Naphthyl Ring System Patents (Class 514/481)
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Patent number: 10517835Abstract: The present invention relates to a composition comprising nanoparticles formed of a polymer and terbinafine, wherein the nanoparticles comprise particles in the range of 0.5 to 5 nm and/or in the range of 150 to 250 nm. Such compositions are particularly suited, but not limited, to the treatment of fungal nail infections.Type: GrantFiled: July 6, 2016Date of Patent: December 31, 2019Assignee: Bueberry Therapeutics LimitedInventors: John Ridden, Christine Caroline Ridden, David Cook
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Patent number: 9822145Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.Type: GrantFiled: August 4, 2016Date of Patent: November 21, 2017Assignee: Apicore US LLCInventors: Ravishanker Kovi, Jayaraman Kannapan, Vasanthakumar G Ramu, Alaparthi Lakshmi Prasad, Talluri Bhushaiah Chowdary, Gaurav Kulkarni, Saiyed Akeel Ahmed Shakeel Ahmed, Veerabhadra Rao Bobbili, N V Raghavalu Dusanapudi, Anand V. Mantri
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Patent number: 9522124Abstract: Pharmaceutical compositions for treating Alzheimer's disease are disclosed. The pharmaceutical compositions include a compound having the general formula: and a pharmaceutically acceptable carrier. Methods for treating Alzheimer's disease, inhibiting ATase I and/or ATase 2, reducing the activity of BACE1, reducing the level of amyloid ?-peptide (A?), and/or reducing the level of APP intracellular domain peptide (AICD) by administering such compositions are also disclosed.Type: GrantFiled: February 20, 2015Date of Patent: December 20, 2016Assignee: Wisconsin Alumni Research FoundationInventor: Luigi Puglielli
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Patent number: 9421275Abstract: The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: GrantFiled: March 24, 2014Date of Patent: August 23, 2016Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, David Martin
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Patent number: 9370179Abstract: A storage stable capsule suspension formulation comprising clomazone encapsulated within a polymeric shell wall of microcapsules, a process for the preparation thereof and method of controlling weeds utilizing said formulation.Type: GrantFiled: March 31, 2015Date of Patent: June 21, 2016Assignee: UPL LimitedInventors: Jaidev Rajnikant Shroff, Vikram Rajnikant Shroff, Prakash Mahadev Jadhav, Christian Becker
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Publication number: 20150056164Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: April 24, 2014Publication date: February 26, 2015Applicant: AbbVie Inc.Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
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Publication number: 20140370089Abstract: The present invention relates to a method for treating muscular dystrophy which comprises administering diethyl-[6-(4-hydroxycarbamoyl-phenyl-carbamoyloxy-methyl)-naphthalen-2-yl-methyl]-ammonium chloride or other pharmaceutically acceptable salts and/or solvates thereof to a patient in need of such a treatment. The invention further relates to a method for treating muscular dystrophy which comprises administering diethyl-[6-(4-hydroxycarbamoyl-phenyl-carbamoyloxy-methyl)-naphthalen-2-yl-methyl]-ammonium chloride or other pharmaceutically acceptable salts and/or solvates thereof in combination with one or more additional anti-inflammatory active agents to a patient in need of such a treatment.Type: ApplicationFiled: July 28, 2014Publication date: December 18, 2014Inventors: Valentina Saccone, Silvia Consalvi, Pier Lorenzo Puri, Paolo Mascagni
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Publication number: 20140323565Abstract: The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: ApplicationFiled: March 24, 2014Publication date: October 30, 2014Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, David Martin
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Patent number: 8722732Abstract: The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: GrantFiled: March 28, 2012Date of Patent: May 13, 2014Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, David Martin
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Publication number: 20140031331Abstract: 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: September 19, 2013Publication date: January 30, 2014Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
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Publication number: 20140011871Abstract: The subject invention is based upon the discovery that an antifungal agent can be delivered through the fingernail or the toenail of an infected human to treat onychomycosis by dissolving or dispersing the antifungal agent in a solvent system which is comprised of a combination of an alkyl lactate and Simmondsia chinesis seed oil. In accordance with this invention the antifungal agent is absorbed by and incorporated into the nail matrix by diffusing through the epithelium of the nail bed to reach the nail bed hyperkeratosis. The antifungal agent additionally penetrates into the ventral surface of the nail plate. The subject invention more specifically discloses an antifungal serum which is comprised of (1) an alkyl lactate, such as isoamyl lactate, (2) Simmondsia chinesis seed oil, and (3) an antifungal agent, such as tolnaftate or undecylenic acid.Type: ApplicationFiled: September 10, 2013Publication date: January 9, 2014Applicant: AD LUNAM LABSInventor: Turner Rockhill
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Patent number: 8609641Abstract: The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.Type: GrantFiled: December 13, 2004Date of Patent: December 17, 2013Assignee: UCB Pharma GmbHInventors: Dieter Scheller, Klaus Hansen
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Publication number: 20130281453Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.Type: ApplicationFiled: October 21, 2011Publication date: October 24, 2013Applicant: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
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Publication number: 20130203727Abstract: 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 treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 8, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
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Publication number: 20130137720Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.Type: ApplicationFiled: November 30, 2012Publication date: May 30, 2013Applicant: The Regents of the University of Colorado, a body corporatedInventors: Xiang Wang, Wenqing Xu
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Publication number: 20130052248Abstract: An item of clothing (10) for daily pharmacological treatment of a fungal infection, comprising: a textile material (20) to manage moisture when the item of clothing (10) is worn; microcapsules (30) grafted on the textile material (20); and antifungal agents encapsulated within the microcapsules (30) to pharmacologically treat the fungal infection when released from the microcapsules (30).Type: ApplicationFiled: August 26, 2011Publication date: February 28, 2013Inventors: Marcus Chun Wah YUEN, Joanne Yiu Wan YIP, Kevin CHEUK, Chi Wai KAN, Shuk Yan CHENG
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Publication number: 20120283216Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is O or S; Z1 and Z2 are each independently CR9 or N; and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 22, 2010Publication date: November 8, 2012Inventors: Alvin Donald Crews, JR., Amy X. Ding, Chi-Ping Tseng
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Publication number: 20120252870Abstract: Methods of diagnosing osteoarthritis are carried out by measuring levels of Ihh, and methods of treating osteoarthritis comprise inhibiting Ihh to reduce or prevent cartilage degradation.Type: ApplicationFiled: February 17, 2012Publication date: October 4, 2012Inventor: Lei Wei
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Publication number: 20120238621Abstract: The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: ApplicationFiled: March 28, 2012Publication date: September 20, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, David Martin
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Publication number: 20120220577Abstract: The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.Type: ApplicationFiled: June 4, 2010Publication date: August 30, 2012Inventors: Markus Henrich, Angela Hansen, Jens Nagel, Valerjans Kauss, Jevgenijs Rozhkovs, Ginta Grunsteine, Dina Trifanova
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Patent number: 8153686Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 31, 2009Date of Patent: April 10, 2012Assignee: Theravance, Inc.Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
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Publication number: 20120082646Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: March 25, 2010Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
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Publication number: 20120058199Abstract: The present invention provides the use of surface active proteins, especially class I and class II hydrophobins, in topically applied pharmaceutical formulations. The invention is particularly directed to topically applied pharmaceutical products for enhancing the penetration to achieve a transungual delivery of a prophylactically and/or therapeutically effective amount of an active ingredient (drug) to a patient (including animals and humans) into and/or through a nail, of the animal or human body, in order to treat one or more of a variety of diseases or disorders. Related embodiments of the invention are also disclosed.Type: ApplicationFiled: February 19, 2010Publication date: March 8, 2012Applicant: BASF SEInventors: Andreas Buthe, Andreas Hafner, Franz Kaufmann, Babette Fiedler, Guido Meurer, Gordon Bradley
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Publication number: 20110319416Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.Type: ApplicationFiled: January 28, 2010Publication date: December 29, 2011Applicant: EMORY UNIVERSITYInventors: Stephen F. Traynelis, Dennis C. Liotta, Cara Mosley, Timothy M. Acker, Sommer Zimmerman
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Publication number: 20110312875Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: December 22, 2011Applicant: UNIVERSITY OF WOLLONGONGInventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110251067Abstract: Three types of trisiloxane surfactants having the basic formula: MDM? are described wherein the substituents on the differing M and M? groups, in conjunction with pendant polyalkylene oxide substituents on the D group render the surfactant resistant to hydrolysis under either basic or acidic conditions outside the pH range of 6.0 to 7.5. The compositions are useful in agricultural, household and cosmetic applications.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Applicant: Momentive Performance Materials Inc.Inventors: George A. Policello, Mark D. Leathermani, Wenqing Peng, Suresh K. Rajaraman, Sophia Xia
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Publication number: 20110251146Abstract: A topical, foamable composition is provided that includes at least one antifungal agent that is able to penetrate the upper layers of skin and is retained in or on an area to be treated for a prolonged period of time, and that has a residual non-volatile component content less than 25%. In addition, a method of treating fungal diseases including jock itch, tinea, dandruff and sebborheic dermatitis is provided, and includes applying to the affected area of patient requiring such treatment an antifungal composition.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Applicant: STIEFEL RESEARCH AUSTRALIA PTY LTDInventors: Greg DAVEY, Albert Zorko ABRAM
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Publication number: 20110237595Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.Type: ApplicationFiled: June 9, 2011Publication date: September 29, 2011Applicant: SANOFI-AVENTISInventors: Ahmed ABOUABDELLAH, Regine BARTSCH-LI, Christian HOORNAERT, Antoine RAVET
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Patent number: 8003693Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: GrantFiled: July 28, 2006Date of Patent: August 23, 2011Assignees: The Regents of the University of California, Universita Degli Studi di Urbino, Universita Degl Studi di ParmaInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Publication number: 20110098253Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.Type: ApplicationFiled: December 28, 2010Publication date: April 28, 2011Applicant: Nicox S.A.Inventors: Richard Earl, Maiko Ezawa, Xinquin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20110076244Abstract: 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 an alcohol solvent. In some embodiments, the alcohol may function as an antiseptic on skin.Type: ApplicationFiled: September 24, 2010Publication date: March 31, 2011Applicant: Pharmasol CorporationInventor: James Donald Hammer
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Publication number: 20100204289Abstract: A viscose fiber having property modifying constituents such as thermoregulatory activity, antimicrobial activity, and perfumed and a method of making thereof is disclosed. Micro-reservoirs are formed in the fibers having thermoregulatory activity, antimicrobial constituents, and perfumed constituents.Type: ApplicationFiled: July 3, 2008Publication date: August 12, 2010Applicant: ADITYA BIRLA SCIENCE & TECHNOLOGY CO. LTD.Inventors: Preeti Lodha, Bir Kapoor, Tushar Mahajan
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Publication number: 20100137333Abstract: An antifungal composition is provided according to the present invention. The antifungal composition comprises an effective amount of an antifungal component to provide antifungal properties to skin tissue, an effective amount of a skin bonding polymer component to provide a sustained release of the antifungal component over a prolonged period of time after application of the antifungal treatment composition to skin tissue, and water. A method for using the antifungal composition is provided.Type: ApplicationFiled: October 19, 2007Publication date: June 3, 2010Inventor: James A. Roszell
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Publication number: 20100062083Abstract: The present invention is directed to liquid compositions containing chitosan, a chitosan derivative or a physiologically acceptable salt thereof, forming a dermal film after application onto the skin, useful for delivery of actives onto the skin surface and in the stratum corneum.Type: ApplicationFiled: December 13, 2007Publication date: March 11, 2010Applicant: POLICHEM S.A.Inventors: Federico Mailland, Michela Legora
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Publication number: 20090247627Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 31, 2009Publication date: October 1, 2009Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
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Publication number: 20090234001Abstract: The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, ZP, LP1, LP2 LNP, RP3, RN, and ZNP are defined herein, their preparation, pharmaceutical compositions, and methods of use.Type: ApplicationFiled: December 19, 2005Publication date: September 17, 2009Inventors: Lynn Stacy Gossett, Jose Eduardo Lopez, Alan M. Warshawsky, Ying Kwong Yee
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Patent number: 7572774Abstract: The present invention relates to the use of beta-naphthoquinone derivatives, and salts thereof, for the prevention and/or the treatment of glutamate cytotoxicity. It further relates to the use of beta-naphthoquinone derivatives, and salts thereof, for preventing and/or treating glutamate induced neurological disorders. Additionally, it concerns the use of beta-naphthoquinone derivatives, and salts thereof, for making drugs exerting an inhibitory effect on the release of glutamate.Type: GrantFiled: January 22, 2002Date of Patent: August 11, 2009Assignee: Centre National de la Recherche Scientific (C.N.R.S.)Inventors: Maurice Israel, Jordi Molgo, Christian Bloy, Cesar Mattei
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090099135Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a pest control product and at least one active agent, wherein: the active agent can be capable of interacting with a receptor in the target pest; the pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity.Type: ApplicationFiled: January 16, 2008Publication date: April 16, 2009Applicant: TyraTech, Inc.Inventor: Essam Enan
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Publication number: 20090042811Abstract: The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.Type: ApplicationFiled: June 12, 2006Publication date: February 12, 2009Inventors: Robert Bittman, Hoe-Sup Byun, Gilbert Arthur
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Patent number: 7208528Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: September 15, 1999Date of Patent: April 24, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7160923Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: November 14, 2000Date of Patent: January 9, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7102008Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, R1, R2, R3, R4, Z, U, X, Y, Za, and n are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP) and/or TNF-? converting enzyme (TACE), or a combination thereof.Type: GrantFiled: July 31, 2003Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Thomas P. Maduskuie
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Patent number: 7064130Abstract: A method of treatment of the human or non-human animal body for treating NO-dependent microcirculation disorders is disclosed, for example microcirculation disorders caused by metabolic diseases, such as elevated levels of homocystin-homocystein inflammatory reactions or autoimmune diseases, furthermore peripheral microcirculation disorders or microcirculation disorders associated with increased cell fragmentation, which method comprises administering to a human or non-human animal body in need of such treatment an effective amount of a pharmaceutical composition containing a substance which scavenges free radicals, e.g. a pyrimido-pyrimidine selected from Dipyridamole, Mopidamol and the pharmaceutically acceptable salts thereof, and the use such substance for the manufacture of a corresponding pharmaceutical composition, optionally in combination with an agent capable of increasing NO procution.Type: GrantFiled: April 12, 2002Date of Patent: June 20, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventor: Wolfgang Eisert
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Patent number: 7029706Abstract: The inventions relates to the use of silica in the formulation of antifungal composition for the treatment of cutaneous mycoses, and method to manufacture an antifungal powder with boric acid and silica.Type: GrantFiled: November 21, 2002Date of Patent: April 18, 2006Inventor: Carlos Alberto Marrodan
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Patent number: 6974832Abstract: The invention relates to compositions in the form of a powder or granules containing L-ascorbic acid and/or a pharmaceutically acceptable salt thereof, and pectin in a quantity within the range of about 0.1 to about 10% by weight.Type: GrantFiled: December 15, 2000Date of Patent: December 13, 2005Assignee: DSM Nutritional Products Inc.Inventors: Chyi-Cheng Chen, Bruno Leuenberger, Denise Voelki
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6835386Abstract: The present invention provides a device, preferably a collar or ear tag, capable of the controlled, sustained release of an effective amount of an active ingredient that can protect an animal against arthropod pests, comprising a reservoir containing a novel gel formulation comprising a fatty acid, an organic solvent which is a linear aliphatic ester, a silicone-based fluid, or a combination thereof, and an active ingredient that can protect the animal against one or more arthropod pests.Type: GrantFiled: October 18, 2002Date of Patent: December 28, 2004Assignee: Pfizer Inc.Inventor: Luis Gutierrez
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Patent number: RE39616Abstract: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: March 25, 2005Date of Patent: May 8, 2007Assignees: Teva Pharmaceutical Industries, Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation, Ltd.Inventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B. H. Youdim