Bicyclo Ring System Having The 1,3-diazine As One Of The Cyclos Patents (Class 514/258.1)
  • Patent number: 6492383
    Abstract: The invention relates to compounds of the formulas 1 and 2 and to pharmaceutically acceptable salts and hydrates thereof, wherein X1, R1, R2 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1 and 2 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas 1 and 2.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: December 10, 2002
    Assignee: Pfizer Inc.
    Inventors: Michael John Munchhof, Susan Beth Sobolov-Jaynes, Matthew Arnold Marx
  • Patent number: 6492366
    Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;):  wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: December 10, 2002
    Assignee: Les Laboratoires Servier
    Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Didier Cussac, Anne Dekeyne
  • Patent number: 6479484
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: November 12, 2002
    Assignee: Euro-Celtique S.A.
    Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
  • Publication number: 20020165240
    Abstract: The invention provides a method for treating a condition via modulation of the Eg5 protein activity comprising administering to a mammalian species in need of such treatment an effective amount of at least one small molecule Eg5 protein inhibitor. The invention also provides a method for treating a condition via modulation of the Eg5 protein activity comprising administering to a mammalian species in need of such treatment an effective amount of at least one small molecule Eg5 protein inhibitor in combination with at least one other anti-cancer agent.
    Type: Application
    Filed: March 28, 2002
    Publication date: November 7, 2002
    Inventors: Spencer David Kimball, Louis J. Lombardo, David B. Rawlins, Hai-Yun Xiao, Deborah L. Roussell
  • Publication number: 20020161004
    Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.
    Type: Application
    Filed: October 23, 2001
    Publication date: October 31, 2002
    Applicant: Syntex (U.S.A.) LLC
    Inventors: Michelle F. Browner, David L. Clark, Timothy D. Cushing, Xiaolin Hao, Ronald C. Hawley, Xiao He, Juan C. Jaen, Sharada S. Labadie, Marie-Louise Smith, Francisco X. Talamas, Nigel P.C. Walker, Marc Labelle
  • Publication number: 20020161011
    Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
    Type: Application
    Filed: December 7, 2001
    Publication date: October 31, 2002
    Applicant: ICAgen
    Inventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
  • Patent number: 6469006
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: October 22, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Wade S. Blair, Milind Deshpande, Haiquan Fang, Pin-Fang Lin, Timothy P. Spicer, Owen B. Wallace, Hui Wang, Tao Wang, Zhongxing Zhang, Kap-Sun Yeung
  • Patent number: 6462044
    Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: October 8, 2002
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
  • Publication number: 20020103212
    Abstract: A pharmaceutical composition containing an anti-human Fas antibody having apoptosis inducing activity and a compound having a folate antagonist activity or a dihydrofolate reductase inhibiting activity, as active ingredients for the prophylaxis and/or treatment of an autoimmune disease or rheumatoid arthritis. According to the present invention, the amount of the anti-Fas antibody to be used can be reduced and thereby the possibility that a patient may become tolerant to anti-Fas antibody as a result of the production of antibodies against the anti-Fas antibody in the patient's body or the like can be decreased, and thus is provided a pharmaceutical composition which can be used for a long time.
    Type: Application
    Filed: November 20, 2001
    Publication date: August 1, 2002
    Applicant: SANKYO COMPANY, LIMITED
    Inventors: Nobufusa Serizawa, Kimihisa Ichikawa, Hiroko Yoshida, Setsu Serizawa
  • Publication number: 20020099050
    Abstract: Compounds useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof, and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.
    Type: Application
    Filed: August 13, 2001
    Publication date: July 25, 2002
    Inventors: Gary S. Lynch, Gary A. Rogers