Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
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Publication number: 20140235646Abstract: The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.Type: ApplicationFiled: May 5, 2014Publication date: August 21, 2014Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
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Patent number: 8809381Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: GrantFiled: August 18, 2008Date of Patent: August 19, 2014Assignees: The University of Mississippi, L'Universite Catholique de LouvainInventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
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Publication number: 20140227225Abstract: The present invention discloses thioflavine S and primuline derivatives which inhibit hepatitis C virus helicase and protease activity. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are useful as antiviral agents. The present invention further relates to pharmaceutical compositions containing the aforementioned compounds and methods of treating an HCV infection.Type: ApplicationFiled: September 7, 2012Publication date: August 14, 2014Applicants: UWM RESEARCH FOUNDATION, INC., UNIVERSITY OF KANSASInventors: Jeffrey Aube, Brian Scott Jonathan Blagg, Kevin John Frankowski, David Norman Frick, Kelin Li, Frank John Schoenen
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Publication number: 20140228321Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 14, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
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Publication number: 20140228355Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.Type: ApplicationFiled: February 11, 2013Publication date: August 14, 2014Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine, University of Medicine and Dentistry New Jersey Medical School
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Patent number: 8802664Abstract: The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.Type: GrantFiled: September 27, 2011Date of Patent: August 12, 2014Assignee: BioprojectInventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stephane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Publication number: 20140221351Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: April 8, 2014Publication date: August 7, 2014Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
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Publication number: 20140221319Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.Type: ApplicationFiled: April 13, 2012Publication date: August 7, 2014Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard CollegeInventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Patent number: 8796323Abstract: Disclosed are methods of treating and/or preventing infections in mammals caused by microorganisms, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are the use of such defensin-like molecules for treating and/or preventing infections in mammals; and kits that may include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.Type: GrantFiled: November 4, 2011Date of Patent: August 5, 2014Assignee: University of Maryland, BaltimoreInventors: Erik De Leeuw, Alexander D. MacKerell
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Publication number: 20140213584Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 8, 2011Publication date: July 31, 2014Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Publication number: 20140213538Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: January 15, 2014Publication date: July 31, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
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Publication number: 20140205537Abstract: Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.Type: ApplicationFiled: June 22, 2012Publication date: July 24, 2014Applicant: ZENOBIA THERAPEUTICS, INC.Inventors: Pierre-Yves Bounaud, Vicki Nienaber, Ruo W. Steensma, John A. Lowe, III
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Publication number: 20140206676Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: January 12, 2013Publication date: July 24, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Patent number: 8785483Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD.Type: GrantFiled: December 23, 2011Date of Patent: July 22, 2014Assignee: The Board of Regents of the University of Texas SystemInventors: Satish K. Srivastava, Kota V. Ramana, Umesh Yadav
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Publication number: 20140200215Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: March 12, 2013Publication date: July 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20140200212Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: March 17, 2014Publication date: July 17, 2014Applicant: High Point Pharmaceuticals, LLCInventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
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Patent number: 8778979Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.Type: GrantFiled: April 5, 2006Date of Patent: July 15, 2014Assignee: Yale UniversityInventors: Vladimir Coric, John H. Krystal, Gerard Sanacora
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Patent number: 8778981Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.Type: GrantFiled: November 21, 2013Date of Patent: July 15, 2014Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Patent number: 8778938Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Publication number: 20140194425Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20140187593Abstract: Methods and compositions relating to diagnosing and treating a VMAT-2 deficiency disease are described. Provided are methods for screening for, diagnosing or detecting a risk of developing a VMAT-2 deficiency disease comprising detecting the presence of a VMAT-2 variant in a sample of a subject, wherein the presence of the VMAT-2 variant is indicative that the subject has a VMAT-2 deficiency disease or an increased risk of developing a VMAT-2 deficiency disease compared to an individual having wild type VMAT-2. Also provided are methods of treating a VMAT-2 deficiency disease with a dopamine agonist.Type: ApplicationFiled: December 4, 2013Publication date: July 3, 2014Inventor: Berge Minassian
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Publication number: 20140187543Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: September 25, 2013Publication date: July 3, 2014Inventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
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Patent number: 8765150Abstract: Physically and chemically stable aqueous oral suspensions of riluzole and manufacturing methods thereof. The suspensions contain riluzole in particle form and at least a wetting agent, preferably a surfactant. Riluzole is present in amounts from about 0.1% to about 20% w/v and has an average particle size lower than 200 ?m. The suspensions are devoid of the known local (mouth) anaesthetic effects of riluzole.Type: GrantFiled: March 2, 2010Date of Patent: July 1, 2014Assignee: Italfarmaco SpAInventors: Roberta Artico, Marco Adami, Daniele Barbareschi, Jaime Moscoso, Tiziano Oldoni, Paolo Mascagni
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Publication number: 20140179697Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: December 23, 2013Publication date: June 26, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20140178449Abstract: Methods for restoring normal patterns of activity in a subject suffering from Parkinson's Disease are disclosed that include administering an effective steady state concentration of a dopamine modulating compound continuously for a prolonged period of time such that normal patterns of activity are substantially restored in the subject.Type: ApplicationFiled: October 30, 2013Publication date: June 26, 2014Applicant: NuPathe, Inc.Inventors: Terri B. Sebree, Steven J. Siegel
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Publication number: 20140179693Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.Type: ApplicationFiled: December 21, 2012Publication date: June 26, 2014Inventors: Robert Shalwitz, Kevin G. Peters
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Patent number: 8759380Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 13, 2012Date of Patent: June 24, 2014Assignee: Cytokinetics, Inc.Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Patent number: 8759535Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: GrantFiled: February 16, 2011Date of Patent: June 24, 2014Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
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Patent number: 8759539Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: GrantFiled: November 11, 2009Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
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Patent number: 8759381Abstract: Disclosed are fluorescent compounds useful as intracellular pH probes. In particular, the invention teaches a two-photon absorbing, water soluble, fluorescent compound, a fluorene derivative, which is effective as a near-neutral pH indicator and particularly as an intracellular probe. A method for chemical synthesis of the claimed compounds is provided.Type: GrantFiled: July 11, 2012Date of Patent: June 24, 2014Assignee: University of Central Florida Research Foundation, Inc.Inventors: Kevin Belfield, Sheng Yao
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Patent number: 8759537Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.Type: GrantFiled: August 17, 2011Date of Patent: June 24, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn
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Patent number: 8759382Abstract: Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis.Type: GrantFiled: September 29, 2011Date of Patent: June 24, 2014Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Eliezer Falb, Jeffrey Sterling, Yaacov Herzig, Raphael Nudelman, Konstantin Ulanenko
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Publication number: 20140171430Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: April 20, 2012Publication date: June 19, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
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Publication number: 20140171438Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.Type: ApplicationFiled: December 9, 2013Publication date: June 19, 2014Applicant: CELLCEUTIX CORPORATIONInventors: Wenxi Pan, Haizhong Tang
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Patent number: 8754233Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.Type: GrantFiled: February 25, 2013Date of Patent: June 17, 2014Assignee: Dermira (Canada), Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Patent number: 8754113Abstract: A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is —O— or —S—, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.Type: GrantFiled: December 14, 2010Date of Patent: June 17, 2014Assignee: Shionogi & Co., Ltd.Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
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Patent number: 8748433Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: GrantFiled: April 25, 2011Date of Patent: June 10, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Patent number: 8748429Abstract: The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).Type: GrantFiled: April 4, 2012Date of Patent: June 10, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Guanglin Luo, Gene M. Dubowchik, John E. Macor, Ling Chen
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Publication number: 20140155420Abstract: The invention provides small molecule inhibitors of EYA2 phosphatase activity and EYA2 binding to Six1. These inhibitors are proposed for use in methods of treating cancer in a subject, such as those involving Six1 and/or EYA2 disregulation. In some embodiments, the invention further provides for the administration of a second cancer therapy to the subject.Type: ApplicationFiled: January 10, 2012Publication date: June 5, 2014Applicants: The Regents of the University of Colorado, a body corporate, Department of Health and Human ServicesInventors: Rui Zhao, Heide L. Ford, Noel Southall, Erika Englund, Samarjit Patnaik, Marc Ferrer, Wei Zheng, Seameen Dehdashti, Juan Marugan
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Patent number: 8741883Abstract: The invention is in general directed to compounds and methods for diagnosing, preventing or alleviating the symptoms of amyloid-associated diseases, for example, neuronal diseases, such as, for example, Alzheimer's disease, methods of screening for compounds useful in preventing or alleviating the symptoms of amyloid-associated diseases, methods of diagnostic imaging of A-beta fibrils, and compounds and methods useful for studying normal or disease-associated cellular mechanisms relating to amyloid proteins.Type: GrantFiled: January 13, 2010Date of Patent: June 3, 2014Assignee: The Regents of the University of California—San DiegoInventors: Jerry Yang, Petra Inbar
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Publication number: 20140148398Abstract: Compounds useful for the treatment of giardiasis are described.Type: ApplicationFiled: October 12, 2011Publication date: May 29, 2014Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, UNIVERSITY OF MARYLAND, COLLEGE PARKInventors: Wei Zheng, Catherine Chen, Juan Jose Marugan, Noel Southall, Christopher P. Austin, Andrey Galkin, Liudmila Kulakova, Osnat Herzberg
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Publication number: 20140148462Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: November 25, 2013Publication date: May 29, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Elke LANGKOPF, Holger WAGNER
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Publication number: 20140147448Abstract: The invention includes compositions and methods useful for treating preventing abnormal thrombus formation and subsequent cardiovascular disease in diabetic patients and patients with increased cardiovascular risk.Type: ApplicationFiled: June 5, 2012Publication date: May 29, 2014Applicant: Yale UniversityInventors: John Hwa, WaiHo Tang
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Patent number: 8735434Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 15, 2008Date of Patent: May 27, 2014Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Jennifer M. Frost, Sridhar Peddi
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Publication number: 20140140932Abstract: The present disclosure provides functionalized magnetic nanoparticles (MNPs) comprising a functional group that binds to ?-amyloid deposits and/or neurofibrillary tangles. The present disclosure provides compositions comprising the functionalized MNPs, and methods of using the functionalized MNPs in imaging ?-amyloid deposits and neurofibrillary tangles.Type: ApplicationFiled: April 4, 2012Publication date: May 22, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: Masoud Akhtari
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Publication number: 20140141079Abstract: An orally deliverable pharmaceutical composition comprises a therapeutically effective amount of pramipexole or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient, said composition exhibiting at least one of (a) an in vitro release profile wherein on average no more than about 20% of the pramipexole is dissolved within 2 hours after placement of the composition in a standard dissolution test; and (b) an in vivo pramipexole absorption profile following single dose administration to healthy adult humans wherein the time to reach a mean of 20% absorption is greater than about 2 hours and/or the time to reach a mean of 40% absorption is greater than about 4 hours. The composition is useful for oral administration, not more than once daily, to a subject having a condition or disorder for which a dopamine receptor agonist is indicated.Type: ApplicationFiled: January 28, 2014Publication date: May 22, 2014Applicant: Pharmacia CorporationInventors: Ernest J. Lee, Gerard M. Bredael, John R. Baldwin, Steven R. Cox, Mark J. Heintz
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Publication number: 20140142147Abstract: Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.Type: ApplicationFiled: July 18, 2012Publication date: May 22, 2014Applicant: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Maged Henary, W. David Wilson
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Patent number: 8715728Abstract: An extended release pellet comprising an active ingredient selected from pramipexole and the pharmaceutically acceptable salts thereof, and at least one release-modifying excipient.Type: GrantFiled: December 3, 2009Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Thomas Friedl, Rolf-Stefan Brickl
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Patent number: 8716283Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.Type: GrantFiled: April 1, 2009Date of Patent: May 6, 2014Assignees: University of Massachusetts, President and Fellows of Harvard CollegeInventors: Jon Goguen, Ning Pan, Kyungae Lee