Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimide, Etc.) Patents (Class 514/417)
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Patent number: 8124646Abstract: This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.Type: GrantFiled: June 15, 2010Date of Patent: February 28, 2012Assignee: Concert Pharmaceuticals, Inc.Inventor: Julie F. Liu
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Publication number: 20120035238Abstract: The present application relates to the use of one or more compounds of Formula (I) or pharmaceutically acceptable solvates or prodrugs thereof, for treating cancer or for treating or preventing a viral infection.Type: ApplicationFiled: March 2, 2010Publication date: February 9, 2012Applicant: GOFF HILL LIMITEDInventor: William G. Tucker
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Patent number: 8110568Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: GrantFiled: March 18, 2010Date of Patent: February 7, 2012Assignee: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20120028955Abstract: In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 10, 2011Publication date: February 2, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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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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Publication number: 20110319465Abstract: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C?O) (C1-7)alkyl; Ra is (C1-7)alkyl or (C?O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.Type: ApplicationFiled: June 21, 2011Publication date: December 29, 2011Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: William Welsh, Ching Y. Wang, Ni Ai
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Publication number: 20110312965Abstract: The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.Type: ApplicationFiled: December 21, 2009Publication date: December 22, 2011Inventors: Walter Cabri, Giuseppe Giannini, Gianfranco Battistuzzi, Domenico Alloatti, Claudio Pisano, Sabrina Dallavalle, Tiziana Brunetti
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Patent number: 8076369Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.Type: GrantFiled: February 12, 2010Date of Patent: December 13, 2011Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller
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Patent number: 8071579Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.Type: GrantFiled: November 30, 2004Date of Patent: December 6, 2011Assignees: The Institute of Cancer Research: Royal Cancer Hospital, Kudos Pharmaceuticals LimitedInventors: Alan Ashworth, Stephen Jackson, Niall Martin, Graeme Smith
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Publication number: 20110275630Abstract: Compounds having the formula: are useful for inhibiting protein kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: November 3, 2010Publication date: November 10, 2011Applicant: ABBOTT LABORATORIESInventors: Mark Matulenko, Tammie Jinkerson, Brian S. Brown, Wilfried Braje, Michael Curtin, Howard Robin Heyman, Victoria Scott, Karen Kage, Steven Cassar, Anil Vasudevan
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Publication number: 20110269811Abstract: Compositions and methods of using compositions for treatment of inflammatory diseases and immune disorders are provided. Allylamino compounds are disclosed which are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein 1 (VAP-1). The compounds have therapeutic utility in suppressing inflammation and inflammatory responses, and in treatment of several disorders, including multiple sclerosis and stroke.Type: ApplicationFiled: May 3, 2011Publication date: November 3, 2011Inventors: Eric Yanjun WANG, David S. Jones, Anne M. O'Rourke, Mary T. MacDonald, Hongfeng Gao, Huong-thu Ton-Nu, Christina A. Kessler, Matthew D. Linnik
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Publication number: 20110263540Abstract: Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.Type: ApplicationFiled: July 24, 2009Publication date: October 27, 2011Inventors: Yuan-Ping Pang, Nilgun Ereken Tumer, Charles B. Millard
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Publication number: 20110251067Abstract: Three types of trisiloxane surfactants having the basic formula: MDM? are described wherein the substituents on the differing M and M? groups, in conjunction with pendant polyalkylene oxide substituents on the D group render the surfactant resistant to hydrolysis under either basic or acidic conditions outside the pH range of 6.0 to 7.5. The compositions are useful in agricultural, household and cosmetic applications.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Applicant: Momentive Performance Materials Inc.Inventors: George A. Policello, Mark D. Leathermani, Wenqing Peng, Suresh K. Rajaraman, Sophia Xia
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RADIOISOTOPE-LABELED LYSINE AND ORNITHINE DERIVATIVES, THEIR USE AND PROCESSES FOR THEIR PREPARATION
Publication number: 20110250137Abstract: The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.Type: ApplicationFiled: November 26, 2009Publication date: October 13, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLCHAFTInventors: Norman Koglin, Lutz Lehmann, Holger Siebeneicher, Andre Müller, Niels Böhnke -
Publication number: 20110245206Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: February 23, 2011Publication date: October 6, 2011Inventors: XIN JIANG, XIAOFENG LIU, JACK GREINER, STEPHEN S. SZUCS, MELEAN VISNICK
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Patent number: 8030343Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.Type: GrantFiled: October 14, 2003Date of Patent: October 4, 2011Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller
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Publication number: 20110236349Abstract: The present invention provides methods of treating a viral infection in an individual. The methods generally involve administering to an individual an effective amount of an epidermal growth factor receptor (EGF-R) inhibitor.Type: ApplicationFiled: December 16, 2009Publication date: September 29, 2011Inventors: Jonathan L. Koff, Jay A. Nadel
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Patent number: 8026269Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.Type: GrantFiled: February 9, 2009Date of Patent: September 27, 2011Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Publication number: 20110230452Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: September 23, 2010Publication date: September 22, 2011Inventor: Irving Sucholeiki
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Publication number: 20110224274Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.Type: ApplicationFiled: June 25, 2009Publication date: September 15, 2011Inventors: Bernard Thomas Golding, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcasctle, Eric Valeur, Anna Frances Watson, Martin Noble
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Publication number: 20110212078Abstract: This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: June 24, 2009Publication date: September 1, 2011Inventors: Panduranga Adulla P. Reddy, Umar Faruk Mansoor, M. Arshad Siddiqui
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20110195935Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.Type: ApplicationFiled: September 24, 2009Publication date: August 11, 2011Inventor: Michael Farber
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Publication number: 20110190368Abstract: Organosulfur compounds of the general formula (2) are described, wherein R1 and R2 are linear or branched C1-C5 alkyl; linear or branched C1-C5 alkenyl with the proviso that R1 is not prop-1-enyl (allyl); substituted linear or branched C1-C5 alkenyl or substituted linear or branched C1-C5 alkyl, in which the substituents are selected from OR3, NR4R5, COOR6, CON—R7R8, in which R3 is selected from H, COR9, para-methoxybenzyl and trialkylsilyl, in which R9 is alkyl or substituted alkyl; R4 N and R5 are alkyl or R4 and R5 together form a phthalimido group; R6 is alkyl or substituted alkyl; and R7 and R8 are alkyl or substituted alkyl; substituted or unsubstituted aromatic specifically where R1 and R2 are benzyl, para-methoxybenzyl and/or ortho,para-methoxybenzyl and substituted or unsubstituted heteroaromatic. The compounds can be used for inhibiting the growth of tumour cells and for treating cancer. A pharmaceutical composition and a method of preparing the compounds are also described.Type: ApplicationFiled: August 5, 2009Publication date: August 4, 2011Applicant: University of Cape TownInventors: Catherine Hart Kaschula, Roger Hunter, Mohamed Iqbal Parker
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Publication number: 20110189294Abstract: A formulated composition suitable for controlling or preventing pathogenic damage in a plant comprising (A) at least one solid active ingredient having a water solubility of at most 100 ?g/litre at 25° C. at neutral pH, in an amount of at least 1 weight %, based on the total weight of the formulated composition, (B) at least one non-ionic surface active compound having a hydrophile-lipophile balance (HLB) of between 10 and 18, one or more customary formulation auxiliaries, and water; wherein active ingredient (A) is suspended or dispersed in the water, the weight ratio of surface active compound (B) to active ingredient (A) is in the range of from 1.5 to 15.0, provided the minimum amount of surface active compound (B) is at least 6 weight %, based on the total weight of the formulated composition. Also a method of improving pesticide residue levels in agriculture.Type: ApplicationFiled: May 25, 2009Publication date: August 4, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Jason Keiper, Joshua Koon, Sarah Beth Cush, Michael James Hopkinson, Johnny D. Reynolds, Jorge Cisneros, Jennifer Peterson, Roy Boykin
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Patent number: 7960567Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: GrantFiled: April 30, 2008Date of Patent: June 14, 2011Assignee: Amgen Inc.Inventors: Matthew Brown, Michael G. Johnson, An-Rong Li, Jiwen Liu, Sarah E. Lively, Julio C. Medina, Wang Shen, Xuemei Wang, Yingcai Wang
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Publication number: 20110136824Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: February 14, 2011Publication date: June 9, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110130436Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Publication number: 20110124702Abstract: Provided are compositions and methods for preparation and administration of an oral nanosuspension of a poorly soluble drug with improved bioavailability. The method is optimized through microfluidization process with water soluble polymeric excipients in the absence of surfactants.Type: ApplicationFiled: November 9, 2010Publication date: May 26, 2011Inventors: Ming J. CHEN, Ho-Wah Hui, Thomas Lee, Paul Kurtulik, Sekhar Surapaneni
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Patent number: 7943657Abstract: Imidoalkancarboxylic acids of formula: are described, wherein A, X and M are as defined in the application, said acids being in a crystalline form which in contact with water gives rise to crystals having sizes lower than 30 micron.Type: GrantFiled: February 29, 2008Date of Patent: May 17, 2011Assignee: Solvay Solexis S.p.A.Inventors: Ugo Piero Bianchi, Roberto Garaffa
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Patent number: 7939557Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: GrantFiled: April 19, 2007Date of Patent: May 10, 2011Assignee: Nova Southeastern UniversityInventors: Appu Rathinavelu, Nagarajan Pattabiraman, Jayalakshmi Sridhar, Sivanesan Dakshanamurthy
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Publication number: 20110081555Abstract: A stable, aqueous suspension concentrate which includes a solid polymeric dispersant comprising one or more anionic polymeric dispersing agents, optionally a co-dispersant which preferably is a homopolymer and/or a copolymer of a heterocyclic vinyl lactam, preferably in a wt. ratio of 0.1:1 to 1:0.1, a UV-labile, water-insoluble biocide active, and a UV-blocker or UV-absorber to stabilize said active upon storage and/or exposure to sunlight or UV radiation.Type: ApplicationFiled: December 13, 2010Publication date: April 7, 2011Applicant: ISP INVESTMENTS INC.Inventors: Xianbin Liu, Karen Winkowski, Kolazi S. Narayanan, Jean-Jacques Gulka
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Patent number: 7893102Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.Type: GrantFiled: January 30, 2009Date of Patent: February 22, 2011Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Publication number: 20110039802Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylone, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereofType: ApplicationFiled: July 2, 2010Publication date: February 17, 2011Inventors: Yasuyuki KAWANISHI, Hideyuki TAKENAKA, Kohji HANASAKI, Tetsuo OKADA
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Publication number: 20110038832Abstract: Provided herein are methods of treating macular degeneration, which comprises administering to a patient in need thereof a therapeutically effective amount of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: August 16, 2010Publication date: February 17, 2011Inventor: Jerome B. ZELDIS
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Publication number: 20110003878Abstract: The invention relates to novel compounds of general formula (I), or one of the salts thereof, particularly one of the pharmaceutically acceptable salts thereof, or one of the corresponding solvates thereof. These compounds are inhibitors of the histone deacetylase enzymes and are suitable as pharmacologically active agents in a medicament for the treatment and/or prophylaxis of disorders or diseases associated with histone deacetylases. The invention also relates to a process for obtaining the mentioned compounds and the pharmaceutical compositions containing them.Type: ApplicationFiled: June 20, 2007Publication date: January 6, 2011Applicant: UNIVERSIDAD DE GRANADAInventors: Jose Antonio Gomez Vidal, Jose Francisco Dominguez Seglar, Mavys Tabraue Chavez
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Publication number: 20100324108Abstract: This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.Type: ApplicationFiled: June 15, 2010Publication date: December 23, 2010Inventor: Julie F. LIU
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Publication number: 20100324107Abstract: The present invention refers to the use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, which have important activities in increasing the gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-? levels and an exogenous source of nitric oxide. More particularly, the present invention describes the use of such phthalimide and/or sulphonamide derivatives for the treatment of sickle-cell disease. The invention also has as a novel characteristic the disclosure of new functionalized phthalimide derivatives designed from the prototypes thalidomide and hydroxyurea, and designed rationally through the strategy of molecular hybridization for the treatment of said diseases.Type: ApplicationFiled: December 12, 2008Publication date: December 23, 2010Applicants: UNIVERSIDADE ESTADUAL DE CAMPINAS - UNICAMP, UNIVERSIDADE FEDERAL DO RIO DE JANEIRO - UFRJInventors: Jean Leandro Dos Santos, Chin Chung Man, Lidia Moreira Lima, Fernando Ferreira Costa, Carolina Lanaro
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Publication number: 20100292237Abstract: The present invention relates to the use of an active compound that inhibits the mitochondrial breathing chain at the level of the b/c1 complex for combating phytopathogenic fungi.Type: ApplicationFiled: March 20, 2007Publication date: November 18, 2010Applicant: BASF SEInventors: Erich Birner, Luis Carlos Mateo Garcia
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Publication number: 20100273853Abstract: A compound of formula (1) or a pharmaceutically acceptable derivative thereof, where R1, R2, R3, R4, R5, X and Y are as defined in the specification; corresponding processes for preparing; pharmaceutical compositions comprising; and medicinal uses of such compounds.Type: ApplicationFiled: August 16, 2007Publication date: October 28, 2010Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy, David George Livermore, Helen Susanne Price, Martin Edward Swarbrick
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100247659Abstract: Novel methods are provided to prevent blindness associated with diabetic macular edema by administration of a phenylphthalimide analog. Additionally, sustainability of the effect of administration of the phenylphthalimide analog is improved via encapsulation with poly(lactic-co-glycolic acid) nanoparticles. Finally, a novel method for synthesizing (2,6-diisopropylphenyl)-5-amino-1H-isoindole-1,3-dione is disclosed.Type: ApplicationFiled: July 24, 2009Publication date: September 30, 2010Applicant: Charlesson, LLCInventors: Dumitru Ionescu, CherylAnn Love, Danyang Chen, Ronald Andrew Wassel
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Publication number: 20100227811Abstract: The present invention concerns farnesylamine derivatives, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of ras-mediated signal transduction and inhibitors of aberrant cell growth, e.g., as anti-cancer agents, as well as anti-fungal agents. Other non-malignant diseases characterized by proliferation of cells that may be treated using the farneylamine derivatives of the include, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.Type: ApplicationFiled: May 14, 2008Publication date: September 9, 2010Applicant: University of South FloridaInventors: Ravi Kothapalli, Kirpal S. Bisht
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Publication number: 20100204252Abstract: The present invention relates to a method of treating hypertension in a subject or patient needing treatment thereof by administering to said subject or patient at least one angiotensin II receptor blocker in combination with chlorthalidone.Type: ApplicationFiled: December 22, 2009Publication date: August 12, 2010Applicant: TAKEDA PHARMACEUTICALS NORTH AMERICA, INC.Inventor: Stuart R. Kupfer
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Publication number: 20100197676Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].Type: ApplicationFiled: April 1, 2010Publication date: August 5, 2010Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
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Publication number: 20100184762Abstract: The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, —C1-20-alkyl, —C2-20-alkenyl, —C2-20-alkinyl, —C5-6-cykloalkyl, aryl, aralkyl, adamantyl, heterocyclic, hydroxyl, hydroxyalkyl, Or —N—(R1, R2) group; n is 0, 1, 2, 3, or 4; R1 and R2 may each be independently hydrogen, straight or branching alkyl, cyclo-alkyl, aryl, aralkyl, heterocyclic group, wherein each is un-substituted or halogen substituted; or R1 and R2 together with the nitrogen in between them form a 5 or 6 member ring; A is a single bond, —O—, —S—, —CH2-, or —NH—; Y is O or S; Z is O or S; R? and R? are each independently methyl, ethyl, isopropyl, isobuthyl, sec-butyl or terc-butyl; with the restriction that: X(n) cannot all be fluorine, and A be a single bond, and Y, as well as Z be O, and R?, as well as R? bType: ApplicationFiled: June 20, 2008Publication date: July 22, 2010Applicant: AVIDIN KFTInventors: Laszlo Puskas, Liliana Feher, Eszter Molnar
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Patent number: 7759388Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the ? 4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which ? 4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.Type: GrantFiled: October 16, 2008Date of Patent: July 20, 2010Assignee: Ajinomoto Co., Inc.Inventors: Nobuyasu Suzuki, Toshihiko Yoshimura, Hiroyuki Izawa, Kazuyuki Sagi, Shingo Makino, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Publication number: 20100179187Abstract: This invention provides a method of treating a subject suffering from a cognitive impairment or a cognitive disorder which comprises administering to the subject an amount of an indolone compound effective to treat the subject's cognitive impairment or disorder.Type: ApplicationFiled: January 4, 2010Publication date: July 15, 2010Inventor: Thomas P. Blackburn