Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Type:
Grant
Filed:
August 23, 2010
Date of Patent:
February 5, 2013
Assignee:
Merck, Sharp & Dohme, Corp.
Inventors:
Ying Huang, Guoqing Li, Andrew W. Stamford
Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
Type:
Grant
Filed:
April 12, 2006
Date of Patent:
January 22, 2013
Assignee:
Vicore Pharma AB
Inventors:
Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah
Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
Type:
Application
Filed:
December 21, 2010
Publication date:
January 17, 2013
Inventors:
Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
Abstract: Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.
Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
Type:
Application
Filed:
March 22, 2011
Publication date:
January 10, 2013
Inventors:
Michael K. Wong, Brian J. Lavey, Wensheng Yu, Joseph A. Kozlowski, Duanc E. DeMong, Xing Dai, Andrew W. Stamford, Michael W. Miller, Guowei Zhou, De-Yi Yang, William J. Greenlee
Abstract: The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.
Type:
Application
Filed:
December 26, 2011
Publication date:
January 3, 2013
Applicant:
BAYER PHARMA AKTIENGESELLSHAFT
Inventors:
Heinrich Meier, Eckhard Bender, Ulf Brüggemeier, Ingo Flamme, Dagmar Karthaus, Peter Kolkhof, Daniel Meibom, Dirk Schneider, Verena Voehringer, Chantal Fürstner, Jörg Keldenich, Dieter Lang, Elisabeth Pook, Carsten Schmeck
Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.
Type:
Application
Filed:
August 23, 2012
Publication date:
January 3, 2013
Applicant:
Medicis Pharmaceutical Corporation
Inventors:
Michael T. NORDSIEK, Kodumudi S. Balaji
Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
Type:
Grant
Filed:
December 29, 2010
Date of Patent:
December 18, 2012
Assignee:
PTC Therapeutics, Inc.
Inventors:
Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
Abstract: A sensitive, multicomponent diagnostic test for infection with T. cruzi, the causative agent of Chagas disease, including methods of making and methods of use. Also provided is a method for screening T. cruzi polypeptides to identify antigenic polypeptides for inclusion as components of the diagnostic test, as well as compositions containing antigenic T. cruzi polypeptides.
Type:
Application
Filed:
August 9, 2012
Publication date:
December 13, 2012
Applicant:
University of Georgia Research Foundation, Inc.
Inventors:
Rick L. Tarleton, Ronald D. Etheridge, JR.
Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.
Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
Type:
Grant
Filed:
December 21, 2007
Date of Patent:
October 16, 2012
Assignee:
Bayer CropScience AG
Inventors:
Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
Abstract: Disclosed is a method for producing precursors for 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof, to the precursor, and to a method for producing 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof from particular precursor. A compound of formula (3) is provided which enables an automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine. The enantiomeric purity of the product is ?98%.
Type:
Grant
Filed:
November 21, 2008
Date of Patent:
September 25, 2012
Assignee:
Forschungszentrum Juelich GmbH
Inventors:
Franziska Wagner, Johannes Ermert, Heinrich Hubert Coenen
Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Type:
Grant
Filed:
November 19, 2010
Date of Patent:
August 14, 2012
Assignee:
Novartis AG
Inventors:
Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.
Type:
Application
Filed:
September 15, 2010
Publication date:
July 12, 2012
Applicant:
SHIRE LLC
Inventors:
Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
Abstract: The present invention relates to substituted cyclic urea derivatives corresponding to formula I, to processes for the preparation thereof, to medicinal drugs containing such compounds, to the use of such compounds in the preparation of medicinal drugs and in related treatment methods.
Type:
Grant
Filed:
October 19, 2007
Date of Patent:
June 26, 2012
Assignee:
Gruenenthal GmbH
Inventors:
Robert Frank, Bernd Sundermann, Hans Schick, Helmut Sonnenschein
Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Type:
Grant
Filed:
December 10, 2004
Date of Patent:
June 5, 2012
Assignee:
Abbott Laboratories
Inventors:
Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
Type:
Grant
Filed:
June 17, 2009
Date of Patent:
May 29, 2012
Assignee:
Sanofi-Aventis
Inventors:
Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
Abstract: The present application describes compounds of Formula I and Formula IA and as disclosed herein, that are useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.
Type:
Application
Filed:
October 18, 2011
Publication date:
May 24, 2012
Inventors:
Rakesh K. Jain, Timothy Shiau, Charles Francavilla, Eddy Low, Eric Douglas Turtle, Donogh John Roger O'Mahony
Abstract: There is provided a novel LXR? agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.
Abstract: A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.
Type:
Grant
Filed:
January 31, 2008
Date of Patent:
April 17, 2012
Assignee:
Bial-Portela & C.A., S.A.
Inventors:
Patrício Manuel Vieira Araújo Soares Da Silva, Alexander Beliaev, David Alexander Learmonth
Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
Type:
Application
Filed:
March 25, 2010
Publication date:
April 5, 2012
Applicant:
ABBOTT LABORATORIES
Inventors:
David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
Type:
Application
Filed:
November 22, 2011
Publication date:
March 22, 2012
Applicant:
Bayer CropScience AG
Inventors:
Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
Type:
Grant
Filed:
October 12, 2007
Date of Patent:
March 6, 2012
Assignee:
Hoffman-La Roche Inc.
Inventors:
Jean Ackermann, Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart, Tadakatsu Takahashi
Abstract: Novel 4-phenylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.
Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
Type:
Application
Filed:
June 16, 2011
Publication date:
January 26, 2012
Applicant:
AiCuris GmbH & Co. KG
Inventors:
Kai THEDE, Susanne Greschat, Steffen Wildum, Daniela Paulsen
Abstract: The present invention relates to novel substituted (thiophenyl-carbonyl)imidazolidinones, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
Type:
Application
Filed:
June 16, 2011
Publication date:
January 26, 2012
Applicant:
AiCuris GmbH & Co. KG
Inventors:
Kai THEDE, Susanne GRESCHAT, Steffen WILDUM, Daniela PAULSEN
Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
Type:
Application
Filed:
September 23, 2011
Publication date:
January 19, 2012
Applicant:
Bayer CropScience AG
Inventors:
Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
Type:
Grant
Filed:
February 16, 2008
Date of Patent:
December 6, 2011
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Todd Heidelbaugh, Daniel Gil, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
Type:
Grant
Filed:
October 17, 2007
Date of Patent:
November 22, 2011
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Todd M. Heidelbaugh, Daniel W. Gil, Michael E. Garst, Larry A. Wheeler
Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
Type:
Grant
Filed:
July 25, 2008
Date of Patent:
November 22, 2011
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Todd Heidelbaugh, Daniel Gill, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
Abstract: The present invention relates to novel active substance combinations which contain spiroxamine, which is known, a known azole and a known carboxamide and which are very suitable for controlling undesired phytopathogenic fungi.
Type:
Grant
Filed:
September 3, 2005
Date of Patent:
October 18, 2011
Assignee:
Bayer CropScience AG
Inventors:
Peter Dahmen, Ulrike Wachendorff-Neumann, Ralf Dunkel
Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
Type:
Application
Filed:
August 14, 2009
Publication date:
September 8, 2011
Applicant:
VITAE PHARMACEUTICALS, INC.
Inventors:
Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
Type:
Application
Filed:
October 2, 2009
Publication date:
September 1, 2011
Inventors:
Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
Abstract: The present invention is directed to imidazolidinone compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Grant
Filed:
November 10, 2006
Date of Patent:
August 23, 2011
Assignee:
Merck. Sharp & Dohme Corp.
Inventors:
James C. Barrow, Kenneth E. Rittle, Phung Le Bondiskey
Abstract: A disinfecting, nonbleaching N-halamine for use in contact lens soaking solutions. The N-halamine compound is soluble in water and contact lens formulation solutions to the extent necessary to provide disinfection, but not to cause significant bleaching of dye materials incorporated into the contact lenses.
Type:
Application
Filed:
February 17, 2011
Publication date:
August 18, 2011
Applicant:
Auburn University
Inventors:
Shelby D. Worley, Xuehong Ren, Hasan B. Kocer
Abstract: Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.
Type:
Grant
Filed:
December 4, 2009
Date of Patent:
August 2, 2011
Assignee:
Galderma Research & Development
Inventors:
Jean Guy Boiteau, Corinne Millois Barbuis, Karine Bouquet
Abstract: The use of a compound of formula (I), is disclosed in treating and/or preventing 5 chemotherapy-induced peripheral neurotoxicity (CIPN). The invention includes pharmaceutical compositions wherein the compound of formula (I) is present in a mixture with anticancer agents. An improved anticancer treatment with reduced CIPN-related side effects is also provided.
Type:
Grant
Filed:
November 14, 2007
Date of Patent:
July 5, 2011
Assignee:
Neurotune AG
Inventors:
Carlo Farina, Carla Ghelardini, Paola Petrillo
Abstract: The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
Type:
Grant
Filed:
October 17, 2007
Date of Patent:
June 14, 2011
Assignee:
Allergan, Inc
Inventors:
Ken Chow, Todd M. Heidelbaugh, Daniel W. Gil, Michael E. Garst, Larry A. Wheeler
Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Application
Filed:
November 30, 2010
Publication date:
June 9, 2011
Inventors:
David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
Abstract: The present invention relates to novel substituted (pyrazolylcarbonyl)imidazolidinones, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.
Type:
Application
Filed:
September 17, 2010
Publication date:
May 26, 2011
Applicant:
AiCuris GmbH & Co. KG
Inventors:
Kai THEDE, Susanne GRESCHAT, Steffen WILDUM, Daniela PAULSEN
Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.
Abstract: The invention relates to novel derivatives of short-chain fatty acids, in particular derivatives of butyric acid, useful for all the known clinical applications of the latter, which show physicochemical characteristics suitable for an easy oral administration, being devoid of the unpleasant organoleptic properties that characterize butyrate. The new compounds are amide derivatives which can be synthesized by reaction of the corresponding fatty acid halide with a naturally occurring amino acid, phenylalanine or a suitable derivative thereof, and which are in a poorly hygroscopic, easily weighable form, stable to acids and alkalis and able to release the acid at the small and large bowel level in a constant manner over time. They do not have disagreeable odors and are practically tasteless, thus allowing the manufacture of preparations for oral administration also suitable for the therapy of chronic diseases and in the pediatric field.
Type:
Application
Filed:
April 21, 2009
Publication date:
April 28, 2011
Inventors:
Roberto Berni Canani, Antonio Calignano, Orietta Mazzoni, Anna Coruzzo
Abstract: Methods of ameliorating episodes of accute or chronic colitis are provided by using methimazole derivatives and tautomeric cyclic thiones in combination with another pharmaceutical compound.
Type:
Grant
Filed:
August 6, 2004
Date of Patent:
April 19, 2011
Assignee:
Ohio University
Inventors:
Leonard D. Kohn, Douglas J. Goetz, Uruguaysito Benavides-Peralta, Mariana Gonzalez-Murguiondo, Norikazu Harii, Christopher J. Lewis, Giorgio Napolitano, Nilesh D. Dagia
Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Type:
Application
Filed:
November 19, 2010
Publication date:
March 24, 2011
Inventors:
Olga M. FRYSZMAN, Hengyuan LANG, Jiong LAN, Edcon CHANG, Yunfeng FANG
Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
Type:
Application
Filed:
March 12, 2010
Publication date:
March 24, 2011
Inventors:
Salvacion CACATIAN, David A. CLAREMON, Lawrence W. DILLARD, Klaus FUCHS, Niklas HEINE, Lanqi JIA, Katerina LEFTHERIS, Brian McKEEVER, Angel MORALES-RAMOS, Suresh B. SINGH, Shankar VENKATRAMAN, Guosheng WU, Zhongren WU, Zhenrong XU, Jing YUAN, Yajun ZHENG
Abstract: A composition comprising at least one physiologically tolerated film-forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.
Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
Type:
Grant
Filed:
June 17, 2008
Date of Patent:
March 8, 2011
Assignee:
PTC Therapeutics, Inc.
Inventors:
Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Type:
Application
Filed:
August 23, 2010
Publication date:
January 6, 2011
Applicant:
Schering Corporation
Inventors:
Ying Huang, Guoqing Li, Andrew W. Stamford
Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
Type:
Grant
Filed:
July 2, 2008
Date of Patent:
November 23, 2010
Assignee:
Allergan, Inc.
Inventors:
Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gill, John E. Donello, Michael E. Garst, Larry A. Wheeler