Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 549/405)
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Patent number: 11555023Abstract: This invention relates to a method for preparing a desired isomer of a substituted 2-trifluoromethyl-2H-chromene-3-carboxylic acid, which is characterized by comprising: (a) contacting the substituted 2-trifluoromethyl-2H-chromene-3-carboxylic acid with a chiral amine to form salts, wherein the chiral amine is selected so that the solubility of the amine salt of the undesired substituted 2-trifluoromethyl-2H-chromene-3-carboxylic acid is greater than the amine salt of the desired substituted 2-trifluoromethyl-2H-chromene-3-carboxylic acid, and (b) irradiating the mixture with an ultraviolet (UV) light, wherein the irradiation increases the amount of the less soluble chiral amine salt of the substituted of the 2-trifluoromethyl-2H-chromene-3-carboxylic acid in the mixture.Type: GrantFiled: January 20, 2020Date of Patent: January 17, 2023Assignee: AskAt Inc.Inventors: Yoshiyuki Okumura, Yukari Inami, Bas Dros, Michel Sebastiaan Leeman
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Patent number: 10377733Abstract: Novel antimicrobial compounds against drug targets such as Eskape pathogens, Leishmania donovani, Mycobacterium tuberculosis, Clostridium difficile, Naegleria fowleri, and cancer are presented herein.Type: GrantFiled: June 29, 2018Date of Patent: August 13, 2019Assignees: University of South Florida, King Abdulaziz UniversityInventors: Danielle H. Demers, Bill J. Baker, Ala Azhari, Renee M. Fleeman, Dennis E. Kyle, Lindsey Neil Shaw
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Patent number: 9045714Abstract: Compounds and methods of using of compounds or mixtures thereof, as fragrance and/or flavoring material or as fragrance and/or flavoring material mixture, new fragrance and/or flavoring material mixtures, new perfumed and/or flavored articles, and new, particularly advantageous compounds and mixtures to be used are described.Type: GrantFiled: March 15, 2013Date of Patent: June 2, 2015Assignee: Symrise AGInventors: Heiko Oertling, Claudia Gömann, Marc Vom Ende
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Publication number: 20150133538Abstract: The present invention discloses deuterated benzopyran compounds having structure features as shown in Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or prodrug molecules thereof. With excellent anti-inflammatory and analgesic effects and the capability to inhibit growth of tumor cells, such compounds are novel COX-2 selective inhibitors. The compounds and pharmaceutically acceptable salts thereof disclosed by the present application can be applied in preparing anti-inflammatory and analgesic drugs and drugs for treating or preventing tumors.Type: ApplicationFiled: August 10, 2012Publication date: May 14, 2015Applicant: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of SciencesInventors: Yanmei Zhang, John Jeffrey Talley, Mark G. Obukowicz, Zhengchao Tu, Micky Tortorella, Yican Wang, Jianqi Liu, Yan Chen, Xiaorong Liu, Xin Lu
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Publication number: 20150133659Abstract: The present invention relates to millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) and its analogues. The present invention provides methods for preparing these compounds, pharmaceutical compositions including these compounds, and methods of treating diseases utilizing pharmaceutical compositions including these compounds.Type: ApplicationFiled: May 25, 2012Publication date: May 14, 2015Applicant: Sichuan UniversityInventors: Lijuan Chen, Yuquan Wei
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Patent number: 8981127Abstract: The present invention relates to a process for the preparation of nebivolol and, more particularly, to an improved process of synthesizing an alpha-haloketone of formula a key intermediate in the preparation of nebivolol.Type: GrantFiled: September 22, 2009Date of Patent: March 17, 2015Assignee: Zach SystemInventors: Yvon Derrien, Eric Chenard, Alain Burgos
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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: 20140364465Abstract: The present invention relates to thiazolidinedione derivatives, to the processes for preparing same and to the therapeutic use thereof for preventing or treating cancer, and more specifically breast cancer. These compounds are of formula (I) and exhibit, at a concentration of 100 ?M, a hepatocyte viability preferably greater than 60%, preferably greater than 80% and more preferentially greater than 85%.Type: ApplicationFiled: January 25, 2013Publication date: December 11, 2014Applicants: UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCH SCIENTIFIQUE - CNRSInventors: Michel Boisbrun, Yves Chapleur, Andrea Bordessa, Stephane Flament, Isabelle Grillier-Vuissoz, Sandra Kuntz
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Publication number: 20140256804Abstract: The present invention provides a pharmaceutical composition which prevents from decreasing the blood exposure of the third generation coxib-drugs, a process for preparing the said pharmaceutical composition and its use. It has been founded in this invention that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can afford a pharmaceutical composition which can prevent from decreasing the blood exposure, AUC and bioavailability. The pharmaceutical composition of the present invention has also good stability, which is useful for drugs. Namely, the technological thought that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can prevent from decreasing the blood exposure, AUC and bioavailability has been established in this invention.Type: ApplicationFiled: October 18, 2012Publication date: September 11, 2014Applicant: RAQUALIA PHARMA INC.Inventors: Yasuhiro Iwata, Kaoru Shimada, Yoshiyuki Okumura, Mayumi Kashino, Hiromitsu Yoshida
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Publication number: 20140235672Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W1, W2, W3, Y, Z, R2, R3, R3? and R4, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Inventor: Douglas G. Batt
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Publication number: 20140183409Abstract: A liquid crystal composition including an antioxidant, and a liquid crystal display device containing this composition are described. The liquid crystal composition has a nematic phase, has a high solubility in a liquid crystal composition, and includes a specific antioxidant useful for preventing deterioration of the composition. The liquid crystal composition may also include a specific compound having a high maximum temperature or a small viscosity as a first component, a specific compound having a high maximum temperature or a large dielectric anisotropy as a second component, and a specific compound having a large negative dielectric anisotropy as a third component.Type: ApplicationFiled: December 26, 2013Publication date: July 3, 2014Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: YASUYUKI GOTOH, RYUSHI SHUNDO, NORIKATSU HATTORI
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Patent number: 8759390Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W1, W2, W3, Y, Z, R2, R3, R3? and R4, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: GrantFiled: July 14, 2009Date of Patent: June 24, 2014Assignee: Bristol-Myers Squibb CompanyInventor: Douglas G. Batt
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Publication number: 20140142220Abstract: The present invention relates to a fluorine-containing polymer comprising a structure represented by the following general formula (I), as well as the preparation process and use thereof. According to the technical solution of the invention, a novel fluorine-containing polymer with a larger molecular weight and an aromatic side group is obtained through a simple reaction, and it can be used as a non-ionic fluorine carbon surfactant, and especially, is applicable to the preparation of a pigment dispersion. Additionally, the invention further relates to a pigment dispersion and the preparation process thereof.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Inventors: Xuelan Wang, Zhuo Zhang, Jisheng Zhao, Chen Liu
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Patent number: 8716498Abstract: A compound having the formula: is useful in the preparation of compounds of Formula I.Type: GrantFiled: August 29, 2013Date of Patent: May 6, 2014Assignee: Array Biopharma, Inc.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
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Publication number: 20140094512Abstract: The present invention relates to compositions and methods for modulating the degree of adipose tissue deposited intramuscularly in cattle by administration of a retinoic receptor antagonist or inverse agonist and compounds for use in such method.Type: ApplicationFiled: September 26, 2013Publication date: April 3, 2014Inventors: Nikolas Gunkel, Thorsten Meyer, John Michael Graettinger
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Publication number: 20140005418Abstract: A compound having the formula: is useful in the preparation of compounds of Formula I.Type: ApplicationFiled: August 29, 2013Publication date: January 2, 2014Applicant: ARRAY BIOPHARMA INC.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
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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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Patent number: 8603947Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.Type: GrantFiled: July 20, 2011Date of Patent: December 10, 2013Assignee: Bayer Cropscience AGInventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
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Patent number: 8586768Abstract: A method of synthesizing rottlerin analogs is described. The synthesis methods described are the first known method of synthesizing rottlerin analogs from commercially-available materials to produce cost effective analogs. Rottlerin analog structures made by the synthesis methods and methods of use for treating a neurological or inflammatory response mediated by protein kinase C (PKC) are further described.Type: GrantFiled: November 12, 2010Date of Patent: November 19, 2013Assignee: Iowa State University Research Foundation, Inc.Inventors: Anumantha G. Kanthasamy, George A. Kraus, Vellareddy Anantharam
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Publication number: 20130289034Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER
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Patent number: 8569522Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: GrantFiled: June 24, 2009Date of Patent: October 29, 2013Assignee: Array BioPharma Inc.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
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Publication number: 20130203830Abstract: The invention is related to compounds for prevention of cell injury or protection of cells. The compounds are involved in the maintenance or the increase of hydrogen sulphide in cells, which results in a protection of the cells or the prevention of cell injury. The compounds of the invention can be used in cell culture and tissue culture techniques. They can also be used in several medical conditions such as ischemia, reperfusion and hypothermia, or for preserving organs which are used for transplantation.Type: ApplicationFiled: April 18, 2011Publication date: August 8, 2013Applicant: SULFATEQ B.V.Inventors: Fatemeh Talaei, Robert Henk Henning, Adrianus C. Van der Graaf
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Publication number: 20130028837Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: ApplicationFiled: August 10, 2012Publication date: January 31, 2013Applicant: Lantheus Medical Imaging, Inc.Inventors: Heike S. Radeke, David S. Casebier, Michael T. Azure, Douglas D. Dischino
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Patent number: 8344181Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10? (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxType: GrantFiled: August 26, 2005Date of Patent: January 1, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens, François Paul Bischoff
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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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Patent number: 8080664Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.Type: GrantFiled: February 20, 2008Date of Patent: December 20, 2011Assignee: Universidad De ZaragozaInventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
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Patent number: 8080676Abstract: The present invention provides an industrially available method for efficiently producing high-purity S-(?)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid excellent in solid-liquid separability from an S-(?)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid ester, and also provides products obtained by the method. Under a temperature condition of 50-80° C. in an aqueous solvent, (A) an S-(?)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid ester represented by the general formula (1) is hydrolyzed under a basic condition for 1-3 hours; then (B) the insoluble matters contained in the reaction solution resulting from the hydrolysis are removed; and (C) an acid is added to the resulting solution to effect crystallization; provided that R in the general formula (1) represents an alkyl or aryl group.Type: GrantFiled: October 25, 2007Date of Patent: December 20, 2011Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Akifumi Iida, Youichi Kyuuko, Toshio Hidaka
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Patent number: 8071575Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: GrantFiled: February 22, 2008Date of Patent: December 6, 2011Assignee: University of Louisville Research FoundationInventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
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Publication number: 20110263697Abstract: The present invention is directed to methods for reducing oxidative modification of one or more proteins or other cellular constituents involved in muscle cell contraction, for reducing muscle fatigue or for increasing muscle performance.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: STOKELY-VAN CAMP, INC.Inventor: Jeffrey J. Zachwieja
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Publication number: 20110251407Abstract: The present invention is a simple method, in which a specific amount of alkali is added to an enantiomeric mixture of an optically active organic carboxylic acid where enantiomers are present in a non-equimolar ratio, or in which the enantiomeric mixture of an optically active organic carboxylic acid is neutralized with an alkali, and then a specific amount of acid is added thereto, thereby separating an organic carboxylic acid salt in the mother liquor and a crystallized organic carboxylic acid from each other. The method makes it possible to obtain an optically active organic carboxylic acid with improved enantiomeric excess. The present invention provides a simple production method for obtaining an optically active organic carboxylic acid with improved enantiomeric excess from an enantiomeric mixture of an optically active organic carboxylic acid where enantiomers are present in a non-equimolar ratio.Type: ApplicationFiled: October 28, 2009Publication date: October 13, 2011Applicant: Mitsubishi Gas Chemical Company, Inc.Inventor: Youichi Kyuuko
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Publication number: 20110237808Abstract: The present invention relates to a process for the preparation of nebivolol and, more particularly, to an improved process of synthesizing an alpha-haloketone of formula a key intermediate in the preparation of nebivolol.Type: ApplicationFiled: September 22, 2009Publication date: September 29, 2011Applicant: ZACH SYSTEMInventors: Yvon Derrien, Eric Chenard, Alain Burgos
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Publication number: 20110207729Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT5A receptor modulating action. It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.Type: ApplicationFiled: August 7, 2008Publication date: August 25, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Isao Kinoyama, Satoshi Miyamoto, Takehiro Miyazaki, Yohei Koganemaru, Yuichiro Kawamoto, Nobuyuki Shiraishi, Hiroaki Hoshii, Akio Kuroda, Mayako Yamazaki, Minoru Yasuda, Hiroaki Mizuno
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Patent number: 7960573Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: May 4, 2009Date of Patent: June 14, 2011Assignees: Children's Hospital Medical Center, Girindus America, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
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Patent number: 7960572Abstract: The present invention relates to a process for the preparation of Nebivolol and, more particularly, to an improved method of synthesizing 6-fluoro chroman epoxides of formula (I) key intermediates in preparing nebivolol.Type: GrantFiled: October 2, 2007Date of Patent: June 14, 2011Assignee: Zach System S.p.A.Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto
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Publication number: 20110112071Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
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Publication number: 20110112146Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W1, W2, W3, Y, Z, R2, R3, R3? and R4, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: ApplicationFiled: July 14, 2009Publication date: May 12, 2011Inventor: Douglas G. Batt
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Publication number: 20110105463Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: June 24, 2009Publication date: May 5, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
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Patent number: 7893262Abstract: The invention concerns a novel process for the preparation of 2H-chromenes of formula I and formula 5 and valuable intermediates of formulae 3 and 4 of this process.Type: GrantFiled: August 3, 2004Date of Patent: February 22, 2011Assignee: Arpida AGInventors: Jurgen Jaeger, Kaspar Burri, Sorana Greiveldinger-Poenaru, Johannes Hoffner
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Publication number: 20110021514Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: November 13, 2008Publication date: January 27, 2011Applicants: RENOVIS, INC., PFIZER GLOBAL RESEARCH AND DEVELOPMENTInventors: Matthew Cox, Donogh John Roger O'Mahony, Maria De Los Angeles Estiarte-Martinez, Tadashi Kawashima, Satoshi Nagayama, Yuji Shishido, Hirotaka Tanaka, Matthew Alexander James Duncton, Andrew Antony Calabrese
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Publication number: 20100317862Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.Type: ApplicationFiled: February 20, 2008Publication date: December 16, 2010Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
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Patent number: 7851220Abstract: The present invention relates to methods to use non-steroidal ligands in nuclear receptor-based inducible gene expression system to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: November 2, 2007Date of Patent: December 14, 2010Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
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Publication number: 20100298580Abstract: Compounds of formula I, V, VI and II, and processes for their preparation, wherein R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl. There is also provided a process for preparing a compound of formula B from the compounds of formula V and I.Type: ApplicationFiled: November 13, 2008Publication date: November 25, 2010Applicant: BIAL - PORTELA & CA, S.A.Inventors: Brian Broadbelt, Alexander Beliaev, David Alexander Learmonth
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Patent number: 7754759Abstract: Compounds of the formula I: wherein m, n, p, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Methods of making the compounds and using the compounds for treatment of 5-HT6 receptor-mediated diseases are disclosed.Type: GrantFiled: November 3, 2006Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: Jacob Berger, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Jr., Dov Nitzan, Shu-Hai Zhao
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Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
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Patent number: 7638648Abstract: Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.Type: GrantFiled: March 23, 2007Date of Patent: December 29, 2009Assignee: Allergan Inc.Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok Yin Tsang, Ling Li, Janet A. Takeuchi, Thong Vu, Richard Beard, Smita Bhat, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Publication number: 20090291998Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, A, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.Type: ApplicationFiled: March 3, 2009Publication date: November 26, 2009Inventors: Sergei Agoulnik, Kozo Akasaka, Francis Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuinness, Erin A. Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu
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Patent number: 7615650Abstract: The invention provides a process for producing a chroman compound represented by formula (1), characterized in that the process includes allowing a phenol, an unsaturated compound, and a formaldehyde to react in the absence of catalyst and in the presence of water in an amount by mole 1 to 10 times that of the phenol. According to the present invention, a high-purity chroman compound can be produced in the absence of catalyst and under mild conditions. In addition, the invention provides an industrial means for producing the compound, without using a large amount of an acid or a base serving as a reaction promoter or a catalyst, which would otherwise cause side reactions, apparatus corrosion, etc.Type: GrantFiled: January 28, 2005Date of Patent: November 10, 2009Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Kazuo Tanaka, Youichi Kyuuko, Toshio Hidaka
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Patent number: 7563913Abstract: There are provided novel compounds that have been extracted and isolated from a plant belonging to the family Compositae. Compounds represented by general formula (I): wherein R1 represents hydroxyl and R2 represents methoxy.Type: GrantFiled: November 25, 2003Date of Patent: July 21, 2009Assignee: Hiro International Co., Ltd.Inventors: Yutaka Sashida, Yoshihiro Mimaki, Minpei Kuroda, Ryosuke Kobayashi, Hiroaki Kando, Kosuke Nosaka, Hiroyasu Ishii, Takao Yamori
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Patent number: 7560575Abstract: A process of making racemic [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)?,??-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] of the compound of the formula (I) and its pure [2S*[R*[R*[R*]]]]- and [2R*[S*[S*[S*]]]]-enantiomer compounds and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 28, 2005Date of Patent: July 14, 2009Assignee: Acino Pharma AGInventors: Thomas Bader, Alfred Stutz, Harald Hofmeier, Hans-Ulrich Bichsel
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Publication number: 20090130051Abstract: Novel flavonoid compounds having anti-oxidant activity are described. The compounds and compositions have been shown to exhibit anti-oxidant properties and are particularly useful in the treatment of ischemia and reperfusion injuries. The invention also describes a method to chemically synthesize such flavonoid compounds and test their efficacy. Such compounds and corresponding pharmaceutically acceptable derivatives and/or salts have uses in the areas of pharmaceuticals, nutraceutical, and veterinary applications.Type: ApplicationFiled: March 10, 2006Publication date: May 21, 2009Applicants: Howard Florey Institute Of Experimental Physiology And Medicine, Neuprotect Pty LtdInventors: Bevyn Jarrott, Clive Newton May, Owen Llewellyn Woodman, Gregory James Dusting