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)
  • 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
  • 1,4-Dihydropyridine-Fused Heterocycles, Process for Preparing the Same, Use and Compositions Containing Them
    Publication number: 20080261969
    Abstract: This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
    Type: Application
    Filed: January 15, 2008
    Publication date: October 23, 2008
    Applicant: AVENTIS PHARMA S.A.
    Inventors: Jacques MAUGER, Anil NAIR, Nina MA, Kirsten BJERGARDE, Bruno FILOCHE-ROMME, Odile ANGOUILLANT-BONIFACE, Serge MIGNANI, Jean-Christophe CARRY, Francois CLERC, Herve MINOUX, Laurent SCHIO, Cecile COMBEAU
  • Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors
    Patent number: 7439253
    Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: October 21, 2008
    Assignee: Novexel
    Inventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
  • Process For the Preparation of (2R,3R)-2-Hydroxy-3-Amino-3-Aryl-Propionamide and (2R,3R)-2-Hydroxy-3-Amino-3-Aryl-Propionic Acid Alkyl Ester
    Publication number: 20080249310
    Abstract: The invention relates to a novel compound (2R,3R)-2-hydroxy-3-amino-3-aryl-propionamide according to formula (1), wherein aryl A represents a substituted or unsubstituted aromatic ring, and to a process for the preparation of said compound of formula (1), wherein a reaction mixture comprising the two enantiomers (2R,3S) and (2S,3R) of trans-3-aryl glycidic acid alkyl ester and the two enantiomers (2R,3R) and (2S,3S) of cis-3-aryl glycidic acid alkyl ester, said mixture being enantiomerically and diastereomerically enriched in the (2R,3S)-trans-3-arylglycidic acid alkyl ester, is reacted with ammonia. The invention further relates to a process for the preparation of (2R,3R)-2-hydroxy-3 amino-3-aryl-propionic alkyl ester.
    Type: Application
    Filed: July 20, 2005
    Publication date: October 9, 2008
    Inventors: Thijs Kuilman, Horst Straatman
  • Imidazoquinoline Compounds
    Publication number: 20080213308
    Abstract: The invention provides novel compositions comprising imidazoquinoline 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: September 14, 2005
    Publication date: September 4, 2008
    Inventors: Nicholas Valiante, Feng Xu, Xiaodong Lin, Daniel Chu, Xiaojing Michael Wang
  • Aqueous Gel Formulations Containing 1-(2-Methylpropyl)-1H-Imidazo[4,5-C][1,5]Naphthyridin-4-Amine
    Publication number: 20080207675
    Abstract: Pharmaceutical formulations in an aqueous gel formulation including 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine are provided. Methods of use and kits are also provided.
    Type: Application
    Filed: February 3, 2006
    Publication date: August 28, 2008
    Inventors: David Q. Ma, Christopher S. Perman, Raymond D. Skwierczynski, John C. Hedenstrom
  • Gyrase inhibitors and uses thereof
    Patent number: 7414046
    Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
    Type: Grant
    Filed: May 23, 2003
    Date of Patent: August 19, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
  • 1,3-Dihydro-Imidazo [4,5-C] Quinolin-2-Ones as Lipid Kinase Inhibitors
    Publication number: 20080194579
    Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.
    Type: Application
    Filed: May 18, 2006
    Publication date: August 14, 2008
    Inventors: Carlos Garcia-Echeverria, Frederic Stauffer, Pascal Furet
  • IMIQUIMOD PRODUCTION PROCESS
    Publication number: 20080194822
    Abstract: The present invention provides a process for preparing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod). The process preferably includes heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with ammonia in a polar aprotic solvent at relatively moderate pressure to produce imiquimod, and optionally purifying the imiquimod. The process of the present invention can produce highly pure imiquimod in high yield.
    Type: Application
    Filed: February 14, 2007
    Publication date: August 14, 2008
    Applicant: CHEMAGIS LTD.
    Inventors: Vladimir Naddaka, Shady Saeed, Stephen Cherkez, Oded Arad
  • 1-(2-Methylpropyl)-1H-Imidazo[4,5-C](1,5]Naphthyridin-4-Amine Ethanesulfonate and 1-(2-Methylpropyl)-1H-Imidazo[4,5-C](1,5]Naphthyridin-4-Amine Methanesulfonate
    Publication number: 20080188513
    Abstract: This invention provides methanesulfonate and ethanesulfonate salts of 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine, pharmaceutical compositions containing the salts, methods of making, and methods of use.
    Type: Application
    Filed: December 28, 2005
    Publication date: August 7, 2008
    Inventors: Raymond D. Skwierczynski, Myles L. Brostrom, Tai T. Tran, Joel R. Jacobson
  • Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof
    Patent number: 7407963
    Abstract: A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing the compound, their use, and processes for preparing them.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: August 5, 2008
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
  • Imiquimod Production Process
    Publication number: 20080177074
    Abstract: Provided is a process for producing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod), which includes reacting 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline with a non-gaseous amine precursor. Also provided are methods for isolating highly pure imiquimod. Further provided are intermediates useful in the production of imiquimod, methods for producing such intermediates, and methods for obtaining imiquimod from such intermediates.
    Type: Application
    Filed: January 24, 2007
    Publication date: July 24, 2008
    Applicant: CHEMAGIS LTD.
    Inventors: Vladimir Naddaka, Eyal Klopfer, Shady Saeed, Stephen Cherkez, Oded Arad
  • Inhibitors of Akt activity
    Publication number: 20080161317
    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: December 4, 2007
    Publication date: July 3, 2008
    Inventors: Michael J. Kelly, Mark E. Layton, Philip E. Sanderson
  • PROCESS FOR THE PREPARATION OF IMIQUIMOD AND INTERMEDIATES THEREOF
    Publication number: 20080161573
    Abstract: Novel intermediates useful for the preparation of Imiquimod and a process for the preparation of Imiquimod with the intermediates.
    Type: Application
    Filed: October 16, 2007
    Publication date: July 3, 2008
    Applicant: DIPHARMA S.P.A.
    Inventors: Lino COLOMBO, Enrico Mariotti, Pietro Allegrini, Graziano Castaldi
  • Amide substituted imidazoquinolines
    Patent number: 7393859
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: July 1, 2008
    Assignee: Coley Pharmaceutical Group, Inc.
    Inventors: Patrick L. Coleman, Stephen L. Crooks, George W. Griesgraber, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
  • Tetrahydropyridoethers
    Patent number: 7393860
    Abstract: The compound (7R,8R,9R)-2,3-Dimethyl-8-hydroxy-7-(2-methoxyethoxy)-9-phenyl-7,8,9,10-tetrahydro-imidazo-[1,2-h] [1,7] naphthyridine inhibits the secretion of gastric acid.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: July 1, 2008
    Assignee: Altana Pharma AG
    Inventor: Jörg Senn-Bilfinger
  • Pharmaceutical Use of Fused 1,2,4-Triazoles
    Publication number: 20080153807
    Abstract: The use of fused 1,2,4-triazoles for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: February 27, 2008
    Publication date: June 26, 2008
    Applicant: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen
  • Bicyclic and Tricyclic Heteroaromatic Compounds
    Publication number: 20080146546
    Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
    Type: Application
    Filed: February 4, 2008
    Publication date: June 19, 2008
    Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
  • Hydroxylamine Substituted Imidazoquinolines
    Publication number: 20080114019
    Abstract: Imidazoquinoline compounds with an oxime substituent at the 1-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: August 12, 2004
    Publication date: May 15, 2008
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: Tushar A. Kshirsagar, David T. Amos, Joseph F. Dellaria, Jr., Philip D. Heppner, Scott E. Langer, Bernhard M. Zimmermann
  • HCV inhibitors and methods of using them
    Patent number: 7358259
    Abstract: The present invention comprises tetrazoloquinoline-compounds that are inhibitors of HCV. Compositions comprising the compounds in combination with a pharmaceutically acceptable carrier are also disclosed, as are methods of using the compounds and compositions to inhibit HCV infection of a cell, particular in the form of treating HCV infection in a mammal.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: April 15, 2008
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Sambaiah Thota, Ankush Argade, Rajinder Singh, Henry H. Lu, Peiyong Huang
  • Cyclic amine compounds as CCR5 antagonists
    Patent number: 7348324
    Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.
    Type: Grant
    Filed: October 18, 2002
    Date of Patent: March 25, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shinichi Imamura, Shohei Hashiguchi, Taeko Hattori, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba, Yoshihiro Sugihara
  • 1H-imidazo [4,5-c] quinolin-4-cyano and 1H-imidazo [4,5-c] quinolin-4-carboxamide intermediates
    Patent number: 7335772
    Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C]quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C]quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C]quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-carboxamide, and to the said intermediates.
    Type: Grant
    Filed: December 9, 2004
    Date of Patent: February 26, 2008
    Assignee: TEVA Gyógyszergyár Zártkörüen Müködö Részvénytársaság
    Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
  • RSV polymerase inhibitors
    Patent number: 7323567
    Abstract: Compounds or enantiomers of formula (I) or a salt thereof: wherein R1, R2, R3, R4 and R5 are as defined herein, are useful for the manufacture of a medicament for the treatment or prevention of respiratory syncytial virus infection in a mammal.
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: January 29, 2008
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Bruno Simoneau, Josee Bordeleau, Gulrez Fazal, Serge Landry, Steve Mason, Jean Rancourt
  • Process for preparing Imiquimod
    Patent number: 7323568
    Abstract: The present invention provides a process for preparing 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (Imiquimod) of formula (I). The process comprises heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with formamide, and optionally with bubbling of gaseous ammonia to afford Imiquimod of formula (I). According to the present invention, by using this process and novel purification methods, essentially as described herein, highly pure Imiquimod is obtained.
    Type: Grant
    Filed: December 12, 2005
    Date of Patent: January 29, 2008
    Assignee: Chemagis Ltd.
    Inventors: Vladimir Naddaka, Shady Saeed, Dionne Montviliski, Lior Zelikovitch, Oded Arad, Joseph Kaspi
  • Fused tri and tetra-cyclic pyrazole kinase inhibitors
    Patent number: 7320986
    Abstract: Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: March 3, 2004
    Date of Patent: January 22, 2008
    Assignee: Abbott Labortories
    Inventors: Yunsong Tong, Akiyo K. Claiborne, Gaoquan Li, Nan-Horng Lin, Hing L. Sham, Thomas J. Sowin, Zhi-Fu Tao
  • Tricyclic n-acyl compounds
    Patent number: 7314935
    Abstract: The invention relates to compounds of the formula (1) where the substituents and symbols are as defined in the description. The compounds are valuable intermediates for preparing active pharmaceutical ingredients.
    Type: Grant
    Filed: February 12, 2003
    Date of Patent: January 1, 2008
    Assignee: Altana Pharma AG
    Inventors: Wilm Buhr, Jörg Senn-Bilfinger, Peter Jan Zimmerman, Peter Zimmerman
  • Cyclic benzimidazoles
    Patent number: 7307084
    Abstract: The invention relates to cyclic benzimidazoles of formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
    Type: Grant
    Filed: April 2, 2004
    Date of Patent: December 11, 2007
    Assignee: Altana Pharma AG
    Inventors: Wilm Buhr, M. Vittoria Chiesa, Peter Jan Zimmermann
  • Process for the preparation of Imiquimod and intermediates thereof
    Patent number: 7301027
    Abstract: Novel intermediates useful for the preparation of Imiquimod and a process for the preparation of Imiquimod with the intermediates.
    Type: Grant
    Filed: November 3, 2004
    Date of Patent: November 27, 2007
    Assignee: Dipharma S.p.A.
    Inventors: Lino Colombo, Enrico Mariotti, Pietro Allegrini, Graziano Castaldi
  • N-sulfonylaminothiazole
    Patent number: 7291734
    Abstract: N-(4,5,6,7-tetrahydro-thiazolo-[5,4-c]pyridin-2-yl)-(C6-18)arylsulfonamides, wherein the nitrogen atom of the pyridine is substituted, and wherein the pyridine ring is optionally bridged, useful as a pharmaceutical related to steroid sulfatase
    Type: Grant
    Filed: November 13, 2003
    Date of Patent: November 6, 2007
    Assignee: Novartis AG
    Inventor: Erwin P Schreiner
  • Immunomodulatory compounds
    Patent number: 7291612
    Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.
    Type: Grant
    Filed: May 30, 2006
    Date of Patent: November 6, 2007
    Assignee: Active Biotech A.B.
    Inventors: Ian Richard Matthews, Thomas Stephen Coutler, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Goran Pettersson, Dorthe da Graca Thrige, Philip Huxley
  • Inhibitors of checkpoint kinases
    Publication number: 20070254879
    Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones 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: April 24, 2007
    Publication date: November 1, 2007
    Inventors: Kenneth L. Arrington, Edward J. Brnardic, Vadim Y. Dudkin, Mark E. Fraley, Shaei Y. Huang, Cheng Wang
  • Heterocyclic compounds, method for preparing same and use thereof as medicines, in particular as antibacterial agents
    Patent number: 7288549
    Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds, as well as their use as medicaments, in particular as anti-bacterial agents.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: October 30, 2007
    Assignee: Aventis Pharma S.A.
    Inventors: Joseph Aszodi, Maxime Lampilas, Branislav Musicki, David Alan Rowlands, Pascal Colette
  • Thioether substituted imidazoquinolines
    Patent number: 7288550
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: May 19, 2005
    Date of Patent: October 30, 2007
    Assignee: 3M Innovative Properties Company
    Inventors: Joseph F. Dellaria, Matthew R. Radmer, Bryon A. Merrill
  • Imidazo-substituted compounds as p38 kinase inhibitors
    Patent number: 7285561
    Abstract: The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: October 23, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Ronald Charles Hawley, Alfred Sui-Ting Lui, Eric Brian Sjogren
  • Thioether substituted imidazoquinolines
    Patent number: 7276515
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: May 19, 2005
    Date of Patent: October 2, 2007
    Assignee: Coley Pharmaceutical Group, Inc.
    Inventors: Joseph F. Dellaria, Matthew R. Radmer
  • TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE
    Publication number: 20070173508
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.
    Type: Application
    Filed: January 23, 2007
    Publication date: July 26, 2007
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard Hutchinson, Thomas Jonathan Seiders, Brian Andrew Stearns, Bowei Wang, Jill Melissa Scott, Yen Pham Truong
  • Imidazolyl derivatives as corticotropin releasing factor inhibitors
    Patent number: 7238699
    Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: July 3, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Bireshwar Dasgupta, Gene M. Dubowchik, John E. Macor
  • Imidazolyl derivatives as corticotropin releasing factor inhibitors
    Patent number: 7211669
    Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: May 1, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta
  • Substituted pyrazolyl compounds for the treatment of inflammation
    Patent number: 7211597
    Abstract: The present invention relates to compounds of Formula I: wherein A is (CH2)m-Q-(CH2)n, wherein each CH2 may be independently substituted with one or more substitution selected from the group consisting of: hydroxy, halo, alkoxy, lower alkyl, amino, aminoalkyl, alkylamino, alkenyl, and alkynyl; B is a 5 or 6 membered heteroaryl, or aryl, optionally saturated, or optionally substituted with R1, R2, or R12; X is selected from the group consisting of: N and C; and Y and Z are independently selected from the group consisting of: N, C, CH, CR3, S, and O; compositions comprising such compounds, intermediates thereof, methods of making such compounds, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Grant
    Filed: September 19, 2002
    Date of Patent: May 1, 2007
    Inventors: Suzanne Metz, Michael Clare, Joyce Z. Crich, Timothy J. Hagen, Gunnar J. Hanson, He Huang, Stephen C. Houdek, Michael A. Stealey, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu
  • Substituted imidazo[1, 2-a]-5,6,7,8-tetrahydropyridine-8-ones, method for their production and the use thereof for producing imidazo[1,2-a]pyridines
    Patent number: 7196196
    Abstract: A process for the preparation of imidazo[1,2-a]-5,6,7,8-tetra hydropyridin-8-ones by reaction of ?-butyrolactones with imidazols, novel imidazo[1,2-a]-5,6,7,8-tetrahydropyridin-8-ones, and their use for the preparation of imidazo[1,2-a]pyridines are described.
    Type: Grant
    Filed: September 3, 2002
    Date of Patent: March 27, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Hagen Weigl, Klaus Ebel
  • Prodrugs of imidazopyridine derivatives
    Patent number: 7189736
    Abstract: Compounds of formula 1, in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.
    Type: Grant
    Filed: April 19, 2004
    Date of Patent: March 13, 2007
    Assignee: Altana Pharma AG
    Inventors: Jörg Senn-Bilfinger, Wilm Buhr
  • Condensed heterocyclic compounds as calcitonin agonists
    Patent number: 7189851
    Abstract: The present invention relates to novel fused heterocyclic ring system compounds and methods for their use in the treatment and prevention of diseases or conditions.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: March 13, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Ashok Bhandari, Eric Eugene Boros, David John Cowan, Anthony Louis Handlon, Clifton Earl Hyman, Jeffrey Alan Oplinger, Michael Howard Rabinowitz, Philip Stewart Turnbull
  • Dipeptidyl peptidase inhibitors
    Patent number: 7169926
    Abstract: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: January 30, 2007
    Assignees: Takeda Pharmaceutical Company Limited, Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Scott D. Cowen, Stephen L. Gwaltney, II, Jeongboeb Seo, Jeffrey A. Stafford
  • Preparation of 1H-imidazo[4,5-C] quinolin 4-amines via novel 1H-imidazo[4,5-c] quinolin 4-cyano and 1H-imidazo[4,5-c] quinolin 4-carboxamide intermediates
    Patent number: 7166721
    Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C] quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C] quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C] quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-carboxamide, and to the said intermediates.
    Type: Grant
    Filed: December 9, 2004
    Date of Patent: January 23, 2007
    Assignee: TEVA Gyógyszergyár Zártkörűen Működő Részvénytársaság
    Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
  • 1-Amino 1H-imidazoquinolines
    Patent number: 7163947
    Abstract: 1-Amino 1H-imidazoquinoline compounds, 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: Grant
    Filed: September 3, 2004
    Date of Patent: January 16, 2007
    Assignee: 3M Innovative Properties Company
    Inventors: George W. Griesgraber, Karl J. Manske
  • Urea substituted imidazoquinolines
    Patent number: 7157453
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain urea, thiourea, acylurea, or sulfonylurea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: January 20, 2005
    Date of Patent: January 2, 2007
    Assignee: 3M Innovation Properties Company
    Inventors: Stephen L. Crooks, Michael J. Rice
  • Preparation of 1H-imidazo [4,5-C] quinolin-4-amines via 1H-imidazo [4,5-C] quinolin-4-phthalimide intermediates
    Patent number: 7153967
    Abstract: The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: December 26, 2006
    Assignee: TEVA Gyógyszergyár Zártkörüen Müködö Részvénytársaság
    Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
  • Oxazolo, thiazolo and selenazolo [4,5-c]-quinolin-4-amines and analogs thereof
    Patent number: 7148232
    Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
    Type: Grant
    Filed: August 25, 2004
    Date of Patent: December 12, 2006
    Assignee: 3M Innovative Properties Company
    Inventors: John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek
  • Pest controllers
    Patent number: 7144843
    Abstract: An objective of the present invention is to provide a harmful organism control agent that possesses excellent control effect against harmful organisms and can be safely used. The present invention provides a compound of formula (1) or a salt thereof. The present invention also provides a harmful organism control agent comprising the compound of formula (1). wherein R1, n, R2, and R3 are as defined in the specification.
    Type: Grant
    Filed: January 31, 2002
    Date of Patent: December 5, 2006
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazuhiko Oyama, Takeshi Teraoka, Kazumi Yamamoto
  • Gyrase inhibitors and uses thereof
    Patent number: RE40245
    Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
    Type: Grant
    Filed: April 28, 2004
    Date of Patent: April 15, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau