Q Is Monocyclic Patents (Class 514/604)
-
Publication number: 20130165523Abstract: The present invention concerns a method for treating and/or preventing a disease in a subject comprising the step of administrating an effective amount of a compound of formula I to a subject in need thereof.Type: ApplicationFiled: November 5, 2012Publication date: June 27, 2013Applicants: Universite Montpellier 2 Sciences Et Techniques, Centre National De Al Recherche Scientifique (CNRS)Inventors: Centre National De Al Recherche Scientifique (CN, Universite Montpellier 2 Sciences Et Techniques
-
Publication number: 20130165460Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
-
Publication number: 20130158063Abstract: Disclosed are compounds, compositions and methods related PPAR antagonists. Certain compounds are effective at inhibiting PPARs. The compositions can be used to inhibit PPARs, treat cancer and treat metabolic disorders.Type: ApplicationFiled: August 24, 2011Publication date: June 20, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Milton Lang Brown, Yali Kong, Yong Liu, Robert Glazer, York Tomita
-
Publication number: 20130150333Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).Type: ApplicationFiled: February 13, 2013Publication date: June 13, 2013Applicant: ORPHAGEN PHARMACEUTICALSInventor: Orphagen Pharmaceuticals
-
Publication number: 20130123287Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Hiroyuki Hayashi
-
Publication number: 20130109658Abstract: A method of treating Friedreich's Ataxia with compounds of formula I including pharmaceutically acceptable salts, tautomers or stereoisomers of compounds of formula Lp.Type: ApplicationFiled: December 7, 2010Publication date: May 2, 2013Inventors: Roberto Testi, Ottaviano Incani
-
Patent number: 8425890Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.Type: GrantFiled: February 23, 2010Date of Patent: April 23, 2013Inventors: David J. Schneider, Charles A. Schneider
-
Publication number: 20130090367Abstract: This application relates to the modulation of host cell factors required for influenza virus replication. The application relates to compounds, including nucleic acid compounds (such as, e.g., small interfering RNAs (siRNAs)) and small molecules, that target human host cell factors involved in influenza virus replication, and the use of such compounds for modulating influenza virus replication and as antiviral agents. The application also relates to methods of treating an influenza virus infection and methods of treating or preventing a symptom or disease associated with influenza virus infection, comprising administering to a subject a composition comprising a compound, such as a nucleic acid compound (e.g., an siRNA) or small molecule, that targets a human host cell factor involved in influenza virus replication.Type: ApplicationFiled: December 10, 2010Publication date: April 11, 2013Inventors: Megan Shaw, Peter Palese, Adolfo Garcia-Sastre, Silke Stertz, John Young, Renate König, Sumit Chanda
-
Publication number: 20130090385Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy.Type: ApplicationFiled: November 28, 2012Publication date: April 11, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventor: Merck Patent Gesellschaft mit Beschrankter Haftu
-
Patent number: 8389739Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).Type: GrantFiled: May 24, 2011Date of Patent: March 5, 2013Assignee: Orphagen PharmaceuticalsInventors: Scott Thacher, Xiaolin Li, Robert Babine, Bruno Tse
-
Publication number: 20130053417Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.Type: ApplicationFiled: March 21, 2012Publication date: February 28, 2013Applicant: JAPAN TOBACCO INC.Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
-
Patent number: 8377639Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: GrantFiled: June 25, 2010Date of Patent: February 19, 2013Assignee: University of MassachusettsInventor: Sean Ryder
-
Publication number: 20130005802Abstract: Methods of treating Wnt/Frizzled-related diseases, comprising administering niclosamide compounds are provided. Methods of predicting whether a disease will respond to treatment with a niclosamide compound are also provided.Type: ApplicationFiled: September 21, 2010Publication date: January 3, 2013Inventors: Wei Chen, Minyong Chen, H. Kim Lyerly, Lawrence S. Barak, Robert Mook, Takuya Osada, Michael A. Morse
-
Publication number: 20120329877Abstract: The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R1 is H or C1-6alkyl and R2 is H, C1-6 alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and X is O or N; as well as tautomers and pharmaceutically acceptable salt forms thereof. Uses of these compounds are also described.Type: ApplicationFiled: June 6, 2012Publication date: December 27, 2012Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Onur Atasoylu, Carlo Ballatore, Kurt R. Brunden, Longchun Huang, Donna M. Huryn, Michael James, Virginia M.Y. Lee, Francesco Piscitelli, Amos B. Smith, III, James Soper, John Q. Trojanowski
-
Patent number: 8329754Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: June 21, 2011Date of Patent: December 11, 2012Assignee: Novartis AGInventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
-
Patent number: 8324190Abstract: Methods of treating cancer using compounds according to Formula (I) are disclosed herein, wherein X, X1, X2, Ra, R1, R2, R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.Type: GrantFiled: July 14, 2009Date of Patent: December 4, 2012Assignees: Temple University—Of The Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
-
Patent number: 8318810Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: GrantFiled: September 19, 2007Date of Patent: November 27, 2012Assignees: University of Maryland, Baltimore, The United States of America as represented by the Department of Veterans AffairsInventors: J. Marc Simard, Mingkui Chen
-
Publication number: 20120283249Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.Type: ApplicationFiled: June 17, 2009Publication date: November 8, 2012Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
-
Publication number: 20120282180Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration.Type: ApplicationFiled: June 8, 2011Publication date: November 8, 2012Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
-
Publication number: 20120270902Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).Type: ApplicationFiled: February 13, 2012Publication date: October 25, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Martin Neitzel, Jennifer Marugg
-
Publication number: 20120252820Abstract: Methods of identifying compounds that potentiate the activity of antifungal agents, potentiators identified by these methods, and methods of using potentiators to treat fungal infections are disclosed.Type: ApplicationFiled: April 22, 2009Publication date: October 4, 2012Applicant: NORTHEASTERN UNIVERSITYInventors: Kim Lewis, Michael David Lafleur
-
Patent number: 8268885Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.Type: GrantFiled: September 10, 2004Date of Patent: September 18, 2012Assignee: Janssen R&D IrelandInventors: Koenraad Lodewijk August Van Acker, Piet Tom Bert Paul Wigerinck, Lieve Emma Jan Michiels, Abdellah Tahri
-
Publication number: 20120225913Abstract: The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: The Medicine Company (Leipzig) GmbHInventors: Torsten STEINMETZER, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soeffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghisch, Jochen Heinicke
-
Publication number: 20120225882Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: May 11, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Thomas Leutert, Jonathan E. Grob, Ruben Alberto Tommasi, Erin E. Pusateri, Ayako Honda
-
Publication number: 20120220635Abstract: The present invention relates to aromatic compounds of the formula (I) and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.Type: ApplicationFiled: February 27, 2012Publication date: August 30, 2012Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
-
Patent number: 8242118Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: GrantFiled: April 19, 2010Date of Patent: August 14, 2012Assignee: Axikin Pharmaceuticals Inc.Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
-
Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
-
Patent number: 8227639Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.Type: GrantFiled: September 26, 2008Date of Patent: July 24, 2012Assignees: Cardioxyl Pharmaceuticals, The Johns Hopkins UniversityInventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
-
Publication number: 20120178805Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.Type: ApplicationFiled: March 13, 2012Publication date: July 12, 2012Inventor: Yousef Al-Abed
-
Publication number: 20120178747Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: July 12, 2012Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
-
Publication number: 20120165360Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Applicant: THERAVANCE, INC.Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
-
Publication number: 20120157487Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
-
Publication number: 20120157465Abstract: A number of DNA methylation inhibitors are described. The DNA methylation inhibitors were identified using a two-component enhanced green fluorescent protein reporter system to screen a compound library containing procainamide derivatives. The DNA methylation inhibitors can be used for cancer therapy and prevention.Type: ApplicationFiled: December 19, 2011Publication date: June 21, 2012Applicant: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Arthur Y. Shaw, Yu-Wei Leu, Shu-Huei Hsiao
-
Publication number: 20120148604Abstract: The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.Type: ApplicationFiled: August 20, 2010Publication date: June 14, 2012Applicant: TRANSPOSAGEN BIOPHARMACEUTICALS, INC.Inventors: Eric M. Ostertag, John Stuart Crawford
-
Patent number: 8193389Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).Type: GrantFiled: March 11, 2005Date of Patent: June 5, 2012Assignee: Elan Pharmaceuticals, Inc.Inventors: Martin Neitzel, Jennifer Marugg
-
Patent number: 8193184Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.Type: GrantFiled: April 20, 2008Date of Patent: June 5, 2012Assignee: Unimed Pharma, SPOL, S.R.O.Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
-
Publication number: 20120134929Abstract: The present invention provides a method of treating a macrophage related disease comprising administering to a subject in need thereof an effective amount of an oxidative agent or an immunosuppressive agent. The present invention also provides a method of modulating macrophage accumulation or activation comprising administering to a subject in need thereof an effective amount of an oxidative agent or an immunosuppressive agent. The oxidative agent can be chlorite or a chlorite containing compound.Type: ApplicationFiled: July 23, 2010Publication date: May 31, 2012Inventors: Michael S. McGrath, Arasteh Ari Azhir
-
Patent number: 8183293Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: GrantFiled: December 18, 2008Date of Patent: May 22, 2012Assignee: Amgen Inc.Inventors: Mark Grillo, An-Rong Li, Jiwen Liu, Julio C. Medina, Yongli Su, Yingcai Wang, Janan Jona, Alan Allgeier, Jacqueline Milne, Jerry Murry, Joseph F. Payack, Thomas Storz
-
Publication number: 20120122787Abstract: The present invention is directed to, inter alia, methods of treating or ameliorating an effect of a polycystic disease. This method include administering to a patient in need thereof an amount of a modulator of a histone deacetylase (HDAC) path-way, which is sufficient to treat or ameliorate an effect of a polycystic disease, particularly a polycystic kidney disease.Type: ApplicationFiled: July 9, 2010Publication date: May 17, 2012Inventor: Rong Li
-
Publication number: 20120122920Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.Type: ApplicationFiled: December 22, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
-
Publication number: 20120108573Abstract: 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: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Inventors: Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
-
Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
-
Publication number: 20120095024Abstract: The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I).Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicants: Elara Pharmaceuticals GmbH, European Molecular Biology Laboratory (EMBL)Inventors: Jorge Alonson, Arantxa Encionas Lopez, Marcel Muelbaler, Lochen Ammenn, Bernd Vendt, Joe Lewis, Christoph Schultes, Bernd Janssen
-
Publication number: 20120094964Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.Type: ApplicationFiled: May 6, 2010Publication date: April 19, 2012Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
-
Publication number: 20120065204Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
-
Patent number: 8119693Abstract: Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases.Type: GrantFiled: May 8, 2008Date of Patent: February 21, 2012Assignee: Sanford-Burnham Medical Research InstituteInventors: Jose Luis Millan, Eduard Sergienko
-
Publication number: 20120035179Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: ApplicationFiled: March 9, 2011Publication date: February 9, 2012Inventors: Sara S. Hadida-Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
-
Patent number: 8101657Abstract: The invention provides a plant disease and insect damage control composition including, as active ingredients, dinotefuran and at least one fungicidal compound; and a plant disease and insect damage prevention method that includes applying such a composition to a plant body, soil, plant seed, stored cereal, stored legume, stored fruit, stored vegetable, silage, stored flowering plant, or export/import timber. The invention provides a new plant disease and insect damage control composition and a plant disease and insect damage prevention method with very low toxicity to mammals and fishes, the composition and method showing an effect against plural pathogens and pest insects, including emerging resistant pathogens and resistant pest insect, by application to a plant body, soil, plant seed, stored cereal, stored legume, stored fruit, stored vegetable, silage, stored flowering plant, or export/import timber.Type: GrantFiled: November 22, 2007Date of Patent: January 24, 2012Assignee: Mitsui Chemicals, Inc.Inventors: Eiichi Yamada, Ryutaro Ezaki, Hidenori Daido
-
Publication number: 20110313000Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
-
Patent number: 8076376Abstract: Aniline sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R1, R2, R3, R4, R5, R6, and L are set forth in the description.Type: GrantFiled: July 21, 2006Date of Patent: December 13, 2011Inventors: Jay P. Powers, Xiao He, Dustin McMinn, Yosup Rew, Daqing Sun