Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly To Ring Carbon Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/386)
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Patent number: 10766867Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.Type: GrantFiled: December 6, 2017Date of Patent: September 8, 2020Assignee: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 10441576Abstract: The invention relates to antibacterial compounds of formula I wherein M is one of the groups MA, MB and MC represented below and either R1 represents H and R2 represents a cleavable group as defined in the claims or R2 represents H and R1 represents a cleavable group as defined in the claims; and salts thereof.Type: GrantFiled: August 10, 2016Date of Patent: October 15, 2019Assignee: IDORSIA PHARMACEUTICALS LTD.Inventors: Stefan Diethelm, Philippe Panchaud, Georg Rueedi, Jean-Luc Specklin, Jean-Philippe Surivet
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Patent number: 9326972Abstract: Treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. The use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune and inflammatory diseases associated with TLR3 as well as TLR4 and/or TLR3/TLR4 cellular signaling in association with related pathologies is disclosed. Methods of treating a subject having a disease or condition associated with abnormal TLR-3 as well as TLR-4 and/or TLR3/TLR4 cellular signaling in association with related pathologies are also disclosed. The present disclosure also relates to the treatment of autoimmune-inflammatory pathologies and chemokine and cytokine-mediated diseases associated with TLR overexpression and signaling.Type: GrantFiled: February 9, 2012Date of Patent: May 3, 2016Assignee: Ohio UniversityInventors: Leonard D. Kohn, Norikazu Harii, Uruguaysito Benavides-Peralta, Mariana Gonzalez-Murguiondo, Christopher J. Lewis, Douglas J. Goetz, Giorgio Napolitano, Cesidio Giuliani, Ramiro Malgor, Frank Schwartz, Kelly D. McCall
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Patent number: 9133182Abstract: This invention provides compounds of formula I, pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds and intermediates useful in the preparation of same.Type: GrantFiled: September 27, 2011Date of Patent: September 15, 2015Assignee: Radius Health, Inc.Inventor: Chris P. Miller
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Patent number: 9133228Abstract: Polyamide compositions containing guanidinyl radicals, including tetramethylguanidinyl radicals, are described. These polyamides are useful for medical applications, for example, for treating human papilloma virus infections.Type: GrantFiled: October 10, 2012Date of Patent: September 15, 2015Assignees: NanoVir LLC, THE CURATORS OF THE UNIVERSITY OF MISSOURIInventors: James Bashkin, Terri G. Edwards, Christopher Fisher, George D. Harris, Jr., Kevin J. Koeller
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Patent number: 9089558Abstract: The present invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, which comprises the solid preparation and an environment-controlling agent packaged together. The packaged product of present invention is useful as a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, with which discoloration of the solid preparation is suppressed, and superior storage stability of the solid preparation is obtained.Type: GrantFiled: October 30, 2014Date of Patent: July 28, 2015Assignee: FUJIFILM CorporationInventor: Shumma Nakano
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Publication number: 20150132239Abstract: The present invention relates to a material comprising dendritic molecules each constituted of fragments that are at least bifunctional and of fragments that are of least trifunctional joined together by ester or thioester bridges, alone or in combination with amide or urea bridges, said bridges being formed from two functions carried by different fragments, said molecules containing, on the fragments located at the ends of the dendritic branches, associative end groups capable of forming associations with one another by hydrogen bonds and joined covalently to the functions that are not involved in said bridges. It also relates to the method of production thereof, as well as to its uses and to compositions, notably cosmetic, containing this material.Type: ApplicationFiled: January 8, 2015Publication date: May 14, 2015Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIGIQUE CNRS, ARKEMA FRANCEInventors: François-Genes TOURNILHAC, Manuel HIDALGO, Ludwik LEIBLER
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Patent number: 9012483Abstract: The present invention discloses the use of L-Histidine to reduce Gadolinium accumulation into target organs, preventing its toxic effects, after administration of gadolinium based contrast agents. The invention thus, also disclose the use of L-Histidine to prevent the NSF syndrome in patients with renal functionality impairment. A kit of part is also disclosed by the use of which toxicity associated to free Gd3+, deriving from GDBCA, is prevented by oral administration of L-histidine before administration of the contrast agent. A method for the prevention of toxic metal accumulation which consists in the administration, preferably by the oral route, of L-Histidine is also disclosed. L-Histidine is preferably administered as a single oral dose comprised from 0.2-20 g.Type: GrantFiled: July 24, 2012Date of Patent: April 21, 2015Assignee: Bracco Imaging S.p.A.Inventors: Baranyai Zsolt, Ernö Brücher, Simona Bussi, Alessandro Maiocchi, Fulvio Uggeri
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Publication number: 20150080443Abstract: The present disclosure provides novel formulations suitable for the intravaginal delivery of tinidazole, as well as methods of using the same.Type: ApplicationFiled: June 25, 2014Publication date: March 19, 2015Applicants: UNIVERSITE LAVAL, MISSION PHARMACAL COMPANYInventors: Michel G. BERGERON, Jian GAO, Rabeea F. OMAR, Mary Ann WALTER
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Patent number: 8980894Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the prolongation of time until onset of clinical symptoms in patients having an asymptomatic (occult) heart failure or for the reduction of heart size in patients having symptomatic or asymptomatic (occult) heart failure.Type: GrantFiled: June 11, 2009Date of Patent: March 17, 2015Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Juergen Daemmgen, Olaf Joens, Rainer Kleemann, Christian Troetschel, Andrea Vollmar
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Publication number: 20150056164Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: April 24, 2014Publication date: February 26, 2015Applicant: AbbVie Inc.Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
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Patent number: 8921359Abstract: 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: GrantFiled: April 22, 2013Date of Patent: December 30, 2014Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20140371066Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1 and R2 are as defined in the description, and the active compound groups (2) to (24) listed in the description have very good fungicidal properties.Type: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN, Ralf DUNKEL, Hans-Ludwig ELBE, Heiko RIECK, Anne SUTY-HEINZE
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Publication number: 20140371283Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.Type: ApplicationFiled: February 12, 2014Publication date: December 18, 2014Applicant: Buck Institute for Research on AgingInventors: VARGHESE JOHN, Dale E. BREDESEN
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Patent number: 8883077Abstract: 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: GrantFiled: February 17, 2011Date of Patent: November 11, 2014Assignee: Auburn UniversityInventors: Shelby D. Worley, Xuehong Ren, Hasan B. Kocer
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Publication number: 20140329871Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.Type: ApplicationFiled: December 2, 2012Publication date: November 6, 2014Applicant: ANGION BIOMEDICA CORP.Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
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Publication number: 20140309195Abstract: Provided herein are small molecules for the induction of fibroblast proliferation and increased secretion or production of proteins. The small molecules described herein can be used for the promotion of skin regeneration. Also provided herein are methods for promoting skin regeneration and wound healing.Type: ApplicationFiled: January 8, 2014Publication date: October 16, 2014Applicant: INTERNATIONAL STEM CELL CORPORATIONInventors: Rodolfo Gonzalez, Maxim Poustovoitov, Ruslan Semechkin
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Patent number: 8835477Abstract: Methods for the synthesis of 2-thiohistidine or a derivative thereof of the formula (I), or of a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, from a compound of the formula (II) or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, by cleavage reaction in the presence of a thiol at a temperature higher than or equal to 60° C. The invention also relates to compounds of the formula (II) and a method for the synthesis thereof.Type: GrantFiled: October 6, 2010Date of Patent: September 16, 2014Assignee: TetrahedronInventors: Irène Erdelmeier, Sylvain Daunay
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Patent number: 8815923Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: August 26, 2014Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
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Patent number: 8802666Abstract: 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: GrantFiled: December 21, 2010Date of Patent: August 12, 2014Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20140128361Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables 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 pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: ApplicationFiled: January 6, 2014Publication date: May 8, 2014Applicants: Pharmacopeia Drug Discovery, Inc., Merck Sharp & Dohme Corp.Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey H. Lowrie, Kurt W. Salonz, Suresh D. Babu
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Publication number: 20140050680Abstract: The methods described herein provide treatment of rosacea using topical formulations of dapsone. The methods also provide treatment of rosacea with topical dapsone in combination with other active agents, including metronidazole. The methods avoid negative hematologic side effects, including hemolysis and hemolytic anemia, that are associated with oral administration of dapsone.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicant: Allergan, Inc.Inventor: John S. Garrett
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Publication number: 20140030254Abstract: The present invention relates to the identification and diagnostic use of biomarkers in primary colorectal cancer tumors whose activation level are predictive of the likelihood of the onset of metastatic disease. These biomarkers may be used to determine the suitability of a patient for aggressive and/or targeted treatments. Kits and compositions of the invention are also provided.Type: ApplicationFiled: March 27, 2013Publication date: January 30, 2014Inventors: Emanuel F. Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Alessandra Silvestri
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Patent number: 8637560Abstract: The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination.Type: GrantFiled: July 18, 2008Date of Patent: January 28, 2014Assignee: The United States of America as Represented by the Secretary of the Department of Health and Human ServicesInventors: William Trenkle, Adrian Wiestner, Qiuyan Wang, Yihong Ye, Helena Mora-Jensen
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Patent number: 8633231Abstract: The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: July 8, 2011Date of Patent: January 21, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Duane DeMong, Michael W. Miller, Xing Dai, Andrew Stamford
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Publication number: 20130345246Abstract: 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. methods of therapy, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 13, 2013Publication date: December 26, 2013Applicant: ASTRAZENECA ABInventors: Sofia Karlstrom, Gabor Csjernyik, Britt-Marie Swahn, Lars Sandberg, Karin Kolmodin, Peter Soderman, Liselotte Ohberg
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Publication number: 20130345247Abstract: Cyclohexane-1,2?-indene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 13, 2013Publication date: December 26, 2013Applicant: ASTRAZENECA ABInventors: Sofia Karlstrom, Peter Soderman, Laszlo Rakos, Liselotte Ohberg, Karin Kolmodin, Lars Sandberg
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Publication number: 20130345272Abstract: Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 13, 2013Publication date: December 26, 2013Applicant: AstraZeneca ABInventors: Sofia Karlstrom, Peter Soderman, Britt-Marie Swahn, Laszlo Rakos, Liselotte Ohberg
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Publication number: 20130345248Abstract: Cyclohexane-1,2?-naphthalene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 13, 2013Publication date: December 26, 2013Applicant: AstraZeneca ABInventors: Sofia Karlstrom, Lars Sandberg, Peter Soderman, Karin Kolmodin, Liselotte Ohberg
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Publication number: 20130331328Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
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Publication number: 20130317014Abstract: 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: ApplicationFiled: April 22, 2013Publication date: November 28, 2013Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Patent number: 8569336Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: October 29, 2013Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K. C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Patent number: 8563588Abstract: Imidazolone derivatives, as medicaments, of formula wherein: R1?H, C1 to C5 alkyl, aryl or a 5- or 6-membered heterocyclic group; Ar1=optionally substituted aryl or an aromatic heterocycle; R?R2—S—, R3—HN—, R4COHN or Ar2, with R2=a C1-C5 alkyl, vinyl or vinyl(C1-C5)alkyl, nitrile or nitrile(C1-C5)alkyl, aryl or benzyl radical, which are optionally substituted; R3=the meanings given above and H; Ar2=substituted or unsubstituted aryl.Type: GrantFiled: August 1, 2008Date of Patent: October 22, 2013Assignees: Universite de Rennes 1, Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Francois Carreaux, Jean-Pierre Bazureau, Steven Renault, Laurent Meijer, Olivier Lozach
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Publication number: 20130274101Abstract: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R1 and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Ulrike WACHENDORFF-NEUMANN, Peter Dahmen, Ralf Dunkel
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Patent number: 8546438Abstract: 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: GrantFiled: June 16, 2011Date of Patent: October 1, 2013Inventors: Kai Thede, Susanne Greschat, Steffen Wildum, Daniela Paulsen
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Patent number: 8486858Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: September 14, 2010Date of Patent: July 16, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8450308Abstract: 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: GrantFiled: August 14, 2009Date of Patent: May 28, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Patent number: 8445523Abstract: SOAT-1 inhibitors of general formula (I) and cosmetic and pharmaceutical compositions containing such a compound are described.Type: GrantFiled: February 26, 2010Date of Patent: May 21, 2013Assignee: Galderma Research & DevelopmentInventors: Laurence Dumais, Cédric Poinsard, Thibaud Portal
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Publication number: 20130123315Abstract: The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: July 8, 2011Publication date: May 16, 2013Inventors: Duane DeMong, Michael W. Miller, Xing Dai, Andrew Stamford
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Publication number: 20130122102Abstract: A delivery system for administration to a patient of Fenobam, its hydrates, and salts optimizes solubility and dissolution properties of Fenobam, its hydrates, and salts using either microemulsions, solid dispersions, cyclodextrin, gastroretentives, enteric coatings, and sustained delivery techniques to provide a vehicle for oral administration of these drugs.Type: ApplicationFiled: November 2, 2012Publication date: May 16, 2013Applicant: MURTY PHARMACEUTICALS, INC.Inventors: Santos B. Murty, Ram B. Murty
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Patent number: 8426454Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: GrantFiled: August 14, 2008Date of Patent: April 23, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
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Patent number: 8420682Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions including such a compound are described.Type: GrantFiled: February 26, 2010Date of Patent: April 16, 2013Assignee: Galderma Research & DevelopmentInventors: Cédric Poinsard, Thibaud Portal
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Patent number: 8420680Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.Type: GrantFiled: June 30, 2008Date of Patent: April 16, 2013Assignees: Emory University, NeurOp, Inc.Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Yesim Altas Tahirovic, Scott J. Myers
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Patent number: 8420684Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(heType: GrantFiled: November 8, 2007Date of Patent: April 16, 2013Assignee: Probiodrug AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Patent number: 8420681Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions containing such a compound are described.Type: GrantFiled: February 26, 2010Date of Patent: April 16, 2013Assignee: Galderma Research & DevelopmentInventor: Cédric Poinsard
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Publication number: 20130090362Abstract: Polyamide compositions containing guanidinyl radicals, including tetramethylguanidinyl radicals, are described. These polyamides are useful for medical applications, for example, for treating human papilloma virus infections.Type: ApplicationFiled: October 10, 2012Publication date: April 11, 2013Applicant: NANOVIR, LLCInventor: NANOVIR, LLC
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Patent number: 8399500Abstract: The present disclosure relates to a method for synthesizing ergothioneine or one of the derivatives thereof of following formula (I): or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in all proportions thereof, from a compound of betaine type of following formula (II): or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in all proportions thereof, by cleavage reaction in the presence of a thiol, at a temperature above or equal to 60° C. The present disclosure also relates to compounds of formula (II) and the method of synthesis thereof.Type: GrantFiled: October 6, 2010Date of Patent: March 19, 2013Assignee: TetrahedronInventor: Irene Erdelmeier
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Patent number: 8399499Abstract: The present invention provides 3- to 7-membered 1,3-diaza-4-oxo-heterocyclic derivatives, such as imidazolidinone O derivatives, capable of releasing in a controlled manner a biologically active aldehyde or ketone in the surrounding. The invention also relates to the use of these compounds as perfuming or flavoring ingredients, as well as to the perfuming compositions and consumer articles containing such derivatives. It also provides a process for preparing said derivatives of the invention.Type: GrantFiled: April 30, 2008Date of Patent: March 19, 2013Assignee: Firmenich SAInventors: Andreas Herrmann, Guillaume Godin
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Patent number: 8399682Abstract: 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: GrantFiled: September 17, 2010Date of Patent: March 19, 2013Assignee: AiCuris GmbH & Co. KGInventors: Kai Thede, Susanne Greschat, Steffen Wildum, Daniela Paulsen
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Publication number: 20130040963Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences, Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, David A. PAISNER