Abstract: The present invention relates to methods for myocardial imaging by administering at least one 2-adenosine N-pyrazole, 2-adenosine C-pyrazole or a combination thereof A2A adenosine receptor agonist to a human undergoing myocardial imaging. The invention also relates to methods of producing coronary vasodilation without significant peripheral vasodilation by administering at least one 2-adenosine N-pyrazole, 2-adenosine C-pyrazole or a combination thereof adenosine A2A adenosine receptor agonist to a human.
Abstract: Synthesis methods suitable for large scale manufacture of the A2A-adenosine receptor agonist (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide and precursors thereof.
Abstract: The present invention relates to methods for producing coronary vasodilation with little peripheral vasodilation by administering doses of a pharmaceutical composition including regadenoson, named (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, — an adenosine A2A receptor agonist — to a human in an amount sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm/sec.
Type:
Grant
Filed:
October 19, 2005
Date of Patent:
February 2, 2010
Assignee:
Gilead Palo Alto, Inc.
Inventors:
Toufigh Gordi, Ann Walls Olmsted, Hsiao Dee Lieu, Luiz Belardinelli
Abstract: 2-{[2-(Substituted amino)ethyl]sulfonyl}ethyl N,N,N?,N?-tetrakis(2-chloroethyl)-phosphorodiamidates, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
Type:
Grant
Filed:
November 29, 2006
Date of Patent:
February 2, 2010
Assignee:
Telik, Inc.
Inventors:
Wenli Ma, Kevin T. Weber, Robert M. Yee
Abstract: 2-adenosine N-pyrazole compounds having the following formula: wherein R1?CH2OH; R2 is hydrogen; R3 is selected from the group consisting of CO2R20; —CONR7R8 ,and aryl wherein the aryl substituent is optionally substituted with one substituent selected from the group consisting of halo, C 1-3alkyl and OR20;R4 is hydrogen; R7 is selected from hydrogen, and C1-3alkyl; R8 is hydrogen; and R20 is selected from hydrogen and methyl as well as methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart are disclosed.
Type:
Grant
Filed:
October 27, 2006
Date of Patent:
February 2, 2010
Assignee:
Gilead Palo Alto, Inc.
Inventors:
Jeff A. Zablocki, Elfatih O. Elzein, Venkata Palle, Luiz Belardinelli
Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Type:
Grant
Filed:
October 5, 2006
Date of Patent:
January 5, 2010
Assignee:
Rogel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
Abstract: Compounds, compositions, and methods relating to 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine or a pharmaceutically acceptable salt thereof are provided for the treatment of Type II diabetes and other diseases associated with poor glycemic control.
Type:
Grant
Filed:
December 26, 2007
Date of Patent:
December 29, 2009
Assignee:
Metabolex Inc.
Inventors:
Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christoper J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
Abstract: Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.
Type:
Grant
Filed:
May 5, 2006
Date of Patent:
December 22, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Francine S. Grant, Sarah Bartulis, Louis Brogley, Michael S. Dappen, Ramesh Kasar, Mohammed A. Khan, Martin Neitzel, Michael A. Pleiss, Eugene D. Thorsett, John Tucker, Michael Ye, Jon E. Hawkinson
Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.
Type:
Grant
Filed:
May 26, 2006
Date of Patent:
December 8, 2009
Assignee:
FibroGen, Inc.
Inventors:
Michael P. Arend, Lee A. Flippin, Volkmar Guenzler-Pukall, Web-Bin Ho, Eric Turtle, Xiaohui Du
Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.
Type:
Grant
Filed:
January 18, 2008
Date of Patent:
October 20, 2009
Assignees:
Sutter West Bay Hospitals, Catholic Healthcare West
Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
Type:
Grant
Filed:
November 7, 2006
Date of Patent:
October 6, 2009
Assignee:
Millenium Pharmaceuticals, Inc.
Inventors:
Craig Grant, James P. Kanter, Graeme Langlands
Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.
Type:
Grant
Filed:
October 31, 2005
Date of Patent:
September 8, 2009
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Ankush Argade, David Carroll, Alexander B. Rossi
Abstract: Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
February 26, 2007
Date of Patent:
August 25, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Jenifer Smith, Christopher Semko, Ying-Zi Xu, Andrei W. Konradi