Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 544/252)
  • Patent number: 9256062
    Abstract: The electrowetting display apparatus includes a display unit including: a first substrate at least one surface of which is electroconductive; a second substrate disposed to face the electroconductive surface of the first substrate; a hydrophobic insulation film disposed on the electroconductive surface side of the first substrate; a non-electroconductive oil which is provided between the hydrophobic insulation film and second substrate movably on the hydrophobic insulation film and includes a non-polar solvent and an azamethine-based colorant containing two colorant mother nuclei bonded via a linking group represented by ?N—; and an electroconductive hydrophilic liquid provided between the hydrophobic insulation film and second substrate to contact the oil; in which an image is displayed by applying a voltage between the hydrophilic liquid and the electroconductive surface of first substrate and changing the shape of interface between the oil and hydrophilic liquid.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: February 9, 2016
    Assignee: FUJIFILM Corporation
    Inventors: Hiroyuki Naito, Yasuhiro Ishiwata, Takashi Kato
  • Patent number: 9006258
    Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: April 14, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
  • Patent number: 8927543
    Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: January 6, 2015
    Assignee: Galapagos NV
    Inventors: Frédéric Gilbert Labéguére, Gregory John Robert Newsome, Luke Jonathan Alvey, Laurent Raymond Maurice Saniére, Stephen Robert Fletcher
  • Publication number: 20140378487
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Zehong Wan, Xiaomin Zhang, Zhaolong Tong, Kai Long, Saiah E. Dowdell, Eric Steven Manas, Krista Beaver Goodman
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140322229
    Abstract: The present document describes compounds of Formula I, pharmaceutical compositions comprising the same as well as methods of treating diseases such as a cancer, neurological disease, neurodegenerative disorder, stroke, traumatic brain injury, parasitic infection, inflammation or an autoimmune disease with said compounds.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 30, 2014
    Inventors: Zhaoyin Wang, Lianhai Li
  • Patent number: 8871928
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: October 28, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Zhaolong Tong, Kai Long, Sarah E. Dowdell, Eric Steven Manas, Krista Beaver Goodman
  • Publication number: 20140243320
    Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.
    Type: Application
    Filed: July 12, 2012
    Publication date: August 28, 2014
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
  • Publication number: 20140206536
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a-R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: WENMING ZHANG, CALEB WILLIAM HOLYOKE, JR., KENNETH ANDREW HUGHES, GEORGE PHILIP LAHM, THOMAS FRANCIS PAHUTSKI, JR., MY-HANH THI TONG, MING XU
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Publication number: 20140179682
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 26, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140121204
    Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: GALAPAGOS NV
    Inventors: Frédéric Gilbert Labéguère, Gregory John Robert NEWSOME, Luke Jonathan ALVEY, Laurent Raymond Maurice Sanière, Stephen Robert FLETCHER
  • Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Publication number: 20140051689
    Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.
    Type: Application
    Filed: October 24, 2013
    Publication date: February 20, 2014
    Applicant: Biota Scientific Management Pty Ltd.
    Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
  • Patent number: 8557818
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: October 15, 2013
    Assignee: Vertex Phamaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Ronald Knegtel, David Kay
  • Publication number: 20130225616
    Abstract: The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 29, 2013
    Applicant: VERONA PHARMA PLC
    Inventors: Michael J.A. Walker, Bertrand M.C. Plouvier, Julian S. Northen, Philippe Fernandes
  • Publication number: 20130178488
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: September 20, 2011
    Publication date: July 11, 2013
    Inventors: Zehong WAN, Xiaomio Zhang, Zhaolong Tong, Kai Long, Sarah E. Dowdell, Eric Steven Manas, Krista Beaver Goodman
  • Publication number: 20130165437
    Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: GALAPAGOS NV
    Inventor: GALAPAGOS NV
  • Patent number: 8461149
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: June 11, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Francoise Pierard, Jean-Damien Charrier
  • Patent number: 8445700
    Abstract: The present invention relates to a facile, highly efficient and economical process for the preparation of optically active N-benzyl-3-hydroxypyrrolidine in high yield from a naturally occurring alkaloid vasicine. The natural alkaloid vasicine is used as a precursor of (S)—N-benzyl-3-hydroxypyrrolidine and (R)—N-benzyl-3-hydroxypyrrolidines which can easily be sourced from the medicinal plant Adatoda vasica by the method known in the art and transformed to optical isomers (R) and (S)—N-benzyl-3-hydroxypyrrolidine by the method described in the present invention.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: May 21, 2013
    Assignee: Council of Scientific & Industrial Research
    Inventors: Subhash Chandra Taneja, Mushtaq Ahmad Aga, Brijesh Kumar, Vijay Kumar Sethi, Samar Singh Andotra, Ghulam Nabi Qazi
  • Publication number: 20120277100
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a—R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 3, 2010
    Publication date: November 1, 2012
    Inventors: Wenming Zhang, Caleb William Holyoke, JR., Kenneth Andrew Hughes, George Philip Lahm, Thomas Francis Pahutski, JR., My-Hanh Thi Tong, Ming Xu
  • Patent number: 8242127
    Abstract: The present invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their application as inhibitors of phosphodiesterase (PDE) isoenzymes. More particularly the invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their use in medicine for example as bronchodilators with anti-inflammatory properties.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: August 14, 2012
    Assignee: Verona Pharma plc
    Inventors: Alexander William Oxford, David Jack
  • Patent number: 8129398
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: March 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Francis Beaulieu, Carl Ouellet, B. Narasimhulu Naidu, Manoj Patel, Yasutsugu Ueda, Timothy P. Connolly, Jonathan R. Weiss, Michael A. Walker, Nicholas A. Meanwell, Kevin M. Peese, Margaret E. Sorenson, Chen Li
  • Patent number: 8129387
    Abstract: The present invention relates to substituted 5,6-dihydroimidazo[1,5-f]pteridines of formula I: which are useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: March 6, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Ronald Knegtel, David Kay
  • Publication number: 20120022045
    Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, ?3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) 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: January 25, 2010
    Publication date: January 26, 2012
    Inventors: Shankar Venkatraman, John S. Wai, Wayne Thompson, Boyoung Kim, Richard C.A. Isaacs, H. Marie Loughran, Dai-Shi Su, John Lim, Mark W. Embrey, Peter D. Williams
  • Publication number: 20120004233
    Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: January 26, 2010
    Publication date: January 5, 2012
    Applicant: AMIRA PHARMACEUTICALS, INC
    Inventors: Brian Andrew Stearns, Ryan Clark
  • Patent number: 8067417
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: November 29, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
  • Patent number: 8053762
    Abstract: The present invention relates to a novel imidazoquinazoline derivative, a process for preparing the same, and an organic electronic device using the same. The imidazoquinazoline derivative according to the present invention serves as hole injecting, hole transporting, electron injecting, electron transporting, or a light emitting material in an organic electronic device including an organic light emitting device, and the device according to the present invention exhibits excellent characteristics in efficiency, operating voltage, and stability.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: November 8, 2011
    Assignee: LG Chem, Ltd.
    Inventors: Jae-Soon Bae, Dong-Hoon Lee, Dae-Woong Lee, Jun-Gi Jang, Sang-Young Jeon
  • Patent number: 7947697
    Abstract: 8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidine methanesulfonate of the structural formula (I) has Corticotropin Releasing Factor (CRF) antagonist activity and is useful in treating neuropsychiatric and digestive system diseases.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: May 24, 2011
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Tomoyuki Hasegawa, Toshiaki Matsui, Hiroshi Araki, Tetsuji Saito, Tetsuo Obitsu, Masaki Okamoto, Yuichi Gemba, Yutaka Mikami
  • Publication number: 20110009394
    Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.
    Type: Application
    Filed: January 7, 2009
    Publication date: January 13, 2011
    Applicant: Glaxo Group Limited
    Inventors: Pamela Brown, Steven Dabbs, Alan Joseph Hennessy
  • Publication number: 20110003824
    Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
    Type: Application
    Filed: September 16, 2010
    Publication date: January 6, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORDTED
    Inventors: Jean-Damien Charrier, Guy Brenchley
  • Publication number: 20100069393
    Abstract: The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumours and related conditions. The therapeutic agent comprises two fused 6-membered rings with at least a nitrogen at position 1 and a hydroxyl at position 8.
    Type: Application
    Filed: June 22, 2007
    Publication date: March 18, 2010
    Applicant: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Ashley Bush, Penelope Jane Huggins, Jack Gordon Parsons, Gaik Beng Kok, Vijaya Kenche
  • Publication number: 20100069415
    Abstract: A chemical compound having the following structural formula wherein optionally at least one of the phenyl —C6H5 groups bound to the Carbon atoms in position 2 and 6 is independently substituted with a methyl —CH3 or ethyl —C2H5 group, and wherein optionally the ?CH2 group in position 10 is substituted with a sulphinyl ?SO or sulphonyl ?SO2 group. Subject-matter of the invention is also a process of manufacture of 2,6-diphenyl-4,8-diazoadamantan-1-one and the use of this chemical compound and above-mentioned derivatives thereof as components for the formulation of solutions with sterilizing and disinfectant effect. The figure shows the IR spectrum of 2,6-diphenyl-4,8-diazoadamantan-1-one.
    Type: Application
    Filed: November 12, 2007
    Publication date: March 18, 2010
    Applicant: PIETRO AFFAITATI
    Inventors: Pietro Affaitati, Giancarlo Folchitto
  • Publication number: 20090253677
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
    Type: Application
    Filed: March 18, 2009
    Publication date: October 8, 2009
    Inventors: Francis Beaulieu, Carl Ouellet, B. Narasimhulu Naidu, Manoj Patel, Yasutsugu Ueda, Timothy P. Connolly, Jonathan R. Weiss, Michael A. Walker, Nicholas A. Meanwell, Kevin M. Peese, Margaret E. Sorenson
  • Patent number: 7501512
    Abstract: This invention relates to newly identified inhibitors of kinases for treating various disorders.
    Type: Grant
    Filed: July 7, 2004
    Date of Patent: March 10, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Hideyuki Sato, Mio Takada, Yoshiaki Washio
  • Patent number: 7459459
    Abstract: Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: December 2, 2008
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Nakai, Yoshifumi Kagamiishi
  • Publication number: 20080206163
    Abstract: Compounds of general formula (I) wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy or C3-6 cycloalkyl group; X represents OCH2 or a group CR3R4, wherein each of R3 and R4 independently represents a hydrogen atom or a C1-3 alkyl group; each of R10 and R11 independently represents a hydrogen atom, a C1-3 alkyl, C3-6 cycloalkyl or phenyl group; y represents an oxygen atom or a group CHNO2, NCN, NH or NNO2, n is
    Type: Application
    Filed: April 24, 2008
    Publication date: August 28, 2008
    Applicant: Verona Pharma PLC
    Inventors: Alexander William Oxford, David Jack
  • Patent number: 7407964
    Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: August 5, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Guy Brenchley
  • Publication number: 20080176877
    Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: November 28, 2007
    Publication date: July 24, 2008
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding
  • Patent number: 7285559
    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
  • Patent number: 7256198
    Abstract: Novel pyrimidoindolone compounds are disclosed. Methods of using the pyrimidoindolone compounds and compositions containing the compounds in the treatment and/or prevention of disease and other conditions related to inflammation, neurodegeneration, osteoarthritis and apoptosis are also disclosed.
    Type: Grant
    Filed: February 18, 2005
    Date of Patent: August 14, 2007
    Assignee: Wyeth
    Inventors: Paul Jeffrey Dollings, Arlene Joan Dietrich, Lisa Marie Havran, Chae-Koo Dan Chong, Donna Mary Huryn, Albert Jean Robichaud, Boyd Lynn Harrison, Wayne Everett Childers, Alexander A. Greenfield, James Jacob Bicksler, Vasilios Marathias
  • Patent number: 7196094
    Abstract: This invention comprises the novel compounds of formula (I) wherein r, t, Y1—Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: March 27, 2007
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René Angibaud, Marc Gaston Venet, Laurence Anne Mevellec
  • Patent number: 7173040
    Abstract: This invention comprises the compounds of formula (I): wherein r, s, t, Y1–Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: February 6, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Patrick René Angibaud, Marc Gaston Venet, Ashis Kumar Saha, Laurence Anne Mevellec
  • Patent number: 7105663
    Abstract: Compounds of general formula (I) wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6)alkylamino or C2-7 acylamino group, each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy or C3-6 cycloalkyl group; X represents OCH2 or a group CR3R4, wherein each of R3 and R4 independently represents a hydrogen atom or a C1-3 alkyl group; each of R10 and R11 independently represents a hydrogen atom, a C1-3 alkyl, C3-6 cycloalkyl or phenyl group; y represents an oxygen atom or a group CHNO2, NCN, NH or NNO2, n is a
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: September 12, 2006
    Assignee: Rhinopharma Limited
    Inventors: Alexander William Oxford, David Jack
  • Patent number: 7067519
    Abstract: The invention relates to novel 7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: June 27, 2006
    Inventors: Hamed Aissaoui, Martine Clozel, Walter Fischli, Ralf Koberstein, Thierry Sifferlen, Thomas Weller
  • Patent number: 6893650
    Abstract: The invention provides fungicidal compounds of formula (I) and salts thereof wherein: R1 is alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted, or hydrogen; R2 and R3, which may be the same or different, are any group defined for R1; cyano; acyl; —ORa or —SRa, where Ra is alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted; or R2 and R3, or R2 and R1, together with their interconnecting atoms may form a ring, which may be substituted; R4 is alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted; hydroxy; mercapto; azido; nitro; halogen; cyano; acyl; optionally substituted amino; cyanato; thiocyanato; —SF5; —ORa; —SRa or —Si(Ra)3; m is 0 to 3; when present R5, which may be the same or different to any other R5, is any group defined for R4; R6 is optionally substituted carbo- or heterocylclyl; and A is a defined linking group, or —A—R6 and R5 together with benzene ring M form an optionally substituted fused ri
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: May 17, 2005
    Assignee: Bayer Cropscience GmbH
    Inventors: Mark David Charles, Wilfried Franke, David Eric Green, Thomas Lawley Hough, Dale Robert Mitchell, Donald James Simpson, John Frederick Atherall
  • Patent number: 6875771
    Abstract: Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.
    Type: Grant
    Filed: July 15, 2003
    Date of Patent: April 5, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Shuanghua Hu, Paul M. Scola, Yazhong Huang, Katharine A. Grant-Young
  • Patent number: 6858613
    Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: February 22, 2005
    Assignee: Pfizer Inc.
    Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
  • Patent number: 6844089
    Abstract: The invention relates to an electroluminescent device, in which the luminescent layer contains a luminescent compound and a compound of the general formula I as doping agent, wherein B is an unsaturated carbocyclic or heterocyclic 4-8-link ring, which can also contain an alicyclic bridge, the rings D and E are five- or six-link rings, which each can contain one more hetero-atom N, O and S, the radicals R are one or more substituents H or straight-chain or branched C1-C6-alkyl, X and Y are carbon or nitrogen, R1; R2 and R9 are H or straight-chain or branched C1-C6-alkyl, R3 and R9 are hydrogen, straight-chain or branched C1-C6-alkyl, hydroxy, —OR16, —COOR16, N,N-dialkylamino, acetylamino or halogen, wherein R16 is hydrogen, or straight-chain or branched C1-C6-alkyl, R1 and R2 or R2 and R3 and/or R9 and R9 together can form an alicyclic, heterocyclic or aromatic ring, and A1 and A2, which can be the same or different, are cyan, nitro or —COOR16. The compounds I are partly new.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: January 18, 2005
    Assignee: Sensient Imaging Technologies GmbH
    Inventors: Andreas Richter, Dietmar Keil, Gerhard Diener
  • Patent number: 6831074
    Abstract: The present invention provides a compound of formula (I): where Q is a group of formula: These compounds inhibit cyclic guanosine 3′,5′-monophosphate phosphodiesterases (cGMP PDEs). More notably, the compounds are potent and selective inhibitors of the type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterases and have utility therefore in a variety of therapeutic areas. In particular, the present compounds are of value for the curative or prophylactic treatment of mammalian sexual disorders.
    Type: Grant
    Filed: March 6, 2002
    Date of Patent: December 14, 2004
    Assignee: Pfizer Inc
    Inventors: Graham Nigel Maw, Christopher Gordon Barber