Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 549/405)
  • Patent number: 10377733
    Abstract: Novel antimicrobial compounds against drug targets such as Eskape pathogens, Leishmania donovani, Mycobacterium tuberculosis, Clostridium difficile, Naegleria fowleri, and cancer are presented herein.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: August 13, 2019
    Assignees: University of South Florida, King Abdulaziz University
    Inventors: Danielle H. Demers, Bill J. Baker, Ala Azhari, Renee M. Fleeman, Dennis E. Kyle, Lindsey Neil Shaw
  • Patent number: 9045714
    Abstract: 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: Grant
    Filed: March 15, 2013
    Date of Patent: June 2, 2015
    Assignee: Symrise AG
    Inventors: Heiko Oertling, Claudia Gömann, Marc Vom Ende
  • Publication number: 20150133538
    Abstract: 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: Application
    Filed: August 10, 2012
    Publication date: May 14, 2015
    Applicant: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences
    Inventors: Yanmei Zhang, John Jeffrey Talley, Mark G. Obukowicz, Zhengchao Tu, Micky Tortorella, Yican Wang, Jianqi Liu, Yan Chen, Xiaorong Liu, Xin Lu
  • Publication number: 20150133659
    Abstract: 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: Application
    Filed: May 25, 2012
    Publication date: May 14, 2015
    Applicant: Sichuan University
    Inventors: Lijuan Chen, Yuquan Wei
  • Patent number: 8981127
    Abstract: 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: Grant
    Filed: September 22, 2009
    Date of Patent: March 17, 2015
    Assignee: Zach System
    Inventors: Yvon Derrien, Eric Chenard, Alain Burgos
  • Patent number: 8921413
    Abstract: 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: Grant
    Filed: November 21, 2013
    Date of Patent: December 30, 2014
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Publication number: 20140364465
    Abstract: 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: Application
    Filed: January 25, 2013
    Publication date: December 11, 2014
    Applicants: UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCH SCIENTIFIQUE - CNRS
    Inventors: Michel Boisbrun, Yves Chapleur, Andrea Bordessa, Stephane Flament, Isabelle Grillier-Vuissoz, Sandra Kuntz
  • Publication number: 20140256804
    Abstract: 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: Application
    Filed: October 18, 2012
    Publication date: September 11, 2014
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Yasuhiro Iwata, Kaoru Shimada, Yoshiyuki Okumura, Mayumi Kashino, Hiromitsu Yoshida
  • Publication number: 20140235672
    Abstract: 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: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventor: Douglas G. Batt
  • Publication number: 20140183409
    Abstract: 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: Application
    Filed: December 26, 2013
    Publication date: July 3, 2014
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: YASUYUKI GOTOH, RYUSHI SHUNDO, NORIKATSU HATTORI
  • Patent number: 8759390
    Abstract: 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: Grant
    Filed: July 14, 2009
    Date of Patent: June 24, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventor: Douglas G. Batt
  • Publication number: 20140142220
    Abstract: 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: Application
    Filed: November 18, 2013
    Publication date: May 22, 2014
    Inventors: Xuelan Wang, Zhuo Zhang, Jisheng Zhao, Chen Liu
  • Patent number: 8716498
    Abstract: A compound having the formula: is useful in the preparation of compounds of Formula I.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: May 6, 2014
    Assignee: 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
  • Publication number: 20140094512
    Abstract: 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: Application
    Filed: September 26, 2013
    Publication date: April 3, 2014
    Inventors: Nikolas Gunkel, Thorsten Meyer, John Michael Graettinger
  • Publication number: 20140005418
    Abstract: A compound having the formula: is useful in the preparation of compounds of Formula I.
    Type: Application
    Filed: August 29, 2013
    Publication date: January 2, 2014
    Applicant: 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
  • Patent number: 8609717
    Abstract: 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: Grant
    Filed: August 17, 2011
    Date of Patent: December 17, 2013
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Patent number: 8603947
    Abstract: 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: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8586768
    Abstract: 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: Grant
    Filed: November 12, 2010
    Date of Patent: November 19, 2013
    Assignee: Iowa State University Research Foundation, Inc.
    Inventors: Anumantha G. Kanthasamy, George A. Kraus, Vellareddy Anantharam
  • Publication number: 20130289034
    Abstract: 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: Application
    Filed: June 21, 2013
    Publication date: October 31, 2013
    Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER
  • Patent number: 8569522
    Abstract: 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: Grant
    Filed: June 24, 2009
    Date of Patent: October 29, 2013
    Assignee: 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
  • Publication number: 20130203830
    Abstract: 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: Application
    Filed: April 18, 2011
    Publication date: August 8, 2013
    Applicant: SULFATEQ B.V.
    Inventors: Fatemeh Talaei, Robert Henk Henning, Adrianus C. Van der Graaf
  • Publication number: 20130028837
    Abstract: 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: Application
    Filed: August 10, 2012
    Publication date: January 31, 2013
    Applicant: Lantheus Medical Imaging, Inc.
    Inventors: Heike S. Radeke, David S. Casebier, Michael T. Azure, Douglas D. Dischino
  • Patent number: 8344181
    Abstract: 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, hydrox
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: January 1, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens, François Paul Bischoff
  • Publication number: 20120129818
    Abstract: 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: Application
    Filed: April 23, 2010
    Publication date: May 24, 2012
    Inventor: Desikan Rajagopal
  • Patent number: 8080664
    Abstract: 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: Grant
    Filed: February 20, 2008
    Date of Patent: December 20, 2011
    Assignee: Universidad De Zaragoza
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Patent number: 8080676
    Abstract: 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: Grant
    Filed: October 25, 2007
    Date of Patent: December 20, 2011
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Akifumi Iida, Youichi Kyuuko, Toshio Hidaka
  • Patent number: 8071575
    Abstract: 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: Grant
    Filed: February 22, 2008
    Date of Patent: December 6, 2011
    Assignee: University of Louisville Research Foundation
    Inventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
  • Publication number: 20110263697
    Abstract: 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: Application
    Filed: April 22, 2011
    Publication date: October 27, 2011
    Applicant: STOKELY-VAN CAMP, INC.
    Inventor: Jeffrey J. Zachwieja
  • Publication number: 20110251407
    Abstract: 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: Application
    Filed: October 28, 2009
    Publication date: October 13, 2011
    Applicant: Mitsubishi Gas Chemical Company, Inc.
    Inventor: Youichi Kyuuko
  • Publication number: 20110237808
    Abstract: 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: Application
    Filed: September 22, 2009
    Publication date: September 29, 2011
    Applicant: ZACH SYSTEM
    Inventors: Yvon Derrien, Eric Chenard, Alain Burgos
  • Publication number: 20110207729
    Abstract: 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: Application
    Filed: August 7, 2008
    Publication date: August 25, 2011
    Applicant: 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
  • Patent number: 7960573
    Abstract: 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: Grant
    Filed: May 4, 2009
    Date of Patent: June 14, 2011
    Assignees: Children's Hospital Medical Center, Girindus America, Inc.
    Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
  • Patent number: 7960572
    Abstract: 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: Grant
    Filed: October 2, 2007
    Date of Patent: June 14, 2011
    Assignee: Zach System S.p.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto
  • Publication number: 20110112071
    Abstract: 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: Application
    Filed: January 18, 2011
    Publication date: May 12, 2011
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
  • Publication number: 20110112146
    Abstract: 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: Application
    Filed: July 14, 2009
    Publication date: May 12, 2011
    Inventor: Douglas G. Batt
  • Publication number: 20110105463
    Abstract: 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: Application
    Filed: June 24, 2009
    Publication date: May 5, 2011
    Applicant: 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
  • Patent number: 7893262
    Abstract: 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: Grant
    Filed: August 3, 2004
    Date of Patent: February 22, 2011
    Assignee: Arpida AG
    Inventors: Jurgen Jaeger, Kaspar Burri, Sorana Greiveldinger-Poenaru, Johannes Hoffner
  • Publication number: 20110021514
    Abstract: 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: Application
    Filed: November 13, 2008
    Publication date: January 27, 2011
    Applicants: RENOVIS, INC., PFIZER GLOBAL RESEARCH AND DEVELOPMENT
    Inventors: 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
  • Publication number: 20100317862
    Abstract: 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: Application
    Filed: February 20, 2008
    Publication date: December 16, 2010
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Patent number: 7851220
    Abstract: 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: Grant
    Filed: November 2, 2007
    Date of Patent: December 14, 2010
    Assignee: Intrexon Corporation
    Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Publication number: 20100298580
    Abstract: 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: Application
    Filed: November 13, 2008
    Publication date: November 25, 2010
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: Brian Broadbelt, Alexander Beliaev, David Alexander Learmonth
  • Patent number: 7754759
    Abstract: 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: Grant
    Filed: November 3, 2006
    Date of Patent: July 13, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Jacob Berger, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Jr., Dov Nitzan, Shu-Hai Zhao
  • Publication number: 20100098634
    Abstract: 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: Application
    Filed: July 24, 2009
    Publication date: April 22, 2010
    Inventors: 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
  • Patent number: 7638648
    Abstract: 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: Grant
    Filed: March 23, 2007
    Date of Patent: December 29, 2009
    Assignee: 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
  • Publication number: 20090291998
    Abstract: 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: Application
    Filed: March 3, 2009
    Publication date: November 26, 2009
    Inventors: 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
  • Patent number: 7615650
    Abstract: 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: Grant
    Filed: January 28, 2005
    Date of Patent: November 10, 2009
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Kazuo Tanaka, Youichi Kyuuko, Toshio Hidaka
  • Patent number: 7563913
    Abstract: 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: Grant
    Filed: November 25, 2003
    Date of Patent: July 21, 2009
    Assignee: Hiro International Co., Ltd.
    Inventors: Yutaka Sashida, Yoshihiro Mimaki, Minpei Kuroda, Ryosuke Kobayashi, Hiroaki Kando, Kosuke Nosaka, Hiroyasu Ishii, Takao Yamori
  • Patent number: 7560575
    Abstract: 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: Grant
    Filed: December 28, 2005
    Date of Patent: July 14, 2009
    Assignee: Acino Pharma AG
    Inventors: Thomas Bader, Alfred Stutz, Harald Hofmeier, Hans-Ulrich Bichsel
  • Publication number: 20090130051
    Abstract: 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: Application
    Filed: March 10, 2006
    Publication date: May 21, 2009
    Applicants: Howard Florey Institute Of Experimental Physiology And Medicine, Neuprotect Pty Ltd
    Inventors: Bevyn Jarrott, Clive Newton May, Owen Llewellyn Woodman, Gregory James Dusting
  • Publication number: 20090111868
    Abstract: The present invention provides compositions and methods for regulating the BK channel using rottlerin and derivatives thereof. In particular, the present invention provides pharmaceutical compositions for use in treating or preventing BK channel medicated disorders including hypertension and various hyperexcitability disorders. Also provided are compositions and methods for use in post-stroke neuroprotection and in treating or preventing erectile dysfunction. The present invention further provides kits for use in treating or preventing BK channel mediated disorders, comprising the compositions of the present invention.
    Type: Application
    Filed: November 18, 2005
    Publication date: April 30, 2009
    Inventors: Steven O. Marx, Sergey I. Zakharov