The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/143)
  • Publication number: 20080064691
    Abstract: A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein, for example, Z is CH or nitrogen, R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from hydrogen, halo, nitro, cyano, hydroxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoromethoxy, carboxy and carbamoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; r is 1 or 2; R1 is halo, cyano or carboxy; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); R2 and R3 are independently selected from hydrogen, —O(1-4C)alkyl, —S(1-4C)alkyl, —N(1-4C)alkyl, heterocyclyl, aryl, and (1-4C)alkyl [optionally substituted]; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.
    Type: Application
    Filed: August 4, 2004
    Publication date: March 13, 2008
    Applicant: AstraZeneca AB
    Inventors: Alan Martin Birch, Stuart Norman Lile Bennett, Andrew Duncan Campbell, Iain Simpson, Paul Robert Owen Whittamore, David Paul Whalley, Linda Godfrey
  • Patent number: 7342041
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: March 11, 2008
    Assignee: Schering Corporation
    Inventors: F. George Njoroge, Srikanth Venkatraman, Ashok Arasappan, Francisco Velazquez, Viyyoor M. Girijavallabhan
  • Patent number: 7256188
    Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity.
    Type: Grant
    Filed: May 8, 2002
    Date of Patent: August 14, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
  • Publication number: 20070173500
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: January 23, 2007
    Publication date: July 26, 2007
    Applicant: ALLERGAN, INC.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
  • Patent number: 7208491
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: April 24, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Patent number: 7205330
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: April 17, 2007
    Assignee: Schering Corporation
    Inventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
  • Patent number: 7192957
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: March 20, 2007
    Assignee: Schering Corporation
    Inventors: Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanli Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyoor M. Girijavallabhan
  • Patent number: 7176200
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: February 13, 2007
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7173129
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: February 6, 2007
    Assignee: Athero Genics, Inc.
    Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
  • Patent number: 7173057
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: February 6, 2007
    Assignee: Schering Corporation
    Inventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
  • Patent number: 7173027
    Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.
    Type: Grant
    Filed: January 29, 2002
    Date of Patent: February 6, 2007
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Hongfeng Deng
  • Patent number: 7141568
    Abstract: Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: July 1, 2004
    Date of Patent: November 28, 2006
    Assignee: Pfizer Italia S.r.l.
    Inventors: Daniele Fancelli, Barbara Forte, Jürgen Moll, Mario Varasi, Paola Vianello
  • Patent number: 7105516
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.
    Type: Grant
    Filed: September 15, 2003
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Derek John Denhart, Jonathan L. Ditta, Dalton King, John E. Macor, Lawrence R. Marcin, Ronald J. Mattson, Zhaoxing Meng
  • Patent number: 7101877
    Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: September 5, 2006
    Assignee: Cardiome Pharma Corp.
    Inventors: Allen I Bain, Gregory N Beatch, Cindy J Longley, Bertrand M C Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L Yong, Jeff Jiqun Zhu, Alexander B Zolotoy
  • Patent number: 7091220
    Abstract: The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: August 15, 2006
    Assignee: Gruenenthal GmbH
    Inventors: Matthias Gerlach, Corinna Maul
  • Patent number: 7049314
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.
    Type: Grant
    Filed: September 15, 2003
    Date of Patent: May 23, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dalton King, Jeffrey A. Deskus, John E. Macor, Ronald J. Mattson, Zhaoxing Meng, Charles P. Sloan
  • Patent number: 7041235
    Abstract: The present invention relates to fluorescent diketopyrrolopyrrole analogues of the general formula (I), wherein A1 and A2 are C1–C18alkyl, C2–C18alkenyl, C2–C18alkynyl, C5–C8cycloalkyl, C5–C8cycloalkenyl, aryl or heteroaryl, A3 and A4 are independently of each other C1–C18alkyl, Ar3, —CR30R31—(CH2)m—Ar3, or Y—R32, wherein R30 and R31 independently of each other stand for hydrogen or C1–C4alkyl, or phenyl which can be substituted up to three times with C1–C3alkyl, Ar3 stands for aryl, in particular phenyl or 1- or 2-naphthyl, C5–C8cycloalkyl, in particular cyclohexyl, or heteroaryl, which can be substituted one to three times with C1–C8alkyl, C1–C8alkoxy, halogen or phenyl, which can be substituted with C1–C8alkyl or C1–C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, Y is C(O)— or SO2— and R32 is C1–C18alkyl, Ar3, or aralkyl and A3 can additionally be hydrogen, C1–C8alkyloxycarbonyl, such as tertbutoxycarbonyl, or aralkyloxycarbonyl, such as benzyloxycarbonyl, a process for their preparation and
    Type: Grant
    Filed: August 1, 2002
    Date of Patent: May 9, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Colin Morton, David Macdonald Smith, Abul Iqbal
  • Patent number: 6849622
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: February 1, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Publication number: 20040266762
    Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.
    Type: Application
    Filed: June 2, 2004
    Publication date: December 30, 2004
    Inventor: Matthias Gerlach
  • Publication number: 20040235833
    Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Application
    Filed: March 12, 2004
    Publication date: November 25, 2004
    Applicant: Pfizer Inc
    Inventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
  • Publication number: 20040220183
    Abstract: The invention relates to new hydroxyindoles of the Formula, 1
    Type: Application
    Filed: May 27, 2004
    Publication date: November 4, 2004
    Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
  • Publication number: 20040214820
    Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.
    Type: Application
    Filed: December 31, 2003
    Publication date: October 28, 2004
    Applicant: AVENTIS PHARMA DEUTSCHLAND GmbH
    Inventors: Heinz-Werner Kleemann, Jean-Christophe Carry, Pascal Desmazeau, Serge Mignani, Jean Bouoquerel, Arielle Genevois-Borella, Baptiste Ronan
  • Patent number: 6809098
    Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.
    Type: Grant
    Filed: August 21, 2002
    Date of Patent: October 26, 2004
    Assignee: AstraZeneca AB
    Inventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
  • Publication number: 20040209867
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: April 20, 2004
    Publication date: October 21, 2004
    Applicant: Wyeth
    Inventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
  • Publication number: 20040204407
    Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Application
    Filed: March 8, 2004
    Publication date: October 14, 2004
    Applicant: SUGEN Inc.
    Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
  • Patent number: 6797708
    Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: September 28, 2004
    Assignee: Wyeth
    Inventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
  • Publication number: 20040180888
    Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.
    Type: Application
    Filed: March 22, 2004
    Publication date: September 16, 2004
    Applicant: IDENIX PHARMACEUTICALS INC.
    Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
  • Publication number: 20040173777
    Abstract: The present invention relates to fluorescent diketopyrrolopyrrole analogues of the general formula (I), wherein A1 and A2 are C1-C18alkyl, C2-C18alkenyl, C2-C18alkynyl, C5-C8cycloalkyl, C5-C8cycloalkenyl, aryl or heteroaryl, A3 and A4 are independently of each other C1-C18alkyl, Ar3, —CR30R31—(CH2)m—Ar3, or Y-R32, wherein R30 and R31 independently of each other stand for hydrogen or C1-C4alkyl, or phenyl which can be substituted up to three times with C1-C3alkyl, Ar3 stands for aryl, in particular phenyl or 1- or 2-naphthyl, C5-C8cycloalkyl, in particular cyclohexyl, or heteroaryl, which can be substituted one to three times with C1-C8alkyl, C1-C8alkoxy, halogen or phenyl, which can be substituted with C1-C8alkyl or C1-C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, Y is C(O)— or SO2— and R32 is C1-C18alkyl, Ar3, or aralkyl and A3 can additionally be hydrogen, C1-C8alkyloxycarbonyl, such as tertbutoxycarbonyl, or aralkyloxycarbonyl, such as benzyloxycarbonyl, a pro
    Type: Application
    Filed: February 4, 2004
    Publication date: September 9, 2004
    Inventors: Colin Morton, David MacDonald Smith, Abdul Iqbal
  • Patent number: 6787651
    Abstract: Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-&ggr; mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: September 7, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Andreas Stolle, Jacques P. Dumas, William Carley, Philip D. G. Coish, Steven R. Magnuson, Yamin Wang, Dhanapalan Nagarathnam, Derek B. Lowe, Ning Su, William H. Bullock, Ann-Marie Campbell, Ning Qi, Jeremy L. Baryza, James H. Cook
  • Publication number: 20040157841
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Patent number: 6774233
    Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: August 10, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • Patent number: 6759428
    Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: July 6, 2004
    Assignee: Roche Palo Alto LLC
    Inventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
  • Patent number: 6753327
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and  and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: June 22, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Patent number: 6743788
    Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: May 17, 2002
    Date of Patent: June 1, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
  • Patent number: 6743817
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Neurogen Corporation
    Inventors: George Maynard, LingHong Xie, Stanislaw Rachwal
  • Publication number: 20040087584
    Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs.
    Type: Application
    Filed: July 18, 2003
    Publication date: May 6, 2004
    Applicant: MEMORY PHARMACEUTICALS CORP.
    Inventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
  • Patent number: 6730671
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: May 4, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Publication number: 20040077851
    Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.
    Type: Application
    Filed: July 25, 2003
    Publication date: April 22, 2004
    Inventors: Alexandros Makriyannis, Hongfeng Deng
  • Publication number: 20040067939
    Abstract: The present invention provides glucokinase activators of formula I: 1
    Type: Application
    Filed: September 30, 2003
    Publication date: April 8, 2004
    Inventor: Wendy Lea Corbett
  • Patent number: 6716837
    Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c a
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: April 6, 2004
    Assignee: NPS Allelix Biopharmaceuticals, Inc.
    Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
  • Publication number: 20040063939
    Abstract: The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.
    Type: Application
    Filed: July 31, 2003
    Publication date: April 1, 2004
    Inventors: Hans-Joachim Jansch, Helge Hartenhauer, Hans Stange, Norbert Hofgen, Jurgen Schafer
  • Patent number: 6710068
    Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: March 23, 2004
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
  • Patent number: 6706709
    Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: March 16, 2004
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
  • Publication number: 20040048858
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula 1
    Type: Application
    Filed: December 19, 2002
    Publication date: March 11, 2004
    Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten, Kimberly J. Worsencroft, Liming Ni
  • Patent number: 6699862
    Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&m
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: March 2, 2004
    Assignee: Pfizer Inc.
    Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
  • Publication number: 20040029858
    Abstract: 2-(III-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.
    Type: Application
    Filed: July 10, 2003
    Publication date: February 12, 2004
    Inventors: Ernesto Menta, Nicoletta Pescalli
  • Publication number: 20040030131
    Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.
    Type: Application
    Filed: September 3, 2003
    Publication date: February 12, 2004
    Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
  • Publication number: 20040019207
    Abstract: The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; or aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitr
    Type: Application
    Filed: July 17, 2003
    Publication date: January 29, 2004
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Simon Feldback Nielsen, Elsebet Ostergaard Nielsen
  • Publication number: 20040002495
    Abstract: A compound of formula I 1
    Type: Application
    Filed: May 19, 2003
    Publication date: January 1, 2004
    Inventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth
  • Publication number: 20030229069
    Abstract: The present invention provides a compound of the formula: 1
    Type: Application
    Filed: June 4, 2003
    Publication date: December 11, 2003
    Applicant: Roche Palo Alto LLC
    Inventors: Robin Douglas Clark, Shu-Hai Zhao