- Synthesis, characterization, X-ray crystallography analysis and cell viability study of (η6-p-cymene)Ru(NH2R)X2 (X = Cl, Br) derivatives
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Studies over the past few decades demonstrate the potential for metallodrugs as bioactive therapeutics. Here, we describe six new ruthenium(II) complexes with the general motif of (η6-p-cymene)Ru(NH2R)X2, where NH2R is either the influenza A antiviral drugs rimantadine or amantadine or the N-methyl-D-aspartate [NMDA] receptor antagonist, memantine and X = Cl or Br. All complexes were synthesized in high yield and purity and characterized by NMR spectroscopy and X-ray crystallography. Both the chlorine and bromine ruthenium(II) p-cymene complexes demonstrated cellular toxicity profiles similar to their respective free ligand, indicating that complexation to ruthenium(II) centers does not significantly increase toxicity of the bioactive ligand.
- McDarmont, Sarah L.,Jones, Meredith H.,McMillen, Colin D.,Smith, Everett Clinton,Pienkos, Jared A.,Joslin, Evan E.
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Read Online
- Synthesis, crystallographic studies, molecular modeling and in vitro biological studies of silver(I) complexes with aminoadamantane ligands
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Silver(I) complexes with amantadine (atd) and memantine (mtn) were synthesized and characterized. Elemental, thermogravimetric and mass spectrometric analyses indicated a 1:2 metal/ligand ratio, with the molecular composition AgC20H34N2·NO3 for Ag–atd and AgC24H42N2·NO3·H2O for Ag–mtn. The crystal structures of the silver(I) complexes were determined by single crystal X-ray diffractometric studies and show the coordination of amantadine and memantine to the Ag(I) ion by the nitrogen atom of the NH2 group. The spectral analysis by infrared and 1H, 13C and {15N,1H} nuclear magnetic resonance (NMR) spectroscopies confirmed the coordination sites of the ligands to the silver ions. Computational studies revealed modes of vibration and bond lengths similar to those found experimentally. The in vitro antibacterial activity assays showed that amantadine is not active over the tested strains while memantine showed a low activity against Staphylococcus aureus and Pseudomonas aeruginosa. On the other hand, the complexes had a pronounced antibacterial activity over the same strains with minimum inhibitory concentration (MIC) values in the micromolar range. Biophysical assays based on fluorescence spectroscopy indicated that the silver(I) complexes interact weakly with bovine serum albumin, while agarose gel electrophoresis and competitive binding experiments revealed that the compounds interact with DNA by non-covalent interactions.
- dos Santos Pereira, Anna Karla,Nakahata, Douglas Hideki,Manzano, Carlos Marrote,de Alencar Simoni, Déborah,Pereira, Douglas Henrique,Lustri, Wilton Rogério,Formiga, André Luiz Barboza,Corbi, Pedro Paulo
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Read Online
- Green preparation method of memantine
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The method comprises the following steps: (1) mixing 1 - chlorine -3 and 5 - dimethyl adamantane with acetamide to obtain 1 -acetylamino -3 and 5 -dimethyladamantane. (2) The 1 -acetylamino -3, 5 -dimethyladamantane was deacetylated in a hot-water system to obtain a memantine. The preparation method provided by the invention is simple to operate. The method is safe, environment-friendly, high in yield and purity, cost-saving, low in production cost and beneficial to industrial production.
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Paragraph 0047-0056
(2021/09/15)
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- Cerium-Catalyzed C-H Functionalizations of Alkanes Utilizing Alcohols as Hydrogen Atom Transfer Agents
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Modern photoredox catalysis has traditionally relied upon metal-to-ligand charge-transfer (MLCT) excitation of metal polypyridyl complexes for the utilization of light energy for the activation of organic substrates. Here, we demonstrate the catalytic application of ligand-to-metal charge-transfer (LMCT) excitation of cerium alkoxide complexes for the facile activation of alkanes utilizing abundant and inexpensive cerium trichloride as the catalyst. As demonstrated by cerium-catalyzed C-H amination and the alkylation of hydrocarbons, this reaction manifold has enabled the facile use of abundant alcohols as practical and selective hydrogen atom transfer (HAT) agents via the direct access of energetically challenging alkoxy radicals. Furthermore, the LMCT excitation event has been investigated through a series of spectroscopic experiments, revealing a rapid bond homolysis process and an effective production of alkoxy radicals, collectively ruling out the LMCT/homolysis event as the rate-determining step of this C-H functionalization.
- An, Qing,Chen, Yuegang,Liu, Weimin,Pan, Hui,Wang, Xin,Wang, Ziyu,Zhang, Kaining,Zuo, Zhiwei
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supporting information
p. 6216 - 6226
(2020/04/27)
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- Memantine hydrochloride synthesis method
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The invention provides a memantine hydrochloride synthesis method, and belongs to the technical field of medicine synthesis. The preparation method comprises the following steps: carrying out a substitution reaction on 1-bromo-3,5-dimethyladamantane and acetamide to obtain 1-acetamido-3,5-dimethyladamantane, mixing the 1-acetamido-3,5-dimethyladamantane, an alcohol and an alkali, carrying out an alcoholysis reaction to obtain 1-amino-3,5-dimethyladamantane, and finally carrying out an acidification reaction on the 1-amino-3,5-dimethyladamantane and hydrochloric acid to obtain memantine hydrochloride. According to the method of the invention, 1-bromo-3,5-dimethyl adamantane and acetamide are used as the starting raw materials, so the sources of the raw materials are wide, the use of acetonitrile is avoided, and no pollution is caused to the human body and the environment; the use of catalysts is avoided in the whole reaction process, the reaction product is easy to separate, and the yield of the obtained memantine hydrochloride is high; and the method is mild in reaction condition and suitable for industrial production.
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- Deacetylative Amination of Acetyl Arenes and Alkanes with C-C Bond Cleavage
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The Br?nsted acid-catalyzed synthesis of primary amines from acetyl arenes and alkanes with C-C bond cleavage is described. Although the conversion from an acetyl group to amine has traditionally required multiple steps, the method described herein, which uses an oxime reagent as an amino group source, achieves the transformation directly via domino transoximation/Beckmann rearrangement/Pinner reaction. The method was also applied to the synthesis of γ-aminobutyric acids, such as baclophen and rolipram.
- Hyodo, Kengo,Hasegawa, Genna,Maki, Hiroya,Uchida, Kingo
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supporting information
p. 2818 - 2822
(2019/04/25)
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- CRYSTAL OF 1-AMINO-3,5-DIMETHYL ADAMANTANE HYDROCHLORIDE
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PROBLEM TO BE SOLVED: To provide a crystals of 1-amino-3,5-dimethyl adamantane hydrochloride that has excellent fluidity. SOLUTION: Provided is a crystal of 1-amino-3,5-dimethyl adamantane hydrochloride having a crystal aspect ratio of 1.0 to 1.5. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0067; 0072
(2019/05/11)
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- Synthesis, molecular docking studies, and antimicrobial evaluation of new structurally diverse ureas
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A series of new urea derivatives (3a-p) have been synthesized from readily available isocyanates and amines in good to high yields. All synthesized compounds were fully characterized using 1H NMR, 13C NMR, IR, and mass spectrometry. Additionally, the structure of the compound (3n) was confirmed by single-crystal X-ray diffraction. Furthermore, all compounds were evaluated for antimicrobial activity against five bacteria and two fungi. Last but not the least, molecular docking studies with Candida albicans dihydropteroate synthetase were performed and the results are presented herein.
- Patil, Mahadev,Poyil, Anurag Noonikara,Joshi, Shrinivas D.,Patil, Shivaputra A.,Patil, Siddappa A.,Bugarin, Alejandro
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p. 302 - 311
(2019/03/26)
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- A hydrochloric acid just preparation method
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The invention discloses a method for preparing memantine hydrochloride. The method is characterized in that the method provided by the invention uses 1-bromo-3,5-dimethyladamantane (represented by a general formula IV in the description) as a starting material which is subjected to an amination reaction with acetamine to obtain a key intermediate 1-actamido-3,5-dimethyladmantane (represented by a general formula III in the description); the compound represented by the general formula III is subjected to alcoholysis in a mixture system of inorganic base and n-butyl alcohol for deacetylated to obtain memantine; memantine is treated using hydrochloric acid in a ketone solvent to obtain memantine hydrochloride. The method provided by the invention overcomes deficiencies in the prior art and has the advantages that the raw materials are simple and readily available, the reaction steps are simple and short, and the operations are convenient and fast, therefore, the method is suitable for industrial production.
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- METHOD FOR PRODUCING 1-AMINO-3,5-DIMETHYL ADAMANTANE HYDROCHLORIDE
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PROBLEM TO BE SOLVED: To provide a novel method for producing 1-amino-3,5-dimethyl adamantane hydrochloride. SOLUTION: The production method comprises: a step of producing a compound (2) by reacting 1,3-dimethyl adamantane with compound (1) in a reaction solution, and then compound (3) is added to the reaction solution containing compound (2) to produce compound (4); a step of converting compound (4) to compound (5); and a step of bringing compound (5) into contact with hydrogen chloride or a solution thereof to convert to 1-amino-3,5-dimethyl adamantane hydrochloride (6). [X is a halogen atom; R is H, a hydroxy group, an optionally substituted C1 to 4 alkyl group, an optionally substituted C1 to 4 alkoxy group or an optionally substituted C7 to 13 aralkyl-oxy group.]. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0048
(2017/07/23)
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- Preparation method of memantine hydrochloride
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The invention relates to a preparation method of memantine hydrochloride. According to the preparation method, crude 1-acetylamino-3,5-dimethyladamantane is prepared via direction reaction of a system composed of 1,3-dimethyladamantane, acetonitrile, and concentrated sulfuric acid; the crude 1-acetylamino-3,5-dimethyladamantane is subjected to hydrolysis without purifying directly; ethanediol is taken as a solvent, and crude memantine is obtained via hydrolysis under alkaline conditions; crude memantine is extracted with hydrocarbon solvents such as n-heptane; concentrated hydrochloric acid or an organic solution of hydrochloric acid is added into an obtained extracted solution directly so as to obtain a crude memantine hydrochloride solid; and recrystallization is carried out with an alcohol-ethyl acetate system so as to obtain refined memantine hydrochloride. Operation of the preparation method is simple; the preparation method is simplified; yield is high; production cost is low; and the preparation method is suitable for industrialized production.
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- A hydrochloric acid just preparation method
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The present invention discloses a memantine hydrochloride preparation method, especially a method for synthesizing memantine hydrochloride by adopting 1-bromo-3,5-dimethyl adamantane as a starting raw material. The memantine hydrochloride preparation method is characterized in that the reaction process from the starting raw material to the final product is shortened into the one-step reaction, the 1-bromo-3,5-dimethyl adamantane is adopted as the starting raw material, the 1-bromo-3,5-dimethyl adamantine and ammonium acetate are subjected to direct amination, and the adjustment is performed to obtain the memantine hydrochloride. Compared with the memantine hydrochloride preparation method in the prior art, the memantine hydrochloride preparation method of the present invention has the following advantages that: the memantine hydrochloride prepared by the preparation method of the present invention has characteristics of stable quality, high purity, the total impurity of less than 0.3%, the single impurity of less than 0.05% and the yield of 88-90%, and the preparation method has characteristics of less reaction steps, simple operation, mild reaction conditions, and easy industrial production achieving.
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Paragraph 0033; 0034
(2017/04/14)
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- NOVEL ADAMANTANE AND MEMANTINE DERIVATIVES AS PERIPHERAL NMDA RECEPTOR ANTAGONISTS
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The present invention relates to cationic compounds of formula (I) for use as peripheral NMDA receptor antagonists.
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Page/Page column 17
(2017/02/24)
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- One-Pot Amination of Cage Hydrocarbons
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A one-pot procedure has been proposed for the synthesis of amines directly from cage hydrocarbons. A number of cage amines have been synthesized by treatment of adamantane, its homologs, and structurally related cage hydrocarbons with nitric acid in acetic acid and subsequent addition of urea and heating.
- Leonova,Skomorokhov,Moiseev,Klimochkin
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p. 1703 - 1709
(2016/02/03)
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- Silver-Catalyzed Decarboxylative Azidation of Aliphatic Carboxylic Acids
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The catalytic decarboxylative nitrogenation of aliphatic carboxylic acids for the synthesis of alkyl azides is reported. A series of tertiary, secondary, and primary organoazides were prepared from easily available aliphatic carboxylic acids by using K2S2O8 as the oxidant and PhSO2N3 as the nitrogen source. The EPR experiment sufficiently proved that an alkyl radical process was generated in the process, and DFT calculations further supported the SET process followed by a stepwise SH2 reaction to afford azide product.
- Zhu, Yuchao,Li, Xinyao,Wang, Xiaoyang,Huang, Xiaoqiang,Shen, Tao,Zhang, Yiqun,Sun, Xiang,Zou, Miancheng,Song, Song,Jiao, Ning
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p. 4702 - 4705
(2015/10/12)
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- MANUFACTURING PROCESS FOR MEMANTINE
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A method for manufacturing 3,5-dimethyl-1-adamantanamine of the present invention comprises: (i) a step of reacting 3,5-dimethyl-1-adamantanol with an acid and nitrile in an organic solvent to obtain a reaction solution; (ii) a step of adding water to the reaction solution obtained in step (i) to obtain 1-amido-3,5-dimethyladamantane; and (iii) a step of hydrolyzing 1-amido-3,5-dimethyladamantane obtained in step (ii) in the presence of an alcohol-containing solvent and an inorganic base.
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Paragraph 0063
(2015/12/18)
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- Selective intermolecular amination of C-H bonds at tertiary carbon centers
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C-H insertion: A method for intermolecular amination of tertiary C-H bonds is described that uses limiting amounts of substrate and a convenient phenol-derived nitrogen source. Structure-selectivity and mechanistic studies suggest that steric interaction between the substrate and active oxidant is the principal determinant of product selectivity. Copyright
- Roizen, Jennifer L.,Zalatan, David N.,Du Bois
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supporting information
p. 11343 - 11346
(2013/11/06)
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- Synthesis and IR/MS study of 3,5-dimethyladamantanamine hydrochloride salt
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This paper studied the synthesis of memantine hydrochloride characteristics by optimizing the synthetic route in the bromination of acid hydrolysis under the conditions of acetonitrile and the final salt formation reaction, so that memantine hydrochloride in an overall yield of the products from the 67.3 % reported in the literature increased to 81.5 %. Compared to 1,3-dimethyl adamantane and 3,5-dimethyladamantanamine, the infrared spectra showed the characteristic absorptions of 3,5-dimethyl-adamantanamine hydrochloride. Especially by the use of ESI method Spray ionization mass spectrometry analysis of fragments of memantine hydrochloride mass characteristics of ammonia compounds. By IR and MS studies to determine the spectrum of memantine hydrochloride microscopic molecular structure of ammonia.
- Ren, Huixue,Ying, Hanjie,Ouyang, Pingkai,Lin, Jimao,Jing, Liu
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p. 5107 - 5110
(2012/10/08)
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- METHOD FOR PRODUCING MEMANTINE
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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.
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Page/Page column 19-21
(2010/08/05)
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- PROCESS FOR THE PREPARATION OF MEMANTINE AND ITS SALTS AND INTERMEDIATE FOR USE THEREIN
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The present invention provides 2-(3,5-dimethyl-adamantan-1-yl)-isoindole-1,3-dione of formula II, which is useful as an intermediate in the preparation of memantine and its salts. The present invention also provides a process for preparing 2-(3,5-dimethyl-adamantan-1- yl)-isoindole-1,3-dione and a process for preparing memantine or a salt thereof using 2- (3,5-dimethyl-adamantan-1 -yl)-isoindole-1,3-dione.
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Page/Page column 13
(2010/04/03)
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- Novel treatment for alzheimer's disease
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The present invention concerns a new pharmaceutical composition comprising an antagonist and a co-agonist of the N-methyl-D-aspartate-type glutamate receptor (NMDAR). The inventors found that the co-administration of these two compounds effectively inhibits production of amyloide-β peptide. In patient's suffering from Alzheimer's disease, these peptides are deposited in the extracellular matrix forming neuritic "plaques". Therefore, the present inventors identified a new possibility for prophylaxis and/or treatment of Alzheimer's disease by stopping the continued formation of neuropathological extracellular deposits.
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- METHODS OF TREATING CNS DISORDERS
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The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.
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- Pharmaceutical compositions comprising aminoadamantane derivatives
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The present invention relates to pharmaceutical compositions comprising 1-aminoadamantane derivatives and a cyclodextrin, which compositions exhibit advantageous safety, convenience, and dosing characteristics. The compositions of the instant invention find particular application in the treatment of various diseases and conditions of the CNS, including those involving the impairment of cognitive function or dementia, such as Alzheimer's disease.
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- PROCESS FOR PREPARING MEMANTINE HYDROCHLORIDE SUBSTANTIALLY FREE OF !MPURITIES
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A process for preparing memantine hydrochloride free from impurities comprises (a) reacting 1,3-dimethyladarnantane with acetontitrile and sulphuric acid to produce 1- acetamido-3,5-dimethyl adamantane; (b) treating l-acetamido-3,5-dimethyl adamantane with base in the presence of solvent to produce memantine; (c) reacting memantine with alcoholic HCl in the presence of solvents to produce memantine hydrochloride; and purification of memantine hydrochloride using aliphatic solvents.
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Page/Page column 7
(2010/01/12)
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- IMPROVED PROCESS FOR MEMANTINE HYDROCHLORIDE
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The present invention provides an improved eco-friendly process for the preparation of memantine hydrochloride compound of formula (1). The present invention also provides one-pot process for the preparation of memantine hydrochloride compound of fomula (1) from 1,3 -dimethyl adamantane without isolating any intermediates.
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Page/Page column 11-12
(2009/06/27)
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- ADAMANTANAMINES AND NERAMEXANE SALTS OF THIOMOLYBDIC AND THIOTUNGSTIC ACIDS
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This invention concerns adamantanamines (e.g. memantine, amantadine, and rimantadine) and neramexane salts of thiomolybdic and thiotungstic acids, including their preparation and pharmaceutical compositions, as dual acting drugs. These salts are used to treat or potentially arrest the neurodegenerative pathophysiology, clinical signs and symptoms of dementia of the Alzheimer's type, Parkinson's, Huntington's, AIDS-related dementia and Schizophrenia and its cognitive deficits. Additional uses of these derivatives include antiviral activity. The novel compositions of the present invention appear particularly useful in enhancing the therapeutic benefits of copper-sequestering tetrathiomolybdates in treating elevated copper-induced toxicities in neurologically presenting Wilson's disease, and in treating diseases of the inflammatory etiology and abnormal copper biochemistry, such as tumor angiogenesis, liver cirrhosis, hepatitis, pulmonary fibrosis and other fibrotic diseases, cardiovascular disease, cerebral ischemia, renal anemia, rheumatoid arthritis, diabetes, obesity, gastrointestinal disorders, and eye diseases such as glaucoma, proliferative diabetic retinopathy, and age related macular degeneration. These compounds have excellent stability and aqueous solubility for good oral bioavailability.
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Page/Page column 28-29
(2008/12/08)
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- PROCESS FOR THE PREPARATION OF MEMANTINE
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A process for the preparation of Memantine of formula (I) or its pharmaceutically acceptable salts is disclosed. The process comprises formula (I): (a) reacting halogenated-3, 5 -dimethyl adamantine of formula (III) with acetamide in presence of sulfuric acid to provide l-Acetamido-3,5-dimethyl adamantine of formula (II), wherein X is Cl or Br. Formula (III), (II): (b) treating l-Acetamido-3,5-dimethyl adamantine of formula (II) with base in presence of solvent to obtain Memantine of formula (I) (c) optionally converting Memantine of formula (I) in to pharmaceutically acceptable salts.
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Page/Page column 16-17
(2008/12/05)
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- Process for the preparation of memantine and its hydrochloric acid salt form
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The present invention relates to the synthesis of 1-amino-3,5-dimethyladamantane ("memantine") and its hydrochloric acid salt form. In particular a new intermediate (N-chloro-acetylamino-3,5-dimethyladamantane) for the synthesis of memantine as well as a new process for the preparation of memantine and its hydrochloric acid salt form using said intermediate is disclosed.
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Page/Page column 8
(2008/06/13)
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- CARNITINE CONJUGATES OF ADAMANTANAMINES AND NERAMEXANE DERIVATIVES AS DUEL PRODRUGS FOR VARIOUS USES
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This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutical ly-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.
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Page/Page column 38-39
(2008/06/13)
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- A PROCESS FOR THE PREPARATION OF MEMANTINE HYDROCHLORIDE
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3,5-Dimethyladamantane is reacted with bromine to form l-bromo-3,5,- dimethyladamantane of formula (I), it is reacted with acetonitrile in the presence of acid to form l-acetamido-3,5-dimethyladamantane of formula (II). Optionally formula (II) is treated with an organic acid to form the corresponding salt of formula (Ill), which is setting free of salt in the presence of base to get the pure formula (II). A formula (II) is subjected to hydrolysis followed by in-situ reaction with hydrochloric acid to form memantine hydrochloride. The memantine hydrochloride is treated with base to get the pure memantine base.
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Page/Page column 6; 13
(2008/06/13)
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- New synthetic approach to memantine hydrochloride starting from 1,3-dimethyl-adamantane
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A short and practical method for the synthesis of 1-amino-3,5-dimethyl- adamantane (Memantine hydrochloride) was established by using tertiary butyl alcohol under Ritter conditions to give 1-acetamido-3,5-dimethyl-adamantane. The 1-acetamido-3,5-dimethyl-adamantane is hydrolyzed using alkali to give free base which was then converted into its hydrochloride acid.
- Madhra, Mukesh K.,Sharma, Mukesh,Khanduri
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p. 922 - 923
(2012/12/30)
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- Process for the preparation of adamantanamines
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The present invention concerns a process for the manufacture of an adamantanamine of formula wherein R, R' and X are as defined in the claims, which comprises (i) reacting a compound of formula with thiourea; (ii) subjecting the resulting compound of formula to an acid treatment and (iii) isolating the resulting adamantanamine or a hydrohalogenide thereof. According to the process of the invention, valuable pharmaceuticals are obtainable, such as Memantine hydrochloride (R,R' = methyl), an uncompetitive NMDA(N-methyl-D-aspartate) receptor antagonist used as a new treatment for Alzheimer's disease, or Amantadine hydrochloride (R,R' = hydrogen) used as an antiviral or in the treatment of Parkinson's disease.
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Page/Page column 6
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF ADAMANTANAMINES
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The invention relates to a process for preparing certain adamantanamines, of formula (IV) wherein R, R' are each methyl and X is halogen, to intermediates used in the process, and to processes for preparing such intermediates.
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Page/Page column 12; 13-14
(2010/11/28)
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- A METHOD OF PREPARING MEMANTINE HYDROCHLORIDE
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A new method of preparing memantine hydrochloride, comprises the following steps: reacting 1-bromo-3,5-dimethyl adamantane and urea/formic acid with formic acid also acting as the solvent; hydrolysising with aqueous inorganic acid; alkalifying, extracting and acidifying with hydrochloric acid; finally collecting target compound. The method uses cheaper raw materials and conducts in homogeneous phase under mild conditions. It can reach high yield and good product purity, and be suitable for macrochemistry. The purity of crude product is 99.0%, and reaches 99.98% after first recrystallization, yield: 69.5%, mp: 332 C (DSC).
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Page/Page column 3-4
(2008/06/13)
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- Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors
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The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
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- NMDA receptor antagonists and their use in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau
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Aminocyclohexane and aminoalkylcyclohexane compounds, which are systemic-ally-active as NMDA receptor antagonists, are effective in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau, method of treating disorders resulting from or associated with abnormal hyperphosphorylation of microtubule associated protein tau, and pharmaceutical compositions comprising the same.
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- Use of aminoadamantane compounds as immunoregulators
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wherein R1, R2, R3 and R4 are selected independently from each other from —NR5R6, —NR5R6R7+, hydrogen, aryl or heteroaryl with up to 7 ring members, C1-C20-alkyl, C1-C20-alkenyl and C1-C20-alkinyl, wherein the alkyl, alkenyl and alkinyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, with the proviso that at least one of the residues R1, R2, R3 and R4 are represented by —NR5R6 or —NR5R6R7; andR5, R6 and R7 are selected independently from each other from hydrogen, aryl or heteroaryl with up to 7 ring members, C1-C20-alkyl, C1-C20-alkenyl, C1-C20-alkinyl, wherein the alkyl, alkenyl and alkinyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, or R5 and R6, together with the nitrogen atom, form a heterocyclic group with up to 7 ring members;for the regulation of the activity of already activated neutrophils.
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- Reaction of Adamantane, Adamantanecarboxylic Acids, and Bicyclo[3.3.1]nonanecarboxylic Acids with Acetonitrile in Liquid Bromine
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Carboxylic acids of the adamantane and bicyclo[3.3.1]nonane series react with acetonitrile in a liquid bromine medium in the presence of water to give corresponding acetamido derivatives. Reaction of adamantane and some its alkyl derivatives with acetonitrile in liquid bromine in the presence of methanol produces 1-aminoadamantanes.
- Khil'chevskii,Baklan,Kukhar'
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p. 982 - 984
(2007/10/03)
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- Adamantane derivatives in the prevention and treatment of cerebral ischemia
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A method for the prevention and treatment of cerebral ischemia using an adamantane derivative of the formula STR1 wherein R1 and R2 are identical or different, representing hydrogen or a straight or branched alkyl group of 1 to 6 C atoms or, in conjunction with N, a heterocyclic group with 5 or 6 ring C atoms; wherein R3 and R4 are identical or different, being selected from hydrogen, a straight or branched alkyl group of 1 to 6 C atoms, a cycloalkyl group with 5 or 6 C atoms, and phenyl; wherein R5 is hydrogen or a straight or branched C1 -C6 alkyl group, or a pharmaceutically-acceptable salt thereof, is disclosed.
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- Salts of dihalo-3,4-dihydro-3-oxo-2-quinoxaline carboxylic acids and hindered amines
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Salts of 6,7-dihalo-3,4-dihydro-3-oxo-2-quinoxaline carboxylic acids and hindered amines, useful in combating influenza A and B.
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