Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and respiratory viruses including the common cold.
Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
Type:
Application
Filed:
December 23, 2011
Publication date:
June 21, 2012
Inventors:
David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
Abstract: This invention relates to novel compounds of the Formula (I), (I*), (I**), I, Ia, Ib, Ic, Id, Ie, If, Ig, Il1-3, Im1-3, In1-3, or Io1-2, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Type:
Grant
Filed:
August 11, 2009
Date of Patent:
June 19, 2012
Assignee:
Vitae Pharmaceuticals, Inc.
Inventors:
David A. Claremon, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye, Wei Zhao, Katerina Leftheris
Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
Type:
Grant
Filed:
June 13, 2007
Date of Patent:
June 19, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
June 19, 2012
Assignee:
Cytokinetics, Inc.
Inventors:
Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
Abstract: The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
Type:
Application
Filed:
November 1, 2011
Publication date:
June 7, 2012
Applicants:
Abbott Laboratories, Abbott GmbH & Co. KG
Inventors:
Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
Abstract: The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.
Type:
Application
Filed:
February 27, 2009
Publication date:
June 7, 2012
Applicant:
MIMETICA PTY LTD
Inventors:
Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
Abstract: There is Provided an Agent for Prevention of glaucoma or an agent for prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. An agent for prevention or treatment of glaucoma comprising a Rho kinase inhibitor and a carbonic anhydrase inhibitor in combination.
Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
Type:
Grant
Filed:
September 12, 2008
Date of Patent:
June 5, 2012
Assignee:
Janssen Pharmaceutica NV
Inventors:
James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
Type:
Application
Filed:
November 30, 2011
Publication date:
May 31, 2012
Inventors:
Xiangping QIAN, Chihyuan (Grace) CHUANG, Pu-Ping LU, Bing YAO, Qing (Kevin) LU, Hong JIANG, Wenyue WANG, Bradley P. MORGAN, David J. MORGANS, JR.
Abstract: Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.
Type:
Application
Filed:
May 1, 2010
Publication date:
May 31, 2012
Inventors:
Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty, Geoffrey Richard Heintzelman, Jeffrey D. Yingling, Casey Kopczynski
Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
Type:
Application
Filed:
September 28, 2011
Publication date:
May 31, 2012
Inventors:
Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.
Type:
Application
Filed:
November 1, 2011
Publication date:
May 31, 2012
Inventors:
Alan Ashworth, Stephen Jackson, Niall Martin, Graeme Smith
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase of the following structural formula: The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
August 7, 2008
Date of Patent:
May 29, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Juan-Miguel Jimenez, Guy Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
Type:
Application
Filed:
October 20, 2011
Publication date:
May 24, 2012
Inventors:
Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and compositions, and methods for the administration and use of those compounds. provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing serum, plasma, and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.
Type:
Application
Filed:
October 17, 2011
Publication date:
May 24, 2012
Inventors:
Liangxian Cao, Samit Hirawat, Langdon Miller, Thomas Davis, Marla L. Weetall
Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
Type:
Application
Filed:
January 30, 2012
Publication date:
May 24, 2012
Inventors:
Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
Type:
Application
Filed:
January 26, 2012
Publication date:
May 24, 2012
Inventors:
David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
Type:
Application
Filed:
August 5, 2010
Publication date:
May 24, 2012
Applicant:
KATHOLIEKE UNIVERSITEIT LEUVEN
Inventors:
Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
Type:
Application
Filed:
November 16, 2011
Publication date:
May 24, 2012
Inventors:
Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, and R6 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
Type:
Application
Filed:
November 16, 2011
Publication date:
May 24, 2012
Inventors:
Yan ZHANG, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Kristi Anne Leonard, Joseph Kent Barbay, Umar S.M. Maharoof
Abstract: The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I? and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein n is 1 or 2; R1 is hydrogen or methyl and is positioned vicinal to the radical R1; R2 is hydrogen or methyl; R3 is C1-C3 alkyl; R4 is hydrogen, C1-C4 alkyl, cyclopropyl, C3-C4 cycloalkylmethyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, chlorine, C1-C4 alkyl, fluorinated C1-C4 alkyl, C1-C4 alkoxy or fluorinated C1-C4 alkoxy; and R6 is hydrogen, fluorine or chlorine.
Type:
Grant
Filed:
April 29, 2010
Date of Patent:
May 22, 2012
Assignees:
Abbott Laboratories, Abbott GmbH & Co. KG
Inventors:
Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang
Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
Type:
Application
Filed:
January 23, 2012
Publication date:
May 17, 2012
Applicant:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Application
Filed:
January 11, 2012
Publication date:
May 17, 2012
Applicant:
THERAVANCE, INC.
Inventors:
Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
Type:
Application
Filed:
November 4, 2011
Publication date:
May 17, 2012
Inventors:
Francesco G. Salituro, Jeffrey O. Saunders
Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.
Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.
Type:
Application
Filed:
March 30, 2007
Publication date:
May 17, 2012
Applicant:
Cylene Pharmaceuticals, Inc.
Inventors:
Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.
Type:
Application
Filed:
January 17, 2012
Publication date:
May 17, 2012
Applicant:
Priaxon AG
Inventors:
Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.
Type:
Application
Filed:
November 7, 2011
Publication date:
May 10, 2012
Inventors:
Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
Type:
Application
Filed:
November 7, 2011
Publication date:
May 10, 2012
Inventors:
Gregory A. Demopulos, George A. Gaitanaris
Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.
Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
Type:
Application
Filed:
April 8, 2010
Publication date:
May 10, 2012
Inventors:
Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, JR., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Asshad Siddiqui
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
November 15, 2007
Date of Patent:
May 8, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu
Abstract: Isoquinolone derivatives of the general formula are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.
Type:
Grant
Filed:
April 11, 2008
Date of Patent:
May 8, 2012
Assignee:
H. Lundbeck A/S
Inventors:
Klaus Baek Simonsen, Jan Kehler, Karsten Juhl, Nikolay Khanzhin, Soren Moller Nielsen
Abstract: Compositions for treating, reducing, ameliorating, or preventing infections comprise a fluoroquinolone having Formulae I-VIII and an additional anti-infective agent. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Such compositions and methods can be effective against mixed types of pathogens including certain antibiotic-resistant microbial pathogens found in such infections.
Type:
Grant
Filed:
May 6, 2008
Date of Patent:
May 8, 2012
Assignee:
Bausch & Lomb Incorporated
Inventors:
Praveen Tyle, Erning Xia, Honga Wang, Susan E. Norton, Pramod Kumar Gupta, Keith W. Ward, Lynne Brunner
Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.
Type:
Application
Filed:
January 6, 2012
Publication date:
May 3, 2012
Applicant:
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
Type:
Application
Filed:
January 6, 2012
Publication date:
May 3, 2012
Inventors:
Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
Type:
Application
Filed:
August 26, 2009
Publication date:
May 3, 2012
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.
Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
Type:
Application
Filed:
April 30, 2010
Publication date:
April 26, 2012
Applicants:
Astex Therapeutics Limited, Novartis AG
Inventors:
Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Grialdes, Michael Joseph Luzzio, Lawrence Blas Perez
Abstract: The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
Type:
Grant
Filed:
January 16, 2008
Date of Patent:
April 24, 2012
Assignees:
Wyeth, Siena Biotech S.p.A.
Inventors:
Chiara Ghiron, Arianna Nencini, Iolanda Micco, Riccardo Zanaletti, Laura Maccari, Hendrick Bothmann, Simon N. Haydar, Maurizio Varrone, Carmela Pratelli, Boyd L. Harrison
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Type:
Application
Filed:
October 14, 2011
Publication date:
April 19, 2012
Inventors:
Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
Abstract: This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments.
Type:
Application
Filed:
June 16, 2010
Publication date:
April 19, 2012
Inventors:
Christophe Pierre Alain Chassaing, Thorsten Meyer
Abstract: The present invention relates, in general, to the Smoothened receptor and, in particular, to a method of modulating Smoothened receptor activity and to compounds and compositions suitable for use in such a method.
Type:
Application
Filed:
June 16, 2009
Publication date:
April 19, 2012
Inventors:
Wei Chen, Lawrence Barak, H. Kim Lyerly, Jiangbo Wang
Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, X1, X1, X3, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell pro-liferation, and the use thereof in such a treatment.
Type:
Application
Filed:
September 8, 2009
Publication date:
April 19, 2012
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Andreas Mantoulidis, Georg Dahmann, Peter Ettmayer, Christian Klein, Steffen Steurer, Irene Waizenegger, Stephan Karl Zahn
Abstract: The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is —NR7(CO)R11; R2 is aryl, heteroaryl, fused aryl-C3-6-heterocycloalkyl or fused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted; each R7 is selected from hydrogen, C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6alkyl-C3-7-cycloalkyl, C?-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease.
Type:
Application
Filed:
March 4, 2010
Publication date:
April 12, 2012
Applicant:
MEDICAL RESEARCH COUNCIL TECHNOLOGY
Inventors:
Edward Giles Mciver, Joanne HOUGH, Joanne Hough
Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
Type:
Application
Filed:
December 14, 2011
Publication date:
April 12, 2012
Inventors:
Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van heusden
Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
Type:
Application
Filed:
June 4, 2010
Publication date:
April 5, 2012
Inventors:
Didier Jean-Claude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Wei Xiao, Bryan Branstetter, Guy J. Breitenbucher