The Nitrogen In R Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Bonding Patents (Class 514/620)
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Patent number: 8183295Abstract: The invention relates to a pharmaceutical composition comprising (i) a renin inhibitor, (ii) a calcium channel blocker (CCB), and a diuretic and to a method of using such composition for the treatment of cardiovascular disease.Type: GrantFiled: August 8, 2008Date of Patent: May 22, 2012Assignee: Novartis Pharmaceuticals CorporationInventors: David L Feldman, Randy L Webb
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Publication number: 20120115804Abstract: The invention features compositions and methods for characterizing the methylation status of the Vitamin D Receptor (VDR) in neoplasia (e.g., breast carcinoma), selecting an appropriate therapy, and treating the neoplasia (e.g., breast carcinoma).Type: ApplicationFiled: March 10, 2010Publication date: May 10, 2012Applicant: The John Hopkins UniversityInventors: Radharani Marik, Christopher B. Umbricht, Martha A. Zeiger
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Publication number: 20120107400Abstract: A pH dependent drug delivery system comprising a pH sensitive graft copolymer, a therapeutically active agent and other pharmaceutically acceptable ingredients. More specifically, a composition which is capable of suppressing the drug release in the acidic pH prevalent in the stomach and releasing the drug over an extended period of time at pH prevalent in the intestinal region.Type: ApplicationFiled: March 5, 2010Publication date: May 3, 2012Inventors: Ramesh Muthusamy, Mohan Gopalkrishna Kulkarni
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Publication number: 20120108570Abstract: 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: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Patent number: 8168631Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: February 3, 2009Date of Patent: May 1, 2012Assignee: Allergan, Inc.Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Publication number: 20120077806Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
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Publication number: 20120064130Abstract: The present invention relates to a batch method for impregnating a nonporous polymer pharmaceutical carrier with an active substance, characterised in that said method includes the following consecutive steps: a) mixing the active substance and the nonporous polymer pharmaceutical carrier, the pharmaceutical carrier being in a solid form and insoluble in supercritical CO2 and not being non-crosslinked polyvinylpyrrolidone; b) performing a step of molecular diffusion in the absence of water by contacting, in a static mode without agitation, the mixture obtained in step a) with supercritical CO2 at a pressure of 80 to 170 bars, at a temperature of 31 to 90° C. for 1 to 6 hours; c) recovering the polymer pharmaceutical carrier impregnated with the active substance obtained in step b), the impregnated pharmaceutical carrier being nonporous and being in a solid form and the active substance being in an amorphous form, the method being implemented in the absence of an additional solvent.Type: ApplicationFiled: May 12, 2010Publication date: March 15, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Hubert Lochard, Bernard Freiss
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Publication number: 20120065208Abstract: A method for treating, preventing or ameliorating a hyperliferative disease and/or disorder in a mammal, comprises administering a therapeutically effective amount of one or more compounds selected from the group consisting of a compound of Formula (III), a compound of Formula (IV), and a pharmaceutically acceptable salt of Formula (III) or Formula (IV): wherein R2 is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, vinyl and allyl.Type: ApplicationFiled: September 28, 2011Publication date: March 15, 2012Inventors: Gilles Klopman, Suman K. Chakravarti
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Publication number: 20120053130Abstract: A composition for enhancing absorption of a pharmaceutical which may have poor oral bioavailability, which composition has surprisingly little cytotoxicity, is provided which is in the form of a liquid or semi-solid or solid containing an admixture (1) a mucoadhesive polymer which is a polyacrylic acid polymer, preferably Carbopol 971P, and (2) an absorption or permeation enhancer which preferably is L-?-lyso-phosphatidylcholine (LPC), and which composition is free of polysaccharides. A method for improving bioavailability of a drug which has poor absorption properties is also provided wherein the above bioadhesive composition is administered with said pharmaceutical to the mucosal membrane of the GI tract, nose, oral cavity, sublingual, buccal, and vaginal mucosa. A method for reducing the cytotoxic effect of an absorption enhancer such as LPC is also provided wherein a mucoadhesive polymer as described above is administered with the LPC to a patient in need of treatment.Type: ApplicationFiled: August 30, 2010Publication date: March 1, 2012Inventors: Neil R. Mathias, Lianli Li
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Publication number: 20120046293Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: October 10, 2011Publication date: February 23, 2012Applicant: Merck Frosst Canada Ltd.Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Publication number: 20120041036Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.Type: ApplicationFiled: February 8, 2010Publication date: February 16, 2012Inventors: Isao Kinoyama, Yohei Koganemaru, Takehiro Miyazaki, Takuya Washio
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Publication number: 20120041039Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
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Publication number: 20120041038Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
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Publication number: 20120029013Abstract: The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3? each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.Type: ApplicationFiled: April 2, 2010Publication date: February 2, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Stéphane Cuisiat, Adrian Newman-Tancredi, Olivier Vitton, Bernard Vacher
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Publication number: 20120027844Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.Type: ApplicationFiled: February 9, 2010Publication date: February 2, 2012Applicants: XAVIER UNIVERSITY OF LOUISIANA, TULANE UNIVERSITYInventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
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Publication number: 20120021989Abstract: The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: deCODE Genetics ehf.Inventors: Hilma Holm, Daniel Gudbjartsson
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Publication number: 20120022021Abstract: The present invention relates to mixtures comprising a) a compound of the formula I in which X, m, Q and a are as defined in the description and b) one or more ethylene modulators (II) selected from the group consisting of: inhibitors of ethylene biosynthesis which inhibit the conversion of S-adenosyl-L-methionine into 1-aminocyclopropane-1-carboxylic acid (ACC), inhibitors of ethylene biosynthesis which block the conversion of ACC into ethylene, or inhibitors of ethylene action, and also to compositions comprising them and to their use for controlling harmful fungi.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Applicant: BASF SEInventors: Wilhelm RADEMACHER, John S. HARDEN, Dan E. WESTBERG, Joseph E. ZAWIERUCHA, Thomas J. HOLT, Hendrik YPEMA, Ted R. BARDINELLI, Albert C. EVERSON, Edson BEGLIOMINI
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Publication number: 20120022086Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: March 17, 2010Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20120015909Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).Type: ApplicationFiled: March 30, 2011Publication date: January 19, 2012Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
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Publication number: 20120010296Abstract: The invention provides methods for treating disorders in patients with catechol-o-methyl-transferase inhibitors, such as impulse control disorders and cognitive disorders, such as attention deficit hyperactivity disorder. The invention also provides methods for treating patients with obsessive compulsive disorders and substance addictions with catechol-o-methyl-transferase inhibitors.Type: ApplicationFiled: September 20, 2011Publication date: January 12, 2012Inventor: Jon E. Grant
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Patent number: 8093426Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.Type: GrantFiled: December 3, 2008Date of Patent: January 10, 2012Assignee: Ranbaxy Laboratories LimitedInventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
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Publication number: 20120004269Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: August 3, 2011Publication date: January 5, 2012Applicant: Acucela Inc.Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
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Publication number: 20110319490Abstract: A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I:Type: ApplicationFiled: April 4, 2011Publication date: December 29, 2011Inventors: Kazuko MATSUDA, Yuichi Iwaki, Kale Ruby
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Publication number: 20110311624Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.Type: ApplicationFiled: April 16, 2010Publication date: December 22, 2011Applicant: PHARMACYCLICS, INC.Inventors: David J. LOURY, Joseph J. BUGGY, Tarak D. MODY, Erik J. VERNER, Norbert PURRO, Sriram BALASUBRAMANIAN
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Patent number: 8076515Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.Type: GrantFiled: December 18, 2008Date of Patent: December 13, 2011Assignee: Newron Pharmaceuticals S.p.A.Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
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Patent number: 8076514Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR1 1, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.Type: GrantFiled: July 14, 2006Date of Patent: December 13, 2011Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley
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Publication number: 20110301179Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.Type: ApplicationFiled: October 21, 2009Publication date: December 8, 2011Inventors: Xiangshu Xiao, Bingbing Li
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Patent number: 8063105Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.Type: GrantFiled: July 20, 2006Date of Patent: November 22, 2011Assignee: Merck Canada Inc.Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Publication number: 20110281853Abstract: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Inventors: Rishi Arora, David E. Zembower
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Patent number: 8058476Abstract: A crystalline salt of 3-[2-(dimethylamino)methyl(cyclohex-1-yl)]phenol and hydrogen chloride, preferably in a 1:1 composition, including various crystalline forms of this salt, processes for preparing the various crystalline forms of this salt, pharmaceutical compositions containing the various crystalline forms of this salt, and the use of this salt as a pharmacologically active agent in a pharmaceutical composition to treat or inhibit pain or other disorders or disease states.Type: GrantFiled: January 18, 2008Date of Patent: November 15, 2011Assignee: Gruenenthal GmbHInventors: Michael Gruss, Andreas Fischer, Markus Kegel, Wolfgang Hell, Markus Von Raumer, Joerg Berghausen, Susan Margaret Paul
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Publication number: 20110275615Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unType: ApplicationFiled: October 29, 2010Publication date: November 10, 2011Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
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Patent number: 8053452Abstract: There is provided a novel pest control agent (pesticide), particulally insecticide or miticide. A substituted isoxazoline compound or a substituted enone oxime compound represented by Formula (1) or (2), and apest control agent containing them: wherein A1, A2, A3 and A4 are C or N, G1 is a benzene ring, etc., G2 is 1-trazolyl, etc., X and Y are halogen atom, etc., R3 is haloalkyl, etc., R3a is halogen atom, etc., R3b and R3c are H, etc., is haloalkyl, etc., m is 0-5, n is 0-4.Type: GrantFiled: June 27, 2008Date of Patent: November 8, 2011Assignee: Nissan Chemical Industries, Ltd.Inventors: Takeshi Mita, Kenichi Toyama, Yuki Furukawa, Mitsuaki Komoda
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Publication number: 20110269834Abstract: Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).Type: ApplicationFiled: August 21, 2009Publication date: November 3, 2011Applicants: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Jun Takayama, Andrew David Mesecar, Michael E. Johnson, Kiira M. Ratia, Rima Chaudhuri, Debbie C. Mulhearn
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Publication number: 20110269689Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Inventor: Chongxi Yu
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Patent number: 8048926Abstract: L-DOPA amide derivatives, pharmaceutical compositions containing same and their use in the treatment of conditions associated with impaired dopaminergic activity/signaling (e.g., Parkinson disease) are disclosed.Type: GrantFiled: August 4, 2005Date of Patent: November 1, 2011Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventor: Daphne Atlas
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Publication number: 20110263604Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.Type: ApplicationFiled: April 18, 2011Publication date: October 27, 2011Applicant: Oryzon Genomics, S.A.Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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Publication number: 20110263658Abstract: The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: August 18, 2008Publication date: October 27, 2011Inventors: Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Rejean Fortin, Patrick Lacombe, Daniel McKay, Tom Yao-Hsiang Wu
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Publication number: 20110237541Abstract: Dosage form of aliskiren, comprising a device for transdermal administration of aliskiren and aliskiren (including salts, prodrugs and metabolites thereof), optionally together with pharmaceutically acceptable carrier(s) to a human being or an animal in order to achieve a desired therapeutic effect. Use of a compound comprising aliskiren, optionally encompassing salts, prodrugs and metabolites thereof, and optionally together with pharmaceutically acceptable carrier(s), for the manufacture of a composition to be administered transdermally for achieving a desired therapeutic effect. Method for achieving a desired therapeutic effect by transdermal administration of a compound comprising aliskiren, optionally encompassing salts, prodrugs and metabolites thereof, and optionally together with pharmaceutically acceptable carrier(s).Type: ApplicationFiled: November 23, 2009Publication date: September 29, 2011Inventors: Sylvie Toulmond, Elizabeth Kwong, Dwight MacDonald
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Publication number: 20110218200Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.Type: ApplicationFiled: August 28, 2009Publication date: September 8, 2011Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
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Publication number: 20110212943Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.Type: ApplicationFiled: October 14, 2009Publication date: September 1, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
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Publication number: 20110207783Abstract: The present invention relates to acyclic amino amide renin inhibitor compounds and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: August 4, 2008Publication date: August 25, 2011Inventors: Daniel Dube, Austin Chen, Daniel J. McKay
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Publication number: 20110206781Abstract: Described herein are methods, compositions and kits related to manipulating hematopoietic stem cells (HSC) and more particularly to methods, compositions and kits related to increasing the number of hematopoietic stem cells in vitro, ex vivo and/or in vivo. Also described are methods, compositions and kits related to making an expanded population of HSC and methods, compositions and kits related to using the expanded population of HSC. For example, HSC growth may be enhanced by contacting the nascent stem cells or HSC with an agent that stimulates the nitric oxide signaling pathway.Type: ApplicationFiled: May 28, 2009Publication date: August 25, 2011Inventors: Leonard I. Zon, Trista E. North, Wolfram Goessling
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Patent number: 8003689Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.Type: GrantFiled: June 19, 2009Date of Patent: August 23, 2011Assignee: GTx, Inc.Inventor: Karen A. Veverka
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Publication number: 20110195977Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 23, 2009Publication date: August 11, 2011Inventors: Daniele Fancelli, Varasi Mario, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20110195979Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.Type: ApplicationFiled: February 7, 2011Publication date: August 11, 2011Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
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Publication number: 20110172310Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 11, 2011Publication date: July 14, 2011Applicant: ViroBay, Inc.Inventors: John O. Link, Craig J. Mossman, Jie Liu, Soon Hyung Woo
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Patent number: 7977386Abstract: The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy) -2-hydroxy-2-methylpropanamide and process for producing the same.Type: GrantFiled: September 11, 2008Date of Patent: July 12, 2011Assignee: Universtiy of Tennessee Research FoundationInventors: James T. Dalton, David A. Dickason, David Hong, Thomas G. Bird, Tai Ahn
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Publication number: 20110160308Abstract: Compositions and methods for treating disorders of the outer retina with compounds that inhibit monoamine oxidase are disclosed.Type: ApplicationFiled: July 27, 2007Publication date: June 30, 2011Applicant: ALCON RESEARCH, LTD.Inventors: Robert J. Collier, JR., Michael A. Kapin, John M. Yanni
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Publication number: 20110158983Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.Type: ApplicationFiled: March 5, 2009Publication date: June 30, 2011Inventors: Newell Bascomb, John Maki, Fredric S. Young
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Publication number: 20110160230Abstract: The present invention refers to a ceramic nanosystem constructed for releasing medications in a controlled manner, in the treatment of human beings and animals presenting an organic deficiency which requires the application of said medications. The present invention further refers to the method for preparing said nanosystem, in the form of a ceramic matrix, and also to the method of incorporating a drug to said ceramic matrix, forming a tablet.Type: ApplicationFiled: December 13, 2010Publication date: June 30, 2011Inventors: Antonio Hortencio Munhoz, JR., Richard Wagner Novickis, Leila Figueiredo De Miranda, Sonia Braunstein Faldini, Mauro Cesar Terence, Roberto Rodrigues Ribeiro