Chalcogen Bonded Directly To The Triazole Ring Patents (Class 514/384)
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Publication number: 20090105230Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: April 23, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20090069178Abstract: An active-compound combination of has very good fungicidal properties.Type: ApplicationFiled: May 24, 2006Publication date: March 12, 2009Applicant: Bayer CorpScience AktiengesellschaftInventors: Anne Suty-Heinze, Burkhard Schutz
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Publication number: 20090062358Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.Type: ApplicationFiled: July 26, 2007Publication date: March 5, 2009Inventors: Ivan Collado Cano, Samuel James Dominianni, Garret Jay Etgen, JR., Cristina Garcia-Paredes, Richard Duane Johnston, Michael Edward Letourneau, Nathan Bryan Mantlo, Michael John Martinelli, Daniel Ray Mayhugh, Ashraf Saeed, Richard Craig Thompson, Xiaodong Wang, David Scott Coffey, Christopher Randall Schmid, Jeffrey Thomas Vicenzi, Yanping Xu
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Publication number: 20090048248Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: December 18, 2006Publication date: February 19, 2009Inventors: Robert J. DeVita, Jianming Bao, Sander G. Mills
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Publication number: 20090030055Abstract: The present invention relates to compositions and methods to modulate ?-secretase and/or to improve cognitive ability. The invention further relates the improved/enhanced cognitive ability in diseased individuals, particularly Alzheimer's Disease patients, and treatment thereof through increased sAPP production. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are compounds preferred for use with the present composition. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP comprising the activation of protein kinase C (PKC) by administering an effective amount of PKC activator(s).Type: ApplicationFiled: May 24, 2007Publication date: January 29, 2009Inventors: Thomas Nelson, Daniel L. Alkon
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Publication number: 20090018176Abstract: The present invention relates to a fungicide composition comprising a N2-phenylamidine derivative and two other fungicide compounds, at least, as well as and the corresponding methods of protection by application of the said composition. This composition is intended for protecting crops against fungal diseases.Type: ApplicationFiled: September 12, 2006Publication date: January 15, 2009Applicant: Bayer CropScience AGInventors: Peter Dahmen, Thomas Seitz, Ulrike Wachendorff-Neumann
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Patent number: 7476743Abstract: 1,2,4-Tiazole-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: October 2, 2003Date of Patent: January 13, 2009Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Xiangping Qian, Gustave Bergnes, David J. Morgans, Jr., Steven David Knight, Dashyant Dhanak
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Patent number: 7446120Abstract: Peptidomimetics of cyclic peptides, and compositions comprising such peptidomimetics are provided. The peptidomimetics have a three-dimensional structure that is substantially similar to a three-dimensional structure of a cyclic peptide that comprises a cadherin cell adhesion recognition sequence HAV. Methods for using such peptidomimetics for modulating cadherin-mediated cell adhesion in a variety of contexts are also provided.Type: GrantFiled: June 12, 2007Date of Patent: November 4, 2008Assignee: Adherex Technologies, Inc.Inventors: Barbara J. Gour, Orest W. Blaschuk, Anmar Ali, Feng Ni, Zhigang Chen, Stephanie D. Michaud, Shoameng Wang, Zenjian Hu
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Publication number: 20080269218Abstract: Disclosed is a triazole derivative represented by the general formula (1) below or a pharmacologically acceptable salt thereof. Also disclosed are a prodrug of such a triazole derivative and an HSP90 inhibitor containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or amino group or the like.Type: ApplicationFiled: March 8, 2006Publication date: October 30, 2008Inventors: Hiroshi Kuramochi, Setsuko Niitsuma, Masaharu Nakamura, Yoshitaka Sato, Seiichi Saito, Arihiro Tomura, Yuh-Ichiro Ichikawa, Yousuke Kasuga
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Publication number: 20080269171Abstract: A fungicidal mixture, comprising (1) 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione (prothioconazole) of the formula I or its salts or adducts and at least one insecticide selected from the group consisting of (2) fipronil of the formula II (3) chlorpyrifos of the formula III (4) thiamethoxam of the formula IV in a synergistically effective amount is described.Type: ApplicationFiled: July 17, 2007Publication date: October 30, 2008Inventors: Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, V. James Spadafora, Thomas Christen
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Publication number: 20080269263Abstract: The present invention relates to novel active substance combinations which contain spiroxamine, which is known, a known azole and a known carboxamide and which are very suitable for controlling undesired phytopathogenic fungi.Type: ApplicationFiled: September 3, 2005Publication date: October 30, 2008Applicant: Bayer Cropscience AGInventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Ralf Dunkel
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Patent number: 7435752Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O)N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: GrantFiled: November 30, 2005Date of Patent: October 14, 2008Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha de la Rosa, Zhi Hong, Stanley Lang
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Publication number: 20080249131Abstract: Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds.Type: ApplicationFiled: May 2, 2008Publication date: October 9, 2008Applicant: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Zhijun Zhang, Robert Hamatake, Martha A. De La Rosa, Esmir Gunic, Zhi Hong, Hong Woo Kim, Yung-hyo Koh, Shahul Nilar, Stephanie Shaw, Nanhua Yao
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Publication number: 20080249151Abstract: Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, and Ar are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: ApplicationFiled: March 28, 2008Publication date: October 9, 2008Inventors: Zachary Kevin Sweeney, Michael Welch
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Publication number: 20080242715Abstract: The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl,Type: ApplicationFiled: August 18, 2006Publication date: October 2, 2008Inventors: Anna Marie Capelli, Elettra Fazzolari, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
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Publication number: 20080227837Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is C1-4 alkyl or C1-6 cycloalkyl optionally substituted by 1 or 2 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; processes for their preparation, interType: ApplicationFiled: June 13, 2006Publication date: September 18, 2008Inventors: Luca Arista, Giorgio Bonanomi, Dieter Hamprecht, Fubrizio Micheli
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Publication number: 20080207716Abstract: The present invention provides dosing regimens for PPAR-alpha agonist and compositions thereof. A further embodiment of the present invention is a solid oral formulation of Propanoic Acid, 2-[4-[3-[2,5-dihy-dro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxyl-2-methyl- comprising 75 ?g or less of Propanoic Acid, 2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl- per dosage unit.Type: ApplicationFiled: January 25, 2006Publication date: August 28, 2008Applicant: Eli Lilly and Company Patent DivisionInventors: Eyas Jamal Abu-Raddad, Michael Arthur Derby, Cynthia Joyce Harris, Daniel Charles Howey, Laura Frey Michael
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Publication number: 20080200518Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: May 18, 2005Publication date: August 21, 2008Applicant: Bayer CropScience AGInventors: Edward J. Barron, Larry Y. Zhang, John W. Lyga, Matthew P. Whiteside
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Publication number: 20080194599Abstract: A method of Controlling mollusc damage to plants in horticulture or agriculture comprises treating the plant's propagation material with a combination of, as active ingredients, at least (a) clothiainidin and prothioconazole, (b) clothiainidin, fluoxastrobin and prothioconazole, (c) clothiainidin, tebuconazole, triazoxide and prothioconazole, (d) imdiacloprid and prothioconazole, (e) thiamethoxam, tebuconazole and fludioxonil, (f) imidacloprid and carboxin, (g) thiamethoxam, tefluthrin, azoxystrobin and tebuconazole, or (h) imidacloprid and tebuconazole.Type: ApplicationFiled: May 29, 2006Publication date: August 14, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Martin Weiss, Franz Brandl
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Publication number: 20080193397Abstract: The invention relates to the use of compounds with certain sulfur and optionally nitrogen atom-containing structures as peroxide decomposers in cosmetic and pharmaceutical agents for treating the skin. The invention also relates to cosmetic and pharmaceutical agents comprising compounds having such structures.Type: ApplicationFiled: May 12, 2006Publication date: August 14, 2008Applicant: BASF AktiengesellscaftInventors: Manfred Kroll, Gerhard Wagenblast, Arne Ptock, Sylke Haremza, Axel Jentzsch
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Patent number: 7407963Abstract: A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing the compound, their use, and processes for preparing them.Type: GrantFiled: June 27, 2005Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Publication number: 20080182857Abstract: Novel triazole derivatives of the formula (I), in which R1-R6 and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: January 25, 2006Publication date: July 31, 2008Inventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20080176850Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: ApplicationFiled: August 25, 2005Publication date: July 24, 2008Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Woo-Hong Kim
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Publication number: 20080176917Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions contaiType: ApplicationFiled: April 12, 2006Publication date: July 24, 2008Inventors: Daniele Andreotti, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli
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Publication number: 20080167357Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; each R2 is independently hydrogen or C1-4alkyl; n is 2, 3, 4 or 5; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; R5 is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a grouType: ApplicationFiled: April 13, 2006Publication date: July 10, 2008Inventors: Dieter Hamprecht, Caterina Mazzoni, Fabrizio Micheli
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Publication number: 20080153701Abstract: Fungicidal mixtures, comprising as active components 1) carbamate oxime ethers of the formula I, in which X is N or CH, and 2) at least one active compound II selected from the group of the azoles, strobilurins, carboxamides, heterocyclic compounds, carbamates, guanidines, antibiotics, nitrophenyl derivatives, sulfur-containing heterocyclyl compounds, organometallic compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine, in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.Type: ApplicationFiled: December 21, 2005Publication date: June 26, 2008Applicant: BASF AktiengesellschaftInventors: Markus Gewehr, Reinhard Stierl, Matthias Niedenbruck
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Publication number: 20080153808Abstract: Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and a pan-alpha-2 receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Applicant: Allergan, Inc.Inventors: Daniel W. Gil, John E. Donello
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Publication number: 20080146544Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Publication number: 20080139560Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.Type: ApplicationFiled: March 7, 2005Publication date: June 12, 2008Inventors: Robert Zelle, Vincent P. Galullo
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Publication number: 20080132506Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: June 5, 2008Inventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20080118564Abstract: New composition of candesartan cilexetil is prepared using up to 20% of carrageenan which suitably stabilized the active ingredient against degradation during the tableting.Type: ApplicationFiled: January 24, 2006Publication date: May 22, 2008Applicant: LEK PHARMACEUTICALS D.DInventors: Zdenka Jerala-Strukelj, Igor Legen
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Patent number: 7361673Abstract: The present invention relates to compositions for controlling plant pests containing the compound of the formula (I) in a mixture with specified fungicidally active compounds.Type: GrantFiled: September 28, 2006Date of Patent: April 22, 2008Assignee: Bayer AktiengesellschaftInventors: Christoph Erdelen, Wolfram Andersch, Klaus Stenzel, Astrid Mauler-Machnik, Wolfgang Krämer
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Patent number: 7348345Abstract: This invention relates to methods of treating an HIV infection with novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts, and methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I.Type: GrantFiled: February 2, 2007Date of Patent: March 25, 2008Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
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Publication number: 20080064688Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: January 20, 2006Publication date: March 13, 2008Inventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 7342037Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: GrantFiled: June 9, 2006Date of Patent: March 11, 2008Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20080039431Abstract: A method of improving the growth of a plant is provided by reducing the incidence of one or more insect-vectored viral infections. The method comprises the step of applying a primary treatment composition in-furrow during planting of a seed or seedling or during transplanting of the plant, wherein the primary treatment composition comprises an effective amount of a fungicide such as prothioconazole.Type: ApplicationFiled: August 1, 2007Publication date: February 14, 2008Inventors: Charles L. Cleary, Richard D. Rudolph, John E. Curtis, George H. Musson
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Patent number: 7329683Abstract: Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11?-HSD1 enzyme. They inhibit the 11?-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11?-hydroxy-glucocorticoids. The 11?-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol.Type: GrantFiled: January 28, 2003Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: James M. Balkovec, Rolf Thieringer, Steven S. Mundt, Anne Hermanowski-Vosatka, Donald W. Graham, Gool F. Patel, Susan D. Aster, Sherman T. Waddell, Steven H. Olson, Milana Maletic
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Patent number: 7317031Abstract: The present invention provides substituted triazole diamine derivatives as selective kinase or dual-kinase inhibitors and a method for treating or ameliorating a selective kinase or dual-kinase mediated disorder.Type: GrantFiled: February 1, 2005Date of Patent: January 8, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ronghui Lin, Shenlin Huang, Steven K. Wetter, Peter J. Connolly, Stuart L. Emanuel, Robert H. Gruninger, Steven A. Middleton
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Patent number: 7309721Abstract: The present invention encompasses compounds or Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: February 27, 2003Date of Patent: December 18, 2007Assignee: Merck + Co., Inc.Inventors: Richard J. Budhu, George A. Doherty, Jeffrey J. Hale, Christopher L. Lynch, Sander G. Mills, William E. Neway, III
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Patent number: 7304082Abstract: Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.Type: GrantFiled: July 21, 2005Date of Patent: December 4, 2007Assignee: SmithKline Beecham CorporationInventors: Joseph P. Marino, Jr., Scott K. Thompson, Daniel Frank Veber
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Patent number: 7208509Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.Type: GrantFiled: March 23, 2004Date of Patent: April 24, 2007Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
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Patent number: 7176226Abstract: This invention relates to crystal form II of 2-[2-(1-chlorocyclopropyl)-3-(2-chloropenyl)-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione of the formula to a process for its preparation and to its use for controlling unwanted microorganisms.Type: GrantFiled: July 10, 2003Date of Patent: February 13, 2007Assignee: Bayer Cropscience AGInventors: Erika Seidel, Ronald Vermeer, Karin Hasenack, Britta Olenik
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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: 7157470Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: May 5, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Patent number: 7144908Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.Type: GrantFiled: March 4, 2002Date of Patent: December 5, 2006Assignee: Glaxo Group LimitedInventors: Diane Mary Coe, Michael John Monteith, Panayiotis Alexandrou Procopiou
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Patent number: 7144911Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: GrantFiled: December 24, 2003Date of Patent: December 5, 2006Assignee: Deciphera Pharmaceuticals LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 7115658Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virusType: GrantFiled: May 9, 2003Date of Patent: October 3, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Peter Scott Dragovich, Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Maria Angelica Linton, John Howard Tatlock, Ru Zhou, Thomas Jay Prins, Melwyn A. Abreo
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 7078424Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: June 24, 2003Date of Patent: July 18, 2006Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 7071223Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: December 30, 2003Date of Patent: July 4, 2006Assignee: Pfizer, Inc.Inventors: Mark A Dombroski, Allen J. Duplantier, Chakrapani Subramanyam