Tricyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/234)
  • Bicyclic and tricyclic hetroaromatic compounds
    Patent number: 7053093
    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: Grant
    Filed: January 28, 2003
    Date of Patent: May 30, 2006
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
  • Process for the synthesis of derivatives of 2, 3-dihydro-1, 4-dioxino- [2, 3-f] quinoline
    Patent number: 7038052
    Abstract: Methods of preparing compounds of Formula I are provided.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: May 2, 2006
    Assignee: Wyeth
    Inventors: Anita W. Chan, Timothy T. Curran, Silvio Iera, Warren Chew, John H. Sellstedt, Galina Vid, Gregg Feigelson, Zhixian Ding
  • Imidazole derivatives, process for their preparation and their use
    Patent number: 6960586
    Abstract: The present invention provides a compound having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism and tumor such as breast cancer and the like. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic alkyl group, and ring A and ring B are each an optionally substituted 5-membered or 6-membered ring having an amide bond in the ring, or a salt thereof.
    Type: Grant
    Filed: November 19, 2001
    Date of Patent: November 1, 2005
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Akihiro Tasaka, Nobuyuki Matsunaga, Akio Ojida, Masami Kusaka
  • Inhibitors of Akt activity
    Patent number: 6958334
    Abstract: The present invention is directed to compounds comprising a triazolo[4,3-b]pyridazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: October 25, 2005
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Andrew Pate Owens, Stanley F. Barnett
  • Imidazolophthalazine derivatives as ligands for GABAA receptors
    Patent number: 6949549
    Abstract: A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I which are partial or full inverse agonists of an ?5 receptor subunit while being relatively free of activity at ?1 and/or ?2 and/or ?3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: September 27, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Richard Alexander Jelley, Tamara Ladduwahetty, Angus Murray MacLeod, Andrew Madin, Francine Sternfeld
  • 1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-diones and their use for the treatment of pain
    Patent number: 6946463
    Abstract: Compounds according to structural diagram (I) are disclosed, wherein R1, A, E and D are as defined in the specification. Also disclosed are pharmaceutical compositions comprising a pain-ameliorating effective amount of a compound in accord with structural diagram (I). The following is an examiner's statement of reasons for allowance: In view of applicants' amendments to the claims which limit “E” to phenyl or cycloalkyl groups the rejections of the previous action no longer pertain as they at best teach “E” as alkyl.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 20, 2005
    Assignee: Astrazeneca AB
    Inventors: Dean Gordon Brown, Rebecca Ann Urbanek, Megan Murphy, Wenhua Xiao, Frances Marie McLaren, Edward Vacek, Thomas Bare, Carey Lynn Horchler, Christine Barlaam, Gary Banks Steelman
  • Imidazolophthalazine derivatives as ligands for GABAA receptors
    Patent number: 6946461
    Abstract: A class of substituted imadazolo[2,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I: which are partial or full inverse agonists of an ?5 receptor subunit while being relatively free of activity at ?1 and/or ?2 and/or ?3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: September 20, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld
  • Compound and method for the treatment of pain
    Patent number: 6943165
    Abstract: A compound, 7-chloro-4-hydroxy-2-(2-chloro-4-methylphenyl)-1,2,5,10-tetrahydropyridazino [4,5-b]quinoline-1,10-dione, pharmaceutically-acceptable salts thereof, a method for treating pain comprising administration of a pain-ameliorating effective amount of the compound and pharmaceutical compositions containing the compound.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: September 13, 2005
    Assignee: AstraZeneca AB
    Inventors: Thomas Michael Bare, Dean Gordon Brown, Megan Murphy, Rebecca Ann Urbanek, Wenhua Xiao
  • 7-chloro-4-hydroxy-2-(2-pyridylethyl)-1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-dione and the use thereof for the treatment of pain
    Patent number: 6933297
    Abstract: A compound, 7-chloro-4-hydroxy-2-(2-pyridylethyl)-1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-dione, its (?) enantiomer, its (+) enantiomer, pharmaceutically-acceptable salts thereof, a method for treating pain comprising administering a pain-ameliorating effective amount of the (?) enantiomer to an individual suffering from pain and pharmaceutical compositions containing the (?) enantiomer are disclosed.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: August 23, 2005
    Assignee: AstraZeneca AB
    Inventors: Dean Gordon Brown, Rebecca Ann Urbanek, Megan Murphy, Wenhua Xiao, Frances Marie McLaren, Edward Vacek, Thomas Bare, Carey Lynn Horchler, Christine Barlaam, Gary Banks Steelman, Vernon Alford
  • Dye labeled imidazoquinoline compounds
    Patent number: 6916925
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 12, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    Patent number: 6900209
    Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.
    Type: Grant
    Filed: November 22, 2001
    Date of Patent: May 31, 2005
    Assignee: Merck sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
  • Sulfur containing dihydrophthalazine antagonists of excitatory amino acid receptors
    Patent number: 6894048
    Abstract: Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neuropsychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.
    Type: Grant
    Filed: September 18, 2003
    Date of Patent: May 17, 2005
    Assignee: Transgenomic, Inc.
    Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
  • Herbicides
    Patent number: 6894005
    Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: May 17, 2005
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
  • Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors
    Patent number: 6844340
    Abstract: The present invention relates to tricyclic 2-pyrimidone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
    Type: Grant
    Filed: January 17, 2003
    Date of Patent: January 18, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventor: Christine M. Tarby
  • 1, 2, 5, 10-tetrahydropyridazino[4, 5-b]quinoline-1,10-diones and their use for the treatment of pain
    Patent number: 6833368
    Abstract: Compounds useful for the treatment of pain in accord with structural diagram (I), or tautomers or pharmaceutically-acceptable salts of such compounds, wherein R1 and A are as disclosed in the specification. Also disclosed are methods for the treatment of pain using compounds according to structural diagram (I) and pharmaceutical compositions comprising compounds according to structural diagram (I).
    Type: Grant
    Filed: October 9, 2003
    Date of Patent: December 21, 2004
    Assignee: AstraZeneca AB
    Inventors: Megan Murphy, Wenhua Xiao, Dean Gordon Brown, Rebecca Ann Urbanek, Frances Marie McLaren, Edward Vacek, Thomas Bare, Carey Lynn Horchler, Christine Barlaam, Gary Banks Steelman, Vernon Alford
  • Compound and method for the treatment of pain
    Patent number: 6787547
    Abstract: A compound, 7-chloro-4-hydroxy-2-(2-chloro-4-methylphenyl)-1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-dione, pharmaceutically-acceptable salts thereof, a method for treating pain comprising administration of a pain-ameliorating effective amount of the compound and pharmaceutical compositions containing the compound.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: September 7, 2004
    Assignee: Astrazeneca AB
    Inventors: Thomas Michael Bare, Dean Gordon Brown, Megan Murphy, Rebecca Ann Urbanek, Wenhua Xiao
  • Imidazolophthalazine derivatives as ligands for gabaa receptors
    Publication number: 20040147517
    Abstract: A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABAA receptors which are partial or full inverse agonists of an &agr;5 receptor subunit while being relatively free of activity at &agr;1 and/or &agr;2 and/or &agr;3 receptor subunit binding sites; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of procon-vulsant activity.
    Type: Application
    Filed: January 16, 2003
    Publication date: July 29, 2004
    Inventors: Richard Alexander Jelley, Tamara Ladduwahetty, Angus Murray MacLeod, Andrew Madin, Francine Sternfeld
  • Tricyclic azaindolizine derivatives having an sPLA2-inhibitory activities
    Patent number: 6756376
    Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein E is N or C—R4; G is N or C—R25; R1 is a carbocyclic group, heterocyclic group or the like; one of R3 and R4 is —(L2)-(acidic group), the other is a hydrogen atom, wherein L2 is a group connecting with an acid group; A ring is optionally substituted 5-8 membered cyclohexane ring or cyclohexene ring; R24 and R25 are a hydrogen atom or the like, its prodrug, their pharmaceutically acceptable salt, or hydrate thereof.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: June 29, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masahiro Fuji, Tetsuo Okada, Makoto Adachi
  • Inhibitors of akt activity
    Publication number: 20040122012
    Abstract: The present invention is directed to compounds comprising a triazolo[4,3-b]pyridazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Application
    Filed: October 2, 2003
    Publication date: June 24, 2004
    Inventors: Andrew Pate Owens, Stanley F. Barnett
  • Aryl imidazoles and related compounds as C5a receptor modulators
    Publication number: 20040116424
    Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula 1
    Type: Application
    Filed: March 28, 2003
    Publication date: June 17, 2004
    Applicant: Neurogen Corporation
    Inventors: George P. Luke, George D. Maynard, Scott Mitchell, Andrew Thurkauf, Linghong Xie, LuYan Zhang, Suoming Zhang, He Zhao, Bertrand L. Chenard, Yang Gao, Bingsong Han, Xiao Shu He
  • Nitrogen-containing heterocyclic compounds
    Patent number: 6750218
    Abstract: 1,3 Diazines according to formula: and pharmaceutically acceptable salts thereof inhibit phosphorylation of platelet-derived growth factor receptor and thereby hinder abnormal cell growth and cell wandering.
    Type: Grant
    Filed: August 26, 2002
    Date of Patent: June 15, 2004
    Assignee: Millenniumium Pharmaceuticals, Inc.
    Inventors: Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shigeki Fujiwara, Shinichi Ide, Eiji Tsukuda, Junko Irie, Shoji Oda
  • Substituted beta carbolines
    Publication number: 20040110759
    Abstract: The subject matter of the present invention is directed to novel substituted beta-carbolines, and specifically compounds of the formula I, 1
    Type: Application
    Filed: July 28, 2003
    Publication date: June 10, 2004
    Applicant: AVENTIS PHARMA DEUTSCHLAND GMBH
    Inventors: Olaf Ritzeler, Alfredo Castro, Louis Grenier, Francois Soucy, Wayne W. Hancock, Hormoz Mazdiyasni, Vito Palombella, Julian Adams
  • Azo compounds for type I phototherapy
    Patent number: 6747151
    Abstract: Novel azo compounds and their bioconjugates for phototherapy and/or photodiagnosis of tumors and other lesions. The azo derivatives of the present invention are designed to absorb at the low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photoexcitation of the azo compound, with the tissue of interest.
    Type: Grant
    Filed: October 15, 2002
    Date of Patent: June 8, 2004
    Assignee: Mallinckrodt, Inc.
    Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Joseph E. Bugaj, Samuel I. Achilefu, Richard B. Dorshow
  • Alpha-substituted pyridazino quinoline compounds
    Patent number: 6737424
    Abstract: Alpha-substituted pyridazino-quinoline compounds of formula Ia useful for the treatment of strokes and neurodegenerative disorders: wherein R1 is selected from a variety of substituents including halogen, (C1-C4)alkyl and nitro; R2 is selected from cycloalkyl moieties of 5-7 carbon atoms and the groups R2′ and R2″ as defined in the specification, a dashed bond indicates a single or double bond, and R7 is selected from H and CO(C1-C3)alkyl.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: May 18, 2004
    Assignee: Zeneca Ltd.
    Inventors: Thomas Michael Bare, James Roy Empfield, Janet Marie Forst, Keith John Herzog, Richard Bruce Sparks
  • Pirazino(aza)indole derivatives
    Publication number: 20040092525
    Abstract: Chemical compounds of formula (I): 1
    Type: Application
    Filed: October 16, 2003
    Publication date: May 13, 2004
    Applicant: VERNALIS RESEARCH LIMITED
    Inventors: David Reginald Adams, Jon Mark Bentley, James Davidson, Matthew Alexander James Duncton, Richard Hugh Phillip Porter
  • Compounds and methods for the treatment of pain
    Patent number: 6730675
    Abstract: Compounds according to structural diagram I are disclosed; wherein R1, A and D are as defined in the specification. Also disclosed are methods for treating pain comprising administration of a pain-ameliorating effective amount of a compound in accord with structural diagram I and pharmaceutical compositions comprising a pain-ameliorating effective amount of a compound in accord with structural diagram I.
    Type: Grant
    Filed: February 12, 2003
    Date of Patent: May 4, 2004
    Assignee: AstraZeneca AB
    Inventors: Megan Murphy, Rebecca Ann Urbanek, Wenhua Xiao, Gary Banks Steelman, Dean Gordon Brown, Thomas Michael Bare
  • Tricyclic and heterocyclic derivative compounds and drugs containing these compounds as the active ingredient
    Publication number: 20040072833
    Abstract: Tri-heterocyclic compound of formula (I) 1
    Type: Application
    Filed: June 30, 2003
    Publication date: April 15, 2004
    Inventors: Hisao Nakai, Yoshifumi Kagashimi
  • 1, 2, 5, 10-tetrahydropyridazino[4, 5-b]quinoline-1,10-diones and their use for the treatment of pain
    Publication number: 20040058927
    Abstract: Compounds useful for the treatment of pain in accord with structural diagram (I), or tautomers or pharmaceutically-acceptable salts of such compounds, wherein R1 and A are as disclosed in the specification. Also disclosed are methods for the treatment of pain using compounds according to structural diagram (I) and pharmaceutical compositions comprising compounds according to structural diagram (I).
    Type: Application
    Filed: October 9, 2003
    Publication date: March 25, 2004
    Inventors: Megan Murphy, Wenhua Xiao, Dean Gordon Brown, Rebecca Ann Urbanek, Frances Marie McLaren, Edward Vacek, Thomas Bare, Carey Lynn Horchler, Christine Barlaam, Gary Banks Steelman, Vernon Alford
  • 1, 2, 5, 10-tetrahydropyridazino[4,5-b]quinoline-1,10-diones and their use for the treatment of pain
    Publication number: 20040053929
    Abstract: Compounds according to structural diagram (I) are disclosed, wherein R1, A, E and D are as defined in the specification. Also disclosed are pharmaceutical compositions comprising a pain-ameliorating effective amount of a compound in accord with structural diagram (I).
    Type: Application
    Filed: September 8, 2003
    Publication date: March 18, 2004
    Inventors: Dean Gordon Brown, Rebecca Ann Urbanek, Megan Murphy, Wenhua Xiao, Frances Marie Mclaren, Edward Vacek, Thomas Bare, Carey Lynn Horchler, Christine Barlaam, Gary Banks Steelman
  • Sulfur containing dihydrophthalazine antagonists of excitatory amino acid receptors
    Patent number: 6703390
    Abstract: Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Transgenomic, Inc.
    Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
  • Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    Publication number: 20040043982
    Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5-or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.
    Type: Application
    Filed: May 21, 2003
    Publication date: March 4, 2004
    Inventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
  • Pirazino(AZA)indole derivatives
    Publication number: 20040039200
    Abstract: Chemical compounds of formula (I): 1
    Type: Application
    Filed: August 5, 2003
    Publication date: February 26, 2004
    Applicant: VERNALIS RESEARCH LIMITED
    Inventors: David Reginald Adams, Jon Mark Bentley, James Davidson, Matthew Alexander James Dunction, Richard Hugh Phillip Porter
  • Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors
    Publication number: 20040023955
    Abstract: The present invention relates to tricyclic 2-pyridone compounds of formula (I): 1
    Type: Application
    Filed: June 10, 2003
    Publication date: February 5, 2004
    Inventors: James D. Rodgers, Haisheng Wang, Mona Patel, Argyrios Arvanitis, Anthony J. Cocuzza
  • Phenylalanine derivatives
    Patent number: 6677339
    Abstract: Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: January 13, 2004
    Assignee: Celltech R & D Limited
    Inventors: John Clifford Head, John Robert Porter, Graham John Warrellow, Sarah Catherine Archibald, Brian Woodside Hutchinson
  • Tricyclic compounds having sPLA2-inhibitory activities
    Patent number: 6673781
    Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: January 6, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Masahiro Fuji, Tetsuo Okada, Makoto Adachi, Tomoyuki Ogawa
  • Tricyclic compounds useful as HIV reverse transcriptase inhibitors
    Publication number: 20040002498
    Abstract: The present invention relates to tricyclic compounds of formula (I): 1
    Type: Application
    Filed: April 24, 2003
    Publication date: January 1, 2004
    Inventors: Barry L. Johnson, Mona Patel, James D. Rodgers, Haisheng Wang, Christine M. Tarby, Rajagopal Bakthavatchalam
  • Aryl and heteroaryl compounds as antibacterial and antifungal agents
    Publication number: 20030220340
    Abstract: This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
    Type: Application
    Filed: May 15, 2003
    Publication date: November 27, 2003
    Inventors: Christoher Don Roberts, Jesse Daniel Keicher, Mikail Hakan Gazginci, Mark Douglas Velligan
  • Methods of modulating tyrosine protein kinase function with indolinone compounds
    Publication number: 20030203901
    Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.
    Type: Application
    Filed: November 25, 2002
    Publication date: October 30, 2003
    Applicant: SUGEN, INC.
    Inventors: Peng Cho Tang, Li Sun
  • Bicyclic and tricyclic hetroaromatic compounds
    Publication number: 20030181455
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: January 28, 2003
    Publication date: September 25, 2003
    Applicant: Neurogen Corporation, A Corporation of the State of Delaware
    Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
  • Heterocycle carboxamides as antiviral agents
    Patent number: 6624159
    Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: September 23, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
  • Compounds and methods for the treatment of pain
    Publication number: 20030176435
    Abstract: Compounds useful for the treatment of pain in accord with structural diagram I, 1
    Type: Application
    Filed: December 17, 2002
    Publication date: September 18, 2003
    Inventors: Dean Gordon Brown, Wenhua Xiao, Rebecca Ann Urbanek, Megan Murphy, Thomas Michael Bare
  • Pentaaza-cyclopental[a]naphthalene derivatives as ligands for GABAa &agr;5 receptors
    Patent number: 6613766
    Abstract: A class of 1,2,3a,4,x-pentaaza-cyclopenta[a]naphthalene compounds (x=6, 7, 8 or 9) is described. The compounds have a high affinity for the GABAA &agr;5 receptors and show inverse agonist activity thereat. The compounds are useful in therapy where cognition enhancement is required.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: September 2, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Francine Sternfeld
  • Compounds and methods for the treatment of pain
    Publication number: 20030153572
    Abstract: Compounds according to structural diagram I are disclosed; 1
    Type: Application
    Filed: February 12, 2003
    Publication date: August 14, 2003
    Inventors: Megan Murphy, Rebecca Ann Urbanek, Wenhua Xiao, Gary Banks Steelman, Dean Gordon Brown, Thomas Michael Bare
  • Imidazolophthalazine derivatives as ligands for gabaa receptors
    Publication number: 20030153562
    Abstract: A class of substituted imadazolo[2,1-a]phthalazine derivatives as ligands for GABAA receptors which are partial or full inverse agonists of an &agr;5 receptor subunit while being relatively free of activity at &agr;1 and/or &agr;2 and/or &agr;3 receptor subunit binding sites; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.
    Type: Application
    Filed: January 16, 2003
    Publication date: August 14, 2003
    Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld
  • Compound and method for the treatment of pain
    Publication number: 20030149042
    Abstract: A compound, 7-chloro-4-hydroxy-2-(2-chloro-4-methylphenyl)-1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-dione, pharmaceutically-acceptable salts thereof, a method for treating pain comprising administration of a pain-ameliorating effective amount of the compound and pharmaceutical compositions containing the compound are disclosed.
    Type: Application
    Filed: January 21, 2003
    Publication date: August 7, 2003
    Inventors: Thomas Michael Bare, Dean Gordon Brown, Megan Murphy, Rebecca Ann Urbanek, Wenhua Xiao
  • Aza- indolyl derivatives for treating obesity
    Patent number: 6583134
    Abstract: Novel compounds of formula (I): wherein X1, X2, X3 and X4, n, R1, R2 and R3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are useful for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea. They are particularly useful for the treatment of obesity.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: June 24, 2003
    Assignees: Hoffman-La Roche Inc., Vernalis Research Limited
    Inventors: Jonathan Mark Bentley, Paul Hebeisen, Sven Taylor
  • Fused heterocyclic inhibitors of factor Xa
    Publication number: 20030087909
    Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): 1
    Type: Application
    Filed: April 8, 2002
    Publication date: May 8, 2003
    Inventors: Irina C. Jacobson, Mimi L. Quan, Ruth R. Wexler
  • Fused heterotricyclic compounds, process for preparing the compounds and drugs containing the same
    Publication number: 20030078277
    Abstract: The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof.
    Type: Application
    Filed: June 5, 2002
    Publication date: April 24, 2003
    Inventors: Shigeki Hibi, Yorihisa Hoshino, Tatsuya Yoshiuchi, Kogyoku Shin, Kouichi Kikuchi, Motohiro Soejima, Mutsuko Tabata, Yoshinori Takahashi, Hisashi Shibata, Takayuki Hida, Tetsuya Hirakawa, Mitsuhiro Ino
  • Azo compounds for type I phototheraphy
    Publication number: 20030072763
    Abstract: Novel azo compounds and their bioconjugates for phototherapy and/or photodiagnosis of tumors and other lesions. The azo derivatives of the present invention are designed to absorb at the low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photoexcitation of the azo compound, with the tissue of interest.
    Type: Application
    Filed: October 15, 2002
    Publication date: April 17, 2003
    Applicant: Mallinckrodt Inc.
    Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Joseph E. Bugaj, Samuel I. Achilefu, Richard B. Dorshow
  • Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same
    Patent number: 6534505
    Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kaufman, Daniel J. Rush