Ring Oxygen In The Additional Hetero Ring Patents (Class 546/281.7)
- Plural ring oxygens in the additional hetero ring (Class 546/283.7)
- Polycyclo ring system having the additional hetero ring as one of the cyclos (Class 546/284.1)
- Chalcogen attached directly to the additional hetero ring by nonionic bonding (Class 546/284.4)
- Nitrogen or -C(=X)-, wherein X is chalcogen, attached directly to the additional hetero ring by nonionic bonding (Class 546/284.7)
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Publication number: 20120015952Abstract: The invention relates to compounds of formulae (1) and (2): and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries.Type: ApplicationFiled: March 25, 2010Publication date: January 19, 2012Applicant: Profectus Biosciences, Inc.Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
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Publication number: 20120010183Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 11, 2011Publication date: January 12, 2012Applicant: PFIZER LIMITEDInventors: Andrew Simon Bell, Alan Daniel Brown, Marcel John De Groot, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Nigel Alan Swain, Steven Matthieu Gaulier
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Publication number: 20110178065Abstract: Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel Chu, Bing Wang, Tao Ye
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Publication number: 20110144163Abstract: Thioloated taxane derivatives are linked to colloidal metal particles such as gold nanoparticles for use as antitumor agents. The antitumor agents may be targeted to tumors.Type: ApplicationFiled: November 10, 2008Publication date: June 16, 2011Inventors: David G. I. Kingston, Shugeng Cao, Jielu Zhao, Mathis Hodge, Giulio F. Paciotti, Marja S. Huhta
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Publication number: 20110112071Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
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Publication number: 20110097347Abstract: The present invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (A?42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease and ischemic stroke.Type: ApplicationFiled: July 9, 2009Publication date: April 28, 2011Inventors: Uday Saxena, Venkateswarulu Akella
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Publication number: 20110077160Abstract: Compounds having the following generic formula are disclosed.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
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Publication number: 20110046139Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.Type: ApplicationFiled: April 27, 2009Publication date: February 24, 2011Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
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Patent number: 7893268Abstract: Epothilone analogues include a molecular scaffold which holds at least one segment of epothilone in a predetermined orientation and which rigidities a region between the macrolactone ring and the aromatic side-chain.Type: GrantFiled: July 20, 2006Date of Patent: February 22, 2011Assignee: University of ToledoInventors: Viranga Tillekeratne, Richard D. Hudson, Mamoun Alhamadsheh
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Publication number: 20110039865Abstract: The present invention relates to novel phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.Type: ApplicationFiled: July 8, 2010Publication date: February 17, 2011Applicant: Bayer CropScience AGInventors: Carl Friedrich Nising, Klaus Kunz, Jörg Nico Greul, Hendrik Helmke, Gorka Peris, Jürgen Benting, Peter Dàhmen, Isolde Häuser-Hahn, Ines Heinemann, Christian Paulitz, Dirk Schmutzler, Ulrike Wachendorff-Neumann, Tomoki Tsuchiya, Christoph Andreas Braun, Ruth Meissner, Thomas Knobloch
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Publication number: 20110009455Abstract: The present invention relates to novel compounds of general formula (I) and uses thereof. The present invention relates to novel compounds of general formula (I) for use as glucokinase activators in the treatment of diabetes and obesity.Type: ApplicationFiled: February 5, 2009Publication date: January 13, 2011Applicant: Merck Patent GesellschaftInventors: Christoph Saal, Lars Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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REGULATOR FOR SIGNALING TOLL-LIKE RECEPTOR, WHICH COMPRISES CATHEPSIN INHIBITOR AS ACTIVE INGREDIENT
Publication number: 20100331545Abstract: [Problems] To provide a modulator for signaling of TLR [Means for solving the problems] A medicament containing cathepsin inhibitor such as monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate as a active ingredient is used as a modulator for signaling of TLR, a therapeutic agent for treating diseases associated with TLR signaling, a therapeutic agent for treating diseases associated with induction of Th17 cells, a therapeutic agent for treating diseases associated with production of IL-6, IL-12, IL-17, or IL-23, or a therapeutic agent for treating systemic lupus erythematosus, lupus nephritis, crohn's disease, psoriasis, or acute disseminated encephalomyelitis.Type: ApplicationFiled: October 23, 2008Publication date: December 30, 2010Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Hiroshi Takayanagi, Masataka Asagiri, Toshitake Hirai -
Publication number: 20100324094Abstract: A method for synthesizing anti-leukemic epothilone analogues includes rigidifying a region between the macrolactone ring and the aromatic side-chain. The anti-leukemic compositions are non-naturally occurring epothilone analogue that are rigidified between the macrolactone ring and the aromatic side-chain.Type: ApplicationFiled: March 20, 2008Publication date: December 23, 2010Applicant: The University of ToledoInventors: Viranga Tillekeratne, Richard A. Hudson, Mamoun Alhamadsheh
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Patent number: 7795267Abstract: The present invention provides a compound represented by the formula: wherein R1 is —(C?O)—NR7R8 or —(C?O)—OR6, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.Type: GrantFiled: August 26, 2004Date of Patent: September 14, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Kohji Fukatsu, Yutaka Nakayama, Naoki Tarui, Masaaki Mori, Hirokazu Matsumoto, Osamu Kurasawa, Hiroshi Banno
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Patent number: 7781591Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.Type: GrantFiled: June 13, 2007Date of Patent: August 24, 2010Assignee: Wyeth LLCInventors: Derek Cecil Cole, Diane Harris Boschelli, Yanong Daniel Wang, Magda Asselin, Diane Marie Joseph-McCarthy, Amarnauth Shastrie Prashad, Allan Wissner, Russell Dushin, Biqi Wu, Lawrence Nathan Tumey, Chuan S. Niu, Joan Chen
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Publication number: 20100168179Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
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Patent number: 7723380Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 19, 2007Date of Patent: May 25, 2010Assignee: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Publication number: 20100048636Abstract: The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.Type: ApplicationFiled: November 13, 2006Publication date: February 25, 2010Inventors: John J. Baldwin, David A. Claremon, Colin Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Wei Zhao, Patrick T. Flaherty
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Publication number: 20090312316Abstract: The present invention relates to derivatives of borrelidin that are useful in medicine, e.g. in the treatment of cancer or B-cell malignancies, or other diseases in which angiogenesis contributes to the pathology including ophthalmic disorders such as diabetic retinopathy as well as age related macular degeneration (AMD), corneal neovascularisation and retinopathy or prematurity. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies and other diseases in which angiogenesis is implicated in the pathogenic process.Type: ApplicationFiled: May 17, 2007Publication date: December 17, 2009Inventors: Barrie Wilkinson, Steven Moss, Ming Zhang
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Publication number: 20090275756Abstract: An aldehyde derivative represented by the general formula (2) is reacted with ketene in the presence of a Lewis acid catalyst to produce a novel 2-oxetanone derivative (1), which is then purified to a 2-oxetanone derivative having a high trans-isomer purity, and then converted to a vinyl derivative (3) through decarboxylation reaction.Type: ApplicationFiled: May 17, 2007Publication date: November 5, 2009Applicants: CHISSO CORPORATION, CHISSO PETROCHEMICAL CORPORATIONInventors: Yasuo Urata, Shunji Oshima, Ryousuke Nishibata, Keiichi Kodaki, Hiroyuki Takeuchi, Shuichi Matsui
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Publication number: 20090258904Abstract: Epothilone analogues include a molecular scaffold which holds at least one segment of epothilone in a predetermined orientation and which rigidities a region between the macrolactone ring and the aromatic side-chain.Type: ApplicationFiled: July 20, 2006Publication date: October 15, 2009Inventors: Viranga Tillekeratne, Richard D. Hudson, Mamoun Alhamadsheh
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Patent number: 7589111Abstract: A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3? and an isopropoxycarbamate substituent at C3?.Type: GrantFiled: February 14, 2005Date of Patent: September 15, 2009Assignee: Florida State University Research Foundation, Inc.Inventors: Robert A. Holton, Phong Vu
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Publication number: 20090216024Abstract: Pioglitazone can be made via a Darzens Condensation reaction in an industrially useful process.Type: ApplicationFiled: April 27, 2009Publication date: August 27, 2009Inventors: Jie Zhu, Lambertus Thijs
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Patent number: 7524869Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: October 1, 2003Date of Patent: April 28, 2009Assignee: Florida State University Research Foundation, Inc.Inventor: Robert A. Holton
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Publication number: 20090093479Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.Type: ApplicationFiled: December 17, 2008Publication date: April 9, 2009Applicant: LOCUS PHARMACEUTICALS, INC.Inventors: Martha KELLY, Younghee LEE, Bin LIU, Ted FUJIMOTO, Joel FREUNDLICH, Bruce D. DORSEY, Gary A. FLYNN, Arifa HUSAIN
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Patent number: 7456302Abstract: Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.Type: GrantFiled: April 27, 2005Date of Patent: November 25, 2008Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Akihiro Imura, Tatsuya Yamaguchi, Yoshihiro Takayanagi, Seishiro Uchida
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Publication number: 20080227806Abstract: The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.Type: ApplicationFiled: September 28, 2006Publication date: September 18, 2008Applicant: AMERICAN LIFE SCIENCE PHARMACEUTICALSInventor: Robert Ternansky
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Publication number: 20080188527Abstract: Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.Type: ApplicationFiled: December 10, 2004Publication date: August 7, 2008Inventor: John R. Cashman
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Publication number: 20080176841Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.Type: ApplicationFiled: June 13, 2007Publication date: July 24, 2008Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Patent number: 7371777Abstract: The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRx1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.Type: GrantFiled: August 16, 2002Date of Patent: May 13, 2008Assignee: Eisai Co., Ltd.Inventors: Richard Clark, Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
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Patent number: 7365095Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: April 29, 2008Assignee: WyethInventors: Gavin David Heffernan, Gary Paul Stack, Jonathan Laird Gross, Dahui Zhou, Hong Gao
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Patent number: 7345059Abstract: The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I): where: R1 represents hydrogen or a (C1-C4)alkyl; R2 represents: a monoazo saturated heterocycle of 5 to 7 atoms, the nitrogen atom being substituted with a (C1-C4)alkanoyl; NR10R11; a nonaromatic (C3-C10) carbocycle more than tri-substituted with (C1-C4)alkyl; a nonaromatic (C11-C12) carbocycle unsubstituted or mono- or polysubstituted with (C1-C4)alkyl; a monooxygenated saturated heterocycle with 5 to 7 atoms, more than tri-substituted with (C1-C4)alkyl; or R1 and R2, together with the nitrogen atom to which the above are bonded, form a 4-disubstituted piperidin-1-yl group; the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.Type: GrantFiled: December 22, 2005Date of Patent: March 18, 2008Assignee: Sanofi-AventisInventors: Francis Barth, Laurent Hortala, Murielle Rinaldi-Carmona
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Patent number: 7288567Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 26, 2001Date of Patent: October 30, 2007Assignee: Methylgene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Patent number: 7279574Abstract: The present invention provides a novel epoxy compound, which can be converted into a cured epoxy resin product having liquid crystal properties by curing with a curing agent. Since the cured epoxy resin product of the present invention exhibits good heat conductivity, it is also useful as an insulating material requiring high heat releasability such as a printed circuit substrate and the like.Type: GrantFiled: June 18, 2004Date of Patent: October 9, 2007Assignees: Sumitomo Chemical Company, Limited, Hitachi, Ltd.Inventors: Shinya Tanaka, Yoshitaka Takezawa, Hiroyuki Takahashi
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Patent number: 7256213Abstract: Taxanes having a methylcarbonate or ethylcarbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(13) side chain substituents.Type: GrantFiled: January 12, 2006Date of Patent: August 14, 2007Assignee: Florida State University Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7256203Abstract: A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR17, where R17 is hydrogen or lower alkyl; A and Y are CH, N, NR17, O, or S; C1 and C2 are each C or N, wherein C1 and C2 are the same or different; D1 and D2 are each C or N, wherein D1 and D2 are the same or different; B and Z are CH, N, or NR17, provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR17; R13, R14, R1 and R8 can be present or absent, and when present are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R15 and Rare selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R3 and R6 are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R2, R4, R5 and R7 are each independently selected frType: GrantFiled: November 25, 2003Date of Patent: August 14, 2007Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Richard R. Tidwell, Mohamed A. Ismail, Reto Brun
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Patent number: 7250389Abstract: Disclosed are novel compounds useful for prevention or control of diseases derived from fungi, a process for producing the same, and novel antifungal agents using the novel compounds. The compounds useful for prevention and treatment of diseases derived from fungi according to the present invention include novel compounds represented by formula (I). The compounds represented by formula (I) have potent antifungal activity against diseases derived from fungi, and do not have phytotoxicity to mammals and agricultural and garden plants, from which diseases should be eliminated, and, even when applied to agricultural and garden plants, have high photostability.Type: GrantFiled: February 8, 1999Date of Patent: July 31, 2007Assignee: Meiji Seika Kaisha, Ltd.Inventors: Osamu Sakanaka, Koichi Mitomo, Takayoshi Tamura, Yasushi Murai, Katsuharu Iinuma, Takeshi Teraoka, Kikuko Kuzuhara, Haruki Mikoshiba, Makoto Taniguchi
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Patent number: 7247735Abstract: In the case of the materials according to the invention, the charge carrier mobility in the correspondingly prepared films is achieved if the molecules are composed in such a way that side chains—consisting of conjugated aromatic or heteroaromatic systems—are attached in direct conjugation to a central aromatic or heteroaromatic ring so that the total molecule acquires an octupolar structure. This octupolar structure permits an effective ?-? interaction of the molecules with one another in a manner such that stacking of a plurality of molecules along an imaginary axis (central ring) can take place and various stacks from among these stacks can interact with one another by intermeshing of the side chains. The electronic properties of the materials are determined both by the arrangement of the molecules in a layer and by the molecular design.Type: GrantFiled: January 24, 2005Date of Patent: July 24, 2007Assignee: Infineon Technologies AGInventors: Marcus Halik, Hagen Klauk, Guenter Schmid
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Patent number: 7230013Abstract: Compositions comprising a taxane having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 28, 2005Date of Patent: June 12, 2007Assignee: Florida State University Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Patent number: 7226944Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: March 17, 2005Date of Patent: June 5, 2007Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7208169Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: April 16, 2003Date of Patent: April 24, 2007Assignee: Bayer CropScience LPInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
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Patent number: 7132425Abstract: The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.Type: GrantFiled: December 10, 2003Date of Patent: November 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
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Patent number: 7087768Abstract: The disclosure relates to a fumagillol compound which can be usefully used not only as an angiogenesis inhibiting agent showing a superior angeogenesis inhibitory effect with less toxicity, but also as a cancer metastasis inhibitor and a therapeutic agent against cancer and other various inflammatory diseases such as rheumatic disease, psoriasis, etc., and diabetic retinopathy related to angeogeneois, and also a method for preparing the same.Type: GrantFiled: June 11, 2002Date of Patent: August 8, 2006Assignee: Equispharm Co., Ltd.Inventors: Cheol-Kyu Han, Jeong-Hyeok Yoon, Seung-Moak Kim, Nam-Doo Kim, Byung-Ha Chang, Jee-Young Lee, Tae-Bo Sim
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Patent number: 7064124Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
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Patent number: 7056946Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: June 6, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7034035Abstract: The present invention relates to compounds of Formula I: wherein: a) ?represents a 6-membered heterocyclic aromatic ring in which X1 is N and X2, X3 and X4 are each independently CR?; R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORZ in which RZ is H or C1-C3 alkyl; and c) A represents (i) C3-C14 cycloalkyl, containing 1 or 3 heteroatoms and 0-2 unsaturations, which may be unsubstituted or substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro, aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroarylthio, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or amido unsubstituted or substituted with one or two C1 -C6 alkyl groups, oType: GrantFiled: December 2, 2002Date of Patent: April 25, 2006Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
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Patent number: 7026352Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.Type: GrantFiled: February 1, 2002Date of Patent: April 11, 2006Assignees: Mercian Corporation, Eisai Co., Ltd.Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
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Patent number: 7002017Abstract: The invention relates to a process for preparing the compounds of general formula I by enantioselective hydrogenation of the compounds of formula II in the presence of special hydrogenation catalysts. The invention is characterised by high enantioselectivity, providing easy access to a category of important pharmaceutical compositions, i.e. intermediates for the synthesis of tipranavir.Type: GrantFiled: March 10, 2004Date of Patent: February 21, 2006Assignee: Boehringer Ingelheim International GmbHInventors: Franz Dietrich Klingler, Michael Steigerwald, Richard Ehlenz
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Patent number: 6992104Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: December 22, 2003Date of Patent: January 31, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton