Hetero Ring Is Six-membered Consisting Of Three Nitrogens And Three Carbon Atoms Patents (Class 514/241)
Asymmetrical (e.g., 1,2,4-triazine, etc.) (Class 514/242)
Hexamethylenetetramines (Class 514/244)
Nitrogen bonded directly to ring carbon of the hetero ring (Class 514/245)
Polycyclo ring system having a 1,3,5-triazine as one of the cyclos (Class 514/246)
  • Capped pyrazinoylguanidine sodium channel blockers
    Patent number: 7410968
    Abstract: The present invention relates to compounds represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: August 12, 2008
    Assignee: PARION SCIENCES, Inc.
    Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
  • Heteroaryl compounds useful as inhibitors or protein kinases
    Patent number: 7407962
    Abstract: The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: August 5, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, Michael R. Hale, Francois Maltais, Qing Tang
  • Opioid receptor agonist compounds and their use in treatment of pain
    Patent number: 7399762
    Abstract: Structurally novel opioid receptor agonists are provided, and the use of these agonists in treatment of chronic and/or acute pain.
    Type: Grant
    Filed: April 25, 2005
    Date of Patent: July 15, 2008
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Hernan A. Navarro
  • PHENYL-ANILINE SUBSTITUTED BICYCLIC COMPOUNDS USEFUL AS KINASE INHIBITORS
    Publication number: 20080167304
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.
    Type: Application
    Filed: March 13, 2008
    Publication date: July 10, 2008
    Inventors: Jagabandhu Das, John Hynes, Katerina Leftheris, Shuqun Lin, Stephen T. Wrobleski, Hong Wu
  • O-LINKED PYRIMIDIN-4-AMINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE TO TREAT CANCER
    Publication number: 20080146571
    Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.
    Type: Application
    Filed: December 12, 2007
    Publication date: June 19, 2008
    Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu
  • 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    Patent number: 7388019
    Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: June 17, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Joseph L. Duffy, Robert J. Mathvink, Liping Wang, Ann E. Weber
  • Substituted Biaryl Analogues
    Publication number: 20080132509
    Abstract: Substituted biaryl analogues of Formula (I) are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localizations studies.
    Type: Application
    Filed: December 13, 2005
    Publication date: June 5, 2008
    Applicant: Neurogen Corporation
    Inventors: Charles A. Blum, Bertrand L. Chenard, Kevin J. Hodgetts, Xiaozhang Zheng
  • Azabicyclylmethyl derivatives of 7,8-dihydro-1,6,9,-trioxa-3-aza-cyclopenta[a]naphthalene as 5-HT antagonists
    Patent number: 7381723
    Abstract: Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and are also useful for the treatment of disorders such as anxiety, aggression and stress, and for the control of various physiological phenomena, such eating disorders, disorders of thermoregulation, and sleep and sexual dysfunction.
    Type: Grant
    Filed: June 28, 2004
    Date of Patent: June 3, 2008
    Assignee: Wyeth
    Inventors: Gary P. Stack, Megan Tran, Adam M. Gilbert
  • 5-Carboxamido Substituted Thiazole Derivatives that Interact With Ion Channels, In Particular With Ion Channels From the Kv Family
    Publication number: 20080125432
    Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.
    Type: Application
    Filed: December 1, 2005
    Publication date: May 29, 2008
    Applicant: Devgen NV
    Inventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
  • Compounds for Nonsense Suppression, and Methods for Their Use
    Publication number: 20080119473
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Application
    Filed: October 13, 2005
    Publication date: May 22, 2008
    Inventors: Neil Almstead, Gary M. Karp, Richard Wilde, Ellen Welch, Hongyu Ren
  • Solid Biocide Formulations
    Publication number: 20080119472
    Abstract: Abstract Biocidal compositions that contain biocidal components, such as an oxidant, and mixed with said components a combination of inorganic compounds capable of reducing the oxidative capacity of the biocidal components by forming a low-melting glass when heated. The biocidal composition may be heated by being ignited or subjected to a heating source, such as a fire.
    Type: Application
    Filed: April 8, 2004
    Publication date: May 22, 2008
    Inventor: Theodor Morel Fishler
  • Carboxylic acid amides, the preparation thereof and their use as medicaments
    Patent number: 7371743
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: February 11, 2005
    Date of Patent: May 13, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Azabicycloalkane compounds
    Patent number: 7358244
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: April 15, 2008
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes
  • Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
    Patent number: 7354924
    Abstract: This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: April 8, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
  • Compositions useful as inhibitors of JAK and other protein kinases
    Patent number: 7348335
    Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
    Type: Grant
    Filed: November 5, 2003
    Date of Patent: March 25, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Randy S. Bethiel, Young-Choon Moon
  • Soil granulates with controlled active ingredient release (cr soil granulates)
    Patent number: 7344730
    Abstract: The present invention relates to soil-applied CR granules obtainable by applying an active-ingredient-comprising coating to a solid carrier in a fluidized bed, to a process for the preparation of these soil-applied granules, and to a method for controlling phytopathogenic fungi, undesired vegetation, undesired attack by insects and/or for regulating the growth of plants using the soil-applied CR granules according to the invention.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: March 18, 2008
    Assignee: BASF SE
    Inventors: Reinhold Stadler, Reiner Kober, Karl-Heinrich Schneider, Reinhold Saur, Herbert Bayer, Karl Kolter, Michael Seufert
  • UV absorber compositions comprising a hydroxyphenyltriazine compound
    Patent number: 7344706
    Abstract: UV absorber compositions are described, comprising (a) from 1 to 99% by weight of a hydroxyphenyltriazine compound of formula (I) wherein R1, R2 and R3 are each independently of the others C1-C18alkyl; C2-C10,alkenyl; or phenyl-C1-C4 alkyl; R4 is hydrogen; or C1-C5alkyl; and (b) from 99 to 1% by weight of a further UV absorber selected from the group of (b) hydroxyphenyltriazines that are different from component (a), (b2) benzotriazoles, (b3) dibenzoylmethane derivatives and (b4) camphor derivatives.
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: March 18, 2008
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Jürg Haase, Thomas Ehlis, Elek Borsos, Dietmar Hüglin, Bernd Herzog
  • Medical devices employing triazine compounds and compositions thereof
    Patent number: 7335656
    Abstract: The present invention relates to methods, compounds, and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses, and is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention also relates to compounds that inhibit smooth muscle proliferation, for example, by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis. This invention also relates to medical devices, such as a stent, comprising a compound or composition of this invention disposed on or within the medical device.
    Type: Grant
    Filed: August 30, 2006
    Date of Patent: February 26, 2008
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Sesha Sridevi Alluri, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Potlapally Rajender Kumar, Gaddam Om Reddy
  • Method for treating allergies using substituted pyrazoles
    Patent number: 7332494
    Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
    Type: Grant
    Filed: February 13, 2002
    Date of Patent: February 19, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
  • Methods and compositions of novel triazine compounds
    Patent number: 7332488
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: February 19, 2008
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
  • Methods and compositions of novel triazine compounds
    Patent number: 7332490
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: May 25, 2006
    Date of Patent: February 19, 2008
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
  • Pyrazine modulators of cannabinoid receptors
    Patent number: 7326706
    Abstract: The present application describes compounds according to Formula I, wherein A, G1, G2 and R1 are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: February 5, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bruce A. Ellsworth, Chongqing Sun, Annapurna Pendri
  • Compositions useful as inhibitors of JAK and other protein kinases
    Patent number: 7312227
    Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
    Type: Grant
    Filed: November 3, 2003
    Date of Patent: December 25, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Ledeboer, Brian Ledford
  • 1,3,5-Triazine derivatives as ligands for human adenosine-A3 receptors
    Patent number: 7307079
    Abstract: The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient. The invention relates to compounds of the general formula (1) wherein Y represents a group of the general formula (A), (B) or (C) and all other symbols have the meanings as given in the description.
    Type: Grant
    Filed: May 30, 2003
    Date of Patent: December 11, 2007
    Assignees: Solvay Pharmaceuticals, B.V., Arqule, Inc.
    Inventors: Jacobus A.J. Den Hartog, Jan H. Reinders, Guustaaf J.M. Van Scharrenburg, Maria L. Pras-Raves, Gary R. Gustafson
  • Mitotic kinesin inhibitors
    Patent number: 7301028
    Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: November 27, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Mark E. Fraley
  • Aryl triazines as LPAAT-? inhibitors and uses thereof
    Patent number: 7291616
    Abstract: The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor cells.
    Type: Grant
    Filed: October 30, 2002
    Date of Patent: November 6, 2007
    Assignee: Cell Therapeutics, Inc.
    Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Anil M. Kumar, John Tulinsky
  • Pyrimidine, quinazoline, pteridine and triazine derivatives
    Publication number: 20070225271
    Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Application
    Filed: March 15, 2007
    Publication date: September 27, 2007
    Inventors: Alfred Binggeli, Andreas Christ, Hans-Peter Maerki, Rainer Eugen Martin
  • Medical devices employing triazine compounds and compositions thereof
    Patent number: 7268134
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: September 11, 2007
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
  • INDOLE-3-CARBOXYLIC ACID AMIDE, ESTER, THIOAMIDE AND THIOL ESTER COMPOUNDS BEARING ARYL OR HETEROARYL GROUPS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY
    Publication number: 20070191313
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.
    Type: Application
    Filed: February 15, 2007
    Publication date: August 16, 2007
    Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
  • PH sensitive prodrugs of 2,6-Diisopropylphenol
    Patent number: 7250412
    Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: March 15, 2004
    Date of Patent: July 31, 2007
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
  • Azacytosine analogs and derivatives
    Patent number: 7250416
    Abstract: Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 4- and 6-position of the triazine ring, at the 1?–6? position of the ribose ring, or combinations thereof. Methods of synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders and cancer.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: July 31, 2007
    Assignee: SuperGen, Inc.
    Inventors: Pasit Phiasivongsa, Sanjeev Redkar
  • Stabilization of oxidation-sensitive or UV-sensitive active ingredients
    Patent number: 7244417
    Abstract: The cosmetic or dermatological formulations of the invention include: (a) at least one oxidation-sensitive or UV-sensitive active ingredient, (b) at least one dialkyl naphthalate which is distinguished by the structural formula in which R1 and R2, independently of one another, are chosen from the group of branched and unbranched alkyl groups having 6 to 24 carbon atoms, and (c) at least one wax and/or one oil thickener. The present invention also includes methods of using the cosmetic or dermatological formulations.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: July 17, 2007
    Assignee: Beiersdorf AG
    Inventors: Volker Wendel, Anja Göppel
  • Prodrugs of heteroaryl compounds
    Patent number: 7244732
    Abstract: The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents.
    Type: Grant
    Filed: March 31, 2004
    Date of Patent: July 17, 2007
    Assignee: Koronis Pharmaceuticals, Incorporated
    Inventors: Richard Daifuku, Alexander Gall, Dmitri Sergueev, Dina Sologub, Kevin Harris
  • Pyrimidine derivative as selective COX-2 inhibitors
    Patent number: 7235560
    Abstract: The invention provides the compounds of formula (I) or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.
    Type: Grant
    Filed: August 15, 2003
    Date of Patent: June 26, 2007
    Assignee: Glaxo Group Limited
    Inventors: Gordon Weingarten, Gianpaolo Bravi
  • Powder containing physiologically active peptide
    Patent number: 7235253
    Abstract: A method is disclosed for stabilizing a physiologically active peptide in a process of preparing a powder containing the physiologically active peptide by drying an aqueous liquid containing the physiologically active peptide, wherein the method comprises adding to the aqueous liquid at least one compound selected from the group consisting of a nonionic surfactant, a water-soluble, nonionic, organic binder, hydrogenated lecithin, and mannitol.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: June 26, 2007
    Assignee: JCR Pharmaceuticals Co., Ltd.
    Inventors: Yoshinobu Hanyu, Mariko Okada, Chihiro Shindo, Satoshi Nishimuro, Tetsuo Yokoyama, Masato Horie
  • Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 7226927
    Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: November 10, 2003
    Date of Patent: June 5, 2007
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A Drewe, P. Sanjeeva Reddy, Bao Nguyen, Azra Pervin
  • Active substance combinations having insecticidal and acaricdal properties
    Patent number: 7214701
    Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: May 8, 2007
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Stablization of oxidation-sensitive or UV-sensitive active ingredients
    Patent number: 7214365
    Abstract: Cosmetic and dermatological formulations comprising at least one hydrophilic active ingredient and at least one dialkyl naphthalate which is characterized by the structural formula in which R1 and R2, independently of one another, are selected from the group of branched and unbranched alkyl groups having 6 to 24 carbon atoms, have been found to be stable and effective, particularly in moisturizing the skin or protection the skin from skin aging.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: May 8, 2007
    Assignee: Beiersdorf AG
    Inventors: Volker Wendel, Anja Göppel
  • Cosmetic and dermatological light protection formulations with a content of hydroxybenzophenones and alkylnaphthalates
    Patent number: 7204973
    Abstract: The invention relates to light-protective cosmetic or dermatological preparations that contain (a) at least one hydroxy-benzophenone, and (b) at last one dialkyl naphthalate of the structural formula (I), wherein R1 and R2 are independently selected form the group of the branched and unbranched alkyl groups that have 6 to 24 carbon atoms.
    Type: Grant
    Filed: November 2, 2002
    Date of Patent: April 17, 2007
    Assignee: Beiersdorf AG
    Inventors: Anja Göppel, Jens Schulz, Volker Wendel
  • Cosmetic and dermatological light-protective formulations with a content of particulate UV-filter substances and alkylnaphthalates
    Patent number: 7204975
    Abstract: Cosmetic or dermatological formulations comprising at least one particulate UV filter substance and at least one dialkyl naphthalate having the structural formula wherein R1 and R2 are selected independently of one another from the group consisting of branched and unbranched alkyl groups having 6 to 24 carbon atoms, are useful for protecting skin from harmful effects of solar radiation, particularly from UV-A and UV-B radiation.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: April 17, 2007
    Assignee: Beiersdorf AG
    Inventors: Volker Wendel, Anja Göppel, Jens Schulz
  • Stabilization of oxidation-sensitive or UV-sensitive active ingredients
    Patent number: 7204974
    Abstract: The invention is a cosmetic or dermatological formulation, comprising: (a) at least one oxidation- and/or UV-sensitive active ingredient; (b) at least one dialkyl naphthalate which is characterized by the structural formula in which R1 and R2, independently of one another, are chosen from the group of branched and unbranched alkyl groups having 6 to 24 carbon atoms; and (c) at least one lipid with a polarity of at most 30 mN/m. The present invention also includes method of using the cosmetic or dermatological formulations.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: April 17, 2007
    Assignee: Beiersdorf AG
    Inventors: Guido Heinsohn, Anja Göppel, Volker Wendel
  • Heterocyclic compound derivatives and medicines
    Patent number: 7205302
    Abstract: The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]: (R1 and R2 are the same or different and each represents optionally substituted aryl, Y represents N or CH, Z represents N or CH, A represents NH, NR5, O, S, or ethylene, R5 represents alkyl, D represents alkylene or alkenylene, E represents phenylene or single bond, G represents O, S, or CH2, R3 and R4 are the same or different and each represents hydrogen or alkyl, Q represents carboxy, alkoxycarbonyl, tetrazolyl, carbamoyl, or N-(alkylsulfonyl)carbamoyl), or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: April 17, 2007
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
  • Stabilization of UV-sensitive active ingredients
    Patent number: 7201893
    Abstract: Cosmetic and dermatological formulations containing at least one UV-sensitive active ingredient have increased UV protection and have the active ingredient stabilized against decomposition through addition of at least one dialkyl naphthalate of the structural formula wherein R1 and R2 are selected independently of one another from the group consisting of branched and unbranched alkyl groups having between 6 and 24 carbon atoms, and at least one emulsifier, selected from the group consisting of phosphate and sulphate emulsifiers.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: April 10, 2007
    Assignee: Beiersdorf AG
    Inventors: Volker Wendel, Anja Göppel
  • LPAAT-? inhibitors and uses thereof
    Patent number: 7199238
    Abstract: The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-? activity.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: April 3, 2007
    Assignee: Cell Therapuetics, Inc.
    Inventors: Lynn Bonham, Baoqing Gong, Robert E Finney, David M Hollenback, J. Peter Klein, David W Leung, Scott A Shaffer, Norina M Tang, John Tulinsky, Thayer H White
  • Sodium channel blockers
    Patent number: 7192959
    Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: March 20, 2007
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Sodium channel blockers
    Patent number: 7192958
    Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: March 20, 2007
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Sodium channel blockers
    Patent number: 7189719
    Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: March 13, 2007
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Fungicidal formulation
    Patent number: 7176209
    Abstract: Adjuvants selectes from mon/ionic water/soluble mixed polyalkoxy-lated aliphatic alcohol surfactants, non ionic water soluble ethoxylated aliphatic alcohol surfactants, amine ethoxylates, and micronized polymeric waxes enhance the efficacy of fungicidal triazolopzrimidines of structural formula I. They can be incorporated into formulations of the fungicidal compounds or be added to spray mixtures (tank mix) as separately formualted additives in order to improve the efficacy and spectrum of these fungicides.
    Type: Grant
    Filed: August 24, 2001
    Date of Patent: February 13, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Aven, Ewald Sieverding
  • Methods and compositions of novel triazine compounds
    Patent number: 7173032
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: February 6, 2007
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Karen A. Campbell
  • Medical devices employing triazine compounds and compositions thereof
    Patent number: 7169784
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: January 30, 2007
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalger Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Bhatlapenumarthy Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy