Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
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Patent number: 8110579Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: GrantFiled: February 11, 2009Date of Patent: February 7, 2012Assignee: Sanofi-AventisInventors: Jean-Michel Altenburger, Valerie Fossey, Philip Janiak, Gilbert Lassalle, Frederic Petit, Jean Claude Vernieres
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Publication number: 20120027682Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: ApplicationFiled: April 15, 2010Publication date: February 2, 2012Inventors: William L. Neumann, John N. Freskos
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Publication number: 20120028941Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclopropyl-3-fluoro-4-methyl-5[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a ?2 adrenoceptor agonist; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a PDE4 inhibitor; a PPAR? agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.Type: ApplicationFiled: December 17, 2009Publication date: February 2, 2012Inventors: Anne Elizabeth Cooper, Timothy John Luker, Jerzy Andrzej Schmidt
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Publication number: 20120015961Abstract: The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-?proteins.Type: ApplicationFiled: March 29, 2010Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Yuusuke Tamura, Shinji Suzuki, Sae Matsumoto, Akihiro Hori, Yuuji Kooriyama
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120010221Abstract: Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation.Type: ApplicationFiled: March 12, 2010Publication date: January 12, 2012Applicant: TOYAMA CHEMICAL CO.,LTD.Inventors: Sahoe Kakuda, Setsuko Nishimura, Takafumi Hirota
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Patent number: 8093252Abstract: A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described.Type: GrantFiled: February 15, 2010Date of Patent: January 10, 2012Assignee: AstraZeneca ABInventors: Sharon Ann Bowden, David Peter Hoile, Karin Lövqvist
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Publication number: 20110319427Abstract: The disclosure provides methods and compositions for treating hematological malignancies.Type: ApplicationFiled: March 2, 2010Publication date: December 29, 2011Applicant: UNIVERSITY HEALTH NETWORKInventor: Aaron D. Schimmer
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Publication number: 20110319353Abstract: A method of treating spinal muscular atrophy. The method includes administering an effective amount of composition including a sodium-proton exchanger inhibitor and a pharmaceutically acceptable carrier or salt, to a subject with spinal muscular atrophy to ameliorate a symptom of spinal muscular atrophy.Type: ApplicationFiled: August 29, 2011Publication date: December 29, 2011Inventors: Jan-Gowth CHANG, Chung-Yee Yuo, Wen-Kuang Yang
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Publication number: 20110319398Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.Type: ApplicationFiled: June 1, 2011Publication date: December 29, 2011Applicant: TUFTS UNIVERSITYInventor: Joan Mecsas
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Patent number: 8084456Abstract: A compound of general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating a hyperproliferation-related disease state or disorder in a subject using a compound of formula (I) is also described.Type: GrantFiled: December 11, 2003Date of Patent: December 27, 2011Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Xianyong Bu, Harrison Sikanyika, Michael Francis Harte
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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: 20110311594Abstract: The present invention provides a controlled release pharmaceutical composition which exhibits reduced food effect.Type: ApplicationFiled: June 21, 2011Publication date: December 22, 2011Inventors: Shou-Chiung Chen, Shao-Ming Lee, Chaur-Ming Jan
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Patent number: 8076341Abstract: A compound of formula (I) wherein R1 is selected from H, F, Cl, Br, CF3, C1-C6 alkoxy and OH; R2 is selected from H and C1-C6 alkyl; n is 1-12; m is O or 1; Y is selected from CH2, NR3, (NR3R4)+X, O and S; R3 and R4 are independently selected from H and C1-C4 alkyl; and X? is selected from phannaceutically acceptable anions. A method of preparing the compound, its use as a pharmaceutical, and a method of treatment.Type: GrantFiled: January 22, 2007Date of Patent: December 13, 2011Assignee: Vironova ABInventors: Mohammed Homman, Robert Engovist, Cecilia E Söderberg-Nauclér, Jan Bergman
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Publication number: 20110301179Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.Type: ApplicationFiled: October 21, 2009Publication date: December 8, 2011Inventors: Xiangshu Xiao, Bingbing Li
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Publication number: 20110300137Abstract: The present application discloses the use of the anti-malarial drug lumefantrine and related compounds in the treatment of cancer.Type: ApplicationFiled: June 1, 2011Publication date: December 8, 2011Inventor: Douglas Tyler McKenzie
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Publication number: 20110301178Abstract: This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides.Type: ApplicationFiled: May 31, 2011Publication date: December 8, 2011Applicant: DOW AGROSCIENCES LLCInventors: Kristy Bryan, George E. Davis, Paul R. Graupner, Beth Lorsbach, W. John Owen, Francis E. Tisdell
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Patent number: 8071594Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.Type: GrantFiled: June 22, 2004Date of Patent: December 6, 2011Assignee: Glaxo Group LimitedInventor: John Liddle
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Patent number: 8071606Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. The variables R1, R2, R3 and R4 are as described herein.Type: GrantFiled: January 20, 2010Date of Patent: December 6, 2011Assignee: Pfizer Inc.Inventors: John William Benbow, Jeffrey Allen Pfefferkorn
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Patent number: 8067420Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: GrantFiled: February 16, 2011Date of Patent: November 29, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Sharon N. Bisaha, Saleem Ahmad, Khehyong Ngu, William N. Washburn
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Patent number: 8058278Abstract: The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a subject in need of increased mucociliary clearance and mucosal hydration.Type: GrantFiled: September 7, 2007Date of Patent: November 15, 2011Assignee: Parion Sciences, Inc.Inventors: Michael Ross Johnson, Richard C. Boucher, Andrew J. Hirsh
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Publication number: 20110275603Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant K. BHAVAR, Srikant VISWANADHA, Swaroop Kumar V.S. VAKKALANKA, Gayatri S. MERIKAPUDI
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Publication number: 20110269760Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: Cytopia Research Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Patent number: 8048886Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:Type: GrantFiled: December 7, 2007Date of Patent: November 1, 2011Assignee: Novartis AGInventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
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Publication number: 20110263601Abstract: Methods are disclosed for treating ulcerative colitis and related diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.Type: ApplicationFiled: October 25, 2010Publication date: October 27, 2011Inventors: Philip Manton Brown, Qingyun Liu, Brian Zambrowicz
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Publication number: 20110263585Abstract: The present invention relates to polypeptides, preferably from Drosophila melanogaster (DmShaI) as target for insecticides.Type: ApplicationFiled: November 5, 2009Publication date: October 27, 2011Applicant: BASF SEInventors: Paul Bernasconi, John Dorsch, Lynn Stam, Scott Zitko, Nancy B. Rankl, Mike Griswold, Franz-Josef Braun, Gang Lu, Robert D. Kirkton, Barbara Wedel, Joachim Dickhaut, Angela Hofhine, Jennifer Zink, Fae Malone, Daniel Houtz, Steffen Gross, Ramani Kandasamy, Damian London, Thomas M. Gurganus
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Publication number: 20110257085Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.Type: ApplicationFiled: April 6, 2011Publication date: October 20, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
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Patent number: 8039623Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: March 9, 2007Date of Patent: October 18, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, Robert B. Perni, Janos Pitlik
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Patent number: 8039475Abstract: The invention relates to compositions and co-crystals each comprising (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-1-carboxamide having the structure: and the co-crystal former salicylic acid. Also within the scope of this invention are methods of making and using the same.Type: GrantFiled: February 27, 2007Date of Patent: October 18, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Patrick R. Connelly, Sherry Collier, Michael Tauber
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Publication number: 20110250139Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.Type: ApplicationFiled: December 17, 2009Publication date: October 13, 2011Inventors: Amruta Poreddy, William L. Neumann
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Publication number: 20110250271Abstract: The present invention provides to a method of administration of two or more therapeutically active agents comprising orally administering to a patient a spaced drug delivery system, wherein the time of release of the two or more therapeutically active agents is designed to provide desired control on the disease condition. The present invention also provides a method of administration of two or more therapeutically active agents comprising orally administering to a patient a spaced drug delivery system at a specified time prior to food intake by the patient. The present invention further provides a spaced drug delivery system that releases two or more antidiabetic agents at different times after oral administration, for the treatment of diabetes mellitus or conditions associated with diabetes mellitus.Type: ApplicationFiled: June 17, 2011Publication date: October 13, 2011Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LIMITEDInventors: Dilip Shantilal Shanghvi, Kirti Wardhaman Ganorkar, Yashoraj Rupsinh Zala, Nitin Bhalachandra Dharmadhikari, Satish C. Khanna
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Patent number: 8034819Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).Type: GrantFiled: March 6, 2008Date of Patent: October 11, 2011Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma LimitedInventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Publication number: 20110237584Abstract: Provided is a kynurenine production inhibitor comprising a nitrogen-containing heterocyclic compound represented by formula (I): (wherein R50 and R51 may be the same or different and each represent a hydrogen atom or the like, G1 and G2 may be the same or different and each represent a nitrogen atom or the like, X represents formula (III): (wherein m1 and m2 may be the same or different and each represent an integer of 0 or 1, Y represents an oxygen atom or the like, and R6 and R7 may be the same or different and each represent a hydrogen atom or the like), R1 represents optionally substituted lower alkyl or the like, R2 represents a hydrogen atom or the like, and R3 represents optionally substituted lower alkyl or the like), and the like.Type: ApplicationFiled: November 9, 2009Publication date: September 29, 2011Inventors: Nobuyoshi Amishiro, Yuichi Fukuda, Keisuke Kinpara, Motoya Mie, Hisashi Tagaya, Takeshi Takahashi
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Publication number: 20110230483Abstract: 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: ApplicationFiled: March 14, 2011Publication date: September 22, 2011Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20110230501Abstract: Disclosed herein is a pharmaceutical composition comprising Hydroxychloroquine or its pharmaceutically acceptable salt and at least one antidiabetic compound, useful in the treatment of diabetes mellitus.Type: ApplicationFiled: September 23, 2009Publication date: September 22, 2011Applicant: IPCA Laboratories Ltd.Inventor: Anil Pareek
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Publication number: 20110224136Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.Type: ApplicationFiled: November 17, 2009Publication date: September 15, 2011Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, David Kim, Hyunjin Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Gang Zhou, Nicolas Zorn
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Publication number: 20110217265Abstract: Screening methods are provided for identifying pharmacologic inhibitors of HCV amphipathic helix (AH) function, which inhibitors are useful in the prevention and treatment of HCV infection. Also provided are compounds useful in the inhibition of viral replication. The methods of the invention are based on the unexpected discovery that the presence of an AH, e.g. an AH of an HCV polypeptide, causes an increase in the apparent diameter of the vesicles. The methods of the invention provide for addition of AH peptides to lipid vesicles, for example in a high-throughput format; which addition may be performed in the absence or presence of a candidate pharmacologic agent. The change in apparent vesicle size is measured, and compared to control samples. An increase in vesicle size or aggregation is indicative of AH function being present; and a lack of increase is indicative that the AH function is absent or has been inhibited by a test agent.Type: ApplicationFiled: September 23, 2009Publication date: September 8, 2011Inventors: Jeffrey S. Glenn, Nam-Joon Cho, Wenjin Yang
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Publication number: 20110218209Abstract: The present invention is a hypoallergenic nutrient delivery drug composition, that includes an active drug, a binder with non-genetically engineered and non-chemically treated starches and food powders, a filler with non-genetically engineered and non-chemically treated vegetable powder and/or extracts and a non-genetically engineered and non-chemically treated fruit powder and/or extract and a preservative that includes non-genetically engineered and non-chemically treated fruit juice, fruit oil and vitamins. There is also a sustained nutrient drug delivery composition that includes non-genetically engineered and non-chemically treated oils, starches and vegetable powders and/or extracts and fruit powder and/or extracts. There is also a broad spectrum nutrient delivery drug composition that includes non-genetically engineered and non-chemically treated pepper and oil mixtures or extracts.Type: ApplicationFiled: March 2, 2011Publication date: September 8, 2011Inventor: Paul Daniel Yered
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Publication number: 20110218208Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: ApplicationFiled: June 23, 2009Publication date: September 8, 2011Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Patent number: 8012984Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: GrantFiled: September 14, 2010Date of Patent: September 6, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Sharon N. Bisaha, Saleem Ahmad, Khehyong Ngu, William N. Washburn
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Publication number: 20110212968Abstract: The invention relates to novel phenethylamide derivatives and their wherein A, B, R1, R2 and R3 are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: October 13, 2009Publication date: September 1, 2011Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen, Daniel Trachsel, Jodi T. Williams
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Publication number: 20110212969Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Patent number: 8003654Abstract: The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.Type: GrantFiled: April 10, 2007Date of Patent: August 23, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornelia Zumbrunn Acklin
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Publication number: 20110201625Abstract: A compound of Formula I or a hydrate or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 8, 2009Publication date: August 18, 2011Inventors: Stephen Paul Collingwood, Nicholas James Devereux, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt
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Publication number: 20110201603Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.Type: ApplicationFiled: July 30, 2009Publication date: August 18, 2011Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
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Patent number: 7998965Abstract: The present invention relates to modulators of metalloproteinase activity.Type: GrantFiled: May 14, 2009Date of Patent: August 16, 2011Assignee: Wyeth LLCInventors: Phaik-Eng Sum, Jerauld Stanley Skotnicki, Steve Yik-Kai Tam, Tarek Suhayl Mansour, David Brian How, Joshua James Sabatini, Jason Shaoyun Xiang, Eric Feyfant
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Publication number: 20110195935Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.Type: ApplicationFiled: September 24, 2009Publication date: August 11, 2011Inventor: Michael Farber
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Publication number: 20110195907Abstract: The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the amiloride conjugates of the present invention for treating cancer or a central nervous system disease or disorder or for preventing or reducing ischemia-reperfusion injury. Further, kits are provided for the treatment of a central nervous system disease or disorder or for the prevention or reduction of ischemia-reperfusion injury using the amiloride conjugates of the present invention.Type: ApplicationFiled: January 3, 2011Publication date: August 11, 2011Applicant: The Regents of the University of California Office of Technology TransferInventors: Fredric A. Gorin, Michael H. Nantz
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Publication number: 20110195979Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.Type: ApplicationFiled: February 7, 2011Publication date: August 11, 2011Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
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Publication number: 20110195973Abstract: The present invention relates to sodium channel blockers. The present Invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: June 11, 2007Publication date: August 11, 2011Applicant: PARION SCIENCES, Inc.Inventor: Michael Ross Johnson