Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 549/436)
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Publication number: 20150099636Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: October 9, 2014Publication date: April 9, 2015Inventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20150093339Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventors: Catherine TACHDJIAN, Andrew P. PATRON, Sara L. ADAMSKI-WERNER, Farid BAKIR, Qing CHEN, Vincent DARMOHUSODO, Stephen Terrence HOBSON, Xiaodong LI, Ming QI, Daniel H. ROGERS, Marketa RINNOVA, Guy SERVANT, Xiao-Qing TANG, Mark ZOLLER, David WALLACE, Amy XING, Klaus GUBERNATOR
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Patent number: 8921413Abstract: The present invention discloses ?-diketones, ?-diketones or ?-hydroxyketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: GrantFiled: November 21, 2013Date of Patent: December 30, 2014Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Publication number: 20140371445Abstract: The present invention relates to a quinic acid derivative, preparation process of the same and pharmaceutical uses thereof. The quinic acid derivative has a quinic acid-like structure which binds to CD28, blocks T-cell signal 2 pathway via CD28, and suppresses T-cell activation. The C-1 carboxyl group, the C-3 hydroxyl group and the C-4 hydroxyl group of quinic acid are modified to attenuate the cytotoxicity of the quinic acid derivative. The preparation process of the quinic acid derivative comprises 2 steps of: treating quinic acid with the first reagent in the presence of the acid catalyst to form an immediate; and treating the immediate with the second reagent to from the quinic acid derivative. With the ability to suppress T-cell activation, the quinic acid derivative is used to treats an autoimmune disease, an allergy, transplant rejection or other related immune disorder.Type: ApplicationFiled: June 13, 2013Publication date: December 18, 2014Inventors: HUEIH-MIN CHEN, CHUNG-MING SUN, CHIH-YU HUANG
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Patent number: 8889678Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: GrantFiled: July 19, 2010Date of Patent: November 18, 2014Assignees: Centre National de la Recherche Scientifique, Universite de StrasbourgInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Publication number: 20140336387Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Applicant: CONCERT PHARMACEUTICALS, INC.Inventors: Andrew D. Jones, Robert E. Zelle, I. Robert Silverman
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Publication number: 20140243349Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Patent number: 8816102Abstract: A method of modulating the flavor of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavor-modulating proportion of at least one compound of the formula I in which X is selected from CHOH, C?O, CH2—CO and CH?C(OH), Y is selected from C1-C7 linear and branched alkyl and CH2CH2OH, Z is selected from CH3 and a moiety of the formula II in which the wavy bond represents bond linking Z to X and R1 and R2 are selected from the possibilities (i) both hydrogen; (ii) independently OH and OCH3; and (iii) R1 and R2 together with their bonds to the phenyl ring form a ring of the formula —O—CH2—O—; such that, when Z is CH3, X is C?O and Y is CH2CH2OH.Type: GrantFiled: June 24, 2010Date of Patent: August 26, 2014Assignee: Givaudan S.A.Inventors: Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
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Patent number: 8716333Abstract: The present application relates to processes for the preparation of intermediates useful in the manufacture of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate and compounds and oseltamivir analogs and to pharmaceutical compositions comprising said analog compounds. The application further relates to a method of using the novel analogs of oseltamivir to treat or prevent influenza.Type: GrantFiled: October 15, 2010Date of Patent: May 6, 2014Assignee: Brock UniversityInventors: Tomas Hudlicky, Lukas Werner, Ales Machara
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Patent number: 8680100Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Patent number: 8664410Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.Type: GrantFiled: June 24, 2011Date of Patent: March 4, 2014Assignee: Universitat PotsdamInventors: Pablo Wessig, Kristian Möllnitz, Robert Wawrzinek
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Publication number: 20140039182Abstract: The present invention relates to compositions, for example, the DBU/Hexafluoroacetone hydrate salt, and processes of preparing and using the same for the modification of chemical compounds via the release of trifluoroacetate. The DBU/Hexafluoroacetone hydrate salt can perform trifluoromethylation reactions on chemical compounds, such as carbonyl group-containing compounds.Type: ApplicationFiled: March 22, 2012Publication date: February 6, 2014Inventors: David A. Colby, Mark V. Riofski, Changho Han
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Patent number: 8637702Abstract: Compound selected from 4-(2(S)-benzoylamino-3-naphthalen-2-yl-propionylamino)-N-hydroxy-benzamide and benzo[1,3]dioxole-5-carboxylic acid [1(S)-(4-hydroxycarbamoyl-phenylcarbamoyl)-2-naphthalen-2-yl-ethyl]-amide, for use in the treatment of a HIV infection. The compound is administered in combination and/or in temporal proximity with at least one anti-retroviral agent.Type: GrantFiled: September 14, 2010Date of Patent: January 28, 2014Assignee: Italfarmaco S.p.A.Inventors: Charles Dinarello, Gianluca Fossati, Paolo Mascagni
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Patent number: 8618335Abstract: An object of the present invention is to provide an industrially advantageous process for preparing a benzaldehyde compound from a benzyl alcohol compound with high yield. The present invention relates to a process for preparing an aromatic aldehyde compound represented by the formula (2); which comprises reacting an aromatic methyl alcohol compound represented by the formula (1); and a peroxide under a pH value of a reaction solution being pH 0.01 or higher and less than 10 in the presence of at least one metallic compound selected from a molybdenum compound and a tungsten compound, a quaternary ammonium salt and an organic phosphonium salt.Type: GrantFiled: October 6, 2009Date of Patent: December 31, 2013Assignee: Ube Industries Ltd.Inventors: Takashi Doi, Yoshihiro Yoshida, Shinji Yasuda, Yoshiyuki Watanabe, Satoru Fujitsu, Daisuke Douyama
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Publication number: 20130338095Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: December 19, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
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Patent number: 8609717Abstract: The present invention discloses ?-diketones, ?-diketones or ?-hydroxyketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: GrantFiled: August 17, 2011Date of Patent: December 17, 2013Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Publication number: 20130331390Abstract: Nitrogen-containing biphenyl compounds as represented by formula (I), pharmaceutically acceptable salts or derivatives thereof, pharmaceutical compositions, and preparation methods therefore, and anti-HIV-1 use of the compound. Each substituent group in formula (I) is as defined in the description.Type: ApplicationFiled: October 13, 2011Publication date: December 12, 2013Applicants: Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming Institute of Zoology, The Chinese Academy of Sciences, Yunnan UniversityInventors: Jingping Liu, Handong Sun, Hongbin Zhang, Yongtong Zheng, Weilie Xiao, Jianxin Pu, Ruirui Wang, Liumeng Yang
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Publication number: 20130288947Abstract: The present invention relates to compounds of formula (I) in the form of any one of its stereoisomers or a mixture thereof, and wherein R1 represents a substituent of the benzene ring and is a bromine atom or a linear, branched or cyclic C1-8 alkyl, alkenyl, alkoxy or alkenyloxy group; R2 represents a C1-3 alkyl group; and R3 represents a hydrogen atom or a methyl or ethyl group; and their use as perfuming ingredients, for instance to impart odor notes of the watery/ozone type.Type: ApplicationFiled: September 29, 2011Publication date: October 31, 2013Applicant: Firmenich SAInventors: Alexandre Huboux, Jean-Marc Gaudin, Pascal Millet, Fabrice Robvieux
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Publication number: 20130281394Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: October 24, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
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Publication number: 20130245275Abstract: The present invention relates to phenyl diamides according to the general formula (1) and their use as a medicament and a pharmaceutical preparation comprising as an active ingredient a phenyl diamide according to the general formula (1). Further, the present invention relates to phenyl diamides according to the formulas (16), (17) and (18) for use in the treatment of gliomas.Type: ApplicationFiled: October 4, 2011Publication date: September 19, 2013Applicant: Rheinische Friedrich-Wilhelms Universitaet BonnInventors: Michael Famulok, Anke Bill, Anton Schmitz, Juergen Bajorath
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 8436013Abstract: The invention features compositions and methods that are useful for treating or preventing AAT deficiency and associated conditions. In addition, the invention provides methods for identifying compounds useful for treatment of AAT deficiency and associated conditions.Type: GrantFiled: July 9, 2009Date of Patent: May 7, 2013Assignee: University of Florida Research Foundation, Inc.Inventors: Chen Liu, David A. Ostrov
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Publication number: 20130096209Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.Type: ApplicationFiled: April 15, 2011Publication date: April 18, 2013Applicants: Kraft Foods Global Brands LLC, Chromocell CorporationInventors: David Hayashi, William P. Jones, Jane V. Leland, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Louise Slade, Kambiz Shekdar, Jessica Langer
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Patent number: 8357825Abstract: A process for preparing a 1,2-diol, a 1,2-diol ether or an alkanolamine comprising converting an olefin oxide, wherein the olefin oxide has been obtained by a process for the epoxidation of an olefin, said process comprising using a catalyst comprising a carrier and silver deposited thereon, wherein the carrier comprises at least 85 weight percent ?-alumina and has a surface area of at least 1.3 m2/g, a median pore diameter of more than 0.8 ?m, and a pore size distribution wherein at least 80% of the total pore is contained in pores with diameters in the range of from 0.1 to 10 ?m, and at least 80% of the pore volume contained in the pores with diameters in the range of from 0.1 to 10 ?m is contained in pores with diameters in the range of from 0.3 to 10 ?m.Type: GrantFiled: November 18, 2011Date of Patent: January 22, 2013Assignee: Shell Oil CompanyInventors: William Herman Gerdes, John Robert Lockemeyer, Donald James Remus, Thomas Szymanski, Randall Clayton Yeates
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Patent number: 8357813Abstract: The invention provides a process for the epoxidation of an olefin, which process comprises reacting a feed comprising an olefin and oxygen in the presence of a catalyst comprising a carrier and silver deposited on the carrier, which carrier comprises at least 85 weight percent ?-alumina and has a surface area of at least 1.3 m2/g, a median pore diameter of more than 0.8 ?m, and a pore size distribution wherein at least 80% of the total pore volume is contained in pores with diameters in the range of from 0.1 to 10 ?m and at least 80% of the pore volume contained in the pores with diameters in the range of from 0.1 to 10 ?m is contained in pores with diameters in the range of from 0.3 to 10 ?m.Type: GrantFiled: November 18, 2011Date of Patent: January 22, 2013Assignee: Shell Oil CompanyInventors: William Herman Gerdes, John Robert Lockemeyer, Donald James Remus, Thomas Szymanski, Randall Clayton Yeates
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Publication number: 20130005782Abstract: This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery base upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.Type: ApplicationFiled: March 23, 2011Publication date: January 3, 2013Inventors: Alexandre Chigaev, Larry A. Sklar
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Publication number: 20120316066Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: December 2, 2011Publication date: December 13, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20120252890Abstract: The present application relates to processes for the preparation of intermediates useful in the manufacture of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate and compounds and oseltamivir analogs and to pharmaceutical compositions comprising said analog compounds. The application further relates to a method of using the novel analogs of oseltamivir to treat or prevent influenza.Type: ApplicationFiled: October 15, 2010Publication date: October 4, 2012Applicant: BROCK UNIVERSITYInventors: Tomas Hudlicky, Lukas Werner, Ales Machara
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Publication number: 20120203014Abstract: Herein disclosed is a method for treating patients affected by HIV comprising administering N-hydroxy-benzamide-based histone deacetylase inhibitors, such as: diethyl-[6-(4-hydroxycarbamoyl-phenyl-carbamoyloxymethyl)-naphtalen-2-yl-methyl]-ammonium chloride; 4-(2-(S)-benzoylamino-3-naphtalen-2-yl-propionylamino)-N-hydroxy-benzamide; and/or benzo[1,3]dioxole-5-carboxylic acid [1(S)-(4-hydroxycarbamoyl-phenylcarbamoyl)-2-naphtalen-2-yl-ethyl]-amide. Such histone deacetylase inhibitors are administered in a dosage ranging from 50 to 200 mg/day, preferably from 100 to 200 mg/day, so as to obtain a blood concentration between 125 and 250 nM.Type: ApplicationFiled: September 14, 2010Publication date: August 9, 2012Inventors: Charles Dinarello, Gianluca Fossati, Paolo Mascagni
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Publication number: 20120201763Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.Type: ApplicationFiled: December 23, 2011Publication date: August 9, 2012Applicant: SENOMYX, INC.Inventors: Catherine Tachdjian, Andrew P. Patron, Sara L. Adamski-Werner, Farid Bakir, Qing Chen, Vincent Darmohusodo, Stephen Terrence Hobson, Xiaodong Li, Ming Qi, Daniel H. Rogers, Marketa Rinnova, Guy Servant, Xiao-Qing Tang, Mark Zoller, Daivd Wallace, Amy Xing, Klaus Gubernator
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Publication number: 20120196865Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: ApplicationFiled: July 19, 2010Publication date: August 2, 2012Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Publication number: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Publication number: 20120116090Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: December 6, 2011Publication date: May 10, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, Bing Li
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Patent number: 8168808Abstract: A production method of fluorinated compounds, for producing a compound represented by formula (3) in a fluorine-based solution in a flow of fluorine gas after reaction of at least one type of compounds represented by formula (1) and at least one type of compounds represented by formula (2). Similarly, fluorinated compounds represented by formula (4) prepared by the fluorination of compounds obtained by the reaction of formula (1) and formula (2)?. The fluorinated polymers obtained by the polymerizations of formula (3) and (4) compounds are useful as an optical or electrical materials. wherein R1, R2, R3, R4, Rff1, Rff2, Rff3, Rff4, X, Y, Z, and n are defined in the specification respectively.Type: GrantFiled: November 9, 2009Date of Patent: May 1, 2012Assignee: Japan Science and Technology AgencyInventors: Yoshiyuki Okamoto, Yasuhiro Koike
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Publication number: 20120095092Abstract: The invention provides a compound of formula (I), a pharmaceutical composition thereof, a method of preparing a medicament for the treatment of a cancer, and a method of treating cancers. The invention exhibits merits against cancers such as significantly higher potency and effectiveness over a broader range of cancers. In formula (I), Ra is a benzyl group with alkyl and/or alkoxy; Rb is selected from H and alkyl groups; Rf is an alkyl; and R3 is selected from a substituted phenyl, a heterocyclic group, and wherein Rc is selected from a fused ring, fused rings, and any bivalent cyclic group.Type: ApplicationFiled: October 18, 2010Publication date: April 19, 2012Inventors: Bin Su, Aimin Zhou, Yan Xu
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Publication number: 20120071672Abstract: An object of the present invention is to provide an industrially advantageous process for preparing a benzaldehyde compound from a benzyl alcohol compound with high yield. The present invention relates to a process for preparing an aromatic aldehyde compound represented by the formula (2); which comprises reacting an aromatic methyl alcohol compound represented by the formula (1); and a peroxide under a pH value of a reaction solution being pH 0.01 or higher and less than 10 in the presence of at least one metallic compound selected from a molybdenum compound and a tungsten compound, a quaternary ammonium salt and an organic phosphonium salt.Type: ApplicationFiled: October 6, 2009Publication date: March 22, 2012Inventors: Takashi Doi, Yoshihiro Yoshida, Shinji Yasuda, Yoshiyuki Watanabe, Satoru Fujitsu, Daisuke Douyama
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120029069Abstract: This invention relates to a novel compound extracted from antrodia Cinnamomea and related compounds of formula (1), and pharmaceutical compositions comprising the compound of formula (1) and a pharmaceutically acceptable carrier or excipient. The invention further comprises the method of inhibit cancer cells by administering an effective amount of the compound of formula (1).Type: ApplicationFiled: May 6, 2011Publication date: February 2, 2012Inventors: Ching-Kuo Lee, Pi-Yu Chen, Jir-Mehng Lo, Wen-Bin Zhong, Tien-Wang Chiu, Chieh-Chou YU
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Publication number: 20110319639Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.Type: ApplicationFiled: June 24, 2011Publication date: December 29, 2011Inventors: Pablo Wessig, Kristian MÖLLNITZ, Robert Wawrzinek
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Publication number: 20110288061Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, R1?, R2?, R3?, and R4? are defined the same as the specification.Type: ApplicationFiled: May 18, 2011Publication date: November 24, 2011Applicant: National Cheng Kung UniversityInventor: Tian-Shung Wu
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Publication number: 20110275663Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 16, 2009Publication date: November 10, 2011Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
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Publication number: 20110071142Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.Type: ApplicationFiled: March 19, 2010Publication date: March 24, 2011Applicant: BETH ISRAEL DEACONESS MEDICAL CENTERInventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
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Patent number: 7906502Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: GrantFiled: June 21, 2006Date of Patent: March 15, 2011Assignee: AstraZeneca ABInventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Ingemar Starke
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Publication number: 20110052492Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: ApplicationFiled: November 3, 2010Publication date: March 3, 2011Inventors: Matthias FRIEBE, Peter Muschick, Andreas Huth
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Publication number: 20110027179Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: ApplicationFiled: October 14, 2010Publication date: February 3, 2011Inventors: Matthias FRIEBE, Peter Muschick, Andreas Huth
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Publication number: 20100311827Abstract: The invention provides chlorogenic acid derivatives of Formula (I) that are capable of inhibiting the growth of fungal cells and are useful as anti-fungal agents. The invention further provides the methods of inhibiting the growth of fungal cells and methods of treating a fungal infection in an animal by administering to the animal an effective amount of a compound of Formula I, either alone or in combination with another anti-fungal agent.Type: ApplicationFiled: July 23, 2007Publication date: December 9, 2010Inventors: Mohsen Daneshtalab, Chao-Mei Ma
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Publication number: 20100249123Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.Type: ApplicationFiled: March 19, 2008Publication date: September 30, 2010Applicant: ADDEX PHARMA SAInventors: Beatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
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Publication number: 20100137428Abstract: The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.Type: ApplicationFiled: December 21, 2005Publication date: June 3, 2010Inventors: Andrea Bozzoli, Clive Leslie Branch, Jacqueline Anne MacRitchie, Howard Robert Marshall, Roderick Alan Porter, Simone Spada
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Publication number: 20100130758Abstract: Disclosed are a catalyst including a hydrotalcite and, immobilized on a surface thereof, particles of at least one metal selected from the group consisting of Cu, Ag, and Au; a method for producing a carbonyl compound through dehydrogenation of an alcohol in the presence of the catalyst; and a method for producing a carbonyl compound through dehydrogenation of an alcohol in the presence of a catalyst including a hydrotalcite and, immobilized on a surface thereof, particles of a metal, in which dehydrogenation is performed in the absence of oxygen.Type: ApplicationFiled: March 9, 2007Publication date: May 27, 2010Inventors: Kiyotomi Kaneda, Noritsugu Yamasaki
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Publication number: 20100117024Abstract: A lapping composition is presented, wherein that lapping composition is formed by mixing a solvent, a base, and a phenolic compound having structure I: wherein R1 is selected from the group consisting of —O?Mx+ wherein x is selected from the group consisting of 1, 2, and 3, —O—R3 wherein R3 is selected from the group consisting of alkyl, allyl, and phenyl, —N(R3R4) wherein R4 is selected from the group consisting of —H, alkyl, allyl, and phenyl, and —S—R3; and wherein R2 is selected from the group consisting of —O?Mx+ wherein x is selected from the group consisting of 1, 2, and 3, —O—R3 wherein R3 is selected from the group consisting of alkyl, allyl, and phenyl, —N(R3R4) wherein R4 is selected from the group consisting of —H, alkyl, allyl, and phenyl, and —S—R3.Type: ApplicationFiled: November 9, 2009Publication date: May 13, 2010Inventor: JOHN L. LOMBARDI