Imidazoles Patents (Class 514/396)
  • Patent number: 9018240
    Abstract: Provided are pharmaceutical compositions, and methods of use of the compositions, for the non-surgical treatment of ptosis (eyelid droop). In one embodiment the composition includes oxymetazoline 0.1% formulated for topical administration to an eye. In one embodiment the composition includes a synergistic combination of oxymetazoline and phenylephrine, formulated for topical administration to an eye. Oxymetazoline alone causes no pupillary dilation (mydriasis), and a synergistic combination of oxymetazoline and phenylephrine induces no clinically significant mydriasis. In addition to providing desirable cosmetic effects, the compositions and methods of the invention can improve visual fields otherwise compromised by ptosis.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: April 28, 2015
    Assignee: Voom, LLC
    Inventor: Mark Silverberg
  • Patent number: 9012483
    Abstract: The present invention discloses the use of L-Histidine to reduce Gadolinium accumulation into target organs, preventing its toxic effects, after administration of gadolinium based contrast agents. The invention thus, also disclose the use of L-Histidine to prevent the NSF syndrome in patients with renal functionality impairment. A kit of part is also disclosed by the use of which toxicity associated to free Gd3+, deriving from GDBCA, is prevented by oral administration of L-histidine before administration of the contrast agent. A method for the prevention of toxic metal accumulation which consists in the administration, preferably by the oral route, of L-Histidine is also disclosed. L-Histidine is preferably administered as a single oral dose comprised from 0.2-20 g.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: April 21, 2015
    Assignee: Bracco Imaging S.p.A.
    Inventors: Baranyai Zsolt, Ernö Brücher, Simona Bussi, Alessandro Maiocchi, Fulvio Uggeri
  • Publication number: 20150098980
    Abstract: Aspects of the invention include transdermal delivery devices for delivering dexmedetomine to a subject, where the transdermal delivery devices include a single layer matrix dexmedetomine composition. Transdermal delivery devices according to certain embodiments include dexmedetomidine and a pressure sensitive adhesive provided as a single layer formulation. Also provide are methods of using the subject transdermal delivery devices to deliver dexmedetomidine to a subject, as well as kits containing the transdermal delivery devices.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Adchara Pongpeerapat, Amit Jain, Bret Berner, Jianye Wen, Jutaro Shudo
  • Publication number: 20150098982
    Abstract: Aspects of the invention include methods of managing pain in a subject by applying a transdermal delivery device containing a dexmedetomidine composition formulated to deliver a pain relieving effective amount of dexmedetomidine to a subject experiencing pain. In practicing methods according to certain embodiments, a transdermal delivery device having a dexmedetomidine composition is applied to a subject and is maintained in contact with the subject in a manner sufficient to deliver an amount of dexmedetomidine effective to manage pain in the subject. Also provided are transdermal delivery devices configured to deliver dexmedetomidine sufficient for practicing the subject methods, as well as kits containing the transdermal delivery devices.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Adchara Pongpeerapat, Amit Jain, Bret Berner, Jianye Wen, Jutaro Shudo
  • Publication number: 20150098997
    Abstract: Aspects of the invention include methods of treating ADHD, anxiety or insomnia by applying a transdermal delivery device containing a dexmedetomidine composition formulated to deliver an amount of dexmedetomidine to a subject diagnosed as having ADHD, anxiety or insomnia. In practicing methods according to certain embodiments, a transdermal delivery device having a dexmedetomidine composition is applied to a subject and is maintained in contact with the subject in a manner sufficient to deliver an amount of dexmedetomidine sufficient to treat ADHD, anxiety or insomnia in the subject. Also provided are transdermal delivery devices configured to deliver an amount of dexmedetomidine sufficient for practicing the subject methods, as well as kits containing the transdermal delivery devices.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Adchara Pongpeerapat, Amit Jain, Bret Berner, Jianye Wen, Jutaro Shudo
  • Publication number: 20150098983
    Abstract: Aspects of the invention include methods of treating withdrawal syndrome by applying a transdermal delivery device containing a dexmedetomidine composition formulated to deliver a non-sedative amount of dexmedetomidine to a subject diagnosed as having withdrawal syndrome. In practicing methods according to certain embodiments, a transdermal delivery device having a dexmedetomidine composition is applied to a subject and is maintained in contact with the subject in a manner sufficient to deliver a non-sedative amount of dexmedetomidine to treat withdrawal syndrome in the subject. Also provided are transdermal delivery devices configured to deliver a non-sedative amount of dexmedetomidine sufficient for practicing the subject methods, as well as kits containing the transdermal delivery devices.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Adchara Pongpeerapat, Amit Jain, Bret Berner, Jianye Wen, Jutaro Shudo
  • Publication number: 20150098981
    Abstract: Aspects of the invention include methods for applying to a subject a transdermal delivery device configured to deliver a non-sedative amount of a dexmedetomidine composition. In practicing methods according to certain embodiments, a non-sedative amount of a dexmedetomidine composition is transdermally applied to a subject and is maintained in contact with the subject in a manner sufficient to deliver a non-sedative amount of dexmedetomidine to a subject. Also provided are transdermal delivery devices having a non-sedative amount of dexmedetomidine sufficient for practicing the subject methods, as well as kits containing the transdermal delivery devices.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Adchara Pongpeerapat, Amit Jain, Bret Berner, Jianye Wen, Jutaro Shudo
  • Patent number: 9000021
    Abstract: Methods of treating bendamustine responsive conditions in patients having fluid and/or sodium intake restrictions are disclosed. The methods include identifying patients having such restrictions and in need of bendamustine, and then administering thereto a bendamustine-containing composition in a volume of about 120 ml or less intravenously over a period of about 15 minutes or less. The smaller volumes and reduced sodium load as compared to currently known methods of treatment minimize cardiac and/or renal stress in patients having diseases such as congestive heart failure or renal disease.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: April 7, 2015
    Assignee: Eagle Pharmaceuticals, Inc.
    Inventors: Srikanth Sundaram, Scott L. Tarriff
  • Patent number: 8999938
    Abstract: The ophthalmic drug delivery vehicles provide comfort and compliance; drug solubility, residence time and permeability; and reduce side effects. In addition, the delivery vehicle can be slightly modified to provide an artificial tear formulation.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: April 7, 2015
    Assignee: GNT LLC
    Inventor: Gerald Horn
  • Patent number: 8975289
    Abstract: This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I): where Ar represents aryl, imidazolil, 1,2,4-triazolyl, benzimidazolil; R1, R2, R4 and R5 are independently hydrogen, halogen, C1-6 alkyl; R3 represents halogen, C1-6alkyl or O—R? where R? represents hydrogen or lower alkyl; R6 represents aryl, substituted aryl, trifluoromethyl, trichloromethyl or O—R? where R? represents hydrogen or lower alkyl; being the substituents of the aryl a halogen or a radical tetrazolyl; n and m represent independently an integer between 0 and 5; With the proviso that when Ar is imidazolil, R3 is chlorine, R6 is p-phenyl and R1, R2, R4 and R5 are hydrogen, n must be different from 2. When n and m are not 0 and 1, R3 or R6 can be represented by substituents not necessarily equal.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: March 10, 2015
    Assignee: Biolab Sanus Farmaceutical Ltda.
    Inventors: Artur Franz Keppler, Sérgio Luiz Sacurai, Marcio Henrique Zaim, Carlos Eduardo da Costa Touzarim
  • Patent number: 8969372
    Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: March 3, 2015
    Assignee: Aptose Boisciences Inc.
    Inventors: Mario Huesca, Raed Al-Qawasmeh, Aiping H. Young, Yoon Lee
  • Patent number: 8969395
    Abstract: Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: March 3, 2015
    Assignee: Universidade de Coimbra
    Inventors: Jorge Antonio Ribeiro Salvador, Rita Catarina Mendes Dos Santos, Marta Cascante Serratosa
  • Patent number: 8962668
    Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: February 24, 2015
    Assignee: Arcion Therapeutics, Inc.
    Inventor: James N. Campbell
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20150018293
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Application
    Filed: May 12, 2014
    Publication date: January 15, 2015
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Patent number: 8933112
    Abstract: A novel method and composition is disclosed for treating burn injuries on human skin by promoting healing of the damaged skin. In particular, a topical liquid drug formulation is used to treat burn injuries caused by exposure of the skin to heat (thermal burns), the sun or ultraviolet radiation (sunburn), ionizing radiation (radiation burns), chemicals (chemical burns) and electricity (electrical burns). The topical burn treatment liquid contains clotrimazole as the active pharmaceutical ingredient to promote the healing of the burn damaged skin by reducing the edema, erythema, blistering, pain and other symptoms associated with burns, as well as preventing the spread of the burn damage and promoting healing.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: January 13, 2015
    Assignee: Memphaceuticals, LLC
    Inventors: Lee K. Roberts, William L. Hickerson, Douglas B. Learn
  • Publication number: 20150011601
    Abstract: This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds in combination with substituted imidazole compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to an animal in need thereof.
    Type: Application
    Filed: September 23, 2014
    Publication date: January 8, 2015
    Applicant: MERIAL LIMITED
    Inventor: Charles Q. Meng
  • Publication number: 20140378401
    Abstract: The ophthalmic drug delivery vehicles provide comfort and compliance; drug solubility, residence time and permeability; and reduce side effects. In addition, the delivery vehicle can be slightly modified to provide an artificial tear formulation.
    Type: Application
    Filed: December 18, 2013
    Publication date: December 25, 2014
    Applicant: GNT, LLC
    Inventor: Gerald Horn
  • Publication number: 20140378391
    Abstract: The ophthalmic drug delivery vehicles provide comfort and compliance; drug solubility, residence time and permeability; and reduce side effects. In addition, the delivery vehicle can be slightly modified to provide an artificial tear formulation.
    Type: Application
    Filed: June 21, 2013
    Publication date: December 25, 2014
    Inventor: Gerald Horn
  • Patent number: 8912225
    Abstract: The present invention provides methods for inhibiting VEGF production or secretion in a subject comprising administering to the subject an effective amount of a compound of Formula I. The invention also provides methods for the treatment or prevention of conditions associated with abnormal levels of VEGF production or secretion.
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: December 16, 2014
    Assignee: Pitney Pharmaceuticals Pty Limited
    Inventors: David L. Morris, Mohammad H. Pourgholami
  • Publication number: 20140363509
    Abstract: Composition comprising at least one active principle, at least one vehicle for said active principle and particles of porous silica, in which the active principle is contained in at least one pore of at least a first portion of such silica particles and in that vehicle, for use in the treatment of a disease of a mucous membrane.
    Type: Application
    Filed: November 27, 2012
    Publication date: December 11, 2014
    Applicant: MISO S.r.I.
    Inventor: Renato Silvio Mortera
  • Publication number: 20140350063
    Abstract: An occlusive dressing made with an elastomeric gel and one or more active agents is described. The elastomeric gel contains a plasticizing oil phase and a block copolymer agent. Methods of preventing, treating, curing or mitigating an infectious disease and methods of making the dressings are also disclosed.
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Applicant: Biological Responsibility, LLC
    Inventor: Gordon Chiu
  • Patent number: 8883747
    Abstract: Described herein are compositions and methods that treat fungal infections of the skin, reduce the severity and duration of symptoms of fungal infections of the skin, and prevent recurrence of fungal infections. The topical compositions described herein are creamy pastes composed of an admixture of an imidazole antifungal and nystatin. The topical compositions can also include optional fillers. The compositions and methods described herein minimize fungal resistance and maximize the number of targeted fungal strains. Additionally, the compounds and methods do not suppress the body's immune system either locally or systemically, thus allowing for a faster restoration of normal skin flora. The compositions and methods described herein are particularly suitable for use in infants and children as well as in immunocompromised individuals, diabetics, and the obese.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: November 11, 2014
    Inventor: Craig W. Carver
  • Patent number: 8883813
    Abstract: Described is a method for treating an individual having a neurological disorder with an associated mutation or mutations in a gene encoding a lysosomal enzyme. Specifically, the individual is administered a specific pharmacological chaperone for the lysosomal enzyme which increases trafficking of the protein from the ER to the lysosome in neural cells, with or without concomitantly increasing enzyme activity in neural cells. Restoration of trafficking relieves cell stress and other toxicities associated with accumulation of mutant proteins. Restoration of enzyme activity relieves substrate accumulation and pathologies associated with lipid accumulation. In a specific embodiment, the neurological disorder is Parkinson's disease or parkinsonism which is associated with mutations in glucocerebrosidase.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: November 11, 2014
    Assignee: Amacus Therapeutics, Inc.
    Inventor: Brandon Wustman
  • Publication number: 20140328895
    Abstract: The present invention discloses a liquid precursor composition adapted for application on a on a desired surface, this composition comprising: a. at least one therapeutic agent suitable for the treatment or prevention of a disorder or pathological condition, wherein said disorder or pathological condition excludes oral disorders, b. at least one acidic-pH sensitive polymer, c. at least one hydrophobic polymer, and d. a pharmaceutically acceptable volatile solvent, wherein a weight ratio between the at least one hydrophobic polymer and the at least one acidic-pH sensitive polymer is larger than 1.
    Type: Application
    Filed: March 25, 2012
    Publication date: November 6, 2014
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd.
    Inventors: Michael Friedman, Doron Steinberg, Eran Lavy
  • Patent number: 8877792
    Abstract: The combination of any two of a polyol, a polyol ether, and a low carbon organic alcohol provides a synergistic effect on the solubility of azole compounds, such as metronidazole, in aqueous fluid.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: November 4, 2014
    Assignee: Dow Pharmaceutical Sciences, Inc.
    Inventors: Meidong Yang, Haigang Chen
  • Patent number: 8871273
    Abstract: In a production process of granules containing a biologically active substance, variation in the elution profile of the biologically active substance is reduced by heating the temperature of granules to about 50° C. or higher and maintaining the temperature for about 1 minute or longer. By setting the spray speed to about 90 mg/min or more per 1 g of cores when a spray agent for a primary agent containing the biologically active substance is sprayed while spraying a binding liquid to the cores and setting the total feeding weight per unit area for a centrifugal fluidized bed coating granulation machine to about 1.5 g/cm2 or more, the variation in the elution profile of the biologically active substance from the granules is reduced.
    Type: Grant
    Filed: February 24, 2006
    Date of Patent: October 28, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Naoki Nagahara, Naoki Asakawa, Muneo Nonomura
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Publication number: 20140303220
    Abstract: This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds in combination with substituted imidazole compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to an animal in need thereof.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 9, 2014
    Applicant: MERIAL LIMITED
    Inventor: Charles Q. Meng
  • Patent number: 8853251
    Abstract: The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: October 7, 2014
    Assignee: Allergan, Inc.
    Inventors: Mohammed I. Dibas, Daniel W. Gil, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello
  • Patent number: 8846732
    Abstract: Biogenic sulfide production is synergistically inhibited by treating sulfate-reducing bacteria (SRB) with a biocide and a metabolic inhibitor. The biocide directly kills a first portion of the SRB. The metabolic inhibitor inhibits sulfate-reducing growth of a second portion of the SRB without directly killing the second portion of the SRB. The treatment of SRB with both a biocide and a metabolic inhibitor provides effective biogenic sulfide inhibition at significantly lower concentrations than would be required if the biocide or metabolic inhibitor was used alone.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: September 30, 2014
    Assignees: ConocoPhillips Company, University Technologies International, Inc.
    Inventors: Gary E. Jenneman, Anne Greene, Gerrit Voordouw
  • Patent number: 8846606
    Abstract: Provided herein are methods and compositions for treating septic hypotension. More specifically, the methods may comprise, administering one alpha-2 agonist or other sympatholytic and at least one vasopressor.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: September 30, 2014
    Inventor: Luc Quintin
  • Patent number: 8846740
    Abstract: An occlusive dressing made with an elastomeric gel and one or more active agents is described. The elastomeric gel contains a plasticizing oil phase and a block copolymer agent. Methods of preventing, treating, curing or mitigating an infectious disease and methods of making the dressings are also disclosed.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: September 30, 2014
    Assignee: Biological Responsibility, LLC
    Inventor: Gordon Chiu
  • Patent number: 8840910
    Abstract: There is provided an antifouling coating composition capable of forming an antifouling coating film which has stable coating film consumption degree on ships, underwater structures and the like and which exhibits excellent antifouling property over a long term. The antifouling coating composition includes a hydrolyzable copolymer (A) and an antifouling agent (B), wherein the hydrolyzable copolymer (A) is, e.g., a metal salt bond-containing copolymer having a component unit derived from a monomer (a21) represented by the general formula (II): CH2?C(R2)—COO-M-O—CO—C(R2)?CH2??(II) [In the formula (II), M is zinc or copper, and R2 is a hydrogen atom or a methyl group], and a component unit derived from other unsaturated monomer (a22) copolymerizable with the monomer (a21), and wherein the antifouling agent (B) includes at least medetomidine.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: September 23, 2014
    Assignee: Chugoku Marine Paints, Ltd.
    Inventors: Satoshi Masuda, Yusuke Hayashi, Yukio Kozono
  • Patent number: 8840923
    Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 23, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
  • Publication number: 20140274684
    Abstract: The disclosure provides for methods of repelling, directing, altering the behavior, and controlling an insect by utilizing a compound or composition described herein. The disclosure also provides for methods of promoting the health of an insect by repelling a pest that preys on insect and/or by providing an antibiotic or nutritional supplement composition to an insect. The disclosure also provides for a composition including at least one repelling, controlling, or directing compound or composition described herein together with an insecticide, herbicide, fungicide, or miticide. Compounds, compositions, seeds, and plants useful in these methods are also described.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 18, 2014
    Applicant: BAYER CROPSCIENCE LP
    Inventors: Tai-Teh WU, Dick ROGERS, Jian ZHANG, Robert CROFT, Chi Yu Roy CHEN
  • Publication number: 20140274962
    Abstract: Described herein are methods of inhibiting or reversing the progression of presbyopia in an eye by administering a ?L-crystallin electrostatic interaction inhibitor. Presbyopia is caused by aggregation of the soluble crystalline lens proteins called the crystallins, particularly ?L-crystallin. It has been found that the aggregation of ?L-crystallin is an electrostatic phenomenon and that electrostatic interaction inhibitors can be employed to prevent the formation of ?L-crystallin aggregates as well as to deaggregate already formed aggregates.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 18, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Murugappan Muthukumar, Zhaoyang Ou, Deniz Civay
  • Patent number: 8835468
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140249161
    Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 4, 2014
    Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: David WATT, Chunming LIU, Vitaliy M. SVIRIPA, Wen ZHANG
  • Patent number: 8815925
    Abstract: The invention relates to the use of an antimycotic agent and an epithelial cell or endothelial cell adhesion inhibitor for producing a combination drug for the topical treatment of Candida mycoses selected from vulvovaginal candidiasis, oropharyngeal candidiasis (oral thrush), diaper dermatitis (diaper thrush) and intertriginous (Candida) eczema.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: August 26, 2014
    Inventors: Christian Noe, Marion Noe-Letschnig
  • Publication number: 20140227206
    Abstract: Methods of improving the appearance of aging skin that include applying a cosmetic composition to a target skin surface having one or more signs of aging. The cosmetic composition includes a substituted azole. In some instances, the substituted azole compound is 1-phenylimidazole, 4-phenylimidazole, or combinations thereof. An effective amount of the cosmetic composition is applied for a period of time sufficient to improve the appearance of at least one sign of aging skin.
    Type: Application
    Filed: January 29, 2014
    Publication date: August 14, 2014
    Applicant: THE PROCTER & GAMBLE COMPANY
    Inventors: Supriya Punyani BAREJA, Stevan David JONES, John Erich OBLONG, Kevin John MILLS, John Crist BIERMAN
  • Publication number: 20140227208
    Abstract: Compositions for alleviating mechanically-induced skin inflammation, such as that caused by shaving, contain substituted azole. Methods for alleviating mechanically-induced skin inflammation include the step of applying a composition comprising substituted azole to a skin surface subject to mechanically-induced inflammation. In particular embodiments the substituted azole compound is 1-phenylimidazole, 4-phenylimidazole, or a combination thereof. An effective amount of the composition is applied for a period of time sufficient to alleviate mechanically-induced skin inflammation.
    Type: Application
    Filed: January 29, 2014
    Publication date: August 14, 2014
    Applicant: The Procter & Gamble Company
    Inventors: Supriya Punyani BAREJA, Stevan David JONES, John Erich OBLONG, Kevin John MILLS, John Crist BIERMAN
  • Publication number: 20140227207
    Abstract: Cosmetic compositions for alleviating the signs of photoaged skin containing a substituted azole. Methods for alleviating the signs of photoaged skin that include applying a cosmetic composition comprising substituted azole to a target UV-exposed skin surface. The substituted azole compound present in the cosmetic composition may be 1-phenylimidazole, 4-phenylimidazole or a combination thereof. An effective amount of the cosmetic composition is applied to the target skin surface for a period of time sufficient to alleviate at least one sign of photoaging.
    Type: Application
    Filed: January 29, 2014
    Publication date: August 14, 2014
    Applicant: The Procter & Gamble Company
    Inventors: Supriya Punyani BAREJA, Stevan David JONES, John Erich OBLONG, Kevin John MILLS, John Crist BIERMAN
  • Patent number: 8802128
    Abstract: Biocompatible intraocular implant systems are formulated for discontinuous or intermittent release of therapeutic levels of a therapeutic agent (such as a steroid) to minimize development of side effects associated with continuous or long term use of such agent. The implant system may comprise one or more implant, and preferably, although not necessarily, also contains an auxiliary agent having an activity effective to lessen at least one side effect associated with said therapeutic agent compared to the use of an otherwise identical implant system lacking said auxiliary agent. The implants containing the therapeutic agent and auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the ocular side effects otherwise accompanying the use of such therapeutic agent.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: August 12, 2014
    Assignee: Allergan, Inc.
    Inventors: Michael R. Robinson, Scott M. Whitcup
  • Patent number: 8802691
    Abstract: The invention relates to the use of domperidone or a pharmaceutically acceptable salt thereof at low doses to prevent and/or treat a disease associated with an alteration of the immune response such as Leishmaniosis.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: August 12, 2014
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: David Sabate Elias, Josep M. Homedes Beguer, Pablo Gomez Ochoa
  • Patent number: 8790703
    Abstract: The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: July 29, 2014
    Assignee: BASF SE
    Inventors: Kathrin Meyer-Böhm, Rainer Dobrawa, Stefan Fischer, Karl Kolter
  • Patent number: 8791124
    Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy-phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methly-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo(3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxypropoxy)-2-carboxy-2,3-didehydro-chronan-4-one (PPL-557212); k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quinazolin
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 29, 2014
    Assignee: Uropep Biotech GBR
    Inventors: Wolf-Georg Forssmann, Christian Georg Stief, Michael Carsten Truβ, Stefan Uckert, Udo Jonas
  • Publication number: 20140206706
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Patent number: 8778913
    Abstract: The disclosure provides compounds and methods to treat a microbial or a bacterial pathogenesis, and demonstrates that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: July 15, 2014
    Assignee: The Regents of the University of California
    Inventors: Victor Nizet, George Y. Liu, Eric Oldfield, Yongcheng Song