Additional Hetero Ring Patents (Class 514/444)
  • Patent number: 9642842
    Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: May 9, 2017
    Assignee: Trevana, Inc.
    Inventors: Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan
  • Patent number: 9321753
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: April 26, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Eda Canales, Michael O'Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Philip Anthony Morganelli, William J. Watkins
  • Patent number: 9309234
    Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: April 12, 2016
    Assignee: Trevena, Inc.
    Inventors: Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan
  • Publication number: 20150126559
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 7, 2015
    Applicant: UNIVERSITA DEGLI STUDI DI FERRARA
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Patent number: 9024042
    Abstract: Compositions and methods for treating glaucoma are provided. In particular hydrophilic ester prodrugs and their use to reduce central corneal thickening is provided.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: May 5, 2015
    Assignee: Allergan, Inc.
    Inventors: Wha-Bin Im, Robert M. Burk
  • Patent number: 9012490
    Abstract: Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: April 21, 2015
    Assignee: Howard University
    Inventors: Evaristus A. Nwulia, Amol Kulkarni
  • Publication number: 20150099733
    Abstract: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 9, 2015
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takahiro KOSHIBA, Munetaka TOKUMASU, Taisuke ICHIMARU, Koji OHSUMI, Tadakiyo NAKAGAWA, Tatsuhiro YAMADA, Kayo MATSUMOTO, Tamotsu SUZUKI
  • Publication number: 20150080349
    Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
    Type: Application
    Filed: July 10, 2014
    Publication date: March 19, 2015
    Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20150065343
    Abstract: The present invention relates to acrylamide compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes, and to a method for producing them. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Pascal Bindschaedler, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Ralph Paulini, Deborah L. Culbertson, Paul Neese, Franz Josef Braun
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Publication number: 20150031658
    Abstract: This invention relates generally to the discovery of a method of inhibiting, preventing or treating bacterial infections. The invention also relates to a method of inhibiting bacterial capsule biogenesis.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Patrick C. Seed, Carlos C. Goller, Apurba Dutta, Brooks Maki, Frank Schoenen, James Noah, Lucile White
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20150018330
    Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 15, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
  • Publication number: 20150018371
    Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Publication number: 20150005319
    Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 1, 2015
    Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Patent number: 8916183
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Publication number: 20140348880
    Abstract: A method for treating or preventing a microbial infection in a subject in need thereof, the method comprising administering to the subject, a therapeutically effective amount of a compound of Formula Ia, a compound of Formula IIa, one or more compounds of Formula Ia or Formula IIa complexed with a metal core, or a pharmaceutically acceptable salt, prodrug or hydrate thereof.
    Type: Application
    Filed: May 23, 2014
    Publication date: November 27, 2014
    Inventors: Matthias Bierenstiel, Harshiny Muthukumar
  • Patent number: 8895608
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: November 25, 2014
    Assignee: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Publication number: 20140341776
    Abstract: Thiophene containing water-soluble oligomers were synthesized and characterized. The photophysical properties of these compounds were studied; transient absorption spectroscopy was used to probe the triplet excited state and their ability to sensitize singlet oxygen was spectroscopically monitored in deuterated methanol. The above compounds were tested for their light activated biocidal properties against S. aureus both under UV and visible radiation. Among the oligomers studied, the terthiophene derivative was found to kill the bacteria efficiently.
    Type: Application
    Filed: July 5, 2012
    Publication date: November 20, 2014
    Applicants: STC.UNM, University of Florida Reearch Foundation, Inc.
    Inventors: Kirk S. Schanze, Anand Parthasarathy, Subhadip Goswami, David G. Witten, Eunkyung Ji, Thomas S. Corbitt, Dimitri Dascier
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Publication number: 20140329809
    Abstract: A process for the characterization of rosacea is disclosed. The process can include identifying for the first time new markers in leukocyte recruitment as well as the therapeutic applications targeting rosacea.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 6, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Isabelle Carlavan, Martin Steinhoff
  • Publication number: 20140323502
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Application
    Filed: February 13, 2014
    Publication date: October 30, 2014
    Inventors: Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Patent number: 8871946
    Abstract: The present invention relates to the benzimidazole-4-carboxamide derivatives, their preparation methods, pharmaceutical compositions and their uses; wherein X represents monosubstituted or bissubstituted or polysubstitued C1-C14 alkoxy, monosubstituted or bisubstituted or polysubstitued C1-C14 alkyl, monosubstituted or bisubstituted or polysubstitued C2-C14 alkenyl, monosubstituted or bisubstituted or polysubstitued C6-C14 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom; Y represents hydrogen, monosubstituted or bisubstituted or polysubstitued C1-C16 alkyl, monosubstituted or bisubstituted or polysubstitued C6-C12 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: October 28, 2014
    Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory
    Inventors: Xianjin Luo, Fei Xue, Zhonglv Zhang, Naiyun Xiu
  • Publication number: 20140315845
    Abstract: The invention provides 19-substituted geldanamycin derivatives, and pharmaceutically acceptable salts thereof that are potent Hsp90 binding agents useful for the treatment of, and/or the amelioration of symptoms of, cancer or neurodegenerative disorders.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 23, 2014
    Inventors: David Ross, David Siegal, Christopher J. Moody, Russell Richard Anthony Kitson
  • Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Publication number: 20140309187
    Abstract: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Ahmad Hashash, Scott Wolckenhauer, Bing Shi
  • Patent number: 8859611
    Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: October 14, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventor: Xicheng Sun
  • Publication number: 20140302137
    Abstract: The present invention is directed a pharmaceutical compositions for co-therapy treatment and prevention of glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Urbain Alfons Clementina Delaet, Anne Faure, Philip Erna Hortentia Gilbert Heyns, Eugeen Maria Jozef Jans, Aniruddha Railkar
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Patent number: 8853196
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: October 7, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
  • Publication number: 20140296256
    Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Toshio MIYATA, Kenji MURANO, Nagahisa YAMAOKA, Akihisa MAEDA
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Patent number: 8841340
    Abstract: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: September 23, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Ahmad Hashash, Scott Wolckenhauer, Bing Shi
  • Publication number: 20140275179
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Chaozhong Cai, Xuqing Zhang
  • Publication number: 20140275185
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Patent number: 8835654
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 16, 2014
    Assignee: BHI Limited Partnership
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Patent number: 8835476
    Abstract: The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: September 16, 2014
    Inventors: Fan Wu, Donald Weaver, Chris Barden, Christopher McMaster, David Byers, Annette Henneberry, Fuqiang Ban
  • Patent number: 8835488
    Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: September 16, 2014
    Assignee: Trevena, Inc.
    Inventors: Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan
  • Publication number: 20140242148
    Abstract: The invention provides methods and materials for decontamination of surfaces and fabrics, such as non-woven fabrics, that are contaminated with infestations of microorganisms such as bacteria. Biocidal oligomers having conjugated oligo-(aryl/heteroaryl ethynyl) structures and comprising at least one cationic group can be used to decontaminate infested surfaces in the presence of oxygen and, optionally, illumination. Fibers incorporating biocidal oligomers having conjugated oligo-(aryl/heteroaryl ethynyl) structures and comprising at least one cationic group, wherein the oligomer is physically associated with or covalently bonded to, or both, the fiber-forming polymer can be used to form non-woven mats. Biocidal non-woven mats prepared by methods of the invention, incorporating the biocidal oligomers, can be used to suppress bacterial growth in wound and surgical dressings and personal hygiene products.
    Type: Application
    Filed: August 3, 2012
    Publication date: August 28, 2014
    Applicant: University of Florida Research Foundation, Inc.
    Inventors: David G. Whitten, Kirk S. Schanze, Eunkyung Ji, Dimitri Dascier, Anand Parthasarathy, Thomas S. Corbitt, Kirsten Cicotte, Elizabeth LeBleu Dirk, Xuzhi Zhu
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Publication number: 20140171444
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 19, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi