Plural Six-membered Hetero Rings Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/332)
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Patent number: 8202889Abstract: The present invention relates to methods of inhibiting bacterial IMPDH comprising administering compounds of formula I: or pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infections.Type: GrantFiled: September 8, 2006Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, Trudy Grossman, Emanuele Perola
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Patent number: 8198275Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: March 30, 2011Date of Patent: June 12, 2012Assignee: H. Lundbeck A/SInventors: Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
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Publication number: 20120134987Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: December 15, 2011Publication date: May 31, 2012Inventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
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Publication number: 20120135002Abstract: The present invention relates to a pharmaceutical composition comprising: a) at least one iron uptake inhibitor, and b) at least one vitamin D and/or at least one analog thereof and/or at least one vitamin D receptor modulator, and optionally a pharmaceutically acceptable carrier.Type: ApplicationFiled: July 16, 2009Publication date: May 31, 2012Inventors: Ivan Cruz Moura, Olivier Hermine, Celine Callens, Severine Coulon
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Patent number: 8188291Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: June 17, 2009Date of Patent: May 29, 2012Assignee: Sanofi-AventisInventors: Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
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Publication number: 20120130144Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.Type: ApplicationFiled: February 4, 2010Publication date: May 24, 2012Applicant: BiPar Sciences, Inc.Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
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Patent number: 8183261Abstract: Disclosed is a microorganism control agent containing not less than 1% by weight but less than 10% by weight of N,N?-hexamethylenebis(4-carbamoyl-1-decylpyridinium bromide), not less than 35% by weight but less than 60% by weight of at least one alcohol having 2 or 3 carbon atoms, water and an acid.Type: GrantFiled: November 13, 2007Date of Patent: May 22, 2012Assignee: Japan Envirochemicals, Ltd.Inventor: Masaaki Nakabayashi
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Publication number: 20120122878Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.Type: ApplicationFiled: June 30, 2008Publication date: May 17, 2012Inventors: Baltazar Gomez-Mancilla, Fabrizio Gasparini
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Publication number: 20120115827Abstract: The present invention relates to a novel 3-aminobenzamide, compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide, compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathicpain, rheumatoid arthritis pain, and neuralgia.Type: ApplicationFiled: June 7, 2011Publication date: May 10, 2012Applicant: Japan Tobacco Inc.Inventors: Yoshihisa Koga, Shinji Yata, Takashi Watanabe, Takuya Matsuo, Masahiro Sakata, Wataru Kondo
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Publication number: 20120115909Abstract: The presently described subject matter relates to new derivatives of tazarotene that also exhibit retinoid activity, pharmaceutical compositions comprising the derivatives, method of treating skin disorders with the pharmaceutical compositions, and process of making the derivatives.Type: ApplicationFiled: July 16, 2010Publication date: May 10, 2012Inventors: Xue Ge, Hansen Wong, Wendy Huang Chern, Hans Hofland, Michael J. Bishop, Xin Frank Cai, Alan Colborn
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Publication number: 20120095051Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.Type: ApplicationFiled: May 14, 2010Publication date: April 19, 2012Inventors: Francis Johnson, Lorne Golub
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Publication number: 20120094964Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.Type: ApplicationFiled: May 6, 2010Publication date: April 19, 2012Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
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Publication number: 20120093759Abstract: Medical devices, wound dressings, and methods of dressing wounds are described. Devices and methods using silicone and pharmaceutically active agents are described. Devices including covers and bases are described.Type: ApplicationFiled: November 17, 2011Publication date: April 19, 2012Inventor: David J. Vachon
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Publication number: 20120094986Abstract: The invention relates to nicotinamide derivatives which can be used as anticancer drugs.Type: ApplicationFiled: March 22, 2010Publication date: April 19, 2012Applicant: SANOFI-AVENTISInventors: Jérôme Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Sandrine Hilairet, Samir Jegham
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Publication number: 20120094980Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
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Patent number: 8158654Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: May 19, 2009Date of Patent: April 17, 2012Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20120083443Abstract: The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCS treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCS. Likewise, RBCS of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCS. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release RBCS. Thus the invention is directed to compositions and methods for improving ATP release by RBCS, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.Type: ApplicationFiled: November 22, 2011Publication date: April 5, 2012Applicant: SAINT LOUIS UNIVERSITYInventors: Randy S. Sprague, Madelyn Stumpf
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Publication number: 20120083489Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.Type: ApplicationFiled: June 2, 2010Publication date: April 5, 2012Inventors: Siegfried Benjamin Christensen IV, Donghui Qin, Shenglin Chen, Xing Huang, Di Li, Fei Li, Lei Li, Xiaojuan Lin, Shi Lu, Zhen Lu, Maoyun Lv, Chuanning Wang, Chengde Wu, Mei Xiao, Haiyu Yu, Weina Zhang, Zhiliu Zhang
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Patent number: 8148535Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: October 17, 2006Date of Patent: April 3, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott Wolkenberg, M. Brad Nolt, Peter Manley, Nathan R. Kett, Mark T. Bilodeau
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Patent number: 8143288Abstract: Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.Type: GrantFiled: June 5, 2006Date of Patent: March 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Michael Serrano-Wu, Makonen Belema, Lawrence B. Snyder, Nicholas A. Meanwell, Denis R. St. Laurent, Ramesh Kakarla, Van N. Nguyen, Yuping Qiu, Xuejie Yang, John E. Leet, Min Gao, Donald R. O'Boyle, II, Julie A. Lemm, Fukang Yang
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Publication number: 20120071539Abstract: Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic compositions comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.Type: ApplicationFiled: December 12, 2007Publication date: March 22, 2012Applicant: Emory UniversityInventor: Peng Jin
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Publication number: 20120070510Abstract: Aqueous wound and mucous membrane disinfectant containing a) octenidine dihydrochloride, and b) one or more active ingredients selected from the group ethanol, 1-propanol, 2-propanol, undecylene amidopropyl trimonium methosulfate, 3-(4-chlorophenoxy)-1,2-propanediol and/or sodium hydroxymethylglycinate and c) glycerin and/or 1,2-diols having 3 to 10 carbon atoms, and d) optionally surfactants, emulsifiers, solubilisers, pH regulators, dyestuffs, perfumes and/or thickeners, the agent being free of phenoxyethanol, phenoxypropanol, phenoxyisopropanol and organic acids.Type: ApplicationFiled: September 20, 2011Publication date: March 22, 2012Inventors: BARBARA KRUG, Sven Dabek, Kai-Martin Mueller, Marco Rudolf, Hanns Pietsch, Hiltraut Pietsch, Christiane Ostermeyer
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Publication number: 20120064121Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Shoujun Chen
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Publication number: 20120065185Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.Type: ApplicationFiled: November 15, 2011Publication date: March 15, 2012Applicant: Amgen Inc.Inventors: Guoqing CHEN, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
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Publication number: 20120053170Abstract: The present invention relates to nicotinamide derivatives of formula (I), to compositions containing same, and to the therapeutic use thereof, in particular as anticancer drugs. The invention also relates to the method for preparing said compounds, as well as to some of the intermediate products.Type: ApplicationFiled: March 22, 2010Publication date: March 1, 2012Applicant: SANOFIInventors: Jérome Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Sandrine Hilairet, Samir Jegham
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Publication number: 20120053209Abstract: The invention relates to nicotinamide derivatives that can be used as anticancer drugs.Type: ApplicationFiled: March 18, 2010Publication date: March 1, 2012Applicant: SANOFIInventors: Jerome Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Samir Jegham, Sandrine Hilairet
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Publication number: 20120039805Abstract: The invention provides diagnostic and therapeutic methods for neoplastic disease patients with neoplasms of for example, the breast, skin, kidney, lung, pancreas, rectum and colon, prostate, bladder, epithelial, non-epithelial; lymphomas, sarcomas, melanomas, and the like, comprising determining the level of caveolin-1 and/or caveolin-2 in stromal cells adjacent to a neoplasm.Type: ApplicationFiled: February 19, 2010Publication date: February 16, 2012Inventors: Michael P. Lisanti, Federica Sotgia, Richard G. Pestell
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Patent number: 8114884Abstract: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis.Type: GrantFiled: January 9, 2006Date of Patent: February 14, 2012Assignee: Emory UniversityInventors: Hyunsuk Shim, Dennis C. Liotta, James P. Snyder, Weiqiang Zhan, Zhongxing Liang
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Patent number: 8114895Abstract: The present invention relates to an isolated bioactive molecule Caerulomycin A, derivatives and analogs thereof as effective immunosuppressive agents. The immunosuppressive property of the compound is targeted in particular against the lymphocytes, CD4+ T cells, CD8+ T cells and B cells and in the production of IL-4 and IFN-? and antibodies. The compound operates through a mechanism by downregulating the expression of activation marker CD28 and upregulating the immunosuppressive marker CTLA-4. Caerulomycin A has previously been isolated from Streptomyces caeruleus and found to have useful antifungal activity. Prior to the present invention however, this compound had not been determined to have immunomodulatory activity.Type: GrantFiled: September 12, 2006Date of Patent: February 14, 2012Assignee: Council of Science and Industrial ResearchInventors: Arvind Kumar Singla, Javed Naim Agrewala, Rakesh Mulraj Vohra, Ravinder Singh Jolly
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Patent number: 8101636Abstract: Novel aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. Also described are processes for synthesizing the compounds.Type: GrantFiled: May 17, 2006Date of Patent: January 24, 2012Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: Richard R. Tidwell, David W. Boykin, W. David Wilson, Reto Brun, Karl Werbovetz, Mohamed A. Ismail, Reem K. Arafa
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Publication number: 20120015961Abstract: The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-?proteins.Type: ApplicationFiled: March 29, 2010Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Yuusuke Tamura, Shinji Suzuki, Sae Matsumoto, Akihiro Hori, Yuuji Kooriyama
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Patent number: 8093385Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.Type: GrantFiled: July 28, 2008Date of Patent: January 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Romyr Dominique, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri
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Patent number: 8093395Abstract: An object of the invention is to provide a novel sphingosine compound with an inhibitory activity against sphingomyelinase, and a method for producing the sphingosine compound. The novel sphingosine compound or a salt thereof according to the invention is represented by Formula (1): wherein one of R1 and R2 is hydrogen, and the other is a group represented by Formula (G): wherein n is 0 or 1; and R3 is hydrogen, C1-23 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C3-8 cycloalkyloxy, phenyl, or furil.Type: GrantFiled: March 5, 2008Date of Patent: January 10, 2012Assignee: Otsuka Chemical Co., Ltd.Inventors: Mugio Nishizawa, Hiroshi Imagawa, Jun Sakurai, Masataka Oda
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Patent number: 8093241Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.Type: GrantFiled: December 17, 2009Date of Patent: January 10, 2012Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Yuji Nakamura, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
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Publication number: 20120004593Abstract: An antimicrobially effective composition includes a) at least 0.15% by weight of bispyridinium alkane, b) at least 3.5% by weight of humectant and c) water. Upon dilution with water, the composition produces a solution with an osmolality of from 230 to 350 mOsmol/kg and is free from surfactant. It is used as an antiseptic and is suitable for use in a method for the disinfection of injured or uninjured skin of a human being or animal, preference being given to use in the case of newborns, in particular those born prematurely.Type: ApplicationFiled: June 9, 2011Publication date: January 5, 2012Applicant: L'AIR LIQUIDE, SOCIETE ANONYME POUR L'ETUDE ET L'EXPLOITATION DES PROCEDES GEORGEInventors: Andreas DETTMANN, Sabine BEHRENDS, Mona GOLOMBIEWSKI, Elke KASSENS
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Patent number: 8088385Abstract: A methods and compounds for inhibiting 6-phosphofructo-2-kinase /fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.Type: GrantFiled: June 18, 2008Date of Patent: January 3, 2012Assignee: University of Louisville Research Foundation Inc.Inventors: Jason Chesney, John O. Trent, Sucheta Telang, Brian Clem, Jason Meier
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Patent number: 8084470Abstract: Substituted nicotinamide compounds corresponding to formula I a process for their preparation, pharmaceutical compositions containing these compounds, and the use thereof for the treatment or inhibition conditions such as pain, epilepsy, migraine, anxiety states, or urinary incontinence.Type: GrantFiled: September 17, 2008Date of Patent: December 27, 2011Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Sven Kuehnert, Robert Frank, Dagmar Kaulartz, Wolfgang Schroeder, Gregor Bahrenberg, Klaus Schiene
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Publication number: 20110312974Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Nicholas Simone Stock, Yen Pham Truong, Jeffrey Roger Roppe, Deborah Volkots, Jill Melissa Scott, Timothy Andrew Parr, Bowei Wang, Thomas Jon Seiders, Ryan Clark, Heather Renee Coate
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Publication number: 20110312875Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: December 22, 2011Applicant: UNIVERSITY OF WOLLONGONGInventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
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Publication number: 20110313000Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20110305729Abstract: Compounds of the invention are of the formula (I); wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: ApplicationFiled: January 26, 2010Publication date: December 15, 2011Inventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi
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Publication number: 20110306597Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 12, 2009Publication date: December 15, 2011Inventors: James Michael Crawforth, Paul Alan Glossop, Bruce Cameron Hamper, Wei Huang, Bradley Elwood Neal, Simon John Mantell, Kirk Olson, Atli Thorarensen, Steve Ronald Turner
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Publication number: 20110300234Abstract: Methods of treating tumor cells in an individual comprise administering to the individual a drug having anti-tumor effect, wherein the drug is delivered into the tumor cells via Right-Handed Coiled-Coil (RHCC) protein or a fragment or variant thereof. The drug may, for example, be a metal-containing compound, a protein or peptide drug, and/or an organic hydrophobic compound.Type: ApplicationFiled: November 11, 2009Publication date: December 8, 2011Inventors: Jürgen Müller, Egbert Figgemeier
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Patent number: 8071616Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.Type: GrantFiled: January 25, 2010Date of Patent: December 6, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, William J. Scott, Bernd Riedl
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Patent number: 8071626Abstract: This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid supports conjugated with said chelates, chelating agents or labeled biomolecules. Especially the invention relates to novel chelating agents useful in solid phase synthesis of oligonucleotides or oligopeptides and the oligonucleotides and oligopeptides so obtained.Type: GrantFiled: December 17, 2007Date of Patent: December 6, 2011Assignee: Wallac OyInventors: Jari Hovinen, Veli-Matti Mukkala, Harri Hakala, Jari Peuralahti
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Patent number: 8067440Abstract: There are provided compounds of formulas (VA), (VIA), (VIIA) (IXA), (XIA), (XIIA), (XIIIA), and (XIVA): wherein A, Z, R2, X?, and L2 represent various different possibilities. Methods for using such compounds are also provided.Type: GrantFiled: December 21, 2010Date of Patent: November 29, 2011Assignee: Valorisation-Recherche, Limited PartnershipInventors: Andre Charette, Jean-Christophe Poupon, Alessandro Boezio
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Publication number: 20110288129Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: July 8, 2011Publication date: November 24, 2011Applicant: ABBOTT LABORATORIESInventors: Anil Vasudevan, Brian S. Brown, Jerome F. Daanen, Arthur R. Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark A. Matulenko
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Patent number: 8063072Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: September 21, 2010Date of Patent: November 22, 2011Assignee: Roche Palo Alto LLCInventors: Jim Li, Javier de Vincente Fidalgo, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Publication number: 20110275674Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis