Tricyclo Ring System Patents (Class 564/459)
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Publication number: 20150105559Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.Type: ApplicationFiled: March 4, 2013Publication date: April 16, 2015Applicant: Kyushu University, National University CorporationInventors: Takashi Ohshima, Hiroyuki Morimoto, Yuhei Shimizu
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Publication number: 20140378551Abstract: The invention relates to an analgesic composition containing memantine. According to the invention, such a composition is administered daily to a human patient having to undergo a surgical operation, over a period ranging from one day to a plurality of days before said surgical operation, in order to prevent and treat the development of post-operative neuropathic pain in this same patient.Type: ApplicationFiled: October 10, 2012Publication date: December 25, 2014Applicant: Universite d'AuvergneInventor: Gisele Pickering
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Publication number: 20140336266Abstract: Compositions and methods for administering memantine to a subject are provided. In particular, a solid pharmaceutical composition in a unit dosage form for once daily oral administration is provided. The compositions comprises an extended release formulation of 22.5 mg to 33.75 mg memantine, or a pharmaceutically acceptable salt thereof, wherein administration of a dose of the composition to a human subject provides a mean plasma memantine concentration profile characterized by a change in memantine concentration as a function of time (dC/dT) that is less than 50% of the dC/dT provided by the same quantity of an immediate release form of memantine, determined in a time period between 0 hours to 6 hours after administration of memantine, and wherein dC/dT is measured in a single-dose human PK study. Methods of treating dementia, in particular Alzheimer's diseases, using the compositions are provided.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Applicant: ADAMAS PHARMACEUTICALS, INC.Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson
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Patent number: 8884059Abstract: The present invention is directed towards an electrocoating composition comprising a cyclic guanidine.Type: GrantFiled: September 17, 2010Date of Patent: November 11, 2014Assignee: PPG Industries Ohio, Inc.Inventors: Steven R. Zawacky, Thomas C. Moriarity, Donald W. Boyd, Geoffrey R. Webster, Joseph Lucas, Alan J. Kaylo, Chester J. Szymanski, Venkatachalam Eswarakrishnan
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Publication number: 20140315952Abstract: The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.Type: ApplicationFiled: November 29, 2012Publication date: October 23, 2014Inventor: Ziqiang Gu
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Publication number: 20140288185Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.Type: ApplicationFiled: November 1, 2012Publication date: September 25, 2014Inventors: Srinivasa Rao Akireddy, Jason Speake, Balwinder Singh Bhatti, Daniel Yohannes, John Genus, Yunde Xiao
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Patent number: 8796491Abstract: The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine: substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.Type: GrantFiled: August 7, 2009Date of Patent: August 5, 2014Assignee: Merz Pharma GmbH & Co. KGaAInventors: Markus-Rene Gold, Herbert Koller, Michael Pyerin
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Patent number: 8772547Abstract: The present invention relates to a process for preparing 1-adamantyltrimethylammonium hydroxide, by A) reacting 1-adamantyldimethylamine with dimethyl sulfate to give 1-adamantyltrimethylammonium sulfate; and B) subjecting the 1-adamantyltrimethylammonium sulfate obtained in A) to anion exchange with an ion exchanger loaded with OH ions.Type: GrantFiled: March 11, 2010Date of Patent: July 8, 2014Assignee: BASF SEInventors: Christof Wilhelm Wigbers, Martin Ernst, Laszlo Szarvas, Giovanni D'Andola, Ellen Dahlhoff, Gabriele Iffland, Peter Raatz, Falk Simon, Matthias Frauenkron
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Publication number: 20140041062Abstract: The present disclosure relates to an ASD genetically engineered model carrying a deletion of Shank2 gene and having reduced NMDA receptor function. According to the present disclosure, genetically engineered mice that show the clinical features of ASD due to the deletion of the Shank2 gene can be obtained, and the genetically engineered mice can be effectively used to screen candidate therapeutic agents.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicants: Industry-Academic Cooperation Foundation, Yonsei University, Korea Advanced Institute of Science and Technology, Seoul National University R&DB FoundationInventors: Min Goo Lee, Bong Kiun Kaang, Eunjoon Kim
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Publication number: 20130302430Abstract: The present invention provides immediate release and modified release oral dosage forms. Specifically, the invention provides modified and immediate release pharmaceutical dosage forms containing memantine that exhibit an enhanced release profile and provide reliable absorption. The dosage forms may be used to treat mild, moderate or severe Alzheimer's disease or neuropathic pain.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: Mahendra G. DEDHIYA, Suneel K. RASTOGI, Anil CHHETTRY, Narasimhan MANI, Niranjan RAO, Antonia PERICLOU
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Publication number: 20130231391Abstract: The present invention relates to adamantane derivatives that are active as antiviral and anti-microbial agents; antiviral or antibacterial compositions comprising adamantane derivatives or pharmaceutically acceptable salts thereof; and methods of preventing or treating viral or bacterial infections in mammalian hosts through the administration of adamantine derivatives or their salts or pharmaceutical compositions comprising the same. In particular, viral infections prevented or treated by the methods of the present invention may include, but are not limited to, those caused by arenavirus or one or more pox viruses, such as vaccinia and/or variola.Type: ApplicationFiled: February 15, 2013Publication date: September 5, 2013Applicant: VYMED CORPORATIONInventor: B. Vithal SHETTY
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Publication number: 20130165527Abstract: Compositions and methods for administering memantine to a subject are provided. In particular, a solid pharmaceutical composition in a unit dosage form for once daily oral administration is provided. The compositions comprises an extended release formulation of 22.5 mg to 33.75 mg memantine, or a pharmaceutically acceptable salt thereof, wherein administration of a dose of the composition to a human subject provides a mean plasma memantine concentration profile characterized by a change in memantine concentration as a function of time (dC/dT) that is less than 50% of the dC/dT provided by the same quantity of an immediate release form of memantine, determined in a time period between 0 hours to 6 hours after administration of memantine, and wherein dC/dT is measured in a single-dose human PK study. Methods of treating dementia, in particular Alzheimer's diseases, using the compositions are provided.Type: ApplicationFiled: January 28, 2013Publication date: June 27, 2013Applicant: ADAMAS PHARMACEUTICALS, INC.Inventor: ADAMAS PHARMACEUTICALS, INC.
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Publication number: 20130131006Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.Type: ApplicationFiled: April 28, 2011Publication date: May 23, 2013Applicant: Gachon University of Industry-Academic Cooperation FoundationInventors: Bong Hee Lee, Kyung Hee Byun
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Patent number: 8436209Abstract: The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 50° C.Type: GrantFiled: March 19, 2009Date of Patent: May 7, 2013Assignee: Merz Pharma GmbH & Co. KGaAInventors: Florian Anton Martin Huber, Giorgio Gallo, Carla De Faveri
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Publication number: 20130072553Abstract: This invention relates to the drugs, derivatives and analogs containing adamantane structures of new indication applications of anti-tumor. The invention also relates to above compounds to treat tumors and other diseases with FIG. 1. These drugs, derivatives and analogs are generated by the modification of the parent or fragment structures and formation of pharmaceutically acceptable salts, complex salts or prodrug. The drugs, derivatives and analogs as described are administered alone or together with at least one known anti-tumor and immune chemotherapeutic agent including treatment of viral, bacterial and fungal diseases, neurological diseases, endocrine system diseases, and immune system diseases.Type: ApplicationFiled: December 25, 2009Publication date: March 21, 2013Inventor: Lifeng Xu
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Publication number: 20130011474Abstract: The present invention provides immediate release and modified release oral dosage forms. Specifically, the invention provides modified and immediate release pharmaceutical dosage forms containing memantine that exhibit an enhanced release profile and provide reliable absorption. The dosage forms may be used to treat mild, moderate or severe Alzheimer's disease or neuropathic pain.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Mahendra G. DEDHIYA, Suneel K. RASTOGI, Anil CHHETTRY, Narasimhan MANI, Antonia PERICLOU, Niranjan Rao
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Publication number: 20120295886Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.Type: ApplicationFiled: May 18, 2012Publication date: November 22, 2012Applicant: INFLUMEDIX, INC.Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20120264978Abstract: The invention provides compostions for administering memantine to a subject. Memantine in an extended release form containing 22.5 to 30 mg memantine or a pharmaceutically acceptable salt achieves particular pharmacokinetic criteria such as change in plasma concentration of memantine over time and ratio of maximum memantine plasma concentration to mean memantine plasma concentration.Type: ApplicationFiled: June 28, 2012Publication date: October 18, 2012Applicant: Adamas Pharmaceuticals, Inc.Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson
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Publication number: 20120201889Abstract: The present invention provides immediate release and modified release oral dosage forms. Specifically, the invention provides modified and immediate release pharmaceutical dosage forms containing memantine that exhibit an enhanced release profile and provide reliable absorption. The dosage forms may be used to treat mild, moderate or severe Alzheimer's disease or neuropathic pain.Type: ApplicationFiled: February 15, 2012Publication date: August 9, 2012Applicant: Forest Laboratories Holdings Ltd.Inventors: Mahendra G. Dedhiya, Suneel K. Rastogi, Anil Chhettry, Narasimhan Mani, Antonia Periclou, Niranjan Rao
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Publication number: 20120040993Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.Type: ApplicationFiled: January 31, 2010Publication date: February 16, 2012Applicants: TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD., YEDA RESEARCH AND DEVELOPMENT CO., LTD.Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
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Publication number: 20120010431Abstract: The present invention relates to a process for preparing 1-adamantyltrimethyl-ammonium hydroxide.Type: ApplicationFiled: March 11, 2010Publication date: January 12, 2012Applicant: BASF SEInventors: Christof Wilhelm Wigbers, Martin Ernst, Laszlo Szarvas, Giovanni D'Andola, Ellen Dahlhoff, Gabriele Iffland, Peter Raatz, Falk Simon, Matthias Frauenkron
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Publication number: 20110306796Abstract: The present invention relates to an improved process for the preparation of 1-bromo-3,5-dimethyl adamantane of formula (III), which is an useful intermediate for synthesis of 1-amino-3,5-dimethyl adamantane of formula (I) or pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 30, 2009Publication date: December 15, 2011Applicant: ALEMBIC LIMITEDInventors: Ravi Ponnaiah, Ashok Prasad, Piyush Maheshbhai Rana, Kamlesh Shankarlal Kanzariya, Mitulkumar Bharatkumar Dolia
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Publication number: 20110288111Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: ApplicationFiled: August 21, 2009Publication date: November 24, 2011Applicant: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Publication number: 20110288336Abstract: Method for producing 1-amino-3,5-dimethyladamantane or a salt thereof, comprising: (i) heating 1-formamido-3,5-dimethyladamantane with a base in a protic solvent.Type: ApplicationFiled: December 16, 2009Publication date: November 24, 2011Applicant: Merz Pharma GmbH & Co. KGaAInventors: Markus-Rene Gold, Aigars Jirgensons, Florian Anton Martin Huber
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Publication number: 20110282100Abstract: The present invention relates to a process for preparing memantine, or a pharmaceutically acceptable salt thereof (e.g., memantine hydrochloride), which is substantially free of impurities.Type: ApplicationFiled: January 20, 2010Publication date: November 17, 2011Applicant: MERZ PHARMA GmbH & Co. KGaAInventors: Gunter Quack, Markus-Rene Gold
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Publication number: 20110263900Abstract: The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine:substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.Type: ApplicationFiled: August 7, 2009Publication date: October 27, 2011Applicant: MERZ PHARMA GmbH & CO. KGaAInventors: Markus-Rene Gold, Herbert Koller, Michael Pyerin
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Patent number: 7981930Abstract: Kits comprising an M2 inhibitor selected from amantadine and rimantadine; ribavirin, and a neuraminidase inhibitor (NAi) in an amount that is antivirally effective in the combination, an oral dosage form containing 75-250 mg of the M2 inhibitor, an oral dosage form comprising 100-400 mg of ribavirin and a neuraminidase inhibitor are provided for the treatment of influenza. Some embodiments of the kits comprise an oral dosage form containing 75-250 mg of the M2 inhibitor, an oral dosage form comprising 100-400 mg of ribavirin, and a neuraminidase inhibitor.Type: GrantFiled: February 29, 2008Date of Patent: July 19, 2011Assignee: Adamas Pharmaceuticals, Inc.Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
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Publication number: 20110082317Abstract: The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 50° C.Type: ApplicationFiled: March 19, 2009Publication date: April 7, 2011Inventors: Florian Anton Martin Huber, Giorgio Gallo, Carla De Faveri
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Publication number: 20110065762Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.Type: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20110064804Abstract: The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.Type: ApplicationFiled: April 9, 2010Publication date: March 17, 2011Applicant: Adamas Pharmaceuticals, Inc.Inventors: Gregory T. Went, Timothy J. Fultz
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Publication number: 20110065766Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.Type: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Patent number: 7902115Abstract: Herein are disclosed adducts of amines and polycarboxylic acids, and methods of making such adducts. Such adducts can be used to remove cyanogen chloride. Also disclosed are methods of providing such adducts on supports to form filter media. Also disclosed are methods of combining such filter media with catalysts and/or with porous polymeric webs to form filter systems.Type: GrantFiled: February 19, 2009Date of Patent: March 8, 2011Assignee: 3M Innovative Properties CompanyInventors: Duane D. Fansler, Allen R. Siedle, Zhongshu Tan, Thomas E. Wood
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Publication number: 20110046232Abstract: Orally dissolving formulations, e.g., tablets (ODTs) and films (ODFs) comprising memantine and methods of treating conditions, including childhood behavioral disorders and Alzheimer's disease, by administering orally dissolving formulations are provided. The orally dissolving formulations of the present invention may be used to treat various conditions, but is particularly suited to treat childhood behavioral disorders, such as autistic spectrum disorders or combined type Attention-Deficit/Hyperactivity Disorder (ADHD) and also to treat elderly patients suffering from Alzheimer's disease.Type: ApplicationFiled: September 23, 2010Publication date: February 24, 2011Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Shashank Mahashabde, Mahendra G. Dedhiya, Anil Chhettry, Ranajoy Sarkar
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Patent number: 7858660Abstract: Compositions, kits and methods are provided for the treatment or prophylaxis of influenza.Type: GrantFiled: June 2, 2009Date of Patent: December 28, 2010Assignee: Adamas Pharmaceuticals, Inc.Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
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Publication number: 20100292341Abstract: The present invention relates to quick dissolve pharmaceutical compositions. More particularly the invention relates to quick dissolve pharmaceutical compositions of memantine hydrochloride capable of dissolving in the oral cavity and process for preparing such compositions. The quick dissolve pharmaceutical compositions of memantine hydrochloride contain at least one water-soluble diluent in particular a mono- or disaccharide and at least one disintegrant and optionally other pharmaceutically acceptable excipients.Type: ApplicationFiled: June 26, 2008Publication date: November 18, 2010Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITEDInventors: Ramakrishnan Sankar, Chidambaram Seshadri Venkateswaran, Praveen Reddy Billa
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Publication number: 20100204470Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.Type: ApplicationFiled: June 25, 2007Publication date: August 12, 2010Inventors: Josef Wieser, Hannes Lengauer, Elfriede Klingler, Arthur Pichler, Hubert Sturm
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Publication number: 20100160302Abstract: The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined. The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.Type: ApplicationFiled: March 30, 2007Publication date: June 24, 2010Inventors: Balasubramanian Gopalan, Dhamjewar Ravi, Mohammed Rasheed, Swamy Hosamane Keshavapura HosamaneSreedhara, Ahmad Ishtiyaque
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Publication number: 20100130528Abstract: The present invention relates to new adamantane modulators of NMDA receptors and/or 5HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Patent number: 7462743Abstract: A crystalline Form II of memantine hydrochloride, pharmaceutical compositions containing crystalline Form II, and methods of preparing crystalline Forms I and II of memantine hydrochloride are provided.Type: GrantFiled: January 11, 2006Date of Patent: December 9, 2008Assignee: Teva Pharmaceutical Fine Chemicals S.r.l.Inventors: Valeriano Merli, Paola Daverio, Adrienne Kovacsne-Mezei, Judith Aronhime
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Publication number: 20080300390Abstract: The present invention relates to reducing carbohydrate derivatives of adamantane amines of Formula A or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R1, R2, R3, and R4 are together or separately H, F, methyl or lower alkyl, alkenyl, or alkynyl groups, and Z is derived from a mono-, di-, oligo-, or poly-saccharide that originally had an aldehyde carbonyl group. The present invention also relates to processes for the preparation of such adamantane amine derivatives, and uses of such derivatives. The compounds of the present invention are useful in the treatment of infections caused by Gram positive or Gram negative bacteria.Type: ApplicationFiled: June 24, 2008Publication date: December 4, 2008Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Sebastian P. Assenza, Nanzhu Shen, Salvatore Iacono, Yuriy B. Kalyan, Peter Viski, Matthew Ronsheim
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Publication number: 20080275112Abstract: The present invention describes 1-aminoadamantane derivatives and 3-aminoadamantane-1-carboxylic derivatives in which the 5- or 7-position of the basic adamantane structure can be optionally substituted, methods for the production of the compounds based on the present invention, and methods for the coupling of the monomeric 3-aminoadamantane-1-carboxylic derivatives thus obtained to oligomers. The compounds based on the present invention are suitable for the utilisation as antiviral active ingredients, artificial ion channels, as well as for the therapy, diagnostics and prophylaxis of diseases in which a dysfunction of the GABA system occurs.Type: ApplicationFiled: July 22, 2005Publication date: November 6, 2008Inventors: Peter R. Schreiner, Lukas Wanka
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Publication number: 20080183003Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: ApplicationFiled: February 4, 2008Publication date: July 31, 2008Applicant: Adamas Pharmaceuticals, Inc.Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
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Patent number: 7329759Abstract: The present invention provides illudin analogs of the general formula (I): where R1 is (CH2)n—X—Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7 membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2(C1-C4)alkyl, O—(C5-C12)aryl or —S—(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).Type: GrantFiled: December 20, 2005Date of Patent: February 12, 2008Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Publication number: 20030050338Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various diseases.Type: ApplicationFiled: March 27, 2002Publication date: March 13, 2003Inventors: Michael Palladino, Emmanuel A. Theodorakis
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Patent number: 6444702Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: GrantFiled: February 22, 2000Date of Patent: September 3, 2002Assignee: NeuroMolecular, Inc.Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stemler, Stuart A. Lipton
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Patent number: 6423871Abstract: A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of protecting groups. Compounds of the class of secondary amines are produced by reacting an alkyl halide with an alkyl amine in anhydrous solvent, preferably dimethyl sulfoxide or N,N-dimethylformamide, in the presence of 0.1 to 3 molar equivalents of a cesium base. Optionally, the extent and selectivity of mono-N-alkylation is enhanced by addition to the reaction mixture of a powdered molecular sieve material for removal of water produced by the reaction, and/or tetrabutylammonium iodide to promote halide exchange. The invention permits selective and efficient mono-N-alkylation of a wide variety of substrates at 23° C.Type: GrantFiled: February 25, 2000Date of Patent: July 23, 2002Assignee: University of South FloridaInventor: Kyung Woon Jung
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Patent number: 6114392Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.Type: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 5912386Abstract: The present invention relates to compounds of the formula (I)R.sup.1 --NH--B--NH--R.sup.2 (I),whereinR.sup.1 and R.sup.2 independently of one another denote an unsubstituted or substituted radical of the formula ##STR1## and B represents an unsubstituted or substituted cycloalkylene-containing bridge member, which are suitable for bulk dyeing of plastics.Type: GrantFiled: February 6, 1998Date of Patent: June 15, 1999Assignee: Bayer AktiengesellschaftInventors: Dietmar Kalz, Karl-Heinz Reinhardt, Helmut Blaser
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Patent number: 5719176Abstract: A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient. In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl. The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields.Type: GrantFiled: October 2, 1996Date of Patent: February 17, 1998Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5609867Abstract: This invention provides novel antitumor agents having the formula: ##STR1## wherein A, B, G, W, R.sup.1, R.sup.2, R.sup.3, n, m and Z are described in the specification which have activity as anticancer agents and inhibit leukemia and solid tumor growth in a mammal.Type: GrantFiled: August 29, 1995Date of Patent: March 11, 1997Assignee: American Cyanamid CompanyInventor: Hwei-Ru Tsou