Imidazoles Patents (Class 514/396)
  • Publication number: 20120329834
    Abstract: The present invention relates to the use of compounds of general formula (I): (I) for the preparation of medicaments that act against mitochondrial pathologies involving a deficiency in ATP production via the oxidative phosphorylation pathway, such as mitochondrial diseases.
    Type: Application
    Filed: April 15, 2010
    Publication date: December 27, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITY OF PITTSBURGH, INSTITUT CURIE
    Inventors: Marc Blondel, Elodie Couplan, Jean-Paul Di Rago, Daniel Dauzonne, Michael Palladino, Alicia Celotto
  • Patent number: 8338421
    Abstract: The invention generally relates to compositions and methods for inducing vasoconstriction with low incidence of rebound hyperemia. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: December 25, 2012
    Assignee: Alpha Synergy Development, Inc.
    Inventor: Gerald Horn
  • Patent number: 8338470
    Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: December 25, 2012
    Assignee: Hospira, Inc.
    Inventors: Priyanka Roychowdhury, Robert A. Cedergren
  • Patent number: 8334293
    Abstract: The present invention provides a combination therapy comprising the compound 4-[4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for use in the treatment of glioblastoma multiforme, adenocarcinomas of the colon, non-small-cell lung cancer, small-cell lung cancer, cisplatin-resistant small-cell lung cancer, ovarian cancer, leukemia, pancreatic cancer, prostate cancer, mammary carcinoma, renal cell carcimoma, multiple myeloma, Kaposis Sarcoma, Hodgkins lymphoma, lymphangioleiomyomatosis, Non-Hodgkins lymphoma or sarcoma.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: December 18, 2012
    Assignee: Eli Lilly and Company
    Inventor: Sandaruwan Geeganage
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Publication number: 20120316210
    Abstract: This invention recites topical formulations comprising demiditraz, fipronil, an acid modifier, at least one veterinarily acceptable carrier, and optionally, at least one antioxidant for treating a parasitic infection or infestation in animals.
    Type: Application
    Filed: January 4, 2011
    Publication date: December 13, 2012
    Applicant: PFIZER INC.
    Inventors: Nathan Anthony Logan Chubb, Guy Francis de Rose, Sunil Thomas Kumar Narishetty
  • Patent number: 8329685
    Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: December 11, 2012
    Assignee: North West University
    Inventor: Petrus Johannes Meyer
  • Patent number: 8329738
    Abstract: The invention relates to the use of imidazole derivatives of the formula (1): in which A, R?1, R?2 and R?3 are as defined in the description, as AMPK activators. The invention also relates to processes for the preparation of the said compounds, to their uses for the preparation of medicaments for the treatment of insulin resistance, diabetes and related pathologies, and also obesity, and to the pharmaceutical compositions comprising them. Certain compounds of the formula (1) are novel and, in this respect, also form part of the invention.
    Type: Grant
    Filed: June 12, 2007
    Date of Patent: December 11, 2012
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Gerard Moinet, Dominique Marais, Sophie Hallakou-Bozec, Christine Charon
  • Publication number: 20120309626
    Abstract: The invention provides a composition comprising an active ingredient with a maximum solubility in water at 20° C. of 10 g/l, and a hyperbranched polyester based on a hydrophobic dicarboxylic acid and a trifunctional alcohol. The invention further relates to the hyperbranched polyester mentioned, to a process for preparation thereof and to the use thereof for solubilizing an active ingredient with a maximum solubility in water at 20° C. of 10 g/l in aqueous solutions.
    Type: Application
    Filed: December 15, 2010
    Publication date: December 6, 2012
    Applicant: BASF SE
    Inventors: Holger Türk, Monika Haberecht, Hiroe Yamada, Bernd Bruchmann, Daniel Schönfelder, Michael Ishaque, Ulrike Troppmann, Joachim Clauss, Chee Chin Liew
  • Publication number: 20120309804
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.
    Type: Application
    Filed: August 14, 2012
    Publication date: December 6, 2012
    Applicant: Alpha Synergy Development Inc.
    Inventor: Gerald Horn
  • Publication number: 20120309720
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.
    Type: Application
    Filed: August 14, 2012
    Publication date: December 6, 2012
    Applicant: Alpha Synergy Development Inc.
    Inventor: Gerald Horn
  • Patent number: 8324260
    Abstract: The presently disclosed subject matter relates to methods of administering an effective amount of dexmedetomidine to a pediatric patient in order to reduce the incidence of neurological damage. More particularly, the presently disclosed subject matter relates to methods of providing sedation or analgesia to a pediatric patient by administering a dexmedetomidine infusion and optionally a loading dose. The dexmedetomidine can be administered before, during, or after surgery.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: December 4, 2012
    Assignee: Hospira, Inc.
    Inventors: Marcelo Garcia da Rocha, Wayne Wisemandle, Dennis James Stalker, Edward Koo
  • Patent number: 8324401
    Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.
    Type: Grant
    Filed: August 18, 2009
    Date of Patent: December 4, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Bin Jiang
  • Publication number: 20120288566
    Abstract: The present invention discloses liquid precursor compositions adapted for application on a hard surface in the oral cavity, comprising at least one therapeutic agent suitable for the treatment of oral disorders, at least one acidic-pH sensitive polymer, at least one hydrophobic polymer, and a pharmaceutically acceptable volatile carrier, wherein a weight ratio between said at least one hydrophobic polymer and said at least one acidic-pH sensitive polymer is larger than 1. The invention also discloses formulations formed of the solidification of these compositions, and methods for treating oral disorders by applying these compositions on hard surfaces in the oral cavity or to be placed in the oral cavity.
    Type: Application
    Filed: October 5, 2010
    Publication date: November 15, 2012
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Michael Friedman, Doron Steinberg, Irith Gati
  • Patent number: 8309591
    Abstract: The present invention relates to a veterinary composition in a semisolid form adapted for transmucosal administration for providing sedation and analgesia in large animals such as horses and cattle. The semisolid transmucosal composition of the invention comprises detomidine or a pharmaceutically acceptable salt thereof as an active ingredient. The composition provides a rapid onset of action while having low irritation potential in the oral mucosa.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: November 13, 2012
    Assignee: Orion Corporation
    Inventors: Mirja Huhtinen, Piritta Koistinen, Lasse Leino, Maria Rantala, Helena Kaukinen, Kaija Af Ursin
  • Patent number: 8304402
    Abstract: A composition and method for treating nosebleed, that is, epistaxis. The composition comprises bismuth subgallate and a vasoconstriction agent, preferably oxymetazoline. The composition is preferably a paste administered intranasally.
    Type: Grant
    Filed: May 5, 2005
    Date of Patent: November 6, 2012
    Assignee: Binyarco, LLC
    Inventor: Jeffrey E. Binder
  • Patent number: 8304419
    Abstract: The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: November 6, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Pek Yoke Chong, Andrew James Peat, Paul Richard Sebahar, Michael Youngman, Huichang Zhang
  • Publication number: 20120276182
    Abstract: The present invention relates to methods for treating and completely curing fungal, yeast, and/or mold infections in human subjects comprising topically administering to a human subject in need thereof an antifungal nanoemulsion composition.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Inventors: James R. Baker, JR., Mary R. Flack, Susan M. Ciotti, Joyce A. Sutcliffe
  • Publication number: 20120277241
    Abstract: In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat inflammatory skin disorders and the symptoms associated therewith.
    Type: Application
    Filed: July 10, 2012
    Publication date: November 1, 2012
    Applicant: GALDERMA LABORATORIES, INC.
    Inventors: Jack A. DeJovin, Isabelle Jean DeJovin
  • Patent number: 8299108
    Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: October 30, 2012
    Assignee: Novartis AG
    Inventors: Payman Amiri, Wendy Fantl, Barry Haskell Levine, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian, Leonard Sung
  • Patent number: 8299102
    Abstract: The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: October 30, 2012
    Assignee: Sanofi
    Inventors: Hartmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
  • Patent number: 8293282
    Abstract: Disclosed is a wood preservative composition comprising micronized copper and copper-amine complex, wherein the copper component of the copper amine complex is from about 5% to about 50% by weight, based upon the total weight of copper in the composition. The copper amine complex serves to avoid wood surface “chalking” that is otherwise attributable to the presence of micronized copper in copper-based slurries used to treat wood products. In addition, the copper-amine complex enhances the antimicrobial efficacy of the composition when used in wood treatment applications by facilitating cell wall penetration of the treated wood.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: October 23, 2012
    Assignee: Arch Wood Protection, Inc.
    Inventor: Jayesh P. Patel
  • Patent number: 8288562
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: October 16, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Publication number: 20120258061
    Abstract: A skin care product comprising from about 0.001% to about 10% of a retinoid in combination with 0.0001% to about 50% of at combination of retinoid hoosters.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 11, 2012
    Applicant: CONOPCO, INC., D/B/A UNILEVER
    Inventors: Stewart Paton Granger, Ian Richard Scott, Robert Mark Donovan, Susanne Teklits Iobst, Lisa Licameli
  • Patent number: 8283350
    Abstract: The invention generally relates to compositions and methods for reducing capillary permeability. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: October 9, 2012
    Assignee: Alpha Synergy Development, Inc.
    Inventor: Gerald Horn
  • Publication number: 20120252820
    Abstract: Methods of identifying compounds that potentiate the activity of antifungal agents, potentiators identified by these methods, and methods of using potentiators to treat fungal infections are disclosed.
    Type: Application
    Filed: April 22, 2009
    Publication date: October 4, 2012
    Applicant: NORTHEASTERN UNIVERSITY
    Inventors: Kim Lewis, Michael David Lafleur
  • Patent number: 8277688
    Abstract: This invention relates to galvanic aluminum alloy powder-pigments coated with a semi-conducting corrosion inhibiting oxide and the process for preparing said coated powder-pigments in combination with film-forming binders for coating metal substrates to inhibit corrosion. The coated aluminum alloy powder-pigments are electrically active and prevent corrosion of metals which are more cathodic (electropositive) than the aluminum alloy pigments.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: October 2, 2012
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Craig Matzdorf, William Nickerson
  • Patent number: 8263634
    Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: September 11, 2012
    Assignee: Novo Nordisk A/S
    Inventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedsø, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce-Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswarak Santhosh
  • Patent number: 8262938
    Abstract: Chromate-free corrosion-inhibiting coating compositions comprising film-forming binders and galvanic aluminum alloy powders prepared in an oxygen (oxidizing), nitrogen (inert) or nitrogen-hydrogen (reducing) atmosphere having particle sizes ranging up to 100 microns. The aluminum alloy powders having the formula: aluminum-zinc-X (AlZnX) wherein X is an element selected from the group consisting of indium, gallium, tin and bismuth. Improvement in corrosion protection is obtained by the addition of chemical inhibitors such as an azole or talcite clay to the coating which further inhibits the self-corrosion of the aluminum alloy and extends the corrosion protection of the metal substrate being protected.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: September 11, 2012
    Assignee: The United States of America, as represented by the Secretary of the Navy.
    Inventors: Craig Matzdorf, William Nickerson
  • Publication number: 20120220454
    Abstract: Coating compositions and methods of use, allowing for improved water and/or nutrient usage by seeds, plants, shrubs, and vegetation, among others, are disclosed.
    Type: Application
    Filed: February 28, 2012
    Publication date: August 30, 2012
    Applicant: RHODIA OPERATIONS
    Inventors: Zhiyun Chen, Jean-Christophe Castaing, PengFei JI, Galder Cristobal
  • Patent number: 8247429
    Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa, Xb, Xc and Xd are each a carbon atom or a nitrogen atom, provided that any one or two of Xa, Xb, Xc and Xd is/are nitrogen atom(s), m is 0 to 2, and rings A to C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: August 21, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
  • Publication number: 20120208858
    Abstract: The present invention is directed to: a) a method of treating telangiectasia; b) a method of treating inflammatory lesions; and c) a method of treating two or more symptoms of rosacea selected from erythema, telangiectasia, or inflammatory lesions comprising topical administration of a pharmaceutical composition comprising oxymetazoline and a pharmaceutically acceptable excipient.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 16, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Stuart D. Shanler, Christopher Powala
  • Patent number: 8242151
    Abstract: The present invention provides a PPAR ? agonist comprising, as an active ingredient, a tricyclic compound represented by the formula (I) (wherein R1 represents lower alkyl optionally having substituent(s) or the like, R2 and R3 are the same or different and each represents lower alkyl optionally having substituent(s) or the like, R4 and R5 are the same or different and each represents a hydrogen atom or the like, Q1-Q2-Q3 represents CH?CH—CH?CH or the like, Y represents a single bond or the like, Z1-Z2 represents C?CR13 (wherein R13 represents a hydrogen atom or the like), or the like, and A represents —COOH or the like), or a pharmaceutically acceptable salt thereof and the like.
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: August 14, 2012
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Arata Yanagisawa, Takeshi Kuboyama, Seiji Aratake, Kazuki Hemmi, Kimihisa Ueno, Michihiko Suzuki, Masahiro Matsubara, Kozo Yao, Akinori Hamaguchi, Yukihito Tsukumo
  • Patent number: 8242158
    Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: August 14, 2012
    Assignee: Hospira, Inc.
    Inventors: Priyanka Roychowdhury, Robert A. Cedergren
  • Publication number: 20120202865
    Abstract: A compound having selective modulating activity at the alpha 2B and or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein R1-R6 is independently selected from the group consisting of H, C1-6 alkyl, halogen, CH2OH, CH2N(R7)2, CH2CN, C(O)R8, CF3, and aryl; wherein R7 is H or C1-6 alkyl; and R8 is H, C1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 9, 2012
    Inventors: Santosh C. Sinha, Todd M. Heidelbaugh, Smita S. Bhat, Ken Chow
  • Publication number: 20120202864
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine at acidic pH and extremely low concentrations.
    Type: Application
    Filed: February 2, 2012
    Publication date: August 9, 2012
    Applicant: ALPHA SYNERGY DEVELOPMENT INC.
    Inventor: Gerald Horn
  • Publication number: 20120202863
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine at near alkaline pH and extremely low concentrations.
    Type: Application
    Filed: February 3, 2011
    Publication date: August 9, 2012
    Inventor: Gerald Horn
  • Publication number: 20120196908
    Abstract: This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I): wherein: 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: Application
    Filed: August 27, 2010
    Publication date: August 2, 2012
    Applicant: BIOLAB SANUS FARMACEUTICA LTDA.
    Inventors: Artur Franz Keppler, Sérgio Luiz Sacurai, Marcio Henrique Zaim, Carlos Eduardo da Costa Touzarim
  • Publication number: 20120196905
    Abstract: Methods and small molecule compounds for smoking and CNS disease harm reduction are provided.
    Type: Application
    Filed: August 5, 2011
    Publication date: August 2, 2012
    Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTE
    Inventor: John R. CASHMAN
  • Publication number: 20120196874
    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: January 27, 2012
    Publication date: August 2, 2012
    Inventors: David WATT, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
  • Publication number: 20120196819
    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 compositon 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: January 4, 2012
    Publication date: August 2, 2012
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Patent number: 8232304
    Abstract: A topical composition and the method using the composition, which contains an antifungal agent and a low potency anti-inflammatory steroid which is safe and effective such as desonide or its derivative. The low potency steroid agent does not cause side effects such as skin atrophy, striae and hypopigmentation. In a representative example, the low potency anti-inflammatory steroid has the following structure: wherein R1, R2, R3, and R4 taken independently can be H, C1-C10 alkyl, C1-C10 alkenyl, C3-C10 cycloalkyl, and phenyl groups; R1 and R2 taken together can be C3-C10 cycloalkyl; and R3, and R4 taken independently can be H, C1-C10 alkyl, C1-C10 alkenyl, C3-C10 cycloalkyl, phenyl, C7-C10 phenylalkyl, carboxylate, sulfonyl, phosphoryl, and phosphonyl groups. The composition can be formulated in a dosage form such as a cream, ointment, gel, lotion, foam, powder, aerosol, spray, shampoo, or liquid solution.
    Type: Grant
    Filed: October 23, 2003
    Date of Patent: July 31, 2012
    Assignee: G & R Pharmaceuticals, LLC
    Inventors: Jay A. Goldstein, Michael Rothman, Whe-Yong Lo
  • Patent number: 8232305
    Abstract: Anti-microbial compositions comprising certain imidazolium ionic liquids and non-ionic or anionic surfactants and methods of using said compositions in the preservation of personal care and cosmetic applications are provided.
    Type: Grant
    Filed: June 8, 2007
    Date of Patent: July 31, 2012
    Assignee: BASF SE
    Inventors: Stewart Todd Elder, Andrea Preuss, Kai-Uwe Schöning, Karin Mühlbauer
  • Publication number: 20120190719
    Abstract: Disclosed herein is a method of treating compulsive disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist.
    Type: Application
    Filed: August 26, 2010
    Publication date: July 26, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Daniel W. Gil, John E. Donello, Lauren M.B. Luhrs
  • Patent number: 8227497
    Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: July 24, 2012
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20120178769
    Abstract: The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: July 12, 2012
    Applicant: The University of Medicine and Dentistry
    Inventor: Alexey G. Ryazanov
  • Publication number: 20120178728
    Abstract: The use of copolymers obtained by free-radical 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 total of components i), ii) and iii) equals 100% by weight, as solubilizers for slightly water-soluble substances.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Applicant: BASF SE
    Inventors: Nathalie Bouillo, Marianna Pierobon, Ralf Widmaier, Rainer Dobrawa, Kathrin Meyer-Böhm, Ronald Frans Maria Lange
  • Publication number: 20120178724
    Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 12, 2012
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Joseph Michael Sprafka, II, Jose Mauro Goulart-Brum
  • Publication number: 20120177585
    Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.
    Type: Application
    Filed: January 6, 2012
    Publication date: July 12, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Stuart D. Shanler, Andrew Ondo
  • Publication number: 20120165347
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Gabor Csjernyik, Sofia Karlström, Annika Kers, Karin Kolmodin, Martin Nylöf, Liselotte Öhberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Söderman, Britt-Marie Swahn, Stefan Von Berg