Ring In Acid Moiety Patents (Class 514/484)
  • Patent number: 11776800
    Abstract: A substance analyzer that includes, to enhance selectivity of substance analysis, the following: a heater that heats a medium for collecting a chemical substance adhering to a surface of an inspection object; a mass spectrometer that performs tandem mass spectrometry of vapor derived from the chemical substance heated and vaporized by the heater from the medium; and a control device that causes the mass spectrometer to perform, based on a temperature of the medium in the heater, tandem mass spectrometry for the chemical substance that is vaporized at the temperature of the medium using the vapor sent from the heater to the mass spectrometer.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: October 3, 2023
    Assignee: Hitachi High-Tech Corporation
    Inventors: Yasuaki Takada, Shun Kumano, Masuyuki Sugiyama, Tsukasa Shishika, Shinji Yoshioka, Akimasa Osaka
  • Patent number: 9872847
    Abstract: The present invention provides a pharmaceutical composition for preventing and/or treating a movement disorder comprising the phenyl carbamate compound as an active ingredient, and a use of the phenyl carbamate compound for preventing and/or treating movement disorder.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: January 23, 2018
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9745255
    Abstract: The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: August 29, 2017
    Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Technologia, Universita Degli Studi di Urbino “Carlo Bo”, Universita Degli Studi di Parma
    Inventors: Daniele Piomelli, Guillermo Moreno-Sanz, Tiziano Bandiera, Marco Mor, Giorgio Tarzia
  • Publication number: 20150133541
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Application
    Filed: January 13, 2015
    Publication date: May 14, 2015
    Inventor: Yong Moon Choi
  • Patent number: 9029589
    Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: May 12, 2015
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9018253
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Grant
    Filed: July 1, 2011
    Date of Patent: April 28, 2015
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9012497
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: April 21, 2015
    Assignee: Symrise AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20150072004
    Abstract: Sustained release oral dosage forms of a gabapentin prodrug, 1-{[(?-isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetic acid, are disclosed. The dosage forms are useful for treating or preventing diseases and disorders for which gabapentin is therapeutically effective.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 12, 2015
    Inventors: Kenneth C. Cundy, Srikonda Sastry, Manshiu Leung, Balaji V. Kadri, Paul E. Stach
  • Publication number: 20140302140
    Abstract: Sustained release oral dosage forms of a gabapentin prodrug, 1-{[(?-isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetic acid, are disclosed. The dosage forms are useful for treating or preventing diseases and disorders for which gabapentin is therapeutically effective.
    Type: Application
    Filed: June 19, 2014
    Publication date: October 9, 2014
    Inventors: Kenneth C. Cundy, Srikonda Sastry, Manshiu Leung, Balaji V. Kadri, Paul E. Stach
  • Publication number: 20140288170
    Abstract: The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.
    Type: Application
    Filed: February 18, 2014
    Publication date: September 25, 2014
    Applicants: The Regents of the University of California, Universita Degli Studi di Parma, Universita Degli Studi di Urbino "Carlo Bo", Fondazione Istituto Italiano di Tecnologia
    Inventors: Daniele Piomelli, Guillermo Moreno-Sanz, Tiziano Bandiera, Marco Mor, Giorgio Tarzia
  • Publication number: 20140275243
    Abstract: The present invention provides a pharmaceutical composition for preventing and/or treating a pediatric epilepsy or epilepsy-related syndrome comprising the phenyl carbamate compound as an active ingredient, and a use of the phenyl carbamate compound for preventing and/or treating pediatric epilepsy or pediatric epilepsy-related syndromes.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: BIO-PHARM SOLUTIONS CO., LTD.
    Inventor: YONG MOON CHOI
  • Publication number: 20140235710
    Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.
    Type: Application
    Filed: March 12, 2014
    Publication date: August 21, 2014
    Applicant: XenoPort, Inc.
    Inventors: Tono Estrada, Stephen P. Raillard, Christine Frauenfelder, Uwe Zacher
  • Patent number: 8680100
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: March 25, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Patent number: 8664247
    Abstract: The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: March 4, 2014
    Assignees: RadioRx, Inc., Alliant Techsystems Inc.
    Inventors: Jan Scicinski, Bryan T. Oronsky, Robert Wardle, Louis Cannizzo, Nicholas A. Straessler
  • Publication number: 20140051753
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 20, 2014
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 8653131
    Abstract: The present invention relates to polymeric derivatives, which can be conjugated to an amino-containing drug to improve its in vivo properties. The polymeric derivative can subsequently be released to yield the drug in its native form. Methods of preparing and using these polymeric derivatives and drug conjugates are described.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: February 18, 2014
    Assignees: Baxter Healthcare S.A., Baxter International Inc.
    Inventors: Guohan Yang, Ton That Hai, Bennett P. Melnick, Paul Sanders, Cong Jiang, Catherine Quinn, Jie Li, Arounaguiry Ambroise, Larry R. Brown
  • Publication number: 20130224151
    Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors alone or in combination for the treatment or prevention of abdominal, visceral or pelvic pain. Also described herein are pharmaceutical compositions comprising a FAAH inhibitor, alone or in combination with an additional therapeutic agent for the treatment of abdominal, visceral or pelvic pain.
    Type: Application
    Filed: March 31, 2011
    Publication date: August 29, 2013
    Applicants: UNITED STATES OF AMERICA, IRONWOOD PHARMACEUTICALS, INC
    Inventors: James Philip Pearson, Mark G. Currie, Yvette Tache, Muriel Larauche
  • Publication number: 20130217764
    Abstract: Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof.
    Type: Application
    Filed: July 22, 2011
    Publication date: August 22, 2013
    Inventors: Daniele Piomelli, Jason R. Clapper, Guillermo Moreno-Sanz, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia, Todd A. Ostomel
  • Publication number: 20130203846
    Abstract: A composition for treating and/or preventing ALS containing the phenyl carbamate compound or a pharmaceutically acceptable salt thereof as an active ingredient; a method of treating and/or preventing ALS comprising administering the phenyl carbamate compound or a pharmaceutically acceptable salt thereof to a patient in need of ALS treatment; and a use of the phenyl carbamate compound or a pharmaceutically acceptable salt thereof in treating and/or preventing ALS, are provided.
    Type: Application
    Filed: December 27, 2012
    Publication date: August 8, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Bio-Pharm Solutions Co., Ltd.
  • Publication number: 20130184338
    Abstract: A phenyl carbamate compound, and a method of treating and/or preventing multiple sclerosis comprising administering a pharmaceutically effective amount of the phenyl carbamate compound to a subject in need of treating and/or preventing multiple sclerosis, are provided.
    Type: Application
    Filed: December 27, 2012
    Publication date: July 18, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Bio-Pharm Solutions Co., Ltd.
  • Publication number: 20130165410
    Abstract: A phenyl carbamate compound; a composition for treating and/or preventing stroke containing the phenyl carbamate compound or a pharmaceutically acceptable salt thereof as an active ingredient; a method of treating and/or preventing stroke comprising administering the phenyl carbamate compound or a pharmaceutically acceptable salt thereof to a patient in need of stroke treatment; and a use of the phenyl carbamate compound or a pharmaceutically acceptable salt thereof in treating and/or preventing stroke, are provided.
    Type: Application
    Filed: December 27, 2012
    Publication date: June 27, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Bio-Pharm Solutions Co., Ltd.
  • Publication number: 20130165509
    Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.
    Type: Application
    Filed: December 27, 2012
    Publication date: June 27, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Bio-Pharm Solutions Co., Ltd.
  • Publication number: 20130137710
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Application
    Filed: May 25, 2010
    Publication date: May 30, 2013
    Applicant: SYMRISE AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130129646
    Abstract: The present invention relates to the cosmetic, dermatological or pharmaceutical (therapeutic) use of compounds of formula (I) or a cosmetically acceptable salt of a compound of formula (I) or a mixture containing two or more of these compounds or the salts thereof wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that a 3 to 8 membered ring is formed, for the lightening of skin and/or hair. The invention further relates to compositions and cosmetic, dermatological or pharmaceutical preparations (compositions) comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.
    Type: Application
    Filed: May 25, 2010
    Publication date: May 23, 2013
    Inventors: Gabriele Vielhaber, Heiko Oertling, Karin Schaper, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130102641
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: December 13, 2012
    Publication date: April 25, 2013
    Applicant: XENOPORT, INC.
    Inventor: XENOPORT, INC.
  • Publication number: 20130053418
    Abstract: The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.
    Type: Application
    Filed: August 24, 2012
    Publication date: February 28, 2013
    Inventors: Jan Scicinski, Bryan T. Oronsky, Robert Wardle, Louis Cannizzo, Nicholas A. Straessler
  • Publication number: 20130046012
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable, stereoisomers, salts or solvates thereof to methods for their synthesis, and use in the treatment of pain.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 21, 2013
    Applicant: LACER, S.A.
    Inventors: Juan Carlos Del Castillo Nieto, Marisabel Mourelle Mancini, Francisco Pubill Coy, José Repollés Moliner
  • Publication number: 20130005801
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Application
    Filed: July 1, 2011
    Publication date: January 3, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Publication number: 20120065206
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 15, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20120053237
    Abstract: The invention relates to (among other things) oligomer-amino acid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated amino acid compounds.
    Type: Application
    Filed: February 24, 2010
    Publication date: March 1, 2012
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Xuyuan Gu, Jennifer Riggs-Sauthier
  • Publication number: 20120041061
    Abstract: Methods of using prodrugs of GABA analogs and pharmaceutical compositions thereof to treat migraine, fibromyalgia, amyotrophic lateral sclerosis, irritable bowel syndrome, social phobia, Parkinson's disease, asthma, cough, or chronic obstructive pulmonary disease, and pharmaceutical compositions of prodrugs of GABA analogs useful in treating migraine, fibromyalgia, amyotrophic lateral sclerosis, irritable bowel syndrome, social phobia, Parkinson's disease, asthma, cough, or chronic obstructive pulmonary disease are disclosed.
    Type: Application
    Filed: October 27, 2011
    Publication date: February 16, 2012
    Inventors: Ronald W. Barrett, Kenneth C. Cundy
  • Publication number: 20120010283
    Abstract: 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 they
    Type: Application
    Filed: August 16, 2011
    Publication date: January 12, 2012
    Applicants: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino
    Inventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
  • Publication number: 20110313036
    Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.
    Type: Application
    Filed: June 20, 2011
    Publication date: December 22, 2011
    Applicant: XenoPort, Inc.
    Inventors: Tono Estrada, Stephen P. Raillard, Christine Frauenfelder, Uwe Zacher
  • Publication number: 20110306600
    Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 15, 2011
    Applicant: Grunenthal GmbH
    Inventor: Ramesh SESHA
  • Publication number: 20110294876
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of compounds of formula (I) given below, in particular as anti-ageing actives. wherein A denotes wherein X, Y and Z independently of one another denote hydrogen, C1-C4-alkyl or C2-C4-alkenyl, wherein optionally two of the radicals X, Y and Z are covalently bonded to one another under formation of a bicyclic ring system, in such a bicyclic ring system two of the radicals X, Y and Z together preferably form a radical having 1 to 4 carbon atoms, preferably a hydrocarbon radical having 1 to 3 carbon atoms, B denotes NR1R2, wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that B is a 3 to 8 membered ring.
    Type: Application
    Filed: May 6, 2011
    Publication date: December 1, 2011
    Applicant: SYMRISE AG
    Inventors: Thomas Küper, Heiko Oertling, Tilman Grune, Matthias Saathoff, Martina Herrmann, Julia Betke, Claudia Gömann, Rahim Brodhage, Imke Meyer
  • Publication number: 20110269709
    Abstract: 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: Application
    Filed: December 23, 2010
    Publication date: November 3, 2011
    Inventor: Apparao Satyam
  • Publication number: 20110263701
    Abstract: The present invention provides a stabilized composition comprising a non-crystalline gabapentin enacarbil and at least one crystallization-inhibiting compound. In particular, the present invention provides a stabilized composition of gabapentin enacarbil, wherein the gabapentin enacarbil is maintained in a non-crystalline form by the composition, for example, as an amorphous form. The invention also provides, among other things, methods of making the stabilized composition, or use of the stabilized composition for making a medicament.
    Type: Application
    Filed: April 20, 2011
    Publication date: October 27, 2011
    Inventors: Sigal BLAU, Ilan ZALIT
  • Publication number: 20110130454
    Abstract: Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed.
    Type: Application
    Filed: November 24, 2010
    Publication date: June 2, 2011
    Applicant: XenoPort, Inc.
    Inventors: Mark A. Gallop, David J. Wustrow
  • Publication number: 20110077231
    Abstract: Novel compounds, with the following being exemplary:
    Type: Application
    Filed: August 12, 2008
    Publication date: March 31, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Walter Rainer
  • Publication number: 20110060040
    Abstract: Methods of using acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof are disclosed.
    Type: Application
    Filed: August 17, 2010
    Publication date: March 10, 2011
    Inventors: Peter A. Virsik, Daniel M. Canafax
  • Publication number: 20110009483
    Abstract: Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.
    Type: Application
    Filed: July 13, 2010
    Publication date: January 13, 2011
    Applicant: XenoPort, Inc.
    Inventors: Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
  • Publication number: 20110003856
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: February 18, 2008
    Publication date: January 6, 2011
    Inventor: Soren Ebdrup
  • Publication number: 20100311794
    Abstract: 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: Application
    Filed: June 7, 2010
    Publication date: December 9, 2010
    Applicant: Gilead Sciences, Inc.
    Inventor: Chandrasekar Venkataramani
  • Patent number: 7799829
    Abstract: Acyloxyalkyl carbamate prodrugs of ?-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of ?-amino acids and methods of using acyloxyalkyl carbamate prodrugs of ?-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of ?-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: September 21, 2010
    Assignee: XenoPort, Inc.
    Inventors: Xuedong Dai, Archana Gangakhedkar, Jia-Ning Xiang, Mark A Gallop
  • Patent number: 7560483
    Abstract: 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: Grant
    Filed: June 21, 2005
    Date of Patent: July 14, 2009
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
  • Publication number: 20090068107
    Abstract: A multidimensional profiling strategy that combines activity-based proteomics and metabolomics was used to determine that an active protein, which is a previously uncharacterized enzyme highly elevated in aggressive cancer cells, serves as a central node in an ether lipid signaling network that bridges platelet-activating factor and the lysophospholipids. Biochemical studies confirmed that the active protein regulates this pathway by hydrolyzing the metabolic intermediate 2-acetyl monoalkylglycerol. Inactivation of the active protein disrupted ether lipid metabolism in cancer cells and impaired cell migration and tumor growth in vivo.
    Type: Application
    Filed: October 2, 2007
    Publication date: March 12, 2009
    Applicant: The Scripps Research Institute
    Inventors: Benjamin F. Cravatt, Kyle P. Chiang, Sherry Niessen, Alan Saghatelian
  • Publication number: 20090048337
    Abstract: Fatty acid amide hydrolase inhibitors of the Formula: I.
    Type: Application
    Filed: July 28, 2006
    Publication date: February 19, 2009
    Applicants: The Regents of the University of California, Universita Degli Studi Du Urbino
    Inventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
  • Publication number: 20090041806
    Abstract: Methods of treating spasticity by administering a colonically absorbable prodrug of a GABA analog having antispastic activity that is not directly mediated by the GABAB receptor, optionally in combination with an antispasticity agent or a colonically absorbable prodrug of a GABAB receptor agonist are disclosed. In particular, methods of treating spasticity by administering a colonically absorbable prodrug of gabapentin or a colonically absorbable prodrug of pregabalin, in combination with a colonically absorbable prodrug of R-baclofen are disclosed.
    Type: Application
    Filed: June 13, 2008
    Publication date: February 12, 2009
    Applicant: XenoPort, Inc.
    Inventor: Kenneth C. CUNDY
  • Publication number: 20090030074
    Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.
    Type: Application
    Filed: August 16, 2007
    Publication date: January 29, 2009
    Applicant: N.V. Organon
    Inventors: David Putman, Olivier Dasse
  • Publication number: 20090018103
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Application
    Filed: October 7, 2005
    Publication date: January 15, 2009
    Applicant: VITAE PHARMACEUTICAL, INC
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillar, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery