Chalcogen Or Nitrogen Bonded Directly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/398)
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Publication number: 20110150819Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: ApplicationFiled: February 2, 2011Publication date: June 23, 2011Inventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Publication number: 20110150941Abstract: The present invention relates to composition comprising vesicles and associated with the vesicles, a chemical agent, for use in a method of treatment by therapy wherein the chemical agent is delivered trans- and/or intra-epithelially to a human or animal body, wherein the constructs comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block. Methods for forming the composition are also provided.Type: ApplicationFiled: May 14, 2009Publication date: June 23, 2011Applicant: Biocompatibles UK LimitedInventor: Giuseppe Battaglia
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Publication number: 20110142920Abstract: 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: ApplicationFiled: February 21, 2011Publication date: June 16, 2011Inventor: James N. Campbell
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Patent number: 7956076Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.Type: GrantFiled: April 8, 2009Date of Patent: June 7, 2011Assignee: City of HopeInventors: Yun Yen, David Horne, Yate-Ching Yuan, Bing-Sen Zhou, Angela L Perkins Harki, Leila Su
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Patent number: 7951958Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 12, 2010Date of Patent: May 31, 2011Assignee: Pfizer Inc.Inventors: Michael A. Brodney, Karen J. Coffman
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Publication number: 20110112151Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other thanType: ApplicationFiled: February 25, 2009Publication date: May 12, 2011Inventors: Nigel Vicker, Xiangdong Su, Fabienne Pradaux-Caggiano, Barry Victor Lioyd Potter
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Publication number: 20110104305Abstract: Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis, cancer and/or another condition responsive to stimulation of thiol-containing compound transport.Type: ApplicationFiled: June 30, 2010Publication date: May 5, 2011Inventors: Brian J. DAY, Remy KACHADOURIAN
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Publication number: 20110097384Abstract: A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.Type: ApplicationFiled: December 29, 2010Publication date: April 28, 2011Inventors: David Kanios, Juan A. Mantelle, Viet Nguyen
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Publication number: 20110097375Abstract: An implantable drug depot useful for preventing, reducing or treating bleeding at a surgical site beneath the skin in a patient is provided. The implantable drug depot comprises a therapeutically effective amount of clonidine or a pharmaceutically acceptable salt thereof, and at least one biodegradable polymer. The drug depot is capable of releasing clonidine or a pharmaceutically acceptable salt thereof over a period of at least three days.Type: ApplicationFiled: October 26, 2009Publication date: April 28, 2011Applicant: Warsaw Orthopedic, Inc.Inventor: Vanja Margareta King
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Publication number: 20110092553Abstract: The present invention provides azole derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and their use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.Type: ApplicationFiled: November 19, 2010Publication date: April 21, 2011Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Dharma R. Polisetti, Govindan Subramanian, James C. Quada, JR., Murty N. Arimilli, Ravindra R. Yarragunta, Robert C. Andrews, Rongyuan Xie
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Publication number: 20110092517Abstract: Provided herein are methods for treatment, prevention, or amelioration of one or more symptoms of a disease or condition related to disorders of insulin and/or glucose metabolism, inflammatory conditions, mitochondrial disease, muscle disorders, or pulmonary disorders, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist. In one embodiment, the disease or condition is selected from myopathy, inflammatory vascular diseases, Parkinson's and Alzheimer's diseases, systemic inflammatory disorders, renal ischemia, inflammatory rheumatic disorders, and inflammatory diseases of the lung. In another embodiment, methods for increasing oxidative muscle fibers, reducing mitochondria disease, decreasing insulin resistance, decreasing plasma glucose, or decreasing weight, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist, are provided.Type: ApplicationFiled: August 13, 2010Publication date: April 21, 2011Inventors: Ronald Barbaras, Daniela Carmen Oniciu, Jean-Louis H. Dasseux, Robert A. Scott, John R. Wetterau
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Publication number: 20110092557Abstract: The present invention provides compounds comprising amino acid R groups, compositions comprising the same, and methods of inhibiting neuraminidase and/or treating influenza, Pseudomonas aeruginosa, or Bacteroides fragilis infection in a mammal.Type: ApplicationFiled: June 24, 2009Publication date: April 21, 2011Applicant: INFLUMEDIX INC.Inventors: Xiaodong Fan, Lidia Cristian
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Publication number: 20110091511Abstract: A blend of at least two polymers in combination with a drug provides a pressure-sensitive adhesive composition for a transdermal drug delivery system in which the drug is delivered from the pressure-sensitive adhesive composition and through dermis when the pressure-sensitive adhesive composition is in contact with human skin. According to the invention, providing drug having differing crystal sizes as well as drug which is solublized in the pressure-sensitive adhesive composition controls the rate of drug delivery from the pressure-sensitive adhesive composition.Type: ApplicationFiled: December 28, 2010Publication date: April 21, 2011Inventor: Viet Nguyen
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Patent number: 7928132Abstract: Methods of ameliorating episodes of accute or chronic colitis are provided by using methimazole derivatives and tautomeric cyclic thiones in combination with another pharmaceutical compound.Type: GrantFiled: August 6, 2004Date of Patent: April 19, 2011Assignee: Ohio UniversityInventors: Leonard D. Kohn, Douglas J. Goetz, Uruguaysito Benavides-Peralta, Mariana Gonzalez-Murguiondo, Norikazu Harii, Christopher J. Lewis, Giorgio Napolitano, Nilesh D. Dagia
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Publication number: 20110071137Abstract: The present invention relates to a novel process for preparing sustained release tablets containing medicinal compounds and the products prepared by said process. The present invention is directed to a method of preparing a sustained release pharmaceutical composition having a predetermined drug release profile, but which is deviated therefrom by adding a tableting effective amount of a water insoluble or partially insoluble cellulose, to said pharmaceutical composition comprised of a drug in a therapeutically effective amount, and sustained release carrier present in amounts effective retard the release of the drug from the pharmaceutical composition and said cellulose, the latter being present in an aqueous system, the improvement comprising adding to the composition an effective amount of maltodextrin to retard the increase on the rate of release of the drug from the addition of said cellulose thereto.Type: ApplicationFiled: August 20, 2010Publication date: March 24, 2011Applicant: NOSTRUM PHARMACEUTICALS, INC.Inventor: Nirmal Mulye
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Patent number: 7906544Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: January 25, 2008Date of Patent: March 15, 2011Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Publication number: 20110053901Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.Type: ApplicationFiled: February 13, 2009Publication date: March 3, 2011Applicants: SIGNUM BIOSCIENCES, INC., Signum Biosciences, Inc.Inventors: Seung-Yub Lee, Michael Voronkov, Peter Wolanin
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110034483Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: February 18, 2009Publication date: February 10, 2011Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
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Patent number: 7884090Abstract: The present invention provides compositions, combination of medicaments, and methods for the treatment of certain conditions such as arthritis, and in particular, reactive arthritis, osteoarthritis, and bursitis, among others.Type: GrantFiled: December 7, 2005Date of Patent: February 8, 2011Inventors: Ernest L. Bonner, Jr., Robert Hines
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Publication number: 20110028528Abstract: When an organosilicone surface active agent is added to a pesticidal aqueous suspension composition containing an active ingredient compound of a sparingly water-soluble pesticide for the purpose of attaining activity enhancement and formulation, the following problems arise: such that (1) the viscosity of the composition increases; (2) a large amount of foams due to the organosilicone surface active agent tends to generate at the time of preparation of a spray solution; and the like. Thus, measuring the composition and preparation of a spray solution were difficult.Type: ApplicationFiled: March 31, 2009Publication date: February 3, 2011Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yoshiaki Ishihara, Takeshi Shindo
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Publication number: 20110020457Abstract: A polymer-surfactant nanoparticle formulation, using the anionic surfactant aerosol OT (AOT) and polysaccharide polymer alginate, is used for sustained release of water-soluble drugs. The AOT-alginate nanoparticles are suitable for encapsulating doxorubicin, verapamil and clonidine, as well as therapeutic agents effective against dermal conditions such as psoriasis. The nanoparticles are also suitable for encapsulating photo-activated compounds such as methylene blue for use in photo-dynamic therapy of cancer and other diseases, and for treating tumor cells that exhibit resistance to at least one chemotherapeutic drug.Type: ApplicationFiled: August 14, 2007Publication date: January 27, 2011Inventors: Jayanth Panyam, Mahesh D. Chavanpatil
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Publication number: 20110008271Abstract: Described herein are novel methods for the treatment of rosacea which include the step of applying of a composition containing a polymetal complex to an area of the skin afflicted with rosacea and novel regimens using such compounds.Type: ApplicationFiled: July 7, 2010Publication date: January 13, 2011Applicant: JR CHEM, LLCInventors: Hovig Ounanian, José E. Ramirez, Joseph R. Faryniarz
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Publication number: 20110008465Abstract: A pharmaceutical composition comprising a water insoluble sesquiterpene, one or more antioxidants and one or more solubilizers selected from the group consisting of an oil, PEG400, a derivative of castor oil and ethylene oxide, and polysorbate 80, and methods of use thereof.Type: ApplicationFiled: June 2, 2008Publication date: January 13, 2011Inventors: Jean Legault, Andre Pichette, Serge Lavoie
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Publication number: 20110003011Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.Type: ApplicationFiled: July 8, 2010Publication date: January 6, 2011Applicant: Bayer CropScience AGInventors: Wilhelm BRANDES, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Krüger
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Patent number: 7858653Abstract: The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2— or —CH2—; and Ar is phenyl or naphthyl, which rings are optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy, lower alkyl and lower alkyl substituted by halogen; or a pharmaceutically-acceptable acid-addition salt thereof; with the proviso that, when X is —NH—, Y is —CH(lower alkyl)- or —CH2—; and the further proviso that the compound is not 2-phenethyl-1H-imidazole hydrochloride, 2-(3,4-dichloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2-chloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2,3-dichloro-phenoxymethyl)-1H-imidazole, benzyl-(1H-imidazol-2-yl)-amine, (4-chloro-benzyl)-(1H-imidazol-2-yl)-amine, or (2-chloro-benzyl)-(1H-imidazol-2-yl)-amine.Type: GrantFiled: December 5, 2007Date of Patent: December 28, 2010Assignee: Hoffman-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20100323979Abstract: The present invention relates, in part, to the use of AMP kinase agonists to reduce or inhibit the proliferation of aneuploid cells. The invention is also directed to the use AMP kinase agonists to reduce or inhibit the proliferation of solid tumors characterized by aneuploidy in an individual.Type: ApplicationFiled: June 16, 2010Publication date: December 23, 2010Inventors: Angelika B. Weis-Amon, Yun-Chi Tang
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Patent number: 7855221Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: GrantFiled: September 29, 2009Date of Patent: December 21, 2010Assignee: Theravance, Inc.Inventors: Robert S. Chao, Weijiang Zhang
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Publication number: 20100317707Abstract: The invention provides (among other things) small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer.Type: ApplicationFiled: October 31, 2008Publication date: December 16, 2010Applicant: Nektar TherapeuticsInventors: Zhongxu Ren, Jennifer Riggs-Sauthier, Michael D. Bentley
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Patent number: 7851565Abstract: Disclosed are water soluble polymeric reagents comprising the structure POLY-[Y—S—W]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, and S—W is a thiol, protected thiol, or thiol-reactive derivative. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are conjugates of such polymeric reagents with pharmaceutically relevant molecules, and methods of their formation and use.Type: GrantFiled: December 21, 2005Date of Patent: December 14, 2010Assignee: Nektar TherapeuticsInventors: Antoni Kozlowski, Samuel McManus
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Patent number: 7851497Abstract: To provide an improved fungicidal composition for agricultural or horticultural use, and a method for controlling plant diseases by applying the composition to plants. A fungicidal composition for agricultural or horticultural use, which comprises at least one imidazole compound of the formula (I): wherein R is a C1-6 alkyl group or a C1-6 alkoxy group, and n is an integer of from 1 to 5, and propamocarb hydrochloride, as active ingredients; and a method for controlling plant diseases by applying the composition to plants.Type: GrantFiled: July 14, 2005Date of Patent: December 14, 2010Assignee: Ishihara Sangyo Kaisha, Ltd.Inventor: Koji Sugimoto
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Publication number: 20100310480Abstract: The methods described herein provide treatment of rosacea using topical formulations of dapsone. The methods also provide treatment of rosacea with topical dapsone in combination with other active agents, including metronidazole. The methods avoid negative hematologic side effects, including hemolysis and hemolytic anemia, that are associated with oral administration of dapsone.Type: ApplicationFiled: February 27, 2008Publication date: December 9, 2010Inventor: John S. Garrett
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Publication number: 20100305178Abstract: A topical composition comprises at least 5-wt % metronidazole or a pharmacologically acceptable derivative thereof in a non-aqueous vehicle. The composition may be used in the treatment of conditions of the colon, rectum, anorectum and perianal region, in particular inflammatory bowel disease and perianal Crohn's disease. The composition also relieves pain and inflammation and promotes healing of the colon, rectum, and anorectum and perianal region following surgical operations. One advantage of the composition is that topical administration of metronidazole results in a primarily local effect and thus side effects observed from systemic administration are avoided.Type: ApplicationFiled: July 12, 2010Publication date: December 2, 2010Applicant: Armstrong Medical Inc.Inventor: David Nigel Armstrong
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Publication number: 20100305105Abstract: Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein.Type: ApplicationFiled: November 16, 2007Publication date: December 2, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Marc Harris Levin
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Publication number: 20100303718Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.Type: ApplicationFiled: August 11, 2010Publication date: December 2, 2010Inventor: David Anderson
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Publication number: 20100303799Abstract: Techniques are disclosed for prevention or treatment of physiological shock by administering a specific therapeutic agent, which is able to use smaller volumes of reagent to achieve complete inhibition, than other previously described techniques.Type: ApplicationFiled: October 6, 2008Publication date: December 2, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Geert W. Schmid-Schönbein, Frank A. DeLano
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Publication number: 20100292274Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100273739Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: February 16, 2010Publication date: October 28, 2010Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
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Publication number: 20100273833Abstract: The invention relates to 2-sulfinyl- or 2-sulfonyl-substituted imidazole derivatives of the formula (I) in which the radicals R1, R2, R3 and R4 have the meaning indicated in the description. The compounds of the invention have an immunomodulating and/or cytokine release-inhibiting effect and are therefore suitable for the treatment of disorders associated with an impairment of the immune system.Type: ApplicationFiled: February 27, 2006Publication date: October 28, 2010Inventors: Wolfgang Albrecht, Cornelia Greim, Hans-Gunter Striegel, Karola Tollmann, Philipp Merkle, Stefan Laufer
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Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
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Patent number: 7812026Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: GrantFiled: December 21, 2006Date of Patent: October 12, 2010Assignee: AstraZeneca ABInventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100256081Abstract: Bioactive, hydroforming luminal liner compositions are formed of high molecular weight crystalline, absorbable copolyesters dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: ApplicationFiled: April 5, 2010Publication date: October 7, 2010Inventors: Shalaby W. Shalaby, Kenneth David Gray, Georgios T. Hilas
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Publication number: 20100256192Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity 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: ApplicationFiled: December 29, 2009Publication date: October 7, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20100249132Abstract: Compounds of the formula (I), in which R1, D, E, L, Q, X and q have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.Type: ApplicationFiled: September 9, 2008Publication date: September 30, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Melanie Schultz, Kai Schiemann, Gerard Botton, Andree Blaukat, Ingo Kober
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Publication number: 20100247433Abstract: The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handle” to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.Type: ApplicationFiled: October 16, 2006Publication date: September 30, 2010Applicant: California Institute of TechnologyInventors: David Tirrell, Daniela C. Dieterich, Aaron J. Link, Erin Schuman
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Publication number: 20100239690Abstract: A composition for oral cavity and skin which contains an antibacterial agent and does not have adverse side effects due to steroids, is provided. The composition contains 0.01 to 4.5% by mass of at least one selected from the group consisting of an antibacterial agent, an antiviral agent, an anti-HIV agent, a non-nucleic acid-based reverse transcriptase inhibitor, an anticancer agent for external use and a disinfectant; 0.01 to 4.5% by mass of a non-steroidal anti-inflammatory agent; 0.001 to 4.5% by mass of a steroidal anti-inflammatory agent; and 0.001 to 10% by mass of a highly water-absorbent polymer or a cellulose derivative.Type: ApplicationFiled: September 19, 2008Publication date: September 23, 2010Inventor: Satoshi Noda
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Publication number: 20100239632Abstract: Effective treatments of pain and/or inflammation are provided. Through the administration of a biodegradable drug depot film, patch, strip or sponge being implantable at or near a cardiac tissue or within a nasal or sinus cavity, one can reduce, prevent or treat pain and/or inflammation.Type: ApplicationFiled: March 23, 2009Publication date: September 23, 2010Applicant: Warsaw Orthopedic, Inc.Inventor: Andrew J. Lowenthal WALSH
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Patent number: 7799797Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, q, Ar, R1, R2 and R7 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: GrantFiled: June 20, 2007Date of Patent: September 21, 2010Assignee: Roche Palo Alto LLCInventor: Ralph New Harris, III