The Hetero Ring Is Six-membered Patents (Class 514/432)
  • Patent number: 11117865
    Abstract: Certain embodiments are directed to small molecule selective inhibitors of the BRD4 bromodomain. Compounds described herein can be used to modulate the bronchiolar NFkB-BRD4 axis, which plays a role in acute neutrophilic response to viral molecular patterns. Compounds described herein can be developed as preventive and therapeutic agents for various human diseases and conditions.
    Type: Grant
    Filed: June 16, 2019
    Date of Patent: September 14, 2021
    Assignee: Board of Regents, The University Of Texas System
    Inventors: Jia Zhou, Allan R. Brasier, Bing Tian, Zhiqing Liu, Haiying Chen, Erik Rytting
  • Patent number: 10961214
    Abstract: Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a generic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compound 6jc48-1 ((E)-2,4-bis(4-bromophenyl)-6-(4-(dimethyl-amino)styryl)pyrylium boron tetrafluoride salt) binds to Lipid II with high affinity, has markedly reduced cytotoxicity than BAS00127538, and retains activity against drug-resistant strains of Enterococci. It is stable in plasma, has dramatically improved pharmacokinetic and pharmacodynamics properties, and possesses in vivo efficacy in a mouse model of sepsis.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: March 30, 2021
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Erik de Leeuw, Alexander MacKerell, Steven Fletcher, Jamal Chauhan
  • Patent number: 10947198
    Abstract: Chemical compounds that inhibit cancer cell growth are provided. The compounds are heteroarotinoids and derivatives thereof with oxygen, nitrogen or sulfur in chroman systems, tetrahydroquinoline systems, and tetrahydrothiochroman systems.
    Type: Grant
    Filed: August 23, 2019
    Date of Patent: March 16, 2021
    Assignee: THE BOARD OF REGENTS FOR OKLAHOMA STATE UNIVERSITY
    Inventors: Kenneth Darrell Berlin, Richard A. Bunce, Krishna Kumar Gnanasekaran, Field M. Watts, Jr., Donghua Howard Zhou
  • Patent number: 10919835
    Abstract: Provided herein are compounds useful for the preparation of compounds that have retinoid-like biological activity. Also provided herein are processes for the preparation of compounds that have retinoid-like biological activity.
    Type: Grant
    Filed: February 24, 2020
    Date of Patent: February 16, 2021
    Assignee: Io Therapeutics, Inc.
    Inventors: Roshantha A. Chandraratna, Vidyasagar Pradeep Vuligonda, Thomas Jacks, Peter Wade, Andrew Thompson
  • Patent number: 10866140
    Abstract: Provided is a spectrophotometer having a positional relationship between the spectroscope and a PDA that is set to have a distance between a reflection position of light reflected on a light receiving surface of a corresponding one of PDs constituting the PDA, being configured to receive at least light having a wavelength of from 200 nm to 300 nm, and an incident position at which light reflected at the reflection position is incident on a light receiving surface of the PDA after being re-reflected on the protective plate, the distance being equal to or less than a width dimension of any one of the PDs constituting the PDA.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: December 15, 2020
    Assignee: Shimadzu Corporation
    Inventors: Masato Watanabe, Masahide Gunji
  • Patent number: 10722575
    Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.
    Type: Grant
    Filed: May 29, 2019
    Date of Patent: July 28, 2020
    Assignee: GENFIT
    Inventors: Raphael Darteil, Rémy Hanf, Dean Hum, Ingrid Dufour
  • Patent number: 10654822
    Abstract: Disclosed is a composition including flocoumafen and an amount of a configurational stereoisomer of flocoumafen, named enantiomer E4, such that the ratio of this amount to the amount of flocoumafen in the composition is less than 10%, the enantiomer E4 being present with the exclusion of a racemic mixture, the enantiomer E4 having, by chromatographic analysis of flocoumafen, a retention time t4 having a value such that t1<t2<t3<t4; t1, t2 and t3 representing the retention times of the configurational stereoisomers of flocoumafen different from the enantiomer E4, the chromatographic analysis being performed at a temperature of 23.5° C.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: May 19, 2020
    Assignees: LIPHATECH, INSTITUT ENSEIGNEMENT SUPERIEUR ET RECHERCHE EN ALIMENTATION SANTE ANIMALE SCIENCES AGRONOMIQUES ET ENVIRONNEMENT (VET AGRO SUP)
    Inventors: Hervé Caruel, Etienne Benoit, Isabelle Fourel, Virginie Lattard
  • Patent number: 10556878
    Abstract: A compound useful as a Sirt2 or Sirt5 inhibitor having the formula (1) wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —O—, —S—, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is —(CH2)n—; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, biological groups, and protecting groups. Also described are pharmaceutical compositions of the inhibiting compounds, and methods of treatment by administration of the inhibiting compounds.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: February 11, 2020
    Assignee: CORNELL UNIVERSITY
    Inventor: Hening Lin
  • Patent number: 10350181
    Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: July 16, 2019
    Assignee: GENFIT
    Inventors: Raphael Darteil, Rémy Hanf, Dean Hum, Ingrid Dufour
  • Patent number: 10315992
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I), or a pharmaceutically acceptable salt thereof, and its therapeutic use.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: June 11, 2019
    Assignee: Tetraphase Pharmaceuticals, Inc.
    Inventors: Xiao-Yi Xiao, Roger B. Clark, Diana Katharine Hunt, Cuixiang Sun, Magnus P. Ronn, Wu-Yan Zhang, Minsheng He
  • Patent number: 10306894
    Abstract: An essential oil blend diluted in soybean oil against the bites of Anopheles stephensi, An. gambiae (the main malaria vectors in Asia and Africa, respectively); Aedes aegypti and Ae. albopictus (the main vectors of arboviruses listed above). Repellency tests, appraising the protection time for each species, were performed under laboratory conditions using human volunteers and nulliparous female mosquitoes. The results show that the natural repellent was extraordinarily effective against both Anopheles and Aedes genera.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: June 4, 2019
    Assignee: BIOVECBLOK s.r.l.
    Inventors: Matteo Valzano, Aurelio Serrao, Claudia Damiani
  • Patent number: 10238655
    Abstract: The invention provides compounds of formula I: and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers, Alzheimer's disease, and conditions associated with demyelination.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: March 26, 2019
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Carl E. Wagner, Pamela A. Marshall, Peter W. Jurutka
  • Patent number: 10238626
    Abstract: The invention provides compounds of formula I: and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers, Alzheimer's disease, and conditions associated with demyelination.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: March 26, 2019
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Carl E. Wagner, Pamela A. Marshall, Peter W. Jurutka
  • Patent number: 10231947
    Abstract: The invention provides compounds of formula I: and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers, Alzheimer's disease, and conditions associated with demyelination.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: March 19, 2019
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Carl E. Wagner, Pamela A. Marshall, Peter W. Jurutka
  • Patent number: 10022343
    Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: July 17, 2018
    Assignee: GENFIT
    Inventors: Raphael Darteil, Rémy Hanf, Dean Hum, Ingrid Dufour
  • Patent number: 9585853
    Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: March 7, 2017
    Assignee: GENFIT
    Inventors: Raphael Darteil, Rémy Hanf, Dean Hum, Ingrid Dufour
  • Patent number: 9278078
    Abstract: A method of inhibiting excitotoxicity by indirectly activating ?4?2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of ?7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate ?4?2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: March 8, 2016
    Inventors: Peter Andrew Ferchmin, Vesna Ana Eterovic De Ferchmin, Hector Manuel Maldonado, Khalid El Sayed
  • Patent number: 9248185
    Abstract: The invention provides methods for inducing, enhancing or increasing satellite cell proliferation, and an assay for screening for a candidate compound for inducing, enhancing or increasing satellite cell proliferation. Also provided is a method for repairing or regenerating a damaged muscle tissue of a subject.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: February 2, 2016
    Assignee: President and Fellows of Harvard College
    Inventors: Lee L. Rubin, Amanda Gee, Amy J. Wagers
  • Patent number: 9221751
    Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: December 29, 2015
    Assignee: GENFIT
    Inventors: Raphael Darteil, Rémy Hanf, Dean Hum, Ingrid Dufour
  • Patent number: 9149476
    Abstract: The present invention relates to novel compounds, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: December 24, 2014
    Date of Patent: October 6, 2015
    Assignee: FIBROGEN, INC.
    Inventors: Wen-Bin Ho, Lee A. Flippin, Craig Mossman, Eric D. Turtle, Lee R. Wright
  • Patent number: 9067894
    Abstract: The present invention provides small molecule activators of GIRK potassium channels and methods for use thereof.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: June 30, 2015
    Assignee: Vanderbilt University
    Inventor: C. David Weaver
  • Patent number: 9044408
    Abstract: Cosmetic and dermatological compositions comprising N-heteroarylbisamide analogs and methods of using such compositions to impart anti-aging benefits to the skin and/or improve skin conditions resulting from reduced collagen and hyaluronic acid production are disclosed. The N-heteroarylbisamides are believed to stimulate collagen and hyaluronic acid production and restore or maintain homeostasis for these compounds.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: June 2, 2015
    Assignee: Avon Products, Inc.
    Inventors: Satish Parimoo, Nancy T. Ilaya, John W. Lyga
  • Publication number: 20150133493
    Abstract: Compounds including those of the Formula I where X, R1, R2 and subscript t are as defined herein, useful as ?-secretase inhibitors, are provided, as are compositions comprising the compounds, as well as methods for use of the compounds for treating or preventing neurodegenerative diseases, such as, for instance, Alzheimer's disease.
    Type: Application
    Filed: July 3, 2014
    Publication date: May 14, 2015
    Inventors: Lei Zhu, Hakim Djaballah, Yueming Li, Christopher Chad Shelton
  • Publication number: 20150133454
    Abstract: Provided is a nanostructured mucoadhesive microparticle including a biocompatible polymer, the microparticle having a surface with a nanostructure formed thereon. The present nanostructured mucoadhesive microparticle having an increased retention time on the mucous as well as with a minimized irritation to the surface can be advantageously used as a drug delivery vehicle. Thus the increased bioavailability of a therapeutic agent administered by the present microparticle leads to an increased therapeutic efficacy, reduced dosage and reduced number of administration as well as significant cost savings and improved patient convenience resulted therefrom.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 14, 2015
    Applicant: SNU R&DB FOUNDATION
    Inventors: Young Bin Choy, Chun Gwon Park
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • 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
  • Publication number: 20150119418
    Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Patent number: 9012493
    Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 21, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
  • Publication number: 20150099789
    Abstract: The present invention relates to a method of treatment of a mucopolysaccharidosis with 4-methyl-2-oxo-2H-1-benzopyran-7-yl-5-thio-?-D-xylopyranoside.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventor: Philippe MASSON
  • Patent number: 9000030
    Abstract: A method of inhibiting excitotoxicity by indirectly activating ?4?2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed Inhibitors of ?7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate ?4?2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 7, 2015
    Inventors: Peter Andrew Ferchmin, Vesna Ana Eterovic De Ferchmin, Hector Manuel Maldonado, Khalid El Sayed
  • Publication number: 20150087675
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds corresponding to general formula (I) are disclosed. Also disclosed, are pharmaceutical compositions including 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: March 26, 2015
    Applicant: GLADERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Patricia Rossio, Marlène Schuppli-Nollet, Laurence Clary, Jean-Guy Boiteau
  • 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: 20150045409
    Abstract: An amide compound represented by formula (I) has an excellent pest control effect. (In the formula, Y represents a 3-7 membered saturated heterocyclic ring which contains, as ring-forming components(s), one or more atoms or groups that are selected from the group consisting of an oxygen atom and —S(O)t—, the saturated heterocyclic ring may have one to three atoms or groups selected from group D and t represents 0 or the like; X represents a C1-C10 chain hydrocarbon group which may have one or more atoms or groups that are selected from group A, or the like; W represents —CR8— or the like; r represents 1 or the like; R1, R2, R3, R4, R5, R6, R7 and R8 may be the same or different and each represents a hydrogen atom or the like; and n represents 1 or the like.
    Type: Application
    Filed: February 5, 2013
    Publication date: February 12, 2015
    Inventors: Hideki Ihara, Tomotsugu Awano, Jun Ohshita, Noritada Matsuo
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150023868
    Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.
    Type: Application
    Filed: February 21, 2014
    Publication date: January 22, 2015
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Othon Iliopoulos, Michael Zimmer
  • Publication number: 20150025110
    Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 22, 2015
    Inventors: Henrietta Dehmlow, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Hans Richter
  • Patent number: 8927591
    Abstract: The present invention relates to novel compounds, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: January 6, 2015
    Assignee: Fibrogen, Inc.
    Inventors: Wen-Bin Ho, Lee R. Wright, Eric D. Turtle, Craig Mossman, Lee A. Flippin
  • Patent number: 8889731
    Abstract: This invention relates to compositions of one or more compounds that incorporate one or more allyl sulfide, allyl disulfide or allyl polysulfide moieties, or one or more allyl sulfide, allyl disulfide or allyl polysulfide moieties and one or more hydroxyl groups, used in effective amount in formulations, including emulsions, to repel blood-feeding ectoparasitic arthropods, including mosquitoes, and to deter them from landing and feeding when applied to the skin, clothing or environment of animals, including humans. Said compounds can include, but are not limited to, 8-allyl-sulfanyloctan-1-ol. This invention also relates to compositions comprising one or more of said compounds in further combination with other arthropod repellent and deterrent compounds, including vanillin. These compounds may be formulated with inert ingredients to form a liquid, gel, paste, soap, spray, aerosol or powder.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: November 18, 2014
    Assignee: Contech Enterprises Inc.
    Inventors: Regine M. Gries, Gerhard G. Gries, Grigori Khaskin, Norman Avelino, Cory Campbell
  • Publication number: 20140323530
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: March 26, 2014
    Publication date: October 30, 2014
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, Ryo Kubota
  • Publication number: 20140303166
    Abstract: The current application is directed to cosmetic methods for changing the appearance of eyes by causing a retraction of the eyelids so that the eyes appear to be more open and have a wider appearance. Various methods involve application of one or more prostaglandins, synthetic prostaglandins, including synthetic prostaglandin F, and synthetic prostaglandin analogues, to eyelids, which results in contraction of eyelid muscles and a wider, more open appearance of the eyes.
    Type: Application
    Filed: April 8, 2013
    Publication date: October 9, 2014
    Inventor: Gordon C. Tang
  • Patent number: 8853258
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: October 7, 2014
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20140296285
    Abstract: A method of inhibiting microorganism growth comprising administering an effective amount of a composition including a compound selected from the group consisting of to the microorganism.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Gengliang YANG, Zhengyue MA, Wei TIAN, Baoling FANG, Ge WANG, Linbo LI, Chunliu YANG, Ligai BAI
  • Publication number: 20140275043
    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 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said 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: March 11, 2014
    Publication date: September 18, 2014
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20140275008
    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: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • 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
  • Publication number: 20140235665
    Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: SUCAMPO AG
    Inventor: Ryuji UENO
  • Publication number: 20140228405
    Abstract: The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like.
    Type: Application
    Filed: August 8, 2012
    Publication date: August 14, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Naoki Tomita, Shigeo Kajii, Douglas Robert Cary, Daisuke Tomita, Shinichi Imamura, Ken Tsuchida, Satoru Matsuda, Ryujiro Hara
  • Publication number: 20140213617
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: January 23, 2014
    Publication date: July 31, 2014
    Applicant: ACUCELA INC.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20140171490
    Abstract: Disclosed is the use of a mist of a pharmaceutical composition for ophthalmic delivery of a protein or peptide active pharmaceutical ingredient, a related method of treatment and a device useful in implementing the use and method. Disclosed is also the use of a mist for ophthalmic delivery of a pharmaceutical composition including a highly irritating penetration enhancer and an ophthalmically acceptable carrier, a related method of treatment and a device useful in implementing the use and method. Disclosed is also a device for ophthalmic administration configured to direct a mist of a pharmaceutical composition to the eye only when the eye is open. Disclosed is also a self-sterlizing device for ophthalmic administration. Disclosed is also a device and a method for increasing the bioavailability of an ophthalmically administered API in a pharmaceutical composition.
    Type: Application
    Filed: August 9, 2013
    Publication date: June 19, 2014
    Applicant: PHARMALINGT INC.
    Inventors: Yossi Gross, Rafi Herzog, Steven B. Koevary