Nitrogen Containing Patents (Class 514/471)
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Publication number: 20120149751Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: February 22, 2012Publication date: June 14, 2012Applicant: Siga Technologies, Inc.Inventors: Dennis E. Hruby, Tove C. Bolken, Sean Amberg, Dongcheng Dai
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Publication number: 20120142528Abstract: What are described are novel active compound combinations comprising a known oxime ether derivative (trifloxystrobin) and imidacloprid, which combinations are highly suitable for controlling phytopathogenic fungi and insects.Type: ApplicationFiled: December 19, 2011Publication date: June 7, 2012Applicant: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Christoph Erdelen, Angelika Lubos-Erdelen, Hirohisa Ohtake
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Patent number: 8183284Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.Type: GrantFiled: July 20, 2006Date of Patent: May 22, 2012Assignee: Warner Chilcott Company, LLCInventors: Joseph Michael Sprafka, II, Jose Mauro Goulart-Brum
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Patent number: 8183281Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Novartis AGInventors: Neil John Press, Simon James Watson
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Publication number: 20120121724Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Inventor: Todd Maibach
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Publication number: 20120121527Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.Type: ApplicationFiled: January 18, 2012Publication date: May 17, 2012Applicant: Galderma Research & DevelopmentInventors: Jean-Guy BOITEAU, Laurence Clary, Corinne Millois Barbuis
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Publication number: 20120122918Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.Type: ApplicationFiled: November 28, 2011Publication date: May 17, 2012Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
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Publication number: 20120122862Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: January 30, 2012Publication date: May 17, 2012Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20120122856Abstract: The present invention relates to liquid termiticide compositions comprising a pyrethroid and a neonicotinoid selected from the group consisting of imidacloprid, nithiazine, thiamethoxam, dinotefuran, nitenpyram, thiacloprid and clothianadin, these compositions result in an increase in termite mortality at low application rates and a continuous chemical bather of a termiticide in soil surrounding and beneath a structure in a locus where termites are suspected or known to exist.Type: ApplicationFiled: January 19, 2012Publication date: May 17, 2012Applicant: FMC CORPORATIONInventors: James B. Ballard, Cristi L. Palmer, Kim Watson
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Patent number: 8178527Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: GrantFiled: October 2, 2007Date of Patent: May 15, 2012Assignee: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20120115851Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
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Patent number: 8173700Abstract: The present invention relates to salts of substituted allophanates, methods for their production, medicaments containing said compounds and the use of said compound for the production of medicaments.Type: GrantFiled: May 17, 2006Date of Patent: May 8, 2012Assignee: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Hans Schick, Fritz Theil, Olga Groeger, Rene Kudick, Helmut Sonnenschein, Birgitta Henkel
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Publication number: 20120108640Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.Type: ApplicationFiled: August 26, 2011Publication date: May 3, 2012Applicant: NEUROTHERAPEUTICS PHARMA, INC.Inventors: Daryl W. Hochman, John J. Partridge
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Patent number: 8168674Abstract: Administration of a loop diuretic in nebulized dry powder form directly to a patient's lungs for treating bronchial disease.Type: GrantFiled: February 21, 2003Date of Patent: May 1, 2012Assignee: Microdose Therapeutx, Inc.Inventor: Andrew Abrams
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Publication number: 20120094977Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: May 25, 2011Publication date: April 19, 2012Applicant: Dendreon CorporationInventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
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Publication number: 20120095042Abstract: Provided are compounds of formula (I) wherein m is 0, 1 or 2; RI is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms: or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.Type: ApplicationFiled: May 4, 2010Publication date: April 19, 2012Inventor: Stefan Michael Furrer
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Publication number: 20120095024Abstract: The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I).Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicants: Elara Pharmaceuticals GmbH, European Molecular Biology Laboratory (EMBL)Inventors: Jorge Alonson, Arantxa Encionas Lopez, Marcel Muelbaler, Lochen Ammenn, Bernd Vendt, Joe Lewis, Christoph Schultes, Bernd Janssen
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Patent number: 8158677Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: GrantFiled: June 2, 2008Date of Patent: April 17, 2012Assignee: The Trustees of Princeton UniversityInventors: Josh Munger, Bryson Bennett, Thomas Shenk, Joshua Rabinowitz
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Publication number: 20120077673Abstract: Compositions and methods for protecting plants from fungal, bacterial, and viral diseases are provided, which compositions comprise at least one compound that produces systemic acquired resistance and at least one antifungal compound. Compositions of the disclosure may be applied directly to seeds, seedlings, shoots, roots, and/or foliage of the plant to be protected, thereby protecting them from the fungal, bacterial, and viral diseases.Type: ApplicationFiled: August 9, 2011Publication date: March 29, 2012Inventors: Jennifer Riggs, Danise Beadle, Katie Vuocolo
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Publication number: 20120077804Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.Type: ApplicationFiled: July 24, 2008Publication date: March 29, 2012Applicant: The Regents of the University of CaliforniaInventor: Shou-Wei Ding
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120064156Abstract: The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.Type: ApplicationFiled: August 23, 2011Publication date: March 15, 2012Inventor: John R. Plachetka
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Publication number: 20120059012Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five- to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.Type: ApplicationFiled: May 12, 2010Publication date: March 8, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
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Publication number: 20120034285Abstract: Dinotefuran and PBO is used for killing mosquitoes, as PBO increases the knockdown speed of Dinotefuran.Type: ApplicationFiled: April 14, 2009Publication date: February 9, 2012Inventors: Mikkel Vestergaard Frandsen, Michael Stanley Pedersen, Matthieu Zellweger, Sebastien Gouin, Georgina Victoria Bingham, Helen Victoria Pates Jamet
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Publication number: 20120035179Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: ApplicationFiled: March 9, 2011Publication date: February 9, 2012Inventors: Sara S. Hadida-Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
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Publication number: 20120035139Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.Type: ApplicationFiled: April 16, 2010Publication date: February 9, 2012Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
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Publication number: 20120035175Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 9, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
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Publication number: 20120035257Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.Type: ApplicationFiled: March 7, 2011Publication date: February 9, 2012Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman, Norbert L. Wiech
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Publication number: 20120022100Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
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Publication number: 20120022080Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.Type: ApplicationFiled: March 31, 2010Publication date: January 26, 2012Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
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Publication number: 20120022039Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.Type: ApplicationFiled: February 12, 2010Publication date: January 26, 2012Applicant: SANOFIInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
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Patent number: 8101657Abstract: The invention provides a plant disease and insect damage control composition including, as active ingredients, dinotefuran and at least one fungicidal compound; and a plant disease and insect damage prevention method that includes applying such a composition to a plant body, soil, plant seed, stored cereal, stored legume, stored fruit, stored vegetable, silage, stored flowering plant, or export/import timber. The invention provides a new plant disease and insect damage control composition and a plant disease and insect damage prevention method with very low toxicity to mammals and fishes, the composition and method showing an effect against plural pathogens and pest insects, including emerging resistant pathogens and resistant pest insect, by application to a plant body, soil, plant seed, stored cereal, stored legume, stored fruit, stored vegetable, silage, stored flowering plant, or export/import timber.Type: GrantFiled: November 22, 2007Date of Patent: January 24, 2012Assignee: Mitsui Chemicals, Inc.Inventors: Eiichi Yamada, Ryutaro Ezaki, Hidenori Daido
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Patent number: 8101799Abstract: This invention concerns N—(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: July 30, 2007Date of Patent: January 24, 2012Assignee: Ardea BiosciencesInventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoui, Zhi Hong
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Patent number: 8093185Abstract: Treatment with N-(2-phenylethyl)succinamic acid or its salts protects against inhibition of growth by a neonicotinoid compound applied as a seed treatment or applied directly on or near the root zone of the seedling.Type: GrantFiled: October 24, 2008Date of Patent: January 10, 2012Assignees: Valent BioSciences Corporation, Valent U.S.A. CorporationInventors: Franklin Paul Silverman, Dale O. Wilson, Jr., Jennifer C. Kochan, Nicole Higgs, Peter D. Petracek, Prem Warrior, Karen S. Arthur
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Publication number: 20120004103Abstract: Insecticidal compositions suitable for use in preparation of insecticidal liquid fertilizers comprising a pyrethroid, a hydrated aluminum-magnesium silicate, and at least one dispersant selected from the group consisting of a sucrose ester, a lignosulfonate, an alkylpolyglycoside, a naphthalenesulfonic acid formaldehyde condensate and a phosphate ester are disclosed.Type: ApplicationFiled: September 9, 2011Publication date: January 5, 2012Applicant: FMC CORPORATIONInventor: Timothy Martin
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Publication number: 20120004198Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: ApplicationFiled: February 2, 2011Publication date: January 5, 2012Applicant: ARGUSINA INC.Inventors: Jiayu LIAO, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Publication number: 20120004104Abstract: Selective insect neonicotinoids is a class of pesticide active ingredients that share some characteristics in their chemical structures and bind to the nAChR acetylcholine receptors. Formulation of such compounds in oil suspension or oil dispersion is challenging due to their electrostatic interactions of the heteroatoms in oily media, that lead to irreversible flocculation or diminished homogeneicity and bleeding of such oil dispersions. Imidacloprid, Thiamethoxam, Thiachloprid, Nitenpyram, Acetamiprid, Clothianidin and Dinetofuran and derivatives thereof with nAChR binding ability are successfully formulated in oil suspension with the use of certain copolymeric anionic fatty-acid based dispersants, sorbitan derivatives, ionic surfactants, other non-ionic surfactants and inorganic polyvalent cationic salt dispersed in the oil.Type: ApplicationFiled: March 4, 2010Publication date: January 5, 2012Applicant: GAT Microencapsulation AGInventors: Victor Casaña Giner, Miguel Gimeno Sierra, Barbara Gimeno Sierra
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Publication number: 20120004225Abstract: The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.Type: ApplicationFiled: January 22, 2010Publication date: January 5, 2012Applicant: NeuroTherapeutics Pharma, Inc.Inventors: Stephen Wanaski, John J. Partridge, Stephen D. Collins
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Patent number: 8088405Abstract: Methods of promoting healing through enhanced regeneration of tissue (e.g. hard tissue or soft tissue) by contacting the tissue or the surrounding tissue with an anti-inflammatory agent. These methods are useful in a variety of dental and orthopedic applications.Type: GrantFiled: September 21, 2006Date of Patent: January 3, 2012Assignee: Rutgers, The State University of New JerseryInventor: Kathryn E. Uhrich
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Patent number: 8088814Abstract: A method for the prevention, treatment, or inhibition of a psychiatric disorder, in particular schizophrenia, is described which comprises administering a COX-2 inhibitor or prodrug thereof to a subject. Moreover, a method for the prevention, treatment, or inhibition of a psychiatric disorder, in particular schizophrenia or depressive disorders, is disclosed comprising administering to a subject a COX-2 inhibitor or prodrug thereof in combination with a neuroleptic drug or an antidepressant. Compositions and kits that are suitable for the practice of the method are also described.Type: GrantFiled: May 31, 2002Date of Patent: January 3, 2012Inventor: Norbert Müller
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Patent number: 8088804Abstract: Described herein are N-hydroxyamide antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) each indicates a point of attachment.Type: GrantFiled: December 4, 2006Date of Patent: January 3, 2012Assignee: Pfizer Inc.Inventors: Rakesh Kumar Jain, Mikhail Fedorovich Gordeev, Jason Gustaf Lewis, Charles Francavilla
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Publication number: 20110318321Abstract: The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.Type: ApplicationFiled: January 8, 2010Publication date: December 29, 2011Applicant: AZIENDE CHIM.RIUN.ANG.FRANC.A.C.R.A.F. S.p.A.Inventors: Stefano Selva, Leonardo Marchitto, Giovanni Battista Ciottoli, Lorella Ragni, Vincenzo Russo, Elisa Liberati
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Publication number: 20110318359Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.Type: ApplicationFiled: December 2, 2009Publication date: December 29, 2011Inventors: Edward P. Feener, Allen Clermont
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Publication number: 20110312964Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic painType: ApplicationFiled: December 18, 2009Publication date: December 22, 2011Applicant: Medivir UK LTDInventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Publication number: 20110311503Abstract: The novel active ingredient combinations which consist of the compounds of the formula (I) in combination with further active insecticidal ingredients (II) are very suitable for control of animal pests such as insects and/or unwanted acarids.Type: ApplicationFiled: June 16, 2011Publication date: December 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Christian FUNKE, Heike HUNGENBERG, Rüdiger FISCHER
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Publication number: 20110311467Abstract: The present invention is directed to a long wearing, transfer resistant cosmetic composition which is waterproof, comfortable and has a unique creamy texture and feel containing: (a) a reaction product of (i) at least one polyamine and (ii) at least one oil soluble high carbon polar modified polymer; (b) water; (c) at least one volatile solvent capable of solubilizing the polar modified polymer; (d) optionally at least one non-volatile solvent; and (e) optionally, at least one colorant.Type: ApplicationFiled: December 16, 2009Publication date: December 22, 2011Applicant: L'OREAL S.A.Inventors: Hy Si Bui, Susan Halpern, Mohamed Kanji
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Publication number: 20110306646Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: February 16, 2010Publication date: December 15, 2011Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Publication number: 20110306493Abstract: The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such sulfoximine compounds. The sulfoximinamid compounds of the present invention are defined by the following formula I: wherein Q, Het, R1, R2, R3, R4 and n are defined as in the description.Type: ApplicationFiled: June 19, 2009Publication date: December 15, 2011Applicant: BASF SEInventors: Ralph Paulini, Delphine Breuninger, Wolfgang Von Deyn, Henricus Maria Martinus Bastiaans, Carsten Beyer, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Faraneh Oloumi