Abstract: Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
November 2, 2012
Date of Patent:
May 13, 2014
Assignee:
Genentech, Inc.
Inventors:
James John Crawford, Daniel Fred Ortwine, Wendy B. Young
Abstract: A method for treating organophosphorous poisoning (OP) comprising administering to a mammal at risk for OP poisoning an OP poisoning-inhibiting amount of galantamine.
Type:
Grant
Filed:
February 14, 2011
Date of Patent:
April 22, 2014
Assignees:
University of Maryland Baltimore, The United States of America as repr. by the Sec. of the Army, U.S. Army Med. Resr. Inst. of Chem. Defense
Inventors:
Edson X. Albuquerque, Michael Adler, Edna F.R. Pereira
Abstract: The present invention is directed to antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs and the preparation of nanometer-sized camptothecin prodrugs. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant camptothecin nanosphere prodrugs and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these antioxidant camptothecin nanosphere prodrugs for the preparation of delivery devices of other pharmaceuticals and/or drugs. Additionally, methods of treating cancer with the camptothecin and antioxidant derivatives of camptothecin analogs, and nanometer-sized camptothecin prodrugs are also provided.
Abstract: The invention provides compositions that include crosslinking agents having multiple photoactivatable groups, such as diaryl ketones, or a diaryl ketone, such as benzophenone, and at least one polymerizable monomer, such as a zwitterionic monomer. The compositions are useful as surface coating agents that provide brush type polymeric coatings. These polymeric coatings can be used on medical devices, such as artificial joints, to reduce wear and tear between the components of the joint and thus reduce or eliminate debris generated by friction between the joint components.
Type:
Grant
Filed:
March 1, 2010
Date of Patent:
April 8, 2014
Assignee:
Innovative Surface Technologies, Inc.
Inventors:
Jie Wen, Laurie R. Lawin, Patrick Guire
Abstract: The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3?, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.
Type:
Grant
Filed:
July 28, 2006
Date of Patent:
April 1, 2014
Assignee:
Neuropharma, S.A.
Inventors:
Ana Martinez Gil, Miguel Medina Padilla, Mercedes Alonso Cascon, Ana Fuertes Huerta, Maria Luisa Navarro Rico, Maria Jose Perez Puerto, Ana Castro Morera, Ester Martin Aparicio
Abstract: The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules.
Abstract: Methods of treating a subject having, or at risk of having, a myeloproliferative disorder are provided according to embodiments of the present invention which include administering a therapeutically effective amount of an arachidonate 5-lipoxygenase (5-LO) inhibitor to the subject. Combinations of therapeutic agents are administered according to embodiments of the present invention. In some embodiments, two or more 5-LO inhibitors are administered to a subject to treat a myeloproliferative disorder. In further embodiments, at least one 5-LO inhibitor and at least one additional therapeutic agent are administered to a subject to treat a myeloproliferative disorder. Methods of inhibiting leukemia stem cells are provided according to embodiments of the present invention which include contacting leukemia stem cells with an effective amount of an arachidonate 5-lipoxygenase inhibitor.
Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.
Type:
Grant
Filed:
November 15, 2011
Date of Patent:
February 4, 2014
Assignee:
Amgen Inc.
Inventors:
Guoqing Chen, Jeffrey A. Adams, Jean E. Bemis, Shon Booker, Guolin Cai, Lucian V. DiPietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael K. Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander S. Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian M. Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael D. Croghan
Abstract: The invention generally relates to methods of treating an overweight or obese subject, and treating overweight- or obesity-related conditions. In certain embodiments, the invention provides a method of treating an overweight or obese subject including administering a MetAP2 inhibitor in which the amount administered does not substantially modulate angiogenesis.
Abstract: Esters of 2-propylheptanol with linear or branched, saturated or unsaturated C5-C36 carboxylic acids and C4-C36 dicarboxylic acids, compositions comprising these esters, and to the use of esters of 2-propylheptanol with linear or branched, saturated or unsaturated C5-C36-carboxylic acids and/or C4-C36-dicarboxylic acids in cosmetic and/or topical pharmaceutical preparations.
Type:
Grant
Filed:
March 9, 2006
Date of Patent:
February 4, 2014
Assignee:
Cognis IP Management GmbH
Inventors:
Markus Dierker, Catherine Weichold, Stefanie Althaus, Lars Zander, Daniela Prinz
Abstract: The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.
Type:
Grant
Filed:
September 13, 2007
Date of Patent:
January 14, 2014
Inventors:
Marc Gerspacher, Pascal Furet, Eric Vangrevelinghe
Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
Abstract: The present invention provides improved pharmaceutical formulations for pulmonary delivery having improved chemical and physical stability of the therapeutic, prophylactic or diagnostic agent as compared to formulations known in the art. The improved pharmaceutical formulations of the invention for administration to the respiratory system of a patient for the treatment of a variety of disease conditions comprise a mass of biocompatible particles comprising an active agent, and a hydrogenated starch hydrosylate (HSH). The improvement over the prior art comprises the presence of HSH in the pharmaceutical formulation. The invention further relates to a method of treating diseases comprising administering the pharmaceutical formulations of the present invention to the respiratory system of a patient in need of treatment.
Type:
Grant
Filed:
August 21, 2008
Date of Patent:
December 24, 2013
Assignee:
Civitas Therapeutics, Inc.
Inventors:
Charles D. Blizzard, Michael M. Lipp, Kevin L. Ward, Rachel Ryznal, Daniel Leblanc, Mark Tracy, Rebecca Martin
Abstract: Disclosed is a method for treating macular degeneration in a mammalian subject, which comprises administering to the subject in need thereof an effective amount of a 15-keto-prostaglandin compound such as 13,14-dihydro-15-keto-20-ethyl-prostaglandin F2? isopropyl ester.
Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
Type:
Grant
Filed:
November 30, 2011
Date of Patent:
December 3, 2013
Assignee:
Pfizer Inc.
Inventors:
Amy B Dounay, Laura McAllister, Vinod D Parikh, Suobao Rong, Patrick R Verhoest
Abstract: Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.
Abstract: The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen, diclofenac, licofelone, or HTB, and one or more antioxidants.
Type:
Grant
Filed:
March 16, 2010
Date of Patent:
November 5, 2013
Assignee:
Genmedica Therapeutics SL
Inventors:
Alec Mian, Luc Marti Clauzel, Eric Mayoux, Silvia Garcia-Vicente, Marta Serrano Munoz, Antonio Zorzano Olarte, Julio Cesar Castro Palomino Laria
Abstract: The invention provides a method for treating septic shock or endotoxemia, which comprises administering to a subject a therapeutically effective amount of a pharmaceutical composition comprising formula I, II, III or IV and their salt, ester or solvate thereof.