Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
  • Publication number: 20100234405
    Abstract: A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have excellent antiviral properties and are useful as antiviral therapeutic agents: [wherein R represents a nitrogen-containing heterocyclic ring which may have any one of a C1-C3 alkyl group or a C1-C3 alkoxy group as a substituent, or a C1-C6 alkyl group which has one primary amino group as a substituent].
    Type: Application
    Filed: February 15, 2007
    Publication date: September 16, 2010
    Applicant: ARIGEN PHARMACEUTICALS, INC.
    Inventors: Haruhiko Machida, Masaichi Yamamoto
  • Publication number: 20100222372
    Abstract: To provide a therapeutic agent for inflammatory bowel disease. The therapeutic agent for inflammatory bowel disease contains, as an active ingredient, a uracil derivative or a pharmaceutically acceptable salt thereof, represented by formula (1).
    Type: Application
    Filed: October 10, 2008
    Publication date: September 2, 2010
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuki Sakamoto, Fumio Nakagawa
  • Publication number: 20100210672
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
    Type: Application
    Filed: October 1, 2008
    Publication date: August 19, 2010
    Inventors: Barbara Bertani, Francesca Cardullo, Paolo Dambruoso, Paola Marzorati, Fabrizio Micheli, Alessandra Pasquarello, Catia Seri, Giovanna Tedesco
  • Publication number: 20100204471
    Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with MEK that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
    Type: Application
    Filed: October 22, 2007
    Publication date: August 12, 2010
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Qing Dong, Victoria Feher, Stephen W. Kaldor, Naoki Tomita
  • Patent number: 7767670
    Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: August 3, 2010
    Assignee: Ambit Biosciences Corporation
    Inventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
  • Publication number: 20100184772
    Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: October 10, 2007
    Publication date: July 22, 2010
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Helmut H. Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
  • Patent number: 7745426
    Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: June 29, 2010
    Assignees: D-Pharm Ltd., Advanced Neuroprotective Systems Ltd.
    Inventors: Svetlana Dolina, Vitaly Shteiman, Marina Vinnikova, Israel Shapiro
  • Patent number: 7745453
    Abstract: Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S(?O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: June 29, 2010
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Minamo Iwata, Yoshiyuki Taoda
  • Patent number: 7737275
    Abstract: A process is described for preparing 3-phenyl(thio)uracils or 3-phenyldithiouracils of the formula I, by reacting a phenyl iso(thio)cyanate of the formula II with an enamine of the formula III and, if appropriate, in a further step, the resulting 3-phenyl(thio)uracil or 3-phenyldithiouracil of the formula I where R1=R1a, when R1=hydrogen, is reacted with an aminating agent of the formula IV to give 3-phenyl(thio)uracils or 3-phenyldithiouracils of the formula I where R1=amino where the variables R1, R1a, R2, R3, R4, X1, X2, X3, Ar, A and L1 are each as defined in claim 1.
    Type: Grant
    Filed: December 1, 2004
    Date of Patent: June 15, 2010
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Michael Keil, Robert Reinhard, Werner Seitz, Guido Mayer
  • Patent number: 7727988
    Abstract: The present invention relates to novel compounds of formula (I)? or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P1 or a group P2 wherein P1 is and the other groups are define in herein.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: June 1, 2010
    Assignee: Glaxo Group Limited
    Inventors: Barbara Bertani, Giorgio Bonanomi, Anna Maria Capelli, Anna Checchia, Romano Di Fabio, Gabriella Gentile, Fabrizio Micheli, Alessandra Pasquarello, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100130503
    Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R2?, L, Het, p and p? are as defined herein, compositions containing them, and their use as medicinal products.
    Type: Application
    Filed: November 24, 2009
    Publication date: May 27, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Fabienne THOMPSON, Patrick MAILLIET, Jean-Marie RUXER, Helene GOULAOUIC, François VALLEE, Herve MINOUX, Fabienne PILORGE, Luc BERTIN, Stephane HOURCADE, Maria MENDEZ-PEREZ, Peter HAMLEY
  • Patent number: 7718668
    Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4-inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions for use, e.g., in treatment of airway disorders.
    Type: Grant
    Filed: March 1, 2006
    Date of Patent: May 18, 2010
    Assignee: Nycomed GmbH
    Inventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
  • Publication number: 20100113413
    Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.
    Type: Application
    Filed: January 5, 2010
    Publication date: May 6, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Qing Dong, Stephen W. Kaldor
  • Publication number: 20100080758
    Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared (NIR) spectral range. The NIR is highly sensitive for tumor detection and tracking. The application discloses targeting a tumor-enriched cell surface receptor with a ligand-conjugated fluorescent probe, which specifically allows detection of the tumor relative to the negligible animal autofluorescence.
    Type: Application
    Filed: October 2, 2009
    Publication date: April 1, 2010
    Applicant: LI-COR,INC.
    Inventors: Daniel R. Draney, Ananda G. Lugade, Narasimhachari Narayanan
  • Patent number: 7678796
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: March 16, 2010
    Assignee: AstraZeneca AB
    Inventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
  • Publication number: 20100055071
    Abstract: Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, L1, V, W, T, Z, R, Y1, and p are as defined herein.
    Type: Application
    Filed: November 20, 2007
    Publication date: March 4, 2010
    Inventors: Martin Robert Leivers, Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi
  • Publication number: 20100034827
    Abstract: The invention is related to compounds of Formula (I), (II), or (III); 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: Application
    Filed: July 24, 2007
    Publication date: February 11, 2010
    Applicants: GILEAD SCIENCES, INC., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Hongyan Guo, Choung U. Kim, Thorsten A. Kirschberg, Iii Young Lee, Michael L. Mitchell, Jong Chan Son, Lianhong Xu
  • Patent number: 7659268
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: February 9, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
  • Publication number: 20100029625
    Abstract: A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R0 represents aryl, —NR1CONR2 (wherein R1 represents a hydrogen atom or the like, and R2 represents lower alkyl or the like) or the like, R3 represents lower alkyl, R4 represents a hydrogen atom or the like, and R5 represents aryl or the like].
    Type: Application
    Filed: June 22, 2006
    Publication date: February 4, 2010
    Applicants: KYOWA HAKKO KIRIN CO., LTD., FUJIFILM CORPORATION
    Inventors: Ryuichiro Nakai, Emi Shimoike, Hideaki Kusaka, Chikara Murakata, Yoshinori Yamashita
  • Publication number: 20100029941
    Abstract: Described herein are methods for making chiral derivatives of 3-aminopiperidine, including the production of such derivatives in quantities exceeding 1 kilogram. The chiral 3-aminopiperidine derivatives include (R)-3-aminopiperidine derivatives which may be used to synthesize inhibitors of Dipeptidyl Peptidase IV. (R)-3-Aminopiperidine dihydrochloride is prepared by reducing (R)-3-aminopiperidin-2-one hydrochloride with lithium aluminum hydride. The preparation of (R)-3-aminopiperidin-2-one hydrochloride starting from (R)-methyl-2,5-diaminopentanoate dihydrochloride or (R)-2,5-diaminopentanoic acid hydrochloride is also described.
    Type: Application
    Filed: March 26, 2007
    Publication date: February 4, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Michael B. Wallace, Jeremy Cody, Richard S. Fornicola, Silvina Garcia-Rubio, Philip B. Kisanga, Maxwell D. Reeve, Chandra Wilson
  • Publication number: 20100016343
    Abstract: The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate ?7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
    Type: Application
    Filed: July 16, 2009
    Publication date: January 21, 2010
    Applicants: WYETH, SIENA BIOTECH S.P.A.
    Inventors: Chiara Ghiron, Michela Valacchi, Ugo Zanelli, Simon N. Haydar
  • Publication number: 20100004445
    Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 7, 2010
    Applicant: PGxHealth, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert Thompson
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Patent number: 7638520
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: December 29, 2009
    Assignee: SmithKline Beecham, plc
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Publication number: 20090318467
    Abstract: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
    Type: Application
    Filed: June 15, 2009
    Publication date: December 24, 2009
    Inventors: Jean-Michel Adam, Johannes Aebi, Alferd Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
  • Publication number: 20090318440
    Abstract: Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.
    Type: Application
    Filed: December 12, 2006
    Publication date: December 24, 2009
    Inventors: Junhu Zhang, Anle Yang, Susan Elizabeth Kephart, Liming Dong, Chuangxing Guo, Yufeng Hong, Mary Catherine Johnson, Indrawan James Mc Alpine, Jayashree Tikhe, Haitao Li
  • Patent number: 7618962
    Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: November 17, 2009
    Assignee: PGX Health, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Patent number: 7615569
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: November 10, 2009
    Assignee: Icagen, Inc.
    Inventors: Alan Fulp, Brian Marron, Mark J. Suto, Xiaodong Wang
  • Publication number: 20090275751
    Abstract: The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).
    Type: Application
    Filed: February 27, 2009
    Publication date: November 5, 2009
    Inventors: Satoshi NAGATO, Kohshi Ueno, Koki Kawano, Yoshihiko Norimine, Koichi Ito, Takaisa Hanada, Masatake Ueno, Hiroyuki Amino, Makoto Ogo, Shinji Hatakeyama, Yoshio Urawa, Hiroyuki Naka, Anthony John Groom, Leanne Rivers, Terrence Smith
  • Patent number: 7601729
    Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: October 13, 2009
    Assignee: Glaxo Group Limited
    Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
  • Patent number: 7598379
    Abstract: The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI. The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: October 6, 2009
    Assignee: PGx Health, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Patent number: 7585974
    Abstract: Compounds complying with the general formula in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1-C6)alkyl, (C1-C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1-C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. The compounds of this invention are useful as therapeutic agents.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: September 8, 2009
    Assignee: Sanofi-Aventis
    Inventors: Frederic Galli, Odile LeClerc, Alistair Lochead, Alain Nedelec
  • Patent number: 7579348
    Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: August 25, 2009
    Assignee: PGxHealth, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Publication number: 20090209565
    Abstract: The present invention relates to a therapeutic agent for inflammatory bowel disease comprising 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof as an active ingredient. According to the present invention, an effective and safe therapeutic agent for inflammatory bowel disease including ulcerative colitis and Crohn's disease can be provided. The balance between the therapeutic effect on a chronic inflammation such as inflammatory bowel disease and the adverse side effect of the compound is superior to those of an aminosalicylic acid preparation and a corticosteroid preparation, which cannot be expected at all from a mere anti-diarrheal effect.
    Type: Application
    Filed: April 12, 2007
    Publication date: August 20, 2009
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventor: Yuji Takebayashi
  • Patent number: 7576076
    Abstract: The present invention provides a compound having the formula: wherein, n and m are 1; X1 and X2 are O; R1 is a member selected from unsubstituted phenyl and substituted phenyl; R2 is a member selected from hydrogen, —CN, —OR2A, -L2A—C(O)R2B, -L2B—S(O)2R2C; R3 is a member selected from unsubstituted benzyl and substituted benzyl; R4 is a member selected from hydrogen and substituted or unsubstituted alkyl, wherein if R4 is methyl, then -L1-R1 is not benzyl or —C(O)—O—CH2—CH3; and L1 is a bond; and compositions and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: June 29, 2005
    Date of Patent: August 18, 2009
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Robin D. Clark, Nicolas C. Ray, Karen Williams, Peter H. Crackett, Gwen Hickin, David A. Clark
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Publication number: 20090196912
    Abstract: Described are pyridinylamines and pharmaceutically acceptable salts thereof, the use of these pyridinylamines for the prophylaxis and/or treatment of various diseases such as infectious diseases, including opportunistic infections, prion diseases immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as pharmaceutical compositions containing at least one pyridinylamine and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the pyridinylamines are disclosed.
    Type: Application
    Filed: August 1, 2005
    Publication date: August 6, 2009
    Applicant: GPC Botech AG
    Inventors: Jan Elke Eickhoff, Doris Hafenbradl, Wilfried Schwab, Matthew Cotton, Bert Matthias Kiebl, Birgit Zech, Stefan Muller, John Harris, Vladimir Savic, Jackie MacRitchie
  • Patent number: 7566710
    Abstract: The invention relates to dual molecules formed from coupling products complying with the formula wherein A represents a residue of molecule with anti-malarial activity, Y1 and Y2, represent a linear or branched alkylene chain at C1 to C5, or either Y1 or Y2 is absent, U is an amine, amide, sulphonamide, carboxyl, ether or thioether function, said function linking Y1 and Y2, Z1 and Z2, represent a linear arylene or alkylene, or either Z1 or Z2 is absent, or Z1+Z2 together represent a cyclic or polycyclic structure including the junction carbons Ci and Cj, R1 and R2, represent a hydrogen atom or a functional group capable of increasing the hydrosolubility of the dual molecule, Rx and Ry form a cyclic peroxide with 4 to 8 chain links, Cj being one of the peaks of said cyclic peroxide, or -Rx or Ry is a cyclic peroxide with 4 to 8 chain links, which may comprise 1 or 2 additional oxygen atoms in the cyclic structure, and one or more substituents R3, identical or different, at least one R3 representing a hal
    Type: Grant
    Filed: August 4, 2005
    Date of Patent: July 28, 2009
    Assignee: Centre National de la Racherche Scientifique (C.N.R.S.)
    Inventors: Bernard Meunier, Anne Robert, Odile Dechy-Cabaret, Francoise Benoit-Vical
  • Publication number: 20090186912
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: September 17, 2008
    Publication date: July 23, 2009
    Applicant: Abbott Laboratories
    Inventors: Charles A. Flengte, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G.Z. Zhang
  • Patent number: 7563788
    Abstract: Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: July 21, 2009
    Assignee: Pfizer Inc.
    Inventors: Richard John Sciotti, Jeremy Tyson Starr, Christopher Richardson, Gordon William Rewcastle, Huifen Chen, Brian Desmond Palmer, Hamish Scott Sutherland, Julie Ann Spicer
  • Publication number: 20090176812
    Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8?, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.
    Type: Application
    Filed: May 2, 2008
    Publication date: July 9, 2009
    Inventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa, Koji Fuji
  • Publication number: 20090176806
    Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
    Type: Application
    Filed: March 11, 2009
    Publication date: July 9, 2009
    Inventors: Han-Cheng Zhang, Gee-Hong Kuo, Bruce E. Maryanoff, Hong Ye, David O'Neill, Lan Shen, Keith Demarest, Bruce R. Conway, David F. McComsey
  • Publication number: 20090176784
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: September 17, 2008
    Publication date: July 9, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Pamela L. Donner, John T. Randolph, Allan C. Krueger, David A. Betebenner, Douglas K. Hutchinson, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, John E. Hengeveld, Rodger F. Henry, Xiaochun Lou, Geoff G.Z. Zhang
  • Publication number: 20090149485
    Abstract: The present invention relates to a compound of formula (I) or its stereoisomers, tautomers, solvates, hydrates, prodrugs, pharmaceutically acceptable salts or mixtures thereof, or pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. The present invention also provides a method for the prophylaxis or treatment of a medical condition associated with protein kinase, by administering a pharmaceutically effective amount of the compound of formula (I) or salts thereof.
    Type: Application
    Filed: October 24, 2008
    Publication date: June 11, 2009
    Applicant: Jubilant Biosys Limited
    Inventors: Balaji Vituduki Narayana Iyengar, Marahanakuli Dattatreya Prasanna, Phukan Samiron, Singh Sudhir Kumar
  • Publication number: 20090137802
    Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Application
    Filed: January 28, 2009
    Publication date: May 28, 2009
    Inventors: Elfatih Elzein, Rao Kalla, Tim Marquart, Jeff Zablocki, Xiaofen Li
  • Patent number: 7521396
    Abstract: The invention relates to compounds of the formula (I) in which Q, R1, R2, R3, R4, R5, R6, R7 are as defined in the disclosure, to processes for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: April 21, 2009
    Assignee: Bayer CropScience AG
    Inventors: Hans-Georg Schwarz, Roland Andree, Dorothee Hoischen, Joachim Kluth, Karl-Heinz Linker, Anton Vidal-Ferran, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 7521554
    Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Grant
    Filed: August 22, 2006
    Date of Patent: April 21, 2009
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Rao Kalla, Tim Marquart, Jeff Zablocki, Xiaofen Li
  • Publication number: 20090082378
    Abstract: This present disclosure relates to compounds of formula (I): The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I) and to their methods of use in therapy.
    Type: Application
    Filed: April 24, 2007
    Publication date: March 26, 2009
    Inventors: Carlos Puig Duran, Maria Prat Quinones, Daniel Perez Crespo
  • Publication number: 20090047252
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 26, 2008
    Publication date: February 19, 2009
    Applicant: Gilead Sciences, Inc.
    Inventors: Zhenhong R. Cai, Aesop Cho, Choung U. Kim, Jie Xu
  • Publication number: 20090048248
    Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Application
    Filed: December 18, 2006
    Publication date: February 19, 2009
    Inventors: Robert J. DeVita, Jianming Bao, Sander G. Mills