Carbonyl In Substituent Q Patents (Class 564/169)
  • Publication number: 20150141465
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Calvin W. YEE, Zhe Li
  • Publication number: 20150119576
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Manabu YAOSAKA, Tomohisa UTSUNOMIYA, Yuji MORIYAMA, Tomohiro MATSUMOTO, Kazutaka MATOBA
  • Patent number: 9000222
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: April 7, 2015
    Assignee: Androscience Corporation
    Inventors: Charles Shih, Qian Shi, Hui-Kang Wang
  • Patent number: 8946479
    Abstract: A process for preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butane amide also known as a diketone intermediate of atorvastatin, completely devoid of impurities 3,4-difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-n-?-diphenylbenzene butane amide; methyl, 2{-2[-(4-fluorophenyl)-2-oxo-1-phenylethyl)]}-4-methyl-3-oxo pentanoate; 1,4-bis(4-fluorophenyl)-2,3-diphenylbutane-1,4-dione, 1-(4-fluorophenyl)-2-phenyl ethanone; 1-(4-fluorophenyl)-2-phenyl ethanone and containing about 0.05% or less of 2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butane amide. In that process the said diketone intermediate of formula 1 is obtained by maintaining temperature ?25° C. to 50° C. during Friedel-Crafts acylation, in situ halogenation of formula II in presence of a solvent and nucleophilic substitution from a compound of formula III with formula IV in presence of a base.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: February 3, 2015
    Assignee: Vijayasri Organics Limited
    Inventors: Jagapathi Raju Srivatsavayi, Sairam Pothukuchi, Srinivasa Sastry Rani, Mallikarjuna Rao Chikka, Chiranjeevi Cheekati, Mallikarjuna Rao Gutti, Trimurthulu Singavarapu, Venkat Reddy Thimmaipally, Venkateswara Rao Tadanki
  • Patent number: 8895552
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: November 25, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Patent number: 8871745
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: October 28, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20140275271
    Abstract: This invention provides a compound having the structure wherein ?, ?, A, B, and R1-R4 are defined herein. This invention also provides pharmaceutical compositions comprising the above compounds, a method of accelerating the healing of a wound, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: October 16, 2012
    Publication date: September 18, 2014
    Applicants: The Research Foundation for the State University of New York, Chem-Master International, Inc.
    Inventors: Lorne M. Golub, Hsi-ming Lee, Francis Johnson
  • Patent number: 8772536
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: July 8, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Patent number: 8722741
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: May 13, 2014
    Assignee: AstraZeneca AB
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20140128463
    Abstract: Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.
    Type: Application
    Filed: June 25, 2012
    Publication date: May 8, 2014
    Applicants: China State Institute of Pharmaceutic Industry, Shanghai Institute of Pharmaceutical Industry
    Inventors: Zhenpeng Yu, Gouping Wang, Zhen Zhang, Minyu Liu, Xiaoling Huang, Ying Liu, Lin Xiao, Li Cai, Xuejun Wu, Yifang Deng, Mianli Pan, Renhai Chen, Shenrong Tang, Quanhai Liu
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Patent number: 8710272
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: April 29, 2014
    Assignee: Androscience Corporation
    Inventors: Charles C. Y. Shih, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Patent number: 8692005
    Abstract: Provided are methods for decreasing the reaction time between an alkanolamine such as triethanolamine and a fatty acid alkyl ester such as, a triglyceride, a vegetable oil, a methyl ester, an ethyl ester, etc., a fatty acid, or a mixture thereof. The methods utilize a divalent zinc catalyst to facilitate and accelerate an esterification or transesterification reaction between the alkanolamine and the fatty acid, or fatty acid alkyl ester.
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: April 8, 2014
    Assignee: Stepan Company
    Inventors: Marshall J. Nepras, Franz J. Luxem, Leonard F. Zaporowski, David Eisenberg
  • Publication number: 20140094613
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 3, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki MURASE, Toshihito KUMAGAI, Hisaya WADA, Hisahide TANIMOTO, Koumei OHTA, Yoshihiro KIMURA
  • Publication number: 20140081047
    Abstract: A compound of the general formula X-[Q-W—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.
    Type: Application
    Filed: November 21, 2013
    Publication date: March 20, 2014
    Applicant: POLYTHERICS LIMITED
    Inventor: Antony GODWIN
  • Publication number: 20140079633
    Abstract: The present invention provides a method of preparing [123I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/?mol and radiochemical purity of 95%. The present invention further provides a method of applying [123I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.
    Type: Application
    Filed: February 1, 2013
    Publication date: March 20, 2014
    Applicant: NATIONAL TSING HUA UNIVERSITY
    Inventors: Chung-Shan Yu, Ho-Lien Huang, Chun-Nan Yeh, Wei-Yuan Lee, Kang-Wei Chang, Ying-Cheng Huang, Kun-Ju Lin, Ching-Shiuann Yang, Shu-Fan Tien, Wen-Chin Su, Jenn-Tzong Chen, Wuu-Jyh Lin, Shiou-Shiow Farn
  • Patent number: 8653134
    Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: February 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Catherine Vidal, Nathalie Adje, Stéphane Yvon, Jean Jacques Zeiller
  • Publication number: 20130338160
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 19, 2013
    Inventors: Charles SHIH, Qian Shi, Hui-kang Wang
  • Patent number: 8580969
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 12, 2013
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jason D. Brubaker
  • Patent number: 8581000
    Abstract: Disclosed is a process for preparing a compound of the formula wherein R1 and R1?, R2 and R2?, and R3 are as defined herein, said process comprising (I) reacting a diacid of the formula HOOC—R2—COOH with a diamine of the formula H2N—R3—NH2 to form an acid-terminated oligoamide intermediate of the formula HOOC—R2—CONH—R3—HNCO—R2?—COOH; and (II) reacting the acid-terminated oligoamide intermediate with a monoalcohol of the formula R1—OH in the presence of a tin or organic titanate catalyst, in the absence of a coupling agent, and in the absence of a solvent to form the product. Also disclosed is a composition prepared by the process.
    Type: Grant
    Filed: June 6, 2011
    Date of Patent: November 12, 2013
    Assignee: Xerox Corporation
    Inventors: Naveen Chopra, Thomas E Enright, Michelle N Chrétien, Barkev Keoshkerian, Daryl W Vanbesien
  • Publication number: 20130261121
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 3, 2013
    Inventors: Charles C.Y. SHIH, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Patent number: 8530694
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 15, 2011
    Date of Patent: September 10, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20130217692
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Application
    Filed: September 2, 2011
    Publication date: August 22, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Publication number: 20130195756
    Abstract: An embodiment of the invention comprises a ligand of Formula I wherein R1 and R2 are independently an alkyl or cycloalkyl; R3 is and alkyl; X is CO or SO2; Y is (CH2)n, C6H4, (OCH2CH2)n(NHCH2CH2)n and (OCH2CH2CH2)n, or a combination thereof; Z is linker group capable of conjugating to a vector; and n is an integer between 0 and 10. Also included are an imaging agent comprising a compound of Formula I complexed to 99mTc and their method of use to image a subject having a target site using single photon emission computed tomography (SPECT).
    Type: Application
    Filed: January 31, 2012
    Publication date: August 1, 2013
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Bruce Fletcher Johnson, Randall Lee Carter, Michael James Rishel, Mark Christopher Patrick Darey, Tao Wu, Yang Yang, John Fitzmaurice Valliant, Karin Ann Stephenson
  • Publication number: 20130184493
    Abstract: A process for preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butane amide also known as a diketone intermediate of atorvastatin, completely devoid of impurities 3,4-difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-n-?-diphenylbenzene butane amide; methyl, 2{-2[-(4-fluorophenyl)-2-oxo-1-phenylethyl)]}-4-methyl-3-oxo pentanoate; 1,4-bis(4-fluorophenyl)-2,3-diphenylbutane-1,4-dione, 1-(4-fluorophenyl)-2-phenyl ethanone; 1-(4-fluorophenyl)-2-phenyl ethanone and containing about 0.05% or less of 2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butane amide. In that process the said diketone intermediate of formula 1 is obtained by maintaining temperature ?25° C. to 50° C. during Friedel-Crafts acylation, in situ halogenation of formula II in presence of a solvent and nucleophilic substitution from a compound of formula III with formula IV in presence of a base.
    Type: Application
    Filed: October 13, 2011
    Publication date: July 18, 2013
    Applicant: VIJAYASRI ORGANICS LIMITED
    Inventors: Jagapathi Raju Srivatsavayi, Sairam Pothukuchi, Srinivasa Sastry Rani, Mallikarjuna Rao Chikka, Chiranjeevi Cheekati, Mallikarjuna Rao Gutti, Trimurthulu Singavarapu, Venkat Reddy Thimmaipally, Venkateswara Rao Tadanki
  • Publication number: 20130156701
    Abstract: The present invention provides a method for preparing [18F]—N-(4-fluorobutyl)ethacrynic amide which is prepared from radiofluorination and deprotection of the precursor tosylate N-Boc-N-[4-(toluenesulfonyloxy)-butyl)ethacrynic amide], obtained from ethacrynic acid via 6-step synthesis in 39% yield, in a radiochemical yield of 44%, aspecific activity of 48 GBq/?mol and radiochemical purity of 98%. The present invention further provides a composition for positron emission tomography (PET) of an animal models of a tumor liver or a liver disease, comprising [18F]—N-(4-fluorobutyl)ethacrynic amide and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Applicant: NATIONAL TSING HUA UNIVERSITY
    Inventor: National Tsing Hua University
  • Publication number: 20130096175
    Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.
    Type: Application
    Filed: November 17, 2010
    Publication date: April 18, 2013
    Applicants: SOUTHERN RESEARCH INSTITUTE, UNIVERSITY OF ROCHESTER
    Inventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucile White, Krister Wennerberg
  • Publication number: 20130079514
    Abstract: (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.
    Type: Application
    Filed: October 15, 2012
    Publication date: March 28, 2013
    Applicant: Dompé S.p.A.
    Inventor: Dompé S.p.A.
  • Patent number: 8367680
    Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: February 5, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen E. Blackwell, Matthew D. Bowman, Joseph R. Stringer
  • Publication number: 20130005759
    Abstract: MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.
    Type: Application
    Filed: January 21, 2011
    Publication date: January 3, 2013
    Inventors: Alexander Deiters, Douglas D. Young
  • Patent number: 8338637
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: December 25, 2012
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120238763
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: November 18, 2010
    Publication date: September 20, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki Murase, Toshihito Kumagai, Hisaya Wada, Hisahide Tanimoto, Koumei Ohta, Yoshihiro Kimura
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Publication number: 20120122784
    Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: May 26, 2010
    Publication date: May 17, 2012
    Applicant: LEO PHARMA A/S
    Inventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
  • Publication number: 20120101087
    Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.
    Type: Application
    Filed: December 12, 2008
    Publication date: April 26, 2012
    Inventors: Randall S. Alberte, Robert D. Smith
  • Patent number: 8163959
    Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: April 24, 2012
    Assignee: Arch Pharmalabs Limited
    Inventors: Ganesh Gurpur Pai, K. Nanda Kishore, Narendra P. Chaudhari, N. Anjaneyulu, B. N. Ghogare
  • Publication number: 20120093742
    Abstract: A method of modulating the flavour of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavour-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: Application
    Filed: June 24, 2010
    Publication date: April 19, 2012
    Applicant: Givaudan S.A.
    Inventors: Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
  • Publication number: 20120095051
    Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: May 14, 2010
    Publication date: April 19, 2012
    Inventors: Francis Johnson, Lorne Golub
  • Patent number: 8143449
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: March 27, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Christophe Hardouin, Jean-Pierre Lecouve
  • Publication number: 20120053346
    Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: August 30, 2011
    Publication date: March 1, 2012
    Inventor: Hubert Maehr
  • Publication number: 20120046247
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Patent number: 8110689
    Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio-C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: February 7, 2012
    Assignee: Bayer Cropsciene AG
    Inventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
  • Patent number: 8093427
    Abstract: A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: January 10, 2012
    Assignee: National Tsing Hua University
    Inventors: Chung-Shan Yu, Yuan-Hsiao Su, Li-Wu Chiang, Chia-Rong Chen, Shao-Wei Chen, Chia-Wen Huang, Ho-Lien Huang, Yin-Cheng Huang
  • Publication number: 20110306671
    Abstract: The invention provides ethacrynic acid derivatives useful to prevent, inhibit or treat a variety of disorders or diseases including cancer and inflammatory disorders.
    Type: Application
    Filed: December 16, 2009
    Publication date: December 15, 2011
    Applicant: The Regents of the The University of California
    Inventors: Dennis A. Carson, Howard B. Cottam, Guangyi Jin, Desheng Lu
  • Publication number: 20110306775
    Abstract: Disclosed are a serious of 2?,5?-dimethoxychalcone derivatives for treating cancer, wherein 2,5-dimethoxyacetophenone and methyl 4-formylbenzoate are condensed to form 4-carboxyl-2?,5?-dimethoxychalcone (compound 1), which is further reacted with alkyl halides or amines to synthesize the chalcone derivatives of compounds 2-17. In addition, 2,5-dimethoxyacetophenone is reacted with 5-formyl-2-thiophenecarboxylic acid to form compound 18 (3-(3-thiophene)carboxyl-1-(2,5-dimethoxyphenyl)prop-2-en-1-one). The synthesized 2?,5?-dimethoxychalcone derivatives can be acted as microtubule-targeted tubulin-polymerizing agents.
    Type: Application
    Filed: October 1, 2010
    Publication date: December 15, 2011
    Applicant: KAOHSIUNG MEDICAL UNIVERSITY
    Inventors: Chun-Nan Lin, Huang-Yao Tu, A-Mei Huang, Tzyh-Chyuan Hoar, Shyh-Chyun Yang, Yeong-Shiau Pu, Jan-Gowth Chang
  • Patent number: 8039513
    Abstract: The present invention relates to cis-1,2-substituted stilbene derivatives, or their pharmaceutically acceptable salts, glucosides or solvates, a pharmaceutical composition comprising the compound, and use of said compound for preparation of a drug for treatment and/or prevention of diabetes or improvement of diabetic complications.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: October 18, 2011
    Assignee: Institute of Radiation Medicine, Academy of Military Medical Sciences, PLA
    Inventors: Zhiyun Kang, Zuze Wu, Zhuangrong Sun, Zhongxiong Tang
  • Publication number: 20110218214
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Application
    Filed: September 9, 2010
    Publication date: September 8, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
  • Publication number: 20110207605
    Abstract: What is described are 3-aminocarbonyl-substituted benzoylcyclohexanediones of the formula (I) as herbicides. In this formula (I), R1 to R5 are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. X is alkylene.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 25, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Chieko UENO, Simon DÖRNER-RIEPING, Andreas VAN ALMSICK, Christopher Hugh ROSINGER, Jan DITTGEN, Dieter FEUCHT, Isolde HÄUSER-HAHN
  • Patent number: 8003819
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: August 23, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20110165606
    Abstract: The present invention relates to methods and compositions for modifying, isolating, detecting, visualizing, and quantifying citrulline and/or homocitrulline-containing peptides, polypeptides, and proteins using mono- and disubstituted glyoxal derivatives. The invention also provides kits for modifying, isolating, detecting, visualizing, and quantifying the relative amounts of citrulline and/or homocitrulline-containing peptides, polypeptides, or proteins in solutions or samples.
    Type: Application
    Filed: June 12, 2008
    Publication date: July 7, 2011
    Inventors: Astrid E.V. Tutturen, Anders Holm, Burkhard Fleckenstein