Sulfur In Substituent Q Patents (Class 564/85)
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Patent number: 9023850Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: October 5, 2011Date of Patent: May 5, 2015Assignee: E I du Pont de Nemours and CompanyInventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
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Patent number: 8987326Abstract: The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.Type: GrantFiled: January 17, 2014Date of Patent: March 24, 2015Assignee: Cardioxyl Pharmaceuticals, Inc.Inventors: Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost, John P. Toscano
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Patent number: 8877970Abstract: Novel radiopharmaceuticals that are useful in diagnostic imaging and therapeutic treatment of disease characterized by over expression of CA-IX comprise a complex that contains a sulfonamide moiety which is capable of binding the active catalytic site of CA-IX, and a radionuclide adapted for radioimaging and/or radiotherapy:Type: GrantFiled: January 8, 2009Date of Patent: November 4, 2014Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: Craig Zimmerman, John W. Babich, John Joyal, Genliang Lu, Kevin P. Maresca, Chris Barone
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Publication number: 20140315954Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
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Publication number: 20140235636Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Patent number: 8809584Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.Type: GrantFiled: December 21, 2011Date of Patent: August 19, 2014Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
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Publication number: 20140206769Abstract: The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.Type: ApplicationFiled: January 17, 2014Publication date: July 24, 2014Applicant: CARDIOXYL PHARMACEUTICALS, INC.Inventors: Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20140163110Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 10, 2013Publication date: June 12, 2014Applicant: GENENTECH, INC.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
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Publication number: 20140046075Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: ApplicationFiled: January 31, 2013Publication date: February 13, 2014Applicant: THERAVANCE, INC.Inventors: Seok-ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
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Patent number: 8642808Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: GrantFiled: April 22, 2011Date of Patent: February 4, 2014Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Publication number: 20130267568Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and pharmaceutically acceptable salts of the compound of formula (1). The compounds of formula (1), and their salts, possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations, such as inflammatory joint diseases, or other diseases caused by chronic inflammation. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds and their use for the preparation of medicaments for the treatment of humans and animals.Type: ApplicationFiled: April 5, 2012Publication date: October 10, 2013Inventors: Hubert Maehr, Donchu Wei
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Patent number: 8524947Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: GrantFiled: February 23, 2009Date of Patent: September 3, 2013Assignees: University of South Florida, H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Hong-Gang Wang, Roman Manetsch, Xiangdong Hu, Sameer Kulkarni, Jiazhi Sun
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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Publication number: 20130190488Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: December 12, 2012Publication date: July 25, 2013Applicant: Abbott LaboratoriesInventor: Abbott Laboratories
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Publication number: 20130121919Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.Type: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
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Patent number: 8425890Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.Type: GrantFiled: February 23, 2010Date of Patent: April 23, 2013Inventors: David J. Schneider, Charles A. Schneider
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Publication number: 20130096105Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or 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-2, and/or MMP-8, and/or 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-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: November 30, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8242118Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: GrantFiled: April 19, 2010Date of Patent: August 14, 2012Assignee: Axikin Pharmaceuticals Inc.Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
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Patent number: 8193184Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.Type: GrantFiled: April 20, 2008Date of Patent: June 5, 2012Assignee: Unimed Pharma, SPOL, S.R.O.Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
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Patent number: 8093386Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.Type: GrantFiled: July 25, 2007Date of Patent: January 10, 2012Assignee: Bracco Imaging S.p.AInventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
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Patent number: 8008297Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: April 4, 2008Date of Patent: August 30, 2011Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valerie Perron
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Publication number: 20110130568Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: February 23, 2009Publication date: June 2, 2011Inventors: Roman Manetsch, Hong-Gang Wang, Xiandong Hu, Sameer Kulkami, Jiazhi G. Sun
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Publication number: 20110014186Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or 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-2, and/or MMP-8, and/or 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-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: March 23, 2009Publication date: January 20, 2011Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
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Patent number: 7834213Abstract: The present invention provides (I) a method of manufacturing a triphenylmethane colorant that can suppress the sub-reactions in conversion to a sulfonamide and is industrially advantageous, (II) a colorant compound that has both excellent spectral characteristics and a high solubility relative to organic solvents or polymers as a coloring agent to be used in color filters and (III) a blue resist composition for use in a color filter that shows a high lightness and an excellent hue particularly for blue color and can be used to display an image that is excellent in terms of spectral characteristics and contrast.Type: GrantFiled: February 14, 2006Date of Patent: November 16, 2010Assignee: Canon Kabushiki KaishaInventors: Yasuaki Murai, Takayuki Toyoda, Yuko Yamagishi, Takeshi Miyazaki
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Publication number: 20100233617Abstract: A photosensitive composition includes: (A) a resin containing a repeating unit corresponding to a compound represented by the following formula (I); the resin being capable of producing an acid group upon irradiation with an actinic ray or radiation: Z-A-X—B—R ??(I) wherein Z represents a group capable of becoming an acid group resulting from leaving of a cation upon irradiation with an actinic ray or radiation; A represents an alkylene group; X represents a single bond or a heteroatom-containing divalent linking group; B represents a single bond, an oxygen atom or —N(Rx)-; Rx represents a hydrogen atom or a monovalent organic group; R represents a monovalent organic group substituted by Y; when B represents —N(Rx)-, R and Rx may combine with each other to form a ring; and Y represents a polymerizable group.Type: ApplicationFiled: September 18, 2008Publication date: September 16, 2010Applicant: FUJIFILM CORPORATIONInventor: Kenji Wada
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Patent number: 7777076Abstract: Macrocyclic compounds of formula (I), in which B1 and X1 taken together are alkylene which is unsubstituted or substituted with ?O and having one CH2 moiety unreplaced or replaced with CH?CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 17, 2006Date of Patent: August 17, 2010Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Christopher L. Lynch, Xilu Wang
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Patent number: 7741519Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: GrantFiled: February 1, 2008Date of Patent: June 22, 2010Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Publication number: 20100137354Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: May 9, 2008Publication date: June 3, 2010Inventors: Wieslaw M. Cholody, Yi Zang, Karina E. Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel, Norman E. Ohler, Sheela K. Chellappan, Janak Padia
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Publication number: 20100130505Abstract: Disclosed are compositions and methods for treating diseases associated with G protein ?? subunit activity.Type: ApplicationFiled: April 28, 2008Publication date: May 27, 2010Applicant: University of RochesterInventors: Alan V. Smrcka, Burns C. Blaxall, Jean M. Bidlack
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Patent number: 7671235Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.Type: GrantFiled: June 20, 2007Date of Patent: March 2, 2010Assignee: Roche Palo Alto LLCInventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20100041657Abstract: The present invention relates to compounds of formula I, in which at least one of R5, R6 and R7 is SR12, S(O)R12 or S(O)2R12 group where R12 is a C1-6haloalkyl group, that act, as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.Type: ApplicationFiled: May 11, 2006Publication date: February 18, 2010Applicant: NOVO NORDICK A/SInventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Flemming Elmelund Nielsen, Anders Klarskov Petersen
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Patent number: 7598418Abstract: 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 following general formula (I) or a salt thereof: wherein one of R1 and R2 represents hydrogen atom and the other represents the formula —X-A wherein A represents hydrogen atom or an acyl group, X represents oxgen atom or NH; one of R3 and R4 represents hydrogen atom and the other represents the following formula: wherein Y represents a sulfonyl group or a carbonyl group, R5 represents a cyclic group, Z represents a single bond or a C1 to C4 alkylene group, R6 represents hydrogen atom or a C1 to C6 alkyl group.Type: GrantFiled: April 18, 2003Date of Patent: October 6, 2009Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Akiko Itai
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Publication number: 20090069302Abstract: The present invention relates generally to novel therapeutic compounds and AXOR 109 agonists, and processes for the manufacture and use of the same.Type: ApplicationFiled: January 19, 2007Publication date: March 12, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jerzy Ryszard Szewczyk, Christopher P. Laudeman, Thomas Dock, Zibin Chen, Anderson Evans, Yue H. Li
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Publication number: 20080305506Abstract: A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection.Type: ApplicationFiled: August 22, 2008Publication date: December 11, 2008Applicant: GluMetrics Inc.Inventor: Jeff T. Suri
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Publication number: 20080293775Abstract: The invention relates to substituted diphenylethers, -amines, -sulfides, and -methanes as useful pharmaceutical compounds for treating respiratory-disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 12, 2006Publication date: November 27, 2008Applicant: ASTRAZENECA ABInventors: Roger Victor Bonnert, Andrew Cook, Timothy Jon Luker, Rukhsana Tasneem Mohammed, Stephen Thom
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Publication number: 20080293751Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: ApplicationFiled: November 15, 2007Publication date: November 27, 2008Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20080194691Abstract: Compounds of formula (I), in which B1 and X1 are together alkylene which is unsubstituted or substituted with ?O and having one CH2 moiety unreplaced or replaced with CH?CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.Type: ApplicationFiled: May 17, 2006Publication date: August 14, 2008Applicant: Abbott LaboratoriesInventors: Steven W. Elmore, Christopher L. Lynch, Xilu Wang
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Patent number: 7388008Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: August 2, 2004Date of Patent: June 17, 2008Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valérie Perron
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Publication number: 20080119555Abstract: The present invention pertains to certain aryl alkyl sulfonamides and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formula: wherein: Ar1 is independently C5-20aryl (e.g., biphenyl, phenanthryl, fluorenyl, or carbazolyl, most preferably biphenyl), and is optionally substituted; RN is independently —H, acyl, C5-20aryl-C1-7alkyl, C3-20heterocyclyl, or C1-7alkyl, and is optionally substituted; Ralk is a C2-10alkylene group, and is optionally substituted; and Q is independently —H or an organic group having from 1 to 30 atoms selected from carbon, nitrogen, oxygen, sulfur, phosphorus, fluorine, chlorine, bromine, and iodine (e.g., an oxy-type group, an amine-type group, etc.); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: ApplicationFiled: May 23, 2005Publication date: May 22, 2008Inventors: Stuart Hamilton Ralston, Iain Robert Greig, Aymen Ibrahim Idris Mohamed, Robert Jurgen Van 'T Hof
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7250526Abstract: A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal hydrocarbyl complex which is coordinated to defined bidentate ligands substituted with at least one group selected from an optionally substituted sulphonated hydrocarbyl group, a sulphonated perhalogenated hydrocarbyl group, or an optionally substituted sulphonated heterocyclyl group. Preferred metals include rhodium, ruthenium and iridium. Preferred bidentate ligands are diamines and aminoalcohols, particularly those comprising chiral centres. The hydrogen donor is advantageously a secondary alcohol or a mixture of triethylamine and formic acid. The process can be employed to transfer hydrogenate ketones and imines, which are preferably prochiral. Catalysts for use in such a process are also provided.Type: GrantFiled: November 29, 2001Date of Patent: July 31, 2007Assignee: NPIL Pharmaceuticals (UK) LimitedInventors: Andrew John Blacker, Christian Bubert, Jonathan Michael Jeremy Williams, Stephen Martin Brown
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Patent number: 7232817Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 27, 2005Date of Patent: June 19, 2007Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 7227035Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: GrantFiled: May 19, 2004Date of Patent: June 5, 2007Assignee: ChemocentryxInventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Patent number: 7208526Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: April 28, 2006Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Matthias Koerner, Manfred Kubbies, Raymond Lau, Ulrike Reiff, Georg Tiefenthaler, Wolfgang von der Saal, Timothy Woodcock
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Patent number: 7169952Abstract: A process for the preparation of a sulfonamide of formula (II), comprising reacting at elevated temperature an aniline of formula (I), with a sulfonating agent A of the formula R1—SO2-Z in the presence of a catalytic amount of either: (i) an amide B-1, other than N,N-dimethylformamide, or (ii) a high boiling tertiary amine B-2. Also provided in accordance with the present invention are processes for preparing sulfonamides of formula (II) by reacting an aniline of formula (I) with sulfanating agent A of the formula R1—SO2-Z in the presence of N,N-dimethylformamide, at a temperature in the range of about 120° C. to about 160° C. for about three to about seven hours.Type: GrantFiled: June 1, 2001Date of Patent: January 30, 2007Assignee: FMC CorporationInventors: Leland A. Smeltz, Thomas C. Sedergran, Harold C. Jarrow
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Patent number: 7163942Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: January 16, 2007Assignee: Pfizer Inc.Inventors: Michael A. Brodney, Karen J. Coffman
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Patent number: 7161031Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.Type: GrantFiled: February 28, 2003Date of Patent: January 9, 2007Assignees: Temple University - Of The Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
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Patent number: 7161006Abstract: The invention provides compounds of formula I: which are inhibitors of ?-secretase and hence useful in the treatment or prevention of Alzheimer's disease.Type: GrantFiled: September 25, 2003Date of Patent: January 9, 2007Assignee: Merck Sharp & Dohme LimitedInventors: James Michael Crawforth, Jason Matthew Elliott, Andrew Pate Owens, Francine Sternfeld
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Patent number: 7122571Abstract: Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia: wherein: Q1, Q2, n, m, X, Y and R are as defined herein.Type: GrantFiled: December 10, 2002Date of Patent: October 17, 2006Assignee: Temple University - Of The Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M.V. Ramana Reddy
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Patent number: RE39682Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: March 30, 2005Date of Patent: June 5, 2007Assignee: Ramot at Tel Aviv University Ltd.Inventor: Yoel Kloog