca UK LimitedInventor: Rajnikant Patel
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Patent number: 6897230Abstract: Oxazolidinones having a bicyclic[3.1.0]hexane containing moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof, and wherein the variables R1, R2, R3, R4, R4a, A, Ar, HAr, n, r, and s are as defined herein.Type: GrantFiled: April 17, 2002Date of Patent: May 24, 2005Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Milton L. Hammond
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Patent number: 6887995Abstract: The present invention relates to a one-step process to prepare pharmacologically active 2-oxo-5-oxazolidinylmethylacetamides.Type: GrantFiled: April 15, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventors: William R. Perrault, Bruce Allen Pearlman, Delara B. Godrej
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Patent number: 6884813Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein A is a structure i, ii, iii, or iv X is CR7; Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NR-het1, —O-het1, —S-het1, or -het2; and n is independently 0, 1, or 2. The compounds of formula I are useful as antimicrobials against a number of human and veterinary pathogens.Type: GrantFiled: January 21, 2003Date of Patent: April 26, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
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Patent number: 6875784Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: October 2, 2003Date of Patent: April 5, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail Fedor Gordeev, Adam Renslo, Dinesh Vinoobhai Patel
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Patent number: 6869965Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: GrantFiled: December 5, 2003Date of Patent: March 22, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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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