Plural Ring Nitrogens In The Seven-membered Hetero Ring Patents (Class 514/211.08)
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Publication number: 20110086797Abstract: Provided are compositions and methods for treating bacterial infections. It is demonstrated herein that bacteria cell wall materials stimulate germination of spores of Gram-positive bacteria, and that such activity requires Ser/Thr kinase PrkC. By modulating one or both, spores (which can be antibiotic resistant) can be stimulated or inhibited from germination, which can be exploited in various methods of therapeutic treatment. Also provided is a method of modulating germination of a spore of a Gram-positive bacterium. Also provided is a method of decontaminating an environment.Type: ApplicationFiled: March 26, 2010Publication date: April 14, 2011Applicant: The Trustees of Columbia University in the City of New YorkInventor: Jonathan Dworkin
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Publication number: 20110071134Abstract: A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role:Type: ApplicationFiled: April 26, 2010Publication date: March 24, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Zhan Shi, Brendan S. Chen, Jane F. Schmidt, John C. Reader, Neal D. Hone, Jeffrey P. Ciavarri
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Publication number: 20110070221Abstract: The present invention provides methods of detecting mutations in a Gnaq gene in a melanocytic neoplasm for diagnostic and prognostic purposes. The invention further provides methods of treating such melanocytic neoplasm by modulating the activity of the mutated Gnaq gene.Type: ApplicationFiled: February 8, 2008Publication date: March 24, 2011Inventors: Boris C. Bastian, Catherine D. Van Raamsdonk, Gregory S. Barsh
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Patent number: 7902183Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R5 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 5, 2007Date of Patent: March 8, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Bodo Betzemeier, Darryl McConnell, Thomas Gerstberger, Matthias Grauert, Matthias Hoffmann, Maria Impagnatiello, Lars van der Veen, Ulrike Weyer-Czernilofsky
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Publication number: 20110052599Abstract: Compositions and methods are provided for enhancing the survival and promoting the maturation of mammalian oocytes, zygotes and preimplantation embryos. BDNF or BDNF agonists may be administered to an individual, or to cells in vitro, to enhance cellular maturation, embryo growth and fertilization. Accordingly, compositions comprising BDNF are herein presented for use in promoting in vivo oocyte maturation as well as for use as a component in culture media for promoting preimplantation maturation of zygotes and embryos, for instance, for use with in vitro fertilization procedures and for the production of stem cells. Additionally, compounds that interfere with the binding of BDNF to its receptor may be administered to an individual to prevent oocyte maturation, thereby acting as a contraceptive. The BNDF receptor, TrkB, and BDNF also find use in the screening and design of agonists and antagonists for use in the methods of the invention.Type: ApplicationFiled: June 17, 2010Publication date: March 3, 2011Inventors: Kazuhiro Kawamura, Aaron J.W. Hsueh, Sabine M. Mulders
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Patent number: 7884097Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising novel diamine compositions for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.Type: GrantFiled: September 7, 2004Date of Patent: February 8, 2011Assignee: Sequella, Inc.Inventors: Elena Bogatcheva, Marina Protopopova, Boris Nikonenko
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Publication number: 20110020362Abstract: The current invention provides mechanisms by which chronic stress induced hypersensitivity exacerbates the symptoms of irritable bowel syndrome. The invention includes methods of treating irritable bowel syndrome using agents which inhibit key molecules involved in the sensitization pathway.Type: ApplicationFiled: July 20, 2010Publication date: January 27, 2011Inventor: Sushil K. Sarna
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Publication number: 20110020338Abstract: The invention relates to the use of compounds of formula (I) or (II) in the treatment of mammalian target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.Type: ApplicationFiled: March 24, 2009Publication date: January 27, 2011Inventor: Carlos Garcia-Echeverria
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Patent number: 7875605Abstract: N-arylsulfonyl-3-substituted indole compounds, derivatives, analogs, tautomeric forms, stereoisomers, geometric forms, N-oxides, polymorphs and pharmaceutically acceptable salts.Type: GrantFiled: June 5, 2003Date of Patent: January 25, 2011Assignee: Suven Life Sciences LimitedInventors: Venkata Satya Nirogi Ramakrishna, Vikas Shreekrishna Shirsath, Rama Sastri Kambhampati, Venkata Satya Veerabhadra Vadlamudi Rao, Venkateswarlu Jasti
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Publication number: 20110009383Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.Type: ApplicationFiled: September 8, 2010Publication date: January 13, 2011Inventors: James Douglas GRIFFIN, Doriano Fabbro
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Publication number: 20110008468Abstract: Aspects of this invention are related, at least in part, to the use of chemical compounds able to inhibit GSK-3 and/or to stabilize ?-catenin and formulations thereof. Some aspects of this invention relate to compositions comprising such compounds. Some aspects of the invention provide methods of using such compounds and/or compositions in the treatment of subjects having a neurological disease and/or psychiatric disorder. Some aspects of this invention provide methods of using ruboxistaurin, enzastaurin, sunitinib, midostaurin, lestaurtinib, 7-hydroxystaurosporine, and/or Chir99021 in the treatment of subjects having a neurological disease and/or psychiatric disorder. In some embodiments, compounds are administered in combination with Lithium.Type: ApplicationFiled: February 27, 2010Publication date: January 13, 2011Inventors: Stephen J. Haggarty, Daniel Fass, Jennifer Pan, Josh Ketterman, Edward Holson, Tracey Lynn Petryshen, Michael C. Lewis
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Publication number: 20100311593Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.Type: ApplicationFiled: March 11, 2010Publication date: December 9, 2010Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
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Publication number: 20100310563Abstract: Methods are provided for treating a subject with a cellular proliferative disorder that include administering to the subject a therapeutically effective amount of a JAK2 inhibitor and a therapeutically effective amount of a TNF-alpha inhibitor. In addition, methods are provided herein for determining if a subject with a cellular proliferative disorder would benefit from treatment with an agent that inhibits tumor necrosis factor (TNF)-alpha. Methods are also provided for identifying an agent of use in treating a subject with a cellular proliferative disorder or with a predisposition for cellular proliferative disorder. The methods include contacting an isolated cell expressing an activating mutation in the JAK2 protein with a test agent, and detecting the amount of tumor necrosis factor (TNF)-alpha produced by the cell.Type: ApplicationFiled: November 28, 2008Publication date: December 9, 2010Inventors: Thomas G.P. Bumm, Michael W.N. Deininger
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Publication number: 20100311716Abstract: Compositions and methods for lowering IOP and/or providing neuroprotection are disclosed. The compositions and methods are particularly directed to the use inhibitors of Jun N-terminal kinases (JNK) to lower IOP and/or provide neuroprotection.Type: ApplicationFiled: August 18, 2010Publication date: December 9, 2010Applicant: ALCON, INC.Inventors: Debra L. Fleenor, Iok-Hou Pang
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Patent number: 7834000Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: June 13, 2007Date of Patent: November 16, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Gutierrez, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Daniele Bergeron, Sanghee Yoo, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar
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Publication number: 20100280003Abstract: The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Nigel Graham Cooke, Paul W. Manley
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Publication number: 20100272706Abstract: This invention provides methods for inhibiting or treating infection by viruses, in particular pox viruses by modulating a kinase, in particular by inhibiting a host cell kinase, involved in mediating viral infection. Methods to identify, validate, and classify the cellular proteins required by viruses during infection of host cells in order to select agents which can inhibit viral infection are described herein. Using a systems biology approach the virus/host cell interaction is studied from initial attachment of the incoming virus to the cell surface, to entry, transcription, replication, biosynthesis, and assembly of progeny particles. The method employs a siRNA screening platform and uses gene silencing to map the ‘viral infectome’—a compilation of cellular proteins that the virus needs to establish infection and drive the infectious cycle.Type: ApplicationFiled: June 20, 2008Publication date: October 28, 2010Inventors: Jason Mercer, Urs Greber, Stefan Moese, Ari Helenius, Lucas Pelkmans
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Publication number: 20100273769Abstract: The present invention relates to the use of specific indolocarbazole compounds for the preparation of pharmaceutical compositions for the treatment of Parkinson's disease. In particular, the compounds of the invention are useful for the prevention or treatment of PD, similar forms of Parkinsonism, and synucleopathies involving Lewy body neurodegeneration.Type: ApplicationFiled: January 26, 2010Publication date: October 28, 2010Inventor: Hanno RODER
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Publication number: 20100240635Abstract: Compounds of formula (I): wherein: R1 and R2, which may be the same or different, each represent a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, acyl, alkoxycarbonyl, carboxy, hydroxy, hydroxyalkyl, cyano, nitro, amino, substituted or unsubstituted aminocarbonyl, aminosulphonyl, alkylsulphonylaminoalkyl, N-hydroxy-carboximidamide or benzyloxy group, R3 represents a hydrogen atom or an alkyl, cycloalkyl or cycloalkylalkyl group, R4 represents a hydrogen atom or a substituted or unsubstituted alkyl group Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator and/or an NMDA receptor antagonist.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: LES LABORATOIRES SERVIERInventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
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Publication number: 20100239563Abstract: The invention relates to the use of at least one active substance for producing a pharmaceutical composition for the prophylaxis and/or treatment of at least one viral disease. It is characterized by active substance(s) which inhibit(s) either at least two kinases or at least one SEK kinase of a cellular signal transmission path such that virus multiplication is inhibited.Type: ApplicationFiled: December 23, 2008Publication date: September 23, 2010Inventors: Stephan Ludwig, Oliver Planz, Hans-Harald Sedlacek, Stephan Pleschka
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Publication number: 20100234348Abstract: The present invention provides compounds that potentiate the activity of antibiotic agents, particularly quinolones such as norflaxin. The invention further provides compositions, e.g., pharmaceutical compositions, comprising the inventive compounds. The invention also provides compositions comprising an antibiotic (e.g., a quinolone) and a compound that potentiates activity of the antibiotic. The invention further provides methods of treating a subject comprising administering any of the inventive compounds or compositions to the subject. The invention also provides screening methods to identify compounds that potentiate the activity of an antibiotic, e.g., a quinolone.Type: ApplicationFiled: August 2, 2007Publication date: September 16, 2010Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Guillaume Cottarel, Timothy S. Gardner, Xiaoguang Lei, John Porco, Scott E. Schaus, Jamey Wierzbowski, Kollol Pal
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Patent number: 7795246Abstract: A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.Type: GrantFiled: November 20, 2003Date of Patent: September 14, 2010Assignee: Cephalon, Inc.Inventors: Dave Dickason, Bradley T. McIntyre, Piyush R. Patel
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Publication number: 20100227849Abstract: A method of inducing high anti-leukemia activity responsive to the combination of hydroxamic acid analogue histone deacetylase inhibitors and PKC412 against human acute leukemia characterized as expressing phosphorylated (p)FLT3 kinase by a novel flow cytometry-based assay.Type: ApplicationFiled: April 22, 2010Publication date: September 9, 2010Applicant: UNIVERSITY OF SOUTH FLORIDAInventor: Kapil N. Bhalla
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Patent number: 7786106Abstract: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4?-bromo-2?-[(5-chloro-2-pyridyl) carbamoyl]-6?-?-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2?-(2-acetamido-2-deoxy-?-D-glucopyranosyloxy)-4?-bromo-6?-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.Type: GrantFiled: January 20, 2009Date of Patent: August 31, 2010Assignee: Astellas Pharma Inc.Inventors: Tsukasa Ishihara, Fukushi Hirayama, Keizo Sugasawa, Yuji Koga, Takeshi Kadokura, Takeshi Shigenaga
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Patent number: 7781596Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.Type: GrantFiled: October 28, 1999Date of Patent: August 24, 2010Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Michael Kock, Thomas Höger
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Publication number: 20100189762Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.Type: ApplicationFiled: December 21, 2009Publication date: July 29, 2010Applicant: EMORY UNIVERSITYInventor: Jack L. Arbiser
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Publication number: 20100189757Abstract: The present invention relates to novel drug depot implant designs for optimal delivery of therapeutic agents to subjects. The invention provides a method for alleviating pain associated with neuromuscular or skeletal injury or inflammation by targeted delivery of one or more therapeutic agents to inhibit the inflammatory response which ultimately causes acute or chronic pain. Controlled and directed delivery can be provided by drug depot implants, comprising therapeutic agents, specifically designed to deliver the therapeutic agent to the desired location by facilitating their implantation, minimizing their migration from the desired tissue location, and without disrupting normal joint and soft tissue movement.Type: ApplicationFiled: March 1, 2010Publication date: July 29, 2010Applicant: WARSAW ORTHOPEDIC, INC.Inventor: William F. McKay
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Patent number: 7759354Abstract: The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.Type: GrantFiled: June 12, 2006Date of Patent: July 20, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
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Publication number: 20100143440Abstract: Methods and compositions related to treating or preventing a proliferative disease in a subject comprising administering an inhibitor of a UL97 or a UL97 homolog to the subject are described.Type: ApplicationFiled: March 4, 2008Publication date: June 10, 2010Applicant: The UAB Research FoundationInventor: Mark N. Prichard
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Publication number: 20100144616Abstract: One aspect of the present application relates to a method for limiting damage to neuronal cells by ischemic or epoxic conditions, e.g., such as may be manifest by a reduction in brain infarct volume, by administering to an individual a hedgehog therapeutic or ptc therapeutic in an amount effective for reducing cerebral infarct volume.Type: ApplicationFiled: July 28, 2008Publication date: June 10, 2010Applicant: Curis, Inc.Inventor: Nagesh K. Mahanthappa
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Publication number: 20100143459Abstract: A pharmaceutical dosage form comprises a solid dispersion product of at least one tyrosine kinase inhibitor, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer.Type: ApplicationFiled: November 8, 2007Publication date: June 10, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Bernd Liepold, Jörg Rosenberg, Martin Knobloch, Christian Nehen
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Publication number: 20100144703Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Patent number: 7678785Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: GrantFiled: July 24, 2007Date of Patent: March 16, 2010Assignee: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Publication number: 20100056467Abstract: The present invention relates to methods of treating hematological malignancies, including acute myeloid leukemia (AML), comprising the combination of a compound that inhibits the binding of the Smac protein to IAPs (“IAP inhibitor”) and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; and a commercial package comprising said combination. The present invention also relates to the use of IAP inhibitors in combination with one or more pharmaceutically active agents for the preparation of a medicament to treat hematological malignancies, including AML.Type: ApplicationFiled: November 27, 2007Publication date: March 4, 2010Applicants: NOVARTIS AG, DANA-FARBER CANCER INSTITUTE, INC.Inventors: James Douglas Griffin, Leigh Zawel
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Publication number: 20100048534Abstract: Crystalline lestaurtinib hydrates and crystalline lestaurtinib hemihydrate hemicetonitrileate and crystalline lestaurtinib hemihydrate hemitetrahydrofuranate, processes to reproducibly make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: November 3, 2009Publication date: February 25, 2010Applicant: ABBOTT LABORATORIESInventors: Walter Dziki, Gowdahalli N. Subbarao, Rodger F. Henry
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Publication number: 20100048533Abstract: Lestaurtinib Crystalline Form 1, isolated crystalline lestaurtinib anhydrate and amorphous lestaurtinib, processes to reproducibly make them and methods of treating patients using them.Type: ApplicationFiled: October 28, 2009Publication date: February 25, 2010Applicant: ABBOTT LABORATORIESInventors: Walter Dziki, Gowdahalli N. Subbarao, Rodger F. Henry
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Publication number: 20100016282Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: ApplicationFiled: July 8, 2009Publication date: January 21, 2010Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20090286770Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving ras or FGFR3 signalling pathways and l or c-fos transcription, especially for the curative and/or prophylactic treatment of myeloma or multiple Myeloma, and to a method of treating diseases involving ras or FGFR3 signalling pathways and/or c-fos transcription.Type: ApplicationFiled: December 7, 2005Publication date: November 19, 2009Inventors: D. Gary Gilliland, James Douglas Griffin, Jing Chen, Kenneth C. Anderson
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Publication number: 20090252757Abstract: This invention provides novel HIV-interacting host factors. The invention also provides methods of using the HIV-interacting host factors to screen for compounds that inhibit HIV infection. The methods comprise first screening test compounds for modulators of an HIV interacting host factor disclosed herein, and then further screening the identified modulating compounds for ability to inhibit HIV infection. The invention further provides methods and pharmaceutical compositions for treating diseases and conditions associated with HIV infection.Type: ApplicationFiled: December 8, 2006Publication date: October 8, 2009Applicant: IRM LLCInventors: Deborah Nguyen, Kelli L. Kuhen, Jeremy S. Caldwell
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Publication number: 20090233905Abstract: The invention relates to a combination comprising a Bcr-Abl, c-Kit and PDGF-R tyrosine kinase inhibitor; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.Type: ApplicationFiled: April 4, 2007Publication date: September 17, 2009Inventors: Gregory Peter Burke, Ronald Richard Linnartz, Paul W. Manley, Richard William Versace
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Publication number: 20090227563Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: September 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Udo Bickers, Hans Philipp Huff, Erwin Hacker, Rainer Süssmann
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Publication number: 20090226500Abstract: Sutures are used in combination with anti-scarring agents to inhibit fibrosis between the sutures and the host tissues into which the sutures are inserted. Compositions and methods are described for use in reducing excessive scarring, surgical adhesion, and other disorders.Type: ApplicationFiled: January 31, 2007Publication date: September 10, 2009Applicant: Angiotech Pharmaceuticals, IncInventors: Rui Avelar, Arpita Maiti, Philip M. Toleikis, Johanne Diane Cashman, David M. Gravett
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Publication number: 20090221550Abstract: The present invention relates to the use of the combination of tyrosine phosphate inhibitors AMN107 and PKC412 for the preparation of a drug for the treatment of a mast cell-related proliferative disease. The present invention is also drawn to a combination treatment of a tyrosine phosphate inhibitor and a TK-inhibitor that is effective against a mast cell-related proliferative disease, including especially systemic mastocytosis (SM) including aggressive SM (ASM) and mast cell leukemia (MCL).Type: ApplicationFiled: July 19, 2006Publication date: September 3, 2009Inventor: Peter Valent
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Publication number: 20090209513Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: August 20, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Peter Marczok, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich Sanwald, Rolf Pontzen
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Publication number: 20090196931Abstract: Methods are provided for inhibiting or treating stenosis or restenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective amount of a therapeutic agent via a catheter. Also provided is a catheter adapted for administering a therapeutically effective amount of a therapeutic agent to a mammalian host for inhibiting or treating stenosis or restenosis.Type: ApplicationFiled: April 3, 2009Publication date: August 6, 2009Inventors: Lawrence L. Kunz, Peter G. Anderson
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Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Publication number: 20090170830Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: July 28, 2006Publication date: July 2, 2009Inventor: Philippe G. Nantermet
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Publication number: 20090155352Abstract: The invention described herein provides a pharmaceutical composition and oral dosage forms containing the same, having high concentrations of solubilized indolocarbazole compounds as the active ingredient in microemulsion form. The invention also provides a process for increasing the solubilized concentration of indolocarbazole compounds such as lestaurtinib using the addition of water in combination with a hydrophilic component as part of the microemulsion formation process.Type: ApplicationFiled: November 20, 2008Publication date: June 18, 2009Applicant: Cephalon, Inc.Inventors: Anthony S. Drager, Bradley T. Mclntyre, Piyush R. Patel
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Publication number: 20090143356Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.Type: ApplicationFiled: October 26, 2006Publication date: June 4, 2009Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda