Patents Examined by Richard Raymond
  • Patent number: 7208602
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
    Type: Grant
    Filed: February 5, 2003
    Date of Patent: April 24, 2007
    Assignees: Schering Corporation, Pharacopeia Drug Discovery, Inc.
    Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
  • Patent number: 7122677
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: October 17, 2006
    Assignee: Scherig Corporation
    Inventors: Gregory A. Reichard, Sunil Paliwal, Neng-Yang Shih, Dong Xiao, Hon-Chung Tsui, Sapna Majmundar Shah, Cheng Wang, Michelle Laci Wrobleski
  • Patent number: 7122675
    Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.
    Type: Grant
    Filed: August 1, 2002
    Date of Patent: October 17, 2006
    Assignee: Schering Corporation
    Inventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
  • Patent number: 7101878
    Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
    Type: Grant
    Filed: August 20, 1999
    Date of Patent: September 5, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
  • Patent number: 7081538
    Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: July 25, 2006
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Michael John Betts
  • Patent number: 7064218
    Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
    Type: Grant
    Filed: December 24, 2002
    Date of Patent: June 20, 2006
    Assignee: Genelabs Technologies, Inc.
    Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
  • Patent number: 7060836
    Abstract: Compounds of the formula (I): or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein R, R1, and Z are as defined herein, are useful in treating or preventing a condition for which an NK2 antagonist is efficacious.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: June 13, 2006
    Assignee: Pfizer, Inc
    Inventors: Donald Stuart Middleton, Alan Stobie
  • Patent number: 7034148
    Abstract: Mixtures of metallocenyl phthalocyanines obtainable by reacting a mixture A comprising two phthalocyanines (I) and (II) with a metallocene derivative in the presence of a catalyst, and also oligomeric metallocenyl phthalocyanines, processes for preparing them, their use for, inter alia, optical recording and optical recording media
    Type: Grant
    Filed: April 9, 2002
    Date of Patent: April 25, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jürgen Beyrich, Rudolf Blattner, Jean-Luc Budry, Wolfgang Freitag, Colin Morton, Gerald Anthony Murphy, Beat Schmidhalter, Michael Schulz, Heinz Spahni, Christian Stern, Annemarie Wolleb, Heinz Wolleb, Roland Zoelper
  • Patent number: 7019147
    Abstract: The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: March 28, 2006
    Assignee: Pfizer Inc.
    Inventors: Wayne E. Barth, Michael J. Luzzio, Joseph P. Lyssikatos
  • Patent number: 7005517
    Abstract: The present invention provides a novel paramagnetic metal-phthalocyanine complexes and pharmaceutically acceptable salts thereof, which are useful as contrast agents for MRI(Magnetic Resonance Imaging), diagnostic X-ray imaging and computed tomography(CT). The present invention also provides contrast agents for imaging, comprising the new paramagnetic metal-phthalocyanine complexes. The new contrast agents of the present invention show high imaging enhancement effects at lower concentration and are safer than the previously reported contrast agents.
    Type: Grant
    Filed: January 4, 2002
    Date of Patent: February 28, 2006
    Inventors: Sung-Young Lee, Kyo-Im Koo
  • Patent number: 7005518
    Abstract: Fluorescent dyes are disclosed which are useful as reporter groups for labeling biomolecules. The silicon phthalocyanine dyes disclosed are preferably water soluble, isomericly pure, possess high quantum yield, and are useful in bioassays.
    Type: Grant
    Filed: October 23, 2003
    Date of Patent: February 28, 2006
    Assignee: Li-Cor, Inc.
    Inventors: Xinzhan Peng, Daniel R. Draney, Jiyan Chen
  • Patent number: 6995269
    Abstract: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: February 7, 2006
    Assignee: Chiron Corporation
    Inventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, David Duhl
  • Patent number: 6989443
    Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head, neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.
    Type: Grant
    Filed: June 28, 2004
    Date of Patent: January 24, 2006
    Assignee: Brookhaven Science Associates, LLC
    Inventors: Haitao Wu, Michiko Miura
  • Patent number: 6974869
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: December 13, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: George V. DeLucca
  • Patent number: 6890915
    Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: May 10, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
  • Patent number: 6846815
    Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
    Type: Grant
    Filed: February 3, 2003
    Date of Patent: January 25, 2005
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Michael R. Myers, Alfred P. Spada, Paul E. Persons, Martin P. Maguire
  • Patent number: 6835726
    Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: December 28, 2004
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
  • Patent number: 6780864
    Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents ═C or —N; —R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl—methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.
    Type: Grant
    Filed: August 14, 2001
    Date of Patent: August 24, 2004
    Assignee: DUPHAR International Research BV
    Inventors: Roelof Feenstra, Johannes A. M. Van Der Heijden, Cornelis G. Kruse, Stephen K. Long, Johannes Mos, Gerben M. Visser, Gustaaf J. M. Van Scharrenburg, Gerrit P. Toorop
  • Patent number: 6770636
    Abstract: Compounds of formula 1, wherein: R1 is hydrogen, hydroxy, CF3, NO2, CN, halogen, C1-C8-alkyl, or C1-C8-alkoxy; R2, R3, and R4 independently of one another are hydrogen, C1-C8-alkyl, hydroxy, NO2, CN, C1-C8-alkoxyl, CF3, or halogen; R5 and R6 independently of one another are hydrogen or a group consisting of C1-C8-alkyl, C2-C8-alkenyl, C3-C8-alkynyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkylene, C5-C8-cycloalkenyl, C5-C8-cycloalkenyl-C1-C6-alkylene, C6-C10-aryl, and C6-C10-aryl-C1-C6-alkylene, each optionally substituted by a group consisting of C1-C6-alkyl, C2-C6-alkenyl, halogen, C1-C6-alkyloxy, —NH2, —NH(C1-C4-alkyl), —N(C1-C4-alkyl)2, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, and CF3, or R5 and R6 together with the nitrogen atom are a saturated or unsaturated 5-, 6-, 7-, or 8-membered heterocyclic group optionally containing one or two further heteroatoms consisting of sulfur, o
    Type: Grant
    Filed: July 24, 2001
    Date of Patent: August 3, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Klaus Fuchs, Werner Stransky, Matthias Grauert, Adrian Carter, Wolfram Gaida, Thomas Weiser, Helmut Ensinger
  • Patent number: 6573265
    Abstract: The invention relates to the use of 1-(aminoalkyl)-3-quinoxaline-2-one derivatives, especially 1-diethylaminoethyl-3-quinoxaline-2-one derivatives of the formula (I), where R 3 is hydroxy, methoxy, ethoxy or hydrogen, or pharmaceutically compatible salts thereof, for the preparation of compounds having an antioxidant action and used for preventing or treating diseases caused by free radicals of the cellular oxygen metabolism, stimulating nerve cell growth, antagonizing glutamate receptors and/or stimulating the growth notably of glutamergic nerve cells.
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: June 3, 2003
    Assignee: Phafag Aktiengesellschaft
    Inventors: Klaus Ehrenberger, Dominik Felix, Peter König, Burkhard Poeggeler