Plural Acyclic Chalcogens Bonded Directly At The 2- And At The 4- Or 5- Positions Of The 1,3-diazole Ring [e.g., N-(5-nitro-2-furfuryliden)-1- Amino-hydantoin, Etc.] Patents (Class 548/316.1)
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Patent number: 9035052Abstract: The present invention is directed to solvates and various polymorphic forms of (E)-1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione dihydrochloride and pharmaceutical compositions thereof.Type: GrantFiled: March 15, 2013Date of Patent: May 19, 2015Assignee: Warner Chilcott Company, LLCInventors: Nancy Lee Redman-Furey, Nicholas William Geary, Tammy Baker
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Publication number: 20140336120Abstract: A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition can include a compound which is a combination of dantrolene and a residue of FMOC-valine. This composition can be used to provide a faster and higher CNS penetration than heretofore experienced with dantrolene. In another form, dantrolene may be formulated as a pro-drug, a pro-pro-drug and the like.Type: ApplicationFiled: May 8, 2014Publication date: November 13, 2014Applicant: Howard UniversityInventors: Harpal S. Mangat, Pradeep K. Karla
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Publication number: 20140275112Abstract: Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Rosalind Franklin University of Medicine and ScienceInventors: Grace E. Stutzmann, Russell Dahl
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Patent number: 8759384Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.Type: GrantFiled: May 11, 2009Date of Patent: June 24, 2014Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
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Patent number: 8536213Abstract: The invention relates to (among other things) oligomer-dantrolene conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: GrantFiled: November 14, 2008Date of Patent: September 17, 2013Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
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Patent number: 8476449Abstract: The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.Type: GrantFiled: February 24, 2011Date of Patent: July 2, 2013Assignees: Nihon Medi-Physics Co., Ltd., Kyoto UniversityInventors: Hideo Saji, Masahiro Ono, Ikuya Seki
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Publication number: 20130123215Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Publication number: 20130028966Abstract: The invention provides compounds represented by the formulae: (I) and (II) where the compounds are useful in treating, for example, viral and/or parasitic infections. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds.Type: ApplicationFiled: April 13, 2011Publication date: January 31, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Benhur Lee, Michael E. Jung, Jihye Lee, Frederic Vigant, Peter J. Bradley, Michael C. Wolf, Bettina E. Hajagos
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Publication number: 20120330024Abstract: The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.Type: ApplicationFiled: February 24, 2011Publication date: December 27, 2012Applicants: Kyoto University, Nihon Medi-Physics Co., Ltd.Inventors: Hideo Saji, Masahiro Ono, Ikuya Seki
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Publication number: 20110046185Abstract: The invention relates to compounds of formula (I) wherein the groups R and R? A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: February 24, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Peter BELOW, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Publication number: 20100317705Abstract: The invention relates to (among other things) oligomer-dantrolene conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: ApplicationFiled: November 14, 2008Publication date: December 16, 2010Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
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Publication number: 20100144723Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancerType: ApplicationFiled: December 1, 2009Publication date: June 10, 2010Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
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Publication number: 20100105719Abstract: The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.Type: ApplicationFiled: October 2, 2009Publication date: April 29, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Norbert TENNAGELS
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Publication number: 20090093531Abstract: The present invention provides for methods of using tert-butyl alcohol (TBA) co-solvent systems in the formulation and production of a pharmaceutical agent with low solubility. The present invention also provides for pharmaceutical compositions made using the novel co-solvent system. In one embodiment, the invention provides for a method of making dantrolene sodium (DS) formulation for intravenous use (DS-IV). This instantaneous reconstitution of the DS-IV product constitutes a significant improvement in the pharmacotherapy of patients undergoing malignant hyperthermia during surgery.Type: ApplicationFiled: September 5, 2008Publication date: April 9, 2009Inventor: Ahmad Malkawi
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Patent number: 6809101Abstract: It is found out that compounds represented by the formula (I): wherein R1 is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; and R2 and R3 taken together with the adjacent carbon atom form an optionally substituted heterocyclic group having one or more of oxo and/or thioxo; have an HCV RNA-dependent RNA synthase inhibitory effect.Type: GrantFiled: February 27, 2003Date of Patent: October 26, 2004Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Kenji Abe
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Patent number: 6420568Abstract: A process for making 1,3-disubstituted-4-oxocyclic ureas of general formula (I): wherein R1, R2, and R3 are independently selected from the group consisting of nil, Cl, F, Br, NH2, NO2, COOH, CH3SO2NH, SO3H, OH, alkoxy, alkyl, alkoxycarbon hydroxyalkyl, carboxyalkyl, and acyloxy; R4 is selected from the group consisting of a substituted or unsubstituted alkyl, alkenyl alkynyl, alkylacyl, and heteroalkyl; and A is a substituted or unsubstituted, saturated or unsaturated, straight-chain or branched alkyl or alkenyl amino group comprised of 1-7 carbon atoms; or A is a substituted or unsubstituted, saturated or unsaturated heterocycle having 5, 6, or 7 members containing at least one nitrogen, and R4 is attached to this nitrogen; wherein said 1,3-disubstituted tuted-4-oxocyclic urea is made without isolation of intermediates and comprising the steps: (Ia) reacting a l-substituted-4-oxocyclic urea with a carbon chain containing at least two leaving groups in the presence of a mild base and a solvType: GrantFiled: October 27, 2000Date of Patent: July 16, 2002Assignee: The Procter & Gamble CompanyInventors: Patricia Ann Matson, Michael Selden Godlewski
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Patent number: 6414151Abstract: A process for making 1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperizinyl)butyl]-2,4-imidazolidinedione having the formula: is disclosed. The process circumvents the use of sodium hydride and isolation of reaction intermediates following the initial coupling of the hydantoin intermediate and 4-N-methylpiperizine.Type: GrantFiled: October 27, 2000Date of Patent: July 2, 2002Assignee: The Procter & Gamble CompanyInventors: Patricia Ann Matson, Michael Selden Godlewski, Daniel Joseph Quarroz, Yves Guggisberg
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Patent number: 6277997Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.Type: GrantFiled: October 20, 2000Date of Patent: August 21, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michelangelo Scalone, Ulrich Zutter
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Patent number: 6222039Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.Type: GrantFiled: July 7, 1999Date of Patent: April 24, 2001Assignee: Hoffman-La Roche Inc.Inventors: Michelangelo Scalone, Ulrich Zutter