C=x Bonded Directly Or Indirectly By An Acyclic Carbon Or Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring (e.g., Tryptophan, Etc.) (x Is Chalcogen) Patents (Class 514/419)
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Patent number: 7985764Abstract: It was found that a compound according to the following formula: or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compound shows good pharmacological action as compared to antagonists selective for only one of these receptors. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: GrantFiled: February 7, 2007Date of Patent: July 26, 2011Assignee: Astellas Pharma Inc.Inventors: Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Ryushi Seo, Shinobu Akuzawa
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Publication number: 20110178104Abstract: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.Type: ApplicationFiled: January 5, 2011Publication date: July 21, 2011Applicant: POLYMEDIX INC.Inventors: Richard W. Scott, Dahui Liu, Robert W. Kavash, Trevor Young, Michael J. Costanzo, Carol Ann Mulrooney
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Publication number: 20110178087Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: March 30, 2011Publication date: July 21, 2011Applicant: Compass Pharmaceuticals LLC.Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Publication number: 20110178111Abstract: The main object here is the use of omega-3 polyunsaturated fatty acids (as ethyl esters, hereinafter called “n-3 PUFA”) as a medicament, either alone or in combination with other therapeutic agents, for reducing mortality for a cardiovascular cause, in particular arrhythmia or for reducing hospitalization for any cause, in particular a cardiovascular cause and for the daily administration to patients with symptomatic heart failure (HF) for more than 3.5 years.Type: ApplicationFiled: July 23, 2009Publication date: July 21, 2011Applicants: SPA SOCIETA' PRODOTTI ANTIBIOTICI S.P.A, SIXTERPHARMA S.R.L.Inventors: Claudio Cavazza, Maria Giovanna Caccia
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Publication number: 20110178150Abstract: The present invention relates to a compound derived from indole, especially a therapeutically useful compound, characterized in that it is selected from compounds of formula (I) in which R1 represents a halogen or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C4 alkyl group, R3 represents an isopropyl (1-methylethyl) group or a tert-butyl (1,1-dimethylethyl) group and n=3 or 4 and pharmaceutically acceptable salts of said compounds of formula (I). Application: Treatment of neurodegenerative diseases and more particularly of Parkinson's disease.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Applicant: Laboratories Fournier S.A.Inventors: Benaissa Boubia, Johannes Bernard Van Vliet, Joseph Antonius Jacobus Den Hartog, Andrew McCreary, Mireille Tallander, Petronella Johanna Maria Van Dongen, Olivia Poupardin-Olivier
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Patent number: 7977380Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: November 20, 2009Date of Patent: July 12, 2011Assignee: Activesite Pharmaceticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20110166114Abstract: A method of treating snoring and/or sleep apnea comprising administering to a patient in need of such treatment a therapeutically effective amount of a leukotriene receptor antagonist.Type: ApplicationFiled: March 14, 2011Publication date: July 7, 2011Inventor: David Gozal
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Publication number: 20110166136Abstract: Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety —O—(CH2)n—O— wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8Type: ApplicationFiled: July 3, 2009Publication date: July 7, 2011Applicant: LECTUS THERAPEUTICS LIMITEDInventors: Nawaz Mohammed Khan, Svenja Burckhardt, Julie Elaine Cansfield, Ngoc-Tri Vo, Richard Edward Armer, Raymond John Boffey
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Patent number: 7973070Abstract: New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.Type: GrantFiled: March 11, 2009Date of Patent: July 5, 2011Assignee: Ajinomoto Co., Inc.Inventors: Kenichi Mori, Eriko Ono
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Publication number: 20110160236Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.Type: ApplicationFiled: November 29, 2010Publication date: June 30, 2011Inventor: Victor L. Serebruany
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Publication number: 20110159017Abstract: The unexpected expression of tryptophan 2,3-dioxygenase (TDO2) in cancer cells and tumors has been established. Methods for diagnosing cancer based on the expression of TDO2 are provided, as are methods for treating cancer and inhibiting the growth of cancer cells by inhibiting TDO2, as well as pharmaceutical compositions.Type: ApplicationFiled: April 10, 2009Publication date: June 30, 2011Applicant: Ludwig Institute for Cancer Research Ltd.Inventors: Benoit Van Den Eynde, Luc Pilotte, Etienne De Plaen
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Publication number: 20110160197Abstract: The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu.Type: ApplicationFiled: May 17, 2007Publication date: June 30, 2011Inventors: Andrey Alexandrovich Ivashchenko, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Oleg Dmitrievich Mitkin, Ilya Matusovich Okun, Alexandr Sergeevich Kyselvev, Volodymyr Mikhailovich Kysil, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivachtchenko
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Publication number: 20110152321Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
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Publication number: 20110152175Abstract: The invention provides dendrimeric compounds of the formula 1 comprising amino acids, wherein n is an integer of 1-4, T is an alkylidene —(CH2)2CONH(CH2)2- group, R2 is an —NH2 group or a moiety of a primary organic amine, and P is an amino acid and/or peptide moiety, wherein at least one hydrogen atom of at least one amino group is optionally replaced by a protective group, and a hyperbranched core compound of the formula 3, wherein T and R2 are as defined above. The invention provides also a process for the preparation of a dendrimeric compound and a hyperbranched core, wherein the process employs addition reactions of alkyl acrylate and a basic amino acid, and use of a hyperbranched core for the preparation of a dendrimeric compound comprising amino acids. The invention provides also use of dendrimeric compounds for the preparation of the medicament for inhibiting growth of bacterial cells, fungi and tumor cells.Type: ApplicationFiled: September 18, 2009Publication date: June 23, 2011Applicant: Instytut Chemii Organicznej Polska Akademia NaukInventors: Zofia Lipkowska, Piotr Polcyn, Andrzej Wojciech Lipkowski
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Patent number: 7964629Abstract: The present invention relates, in general, to isoprenylcysteine carboxyl methyltransferase (Icmt) and, in particular, to inhibitors of Icmt and to methods of disease treatment using same.Type: GrantFiled: March 20, 2006Date of Patent: June 21, 2011Assignee: Duke UniverstiyInventors: Patrick J. Casey, Rudi A. Baron, Ann M. Winter-Vann
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Publication number: 20110144074Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: ApplicationFiled: January 24, 2011Publication date: June 16, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20110142777Abstract: The invention relates to a compound of formula I wherein R1, R2 and R3 are identical or different and each is H or alkyl of 1-6 carbon atoms, R4 is H or methyl, R5 is phenyl or chlorophenyl, and/or physiologically acceptable salts thereof and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said compound.Type: ApplicationFiled: July 30, 2009Publication date: June 16, 2011Inventors: Soheila Anzali, Francis Contard, Jean Jacques Zeiller
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Patent number: 7960428Abstract: 3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other anti-viral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.Type: GrantFiled: September 28, 2007Date of Patent: June 14, 2011Assignee: Idenix Pharmaceuticals, Inc.Inventors: Richard Storer, Francois-Rene Alexandre, Cyril Dousson, Adel M. Moussa, Edward Bridges, Alistair Stewart, Jing Yang Wang, Benjamin Alexander Mayes
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Patent number: 7960569Abstract: The present invention provides indole compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables ring A, X1, X2, X3, X4, R6, and R15 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: October 16, 2007Date of Patent: June 14, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Patrick Y. S. Lam, Charles G. Clark
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Patent number: 7960427Abstract: The present invention relates to 5-hydroxy-indole-3-carboxylate derivatives of formula I, or racemic mixture or optical isomers or pharmaceutically acceptable salts and/or hydrates thereof, wherein: substituents R1, R2, Z, X and Y are as defined in the description. The compounds of formula I can be useful for preparation of medicament for treatment and/or prophylaxis of virus infections, especially for preparation of medicament for anti-HBV (Hepatitis B virus) and anti-HIV (Human immunodeficiency virus).Type: GrantFiled: March 11, 2005Date of Patent: June 14, 2011Assignee: Shenyang Pharmaceutical UniversityInventors: Ping Gong, Yanfang Zhao
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Publication number: 20110136742Abstract: The invention provides antidepressant prodrugs comprising an antidepressant conjugated to one or more amino acids. The invention also relates to pharmaceutical compositions comprising an antidepressant prodrug, and to methods of preparing and using the same.Type: ApplicationFiled: February 22, 2007Publication date: June 9, 2011Inventors: Travis Mickle, Wendy Hirschelman Severs
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Publication number: 20110136807Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: June 29, 2007Publication date: June 9, 2011Applicant: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, JR.
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Patent number: 7956067Abstract: Novel compositions comprising a combination of at least one higher primary aliphatic alcohol preferably selected from those having 18 to 40 carbon atoms or mixtures thereof, at least one source of 5-hydroxytryptophan (5-HTP) optionally additionally comprising a source of caffeine and/or catechin-polyphenol and/or epigallocatechin gallate as active agents, either alone or in combination with other active agent(s), optionally with one or more excipient(s) are provided. Particularly, the invention relates to compositions and process for preparation of such compositions and method of use thereof for the management of obesity and associated disorders.Type: GrantFiled: May 9, 2007Date of Patent: June 7, 2011Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Kour Chand Jindal
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Patent number: 7951834Abstract: This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an ?,?-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.Type: GrantFiled: May 29, 2006Date of Patent: May 31, 2011Assignee: University of Cape TownInventors: Edward Sturrock, Aloysius Nchinda, Kelly Chibale
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Patent number: 7951835Abstract: The present invention provides salt crystals of non-natural stereoisomer forms of monatin and to the use thereof.Type: GrantFiled: June 29, 2010Date of Patent: May 31, 2011Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Kazuko Yuzawa, Kenichi Mori, Tadashi Takemoto
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Publication number: 20110123619Abstract: A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.Type: ApplicationFiled: February 4, 2011Publication date: May 26, 2011Applicant: OZPHARMA PTY. LTD.Inventors: Ernest Alan Hewitt, Richard James Stenlake
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Publication number: 20110124697Abstract: Compositions based on amino acids are described, in particular for oral or parenteral use, suitable for treating heart insufficiency. The compositions according to the invention comprise up to 75% of the branched chain amino acids leucine, isoleucine and valine, as active ingredients. Preferably, the compositions also comprise, as further active ingredients, up to 50% of theronine and lysine. Other essential amino acids are preferably also provided (in particular methionine, phenylalanine, histidine, triphtophan) as well as non essential amino acids (in particular tyrosine and/or cyst(e)ine—i.e., cystine and cyst(e)ine). Other amino acids can be added, provided that their sum is in a percentage being lower than 20% with respect to the other active ingredients, and less than 10% for each single amino acid.Type: ApplicationFiled: January 26, 2011Publication date: May 26, 2011Applicant: PROFESSIONAL DIETETICS S.R.L.Inventor: Francesco Saverio DIOGUARDI
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Publication number: 20110124668Abstract: The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKK? inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKK?.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Kenji Kawashima, Hiroshi Enomoto, Minoru Yamamoto, Masaaki Murai
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Publication number: 20110124683Abstract: The invention relates to compounds of general formula (I): wherein R1, R2, R3, R4 and R5 are as defined herein for the treatment of allergic conditions, wherein the treatment is by pulsed therapy which comprises a first period during which the compound is administered to the patient and a second period of at least seven days during which the compound is administered to the patient in a reduced amount. The invention also relates to compounds of general formula (I) for desensitizing the immune system of a subject to allergens, thus preventing or reducing the symptoms of allergic conditions such as allergic asthma, allergic rhinitis, or atopic dermatitis.Type: ApplicationFiled: May 13, 2010Publication date: May 26, 2011Applicant: Oxagen LimitedInventors: Michael George Hunter, Eric Roy Pettipher, Colin Michael Perkins, Mark Anthony Payton, Luzheng Xue
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Publication number: 20110117106Abstract: Calpains target junctional components that normally seal the epithelium, forming tight junctions. This selective targeting by calpains facilitates the transmigration of leukocytes across the epithelium and into tissue spaces where they can cause inflammation. The present disclosure provides methods of using calpain inhibitors to prevent epithelial junction reorganization such that leukocyte transmigration is inhibited and accordingly, inflammation reduced or prevented. These methods can at least be used to reduce respiratory inflammation by preventing leukocyte accumulation in pulmonary airways.Type: ApplicationFiled: March 6, 2009Publication date: May 19, 2011Inventor: Alice Prince
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Publication number: 20110117211Abstract: An immunomodulatory compound is utilized to treat mucosa disease.Type: ApplicationFiled: January 25, 2011Publication date: May 19, 2011Applicant: SCICLONE PHARMACEUTICALS, INC.Inventors: Israel RIOS, Cynthia TUTHILL
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Publication number: 20110118327Abstract: A pharmaceutical composition and treatment method to reduce the proliferation of cancerous or tumor cells, in which the combined active agents are methylglyoxal, ascorbic acid, creatine and melatonin.Type: ApplicationFiled: August 18, 2010Publication date: May 19, 2011Inventor: Manju Ray
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Publication number: 20110118309Abstract: The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I): wherein the radicals and symbols have the meanings as defined in the specification, for the preparation of a medicament for the treatment of Hodgkins disease.Type: ApplicationFiled: July 16, 2009Publication date: May 19, 2011Inventor: Peter Wisdom Atadja
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Patent number: 7943658Abstract: Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.Type: GrantFiled: July 22, 2008Date of Patent: May 17, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, Stephen T. Wrobleski, Katerina Leftheris, Gang Wu, Philip M. Sher, Bruce A. Ellsworth
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Publication number: 20110111021Abstract: The present invention provides a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active ingredient, and a compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient, wherein one compartment is a prior-release compartment and the other compartment is a delayed-release compartment. The combination preparation of the present invention can deliver a renin inhibitor and an HMG-CoA reductase inhibitor with a time interval at a specific speed, thus reducing undesirable side-effects, improving the drug efficacy and promoting the patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndromes, cardiovascular diseases, renal diseases and the like, as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.Type: ApplicationFiled: February 23, 2009Publication date: May 12, 2011Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Sung Wuk Kim, Sung Soo Jun, Young Gwan Jo, Ja Seong Koo, Jaw Woon Son, Jin Wook Kim
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Patent number: 7939558Abstract: The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., ?F508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-CFTR, that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more phenylglycine-containing compounds or sulfonamide-containing compounds of the invention, or an analog or derivative thereof.Type: GrantFiled: June 2, 2005Date of Patent: May 10, 2011Assignee: The Regents of the University of CaliforniaInventors: Alan Verkman, R. Kiplin Guy, Nicoletta Pedemonte, Luis J. V. Galietta
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Publication number: 20110104282Abstract: The invention provides for new methods for treatment and diagnosis of irritable bowel syndrome (IBS). In particular, there is disclosed the use of a Chlamydia activating agent and one or several antibiotics selected from macroildes and benzoxazinorifamycins in the preparation of combination agent for simultaneous, concomitant or sequential administration for the treatment of IBS.Type: ApplicationFiled: April 27, 2009Publication date: May 5, 2011Inventors: Greger Lindberg, Aldona Dlugosz
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110105532Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Publication number: 20110105574Abstract: The invention concerns in one embodiment a method for treating glaucoma or elevated IOP in a patient comprising administering to the patient an effective amount of a composition comprising an agent that inhibits PAI-1 expression or PAI-1 activity. Another embodiment of the present invention is a method of treating a PAI-1-associated ocular disorder in a subject in need, comprising administering to the patient an effective amount of a composition comprising an agent that inhibits PAI-1 activity or expression.Type: ApplicationFiled: January 14, 2011Publication date: May 5, 2011Applicant: ALCON RESEARCH, LTD.Inventors: Debra L. Fleenor, Allan R. Shepard, Iok-Hou Pang, Mark R. Hellberg, Abbot F. Clark
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Publication number: 20110105572Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is a C5-20heteroaryl or C5-20carboaryl group and is optionally substituted; Q1 is a C2-7alkylene group having a backbone of at least 2 carbon atoms, and is optionally substituted; J is —N(R1)C(?O)— or —C(?O)N(R1)—; R1 is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q2 is C1-7alkylene, C5-20arylene, C5-20arylene-C1-7alkylene, or C1-7alkylene-C5-20arylene having a backbone of at least 3 carbon atoms, and is optionally substituted; and pharmaceutically acceptable salts thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to treat proliferative conditions, such as cancer and psoriasis.Type: ApplicationFiled: January 4, 2011Publication date: May 5, 2011Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Kathryn G. Moore, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M. Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E.S. Duffy
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Publication number: 20110104265Abstract: A composition and method for treating a bone condition of an animal. The compostion includes nanoparticles; a targeted moiety covalently bonded to an outer surface of each nanoparticle; and osteoblast stimulating molecules encapsulated within each nanoparticle. The method for treating a bone condition includes introducing the composition into the animal.Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Inventors: Shaker A. Mousa, Mohammed H. Qari, Mohammed S. Ardawi
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Patent number: 7935377Abstract: A crystal of free (2R,4R)-monatin is useful as a sweet substance. The crystals resist absorption of water even under high humidity, are stable and exhibit a high degree of sweetness. Thus, such crystals may used as a sweetening agent or an ingredient thereof, and as an ingredient for imparting sweetness to foods and beverages.Type: GrantFiled: June 4, 2004Date of Patent: May 3, 2011Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Kazuko Hirasawa, Kenichi Mori, Tadashi Takemoto
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Publication number: 20110098303Abstract: The present invention provides methods and compositions for increasing the rate of nail growth in mammals, especially humans, using thyromimetic compounds.Type: ApplicationFiled: November 18, 2003Publication date: April 28, 2011Inventors: Niall S. Doherty, Tanya Parkinson
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Publication number: 20110098314Abstract: The use of HMG-CoA reductase inhibitors (e.g., statins) to treat glaucoma, control intraocular pressure, preserve the trabecular meshwork, protect against ocular neurodegeneration and/or protect against glaucomatous retinopathy is described. The preferred HMG-CoA reductase inhibitors, which are statins having an RI value of 0.2 to 0.7 (e.g., pravastatin), are administered via topical application to the affected eye(s) of the patient.Type: ApplicationFiled: November 8, 2010Publication date: April 28, 2011Applicant: ALCON, INC.Inventors: Mark R. Hellberg, Debra L. Fleenor, Allan R. Shepard, Iok-Hou Pang
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Publication number: 20110092456Abstract: The present invention shows that cilostazol, a phosphodiesterase 3 inhibitor has additional beneficial effects to atorvastatin on myocardial remodeling by inducing and preserving eNOS phosphorylation. The present invention demonstrates a cardioprotective effect of Cilostazol indicating the therapeutic potency of this drug. In addition, the present invention demonstrates that the additional effect of Cilostazol and atorvastatin therapy against ischemia injury is due to the augmentation of phosphatodylicositol 3-kinase/AKT (PI3-/AKT), PKA and p-eNOS signaling.Type: ApplicationFiled: October 19, 2009Publication date: April 21, 2011Inventor: Yochai Birnbaum
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Publication number: 20110091421Abstract: The present invention discloses multiple treatment regimens for vascular-related diseases and disorders. The present invention provides for methods of treating vascular-related disorders based on gene expression studies from samples collected from individuals having symptoms of vascular-related disorders. Additionally, methods are disclosed involving diagnostic techniques to focus treatment regimens. Finally, methods of treating vascular-related disorder involving targeting microRNAs are also disclosed.Type: ApplicationFiled: March 27, 2009Publication date: April 21, 2011Inventor: David M. Mann
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Publication number: 20110092464Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulating angiotensin activity to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Applicant: BrainCells Inc.Inventors: Carolee BARLOW, Todd A. Carter, Kai Treuner, Kym I. Lorrain
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Patent number: 7928137Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 19, 2011Assignee: Tularik LimitedInventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan