The Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/472)
  • Patent number: 9205073
    Abstract: A method for treating a virus infection in a subject is provided. The method comprising administering to the subject in need an effective amount of a derivative of aniline selected from the group consisting of a compound of formula (I), a pharmaceutically acceptable salt of the compound of formula (I), a pharmaceutically acceptable ester of the compound of formula (I), and combinations thereof: wherein, R1 is C1 to C10 alkyl; R2 is H or C1 to C4 alkyl; and R3, R4, R5, R6 and R7 are independently H, —OH, halogen, C1 to C10 alkyl, C1 to C10 alkoxyl, or (C1 to C10 alkylene)-O—O—(C1 to C10 alkyl).
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: December 8, 2015
    Assignee: CHINA MEDICAL UNIVERSITY
    Inventors: Cheng-Wen Lin, An-Cheng Huang, Jin-Cherng Lien, Jia-Fong Ping, Shih-Wen Li, I-Chieh Chen
  • 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: 20150025042
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 16, 2013
    Publication date: January 22, 2015
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Publication number: 20150010643
    Abstract: This invention relates to a method of treating B cell malignancies, which involves administering to a subject a compound having a structure of formula (I) to cause cell death of a B cell malignancy, thereby treating the B cell malignancy in the subject. Also disclosed are a method of causing cell death of malignant B cells, pharmaceutical compositions and therapeutic systems comprising a compound having a structure of formula (I), and a compound having a structure of formula (I).
    Type: Application
    Filed: February 15, 2013
    Publication date: January 8, 2015
    Applicant: UNIVERSITY OF ROCHESTER
    Inventor: Jiyong Zhao
  • Publication number: 20150004216
    Abstract: A medicant composition is provided. The composition includes a film layer and a powder matrix layer. The powder matrix layer includes a medicant. The powder matrix layer is applied to the film layer by admixing particulate to form a powder matrix and by then applying the powder matrix to the film layer by any desired method. The composition of the powder matrix is varied to alter the dissolution rate of the medicant, the adhesion of the medicant composition, and other physical properties of the powder matrix. The powder matrix layer can be cured.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 1, 2015
    Inventor: Robert Steven Davidson
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • 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
  • 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
  • Patent number: 8815943
    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: Grant
    Filed: February 22, 2011
    Date of Patent: August 26, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen E. Blackwell, Grant D. Geske, Jennifer C. O'Neill
  • Publication number: 20140235683
    Abstract: Compositions and methods for the treatment of norovirus infection are disclosed.
    Type: Application
    Filed: July 9, 2012
    Publication date: August 21, 2014
    Applicants: Alios Biopharma Inc., Indiana University Research & Technology Corporation
    Inventors: Ch. V. Subba-Reddy, C. Cheng Kao, Dave Smith, Leo Beigelman
  • Publication number: 20140200241
    Abstract: Disclosed are methods of inhibiting the growth of pathogens using prodrug compounds as described herein. Also disclosed are methods of treating microbial infections using such compounds.
    Type: Application
    Filed: May 24, 2012
    Publication date: July 17, 2014
    Applicant: Northeastern University
    Inventors: Kim Lewis, Laura Fleck, Gabriele Casadei
  • Publication number: 20140194507
    Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 10, 2014
    Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
  • Publication number: 20140147529
    Abstract: The present invention relates to a method for reducing the production of methane emanating from the digestive activities of a ruminant and/or for improving ruminant animal performance by using, as active compound at least one organic molecule substituted at any position with at least one nitrooxy group, or a salt thereof, which is administrated to the animal together with the feed. The invention also relates to the use of these compounds in feed and feed additives such as premix, concentrates and total mixed ration (TMR) or in the form of a bolus.
    Type: Application
    Filed: December 20, 2011
    Publication date: May 29, 2014
    Applicant: DSM IP ASSETS B.V.
    Inventors: Stephane Duval, Maik Kindermann
  • Publication number: 20140148398
    Abstract: Compounds useful for the treatment of giardiasis are described.
    Type: Application
    Filed: October 12, 2011
    Publication date: May 29, 2014
    Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, UNIVERSITY OF MARYLAND, COLLEGE PARK
    Inventors: Wei Zheng, Catherine Chen, Juan Jose Marugan, Noel Southall, Christopher P. Austin, Andrey Galkin, Liudmila Kulakova, Osnat Herzberg
  • Publication number: 20140107161
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 12, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140094494
    Abstract: A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole.
    Type: Application
    Filed: September 17, 2013
    Publication date: April 3, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Bruce Steven Klein, Brad Mark Tebbets
  • Patent number: 8658693
    Abstract: The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: February 25, 2014
    Assignee: Eli Lilly and Company
    Inventors: Jonathan Edward Green, Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Donald Paul Matthews, Ashraf Saeed, Gregory Alan Stephenson
  • Patent number: 8653120
    Abstract: Chronic pain is treated in an individual suffering from chronic pain by administering to the individual an amount of a therapeutic containing a glycine receptor agonist such as D-cycloserine or a GlyT-1 glycine transporter antagonist such as sarcosine in an amount effective to treat the chronic pain. The therapeutic may also contain a secondary analgesic such as opiates, NSAIDs or cox-2 inhibitors. The analgesic can be formulated in a pharmaceutical composition in the form of an injectable solution that contains at least two different analgesics, at least one of the analgesics of which is a glycine receptor agonist or a GlyT-1 glycine transporter antagonist. Suitable pharmaceutical compositions contain D-cycloserine and/or sarcosine, optionally in combination with opiates, NSAIDs or cox-2 inhibitors.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: February 18, 2014
    Assignee: Apkarian Technologies LLC
    Inventor: A. Vania Apkarian
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Publication number: 20140024707
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Application
    Filed: July 17, 2012
    Publication date: January 23, 2014
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 8609718
    Abstract: Disclosed is a novel use of phytosphingosine. More particularly, disclosed are a composition for preventing or treating hyper-proliferative skin diseases comprising pachastrissamine as an active ingredient, a use of pachastrissamine or a pharmaceutically acceptable salt thereof for preparing a preventing/therapeutic agent of hyper-proliferative skin diseases, and a method for treating hyper-proliferative skin diseases administering an effective amount of pachastrissamine or a pharmaceutically acceptable salt thereof to a subject in need thereof. The pachastrissamine inhibits the degradation of FoxO3a protein and increases the expression of FoxO3a protein. Thus, the inventive pharmaceutical composition has a preventing of treating effect on hyper-proliferative diseases by inducing apoptosis of hyper-proliferative cells and inhibiting the cell cycle.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: December 17, 2013
    Assignee: Catholic University Industry Academy Cooperation Foundation
    Inventors: Dong Heon Shin, Tae Yoon Kim
  • Publication number: 20130331328
    Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.
    Type: Application
    Filed: February 14, 2012
    Publication date: December 12, 2013
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
  • Patent number: 8552033
    Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: October 8, 2013
    Assignee: SANOFI
    Inventors: Stephanie Hachtel, Juergen Dedio, Stephen Shimshock, Carolina Lanter
  • Patent number: 8546444
    Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.
    Type: Grant
    Filed: May 28, 2012
    Date of Patent: October 1, 2013
    Assignee: Magnachem International Laboratories, Inc.
    Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Patent number: 8518968
    Abstract: Disclosed herein are novel hydrazone and diacyl hydrazine derivatives that are inhibitors of the endoplasmic reticulum-associated protein degradation (ERAD) pathway. Also disclosed are hydrazone and diacyl hydrazine derivatives as potent and selective inhibitors of the p97 ATPase. These agents provide useful tools for the study of protein degradation and other processes involving p97. Methods of treating diseases or disorders for which p97 inhibition and/or ER stress induction is an effective treatment with certain hydrazone and diacyl hydrazine derivatives are also disclosed.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: August 27, 2013
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Adrian Wiestner, Yihong Ye, Qiuyan Wang, William C. Trenkle, Bidhan A. Shinkre
  • Publication number: 20130217762
    Abstract: The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
    Type: Application
    Filed: October 5, 2012
    Publication date: August 22, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventor: Eli Lilly and Company
  • Patent number: 8507554
    Abstract: In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well.
    Type: Grant
    Filed: May 3, 2007
    Date of Patent: August 13, 2013
    Assignee: Seoul National University Industry Foundation
    Inventors: Je-Yong Yoon, Cheol-Jin Kim, Jae-Eun Kim, Hyung-Yeon Park
  • Publication number: 20130156816
    Abstract: The invention features compositions, methods, and kits for the administration of an oxidatively transformed carotenoid, or a fractionated component thereof, for use in aquaculture.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 20, 2013
    Applicant: Chemaphor Inc.
    Inventors: Larry Arthur Stobbs, James Gary Nickerson, Clayton Paul Dick
  • Publication number: 20130143841
    Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.
    Type: Application
    Filed: January 29, 2013
    Publication date: June 6, 2013
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventor: UNIVERSITY OF NOTRE DAME DU LAC
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Publication number: 20130060208
    Abstract: The present invention relates to wound care products, devices and methods incorporating acetic acid for the treatment of bacterial infections, in particular bacterial biofilm infections. In particular it relates to a wound care product comprising acetic acid, wherein the product comprises at least one further antibacterial compound; a delivery system comprising a container connected to a means of delivery which is connected to a pad, wherein said container comprises a composition comprising acetic acid and said pad comprises a self-adhesive material; a kit comprising a dressing and an adhesive membrane, wherein the dressing comprises a composition comprising acetic acid; a method of treating a wound comprising a) applying acetic acid to the wound and b) applying a negative pressure to the wound.
    Type: Application
    Filed: December 21, 2010
    Publication date: March 7, 2013
    Applicants: RIGSHOSPITALET, COPENHAGEN UNIVERSITY HOSPITAL, BISPEBJERG HOSPITAL, DANMARKS TEKNISKE UNIVERSITET
    Inventors: Michael Christian Givskov, Thomas Bjarnsholt, Klaus Kirketerp-Møller
  • Patent number: 8389566
    Abstract: The present invention relates to cyclopentane heptenoic acid-5-cis-2-(3?-hydroxy or lower alkyloxy-5-thienylpentyl)-3, 5-dihydroxy, [1?, 2?, 3?, 5?] compounds, lower alkyl, hydroxyl lower alkyl and indole lower alkyl amides and esters thereof as potent ocular hypotensives that are particularly suited for the management of glaucoma.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: March 5, 2013
    Assignee: Allergan, Inc.
    Inventor: Robert M. Burk
  • Publication number: 20130005712
    Abstract: The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivatives represented by general formula (I) being useful as an insecticide or acaricide and one or more compounds selected from the compounds having insecticidal, acaricidal or nematocidal activity: wherein R1, R2 and R3 may be the same or different and each represent hydrogen atom, C3-C6 cycloalkyl, -A1--Qp, etc., each of X and Y may be the same or different and represents hydrogen atom, halogen atom, etc., n is an integer of 1 to 4, m is an integer of 1 to 5, and each of Z1 and Z2 represents O or S.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Inventors: Kazuyuki Sakata, Masayuki Morimoto, Hiroshi Kodama, Tetsuyosi Nishimatsu
  • Publication number: 20120322823
    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: August 28, 2012
    Publication date: December 20, 2012
    Inventors: Anton F. J. Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara E. Segelstein
  • Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • Publication number: 20120316198
    Abstract: Disclosed herein are novel hydrazone and diacyl hydrazine derivatives that are inhibitors of the endoplasmic reticulum-associated protein degradation (ERAD) pathway. Also disclosed are hydrazone and diacyl hydrazine derivatives as potent and selective inhibitors of the p97 ATPase. These agents provide useful tools for the study of protein degradation and other processes involving p97. Methods of treating diseases or disorders for which p97 inhibition and/or ER stress induction is an effective treatment with certain hydrazone and diacyl hydrazine derivatives are also disclosed.
    Type: Application
    Filed: December 3, 2010
    Publication date: December 13, 2012
    Applicant: The United States of American, as Represented by the Secretary, Dept. of Health and Human Services
    Inventors: Adrian Wiestner, Yihong Ye, Qiuyan Wang, William C. Trenkle, Bidhan A. Shinkre
  • Publication number: 20120232028
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Application
    Filed: May 21, 2012
    Publication date: September 13, 2012
    Applicant: Tobira Therapeutics, Inc.
    Inventors: Mitsuru SHIRAISHI, Masanori BABA, Katsuji AIKAWA, Naoyuki KANZAKI, Masaki SETO, Yuji IIZAWA
  • Publication number: 20120202738
    Abstract: There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhoea, chronic idiopathic nausea, IBD-associated constipation and diarrhoea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 9, 2012
    Inventor: Thomas Julius Borody
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Publication number: 20120184608
    Abstract: The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough.
    Type: Application
    Filed: January 18, 2011
    Publication date: July 19, 2012
    Inventor: Edward Tak Wei
  • Publication number: 20120178780
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: March 19, 2012
    Publication date: July 12, 2012
    Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
  • Publication number: 20120148651
    Abstract: According to one embodiment, a coagulant comprising calcium nitrate and an antimicrobial agent is disclosed. The coagulant may be used in the molding process to releasably bond the substrate material to the mold and to bond to the antimicrobial to the substrate material.
    Type: Application
    Filed: December 10, 2010
    Publication date: June 14, 2012
    Applicant: MEDLINE INDUSTRIES INC.
    Inventors: Samuel T. Amdur, Min Yao
  • Publication number: 20120135925
    Abstract: Inhibitors of bacterial communication, such as quorum sensing, and method of use and manufacture thereof.
    Type: Application
    Filed: July 4, 2010
    Publication date: May 31, 2012
    Inventors: Michael M. Meijler, Josep Rayo, Neri Amara
  • Patent number: 8188145
    Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.
    Type: Grant
    Filed: April 18, 2005
    Date of Patent: May 29, 2012
    Assignee: Magnachem International Laboratories, Inc.
    Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
  • Patent number: 8183287
    Abstract: The present invention provides compositions as well as kits and methods based on a selective antagonist of either CXCR2 or both CXCR1 and CXCR2 that are useful for treating inflammatory disorders.
    Type: Grant
    Filed: June 12, 2007
    Date of Patent: May 22, 2012
    Assignee: Schering Corporation
    Inventors: Jim H. Kou, Jonathan D. Eichman
  • Publication number: 20120122877
    Abstract: The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in S. aureus. The compositions also have the ability to inhibit growth of S. aureus and as such are useful as antibiotic compounds.
    Type: Application
    Filed: July 1, 2010
    Publication date: May 17, 2012
    Applicant: TRUSTEES OF DARTMOUTH COLLEGE
    Inventors: Ambrose Cheung, Zhibiao Fu
  • Patent number: 8163796
    Abstract: A novel treatment regimen is described for the control and elimination of cancer cell populations including cancer stem cells. The disclosed protocol consists of a pretreatment step followed by a treatment step. The pretreatment step sensitizes cancer cells to apoptosis by altering their intracellular oxidation-reduction state via reduced glutathione depletion. The treatment step involves the sequential administration of a cancerostatic dicarbonyl compound to induce apoptosis. The use of nanoparticle delivery systems further enhances both the pharmacokinetic and pharmacodynamic properties of the pretreatment compounds and the cancerostatic dicarbonyls. Since the pretreatment and treatment compounds are carefully selected and delivered, normal cells are not affected and side effects are kept to a minimum.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: April 24, 2012
    Assignee: BioChemical Solutions, LLC
    Inventors: Morris A. Johnson, Michael M. Smits
  • Publication number: 20120071430
    Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.
    Type: Application
    Filed: November 1, 2011
    Publication date: March 22, 2012
    Applicant: Los Alamos National Laboratory
    Inventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks