Ring In Acid Moiety Patents (Class 514/484)
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Patent number: 11776800Abstract: 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: GrantFiled: June 20, 2019Date of Patent: October 3, 2023Assignee: Hitachi High-Tech CorporationInventors: Yasuaki Takada, Shun Kumano, Masuyuki Sugiyama, Tsukasa Shishika, Shinji Yoshioka, Akimasa Osaka
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Patent number: 9872847Abstract: 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: GrantFiled: March 11, 2014Date of Patent: January 23, 2018Assignee: Bio-Pharm Solutions Co., Ltd.Inventor: Yong Moon Choi
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Patent number: 9745255Abstract: 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: GrantFiled: February 18, 2014Date of Patent: August 29, 2017Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Technologia, Universita Degli Studi di Urbino “Carlo Bo”, Universita Degli Studi di ParmaInventors: Daniele Piomelli, Guillermo Moreno-Sanz, Tiziano Bandiera, Marco Mor, Giorgio Tarzia
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Publication number: 20150133541Abstract: 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: ApplicationFiled: January 13, 2015Publication date: May 14, 2015Inventor: Yong Moon Choi
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Patent number: 9029589Abstract: 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: GrantFiled: December 27, 2012Date of Patent: May 12, 2015Assignee: Bio-Pharm Solutions Co., Ltd.Inventor: Yong Moon Choi
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Patent number: 9018253Abstract: 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: GrantFiled: July 1, 2011Date of Patent: April 28, 2015Assignee: Bio-Pharm Solutions Co., Ltd.Inventor: Yong Moon Choi
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Patent number: 9012497Abstract: 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: GrantFiled: May 25, 2010Date of Patent: April 21, 2015Assignee: Symrise AGInventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
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Publication number: 20150072004Abstract: 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: ApplicationFiled: November 4, 2014Publication date: March 12, 2015Inventors: Kenneth C. Cundy, Srikonda Sastry, Manshiu Leung, Balaji V. Kadri, Paul E. Stach
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Publication number: 20140302140Abstract: 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: ApplicationFiled: June 19, 2014Publication date: October 9, 2014Inventors: Kenneth C. Cundy, Srikonda Sastry, Manshiu Leung, Balaji V. Kadri, Paul E. Stach
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Publication number: 20140288170Abstract: 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: ApplicationFiled: February 18, 2014Publication date: September 25, 2014Applicants: The Regents of the University of California, Universita Degli Studi di Parma, Universita Degli Studi di Urbino "Carlo Bo", Fondazione Istituto Italiano di TecnologiaInventors: Daniele Piomelli, Guillermo Moreno-Sanz, Tiziano Bandiera, Marco Mor, Giorgio Tarzia
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Publication number: 20140275243Abstract: 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: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: BIO-PHARM SOLUTIONS CO., LTD.Inventor: YONG MOON CHOI
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Publication number: 20140235710Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.Type: ApplicationFiled: March 12, 2014Publication date: August 21, 2014Applicant: XenoPort, Inc.Inventors: Tono Estrada, Stephen P. Raillard, Christine Frauenfelder, Uwe Zacher
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Patent number: 8680100Abstract: 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: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Patent number: 8664247Abstract: 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: GrantFiled: August 24, 2012Date of Patent: March 4, 2014Assignees: RadioRx, Inc., Alliant Techsystems Inc.Inventors: Jan Scicinski, Bryan T. Oronsky, Robert Wardle, Louis Cannizzo, Nicholas A. Straessler
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Publication number: 20140051753Abstract: 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: ApplicationFiled: July 1, 2011Publication date: February 20, 2014Applicant: Bio-Pharm Solutions Co., Ltd.Inventor: Yong Moon Choi
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Patent number: 8653131Abstract: 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: GrantFiled: August 21, 2009Date of Patent: February 18, 2014Assignees: 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
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Publication number: 20130224151Abstract: 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: ApplicationFiled: March 31, 2011Publication date: August 29, 2013Applicants: UNITED STATES OF AMERICA, IRONWOOD PHARMACEUTICALS, INCInventors: James Philip Pearson, Mark G. Currie, Yvette Tache, Muriel Larauche
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Publication number: 20130217764Abstract: 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: ApplicationFiled: July 22, 2011Publication date: August 22, 2013Inventors: Daniele Piomelli, Jason R. Clapper, Guillermo Moreno-Sanz, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia, Todd A. Ostomel
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Publication number: 20130203846Abstract: 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: ApplicationFiled: December 27, 2012Publication date: August 8, 2013Applicant: Bio-Pharm Solutions Co., Ltd.Inventor: Bio-Pharm Solutions Co., Ltd.
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Publication number: 20130184338Abstract: 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: ApplicationFiled: December 27, 2012Publication date: July 18, 2013Applicant: Bio-Pharm Solutions Co., Ltd.Inventor: Bio-Pharm Solutions Co., Ltd.
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Publication number: 20130165410Abstract: 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: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: Bio-Pharm Solutions Co., Ltd.Inventor: Bio-Pharm Solutions Co., Ltd.
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Publication number: 20130165509Abstract: 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: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: Bio-Pharm Solutions Co., Ltd.Inventor: Bio-Pharm Solutions Co., Ltd.
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Publication number: 20130137710Abstract: 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: ApplicationFiled: May 25, 2010Publication date: May 30, 2013Applicant: SYMRISE AGInventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
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Publication number: 20130129646Abstract: 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: ApplicationFiled: May 25, 2010Publication date: May 23, 2013Inventors: Gabriele Vielhaber, Heiko Oertling, Karin Schaper, Claudia Gömann, Rahim Brodhage
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Publication number: 20130102641Abstract: 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: ApplicationFiled: December 13, 2012Publication date: April 25, 2013Applicant: XENOPORT, INC.Inventor: XENOPORT, INC.
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Publication number: 20130053418Abstract: 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: ApplicationFiled: August 24, 2012Publication date: February 28, 2013Inventors: Jan Scicinski, Bryan T. Oronsky, Robert Wardle, Louis Cannizzo, Nicholas A. Straessler
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Publication number: 20130046012Abstract: 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: ApplicationFiled: April 27, 2011Publication date: February 21, 2013Applicant: LACER, S.A.Inventors: Juan Carlos Del Castillo Nieto, Marisabel Mourelle Mancini, Francisco Pubill Coy, José Repollés Moliner
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Publication number: 20130005801Abstract: 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: ApplicationFiled: July 1, 2011Publication date: January 3, 2013Applicant: Bio-Pharm Solutions Co., Ltd.Inventor: Yong Moon Choi
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Publication number: 20120065206Abstract: 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: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120053237Abstract: 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: ApplicationFiled: February 24, 2010Publication date: March 1, 2012Applicant: NEKTAR THERAPEUTICSInventors: Xuyuan Gu, Jennifer Riggs-Sauthier
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Publication number: 20120041061Abstract: 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: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: Ronald W. Barrett, Kenneth C. Cundy
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Publication number: 20120010283Abstract: 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: ApplicationFiled: August 16, 2011Publication date: January 12, 2012Applicants: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Publication number: 20110313036Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.Type: ApplicationFiled: June 20, 2011Publication date: December 22, 2011Applicant: XenoPort, Inc.Inventors: Tono Estrada, Stephen P. Raillard, Christine Frauenfelder, Uwe Zacher
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Publication number: 20110306600Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.Type: ApplicationFiled: June 10, 2011Publication date: December 15, 2011Applicant: Grunenthal GmbHInventor: Ramesh SESHA
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Publication number: 20110294876Abstract: 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: ApplicationFiled: May 6, 2011Publication date: December 1, 2011Applicant: SYMRISE AGInventors: Thomas Küper, Heiko Oertling, Tilman Grune, Matthias Saathoff, Martina Herrmann, Julia Betke, Claudia Gömann, Rahim Brodhage, Imke Meyer
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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: 20110263701Abstract: 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: ApplicationFiled: April 20, 2011Publication date: October 27, 2011Inventors: Sigal BLAU, Ilan ZALIT
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Publication number: 20110130454Abstract: 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: ApplicationFiled: November 24, 2010Publication date: June 2, 2011Applicant: XenoPort, Inc.Inventors: Mark A. Gallop, David J. Wustrow
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Publication number: 20110077231Abstract: Novel compounds, with the following being exemplary:Type: ApplicationFiled: August 12, 2008Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Walter Rainer
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Publication number: 20110060040Abstract: Methods of using acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof are disclosed.Type: ApplicationFiled: August 17, 2010Publication date: March 10, 2011Inventors: Peter A. Virsik, Daniel M. Canafax
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Publication number: 20110009483Abstract: 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: ApplicationFiled: July 13, 2010Publication date: January 13, 2011Applicant: XenoPort, Inc.Inventors: Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
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Publication number: 20110003856Abstract: 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: ApplicationFiled: February 18, 2008Publication date: January 6, 2011Inventor: Soren Ebdrup
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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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Patent number: 7799829Abstract: 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: GrantFiled: April 1, 2009Date of Patent: September 21, 2010Assignee: XenoPort, Inc.Inventors: Xuedong Dai, Archana Gangakhedkar, Jia-Ning Xiang, Mark A Gallop
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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: 20090068107Abstract: 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: ApplicationFiled: October 2, 2007Publication date: March 12, 2009Applicant: The Scripps Research InstituteInventors: Benjamin F. Cravatt, Kyle P. Chiang, Sherry Niessen, Alan Saghatelian
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Publication number: 20090048337Abstract: Fatty acid amide hydrolase inhibitors of the Formula: I.Type: ApplicationFiled: July 28, 2006Publication date: February 19, 2009Applicants: The Regents of the University of California, Universita Degli Studi Du UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Publication number: 20090041806Abstract: 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: ApplicationFiled: June 13, 2008Publication date: February 12, 2009Applicant: XenoPort, Inc.Inventor: Kenneth C. CUNDY
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Publication number: 20090030074Abstract: 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: ApplicationFiled: August 16, 2007Publication date: January 29, 2009Applicant: N.V. OrganonInventors: David Putman, Olivier Dasse
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Publication number: 20090018103Abstract: 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: ApplicationFiled: October 7, 2005Publication date: January 15, 2009Applicant: VITAE PHARMACEUTICAL, INCInventors: 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