The Six-membered Hetero Rings Are Bonded Directly To Each Other Patents (Class 514/334)
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Patent number: 8440656Abstract: Disclosed are methods of treating or preventing a pulmonary disease or disorder in a subject, the methods comprising administering an effective amount of an compound that inhibits Calmodulin Kinase II (CaMKII) activity, either directly or indirectly, thereby treating or preventing the pulmonary disease or disorder in the subject.Type: GrantFiled: June 22, 2010Date of Patent: May 14, 2013Assignee: University of Iowa Research FoundationInventors: Mark E. Anderson, Isabella M. Grumbach, Joel N. Kline
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Publication number: 20130109655Abstract: This invention relates to a method of mitigating side effects of non-steroidal anti-inflammatory drugs, specifically to administration of a pyridine derivative to mitigate and/or prevent prostaglandin e2 reducing side effects of non-steroidal anti-inflammatory drugs. Also provided is the use of a pyridine derivative in the preparation of a medicament for the reduction of said side effects of non-steroidal anti-inflammatory drugs, and a pharmaceutical composition comprising a non-steroidal anti-inflammatory drug and a pyridine derivative.Type: ApplicationFiled: October 31, 2011Publication date: May 2, 2013Inventors: Serghei Gargaun, Ana Gargaun
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Publication number: 20130108605Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.Type: ApplicationFiled: December 17, 2012Publication date: May 2, 2013Applicant: THE UNIVERSITY OF KENTUCKY RESEARCH FOUNDATIONInventor: THE UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
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Publication number: 20130102597Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: October 15, 2012Publication date: April 25, 2013Applicant: INTERMUNE, INC.Inventor: INTERMUNE, INC.
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Publication number: 20130102608Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: ApplicationFiled: June 7, 2011Publication date: April 25, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
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Publication number: 20130101507Abstract: Methods for treating renal cancer by administration of certain 3,3?,4,4?-tetrahydroxy-2,2?-bipyridine-N,N?-dioxide compounds, especially 3,3?,4,4?-tetrahydroxy-2,2?-bipyridine-N,N?-dioxide (Orellanine), conjugated to an alpha-emitting radionuclide (e.g. Astatine-211) to increase the efficacy of the formulation and/or a large molecule (e.g. a oligomer/polymer such as a PEG or a polysaccharide such as a dextran or a Ficoll®) to reduce the filtration and consequently the renal exposure. Particular administration protocols and dosing regimens, as well as pharmaceutical compositions suitable for use in the treatment methods can be used.Type: ApplicationFiled: March 28, 2011Publication date: April 25, 2013Applicant: Oncorena ABInventors: Borje Haraldsson, Ulf Nilsson, Lisa Buvall, Jenny Nystrom
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Patent number: 8426413Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: February 23, 2012Date of Patent: April 23, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Patent number: 8415381Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.Type: GrantFiled: July 26, 2010Date of Patent: April 9, 2013Assignee: Novartis AGInventors: Paul A. Barsanti, Cheng Hu, Jeff Jin, Robert Keyes, Robert Kucejko, Xiaodong Lin, Yue Pan, Keith B. Pfister, Martin Sendzik, James Sutton, Lifeng Wan
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Patent number: 8415380Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and methods for treating CNS disorders with the same.Type: GrantFiled: July 8, 2011Date of Patent: April 9, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Juergen Wichmann, Thomas Woltering
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Patent number: 8410142Abstract: The present invention is directed to bipyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: February 29, 2008Date of Patent: April 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Publication number: 20130053355Abstract: This disclosure provides products, including pharmaceutical compositions and dietary supplements, which are useful for anti-inflammatory support.Type: ApplicationFiled: June 12, 2012Publication date: February 28, 2013Applicant: Rock Creek Pharmaceuticals, Inc.Inventor: Jonnie R. Williams
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Publication number: 20130053350Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing neurodegenerative disorders.Type: ApplicationFiled: December 15, 2010Publication date: February 28, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Rolf F. Kletzien, Steve P. Tanis, Scott D. Larsen
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Patent number: 8383652Abstract: Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.Type: GrantFiled: April 28, 2008Date of Patent: February 26, 2013Assignee: Galderma Research & DevelopmentInventors: Jean-Guy Boiteau, Laurence Clary, Laurent Chantalat, Michel Rivier
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Publication number: 20130030000Abstract: The present invention is directed to a composition useful for the treatment of a FAAH mediated disease, disorder or conditions comprising a FAAH inhibitor and a second activation, comprising a selected imidazole or oxazole FAAH inhibitor and a second active agent. The compositions will be useful in the treatment of a wide range of disease, disorder, or conditions including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease. In another aspect the invention discloses herein is directed to compositions useful in the treatment of neuropathic and nociceptive pain, said compositions comprising etoricoxib.Type: ApplicationFiled: January 25, 2011Publication date: January 31, 2013Inventors: Harry R. Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo, Terence G. Hamill, Wenping Li, Darrell Arthur Henze
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Publication number: 20130012541Abstract: A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.Type: ApplicationFiled: June 18, 2012Publication date: January 10, 2013Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Qun Sun, Laykea Tafesse
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Patent number: 8349872Abstract: The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: August 5, 2009Date of Patent: January 8, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
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Publication number: 20130005765Abstract: A method for inhibiting hatching of an ectoparasite egg, the method comprising exposing the ectoparasite egg to at least one metal chelating agent and/or metalloprotease inhibitor, wherein the metal chelating agent is a compound comprising at least two heteroatoms able to simultaneously coordinate with a metal ion, at least one of the two heteroatoms being selected from nitrogen, sulfur, oxygen and phosphorus, wherein the compound comprises at least one carbocyclic ring substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom, or the compound comprises at least one heterocyclic ring containing at least one heteroatom, wherein said heterocyclic ring is optionally substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom is provided. Methods of treating ectoparasite infestations and compositions for use in such methods are also provided.Type: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Applicant: HATCHTECH PTY LTD.Inventor: Vernon Morrison Bowles
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Patent number: 8344001Abstract: Compound of formula (I) wherein W, X, Y, Z is —C(R1)? or N; R1 is hydrogen or alkyl, V is N or C (i.e.Type: GrantFiled: May 19, 2008Date of Patent: January 1, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Rolf Hohlweg, Jane Marie Lundbeck, Johannes Cornelis de Jong
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Patent number: 8343966Abstract: Compounds of formula I in free or salt or solvate form, where T1, T2, X, Ra, Rb, R8 and R9 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: January 2, 2009Date of Patent: January 1, 2013Assignee: Novartis AGInventors: Claire Adcock, Urs Baettig, Peter Hunt, Catherine Leblanc, Maude Nadine Pierrette Pipet, Robert Alexander Pulz, Katrin Spiegel, Nikolaus Johannes Stiefl
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Patent number: 8343962Abstract: It has been discovered that certain combinations compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.Type: GrantFiled: August 2, 2010Date of Patent: January 1, 2013Assignee: Nuvo Research Inc.Inventors: Edward T. Kisak, John M. Newsam, Dominic King-Smith, Pankaj Karande, Samir Mitragotri
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Patent number: 8343952Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: August 20, 2010Date of Patent: January 1, 2013Assignee: Akebia Therapeutics Inc.Inventors: Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Richard Masaru Kawamoto
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Publication number: 20120322829Abstract: A compound of formula (I) below: or one of the pharmaceutically acceptable salts thereof is described. Also described, are uses thereof in the treatment of rosacea.Type: ApplicationFiled: November 26, 2010Publication date: December 20, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Irina Safonova, Jean-Dominique Pierret
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Publication number: 20120322719Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.Type: ApplicationFiled: June 14, 2012Publication date: December 20, 2012Applicant: The Feinstein Institute For Medical ResearchInventors: Valentin A. Pavlov, Kevin J. Tracey
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Publication number: 20120295905Abstract: The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.Type: ApplicationFiled: January 17, 2011Publication date: November 22, 2012Applicant: MMV MEDICINES FOR MALARIA VENTUREInventors: Michael John Witty, David Hardick
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Patent number: 8304438Abstract: The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: June 17, 2009Date of Patent: November 6, 2012Assignee: SanofiInventors: Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
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Publication number: 20120245124Abstract: Disclosed herein are modulators of TRPV3 of formula (I) wherein X1, X2, R1, R2, Rx, and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: March 23, 2012Publication date: September 27, 2012Applicant: ABBOTT LABORATORIESInventors: Bruce Clapham, Phil B. Cox, Michael J. Dart, Arthur Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark Matulenko, Robert G. Schmidt, Clara I. Villamil, Eric A. Voight, Kevin R. Woller
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Publication number: 20120245202Abstract: Pharmaceutical compositions comprising an isolated form of a compound of Formula I or IA (e.g., anatabine or S-(?)-anatabine) or a salt thereof can be used to treat disorders comprising an inflammatory component, including chronic, low-level inflammation. Compounds of Formula I also can be provided, for example, in other vehicles such as beverage products and consumer products such as lotions and creams.Type: ApplicationFiled: September 19, 2011Publication date: September 27, 2012Applicant: ROCK CREEK PHARMACEUTICALS, INC.Inventor: Jonnie R. Williams
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Publication number: 20120237563Abstract: The subject invention pertains to controlled-release dosage forms of anabaseine compounds, such as 3-(2,4-dimethoxybenzylidene)-anabaseine (also known as DMXBA or GTS-21) or a pharmaceutically acceptable salt thereof, methods of use, and methods for producing controlled-release dosage forms.Type: ApplicationFiled: August 18, 2010Publication date: September 20, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION INC.Inventors: William Reade Kem, Ferenc Soti, Robert Freedman, Lynn Johnson
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Publication number: 20120232033Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.Type: ApplicationFiled: May 25, 2012Publication date: September 13, 2012Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinnard, Henri Stalder
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Publication number: 20120232051Abstract: This invention relates to novel 3-aminopyridines of the formula wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: February 28, 2012Publication date: September 13, 2012Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Prabha Saba Karnachi, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
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Publication number: 20120232115Abstract: Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine. The resulting anatabine is substantially free from contaminants and displays good stability. In an alternative embodiment, the benzylhydrylidene-pyridin-3-yl-methyl-amine may be used in the synthesis of other alkaloids such as anabasine, nornicotine, N-methylanabasine, and anabaseine.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Applicant: ROCK CREEK PHARMACEUTICALS, INC.Inventors: Tom Thomas Puthiaparampil, Thomas Kanathkunn David, Muppala Sarveswara Raju
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Publication number: 20120225857Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Patent number: 8247436Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: March 14, 2011Date of Patent: August 21, 2012Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Hughes, Darren Mark Legrand, Katrin Spiegel
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Publication number: 20120196900Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: April 16, 2012Publication date: August 2, 2012Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20120196899Abstract: Pharmaceutical compositions comprising an isolated form of a compound of Formula IB (e.g., R-(+)-anatabine) or a salt thereof can be used to treat disorders comprising an inflammatory component, including chronic, low-level inflammation. Compounds of Formula I also can be provided, for example, in other vehicles such as beverage products and consumer products such as lotions and creams.Type: ApplicationFiled: September 19, 2011Publication date: August 2, 2012Applicant: Rock Creek Pharmaceuticals, Inc.Inventor: Jonnie R. Williams
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Publication number: 20120190699Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: July 26, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Steven Durrant, Sharn Ramaya, Juan-Miguel Jimenez, Alistair Rutherford
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Publication number: 20120183579Abstract: The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 17, 2012Publication date: July 19, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Gary Bohnert, Zhiqiang Xia, Shoujun Chen, Lijun Sun
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Publication number: 20120177570Abstract: The invention relates to compounds of formula IA? and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: February 14, 2012Publication date: July 12, 2012Applicant: Purdue Pharma L.P.Inventor: Laykea TAFESSE
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Publication number: 20120178782Abstract: Synergistic pharmaceutical compositions and the methods for preventing and treating proliferative diseases such as cancer and psoriasis. The compositions comprise synergistic combinations of: (i) an acyl-CoA-synthetase enzyme inhibitor (AcsI4), (ii) a compound having an inhibiting effect on enzymes with cyclooxygenase activity (COX); and (iii) a compound selected from a 5-lypoxygenase enzyme (LOX-5) inhibitor and a leukotriene receptor antagonist.Type: ApplicationFiled: September 10, 2010Publication date: July 12, 2012Inventor: Ernesto Jorge Podesta
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Publication number: 20120177748Abstract: The present invention relates to pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula III: wherein the variables are as defined herein.Type: ApplicationFiled: May 12, 2011Publication date: July 12, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Philip Michael Reaper
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Publication number: 20120172398Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses in pharmaceutical formulations for the treatment of pain.Type: ApplicationFiled: April 19, 2010Publication date: July 5, 2012Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Carlos Ramon Plata Salaman, Nicolas Tesson
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Publication number: 20120172354Abstract: The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I) Wherein R1, R2, R3, R4, R5, R6 have the meaning defined in the claims. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: September 16, 2010Publication date: July 5, 2012Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Frans Alfons Maria Van den Keybus, Yves Emiel Maria Van Roosbroeck
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Publication number: 20120157317Abstract: The invention provides a composition in concentrated form (“the concentrate”) for dilution with water in the preparation of an agricultural composition for application to crops, soil or animals, comprising a carbohydrate-based pH modifying agent and a pH indicator. The agricultural composition comprises an agricultural chemical whose agricultural activity varies with the pH of the water. The proportions of the pH indicator and the pH modifying agent in the concentrate are selected so that when the concentrate is diluted with an appropriate amount of water, the pH indicator indicates visually by colouration of the composition, whether or not the pH of the water is suitable for acceptable agricultural activity of the chemical. The invention also provides a process for preparing the agricultural composition by mixing the concentrate with water, and adding the agricultural chemical to the composition, if it is not already present in the concentrate.Type: ApplicationFiled: July 27, 2011Publication date: June 21, 2012Applicant: NUTRIAG LTDInventors: Kelly S.E. Tanaka, Martin David Bloomberg
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Publication number: 20120122932Abstract: A method for inhibiting hatching of an ectoparasite egg, the method comprising exposing the ectoparasite egg to at least one metal chelating agent and/or metalloprotease inhibitor, wherein the metal chelating agent is a compound comprising at least two heteroatoms able to simultaneously coordinate with a metal ion, at least one of the two heteroatoms being selected from nitrogen, sulfur, oxygen and phosphorus, wherein the compound comprises at least one carbocyclic ring substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom, or the compound comprises at least one heterocyclic ring containing at least one heteroatom, wherein said heterocyclic ring is optionally substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom is provided. Methods of treating ectoparasite infestations and compositions for use in such methods are also provided.Type: ApplicationFiled: October 12, 2010Publication date: May 17, 2012Applicant: HATCHTECH PTY LTD.Inventor: Vernon Morrison Bowles
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Patent number: 8178560Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: GrantFiled: June 17, 2010Date of Patent: May 15, 2012Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Publication number: 20120094943Abstract: The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.Type: ApplicationFiled: December 16, 2011Publication date: April 19, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventors: William R. Kem, Ferenc Soti
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Publication number: 20120093911Abstract: The present invention provides improved intravaginal drug delivery devices, i.e., intravaginal rings, useful for the prophylactic administration of an antimicrobial compound, e.g., Dapivirine, to a human. The intravaginal rings of the invention address previous stability issues by utilizing a platinum catalyst (e.g., in the form of a platinum-siloxane complex) for the cross-linking reaction. The vaginal rings surprisingly achieve relatively high and steady release rates in vivo with a matrix ring containing a relatively small loading dose. While the matrix rings of the present invention have in vivo the steady release rates associated with reservoir rings, they are easier and less expensive to manufacture. The present invention also provides methods of blocking DNA polymerization by an HIV reverse transcriptase enzyme, methods of preventing HIV infection in a female human, methods of treating HIV infection in a female human, and methods of preparing platinum-catalyzed intravaginal rings.Type: ApplicationFiled: October 19, 2011Publication date: April 19, 2012Applicant: International Partnership for MicrobicidesInventors: Karl Malcolm, David Woolfson, Joseph Romano
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Publication number: 20120077846Abstract: Methods are provided of treating renal cancer by administration of certain 3,3?,4,4?-tetrahydroxy-2,2?-bipyridine-N,N?-dioxide compounds, especially 3,3?,4,4?-tetrahydroxy-2,2?-bipyridine-N,N?-dioxide (Orellanine), using particular administration protocols and dosing regimens, as well as pharmaceutical compositions suitable for use in the treatment methods that are provided.Type: ApplicationFiled: September 21, 2011Publication date: March 29, 2012Inventors: Börje Haraldsson, Ulf Nilsson, Lisa Buvall, Jenny Nyström
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Publication number: 20120071539Abstract: Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic compositions comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.Type: ApplicationFiled: December 12, 2007Publication date: March 22, 2012Applicant: Emory UniversityInventor: Peng Jin