Acyclic Nitrogen Double Bonded To Acyclic Nitrogen, Acyclic Nitrogen Triple Bonded To Acyclic Nitrogen Or Azide Doai Patents (Class 514/150)
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Publication number: 20130210773Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic 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: June 21, 2011Publication date: August 15, 2013Inventor: Craig W. Lindsley
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Publication number: 20130210774Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.Type: ApplicationFiled: August 26, 2011Publication date: August 15, 2013Applicants: EMORY UNIVERSITY, RFS PHARMA, LLCInventors: Steven J. Coats, Franck Amblard, Hongwang Zhang, Longhu Zhou, Richard Anthony Whitaker, Tamara Rosario McBrayer, Raymond F. Schinazi, Junxing Shi
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Publication number: 20130210772Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer.Type: ApplicationFiled: April 15, 2011Publication date: August 15, 2013Applicant: COLBY PHARMACEUTICAL COMPANYInventors: Hirak S. Basu, David A. Zarling, George Wilding, Farideh Mehraein-Ghomi, Dawn R. Church
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Publication number: 20130209550Abstract: Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and/or a delivery agent, such as a liposome.Type: ApplicationFiled: July 28, 2011Publication date: August 15, 2013Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Brian Agnew, David Graham, Upinder Singh, Scott Grecian
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Publication number: 20130210766Abstract: Compositions containing a small molecule therapeutic and an alkyl N,N-disubstituted amino acetate are disclosed. Inclusion of the alkyl N,N-disubstituted amino acetate enhances the pharmacokinetic properties of the small molecule therapeutic.Type: ApplicationFiled: May 4, 2011Publication date: August 15, 2013Applicant: NEXMED HOLDINGS, INC.Inventors: Bassam B. Damaj, Richard Martin
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Patent number: 8506989Abstract: The invention relates to a preparation comprising a creatine component, which has excellent bio-availability and leads to improved creatine retention in the human and animal body. The present invention further relates to a method for the production of said preparation, and to the use thereof as a nutritional supplement, functional food, animal feed additive, pharmaceutical, and as an additive for cosmetic and dermatologic formulations.Type: GrantFiled: December 18, 2008Date of Patent: August 13, 2013Assignee: AlzChem Trostberg GmbHInventors: Thomas Gastner, Frauke Warrikoff, Barbara Nieβ, Josef Fuest
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Publication number: 20130202654Abstract: A topical foam pharmaceutical composition for rectal administration comprising rifaximin in the form of nanosized particles is described. Also described is a method of making the composition and the use of the composition to as a medicament.Type: ApplicationFiled: November 23, 2010Publication date: August 8, 2013Applicant: CIPLA LIMITEDInventors: Amar Lulla, Geena Malhotra, Shrinivas Madhukar Purandare
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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Publication number: 20130184241Abstract: The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.Type: ApplicationFiled: July 28, 2011Publication date: July 18, 2013Applicant: KYOTO UNIVERSITYInventors: Akira Kakizuka, Seiji Hori, Toshiyuki Shudo, Tomohiro Fuchigami
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Patent number: 8476249Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.Type: GrantFiled: May 6, 2010Date of Patent: July 2, 2013Assignee: GlaxoSmithKline LLCInventors: Connie L. Erickson-Miller, Michael Arning
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Patent number: 8466131Abstract: A compound of Formula I: (I) has activity as a cannabinoid receptor antagonist. In Formula 1, R1 is unsubstituted or substituted aryl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted heteroaryl; R2 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl; and R3 is unsubstituted or substituted alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted heteroaralkyl; with the proviso that at least one of Ri and R3 is other than unsubstituted aralkyl or R2 is other than unsubstituted aryl.Type: GrantFiled: October 31, 2008Date of Patent: June 18, 2013Assignee: University of Pittsburgh—of the Commonwealth System of Higher EducationInventors: Xiangqun Xie, Jianzhong Chen, Yuxun Zhang
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Publication number: 20130150332Abstract: 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: EMORY UNIVERSITYInventor: Emory University
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Patent number: 8445466Abstract: The present invention provides amide-protected creatine molecules and compositions, containing one or more bioactive forms of creatine in aqueous compositions, wherein bioactive forms of creatine do not appreciably degrade into creatinine. Also provided are various beneficial effects of administering aqueous compositions having at least one amide-protected creatine molecule.Type: GrantFiled: April 8, 2010Date of Patent: May 21, 2013Inventor: John H. Owoc
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Publication number: 20130123216Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: ApplicationFiled: October 19, 2012Publication date: May 16, 2013Applicants: ALLIANT TECHSYSTEMS INC., RADIORX, INC., C/O INTERWEST VENTURE PARTNERSInventors: RADIORX, INC., C/O INTERWEST VENTURE PA, ALLIANT TECHSYSTEMS INC.
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Publication number: 20130115257Abstract: Methods and compositions for treating biofilms and diseases associated with amyloidosis such as Alzheimer's, Parkinson's and Huntington's disease, and Type 2 diabetes, by destroying amyloid fibrils in a two-step treatment are disclosed. The first step consists of binding to the amyloid fibril an intercalating molecule with a negatively charged group such as Congo red. The second step consists of adding metal ions, such as silver, gold(I), copper(I), palladium or lead ions or metal colloids of silver or gold, which destabilize the amyloid-dye complex. This process results in a disintegration of the fibril into peptide monomers and small aggregates of monomers.Type: ApplicationFiled: July 8, 2011Publication date: May 9, 2013Applicant: KATHOLIEKE UNIVERSITEIT LEUVENInventors: Maarten Gysemans, Johan Snauwaert, Chris Van Haesendonck
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Publication number: 20130078186Abstract: The present invention relates to compounds suitable as modulators of protein misfolding and/or protein aggregation. The compounds are particularly suitable as inhibitors of amyloid aggregate formation and/or modulators of amyloid surface properties, and/or as activators of degradation or reduction of amyloid aggregates.Type: ApplicationFiled: March 23, 2011Publication date: March 28, 2013Applicant: MAX-DELBRUECK-CENTRUM FUER MOLEKULARE MEDIZINInventors: Erich Wanker, Thomas Wiglenda, Julius Tachu Babila, Annett Boeddrich, Michael Schmidt, Franziska Schiele
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Patent number: 8404665Abstract: The present invention provides for a method of simultaneously treating both cancer and the Multidrug Resistance Phenotype via inhibition of cellular thiols, such as Glutathione S-Transferase (GST). This enzyme is overproduced in leukemia and solid tumor cells and is one of the main pathways involved in the Multidrug Resistance phenotype. The treatment provides for the administration of a chemically inert pro-drug, designed to be a specific substrate for the GST enzyme that, once cleaved, liberates the bioactive toxin Nitric Oxide (NO) intracellularly at the site of a malignant growth. NO then acts to inhibit the growth of the malignant cells and to induce cellular differentiation and apoptosis therein, effectively treating an existing cancerous condition. Additionally, once NO is liberated from the pro-drug, the remaining structure acts to inhibit further GST activity, providing a treatment for the Multidrug Resistant phenotype.Type: GrantFiled: March 21, 2003Date of Patent: March 26, 2013Inventor: Paul Shami
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Publication number: 20130065862Abstract: A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.Type: ApplicationFiled: April 4, 2012Publication date: March 14, 2013Applicant: Salix Pharmaceuticals, Inc.Inventor: Lorin Johnson
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Publication number: 20130065864Abstract: The present invention relates to novel iridium and/or rhodium containing complexes for use as a cytotoxic, such as an anti-cancer agent. There is also provided a method of preparing said compounds.Type: ApplicationFiled: May 20, 2011Publication date: March 14, 2013Applicant: UNIVERSITY OF WARWICKInventors: Abraha Habtemariam, Zhe Liu, Joan Josep Soldevila, Ana Maria Pizarro, Peter John Sadler
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Publication number: 20130065863Abstract: Disclosed is a compound of the formula (I) or a pharmaceutically acceptable salt thereof: (I) in which R1, R2, R3, and R4 are defined herein and pharmaceutical compositions thereof. Further provided is a method of treating various disorders, such as a disorder selected from the group consisting of a cardiovascular disorder, cancer, chronic pain, alcohol dependence, and inflammation in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt of formula (I).Type: ApplicationFiled: March 18, 2011Publication date: March 14, 2013Applicants: The Arizona Board of Regents, on behalf of the University of Arizona, Office of Technology Transfer, NIHInventors: Katrina M. Miranda, David A. Wink, Debra J. Salmon, Debashree Basudhar, Larry K. Keefer, Joseph E. Saavedra, Daniela Andrei
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Publication number: 20130059823Abstract: A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen, deuterium, —OH, —OC1-6alkyl, or halogen; R8 is hydrogen, deuterium, or C1-6alkyl; R11 and R12 are independently hydrogen, —C1-6alkyl, —OH, —OC1-6alkyl, or halogen; R13 and R14 are independently —C1-6alkyl, —(CH2)1-2OH, or —OC1-6alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R15 is (CR1R2)nC(O)OR16, wherein n is 0, 1 or 2, —C(O)NHCH(R17)OR16, or —C(O)NHCH(R17)C(O)NHCH(R18)C(O)OR16; R16 is hydrogen, C1-6alkyl, or (CH2)1-2N+R19R20R21; R1, R2, R4, R5, R6, R7, R9, R10, R17, R18, R19, R20, and R21 are independently hydrogen or —C1-6alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.Type: ApplicationFiled: May 16, 2011Publication date: March 7, 2013Inventors: Amjad Ali, Lin Yan, Pei Huo, Ravi Nargund
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Publication number: 20130058915Abstract: Methods for the treatment of Angelman Syndrome autism spectrum disorders are provided. The methods comprise administrating to a subject an agent that increases the expression of or increases activity of, ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) at neuronal synapses.Type: ApplicationFiled: March 1, 2011Publication date: March 7, 2013Applicants: Children's Medica Center Corporation, President and Fellows of Harvard CollegeInventors: Michael E. Greenberg, Paul L. Greer
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Publication number: 20130053348Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: September 12, 2012Publication date: February 28, 2013Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Sing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
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Publication number: 20130053352Abstract: A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, —OH, —O—C1-6 alkyl, ?O, or halogen; R2 is hydrogen, C(O)OR8, C6H5C(O)OR8, (CH2)1-2OH, CR9R10OH, C(O)O(CH2)0-2 aryl, C(O)NR9R10, C(O)SO2NR9R10, C6H5OR9, W—C(O)OR8, W—OR9, Y, or P(O)(OR9)(ORlO); R3 is hydrogen or —C1-6 alkyl; R4 is hydrogen, —OH or —C(O)OR9; R5 is hydrogen or deuterium; R6 and R7 are independently —C1-6 alkyl, fluoro-substituted —C1-6 alkyl, deutero-substituted —C1-6 alkyl or —(CH2)1-2R11, wherein any carbon atom of the fluoro-substituted —C1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C1-6 alkyl is mono- or di-substituted with fluoro; R8, in each instance in which it occurs, is independently hydrogen, —C1-6 alkyl, or —(CH2)2N+(CH3)3; R9 and R10, in each instance in which they occur, are independently —C1-6 alkyl; R11 is —OH, —O—C1-6 alkyl, -0CD3, —OC(O)OC1-6 alkyl, —NH2, —C6H5, —N3, or W; W is an unsubslituted 5- or 6-raembered heteroaryl riType: ApplicationFiled: February 10, 2011Publication date: February 28, 2013Applicant: MERCK SHARP & DOHME CORP.Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lin Yan
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Publication number: 20130039856Abstract: The present invention concerns medicaments for slowing ageing. The medicaments can include an inhibitor of microbial folate biosynthesis as well as agents capable of reducing folate uptake by an animal. Examples of such medicaments include inhibitors that reduce the activity of an enzyme in the folate biosynthesis pathway, such as sulfonamides including sulfamethoxazole. The invention also concerns a food supplement, additive, functional food, or nutraceutial comprising the inhibitor or agent or composition as discussed above, as well as methods for screening for an agent for use as a medicament for slowing ageing comprising determining whether a test agent inhibits microbial folate biosynthesis, or whether the test agent reduces folate uptake by a non-human animal.Type: ApplicationFiled: February 25, 2011Publication date: February 14, 2013Applicant: University of DurhamInventor: David Weinkove
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Publication number: 20130040917Abstract: The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine.Type: ApplicationFiled: September 14, 2012Publication date: February 14, 2013Applicant: Pinnacle Pharmaceuticals, Inc.Inventors: Sidney HECHT, Nour Eddine Fahmi, Samir D. Roy, George Bonneville
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Patent number: 8372822Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.Type: GrantFiled: June 1, 2012Date of Patent: February 12, 2013Assignee: Pliva Hrvatska D.O.O.Inventors: Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
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Publication number: 20130035284Abstract: The present invention concerns methods and compositions involving small molecule inhibitors for the treatment or prophylaxis of flavivirus infection, such as dengue virus and West Nile virus.Type: ApplicationFiled: March 5, 2012Publication date: February 7, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Stanley J. Watowich, Suzanne M. Tomlinson, Scott Gilbertson
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Publication number: 20130029941Abstract: New highly functionalizable Huprine derivatives of formula I: and a method for preparing such compounds and their use for treating neurological diseases in which the level of acetylcholine is affected such as Alzheimer's disease.Type: ApplicationFiled: April 8, 2011Publication date: January 31, 2013Applicant: UNIVERSITE DE ROUENInventors: Cyril Ronco, Pierre Yves Renard, Ludovic Jean, Florian Nachon, Anthony Romieu
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Publication number: 20130023497Abstract: The present invention comprises inter alia triazine compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: June 7, 2010Publication date: January 24, 2013Inventors: Chunlin Tao, Qinwei Wang, Tulay Polat, Laxman Nallan, Neil Desai
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Publication number: 20130023498Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: June 20, 2012Publication date: January 24, 2013Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Patent number: 8357673Abstract: A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as antineurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors.Type: GrantFiled: September 1, 2005Date of Patent: January 22, 2013Assignee: Univerzita Palackeho V OlomouciInventors: Petr Cankar, Iveta Frysova, Vladimir Krystof, Rene Lenobel, Jan Slouka, Miroslav Strnad, Peter Martin Fischer
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Publication number: 20130005693Abstract: The subject invention concerns the reduction of protein aggregation in the neurons of a mammal through the use of a ketogenic treatment such as a ketogenic diet, a physical training regimen and/or administration of agents to increase fatty acid oxidation. Such ketogenic treatment can be useful in the reduction of certain aggregates including amyloid ? peptide, polyglutamine containing huntintin protein, polyglutamine containing androgen receptor, polyglutamine containing atrophin-1, polyglutamine containing ataxins, ?-synclein, prion protein, tau and superoxide dismutase 1 (SOD1).Type: ApplicationFiled: September 10, 2012Publication date: January 3, 2013Applicant: ACCERA, INC.Inventor: Samuel T. Henderson
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Patent number: 8343934Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include naphthalenesulfones, phenylsulfones, and certain peptides with unnatural amino acids and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.Type: GrantFiled: June 30, 2010Date of Patent: January 1, 2013Assignee: University of MemphisInventors: Abby Louise Parrill-Baker, Daniel Lee Baker, Elton Jeffrey North
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Patent number: 8338392Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: GrantFiled: February 20, 2009Date of Patent: December 25, 2012Assignees: The Wistar Institute, North Carolina State UniversityInventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Patent number: 8338140Abstract: The present invention concerns methods and compositions for delivery of therapeutic agents to target cells, tissues or organisms. In preferred embodiments, the therapeutic agents are delivered in the form of therapeutic-loaded polymers that may comprise many copies of one or more therapeutic agents. In more preferred embodiments, the polymer may be conjugated to a peptide moiety that contains one or more haptens, such as HSG. The agent-polymer-peptide complex may be delivered to target cells by, for example, a pre-targeting technique utilizing bispecific or multispecific antibodies or fragments, having at least one binding arm that recognizes the hapten and at least a second binding arm that binds specifically to a disease or pathogen associated antigen, such as a tumor associated antigen. Methods for synthesizing and using such therapeutic-loaded polymers and their conjugates are provided.Type: GrantFiled: September 27, 2011Date of Patent: December 25, 2012Assignee: Immunomedics, Inc.Inventors: Serengulam V. Govindan, Sung-Ju Moon, David M. Goldenberg, Chien-Hsing Chang
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Publication number: 20120309717Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: ApplicationFiled: February 1, 2012Publication date: December 6, 2012Applicant: EISAI INC.Inventors: Vincent J. Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy Dongxia Xing, Qun Liu
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Publication number: 20120294938Abstract: Any pharmaceutical preparation for oral administration with controlled release of active ingredient in the small bowel, on the basis of active ingredient carriers provided with at least one active ingredient which are provided with an inner layer to control the release of active ingredient and with a gastro-resistant coating layer disposed thereon, which is characterized in that the inner layer is formed from at least two diffusion layers whose permeability for the diffusing active ingredient decreases from the inside to the outside, and a method for the production thereof, are described.Type: ApplicationFiled: June 15, 2012Publication date: November 22, 2012Applicant: Dr. R. Pflefger Chemische Fabrik GmbHInventors: Gerd JUNG, Albert SCHAUPP
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Patent number: 8314082Abstract: The present disclosure relates to bisphenyl compounds that are useful for inhibiting the ADP-ribosyl cyclase (ADPR-cyclase). More particularly, the disclosed compounds can be used for treatment and prevention of hypertension, hypertensive cardiac hypertrophy, diabetes, and diabetic nephropathy, in which pathogenesis ADPR-cyclase is involved. The compounds and compositions of the invention can be used for treatment and prevention of cardiovascular disease and related disease states, particularly, hypertension or diabetes related disorders, such as, hypertensive cardiac hypertrophy, diabetic nephropathy, and the like.Type: GrantFiled: May 31, 2011Date of Patent: November 20, 2012Assignee: Industrial Cooperation Foundation Chonbuk National UniversityInventors: Uh-Hyun Kim, Ho-Jeong Kwon, Mie-Jae Im, Seon-Young Kim, Kwang-Hyun Park, So-Young Rah, Tae-Sik Nam, Byung-Ju Kim, Gul Rukhsana
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Patent number: 8288365Abstract: The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine.Type: GrantFiled: January 26, 2011Date of Patent: October 16, 2012Assignee: Pinnacle Pharmaceuticals, Inc.Inventors: Sidney Hecht, Nour Eddine Fahmi, Samir D. Roy, George Bonneville
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Publication number: 20120232039Abstract: A compound having the structure useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.Type: ApplicationFiled: March 5, 2012Publication date: September 13, 2012Inventors: Amjad ALI, Michael Man-Chu Lo, Brent Whitehead, Shrenik K. Shah, Lin Yan, Timothy J. Henderson, Zack Zhiqiang Guo
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Patent number: 8263579Abstract: This invention relates to novel compounds obtained by fermentation of Myxobacteria strain (PM0670013/MTCC 5570). The present invention further relates to the processes for the production of the novel anti-inflammatory compounds, to the culture no. PM0670013 (MTCC 5570), and to pharmaceutical compositions containing compounds of the present invention as an active ingredient and its use in medicines for the treatment of inflammatory diseases or disorders mediated by proinflammatory cytokines such as Tumor Necrosis Factor-alpha (TNF-?) and/or interleukins such as IL-6, having anti-inflammatory activity The invention also includes all stereoisomeric forms of compounds of the present invention.Type: GrantFiled: January 24, 2011Date of Patent: September 11, 2012Assignee: Piramal Healthcare LimitedInventors: Koteppa Pari, Girish Badrinath Mahajan, Nidhi Tomar, Vijaya Phani Kumar Yemparala, Asha Adrian Kulkarni-Almeida, Saji George
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Publication number: 20120213772Abstract: The invention provides for a method for identifying a biomarker in a fecal sample of a subject in need of such identification comprising: determining whether a fecal sample collected from a subject comprises a biomarker.Type: ApplicationFiled: January 13, 2012Publication date: August 23, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Janet R. Jansson, Benjamin Willing, Phillippe Schmitt-Kopplin, Agnes Fekete, Marianna Lucio
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Patent number: 8246942Abstract: The invention relates to synergistic mixtures of o-phenylphenol with other microbicidally active compounds, such as bronopol (2-bromo-2-nitro-1,3-propanedial), 2-methyl-2H-isothiazol-3-one, 1,2-dibromo-2,4-dicyanobutane.Type: GrantFiled: March 1, 2011Date of Patent: August 21, 2012Assignee: LANXESS Deutschland GmbHInventors: Peter Wachtler, Martin Kugler
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Patent number: 8242144Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.Type: GrantFiled: October 15, 2010Date of Patent: August 14, 2012Assignee: Resverlogix Corp.Inventors: Norman C. W. Wong, Joseph E. L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
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Publication number: 20120203102Abstract: This invention is directed to non-benzenoid aromatic compounds. Other aspects include methods of using non-benzenoid aromatic compounds for imaging and phototherapeutic uses thereof. Non-benzenoid compounds provided herein generally have one or more substituent groups which allow tailoring of the spectral properties or provide photoreactivity or targeting ability.Type: ApplicationFiled: September 10, 2010Publication date: August 9, 2012Applicant: MALLINCKRODT LLCInventor: Raghavan Rajagopalan
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Publication number: 20120190651Abstract: This invention relates to novel compounds obtained by fermentation of Myxobacteria strain (PM0670013/MTCC 5570). The present invention further relates to the processes for the production of the novel anti-inflammatory compounds, to the culture no. PM0670013 (MTCC 5570), and to pharmaceutical compositions containing compounds of the present invention as an active ingredient and its use in medicines for the treatment of inflammatory diseases or disorders mediated by proinflammatory cytokines such as Tumor Necrosis Factor-alpha (TNF-?) and/or interleukins such as IL-6, having anti-inflammatory activity The invention also includes all stereoisomeric forms of compounds of the present invention.Type: ApplicationFiled: January 24, 2011Publication date: July 26, 2012Inventors: Koteppa Pari, Girish Badrinath Mahajan, Nidhi Tomar, Vijaya Phani Kumar Yemparala, Asha Adrian Kulkarni-Almeida, Saji George
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Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Patent number: 8217021Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.Type: GrantFiled: August 4, 2011Date of Patent: July 10, 2012Assignee: Pliva Hrvatska D.O.O.Inventors: Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic