Chalcogen Or Nitrogen Bonded Directly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/398)
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Patent number: 8492387Abstract: The present invention is directed to 2-aminoimidazole 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: GrantFiled: February 18, 2009Date of Patent: July 23, 2013Assignee: Merck, Sharp & Dohme, Corp.Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
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Patent number: 8492488Abstract: Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.Type: GrantFiled: June 20, 2012Date of Patent: July 23, 2013Assignee: Nektar TherapeuticsInventors: Antoni Kozlowski, Samuel P. McManus
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Publication number: 20130177621Abstract: Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: January 9, 2013Publication date: July 11, 2013Inventor: North Carolina State University
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Publication number: 20130172352Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38?, and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: ApplicationFiled: February 25, 2013Publication date: July 4, 2013Applicant: NOVARTIS AGInventor: Novartis AG
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Patent number: 8476455Abstract: The invention relates to the compounds of formula (I): in which R1, R2, R3, R4, Q and Z are as defined in the specification. The invention also relates to the pharmaceutical compositions containing these compounds.Type: GrantFiled: December 15, 2004Date of Patent: July 2, 2013Assignee: Laboratoire TheramexInventors: Jean Lafay, Benoit Rondot, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti, Francois Puccio, Christian Blot, Philippe Maillos
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Publication number: 20130158090Abstract: A compound of formula (I): is described, as well as enantiomers, pharmaceutically acceptable salts thereof, for its use as a medicament.Type: ApplicationFiled: June 29, 2011Publication date: June 20, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Jean-Guy Boiteau, Jean-Michel Linget
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Publication number: 20130156816Abstract: The invention features compositions, methods, and kits for the administration of an oxidatively transformed carotenoid, or a fractionated component thereof, for use in aquaculture.Type: ApplicationFiled: February 18, 2011Publication date: June 20, 2013Applicant: Chemaphor Inc.Inventors: Larry Arthur Stobbs, James Gary Nickerson, Clayton Paul Dick
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Publication number: 20130144264Abstract: Bioactive, hydroforming luminal liner compositions are formed of high molecular weight crystalline, absorbable copolyesters dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: ApplicationFiled: January 30, 2013Publication date: June 6, 2013Inventors: Shalaby W. Shalaby, Kenneth David Gray, Georgios T. Hilas
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Patent number: 8455530Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: GrantFiled: March 2, 2012Date of Patent: June 4, 2013Assignee: Theravance, Inc.Inventors: Robert S. Chao, Weijiang Zhang
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Patent number: 8455481Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish fanning and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.Type: GrantFiled: September 14, 2012Date of Patent: June 4, 2013Assignee: Bayer CropScience AGInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Patent number: 8450356Abstract: To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound. The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.Type: GrantFiled: January 31, 2012Date of Patent: May 28, 2013Assignee: Pola Pharma Inc.Inventors: Yasushi Murakami, Naoko Kobayashi, Azuma Nishio, Nobuo Kubota
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Publication number: 20130123287Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Hiroyuki Hayashi
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Patent number: 8436035Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase (CYP11B2), and/or 11 beta-hydroxylase (CYP11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYP11B1. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.Type: GrantFiled: December 14, 2007Date of Patent: May 7, 2013Assignee: Novartis AGInventors: Christopher Adams, Qi-Ying Hu, Gary Michael Ksander, Julien Papillon
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Patent number: 8436027Abstract: This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. This invention also refers to a pharmaceutical composition comprising at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to methods of treatment or inhibition of tuberculosis and leishmaniasis.Type: GrantFiled: December 29, 2010Date of Patent: May 7, 2013Assignee: Fundacão Oswaldo Cruz—FIOCRUZInventors: Nubia Boechat, Marilia dos Santos Costa, Maria Cristina da Silva Lourenço, Ivan Neves, Jr., Marcelo da Silva Genestra, Vitor Francisco Ferreira
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Patent number: 8426458Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 17, 2010Date of Patent: April 23, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Datong Tang
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Publication number: 20130096162Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 3, 2012Publication date: April 18, 2013Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 8420686Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 17, 2010Date of Patent: April 16, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
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Patent number: 8420687Abstract: To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound. The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.Type: GrantFiled: January 31, 2012Date of Patent: April 16, 2013Assignee: Pola Pharma Inc.Inventors: Yasushi Murakami, Naoko Kobayashi, Azuma Nishio, Nobuo Kubota
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Patent number: 8410150Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 6, 2008Date of Patent: April 2, 2013Assignee: University Health NetworkInventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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Patent number: 8410156Abstract: Compositions comprising ergothioneine and a trimethylamine absorber are provided. Also provided are methods for preventing, reducing or minimizing the fishy, amine odor, due to trimethylamine, that is associated with the processing and/or storage of a preparation containing ergothioneine, by combining with the ergothioneine, during processing or prior to storage, a trimethylamine absorber in an amount sufficient to prevent the detection of any trimethylamine odor by the human nose. A method is further provided for ameliorating the methylamine odor associated with an aqueous ergothioneine-containing preparation after it has developed a fishy trimethylamine odor.Type: GrantFiled: January 30, 2009Date of Patent: April 2, 2013Assignee: ELC Management, LLCInventor: Daniel B. Yarosh
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Patent number: 8399463Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: GrantFiled: September 19, 2011Date of Patent: March 19, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 8399501Abstract: The invention provides a micronized 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid having improved stability. The invention also provides pharmaceutical compositions comprising the stable micronized compound, processes for preparing the stable micronized compound, and methods of using the stable micronized compound to treat diseases such as hypertension.Type: GrantFiled: March 3, 2011Date of Patent: March 19, 2013Assignee: Theravance, Inc.Inventor: Paul R. Fatheree
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Publication number: 20130064772Abstract: Provided are wound caring compositions and devices containing a pH-sensitive, preferably acid degradable, components contained in a water-permeable and hydronium ion permeable material. The pH-sensitive component encloses an antibiotic which is released to the wound upon infection by a microorganism at the wound site, and/or encloses a pH indicator. The antibiotic release is triggered by the microorganism's production of CO2 at the wound site which forms carbonic acid, lowers the pH at the pH sensitive components, and thus results in rupture of the liposome.Type: ApplicationFiled: September 7, 2012Publication date: March 14, 2013Inventors: Gerald F. Swiss, Stefan Schwabe, Robert M. Moriarty
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Patent number: 8394788Abstract: Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein.Type: GrantFiled: November 16, 2007Date of Patent: March 12, 2013Assignee: The Regents of the University of CaliforniaInventors: Alan S. Verkman, Marc Harris Levin
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Publication number: 20130059856Abstract: Chemical compounds which act as agonists of, or otherwise modulate the activity of, GPR131 are disclosed. Related compositions, formulations and methods of use are also described.Type: ApplicationFiled: June 13, 2012Publication date: March 7, 2013Inventors: Aaron Robert Novack, Dong-Fang Shi, Jingyuan Ma, Imad Nashashibi, Phuongly Pham, Jiangao Song, David W. G. Wone, Xueyan Wang, Jeffrey D. Johnson, Brian Edward Lavan, Charles A. McWherter, Xin Chen
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Publication number: 20130053353Abstract: The present disclosure relates generally to compositions for cosmetic or pharmaceutical application. The compositions include a carrier and rheology modulators.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Applicant: FOAMIX LTD.Inventors: Dov Tamarkin, Elana Gazal, Yohan Hazot, David Schuz
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Patent number: 8372807Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: May 20, 2010Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet, Karen Watson
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Patent number: 8362060Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.Type: GrantFiled: November 9, 2011Date of Patent: January 29, 2013Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Venkat R. Thalladi
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Patent number: 8362061Abstract: The invention relates to methods for detecting the presence of a compound of formula I in a biological test sample: where R2, R3, and R4 are as defined in the specification; or a salt thereof.Type: GrantFiled: June 27, 2012Date of Patent: January 29, 2013Assignee: Theravance, Inc.Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhou
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Publication number: 20130022661Abstract: A bio-remodable augmentation device including an implantable member configured for maintaining space in a bone defect. The implantable member is formed from a bio-remodable composite having structural properties so as to aid in the generation of new bone tissue and eventually be reabsorbed in the newly formed bone tissue. This structural and bio-remodable implant reduces, if not eliminates, the need to remove the implantable member from the patient once new bone tissue is formed. A kit including the implantable devices and bone growth material is disclosed. Methods of use are also disclosed.Type: ApplicationFiled: July 21, 2011Publication date: January 24, 2013Applicant: Warsaw Orthopedic, Inc.Inventor: William F. McKay
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Publication number: 20130012497Abstract: The invention provides methods of determining an altered susceptibility to develop ADHD, methods of predicting or determining the severity of symptoms of ADHD and associated disorders, and methods of treatment based on the presence or absence of one or more alleles of single nucleotide polymorphism (SNP) markers.Type: ApplicationFiled: May 18, 2012Publication date: January 10, 2013Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Ser.Inventors: Maximilian Muenke, Mauricio Arcos-Burgos, Maria Teresa Acosta
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Publication number: 20130012552Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more azole fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.Type: ApplicationFiled: March 2, 2011Publication date: January 10, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
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Publication number: 20130012558Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish fanning and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Bayer Intellectual Property GmbHInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20130005787Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.Type: ApplicationFiled: June 28, 2012Publication date: January 3, 2013Applicant: Medicis Pharmaceutical CorporationInventors: Michael T. NORDSIEK, Kodumudi S. BALAJI
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Patent number: 8344012Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: September 4, 2009Date of Patent: January 1, 2013Assignee: Ardea Biosciences, Inc.Inventors: Esmir Gunic, Jean-Luc Girardet, David A. Paisner
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Patent number: 8344013Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: March 6, 2012Date of Patent: January 1, 2013Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20120316211Abstract: Provided herein are methods of detecting evidence of Chagas disease in a biological sample, comprising the step of measuring the presence of at least one protein selected from the group consisting of gelsolin, myosin light chain 2, vimentin, myosin heavy chain 11, vinculin, and plasminogen in said sample, wherein significantly elevated levels of the protein is a biomarker for the presence or severity of Chagas disease.Type: ApplicationFiled: May 11, 2012Publication date: December 13, 2012Applicant: The Board or Regents of the University of Texas SystemInventor: Nisha Jain Garg
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Patent number: 8329738Abstract: The invention relates to the use of imidazole derivatives of the formula (1): in which A, R?1, R?2 and R?3 are as defined in the description, as AMPK activators. The invention also relates to processes for the preparation of the said compounds, to their uses for the preparation of medicaments for the treatment of insulin resistance, diabetes and related pathologies, and also obesity, and to the pharmaceutical compositions comprising them. Certain compounds of the formula (1) are novel and, in this respect, also form part of the invention.Type: GrantFiled: June 12, 2007Date of Patent: December 11, 2012Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Gerard Moinet, Dominique Marais, Sophie Hallakou-Bozec, Christine Charon
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Publication number: 20120308516Abstract: Metallocene compounds and pharmaceutical compositions containing these metallocene compounds are disclosed and described. Methods of treating cancer employing such metallocene compounds and pharmaceutical compositions also are provided.Type: ApplicationFiled: June 5, 2012Publication date: December 6, 2012Applicant: CHEVRON PHILLIPS CHEMICAL COMPANY LPInventors: MARK L. HLAVINKA, QING YANG, MANDI MICHELLE MURPH
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Publication number: 20120309805Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: ApplicationFiled: March 2, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Robert S. Chao, Weijiang Zhang
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Publication number: 20120302561Abstract: The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided.Type: ApplicationFiled: April 27, 2012Publication date: November 29, 2012Applicants: THE PENN STATE RESEARCH FOUNDATION, THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David A. Antonetti, Paul Titchenell
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Publication number: 20120295881Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: July 11, 2012Publication date: November 22, 2012Applicant: Abbott GmbH & Co. KGInventors: Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Frauke Pohlki, Charles W. Hutchins
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Publication number: 20120295910Abstract: The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: August 1, 2012Publication date: November 22, 2012Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
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Publication number: 20120289510Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: May 7, 2012Publication date: November 15, 2012Applicants: AstraZeneca AB, Bayer Pharma AGInventors: Markus Berger, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schäcke
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Patent number: 8309554Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: May 14, 2009Date of Patent: November 13, 2012Assignee: Threshold PharmaceuticalsInventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
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Publication number: 20120283303Abstract: The present invention relates to the use of N-aminoimidazole or N-aminoimidazole thione derivatives as cytoprotective compounds in vitro and in vivo and for the treatment or prevention of cell death mediated disorders and/or GSK-3 mediated disorders or processes.Type: ApplicationFiled: April 30, 2012Publication date: November 8, 2012Applicant: K.U.LEUVEN RESEARCH AND DEVELOPMENTInventors: Christophe Pannecouque, Wim Robberecht, Miguel Stevens
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Publication number: 20120276059Abstract: Clostridium difficile disease involves a range of clinical presentations ranging from mild to self-limiting diarrhea to life-threatening pseudomembranous colitis and megacolon. Cases of C. difficile are treated differently depending on severity of disease. Mild and moderate cases may be treated with metronidazole while moderate-to-severe and relapsing cases are often treated with vancomycin or fidaxomicin. The presence of C. difficile disease is detected using a biomarker panel that includes C. difficile antigen (GDH), toxins A and B, and fecal lactoferrin. In patients suspected of C. difficile disease, if GDH is detected indicating the presence of C. difficile, and then toxins A and/or B are detected to indicate toxigenic C. difficile and support a diagnosis of C. difficile-associated disease, fecal lactoferrin concentrations are measured to determine severity of the disease by indicating the amount of intestinal inflammation.Type: ApplicationFiled: April 26, 2012Publication date: November 1, 2012Applicant: TECHLAB, INC.Inventors: JAMES HUNTER BOONE, DAVID M. LYERLY, TRACY D. WILKINS, ROBERT J. CARMAN
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Publication number: 20120276060Abstract: Clostridium difficile disease involves a range of clinical presentations ranging from mild to self-limiting diarrhea to life-threatening pseudomembranous colitis and megacolon. Cases of C. difficile are treated differently depending on severity of disease. Mild and moderate cases may be treated with metronidazole while moderate-to-severe and relapsing cases are often treated with vancomycin or fidaxomicin. The presence of C. difficile disease is detected using a biomarker panel that includes C. difficile antigen (GDH), toxins A and B, and fecal lactoferrin. In patients suspected of C. difficile disease, if GDH is detected indicating the presence of C. difficile, and then toxins A and/or B are detected to indicate toxigenic C. difficile and support a diagnosis of C. difficile-associated disease, fecal lactoferrin concentrations are measured to determine severity of the disease by indicating the amount of intestinal inflammation.Type: ApplicationFiled: April 26, 2012Publication date: November 1, 2012Applicant: TECHLAB, INC.Inventors: JAMES HUNTER BOONE, DAVID M. LYERLY, TRACY D. WILKINS, ROBERT J. CARMAN
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Publication number: 20120269881Abstract: A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.Type: ApplicationFiled: December 29, 2010Publication date: October 25, 2012Inventors: David Kanios, Juan A. Mantelle, Viet Nguyen
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Publication number: 20120264796Abstract: This disclosure described the role of AMPK in circadian rhythms and methods of screening for agents that modulate such rhythms, compositions that are useful for modulating such rhythms and uses thereof.Type: ApplicationFiled: March 22, 2010Publication date: October 18, 2012Inventors: Ronald Evans, Katja A. Lamia, Reuben J. Shaw, Luciano Ditacchio, Satchidananda Panda