A Ring Nitrogen Is Shared By The Two Cyclos Of The Bicyclo Ring System (e.g., Pyrrolo [1,2-a]pyrimidine, Imidazo[1,2-a]pyrimidine, Etc.) Patents (Class 514/259.1)
Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
Type:
Grant
Filed:
June 10, 2009
Date of Patent:
September 13, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'Keefe, Ginger Xu-qiang Yang
Abstract: Disclosed herein are compounds of Formula (I), or a pharmaceutically acceptable salt, ester, amide, thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula I with the cannabinoid CB2 receptor. Also disclosed are methods of imaging of a tissue by positron emission tomography, the method comprising administering to the subject a compound of Formula I, wherein the compound comprises a radioisotope. Also disclosed are methods of measuring the relative concentration of cannabinoid CB2 receptors in tissue of a subject, by using a compound of Formula I which comprises a radioisotope. In addition, method of diagnosing a disorder in a subject are disclosed.
Type:
Application
Filed:
May 9, 2008
Publication date:
August 25, 2011
Inventors:
Roger Olsson, Ethan Burstein, Anne Eeg Knapp, Jorgen Eskildsen, Joel Castillo, James Nairne, Veronique Morisson-Iveson, Edward Robins, Alex Gibson
Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a thiazole ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.
Type:
Application
Filed:
February 18, 2011
Publication date:
August 25, 2011
Inventors:
Long Mao, Xiaobo Wang, Xiao Xu, Li Zhao, Jia Liu
Abstract: The compounds, pharmaceutical compositions, and methods of using such compounds or compositions thereof described herein are useful for treating a disease modulated by B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein expression.
Type:
Application
Filed:
July 1, 2009
Publication date:
August 4, 2011
Applicant:
PTC THERAPEUTICS, INC.
Inventors:
Young-Choon Moon, Nadiya Sydorenko, Thomas Davis, Liangxian Cao, Daniel J. Medina, Marites A. Rafanan
Abstract: Disclosed is a transdermally absorbable preparation in which the crystallization of a medicinal agent can be prevented even when the medicinal agent has poor solubility in a base material and is contained in the base material at a high concentration, and which exhibits excellent long-term stability and transdermal absorbability of the medicinal agent. By adding a complex of an organic acid and an organic acid salt and a medicinal agent to a base material, it becomes possible to produce a transdermally absorbable preparation in which the crystallization of the medicinal agent can be prevented and which has excellent preparation properties and transdermal absorbability. Also disclosed is use of a complex of an organic and an organic acid salt for preventing the crystallization of a medicinal agent in a transdermally absorbable preparation.
Abstract: 5-Quinolinone and Imidazopyrimidine compounds are provided that are useful for inhibiting the efflux of any therapeutic agent that is a MRP1 substrate. Also provided is a method for screening to identify additional MRP1 inhibitors.
Type:
Application
Filed:
July 10, 2009
Publication date:
July 21, 2011
Applicant:
SOUTHERN RESEARCH INSTITUTE OFFICE OF COMMERCIALIZ
Inventors:
Joseph A. Maddry, Adam Keeton, Jason Whitt, Gary Piazza
Abstract: Provided herein are 2H- and 13C-enriched compounds of formula (I) or (II); wherein R is as defined herein, and wherein at least one hydrogen atom, in certain embodiments, three or more hydrogen atoms, are deuterium atoms or at least one carbon atom is a carbon-13 atom. Also provided are pharmaceutical compositions and methods using the 2H- and 13C-enriched compounds, useful for treating CRTH2-related diseases or disorders such as, for example, asthma, allergic rhinitis, atopic dermatitis, allergic conjuvatitis, Churg-Strauss syndrome, sinusitis, basophilic leukemia, chronic urticaria or basophilic leukocytosis.
Abstract: The present invention provides the compounds represented by formula (I): or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being useful for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
Abstract: The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
Type:
Application
Filed:
March 3, 2009
Publication date:
June 23, 2011
Inventors:
Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
Type:
Application
Filed:
June 10, 2010
Publication date:
June 9, 2011
Applicant:
Incyte Corporation
Inventors:
Jincong ZHUO, Meizhong XU, Chunhong HE, Colin ZHANG, Ding-Quan QIAN, David M. BURNS, Yun-Long LI, Brian METCALF, Wenqing YAO
Abstract: A compound of Formula (1) or a salt thereof, methods for the preparation and use of such a compound, especially as an IAP inhibitor, and related compounds, compositions, and methods.
Type:
Application
Filed:
May 5, 2009
Publication date:
May 19, 2011
Applicant:
Aegera Therapeutics, Inc.
Inventors:
Alain Laurent, Melanie Proulx, James Jaquith
Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
Type:
Application
Filed:
June 10, 2009
Publication date:
May 19, 2011
Inventors:
Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum Macleod, Karen Williams
Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Grant
Filed:
September 26, 2006
Date of Patent:
May 10, 2011
Assignee:
Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
Inventors:
Vincenzo Summa, Olaf Kinzel, Monica Donghi
Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (A) are inhibitors N of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
Type:
Application
Filed:
June 8, 2009
Publication date:
May 5, 2011
Inventors:
Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'keefe, Ginger Xu-Qiang Yang
Abstract: The present invention relates to fungicidal compositions and their use for controlling oomycete pathogen induced disease or diseases in one or more plants.
Type:
Application
Filed:
October 13, 2010
Publication date:
April 14, 2011
Applicant:
DOW AGROSCIENCES LLC
Inventors:
Norman R. Pearson, Lei Liu, Robert J. Ehr, John M. Atkinson
Abstract: This invention relates to methods for treating or inhibiting cancers in a mammal in need thereof, which comprises administering an effective amount of a 6-Aryl-7-halo-imidazo[1,2 -a]pyrimidine compound of the formula: or pharmaceutically acceptable salts thereof.
Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
Type:
Application
Filed:
August 19, 2010
Publication date:
March 17, 2011
Applicant:
NOVARTIS AG
Inventors:
Miao DAI, Xingnian FU, Feng HE, Lei JIANG, Yue LI, Fang LIANG, Lei LIU, Yuan MI, Yao-chang XU, Guoliang XUN, Xiaoxia YAN, Zhengtian YU, Ji Yue ZHANG
Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.
Type:
Application
Filed:
May 14, 2008
Publication date:
March 17, 2011
Applicant:
OTSUKA PHARMACEUTICAL FACTORY, INC.
Inventors:
Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
Abstract: The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins.
Type:
Application
Filed:
December 12, 2008
Publication date:
March 3, 2011
Applicant:
ALLA CHEM, LLC
Inventors:
Andrey Alexandrovich Ivaschenko, Yan Vadimovich Lavrovsky, Sergey Viktorovich Malyarchuk, Ilya Matusovich Okun, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Alexander Vasilievich Ivaschenko
Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
Type:
Application
Filed:
June 27, 2008
Publication date:
March 3, 2011
Inventors:
Zhaoning Zhu, William J. Greenlee, Robert D. Mazzola, JR., Jun Qin, Xianhai Huang, Anandan Palani
Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
Type:
Application
Filed:
March 13, 2009
Publication date:
March 3, 2011
Applicants:
The Brigham and Women's Hospital, Inc., The General Hospital Corporation
Inventors:
Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
Abstract: A series of new chemical agents that demonstrate anti-tumor activity are described. The new chemical agents combine two major mechanisms of anti-tumor action. In an embodiment, the agents are capable of both inhibiting EGFR and damaging DNA while also, upon degradation, degrading to an inhibitor of EGFR and to an agent capable of damaging DNA. Moreover, a novel series of molecules capable of releasing two moles of EGFR inhibitor and a potent bi-functional alkylating agent are also described.
Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Type:
Application
Filed:
July 26, 2010
Publication date:
January 27, 2011
Applicant:
Gilead Palo Alto, Inc.
Inventors:
Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
Type:
Application
Filed:
December 4, 2008
Publication date:
January 20, 2011
Inventors:
Xianhai Huang, Anandan Palani, Jun Qin, Robert Aslanian, Zhaoning Zhu, William Greenlee, Hubert Josien, Wei Zhou, Xiaohong Zhou, Chad E. Bennett, Dmitri Pissarnitski, Mihirbaran Mandal, Pawan Dhondi, Troy McCracken, Thomas Bara, Zhiqiang Zhao, Duane Burnett, John Clader
Abstract: The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase ?, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase ? of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.
Type:
Grant
Filed:
December 27, 2007
Date of Patent:
January 18, 2011
Assignee:
AstraZeneca AB
Inventors:
Shaun P. Jackson, Alan D. Robertson, Vijaya Kenche, Philip Thompson, Hishani Prabaharan, Karen Anderson, Belinda Abbott, Isaac Goncalves, Warwick Nesbitt, Simone Shoenwaelder, Dilek Saylik
Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
Type:
Application
Filed:
August 4, 2008
Publication date:
January 13, 2011
Inventors:
Zhaoning Zhu, William J. Greenlee, John P. Caldwell, Robert D. Mazzola, JR., Brian McKittrick, Chad E. Bennett, Xianhai Huang, Hubert B. Josien, Duane A. Burnett
Abstract: There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ring, an optionally substituted piperidine ring or an optionally substituted perhydroazepine ring, Z1 and Z3 independently represent a bond or an optionally substituted divalent linear hydrocarbon group, Z2 represents —N(R1)—, —O—, —S(O)—, —S(O)2—, —CO—, —CH(R1)— or a bond, ring B represents an optionally substituted imidazole ring, wherein a substituent which the optionally substituted imidazole ring represented by ring B may have may be taken together with R1 to form an optionally substituted ring, and a represents 0
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
June 23, 2010
Publication date:
December 30, 2010
Applicant:
Array BioPharma Inc.
Inventors:
Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.
Type:
Application
Filed:
December 1, 2008
Publication date:
November 25, 2010
Applicant:
MERCK FROSST CANADA LTD
Inventors:
Michel Belley, Denis Deschenes, Rejean Fortin, Jean-Francois Fournier, Sebastien Gagne, Yves Gareau, Jacques Yves Gauthier, Lianhai Li, Joel Robichaud, Michel Therien, Geoffrey K. Tranmer, Zhaoyin Wang
Abstract: The present invention provides a method of decreasing the level of ubiquitylated protein in a subject, the method comprising administering a heterocyclic compound disclosed herein or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof.
Type:
Application
Filed:
May 11, 2010
Publication date:
November 25, 2010
Inventors:
Kim Nicholas Green, Eckard Weber, Tilman Oltersdorf, Sharon Rogers, Frank LaFerla
Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Grant
Filed:
March 4, 2005
Date of Patent:
October 26, 2010
Assignee:
Merck & Co., Inc.
Inventors:
Peter D. Williams, John S. Wai, Mark W. Embrey, Donnette D. Staas, Linghang Zhuang
Abstract: Novel compounds of the formula (I), in which W, T, R1, R2, R3, R4, R5, R6 and X7 have the meanings indicated in Patent Claim 1, are suitable as antidiabetics.
Type:
Application
Filed:
September 13, 2008
Publication date:
September 30, 2010
Applicant:
MERCK PATENT GESELLSCHAFT BESCHRANKTER HAFTUNG
Inventors:
Markus Klein, Werner Mederski, Christos Tsaklakidis, Norbert Beier
Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Application
Filed:
June 7, 2006
Publication date:
September 2, 2010
Inventors:
Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang
Abstract: Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
Type:
Application
Filed:
April 6, 2010
Publication date:
August 26, 2010
Applicant:
Takeda Pharmaceutical Company Limited
Inventors:
Qing Dong, David J. Hosfield, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
Abstract: Disclosed are imidazo[1,2-c]pyrimidin-2-ylmethyl substituted piperidine derivatives having the formula: where Ar is and where R1, R2, R3, n, p and q are as defined herein, and their use as pharmaceuticals.
Type:
Application
Filed:
July 1, 2008
Publication date:
August 19, 2010
Inventors:
Giuseppe Alvaro, David Amantini, Sandro Belvedere
Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
Type:
Grant
Filed:
August 14, 2008
Date of Patent:
August 17, 2010
Assignee:
Bayer Schering Pharma AG
Inventors:
Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
February 9, 2010
Publication date:
August 5, 2010
Applicant:
Gilead Palo Alto, Inc.
Inventors:
Matthew Abelman, Robert Jiang, Jeff Zablocki
Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
Type:
Application
Filed:
July 16, 2008
Publication date:
August 5, 2010
Inventors:
Ian Bruce, Darren Mark Legrand, James Dale, Thomas Anthony Hunt
Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
Type:
Application
Filed:
February 11, 2008
Publication date:
August 5, 2010
Applicants:
SCHERING CORPORATION AND PHARMACOPEIA, LLC, PHARMACOPEIA, INC.
Inventors:
Manuel De lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie L. Ciesla, Chia-yu Huang, Bo Liang
Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
Type:
Application
Filed:
March 25, 2010
Publication date:
July 22, 2010
Inventors:
Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
Abstract: The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.
Type:
Grant
Filed:
June 12, 2006
Date of Patent:
July 20, 2010
Assignee:
Schering Corporation
Inventors:
Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
Abstract: The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations.
Type:
Grant
Filed:
January 19, 2005
Date of Patent:
July 6, 2010
Assignee:
Actimis Pharmaceuticals, Inc.
Inventors:
Tai-Wei Ly, Takashi Yoshino, Yuki Takekawa, Takuya Shintani, Hiromi Sugimoto, Kevin Bacon, Klaus Urbahns
Abstract: The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
Type:
Grant
Filed:
May 21, 2008
Date of Patent:
July 6, 2010
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Stefanie Flohr, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Pavel Safar, James Spoonamore, Martin Smrcina
Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated 3-amyloid deposits or 3-amyloid levels in a patient.
Type:
Application
Filed:
March 5, 2010
Publication date:
July 1, 2010
Applicant:
Wyeth LLC
Inventors:
Michael Sotirios Malamas, Keith Douglas Barnes, Matthew Robert Johnson
Abstract: The present invention provides a method of inducing cleavage of amyloid precursor protein to produce an approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof, wherein the approximately 17 kilodalton fragment includes the carboxyterminal amino acid sequence of amyloid precursor protein and amyloid-beta amino acid sequence. Also provided is a screening method for identifying compounds induce cleavage of amyloid precursor protein to produce the approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein.
Type:
Application
Filed:
December 15, 2009
Publication date:
July 1, 2010
Inventors:
Kim Nicholas Green, Tilman Oltersdorf, Eckard Weber
Abstract: The present invention relates to azolopyrimidines of the formula I in which the substituents are defined according to the description, to processes and intermediates for preparing these compounds, to compositions comprising them and to their use for controlling phytopathogenic harmful fungi.
Type:
Application
Filed:
July 5, 2007
Publication date:
June 24, 2010
Applicant:
BASF SE
Inventors:
Jochen Dietz, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou