Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/329)
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Publication number: 20110105465Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.Type: ApplicationFiled: May 29, 2009Publication date: May 5, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
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Publication number: 20110105551Abstract: An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours. The analgesic may be an opioid analgesic or a non-steroidal anti-inflammatory drug.Type: ApplicationFiled: January 12, 2011Publication date: May 5, 2011Applicants: Vernalis (R&D) Limited, Archimedes Development CorporationInventors: Phillip John Birch, Ann Gail Hayes, Peter James Watts, Jonathan David Castile
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Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Publication number: 20110098281Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 8, 2008Publication date: April 28, 2011Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Jiangchao Yao
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Publication number: 20110098322Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.Type: ApplicationFiled: August 5, 2008Publication date: April 28, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: James R. Sanborn, Bruce D. Hammock, Sung Hee Hwang, Paul D. Jones, Christophe Morisseau
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Publication number: 20110092482Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic or inflammatory pain including a neuropathic or inflammatory component of nociceptive pain. More particularly, the present invention provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic or inflammatory pain. The present invention further contemplates combination therapy involved in the treatment of pain in association with the treatment of a particular disease condition or pathology. The present invention further also provides sustained and slow release formulations, tamper-proof deliver systems and stents, catheters and other mechanical devices coated with formulations which permit sustained or slow release of active ingredients involved in pain management.Type: ApplicationFiled: December 1, 2010Publication date: April 21, 2011Applicant: RELEVARE AUST. PTY LTDInventors: Raymond Nadeson, Adam Paul Tucker, Colin Goodchild
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Publication number: 20110077247Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Applicant: DAC S.r.I.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20110073518Abstract: Fentanyl containing dosage forms and methods using same are described. These dosage forms include substantially less fentanyl by weight than know oral formulation and have advantages in terms of cost and side effects. These dosage forms are intended for oral administration of fentanyl across the oral mucosa.Type: ApplicationFiled: November 29, 2010Publication date: March 31, 2011Applicant: CIMA LABS INC.Inventors: Derek Moe, Vikas Agarwal, Walid Habib
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Publication number: 20110070169Abstract: Fentanyl-containing dosage forms and methods using same are described. These dosage forms include substantially less fentanyl by weight than known oral formulation and have advantages in terms of reduced cost and reduced side effects. These dosage forms are intended for oral administration of fentanyl across the oral mucosa.Type: ApplicationFiled: November 29, 2010Publication date: March 24, 2011Applicant: CIMA LABS INC.Inventors: Derek Moe, Vikas Agarwal, Walib Habib
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Publication number: 20110071181Abstract: Opiate containing dosage forms and methods using same are described. These dosage forms include substantially less opiates by weight than known oral formulations. These dosage forms are intended for oral administration across the oral mucosa.Type: ApplicationFiled: November 29, 2010Publication date: March 24, 2011Applicant: CIMA LABS INC.Inventor: Derek Moe
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Publication number: 20110059971Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: IPSEN S.A.S.Inventors: Christophe THURIEAU, Jérôme Gonzalez, Christophe Moinet
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Publication number: 20110052645Abstract: An extrusion process comprises extruding a material that is flowable when heated and passing the extrudate thus formed through a nozzle 10 to shape the extrudate into a plurality of substantially uniformly shaped elements such as minispheres or minicapsules.Type: ApplicationFiled: April 25, 2008Publication date: March 3, 2011Inventor: Ivan Coulter
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Publication number: 20110046180Abstract: This invention relates to novel N-aryl-N-piperidin-4-yl-propionamide derivatives useful as opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: December 18, 2008Publication date: February 24, 2011Applicant: NeuroSearch A/SInventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen
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Publication number: 20110038918Abstract: A transdermal drug delivery composition comprises an acrylate copolymer and from about 8% to about 30% by weight fentanyl. A transdermal fentanyl delivery composition comprising methyl laurate or tetraglycol as a permeation enhancer is also provided. The transdermal drug delivery compositions can be used to make a transdermal drug delivery device for the delivery of fentanyl.Type: ApplicationFiled: August 6, 2010Publication date: February 17, 2011Inventors: Adam S. Cantor, Terrance W. Ocheltree, Cynthia A. Robles
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Publication number: 20110039800Abstract: The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active principle dissolution test of more than 70% over 8 hours and to a method for its preparation. Said bioadhesive therapeutic system comprises quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and comprising between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar.Type: ApplicationFiled: July 2, 2010Publication date: February 17, 2011Inventors: Jean-Marc AIACHE, Dominique Costantini, Christine Chaumont
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Publication number: 20110034511Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)? or N?; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively.Type: ApplicationFiled: September 28, 2010Publication date: February 10, 2011Applicant: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Michael Philip Cohen, Sandra Ann Filla, Kevin John Hudziak, Daniel Timothy Kohlman, Dana Rae Benesh, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Brian Michael Mathes
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Publication number: 20110034417Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: ApplicationFiled: October 5, 2010Publication date: February 10, 2011Applicant: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Publication number: 20110028515Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.Type: ApplicationFiled: July 23, 2010Publication date: February 3, 2011Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Publication number: 20110020450Abstract: The present invention relates to a titratable dosage transdermal delivery system for systemic delivery of a therapeutic agent or drug. The system comprises a plurality of patch units that are connected along one or more borders. The plurality of patch units are divisible into units along the one or more borders having one or more lines of separation. Each patch unit is surrounded by a border. The therapeutic patch has at least a backing layer and a therapeutic agent comprising layer. The dosage of therapeutic agent delivered to a patient is proportional to the number of patch unit applied per treatment. The system enables systemic administration of a titratable dosage of therapeutic agent, adjustable by the patient under the direction of a physician, through the skin or mucosa. Moreover, the invention relates to a method of making the titratable dosage transdermal delivery system.Type: ApplicationFiled: September 30, 2010Publication date: January 27, 2011Inventor: Curtis Wright, IV
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Publication number: 20110021565Abstract: The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5? or to a pharmaceutically active salt thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 4, 2010Publication date: January 27, 2011Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian, Xihan Wu
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Publication number: 20110021972Abstract: Device structure 100 for iontophoresis provides electrode 101 and electrically conductive layer 102. Electrically conductive layer 102 contains active ingredient D and basic water swelling methacrylate copolymer P1 and/or acidic water swelling methacrylate copolymer P2. Electrode 101 and electrically conductive layer 102 are placed into a hollow of backing 103 and electrode terminal 104 is connected to electrode 101 through backing 103. Adhesive layer 105 is set around backing 103, and liner 106 to be removed when using the device, is placed so as to cover the hollow of backing 103.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: HISAMITSU PHARMACEUTICAL CO., INC.Inventors: Hirotoshi Adachi, Noriyuki Kuzumaki, Tetsuya Arimoto, Naruhito Higo
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TRANSDERMAL THERAPEUTIC SYSTEM WITH HIGH RATE OF UTILIZATION OF ACTIVE SUBSTANCE AND DOSING ACCURACY
Publication number: 20110020407Abstract: Transdermal therapeutic system with which at least one pharmaceutical active substance that is non-volatile at room temperature can be administered at a daily dose of at most 30 mg, comprising a rear surface directed away from the skin and impermeable to the active substance, an adjoining polymer layer located away from the skin and based on polyisobutylene with a coating weight of at least 80 g/m2, an adhesive skin contact layer resting on the skin-remote polymer layer and based on acrylate copolymers with a coating weight of at most 50 g/m2, and a protective layer that is impermeable to the active substance and can be peeled off from the skin contact layer.Type: ApplicationFiled: November 9, 2007Publication date: January 27, 2011Applicant: LTS Lohmann Therapie-Systeme AGInventors: Michael Horstmann, Walter Mueller -
Publication number: 20110009449Abstract: This invention relates to N-aryl-N-piperidin-4-yl-propionamide derivatives for use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds, and to novel compounds.Type: ApplicationFiled: December 18, 2008Publication date: January 13, 2011Inventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen
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Publication number: 20110003855Abstract: Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.Type: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: The Regents of the University of CaliforniaInventors: Thomas C. Hermann, Maia Carnevali
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Publication number: 20100330150Abstract: The present invention is directed to pharmaceutical compositions comprising a plurality of taste-masked high-dose/low-dose drug-containing microparticles, dosage forms comprising such pharmaceutical compositions (such as an orally disintegrating tablet), and methods of making the pharmaceutical compositions and dosage forms of the present invention. Dosage forms comprising the pharmaceutical compositions of the present invention are improved homogeneous blends of high-dose and low-dose drugs which provide for more convenient and palatable administration of drug combinations, for example for treating pain, hyperglycemia, cardiovascular disease, and allergies.Type: ApplicationFiled: May 3, 2010Publication date: December 30, 2010Inventors: Gopi Venkatesh, Michael Gosselin, James Clevenger, Jin-Wang Lai
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Publication number: 20100331354Abstract: The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.Type: ApplicationFiled: May 28, 2010Publication date: December 30, 2010Inventor: Daniel P. Wermeling
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Publication number: 20100322999Abstract: A patch for external use which has a laminate structure comprising a substrate and a pressure-sensitive adhesive layer which contains a styrene/isoprene/styrene block copolymer as the base and further contains a tackifier resin consisting of a rosin resin and at least one other tackifier resin, a softening agent consisting of polybutene and liquid paraffin, a fatty acid ester, and fentanyl, characterized in that the weight ratio of the rosin resin to fentanyl is 1 to 5, the weight ratio of the rosin resin to the whole tackifier resin is 0.1 to 0.6, and the tackifier resin accounts for 30 to 60wt % of the whole pressure-sensitive adhesive layer. The patch is excellent in the permeation of fentanyl through the skin and in storage stability, and is weak in irritation to skin.Type: ApplicationFiled: January 26, 2009Publication date: December 23, 2010Inventors: Kunihiko Matsushita, Mamoru Naruse, Kenichi Hattori
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Publication number: 20100317678Abstract: Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: wherein Q, V and W independently represent —N? or —C?; B is a divalent radical selected from (B1), (B2), (B3), (B4), (B5) and (B6).Type: ApplicationFiled: October 30, 2006Publication date: December 16, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Francesca Ann Day, Sanjay Ratilal Patel, Andrew James Belfield, Alistair David Graham Donald, Alan Hornsby Davidson, Alan Hastings Drummond
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Publication number: 20100311665Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.Type: ApplicationFiled: August 2, 2010Publication date: December 9, 2010Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Anil Gulati
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Publication number: 20100311794Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Gilead Sciences, Inc.Inventor: Chandrasekar Venkataramani
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Publication number: 20100311792Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: September 26, 2008Publication date: December 9, 2010Inventors: Bin Shao, Jiangchao Yao
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Publication number: 20100300438Abstract: A drug delivery system includes drug containers, a pump assembly, a sensor, and a controller. The drug containers each contain a different predetermined drug co-formulation of predetermined first and second drugs, wherein the first drug has a sedative effect. The sensor is adapted to sense a variable associated with the drug containers and output a different drug co-formulation identification signal associated with each of the drug containers based on the sensed variable. The controller is programmed to identify the drug co-formulation for the drug container operatively connected to the pump assembly from the associated identification signal and to control the pump assembly to deliver the drug co-formulation of the one drug container to the patient during a medical procedure according to a corresponding drug delivery algorithm which is different for each of the drug containers. A method is also disclosed which uses the drug delivery system.Type: ApplicationFiled: June 1, 2009Publication date: December 2, 2010Applicant: ETHICON ENDO-SURGERY, INC.Inventors: James F. Martin, Paul Bruggeman
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Publication number: 20100291182Abstract: Implants and methods for the delivery of a therapeutic agent to a target location within a patient's body are disclosed. The implants include a fiber comprising a polymeric material and having a diameter of up to about twenty microns, and a first therapeutic agent within the fiber. The therapeutic agent is substantially in particulate form. The implants are of a variety of configurations, such as individual fibers, yarns, ropes, tubes, and patches.Type: ApplicationFiled: November 17, 2009Publication date: November 18, 2010Applicant: Arsenal Medical, Inc.Inventors: Maria Palasis, Upma Sharma, Quyhn Pham, John Marini
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Publication number: 20100286204Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0Type: ApplicationFiled: November 19, 2008Publication date: November 11, 2010Applicant: Sterix LimitedInventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
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Patent number: 7829582Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 27, 2007Date of Patent: November 9, 2010Assignee: Eli Lilly and CompanyInventors: Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
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Publication number: 20100279998Abstract: The present invention relates to piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Applicant: SANOFI-AVENTISInventors: Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Jean Jeunesse
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Publication number: 20100273782Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Baaum
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100267669Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: ApplicationFiled: June 10, 2010Publication date: October 21, 2010Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20100260813Abstract: A rodenticidal mixture comprising a) 0.0015 to 99.89% by weight of at least one rodenticide, b) 10?8 to 95% by weight of at least one painkiller and c) 0.01 to 99.9984% by weight of at least one biocide, where the percentages by weight are based on the total of components (a), (b) and (c), is suitable for the preparation of rodenticidal bait formulations which are employed for controlling rodent pests.Type: ApplicationFiled: September 30, 2008Publication date: October 14, 2010Applicant: BASF SEInventors: Gerhard Schnabel, Michael Ishaque, Dieter Zeller, Lars Weichel, Andrej Brejc
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Publication number: 20100260833Abstract: The invention relates to a solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: GRUNENTHAL GMBHInventors: Johannes BARTHOLOMÄUS, Heinrich Kugelmann
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Publication number: 20100261747Abstract: The present invention provides a standardized method for the detection of narcotic abuse. Narcotics are formulated with a test compound that is not completely metabolized by the body. Narcotic diversion is detected by urinalysis of the suspected abuser, wherein the test compound may be detected even if the diverted narcotic is completely metabolized by the body, or otherwise undetectable in the urine.Type: ApplicationFiled: December 17, 2008Publication date: October 14, 2010Inventor: Peter D. Winch
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Publication number: 20100255073Abstract: A transdermal drug delivery composition comprises an acrylate copolymer and from about 8% to about 30% by weight fentanyl. A transdermal fentanyl delivery composition comprising methyl laurate or tetraglycol as a permeation enhancer is also provided. The transdermal drug delivery compositions can be used to make a transdermal drug delivery device for the delivery of fentanyl.Type: ApplicationFiled: June 22, 2010Publication date: October 7, 2010Inventors: Adam S. Cantor, Terrance W. Ocheltree, Cynthia A. Robles
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Publication number: 20100249045Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.Type: ApplicationFiled: April 26, 2008Publication date: September 30, 2010Applicant: THERAQUEST BIOSCIENCES, INC.Inventor: Najib Babul
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Publication number: 20100240690Abstract: Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.Type: ApplicationFiled: March 22, 2010Publication date: September 23, 2010Applicant: Adolor CorporationInventor: John D. Buehler
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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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Publication number: 20100233257Abstract: The present invention relates to a sublingual tablet and to the method for the preparation thereof.Type: ApplicationFiled: June 8, 2007Publication date: September 16, 2010Applicant: EthypharmInventors: Catherine Herry, Pascal Oury
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Publication number: 20100234426Abstract: The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the activation of opioid receptors, particularly ?-opioid receptors. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: October 31, 2007Publication date: September 16, 2010Applicant: Purdue Pharma L.P.Inventor: Xiaoming Zhou
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Publication number: 20100227876Abstract: The invention provides for compositions and methods of reducing pain in a subject by administering a combination of mu-opioid receptor agonist, kappa1-opioid receptor agonist and a nonselective opioid receptor antagonist in amounts effective to reduce pain and ameliorate an adverse side effect of treatment combining opioid-receptor agonists. The invention also provides for methods of enhancing an analgesic effect of treatment with an opioid-receptor agonist in a subject suffering from pain while reducing an adverse side effect of the treatment. The invention also provides for methods of reducing the hyperalgesic effect of treatment with an opioid-receptor agonist in a subject suffering from pain while reducing an adverse side effect of the treatment. The invention further provides for methods of promoting the additive analgesia of pain treatment with an opioid-receptor agonist in a subject in need while reducing an adverse side effect of the treatment.Type: ApplicationFiled: March 6, 2009Publication date: September 9, 2010Applicant: RECHFENSEN LLPInventor: Richard H. Rech
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Publication number: 20100227886Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.Type: ApplicationFiled: April 13, 2010Publication date: September 9, 2010Inventors: David M. WEINER, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam