Silicon Containing Doai Patents (Class 514/63)
  • Publication number: 20120232033
    Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
    Type: Application
    Filed: May 25, 2012
    Publication date: September 13, 2012
    Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinnard, Henri Stalder
  • Publication number: 20120225845
    Abstract: The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: May 4, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Christine Klein, Andrew D. Gassman, Leena Bhoite, John Manfredi
  • Publication number: 20120225844
    Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 6, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
  • Publication number: 20120220550
    Abstract: The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.
    Type: Application
    Filed: September 2, 2010
    Publication date: August 30, 2012
    Applicant: EWHA UNIVERSITY- INDUSTRY COLLABORATION FOUNDATION
    Inventors: Yun Soo Bae, Jee Hyun Lee, Mi Sun Seo, Soo Young Lee, Sun Choi, Kee In Lee, Hye Rin Bin, Do Min Lee
  • Publication number: 20120220549
    Abstract: Fluid compositions are disclosed containing a branched organopolysiloxane and a carrier fluid. The branched organopolysiloxane is obtainable by reacting an organohydrogencyclosiloxane and an alkenyl terminated polydiorganosiloxane. The disclosed fluid compositions possess pituitous rheological properties.
    Type: Application
    Filed: September 1, 2010
    Publication date: August 30, 2012
    Inventors: Michael Stephen Starch, Paul Cornelius Vandort
  • Publication number: 20120214735
    Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Advinus Therapeutics Limited
    Inventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
  • Publication number: 20120214763
    Abstract: A medicament for promoting memory consolidation, which comprises, as an active ingredient, a non-natural retinoid, preferably a retinoid having a basic skeleton comprising an aromatic ring bound with an aromatic carboxylic acid or tropolone by means of a bridging group, more preferably 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid or 4-[(3,5-bis-trimethylsilylphenyl)-carboxamido]benzoic acid.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 23, 2012
    Applicants: KEMPHYS LTD., RESEARCH FOUNDATION ITSUU LABORATORY
    Inventors: Koichi SHUDO, Hiroyuki KAGECHIKA
  • Publication number: 20120214762
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: March 15, 2012
    Publication date: August 23, 2012
    Applicant: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
  • Publication number: 20120214764
    Abstract: A method of cleansing a mammalian GI tract is described and includes ingestion of polyethylene glycol (PEG) and magnesium citrate in a split-dose regimen. The split-dose regimen provides effective cleansing of the GI tract while minimizing discomfort and side effects to the patient A kit packaged with a first and second portion of PEG, and a first and second portion of magnesium citrate, and optionally simethicone is also provided.
    Type: Application
    Filed: October 19, 2010
    Publication date: August 23, 2012
    Inventor: Jose Rodriguez-San Juan
  • Patent number: 8247392
    Abstract: Compounds of formula (I) are disclosed. The tetrapyrole ring in formula (I) can be substituted with a metal cation (M); R1, R2, R3 and R4 separately represent a hydrogen atom, a C1-4 alkyl or alkyloxy radical, or a phenyl radical optionally substituted by vinyl, hydroxy, nitro, amino, bromo, chloro, fluoro, iodo, benzyloxy, or hydroxymethyl radicals; R5, R6, R7 and R8 separately represent a hydrogen atom or a C1-4 alkyl radical; Ra, Rb and Rc separately represent a hydrogen atom, a C1-4 alkyl or alkyloxy radical optionally substituted by a halogen, or a phenyl radical optionally substituted by vinyl, hydroxy, nitro, amino, bromo, chloro, fluoro, iodo, benzyloxy, or hydroxymethyl radicals, wherein at least one of Ra, Rb, and Rc is a phenyl radical. Compounds of formula (I) bound to a silica, a sol-gel material or a mesoporous silica are useful for selective trapping of carbon monoxide.
    Type: Grant
    Filed: July 19, 2002
    Date of Patent: August 21, 2012
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: François Jerome, Géraud Dubois, Stéphane Brandes, Gabriel Canard, Jean-Michel Barbe, Roger Guilard, Bruno Roux-Fouillet, Henry Ledon
  • Publication number: 20120207810
    Abstract: The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.
    Type: Application
    Filed: February 15, 2012
    Publication date: August 16, 2012
    Inventors: Lon T. SPADA, Jane Guo SHIAH, Patrick HUGHES, Thomas C. MALONE, Gerald W. DEVRIES, Jeffrey L. EDELMAN, Julie A. WURSTER
  • Publication number: 20120202774
    Abstract: The present invention provides acyloxy- and phosphoryloxy-butadiene-Fe(CO)3 complexes which can deliver carbon monoxide to a physiological target, wherein release of carbon monoxide can be enzymatically-triggered. The present invention also provides for methods of manufacturing the enzymatically-triggered carbon monoxide releasing molecules and methods for their use.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 9, 2012
    Applicants: UNIVERSITAET REGENSBURG, UNIVERSITAET ZU KOELN
    Inventors: Hans-Guenther Schmalz, Steffen Romanski, Sabine Amslinger, Benito Yard, Birgit Kraus
  • Publication number: 20120202763
    Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.
    Type: Application
    Filed: May 27, 2010
    Publication date: August 9, 2012
    Applicant: PTC THERAPEUTICS, INC
    Inventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
  • Publication number: 20120202687
    Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: February 6, 2012
    Publication date: August 9, 2012
    Inventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
  • Publication number: 20120196832
    Abstract: Linear polydialkoxysiloxanes with 2-8 polymeric units have been reacted with alcohols by a transetherification reaction to provide hydrophilic and water soluble silicone products. The glycerol substituted siloxanes in particular are effective in topically treating skin lesions such as radiation burns. Compositions including the substituted polydialkoxysiloxane products inhibit biofilm formation when used as coatings on hard surfaces.
    Type: Application
    Filed: April 13, 2012
    Publication date: August 2, 2012
    Applicant: ONE UNLIMITED, INC.
    Inventor: LEONARD WILLIAM LURIA
  • Publication number: 20120196953
    Abstract: Antimicrobial granules comprise carrier particles agglomerated by a binding agent containing a quaternary ammonium organosilane.
    Type: Application
    Filed: August 13, 2010
    Publication date: August 2, 2012
    Inventors: Nicoias Ziolkowski, Jean-Paul Lecomte, Nathalie Wauthier, Veronique Verhelst, Flore Vandemeulebroucke
  • Publication number: 20120195950
    Abstract: A laundry additive such as a fabric dryer sheet formed of a flexible substrate contains an insecticidally effective amount of an insecticide, preferably a pyrethrum, in an amount between about 0.05 and about 10 grams per square foot. Alternatively, the insecticide may be included as a component in a rinse-cycle laundry additive. Such laundry additives are appropriate for use by institutions such as hotels, cruise ships, and nursing homes, hospitals, and shelters in the prevention and control of bed bugs.
    Type: Application
    Filed: April 11, 2012
    Publication date: August 2, 2012
    Inventor: Stevan L. Troutman
  • Publication number: 20120184509
    Abstract: A kind of new compounds, and their pharmaceutically acceptable salts, and hydrates are disclosed. The pharmaceutical composition thereof is also provided. And also are the medical uses of the compounds, pharmaceutically acceptable salts, hydrates and the pharmaceutical composition for treating the TRPV1-mediate diseases.
    Type: Application
    Filed: September 27, 2010
    Publication date: July 19, 2012
    Inventor: Qun Sun
  • Publication number: 20120183619
    Abstract: The present invention is directed to triclosan derivatives and nanoparticles comprising said derivatives together with an organic or an inorganic carrier. The present invention is also directed to uses of the triclosan nanoparticles for preventing or inhibiting bacterial growth.
    Type: Application
    Filed: October 31, 2011
    Publication date: July 19, 2012
    Applicant: BAR ILAN UNIVERSITY
    Inventors: Jean Paul LELLOUCHE, Igor MAKAROVSKY, Yonit BOGUSLAVSKY, Ehud BANIN, Jonatan LELLOUCHE
  • Publication number: 20120183591
    Abstract: A cosmetic or pharmaceutical rinse-off formulation contains 0.2% by weight to 20% by weight of a phase A; 0.1% by weight to 50% by weight of an active substance; a detergent; and the remainder being water. The phase A is a mixture of 20% by weight to 90% by weight of a surfactant mixture of isethionates, acyl lactylates and one of alkyl glutamates and alkyl glucosides and 10% by weight to 80% by weight of water, alcohol, polyol or mixtures thereof. The phase A forms multilamellar vesicles. The cosmetic or pharmaceutical rinse-off formulation is a clear product with the multilamellar vesicles of phase A having an average diameter of less than 100 nm.
    Type: Application
    Filed: March 27, 2012
    Publication date: July 19, 2012
    Applicant: OTC GMBH
    Inventor: Gerd Dahms
  • Publication number: 20120184495
    Abstract: The present invention relates to a photosensitizer-containing nanoparticle, comprising a photosensitizer covalently bonded throughout at least a part of said nanoparticle to the nanoparticle matrix material and incorporated therein in a quasi-aggregated state. The present invention further relates to methods for producing the invention nanoparticles, and to methods of killing cancer cells by PDT treatment using the said nanoparticles.
    Type: Application
    Filed: June 12, 2009
    Publication date: July 19, 2012
    Inventors: Manzoor Koyakutty, Dominic James Robinson, Henricus Johannes Cornelius Maria Sterenborg, Slavka Kascakova, Shantikumar Nair
  • Publication number: 20120184508
    Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
    Type: Application
    Filed: January 11, 2012
    Publication date: July 19, 2012
    Inventors: Wenjian Liu, Kin-Chun Luk, Xiaohu Zhang
  • Publication number: 20120177583
    Abstract: Compositions containing polymetal complexes are useful in treating anorectal disorders.
    Type: Application
    Filed: June 16, 2011
    Publication date: July 12, 2012
    Inventor: José E. Ramirez
  • Publication number: 20120178713
    Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Application
    Filed: March 14, 2012
    Publication date: July 12, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • Publication number: 20120171150
    Abstract: A pharmaceutical composition is provided that is useful for reducing sodium in the bloodstream of animals. In some embodiments, the pharmaceutical composition comprises a high-ion-affinity part and a substrate part. Additionally, methods of using the pharmaceutical composition and methods of treating diseases with the pharmaceutical composition are disclosed.
    Type: Application
    Filed: January 5, 2011
    Publication date: July 5, 2012
    Inventor: Benjamin S. Metelits
  • Publication number: 20120172333
    Abstract: The present invention relates to pyrrolopyridone compounds of the formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds as activators of AMPK.
    Type: Application
    Filed: September 8, 2010
    Publication date: July 5, 2012
    Applicant: GLAXOSMITHKLINE LLC
    Inventor: Olivier Mirguet
  • Publication number: 20120172334
    Abstract: Controlled release particles are obtained by dissolving a hydrophobic antibiotic compound in a hydrophobic polymerizable vinyl monomer without the presence of a solvent, thereby preparing a hydrophobic solution, the hydrophobic antibiotic compound having a melting point of 100° C. or less, a polar term ?p,compound of 2 to 8 [(J/cm3)1/2] of a solubility parameter (?) and a hydrogen bonding term ?h,compound of 5.5 to 9.5[(J/cm3)1/2] of the solubility parameter (?), the solubility parameter (?) defined by Hansen and calculated by van Klevelen and Hoftyzer method; dispersing the hydrophobic solution in water; and polymerizing the polymerizable vinyl monomer in the presence of an oil-soluble initiator by radical polymerization, thereby producing a polymer having a polar term ?p,polymer of 5 to 7[(J/cm3)1/2] and a hydrogen bonding term ?h,polymer of 8 to 10 [(J/cm3)1/2] of the solubility parameter (?).
    Type: Application
    Filed: September 9, 2010
    Publication date: July 5, 2012
    Applicant: Japan EnviroChemicals, Ltd.
    Inventor: Junji Oshima
  • Patent number: 8211871
    Abstract: A topical skin barrier for protecting and promoting healing of skin, and for providing comfort to a patient, comprises a semi-solid hydrocarbon, a water-absorbing compound, and a pain relief agent. The topical skin barrier effectively adheres to skin, affords protection from moisture and waste, provides transparency in use, and is anhydrous and therefore is preservative-free. Methods of in vitro evaluation are for (i) a composition's protection from moisture and waste, and (ii) a composition's adhesion to skin.
    Type: Grant
    Filed: April 28, 2006
    Date of Patent: July 3, 2012
    Assignee: Coloplast A/S
    Inventor: Donald L. Gerrish
  • Publication number: 20120165293
    Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.
    Type: Application
    Filed: July 13, 2010
    Publication date: June 28, 2012
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Stephenie Bosse Abernathy
  • Publication number: 20120165294
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: March 2, 2012
    Publication date: June 28, 2012
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Publication number: 20120157410
    Abstract: The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
    Type: Application
    Filed: February 17, 2012
    Publication date: June 21, 2012
    Applicants: U.S. Government, National Institute of Health (NIH), U.S. Department of Health and Human Services (DHSS),
    Inventors: D. Martin WATTERSON, Linda VAN ELDIK, Wenhui HU
  • Publication number: 20120157400
    Abstract: Methods for treating Kaposi's sarcoma involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.
    Type: Application
    Filed: May 27, 2010
    Publication date: June 21, 2012
    Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Marla L. Weetall
  • Publication number: 20120157373
    Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.
    Type: Application
    Filed: February 29, 2012
    Publication date: June 21, 2012
    Applicant: MEDTRONIC, INC.
    Inventors: Paul Hsien-Fu Wu, Catherine E. Taylor, Linnus Cheruiyot, Jianwei Li, Terese A. Bartlett, Matt Bergan
  • Publication number: 20120157401
    Abstract: Methods for treating neurofibromatosis involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.
    Type: Application
    Filed: May 27, 2010
    Publication date: June 21, 2012
    Inventors: Liangxian Cao, Thomas W. Davis, Harry H. Miao, Langdon Miller, Marla Weetall
  • Publication number: 20120157402
    Abstract: Methods for treating brain tumors involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatment.
    Type: Application
    Filed: May 27, 2010
    Publication date: June 21, 2012
    Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, langdon Miller, Marla Weetall
  • Publication number: 20120149661
    Abstract: The invention relates to tetra-substituted heteroarylic compounds of the formula (I) wherein X1, X3 and X4 are independently C or N, Y is C—H, N—H or N, wherein the total number of nitrogen atoms represented by X1, X3, X4 and Y is 1 or 2; rings A and B are independently selected from phenyl or pyridyl; R1, R4, R?, R?, n and m are as defined herein. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: August 24, 2010
    Publication date: June 14, 2012
    Applicant: NOVARTIS AG
    Inventors: Guido Bold, Pascal Furet, Francois Gessier, Joerg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Andrea Vaupel
  • Publication number: 20120149662
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).
    Type: Application
    Filed: August 27, 2010
    Publication date: June 14, 2012
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pravin L. Kotian, V. Satish Kumar, Minwan Wu, Tsu-Hsing Lin
  • Publication number: 20120148651
    Abstract: According to one embodiment, a coagulant comprising calcium nitrate and an antimicrobial agent is disclosed. The coagulant may be used in the molding process to releasably bond the substrate material to the mold and to bond to the antimicrobial to the substrate material.
    Type: Application
    Filed: December 10, 2010
    Publication date: June 14, 2012
    Applicant: MEDLINE INDUSTRIES INC.
    Inventors: Samuel T. Amdur, Min Yao
  • Publication number: 20120149653
    Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 14, 2012
    Inventors: Alexander Chucholowski, Alisher Khasanov, Gregory Parker, Tong Zhu
  • Publication number: 20120149660
    Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R2, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.
    Type: Application
    Filed: December 9, 2011
    Publication date: June 14, 2012
    Inventors: Jin-Jun Liu, Tina Morgan Ross
  • Publication number: 20120142633
    Abstract: The compounds of Formula (I), wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
    Type: Application
    Filed: August 24, 2010
    Publication date: June 7, 2012
    Applicant: NYCOMED GMBH
    Inventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Alexander Sudau, Torsten Dunkern, Ragna Hussong, Ewald Benediktus, Andreas Pahl
  • Publication number: 20120135958
    Abstract: The invention relates to compounds of formula (I), where: A is a bond, an oxygen, or an —CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are hydrogen or halogen, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally, substituted by one or more halogen atoms, or a —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, and to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano, —OR5, hydroxyalkyl, —COOR5, —NR6R7, ONR6R7, —
    Type: Application
    Filed: July 23, 2010
    Publication date: May 31, 2012
    Applicant: SANOFI
    Inventors: Claudie Namane, Eric Nicolai, Francois Pacquet, Cecile Pascal, Olivier Venier
  • Publication number: 20120134937
    Abstract: The present invention is directed to a stable, minimal energy required self-assembling lamellar and spherulitic composition comprising: mixture water, fatty alcohol, fatty acid, salt of fatty acid, polyglyceryl fatty acid ester and oils. The present invention relates to composition that can benefit eye mildness, even distribution of sunscreen physical filters on skin and enhanced stability.
    Type: Application
    Filed: January 14, 2010
    Publication date: May 31, 2012
    Inventors: Laurence Halimi, Mary Catherine Mack, Delores Santora, Blair Kim
  • Publication number: 20120122678
    Abstract: The present invention relates to 3-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.
    Type: Application
    Filed: January 26, 2012
    Publication date: May 17, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Klaus KUNZ, Ralf Dunkel, Jörg Nico Greul, Kerstin Ilg, Birgit Kuhn, Wahed Ahmed Moradi, Thomas Seitz, Darren James Mansfield, Oliver Guth, Peter Dahmen, Ulrike Wachendorff-Neumann, Arnd Voerste, Dale Robert Mitchell, Tom Hough, Jean-Pierre Vors
  • Publication number: 20120122816
    Abstract: The invention relates to reducing, preventing or reversing organ damage, reducing and/or preventing stem cell damage and/or death, enhancing organ preservation and/or survival, or enhancing stem cell preservation and/or survival comprising administering a compound of formula A, a compound of any one of formulae 1-49 or I-III, a lipoxin compound, an oxylipin compound, or a combination of aspirin and an omega-3 fatty acid.
    Type: Application
    Filed: February 5, 2010
    Publication date: May 17, 2012
    Applicant: Resolvyx Pharmaceuticals, Inc.
    Inventor: Per Gjorstrup
  • Publication number: 20120115812
    Abstract: The present invention relates to skin coating compositions and methods and, in particular, to coatings containing an active agent. In some embodiments, the coating may be applied to a skin surface and may be essentially colorless and transparent. In some aspects, the coating comprises a polymer and an active agent, and the polymer may be configured for sustained release of the active agent. In some aspects, the coating forms a barrier essentially impermeable to microorganisms yet permeable to water vapor. The coating may also be flexible and conformable to the surface. The coating may be applied to the skin using any suitable method. In some embodiments, the polymer and/or active agent are dissolved and/or suspended in a volatile solvent. In some embodiments, the volatile solvent may function as an antiseptic on skin.
    Type: Application
    Filed: January 17, 2012
    Publication date: May 10, 2012
    Applicant: Pharmasol Corporation
    Inventor: James Donald Hammer
  • Patent number: 8173622
    Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: May 8, 2012
    Assignee: Medtronic, Inc.
    Inventors: Paul Hsien-Fu Wu, Catherine E. Taylor, Linnus Cheruiyot, Jianwei Li, Terese A. Bartlett, Matt Bergan
  • Publication number: 20120107254
    Abstract: This disclosure relates to a long wear topical composition for keratinous surface. The composition includes at least one coupling agent having at least two reactive functional groups and at least one performance ingredient.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 3, 2012
    Inventor: Tianxiang Wang
  • Publication number: 20120107328
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Application
    Filed: November 3, 2008
    Publication date: May 3, 2012
    Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
  • Publication number: 20120108545
    Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Application
    Filed: May 19, 2010
    Publication date: May 3, 2012
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott