R Contains Benzene Ring Patents (Class 514/615)
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Patent number: 8030341Abstract: The present invention relates to symmetric and asymmetric dimeric Dmt (2?,6?-ditnethyl) compounds and Dmt derivative compounds with dual ? and ? opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.Type: GrantFiled: August 30, 2006Date of Patent: October 4, 2011Assignees: The United States of America as represented by the Secretary of the Department of Health and Human Services, Kobe Gakuin UniversityInventors: Lawrence H. Lazarus, Yoshio Okada, Tingyou Li
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Publication number: 20110224301Abstract: Methods are described, which include the administration of semapimod or guanylhydrazone containing compounds, salt thereof, or a combination of the compound and a salt thereof for the inhibition, treatment, and/or prevention of any of NEC, a condition associated with the release of HMGB1, a condition associated with the release of iNOS protein, a condition associated with the release of Bax protein, a condition associated with the release of Bad protein, a condition associated with the release of COX-2 protein, or a condition associated with the release of RAGE, or a combination thereof to a subject in need thereof.Type: ApplicationFiled: September 10, 2010Publication date: September 15, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventors: Ruben ZAMORA, Henri R. FORD, Thais SIELECKI-DZURDZ, Vidal F. DE LA CRUZ
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Publication number: 20110224302Abstract: Novel difluorophenyldiacylhydrazide derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseasesType: ApplicationFiled: November 2, 2009Publication date: September 15, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Thomas Fuchss, Ulrich Graedler, Norbert Beier, Rolf Gericke, Florian Lang
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Patent number: 8017654Abstract: A method of treating a subject with cancer includes the step of co-administering to the subject over three to five weeks, a taxane in an amount of between about 243 ?mol/m2 to 315 ?mol/m2 (e.g., equivalent to paclitaxel in about 210-270 mg/m2); and a bis(thiohydrazide amide) in an amount between about 1473 ?mol/m2 and about 1722 ?mol/m2 (e.g., Compound (1) in about 590-690 mg/m2). The bis(thiohydrazide amide) is represented by Structural Formula (I), Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is an optionally substituted aromatic group. R1-R4 are independently —H, an optionally substituted aliphatic group, an optionally substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: GrantFiled: April 13, 2006Date of Patent: September 13, 2011Assignee: Synta Pharmaceuticals Corp.Inventors: Thomas A. Dahl, Matthew McLeod
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Publication number: 20110218226Abstract: A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.Type: ApplicationFiled: March 8, 2011Publication date: September 8, 2011Inventor: MENACHEM SHOHAM
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Patent number: 8003692Abstract: Fluorene-based molecules and their derivatives are described in compositions for the treatment of intestinal fluid loss.Type: GrantFiled: June 13, 2008Date of Patent: August 23, 2011Assignees: Board of Regents, The University of Texas System, Mission Pharmacal Co.Inventors: Catherine H. Schein, Johnny W. Peterson, Scott R. Gilbertson, Deliang Chen, Maria Estrella-Jimenez, Mary A. Walter, Jian Gao
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Publication number: 20110201686Abstract: Provided are methods of inhibiting aggregation of amyloid-beta (A?) or accumulation of aggregated A? using certain guanylhydrazone compounds. Also provided are methods of treating or preventing an amyloid-related disease in a mammal, methods of treating a subject having Alzheimer's disease, methods of treating a subject at risk for Alzheimer's disease, methods of inhibiting aggregation or accumulation of a synuclein, methods of treating a subject having a disease at least partially mediated by synuclein, methods of treating a subject at risk for a disease at least partially mediated by synuclein, and methods of inhibiting aggregation or accumulation of a protein involved in a conformational disease, using the guanylhydrazone compounds.Type: ApplicationFiled: June 22, 2007Publication date: August 18, 2011Inventor: Yousef Al-Abed
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Patent number: 7998496Abstract: The subject invention relates in part to the oral administration of ecdysteroids for controlling subterranean termites. Preferred ecdysteroids for use according to the subject invention are ecdysone, certain ecdysone analogs, and 20-hydroxyecdysone, for example. In some preferred embodiments, one or more of these compounds is used in a termite bait in combination with one or more chitin synthesis inhibitors (CSI), such as hexaflumuron and/or noviflumuron. The subject invention also relates to mixtures comprising these two active ingredients. The ecdysteroid analog or molt-accelerating compound (MAC) typically induces a preliminary molting event in termite workers, which then allows the CSI to further disrupt the molt and cause mortality. The combination of these active ingredients, causing accelerated molting together with inhibition of chitin synthesis, is surprisingly shown herein to enhance activity against termites, as compared to either group of compounds alone.Type: GrantFiled: February 17, 2005Date of Patent: August 16, 2011Assignee: University of Florida Research Foundations, Inc.Inventors: Nan-Yao Su, James Edward King, Paul Allen Neese
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Patent number: 7994221Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: GrantFiled: January 17, 2007Date of Patent: August 9, 2011Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Tové C. Bolken, Dennis E. Hruby, Thomas R. Bailey
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Publication number: 20110189122Abstract: The subject invention relates in part to the oral administration of ecdysteroids for controlling subterranean termites. Preferred ecdysteroids for use according to the subject invention are ecdysone, certain ecdysone analogs, and 20-hydroxyecdysone, for example. In some preferred embodiments, one or more of these compounds is used in a termite bait in combination with one or more chitin synthesis inhibitors. Thus, the subject invention also relates in part to controlling termites by the use of a chitin synthesis inhibitor (CSI), such as hexaflumuron and/or noviflumuron, together with an ecdysteroid (and analogs thereof) or molt-accelerating compound (MAC), such as halofenozide. The subject invention also relates to mixtures comprising these two active ingredients. The MAC/ecdysteroid analog induces a preliminary molting event in termite workers (they could not complete the molting), which then allows the CSI to further disrupt the molt and cause mortality.Type: ApplicationFiled: April 8, 2011Publication date: August 4, 2011Inventors: Nan-Yao SU, James Edward King, Paul Allen Neese
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Publication number: 20110189306Abstract: The present invention relates to therapeutic and/or prophylactic uses of hydrazide compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disease or disorder requiring modulation of vacuolar (H+)-ATPases.Type: ApplicationFiled: January 13, 2011Publication date: August 4, 2011Inventors: Norbert Kartner, Morris Frank Manolson
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Publication number: 20110183984Abstract: The present invention provides materials and methods for modulating an immune response. The materials and methods may be used to treat diseases associated with an aberrant immune response. In some embodiments, materials and methods of the invention may be used to treat autoimmune diseases, for example, rheumatoid arthritis.Type: ApplicationFiled: August 18, 2008Publication date: July 28, 2011Inventors: Jun Hayashi, Alexander Mackerell, Younus Mia, Guanjun Xia
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Publication number: 20110172303Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.Type: ApplicationFiled: July 22, 2009Publication date: July 14, 2011Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: Weiping Tang, James Elliot Bradner, Stuart L. Schreiber
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Publication number: 20110144189Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.Type: ApplicationFiled: December 7, 2010Publication date: June 16, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais SIELECKI-DZURDZ
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Patent number: 7960354Abstract: Synergistic pesticidal mixtures are provided.Type: GrantFiled: May 1, 2008Date of Patent: June 14, 2011Assignee: Dow AgroSciences LLCInventors: Jim X. Huang, Jonathan M. Babcock, Thomas Meade, Marc Farrow
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Publication number: 20110136878Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: Mitsui Chemicals Agro., Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20110124664Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: December 17, 2010Publication date: May 26, 2011Applicant: POLYMEDIX, INC.Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20110119775Abstract: The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more hydrazide-containing compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a hydrazide-containing compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a hydrazide-containing compound.Type: ApplicationFiled: January 21, 2011Publication date: May 19, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan Verkman, Nitin Dattatraya Sonawane, Chatchai Muanprasat
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Publication number: 20110086868Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Applicant: NOVA Southeastern UniversityInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Publication number: 20110059957Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 29, 2009Publication date: March 10, 2011Applicant: R-TECH UENO, LTD.Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
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Publication number: 20110060050Abstract: The present invention relates to a compound of the formula I, Ia and Ib, and its pharmaceutically usable tautomers, salts, stereoisomers and the enantiomers, including mixtures thereof in all ratios.Type: ApplicationFiled: February 17, 2009Publication date: March 10, 2011Applicant: Merck Patent GmbHInventors: Thomas Fuchss, Rolf Gericke, Norbert Beier, Florian Lang, Phillipp Lang, Karl Lang
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Publication number: 20110046101Abstract: The present invention relates to broad spectrum ?-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) ?-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I) wherein R1 is selected from R2 is selected from with certain provisos as herein defined; in combination with a pharmaceutically acceptable ?-lactam antibiotic in an amount which is effective for treating the bacterial infection.Type: ApplicationFiled: March 17, 2008Publication date: February 24, 2011Inventors: Gary I. Dmitrienko, Jarrod W. Johnson, Timothy R. Ramadhar, Thammaiah Viswanatha, Sundaramma Viswanatha
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Patent number: 7888332Abstract: The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more hydrazide-containing compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a hydrazide-containing compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a hydrazide-containing compound.Type: GrantFiled: July 18, 2008Date of Patent: February 15, 2011Assignee: The Regents of the University of CaliforniaInventors: Alan S. Verkman, Nitin D. Sonawane, Chatchai Muanprasat
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Publication number: 20110033393Abstract: The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.Type: ApplicationFiled: May 12, 2010Publication date: February 10, 2011Inventors: Philip STEIN, Robert DAINES, Dennis SPROUS, Harold O'GRADY
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Patent number: 7875603Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: GrantFiled: September 21, 2007Date of Patent: January 25, 2011Assignee: Nova Southeastern UniversityInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Patent number: 7858665Abstract: The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2??(I) wherein c0, b0 and k0 are 0 or 1; R is the radical of an analgesic drug for chronic pain, for instance neurophatic pain; R1c is H or alkyl with from 1 to 5 carbon atoms; B is such that its precursor is selected from amino acids, hydroxy acids, polyalcohol, compounds; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: June 2, 2009Date of Patent: December 28, 2010Assignee: Nicox S.A.Inventors: Ennio Ongini, Nicoletta Almirante, Piero Del Soldato
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Publication number: 20100303803Abstract: The invention relates to a multimeric, non-coding nucleic acid molecule for modulating the activity of the human or animal immune system, and to a production method therefor, and to a vaccine containing said multimeric, non-coding nucleic acid molecule. Said multimeric, non-coding nucleic acid molecules can be non-coding nucleic acid molecules that consist of at least two of said molecules (dimer) or assemblies of several non-coding nucleic acid molecules.Type: ApplicationFiled: November 7, 2008Publication date: December 2, 2010Applicant: Mologen AGInventors: Matthias Schroff, Burghardt Wittig, Manuel Schmidt, Janine Löhr, Christiane Kleuss
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Publication number: 20100298344Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: March 10, 2010Publication date: November 25, 2010Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20100292334Abstract: This invention relates to N-acylhydrazone derivatives, which are found to be useful as modulators of the nicotinic acetylcholine receptors. Due to their to pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: November 19, 2008Publication date: November 18, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Tino Dyhring
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Publication number: 20100286124Abstract: The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 9, 2010Publication date: November 11, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100284905Abstract: The application is based on the observation that tumor stem cell (TSC) replication involves a replicative intermediate configuration wherein a substantial fraction of the TSC genome is present as single-stranded DNA (ssDNA) when bell-shaped nuclei commence separation into two nuclei. During this replicative intermediate configuration large amounts of ssDNA are thus present in the nuclei of cells which the applicant proposes as target for anti-tumor therapy. A method of screening for anti-tumorigenic agents targeting ssDNA and use of such agents in therapy is claimed.Type: ApplicationFiled: June 12, 2008Publication date: November 11, 2010Inventors: Elena V. Gostjeva, William G. Thilly
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Publication number: 20100278912Abstract: The present invention provides a pharmaceutical composition for use in a dosage form for oral administration to a patient. The composition expands upon contact with gastric fluid and promotes retention of the dosage form in the patient's stomach for a prolonged period of time. The present invention further provides pharmaceutical dosage forms containing an active ingredient, and the pharmaceutical composition. The forms are adapted for immediate or controlled release of the active ingredient. The dosage forms may be used advantageously in the treatment of Parkinson's disease with levodopa and hyperactivity and attention deficit disorder with methylphenidate.Type: ApplicationFiled: December 4, 2007Publication date: November 4, 2010Inventors: Moshe Fleshner-Barak, E. Itzhak Lerner, Vered Rosenberger, Mazal Dahan, Yisrael Makov
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Patent number: 7795314Abstract: A method is described wherein semapimod is administered, or a salt thereof, or a combination of semapimod and a salt thereof, for the treatment of necrotizing enterocolitis.Type: GrantFiled: June 1, 2006Date of Patent: September 14, 2010Assignee: Cytokine PharmaSciences, Inc.Inventors: Ruben Zamora, Henri R. Ford, Thais Sielecki-Dzurdz, Vidal F. De La Cruz
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Publication number: 20100216852Abstract: The invention features compounds that have antibacterial activity, their use for the treatment of bacterial infections, screening methods that use whole animals or plant seedlings to identify compounds that inhibit a pathogen in the animal or plant, and screening methods to identify compounds that increase the lifespan of an organism.Type: ApplicationFiled: June 18, 2007Publication date: August 26, 2010Inventors: Frederick M. Ausubel, Kim Lewis, Terence I. Moy, Suresh Gopalan
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Patent number: 7776920Abstract: Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: January 18, 2007Date of Patent: August 17, 2010Assignee: Merck Patent GmbHInventors: Rolf Gericke, Markus Klein, Werner Mederski, Norbert Beier, Florian Lang
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Patent number: 7767716Abstract: Novel acyl hydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: March 10, 2006Date of Patent: August 3, 2010Assignee: Merck Patent GmbHInventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Markus Klein, Norbert Beier, Florian Lang
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Publication number: 20100183581Abstract: This invention provides conjugates of therapeutic or active agents with melanotransferrin or with other ligands of a melanotransferrin receptor, melanotransferrin receptor modulators, and related compositions and methods for modulating blood-brain barrier transport by providing methods of screening and selecting such conjugates, ligands, and modulators in vitro and in vivo, and methods of use of such conjugates, modulators and ligands in diagnosis and the treatment of diseases, including particularly diseases of the central nervous system or lysosomal storage diseases.Type: ApplicationFiled: January 7, 2010Publication date: July 22, 2010Applicant: RAPTOR PHARMACEUTICAL INC.Inventors: Richard Beliveau, Michel Demeule, Joseph Yang, Malcolm L. Kennard, Reinhard Gabathuler
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Publication number: 20100130450Abstract: Methods of identifying compounds that potentiate the activity of antifungal agents, potentiators identified by these methods, and methods of using potentiators are disclosed.Type: ApplicationFiled: May 5, 2008Publication date: May 27, 2010Applicant: NORTHEASTERN UNIVERSITYInventors: Kim Lewis, Michael David Lafleur
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Patent number: 7718702Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: August 15, 2005Date of Patent: May 18, 2010Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
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Patent number: 7705031Abstract: The present invention relates to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the R1, Z, Y, RA, and W groups of formula I are as defined herein. The invention also provides pharmaceutically acceptable compositions and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: November 1, 2007Date of Patent: April 27, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean M. Wilson, Andreas P. Termin, Jesus E. Gonzalez, III, Nicole Zimmermann, Yulian Zhang, Lev T. D. Fanning
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Publication number: 20100099683Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.Type: ApplicationFiled: October 9, 2009Publication date: April 22, 2010Inventors: Alan E. TOMKINSON, Xi CHEN, Barbara DZIEGIELEWSKA, Alexander D. MACKERELL, Shijun ZHONG, Gerald M. Wilson
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Patent number: 7691904Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: July 24, 2007Date of Patent: April 6, 2010Assignee: Auspex Pharmaceuticals, IncInventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
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Patent number: 7687545Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antinflammatory, antiarthritic and antiviral activity.Type: GrantFiled: June 19, 2008Date of Patent: March 30, 2010Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Gabriele Fontana
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Publication number: 20100075923Abstract: The present invention is directed to a method of enhancing TGF-? signaling in a subject comprising administering to said subject a clathrin-dependent endocytosis inhibitor in an amount sufficient to enhance TGF-? signaling. In another aspect, the invention is directed to a method of treating a condition associated with decreased TGF-? signaling in a patient in need thereof comprising administering to said patient a clathrin-dependent endocytosis inhibitor in a therapeutically effective amount.Type: ApplicationFiled: September 15, 2009Publication date: March 25, 2010Inventors: Jung San Huang, Shuan Shian Huang
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Publication number: 20100074927Abstract: Microparticle carriers, particularly protein-encapsulated microbubbles, are used to deliver antiproliferative drugs to target sites in a subject. In particular, antirestenotic drugs are delivered to areas of vascular injury for treatment or prevention of hyperproliferative disease, e.g. stenosis, in blood vessels; and antineoplastic drugs are targeted to tumor sites.Type: ApplicationFiled: September 17, 2009Publication date: March 25, 2010Inventors: Patrick L. Iversen, Nicholas Kipshidze
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Patent number: 7683097Abstract: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.Type: GrantFiled: May 25, 2005Date of Patent: March 23, 2010Assignee: Propharmacon Inc.Inventors: Martin A. Murphy, John Robert Schullek, John S. Ward, Gary C. Look, Brian Siesel
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Publication number: 20100068303Abstract: This invention relates to compositions and methods utilizing a chemotherapeutic drug and 6-bromoindirubin3?-oxime (BIO) for the treatment of cancer, including glioblastoma multiforme. The present invention demonstrates that BIO works synergistically with chemotherapeutic drugs to increase the cytotoxic effects of these drugs in glioma cells.Type: ApplicationFiled: February 25, 2008Publication date: March 18, 2010Applicant: CEDARS-SINAI MEDICAL CENTERInventor: John S. Yu
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Publication number: 20100068174Abstract: Disclosed herein are methods of treating an immunosensitive cancer with bis(thio-hydrazide amides) or pharmaceutically-acceptable salts thereof and an immunotherapy.Type: ApplicationFiled: August 20, 2007Publication date: March 18, 2010Inventor: Eric Jacobson
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Patent number: 7678832Abstract: Disclosed herein are compositions comprising a compound represented by structural formula (I): 2 g of which is reconstitutable in 10 mL of a water in less than 10 minutes, and methods for preparing these compositions. Also disclosed are compositions comprising a compound represented by structural formula (I) and a pharmaceutically acceptable excipient, wherein the molar ratio of said compound to said excipient is from 1:20 to 1:1, and methods for preparing these compositions.Type: GrantFiled: August 10, 2006Date of Patent: March 16, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Walter J. Lunsmann, Ninad Deshpanday
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Patent number: 7671092Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: January 18, 2008Date of Patent: March 2, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono