Abstract: This invention is generally directed to Indazole Derivatives having the following structure: 1
Type:
Application
Filed:
April 16, 2003
Publication date:
July 1, 2004
Inventors:
Shripad S. Bhagwat, Yoshitaka Satoh, Steven T. Sakata, Chris A. Buhr, Ronald Albers, John Sapienza, Veronique Plantevin, Qi Chao, Kiran Sahasrabudhe, Rachel Ferri
Abstract: The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.
Type:
Application
Filed:
October 6, 2003
Publication date:
April 8, 2004
Inventors:
Roland Grandel, Wilfried Lubisch, Michael Kock, Thomas Hoger, Reinhold Muller, Sabine Schult, Uta Holzenkamp
Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B:
which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure:
wherein A, B, D, D′, E, G and R7 are as defined above.
Type:
Grant
Filed:
December 6, 2000
Date of Patent:
September 2, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Michael Robin Hale, Clarence Webster Andrews, III, Eric Steven Furfine, Ronald George Sherrill, Andrew Spaltenstein, Gregory Thomas Lowen
Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Type:
Application
Filed:
February 20, 2002
Publication date:
August 21, 2003
Inventors:
Chih-Hung Lee, Erol K. Bayburt, Stanley DiDomenico, Irene Drizin, Arthur R. Gomtsyan, John R. Koenig, Richard J. Perner, Robert G. Schmidt, Sean C. Turner, Tammie K. White, Guo Zhu Zheng
Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.
Type:
Grant
Filed:
March 11, 2002
Date of Patent:
July 15, 2003
Assignee:
ICAgen, Inc.
Inventors:
Grant Andrew McNaughton-Smith, George Salvatore Amato
Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
Type:
Application
Filed:
April 10, 2002
Publication date:
May 1, 2003
Inventors:
Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below:
are useful in vitro or in vivo for preventing or treating coagulation disorders.
Type:
Grant
Filed:
August 10, 2000
Date of Patent:
March 18, 2003
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Bing-Yan Zhu, Robert M. Scarborough, Lane Clizbe, Brandon Doughan, Zhaozhong Jon Jia, Kim Kane-Maguire, Charles Marlowe, Yonghong Song, Ting Su, Willy Teng, Penglie Zhang
Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
Type:
Grant
Filed:
October 22, 1999
Date of Patent:
March 19, 2002
Assignee:
CeNes Pharmaceuticals, Inc.
Inventors:
N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant
Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).
Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
Type:
Grant
Filed:
March 27, 1998
Date of Patent:
April 10, 2001
Assignee:
Dupont Pharmaceuticals Company
Inventors:
Prabhakar K. Jadhav, Douglas G. Batt, Munir A. Hussain, William J. Pitts, Arnold J. Repta