Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
At least one of the ring hetero atoms is chalcogen (Class 546/83)
  • Hydroxyalkyl Substituted Imidazonaphthyridines
    Publication number: 20090253695
    Abstract: Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: February 22, 2006
    Publication date: October 8, 2009
    Applicant: Coley Pharmaceutical Group, Inc,
    Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, George W. Griesgraber, Philip D. Heppner, Kyle J. Lindstrom
  • INHIBITORS OF AKT ACTIVITY
    Publication number: 20090253734
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: June 10, 2009
    Publication date: October 8, 2009
    Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
  • Aryl substituted imidazoquinolines
    Patent number: 7598382
    Abstract: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: October 6, 2009
    Assignee: Coley Pharmaceutical Group, Inc.
    Inventors: David S. Hays, Tushar Kshirsagar, Philip D. Heppner, Bryon A. Merrill, Michael E. Danielson, John F. Gerster, Chad A. Haraldson, Sarah Johannessen, Maureen A. Kavanagh, Kyle J. Lindstrom, Michael J. Rice, David J. Squire, Sarah A. Strong, Joshua R. Wurst
  • Method for 1H-Imidazo[4,5-C] Pyridines and Analogs Thereof
    Publication number: 20090240055
    Abstract: Methods and intermediates for preparing compounds of the Formulas: (I and X) are disclosed. The methods include a method providing a compound of the Formula: (IV) and converting a compound of Formula IV to a compound of Formula I, a method providing a compound of the Formula: (VIII) and converting a compound of Formula VIII to a compound of Formula I, and a method providing a compound of the Formula: (XI) and converting a compound of Formula XI to a compound of Formula I.
    Type: Application
    Filed: September 22, 2006
    Publication date: September 24, 2009
    Inventors: Larry R. Krepski, Gregory J. Marszalek, Sonja S. Mackey, John F. Gerster
  • IMMUNOPOTENTIATING COMPOUNDS
    Publication number: 20090232844
    Abstract: The invention provides novel compositions comprising Imidazopyridine compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s).
    Type: Application
    Filed: March 23, 2007
    Publication date: September 17, 2009
    Inventors: James Sutton, Nicholas Valiante
  • Fused Aminopiperidines as Dipeptidyl Peptidase-4 Inhibitors for the Treatment or Prevention of Diabetes
    Publication number: 20090233936
    Abstract: The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 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-4 enzyme is involved.
    Type: Application
    Filed: December 8, 2006
    Publication date: September 17, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Jason M. Cox, Scott D. Edmondson, Anthony Mastracchio
  • AROMATIC HETEROCYCLIC COMPOUND, ORGANIC LIGHT EMITTING DIODE COMPRISING ORGANIC LAYER COMPRISING THE SAME AND METHOD OF MANUFACTURING THE ORGANIC LIGHT EMITTING DIODE
    Publication number: 20090230857
    Abstract: Provided are an aromatic heterocyclic compound represented by Formula 1 below, an organic light emitting diode including the same, and a method of manufacturing the organic light emitting diode: wherein descriptions of Formula 1 are the same as defined in the detailed description of the invention.
    Type: Application
    Filed: March 13, 2009
    Publication date: September 17, 2009
    Inventors: Byoung-ki Choi, O-hyun Kwon, Myeong-suk Kim, Dong-woo Shin, Yu-ri Choi, Duk-keun An, Seong-jib Choi
  • Compounds and compositions as protein kinase inhibitors
    Patent number: 7589101
    Abstract: The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.
    Type: Grant
    Filed: August 15, 2006
    Date of Patent: September 15, 2009
    Assignees: IRM LLC, The Scripps Research Institute
    Inventors: Barun Okram, Pingda Ren, Nathanael S. Gray
  • HYDROXY AND ALKOXY SUBSTITUTED 1H-IMIDAZOQUINOLINES AND METHODS
    Publication number: 20090221556
    Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Application
    Filed: November 3, 2006
    Publication date: September 3, 2009
    Inventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
  • CASPASE INHIBITORS AND USES THEREOF
    Publication number: 20090215736
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Application
    Filed: September 23, 2008
    Publication date: August 27, 2009
    Applicant: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • 1-alkoxy 1H-imidazo ring systems and methods
    Patent number: 7579359
    Abstract: Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical compositions containing the compounds and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: September 1, 2005
    Date of Patent: August 25, 2009
    Assignee: 3M Innovative Properties Company
    Inventors: Larry R. Krepski, Daniel E. Duffy, John F. Gerster, Joan T. Moseman
  • Process for Preparation of 4-amino-1-isobutyl-1H-Imidazo[4,5-C]-quinoline (Imiquimod)
    Publication number: 20090209764
    Abstract: A process for the preparation of imiquimod comprising oxidation of 1-Isobutyl-1H-imidazo quinoline quinoline (II) afforded 1-Isobutyl-1H-imidazo-[4,5-c]-quinoline-5-N-oxide (III) which is isolated in pure form as its hydrochloride salt (IV) followed by conversion to 4-chloro derivative (V) and conversion to corresponding 4-iodo derivative (VI) which is a new intermediate. This new intermediate in convened to imiquimod (VIII) and purified via its novel maleate salt.
    Type: Application
    Filed: April 6, 2009
    Publication date: August 20, 2009
    Inventors: Venkatasubramanian Radhakrishnan Tarur, Suresh Mahadev Kadam, Anil Purushottam Joshi, Sachin Baban Gavhane
  • Inhibitors of Akt activity
    Patent number: 7576209
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
  • Inhibitors of checkpoint kinases
    Publication number: 20090182001
    Abstract: The instant invention provides for compounds which comprise fused imidazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: July 18, 2006
    Publication date: July 16, 2009
    Inventors: Mark E. Fraley, Justin T. Steen
  • Amide and Carbamate Derivatives of Alkyl Substituted N-[4-(4-Amino-1H-Imidazo[4,5-C] Quinolin-1-YL)Butyl]Methanesulfonamides and Methods
    Publication number: 20090176821
    Abstract: Amide and carbamate derivatives of N-[4-(4-amino-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamides with an ethyl, methyl, or n-propyl substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, and methods of use of these compounds in modulating the immune system, for inducing cytokine biosyn-thesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Application
    Filed: September 8, 2006
    Publication date: July 9, 2009
    Applicant: COLEY PHARMACEUTICAL GROUP, INC.
    Inventors: Tushar A. Kshirsagar, Shri Niwas, Bryon A. Merrill
  • PYRROLIDINE INHIBITORS OF IAP
    Publication number: 20090176822
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Application
    Filed: April 17, 2008
    Publication date: July 9, 2009
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • New Use
    Publication number: 20090170854
    Abstract: The present invention relates to a new use of certain pharmaceutically active compounds in the treatment and/or prevention of medicament induced gastric ulcer. More particularly the invention is directed to the use of said compounds, and pharmaceutically acceptable salts thereof, for the treatment and/or prevention of NSAID (non-steroidal antiinflammatory drugs) induced gastric ulcer as well as a pharmaceutical composition in the unit dosage form for the prevention of NSAID induced gastric ulcer in a mammal comprising an NSAID together with a 6-carboxamido-imidazo[1,2-a]pyridine compounds. Other pharmaceutically active compounds used in the present invention comprises COX-2 inhibitors, NO-NSAIDs and bisphosphonates.
    Type: Application
    Filed: August 4, 2008
    Publication date: July 2, 2009
    Inventor: Arne Eek
  • 1-Substituted Pyrazolo (3,4-C) Ring Compounds as Modulators of Cytokine Biosynthesis for the Treatment of Viral Infections and Neoplastic Diseases
    Publication number: 20090163533
    Abstract: Pyrazolo[3,4-c] ring compounds of Formula (I), e.g., pyrazolo[3,4-c]pyridines, pyrazolo[3,4-c]quinolines, 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinolines, and pyrazolo[3,4-c]naphthyridines, substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: March 31, 2006
    Publication date: June 25, 2009
    Applicant: COLEY PHARMACEUTICAL GROUP, INC.
    Inventors: David S. Hays, Ryan B. Prince, Chad A. Haraldson, Jason D. Bonk
  • Pyrazolopyridines and analogs thereof
    Patent number: 7544697
    Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, and 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Grant
    Filed: April 1, 2005
    Date of Patent: June 9, 2009
    Assignee: Coley Pharmaceutical Group, Inc.
    Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
  • Heterocycle Compound, and Production Process and Application Thereof
    Publication number: 20090131467
    Abstract: The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
    Type: Application
    Filed: September 15, 2006
    Publication date: May 21, 2009
    Inventors: Hashime Kanazawa, Tomoji Aotsuka, Kentarou Kumazawa, Kouki Ishitani, Takashi Nose
  • Polymorphs of 1-(2-Methylpropyl)-1H-Imidazo[4,5-C][1,5]Naphthyridin-4-Amine Ethane-Sulfonate
    Publication number: 20090124652
    Abstract: The invention provides various crystalline forms of 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine ethanesulfonate, pharmaceutical compositions, methods of making, and methods of use.
    Type: Application
    Filed: December 28, 2005
    Publication date: May 14, 2009
    Inventors: David Ach, Hughes Martin, Anna Van, Joel R. Jacobson, Junshi Y. Wu, Kyle J. Lindstrom, Tai T. Tran, Myles L. Brostrom, Michael J. Rice, Raymond D. Skwierczynski
  • Pyrazolopyridine-1,4-Diamines and Analogs Thereof
    Publication number: 20090124611
    Abstract: Pyrazolopyridine-1,4-diamines and analogs thereof, e.g., pyrazolo[3,4-c]pyridine-1,4-diamines, pyrazolo[3,4-c]quinoline-1,4-diamines, 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinoline-1,4-diamines, and pyrazolo[3,4-c]naphthyridine-1,4-di-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: March 31, 2006
    Publication date: May 14, 2009
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: David S. Hays, Shri Niwas, Gregory D. Lundquist Jr.
  • HYDROXYLAMINE SUBSTITUTED IMIDAZOQUINOLINES
    Publication number: 20090105295
    Abstract: Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and imidazopyridines) with a hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: November 12, 2004
    Publication date: April 23, 2009
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: Tushar A. Kshirsagar, Gregory D. Lundquist, JR., David T. Amos, Joseph F. Dellaria, JR., Bernhard M. Zimmermann, Philip D. Heppner
  • Substituted Imidazoquinolines and Imidazonaphthyridines
    Publication number: 20090099161
    Abstract: Imidazoquinolines and imidazonaphthyridines with a substituent containing a functional group, e.g., an amide, sulfonamide, urea, or heterocyclyl group, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: February 10, 2006
    Publication date: April 16, 2009
    Applicant: Coley Pharmaceutial Group, Inc.
    Inventors: Michael J. Rice, Chad A. Haraldson, John F. Gerster, Joshua R. Wurst, Philip D. Heppner, Bryon A. Merrill, Tushar A. Kshirsagar
  • DEUTERIUM-ENRICHED NVP-BEZ234
    Publication number: 20090082387
    Abstract: The present application describes deuterium-enriched NVP-BEZ235, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 19, 2008
    Publication date: March 26, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Pyrazolopyridines and Analogs Thereof
    Publication number: 20090075980
    Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Application
    Filed: March 31, 2006
    Publication date: March 19, 2009
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
  • Pyrazolo[3,4-c]Quinolines, Pyrazolo[3,4-c]Naphthyridines, Analogs Thereof, and Methods
    Publication number: 20090069299
    Abstract: Pyrazolo[3,4-c]quinolines, pyrazolo[4,5-c]naphthyridines, and analogs thereof, eg., 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinolines, and, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inhibiting cytokine biosynthesis in animals and in the therapeutic or prophylactic treatment of diseases by inhibiting cytokine biosynthesis are disclosed.
    Type: Application
    Filed: March 31, 2006
    Publication date: March 12, 2009
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: Bryon A. Merrill, Michael E. Danielson, David S. Hays, David T. Amos, Philip D. Heppner, Tushar A. Kshirsagar, Gregory D. Lundquist, JR., William H. Moser
  • Hydroxyalkyl Substituted Imidazoquinoline Compounds and Methods
    Publication number: 20090069314
    Abstract: Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, and an aryl or heteroaryl substituent at the 7-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: February 22, 2006
    Publication date: March 12, 2009
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: Tushar A. Kshirsagar, Bryon A. Merrill, Shri Niwas, Gregory D. Lundquist, JR., Philip D. Heppner, Michael E. Danielson
  • IMIDAZOQUINOLINYL SULFONAMIDES
    Publication number: 20090062272
    Abstract: Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: December 23, 2004
    Publication date: March 5, 2009
    Inventors: Jason D. Bonk, Joseph F. Dellaria, JR.
  • Oxime and Hydroxylamine Substituted Imidazo[4,5-c] Ring Compounds and Methods
    Publication number: 20090062328
    Abstract: Imidazo[4,5-c] ring compounds, (e.g. imidazo[4,5-c]pyridines, imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydro imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridine, and 6,7,8,9-tetrahydro imidazo[4,5-c]naphthyridine compounds) having an oxime or hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: February 10, 2006
    Publication date: March 5, 2009
    Applicant: COLEY PHARMACEUTICAL GROUP, INC.
    Inventors: Tushar A. Kshirsagar, Gregory D. Lundquist, JR., Joseph F. Dellaria, Matthew R. Radmer, Bernhard M. Zimmermann
  • A3 Adenosine receptor allosteric modulators
    Publication number: 20090054476
    Abstract: The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
    Type: Application
    Filed: July 28, 2008
    Publication date: February 26, 2009
    Applicants: The Government of the U.S.A., represented by The Secretary, Dept. of Health and Human Services, Unversiteit Leiden
    Inventors: Aniko Goblyos, Johannes Brussee, Adriaan P. Ijzerman, Zhan-Guo Gao, Kenneth Jacobson
  • HIV INTEGRASE INHIBITORS
    Publication number: 20090054399
    Abstract: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: May 5, 2006
    Publication date: February 26, 2009
    Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C.A. Isaacs, Wei Han, Melissa Egbertson, Richard Pracitto
  • OXIME SUBSTITUTED IMIDAZOQUINOLINES
    Publication number: 20090042925
    Abstract: Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and imidazopyridines) with an oxime substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: November 12, 2004
    Publication date: February 12, 2009
    Inventors: Tushar A. Kshirsagar, Gregory D. Lundquist, David T. Amos, Joseph F. Dellaria, JR., Bernhard M. Zimmermann, Philip D. Heppner
  • ARYLALKENYL AND ARYLALKYNYL SUBSTITUTED IMIDAZOQUINOLINES
    Publication number: 20090030030
    Abstract: Arylalkenyl and aryalkynyl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Application
    Filed: December 17, 2004
    Publication date: January 29, 2009
    Inventors: Jason D. Bonk, Joseph F. Dellaria, JR.
  • MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENT AND ORGANIC ELECTROLUMINESCENT ELEMENT EMPLOYING THE SAME
    Publication number: 20090030202
    Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.
    Type: Application
    Filed: July 10, 2007
    Publication date: January 29, 2009
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
  • NOVEL HETEROCYCLIC COMPOUNDS HAVING ANTI-HBV ACTIVITY
    Publication number: 20090029983
    Abstract: This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.
    Type: Application
    Filed: January 3, 2008
    Publication date: January 29, 2009
    Applicant: Valeant Research & Development
    Inventors: Huanming Chen, Robert Tam, Anneke K. Raney
  • 2-Amino 1H-Imidazo Ring Systems and Methods
    Publication number: 20090023720
    Abstract: 1H-Imidazo ring systems (e.g., imidazopyridines, imidazoquinolines, imidazonaphthyridines, 6,7,8,9-tetrahydro imidazoquinolines and imidazonaphthyridines) with an amino substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Application
    Filed: September 1, 2005
    Publication date: January 22, 2009
    Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, Philip D. Heppner, David T. Amos
  • Methods For Modulating The Development Of Dopamine Neuron By The Dopamine D2 Receptor And Compositions Thereof
    Publication number: 20090017489
    Abstract: The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.
    Type: Application
    Filed: June 22, 2006
    Publication date: January 15, 2009
    Applicant: Korea University Industry And Academy Cooperation Foundation
    Inventors: Ja hyun Baik, Sung yul Kim
  • Aryloxy and Arylalkyleneoxy Substituted Imidazoquinolines
    Publication number: 20090018122
    Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Application
    Filed: August 27, 2004
    Publication date: January 15, 2009
    Inventors: Kyle J. Lindstrom, Hugues M.H. Martin, Bryon A. Merrill, Michael J. Rice, Joshua R. Wurst, Chad A. Haraldson, Tushar A. Kshirsagar, Philip D. Heppner, Shri Niwas, George W. Griesgraber, Matthew R. Radmer
  • THERAPEUTIC PYRAZOLONAPHTHYRIDINE DERIVATIVES
    Publication number: 20090005365
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Application
    Filed: June 6, 2008
    Publication date: January 1, 2009
    Applicant: Helicon Therapeutics, Inc.
    Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
  • 1-Alkoxy 1H-Imidazo Ring Systems and Methods
    Publication number: 20090005376
    Abstract: Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical compositions containing the compounds and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Application
    Filed: September 1, 2005
    Publication date: January 1, 2009
    Inventors: Larry R. Krepski, Daniel E. Duffy, John F. Gerster, Joan T. Moseman
  • Method for Making 1-Substituted 1H-Imidazo [4,5-C] Quinolin-4-Amine Compounds and Intermediates Therefor
    Publication number: 20090005566
    Abstract: The present invention concerns a method for manufacturing 1-substituted 1H imidazo[4,5-c]quinolin-4-amine compounds through their corresponding formamides. The invention also concerns new formamide intermediates.
    Type: Application
    Filed: March 20, 2006
    Publication date: January 1, 2009
    Applicant: FERRER INTERNACIONAL, S.A.
    Inventors: Juan Sallares, Ines Petschen, Francesc-Xavier Camps
  • Compounds that Inhibit Hiv Particle Formation
    Publication number: 20080318959
    Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.
    Type: Application
    Filed: February 1, 2005
    Publication date: December 25, 2008
    Inventors: David Rekosh, Marie-Louise Hammarskjold
  • Tricyclic Benzimidazoles and Their Use as Metabotropic Glutamate Receptor Modulators
    Publication number: 20080318999
    Abstract: The invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2, R3, A, B, D, m, n, x, and y are defined as described in the specification. The invention additionally provides a pharmaceutically composition comprising the compound of formula I, together with a method of using the same to treat or prevent neurological and psychiatric disorders. The compounds are useful in therapy related to the treatment or prevention of mGluR2 receptor-mediated disorders.
    Type: Application
    Filed: July 21, 2006
    Publication date: December 25, 2008
    Inventors: Methvin Isaac, Abdelmalik Slassi, Ian Egle, Fupeng Ma
  • PROCESS FOR IMIDAZO [4,5-C] PYRIDIN-4-AMINES
    Publication number: 20080312434
    Abstract: A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine and converting a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine to a 1H-imidazo[4,5-c]pyridin-4-amine.
    Type: Application
    Filed: May 1, 2008
    Publication date: December 18, 2008
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: Kyle J. Lindstrom, Luke T. Dressel, Jason D. Bonk
  • THERAPEUTIC PYRAZOLOQUINOLINE UREA DERIVATIVES
    Publication number: 20080306048
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Application
    Filed: June 6, 2008
    Publication date: December 11, 2008
    Applicant: Helicon Therapeutics, Inc.
    Inventors: Alan P. Kaplan, Varsha Gupta
  • Process for Preparing 2-Methyl-1-(2-Methylpropyl)-1H-Imidazo[4,5-C][1,5]Naphthyridin-4-Amine
    Publication number: 20080306266
    Abstract: The invention provides various processes for preparing 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine.
    Type: Application
    Filed: December 18, 2005
    Publication date: December 11, 2008
    Inventors: Hugues Martin, David Ach, Clement Toussaint, Fabrice Dubois
  • Imidazo-fused oxazolo [4,5-]pyridine and imidazo-fused thiazolo[4,5-]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
    Patent number: 7456194
    Abstract: The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: November 25, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric Dyckman, William J. Pitts, Makonen Belema, Patrice Gill, James Kempson, Yuping Qiu, Claude Quesnelle, Steven H. Spergel, F. Christopher Zusi
  • Pyrazoloisoquinoline Derivatives
    Publication number: 20080269209
    Abstract: New compounds of formula I, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
    Type: Application
    Filed: November 23, 2006
    Publication date: October 30, 2008
    Applicant: PALAU PHARMA, S.A.
    Inventors: Carmen Almansa Rosales, Marina Virgili Bernado
  • 1H-Imidazoquinoline Derivatives as Prote In Kinase Inhibitors
    Publication number: 20080262021
    Abstract: The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease; novel imidazoquinolines; and a process for the preparation of the novel imidazoquinolines.
    Type: Application
    Filed: November 19, 2004
    Publication date: October 23, 2008
    Applicant: NOVARTIS AG
    Inventors: Hans-Georg Capraro, Giorgio Caravatti, Pascal Furet, Carlos Garcia-Echeverria, Patricia Imbach, Frederic Stauffer