Abstract: Disclosed are compounds according to formula (I) as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.
Type:
Grant
Filed:
May 14, 2007
Date of Patent:
May 24, 2011
Inventors:
Duane D. Miller, Gabor Tigyi, Gangadhar G. Durgam, Tamas Virag, Michelle D. Walker, Ryoko Tsukahara
Abstract: This invention relates to new carbocyanine fluorophores comprising a biomolecule targeting moiety containing 1-6 aromatic moieties, wherein the targeting moiety is designed to attach to biocompatible molecules to form in vivo optical imaging agents.
Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea Hydrate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.
Type:
Grant
Filed:
October 15, 2008
Date of Patent:
May 24, 2011
Assignee:
Abbott Laboratories
Inventors:
Thomas B. Borchardt, Michael J. Rozema, Shailendra V. Bordawekar, Alexander F. Chu-Kung
Abstract: The subject invention pertains to pentafluorosulfonyl (SF5) substituted pyrroles, thiophenes, 3-pyrrolines and 2,5-dihydrothiophenes, as well as methods for their synthesis.
Type:
Grant
Filed:
June 17, 2010
Date of Patent:
May 17, 2011
Assignee:
University of Florida Research Foundation, Inc.
Abstract: The present invention encompasses a method for the preparation of Almotriptan and its pharmaceutically acceptable salts comprises, i) Methylation of 3-[5-(1-Pyrrolidinyl sulfonyl methyl)1H-indol-yl]ethane amine ii) Treating crude Almotriptan with a hydroxy benzoic acid yields hydroxy benzoic acid addition salt of Almotriptan iii) Converting Almotriptan hydroxy benzoic acid addition salt to Almotriptan and iv) Salification of Almotriptan to its pharmaceutically acceptable salts.
Abstract: N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N?-(2-fluoro-5-methylphenyl)urea Tolueneate Crystalline Form 1, ways to make it and ways to use it are disclosed.
Abstract: The invention relates to process for the preparation of Candesartan cilexetil. More particularly, it relates to the preparation of pure candesartan cilexetil by the deprotection of Trityl candesartan cilexetil with inorganic acids.
Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
Type:
Grant
Filed:
October 12, 2006
Date of Patent:
May 10, 2011
Assignee:
Neurosearch A/S
Inventors:
William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
Abstract: Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.
Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
Type:
Grant
Filed:
April 9, 2009
Date of Patent:
May 10, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers.
Type:
Grant
Filed:
May 4, 2006
Date of Patent:
May 10, 2011
Assignee:
Chroma Therapeutics Ltd.
Inventors:
Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
Abstract: The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
Type:
Grant
Filed:
June 25, 2008
Date of Patent:
May 3, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
Type:
Grant
Filed:
June 4, 2009
Date of Patent:
May 3, 2011
Assignee:
Athersys, Inc.
Inventors:
Youssef L. Bennani, Bayard Huck, Michael J. Robarge
Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
Type:
Grant
Filed:
December 29, 2007
Date of Patent:
May 3, 2011
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Jing Zhang, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
Type:
Grant
Filed:
May 9, 2008
Date of Patent:
April 26, 2011
Assignees:
InterMune, Inc., Array Biopharma Inc.
Inventors:
Scott Seiwert, Steven W. Andrews, Leonid Beigelman, Lawrence M. Blatt, Brad Buckman, Kevin R. Condroski, Yutong Jiang, Robert J. Kaus, April L. Kennedy, Timothy S. Kercher, Michael A. Lyon, Bin Wang
Abstract: Compounds isolated from the fruiting body of A. camphorata in a solid culture or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. Also disclosed are methods of stimulating immune responses and/or treating an inflammatory disorder with these compounds or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
November 21, 2008
Date of Patent:
April 26, 2011
Assignee:
Well Shine Biotechnology Development Co., Ltd.
Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:
Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].
Abstract: The present invention relates to a process for preparing pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids from 1,4-diketo starting materials. The invention further relates to intermediates in this process formula (I).
Type:
Grant
Filed:
December 16, 2005
Date of Patent:
April 26, 2011
Assignee:
ratiopharm GmbH
Inventors:
Pavel Bobal, Jaroslav Frantisek, Jiri Stohandl, Kane Denike, Armin Boerner, Vitali Tararov, Andrei Korostylev, Gerd Koenig, Nicolas Jeker
Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
Type:
Grant
Filed:
April 2, 2008
Date of Patent:
April 26, 2011
Assignee:
Glaxo Group Limited
Inventors:
Paul John Beswick, David Kenneth Dean, Robert James Gleave, Andrew Peter Moses, Daryl Simon Walter