Polycylo Ring System Having A Ring Nitrogen In The System Patents (Class 514/80)
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Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20120178715Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.Type: ApplicationFiled: September 3, 2010Publication date: July 12, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Steven W. Andrews, Kevin Ronald Condroski, Lisa A. De Meese, Jay Bradford Fell, John P. Fischer, John A. Josey, Kevin Koch, Yvan Le Huerou, Gregory F. Miknis, Martha E. Rodriguez, George T. Topalov, Eli M. Wallace, Rui Xu
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Publication number: 20120178714Abstract: This disclosure concerns a new family of phosphorus-containing compounds of Formula (I): and pharmaceutically acceptable derivatives thereof. Compositions containing such compounds and uses thereof are also provided.Type: ApplicationFiled: November 14, 2011Publication date: July 12, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: David L. Berstein, Leonard W. Rozamus, Yihan Wang, Chester A. Metcalf, III
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Patent number: 8207146Abstract: The present invention relates to substituted phenothiazines with a double bond and physiologically acceptable salts thereof, and their use as a medicament.Type: GrantFiled: March 16, 2010Date of Patent: June 26, 2012Assignee: Sanofi-AventisInventors: Stefanie Keil, Elisabeth Defossa, Dieter Schmoll, Axel Dietrich, Johanna Kuhlmann-Gottke, Karl-Christian Engel
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Patent number: 8207117Abstract: The invention concerns glycosylated proteins having human factor VIII activity. In a preferred embodiment, the protein is glycosylated with oligosaccharides that include an alpha-(2,6)-linked sialic acid and a bisecting GlcNAc linked to a core beta-mannose.Type: GrantFiled: November 8, 2010Date of Patent: June 26, 2012Assignee: Bayer Healthcare LLCInventors: Myung-Sam Cho, Sham-Yuen Chan
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Publication number: 20120156262Abstract: Disclosed is an insecticidal suspension concentrate composition comprising by weight based on the total weight of the composition: (a) from about 0.3 to about 30% of 3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)carbonyl]phenyl]-1H-pyrazole-5-carboxamide; (b) from about 5 to about 70% of a nonionic ethylene oxide-propylene oxide block copolymer component having a water solubility of at least about 5% by weight at 20° C., a hydrophilic-lipophilic balance value ranging from about 5 to about 18 and an average molecular weight ranging from about 900 to about 20000 daltons; and (c) from about 20 to about 95% of water. Also disclosed is a method for controlling an insect pest comprising diluting said suspension concentrate composition with water to form a diluted composition, and contacting the insect pest or its environment with an insecticidally effective amount of said diluted composition.Type: ApplicationFiled: September 3, 2010Publication date: June 21, 2012Inventors: Oiver Walter Gutsche, John Henry Green
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Publication number: 20120157371Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: December 12, 2011Publication date: June 21, 2012Inventors: Chongxi YU, Lina Xu, Yuhua Chen, Binbing Yan, Shiqian Tu
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Publication number: 20120149665Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.Type: ApplicationFiled: August 25, 2010Publication date: June 14, 2012Applicant: Bionomics LimitedInventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
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Publication number: 20120129810Abstract: The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described.Type: ApplicationFiled: May 4, 2010Publication date: May 24, 2012Applicant: The Trustees of the University of PennsylvaniaInventors: Ravi Kumar Amaravadi, Craig B. Thompson
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Publication number: 20120129809Abstract: The invention provides a method for treating NSCLC, especially in cases of KRAS mutation, involving the administration of deforolimus.Type: ApplicationFiled: March 2, 2010Publication date: May 24, 2012Applicant: MERCK & CO.,Inventor: Scot Ebbinghaus
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Publication number: 20120122679Abstract: Disclosed are compounds of Formula 1, N-oxides and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, EC(?X1); a is 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 3, 2010Publication date: May 17, 2012Applicant: E. I. Du Pont De Nemours and CompanyInventors: Wenming Zhang, Caleb William Holyoke, JR., Kenneth Andrew Hughes, George Philip Lahm, Thomas Francis Pahutski, JR., My-Hanh Thi Tong, Stephen Frederick McCann
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Publication number: 20120115722Abstract: Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, wherein R1 is phenyl optionally substituted with up to 5 substituents independently selected from R3, or pyridinyl optionally substituted with up to 4 substituents independently selected from R3; R2 is C1-C4 haloalkyl; or thiazolyl, pyridinyl or pyrimidinyl, each optionally substituted with up to 2 substituents independently selected from the group consisting of halogen and C1-C4 alkyl; each R3 is independently halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C(R4)?NOR4 or Q; each R4 is independently C1-C4 alkyl; Z is CH?CH or S; and each Q is independently phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; and (b) at least one invertebrate pest control agent.Type: ApplicationFiled: August 3, 2010Publication date: May 10, 2012Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Caleb William Holyoke, JR., Wenming Zhang, My-Hanh Thi Tong
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Publication number: 20120116287Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect.Type: ApplicationFiled: October 24, 2011Publication date: May 10, 2012Applicants: Universidad de Buenos Aires, THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Roberto ETCHENIQUE, Rafael Yuste, Luis Baraldo
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Publication number: 20120107274Abstract: Provided are methods for treating Orthomyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein R2 is halogen. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.Type: ApplicationFiled: September 12, 2011Publication date: May 3, 2012Applicant: Gilead Sciences, Inc.Inventors: Michael O'Neil Hanrahan Clarke, Choung U. Kim, Willard Lew
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Publication number: 20120107328Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: November 3, 2008Publication date: May 3, 2012Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
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Patent number: 8163719Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.Type: GrantFiled: July 5, 2011Date of Patent: April 24, 2012Assignee: Johns Hopkins University School of MedicineInventors: Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
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Publication number: 20120088730Abstract: The present invention relates to the discovery that the two ACE domains can have very different effects on cytokine expression. In one embodiment, the present invention provides a method of regulating and/or treating a condition in a subject by administering a therapeutically effective dosage of site specific ACE inhibitor. In another embodiment, the condition is inflammation and/or immune response.Type: ApplicationFiled: June 2, 2010Publication date: April 12, 2012Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Kenneth E. Bernstein, Chentao Lin
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Publication number: 20120082621Abstract: Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula I: wherein: Z is a porphyrinic macrocycle, Alk1 and Alk2 are each independently an alkylidene chain; L is a linking group or is absent; R1 is preferably an ionic group or polar group; R2 is an ionic group, polar group, bioconjugatable group, or targeting group; R3 is present or absent and when present is a halo group, bioconjugatable group, or targeting group, n is O or 1 (that is, the CH group is present, or Alk1 and Alk2 are bonded directly to a carbon of the porphyrinic macrocycle Z); or a salt thereof.Type: ApplicationFiled: December 9, 2011Publication date: April 5, 2012Inventors: K. Eszter Borbas, Jonathan S. Lindsey
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Publication number: 20120076756Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 4, 2011Publication date: March 29, 2012Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20120053051Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22, —S(O)pR25 or —S(O)(?NR28)R29; and R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.Type: ApplicationFiled: February 28, 2011Publication date: March 1, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
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Publication number: 20120046245Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Publication number: 20120040935Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: May 18, 2011Publication date: February 16, 2012Applicant: Vertex Pharmaceuticals, Inc.Inventors: Dean M. Wilson, Andreas P. Termin, Timothy D. Neubert, Jian Wang, Yulian Zhang, Jesus E. Gonzalez, III, Esther Martinborough, Nicole Zimmerman
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Patent number: 8110562Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.Type: GrantFiled: July 19, 2007Date of Patent: February 7, 2012Assignees: University of Tennessee Research Foundation, The Ohio State University Research FoundationInventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Publication number: 20120028907Abstract: The disclosure relates to methods for identifying a tumor as an E2F-responsive gene over-expressing (ERGO) tumor, methods of determining the likelihood that an ERGO tumor patient will survive to a future date, methods of treating an ERGO tumor in a patient, and methods of selecting patients diagnosed as ERGO tumor prostate cancer patients for aggressive clinical treatment. The methods of the disclosure are applicable to ERGO tumors present in different human organs and tissues such as breast, lung, thyroid, ovary, and prostate.Type: ApplicationFiled: November 13, 2009Publication date: February 2, 2012Applicant: Intelligent Oncotherapeutics, Inc.Inventor: Stanley E. Shackney
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Publication number: 20120028924Abstract: The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer.Type: ApplicationFiled: August 2, 2011Publication date: February 2, 2012Applicant: ASTRAZENECA ABInventors: Brian AQUILA, Victor KAMHI, Bo PENG, Timothy PONTZ, Jamal Carlos SAEH, Kumar THAKUR, Bin YANG
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Publication number: 20120028923Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: ApplicationFiled: July 27, 2011Publication date: February 2, 2012Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Publication number: 20120021901Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from the class of the organophosphates or carbamates, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.Type: ApplicationFiled: March 25, 2009Publication date: January 26, 2012Applicant: BAYER CROPsCIENCE AGInventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
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Publication number: 20120015019Abstract: The current invention relates to methods of forming a coating that involves the in-situ formation of drug microspheres. The coating may be applied to a medical device, such as a catheter balloon or a stent. Coated devices and methods of treatment therewith are also encompassed within the embodiments of the present invention.Type: ApplicationFiled: July 14, 2010Publication date: January 19, 2012Applicant: Abbott cardiovascular systems Inc.Inventors: Stephen D. Pacetti, John J. Stankus
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Publication number: 20110319362Abstract: Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: December 7, 2009Publication date: December 29, 2011Inventors: Shaomeng Wang, Jianyong Chen, Cindy Gomez, Longchuan Bai, Zaneta Nikolovska-Coleska, Yu-Jun Zhao
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Publication number: 20110311596Abstract: The current invention relates to poly(amide) and poly(ester-amide) polymers, coatings including the polymers, and narrow polydispersity drug delivery particles including the polymers.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Abbott Cardiovascular Systems Inc.Inventors: Michael Huy Ngo, Mikael O. Trollsas, Thierry Glauser, Jinping Wan, Bozena Zofia Maslanka
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Publication number: 20110300132Abstract: This invention relates to prodrugs of 4-aminoquinazoline compounds, and to pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER2.Type: ApplicationFiled: January 6, 2011Publication date: December 8, 2011Applicant: Concert Pharmaceuticals, Inc.Inventors: Roger Tung, Adam Morgan
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Publication number: 20110294758Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.Type: ApplicationFiled: May 25, 2011Publication date: December 1, 2011Applicant: Metabasis Therapeutics, Inc.Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Publication number: 20110288053Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 20, 2011Publication date: November 24, 2011Applicant: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Heolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoothi Swaninathan, William J. Watkins, Jenneifer Zhang
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Patent number: 8063216Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect.Type: GrantFiled: December 14, 2004Date of Patent: November 22, 2011Assignees: The Trustees of Columbia University in the City of New York, Universidad de Buenos AiresInventors: Roberto Etchenique, Rafael Yuste, Luis Baraldo
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Patent number: 8053423Abstract: The present invention is directed to a stabilized cross-linked hydrogel matrix comprising a first high molecular weight component and a second high molecular weight component that are covalently linked, and at least one stabilizing or enhancing agent, wherein the first high molecular weight component and the second high molecular weight component are each selected from the group consisting of polyglycans and polypeptides. This stabilized hydrogel matrix may be prepared as bioactive gels, pastes, slurries, cell attachment scaffolds for implantable medical devices, and casting or binding materials suitable for the construction of medical devices. The intrinsic bioactivity of the hydrogel matrix makes it useful as a gel or paste in multiple applications, including as a cell attachment scaffold that promotes wound healing around an implanted device, as gels and pastes for induction of localized vasculogenesis, wound healing, tissue repair, and regeneration, as a wound adhesive, and for tissue bulking.Type: GrantFiled: May 18, 2010Date of Patent: November 8, 2011Assignee: Encelle, Inc.Inventors: Francis V. Lamberti, Richard Chris Klann, Ronald Stewart Hill
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Publication number: 20110269716Abstract: The invention relates to antioxidant substituted isoindoline nitroxide compounds and their use in methods of treating or preventing diseases or disorders related to oxidative stress, methods of reducing oxidative stress and methods of protecting a subject from oxidative stress upon exposure to ionising radiation. Pharmaceutical compositions comprising the antioxidant compounds are also described.Type: ApplicationFiled: September 30, 2009Publication date: November 3, 2011Applicant: Queensland University of TechnologyInventors: Steven Bottle, Kathryn Fairfull-Smith, Farina Schill
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Publication number: 20110263530Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: ApplicationFiled: June 28, 2011Publication date: October 27, 2011Applicant: Amgen Inc.Inventors: Victor J. CEE, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Publication number: 20110263533Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: October 12, 2009Publication date: October 27, 2011Inventors: Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka, Brett C. Bookser
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Publication number: 20110263532Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.Type: ApplicationFiled: August 11, 2009Publication date: October 27, 2011Applicant: President and Fellows of Harvard CollegeInventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
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Publication number: 20110263534Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.Type: ApplicationFiled: August 11, 2006Publication date: October 27, 2011Inventors: Yannick Stephane Rose, Stephane Ciblat, Ting Kang, Adel Rafai Far, Evelyne Dietrich, Yanick Lafontaine, Ranga Reddy
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Publication number: 20110257586Abstract: The present invention provides pharmaceutical photosensitizer-loaded nanoparticle formulations and their methods of preparation for photodynamic therapy, comprising a hydrophobic or hydrophilic photosensitizer, nanoparticulate calcium phosphate and in certain cases auxiliary reagents such as stabilizers. The calcium phosphate-based nanoparticle formulations of the present invention provide excellent storage stability and therapeutically effective amounts of photosensitizer for intravenous or topical administration. In a preferred embodiment, tetrapyrrole derivatives such as porphyrins, chlorins and bacteriochlorins, are the preferred hydrophobic photosensitizers to be formulated in calcium phosphate nanoparticle formulations for photodynamic tumor therapy. Additionally, 5,10,15,20-tetrakis(4-phosphonooxyphenyl)porphine (pTPPP) is a preferred hydrophilic photosensitizer for photodynamic tumor therapy.Type: ApplicationFiled: December 18, 2009Publication date: October 20, 2011Applicants: UNIVERSITAT DUISBURG-ESSEN, BIOLITEC AGInventors: Burkhatd Gitter, Susanna Grafe, Arno Wiehe, Volker Albrecht, Matthias Epple, Janine Schwiertz, Kathirvel Ganesan
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Publication number: 20110257129Abstract: 3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other anti-viral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.Type: ApplicationFiled: June 2, 2011Publication date: October 20, 2011Inventors: Richard Storer, Francois-Rene Alexandre, Cyril Dousson, Adel M. Moussa, Edward Bridges, Alistair Stewart, Jing Yang Wang, Benjamin Alexander Mayes
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Patent number: 8034576Abstract: The present invention relates to diuretic pharmaceutical compositions and methods and in particular to certain derivatives of the formula I: or a prodrug or pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.Type: GrantFiled: December 18, 2009Date of Patent: October 11, 2011Assignee: Naturon, Inc.Inventors: Neal Bricker, Stewart Shankel, Christopher D. Cain, Mark Mitchnick, Michael Schmertzler
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Publication number: 20110236437Abstract: Provided herein are nanoparticles and methods for using nanoparticles. The nanoparticles include at least three antiretroviral agents. When introduced to cells the nanoparticles cause an increase in the intracellular concentration of the antiretroviral agents to a level that is at least the IC50 against HIV-I or HIV-2. This concentration may be maintained for at least 21 days after the cells are contacted with the nanoparticle. When administered to a subject the nanoparticles cause the concentration of the antiretroviral agents to increase to at least 100 ng/ml in the serum of the subject, at least 0.5 ?g/gram tissue in an organ of the subject, or a combination thereof. Such a concentration may be maintained for at least 21 days after the administration.Type: ApplicationFiled: December 11, 2009Publication date: September 29, 2011Applicant: Creighton UniversityInventor: Christopher J. Destache
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Publication number: 20110230444Abstract: A pharmaceutical combination comprising an Hsp90 inhibitor and an mTOR inhibitor, and methods of using the combination to treat or prevent proliferative disorders.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Michael Rugaard Jensen
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Publication number: 20110230443Abstract: Novel imidazo[1,2-?]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.Type: ApplicationFiled: September 22, 2009Publication date: September 22, 2011Applicant: ISIS INNOVATION LTD.Inventors: Frank Hallock Ebetino, Adam Mazur, Mark Walden Lundy, Robert Graham Russell
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Publication number: 20110218174Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: October 22, 2009Publication date: September 8, 2011Applicant: MERCK SHARP & DOHME CORP.Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
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Publication number: 20110212923Abstract: The present invention relates to phosphate derivatives of estrogen receptor beta agonists, compositions thereof, preparations thereof, and uses thereof. Formula (I).Type: ApplicationFiled: February 6, 2009Publication date: September 1, 2011Inventors: Reinhardt Baudy, Eugene J. Trybulski, Ronald Magolda, Diane Schneider, Gulnaz Khafizova, Mahdi B. Fawzi, Cuijian Yang
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Patent number: 8008279Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.Type: GrantFiled: June 25, 2008Date of Patent: August 30, 2011Assignee: AstraZeneca ABInventors: Alexander Graham Dossetter, Nicola Murdoch Heron
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Patent number: 8003624Abstract: In its many embodiments, the present invention provides a novel class of indolines as inhibitors of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: February 13, 2007Date of Patent: August 23, 2011Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Kevin D. McCormick, Christopher W. Boyce, Younong Yu