Ring Oxygen In The Additional Hetero Ring Patents (Class 546/281.7)
  • Publication number: 20120015952
    Abstract: 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: Application
    Filed: March 25, 2010
    Publication date: January 19, 2012
    Applicant: Profectus Biosciences, Inc.
    Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
  • Publication number: 20120010183
    Abstract: 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: Application
    Filed: July 11, 2011
    Publication date: January 12, 2012
    Applicant: PFIZER LIMITED
    Inventors: 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
  • Publication number: 20110178065
    Abstract: 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: Application
    Filed: January 13, 2011
    Publication date: July 21, 2011
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20110144163
    Abstract: 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: Application
    Filed: November 10, 2008
    Publication date: June 16, 2011
    Inventors: David G. I. Kingston, Shugeng Cao, Jielu Zhao, Mathis Hodge, Giulio F. Paciotti, Marja S. Huhta
  • Publication number: 20110112071
    Abstract: 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: Application
    Filed: January 18, 2011
    Publication date: May 12, 2011
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
  • Publication number: 20110097347
    Abstract: 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: Application
    Filed: July 9, 2009
    Publication date: April 28, 2011
    Inventors: Uday Saxena, Venkateswarulu Akella
  • Publication number: 20110077160
    Abstract: Compounds having the following generic formula are disclosed.
    Type: Application
    Filed: December 7, 2010
    Publication date: March 31, 2011
    Inventors: 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
  • Publication number: 20110046139
    Abstract: 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: Application
    Filed: April 27, 2009
    Publication date: February 24, 2011
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Patent number: 7893268
    Abstract: 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: Grant
    Filed: July 20, 2006
    Date of Patent: February 22, 2011
    Assignee: University of Toledo
    Inventors: Viranga Tillekeratne, Richard D. Hudson, Mamoun Alhamadsheh
  • Publication number: 20110039865
    Abstract: 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: Application
    Filed: July 8, 2010
    Publication date: February 17, 2011
    Applicant: Bayer CropScience AG
    Inventors: 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
  • Publication number: 20110009455
    Abstract: 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: Application
    Filed: February 5, 2009
    Publication date: January 13, 2011
    Applicant: Merck Patent Gesellschaft
    Inventors: Christoph Saal, Lars Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
  • Publication number: 20100331545
    Abstract: [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: Application
    Filed: October 23, 2008
    Publication date: December 30, 2010
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Hiroshi Takayanagi, Masataka Asagiri, Toshitake Hirai
  • Publication number: 20100324094
    Abstract: 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: Application
    Filed: March 20, 2008
    Publication date: December 23, 2010
    Applicant: The University of Toledo
    Inventors: Viranga Tillekeratne, Richard A. Hudson, Mamoun Alhamadsheh
  • Patent number: 7795267
    Abstract: 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: Grant
    Filed: August 26, 2004
    Date of Patent: September 14, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kohji Fukatsu, Yutaka Nakayama, Naoki Tarui, Masaaki Mori, Hirokazu Matsumoto, Osamu Kurasawa, Hiroshi Banno
  • Patent number: 7781591
    Abstract: 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: Grant
    Filed: June 13, 2007
    Date of Patent: August 24, 2010
    Assignee: Wyeth LLC
    Inventors: 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
  • Publication number: 20100168179
    Abstract: 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: Application
    Filed: March 11, 2010
    Publication date: July 1, 2010
    Inventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
  • Patent number: 7723380
    Abstract: 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: Grant
    Filed: July 19, 2007
    Date of Patent: May 25, 2010
    Assignee: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
  • Publication number: 20100048636
    Abstract: 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: Application
    Filed: November 13, 2006
    Publication date: February 25, 2010
    Inventors: 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
  • Publication number: 20090312316
    Abstract: 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: Application
    Filed: May 17, 2007
    Publication date: December 17, 2009
    Inventors: Barrie Wilkinson, Steven Moss, Ming Zhang
  • Publication number: 20090275756
    Abstract: 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: Application
    Filed: May 17, 2007
    Publication date: November 5, 2009
    Applicants: CHISSO CORPORATION, CHISSO PETROCHEMICAL CORPORATION
    Inventors: Yasuo Urata, Shunji Oshima, Ryousuke Nishibata, Keiichi Kodaki, Hiroyuki Takeuchi, Shuichi Matsui
  • Publication number: 20090258904
    Abstract: 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: Application
    Filed: July 20, 2006
    Publication date: October 15, 2009
    Inventors: Viranga Tillekeratne, Richard D. Hudson, Mamoun Alhamadsheh
  • Patent number: 7589111
    Abstract: 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: Grant
    Filed: February 14, 2005
    Date of Patent: September 15, 2009
    Assignee: Florida State University Research Foundation, Inc.
    Inventors: Robert A. Holton, Phong Vu
  • Publication number: 20090216024
    Abstract: Pioglitazone can be made via a Darzens Condensation reaction in an industrially useful process.
    Type: Application
    Filed: April 27, 2009
    Publication date: August 27, 2009
    Inventors: Jie Zhu, Lambertus Thijs
  • Patent number: 7524869
    Abstract: 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: Grant
    Filed: October 1, 2003
    Date of Patent: April 28, 2009
    Assignee: Florida State University Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Publication number: 20090093479
    Abstract: 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: Application
    Filed: December 17, 2008
    Publication date: April 9, 2009
    Applicant: LOCUS PHARMACEUTICALS, INC.
    Inventors: Martha KELLY, Younghee LEE, Bin LIU, Ted FUJIMOTO, Joel FREUNDLICH, Bruce D. DORSEY, Gary A. FLYNN, Arifa HUSAIN
  • Patent number: 7456302
    Abstract: 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: Grant
    Filed: April 27, 2005
    Date of Patent: November 25, 2008
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Akihiro Imura, Tatsuya Yamaguchi, Yoshihiro Takayanagi, Seishiro Uchida
  • Publication number: 20080227806
    Abstract: 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: Application
    Filed: September 28, 2006
    Publication date: September 18, 2008
    Applicant: AMERICAN LIFE SCIENCE PHARMACEUTICALS
    Inventor: Robert Ternansky
  • Publication number: 20080188527
    Abstract: 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: Application
    Filed: December 10, 2004
    Publication date: August 7, 2008
    Inventor: John R. Cashman
  • Publication number: 20080176841
    Abstract: 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: Application
    Filed: June 13, 2007
    Publication date: July 24, 2008
    Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Patent number: 7390907
    Abstract: 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, d
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: June 24, 2008
    Assignee: Amgen Inc.
    Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
  • Patent number: 7371777
    Abstract: 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: Grant
    Filed: August 16, 2002
    Date of Patent: May 13, 2008
    Assignee: Eisai Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
  • Patent number: 7365095
    Abstract: 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: Grant
    Filed: April 21, 2006
    Date of Patent: April 29, 2008
    Assignee: Wyeth
    Inventors: Gavin David Heffernan, Gary Paul Stack, Jonathan Laird Gross, Dahui Zhou, Hong Gao
  • Patent number: 7345059
    Abstract: 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: Grant
    Filed: December 22, 2005
    Date of Patent: March 18, 2008
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Laurent Hortala, Murielle Rinaldi-Carmona
  • Patent number: 7288567
    Abstract: 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: Grant
    Filed: March 26, 2001
    Date of Patent: October 30, 2007
    Assignee: Methylgene Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
  • Patent number: 7279574
    Abstract: 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: Grant
    Filed: June 18, 2004
    Date of Patent: October 9, 2007
    Assignees: Sumitomo Chemical Company, Limited, Hitachi, Ltd.
    Inventors: Shinya Tanaka, Yoshitaka Takezawa, Hiroyuki Takahashi
  • Patent number: 7256213
    Abstract: 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: Grant
    Filed: January 12, 2006
    Date of Patent: August 14, 2007
    Assignee: Florida State University Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7256203
    Abstract: 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 fr
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: August 14, 2007
    Assignees: 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
  • Patent number: 7250389
    Abstract: 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: Grant
    Filed: February 8, 1999
    Date of Patent: July 31, 2007
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Osamu Sakanaka, Koichi Mitomo, Takayoshi Tamura, Yasushi Murai, Katsuharu Iinuma, Takeshi Teraoka, Kikuko Kuzuhara, Haruki Mikoshiba, Makoto Taniguchi
  • Patent number: 7247735
    Abstract: 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: Grant
    Filed: January 24, 2005
    Date of Patent: July 24, 2007
    Assignee: Infineon Technologies AG
    Inventors: Marcus Halik, Hagen Klauk, Guenter Schmid
  • Patent number: 7230013
    Abstract: 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: Grant
    Filed: February 28, 2005
    Date of Patent: June 12, 2007
    Assignee: Florida State University Research Foundation, Inc.
    Inventors: Robert A. Holton, Weishuo Fang
  • Patent number: 7226944
    Abstract: 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: Grant
    Filed: March 17, 2005
    Date of Patent: June 5, 2007
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7208169
    Abstract: 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: Grant
    Filed: April 16, 2003
    Date of Patent: April 24, 2007
    Assignee: Bayer CropScience LP
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
  • Patent number: 7132425
    Abstract: 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: Grant
    Filed: December 10, 2003
    Date of Patent: November 7, 2006
    Assignee: 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
  • Patent number: 7087768
    Abstract: 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: Grant
    Filed: June 11, 2002
    Date of Patent: August 8, 2006
    Assignee: 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
  • Patent number: 7064124
    Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: June 20, 2006
    Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.
    Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
  • Patent number: 7056946
    Abstract: 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: Grant
    Filed: November 24, 2003
    Date of Patent: June 6, 2006
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7034035
    Abstract: 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, o
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: April 25, 2006
    Assignee: Dow AgroSciences LLC
    Inventors: 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
  • Patent number: 7026352
    Abstract: 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: Grant
    Filed: February 1, 2002
    Date of Patent: April 11, 2006
    Assignees: 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
  • Patent number: 7002017
    Abstract: 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: Grant
    Filed: March 10, 2004
    Date of Patent: February 21, 2006
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Franz Dietrich Klingler, Michael Steigerwald, Richard Ehlenz
  • Patent number: 6992104
    Abstract: 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: Grant
    Filed: December 22, 2003
    Date of Patent: January 31, 2006
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton