- NOVEL AROMATIC COMPOUND AND POLYARYLENE COPOLYMER HAVING NITROGEN-CONTAINING HETEROCYCLE INCLUDING SULFONIC ACID GROUP IN SIDE CHAIN
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Provided is a solid polymer electrolyte having increased heat resistance and high proton conductivity and a proton conductive membrane composed of the electrolyte. Also provided is a copolymer having a sulfonic acid group. The copolymer includes a repeating unit represented by Formula (1): (in the formula, Y denotes at least one kind of structure selected from the group consisting of —CO—, —SO2—, —SO—, —CONH—, —COO—, —(CF2)l— (l is an integer of 1 to 10), and —C(CF3)2—; W denotes at least one kind of structure selected from the group consisting of a direct bond, —CO—, —SO2—, —SO—, —CONH—, —COO—, —(CF2)l— (l is an integer of 1 to 10), —C(CF3)2—, —O—, and —S—; Z denotes a direct bond or at least one kind of structure selected from the group consisting of —(CH2)l—(l is an integer of 1 to 10), —C(CH3)2—, —O—, —S—, —CO—, and —SO2—; R30 denotes a nitrogen-containing aromatic ring having a substituent represented by —SO3H, —O(CH2)hSO3H, or —O(CF2)hSO3H (h is an integer of 1 to 12); p is an integer of 0 to 10; q is an integer of 0 to 10; r is an integer of 1 to 5; and k is an integer of 0 to 4).
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- COMPOUNDS FOR THE TREATMENT OF OSTEOPOROSIS AND CANCERS
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Methods are provided for the treatment of osteoporosis and multiple myeloma, using 3-imidazoyl-pyrazolo[3,4-b]pyridine compounds.
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- OXIDIZED AND MALEATED DERIVATIVE COMPOSITIONS
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Oxidized and maleated derivative compositions, such as chemically modified oxidized and maleated tall oil fatty acid compositions, can be prepared and used in a variety of industrial applications, including as emulsifiers, corrosion inhibitors, concrete admixtures, and in reverse flotation mining applications.
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- Pyridoxine and pyridoxal analogues: new uses
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The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT, stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.
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- Pyridoxine and pyridoxal analogues: new uses
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The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT, stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.
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- BETA-SHEET MIMETICS AND METHODS RELATING TO THE USE THEREOF
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beta -sheet mimetics and methods relating to the same are disclosed. The beta -sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a beta -sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.
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- Pyridoxine and pyridoxal analogues: novel uses
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The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of undesired platelet aggregation, and in the treatment of symptoms thereof.
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- Hypoglycemic imidazoline compounds
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This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.
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- Pyridoxine AMD pyridoxal analogues: cardiovascular therapeutics
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The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of cardiovascular or related diseases and in the treatment of symptoms thereof.
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- BETA-SHEET MIMETICS AND THEREOF AS PROTEASE INHIBITORS
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There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, the β-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The β-sheet mimetics have utility as protease inhibitors generally, including activity as serine protease inhibitors such as thrombin, elastase and Factor X.
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- Methods for regulating transcription factors
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beta -sheet mimetics and methods relating to the same are disclosed. The beta -sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a beta -sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.
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- INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP
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The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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- 1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation
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A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: STR1 wherein R1 -R6 are as described in the specification; or a pharmaceutically-acceptable salt thereof.
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- HYDROXAMIC ACID AND CARBOXYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE THEREOF
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This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.
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- Process for the production of low-viscosity storable amphoteric surfactants from imidazolines
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In order to prepare fluid, storage-stable ampholytic surface-active agents, (a) 1-hydroxyethyl-2-alkyl-2-imidazolines having formula (1), in which R1 stands for an alkyl residue with 5 to 21 carbon atoms, are quaternated or carboxymethylated with halogenated carboxylic acid salts at a pH range from 7.5 to 9, and at the same time hydrolyzed with aqueous bases, then (b) the pH value of the reaction final products is set between 5 and 7. STR1
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- Hetrazepine compounds which have useful pharmaceutical utility
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The invention relates to new hetrazepines of general formula STR1 wherein A, Z, n, X, Y, R 1, R 2, R 3 and R 4 have the meanings given in the specification.The new compounds are intended for use in treating pathological conditions and diseases in which PAF (platelet activating factor) is implicated.
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- Imidazolines N-substituted by a biphenylmethyl group, their medical use and the pharmaceutical compositions therefor
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The invention relates to compounds of the formula STR1 in which X and R1 -R5 are defined in the specification and their salts where appropriate, all of which are useful as angiotensin II antagonists.
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- Ethylenethiourea S-Oxidation Products: Preparation, Degradation, and Reaction with Proteins
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Ethylenethiourea (ETU) is carcinogenic degradation product of major ethylene bis(dithiocarbamate) fungicides with biological activity attributed to poorly characterized oxidation products.The reaction of ETU with H2O2 was examined in aqueous medium at pH percent, 7, and 9 by 1H NMR spectroscopy giving five principal products: sequential formation of sulfenic, suflinic, and sulfonic acids as well as imidazoline and ethyleneurea.Maximum yields with 2 equiv of H2O2 at optimal pH were 10, 71, 5, 53, and 100percent, respectively.Oxidation proceeds mainly through the sulfinic acid to imidazoline in acidic medium and the S-oxide to ethyleneurea in basic medium. 1H NMR of urine from mice treated with ETU revealed ETU and imidazoline (no ethyleneurea or S-oxidation products).Albumin was radiolabeled in ca.17percent yield by a 10-fold excess of ETU/H2O2 oxidation products (primatily the sulfenic and sulfinic acids), and such protein modification aould be prevented by glutathione.Keywords: Ethylenethiourea; ethylenethiourea S-oxidation products; hydrogen peroxide; imidazoline; protein adducts; sulfenic acid
- James, Joyce P.,Quistad, Gary B.,Casida, John E.
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p. 2530 - 2535
(2007/10/03)
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- OXIDATION OF 2-MERCAPTOBENZOHETERAZOLES BY DIMETHYLDIOXIRANE. A NEW METHOD FOR A SYNTHESIS OF C-2 SUBSTITUTED BENZIMIDAZOLE, BENZOXAZOLE, AND BENZOTHIAZOLE DERIVATIVES
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New and efficient reactions in which 2-mercaptobenzoheterazoles are selectively converted by dimethyldioxirane, under mild experimental conditions, to several C-2 substituted benzoimidazole, benzoxazole, and benzothiazole derivatives are reported.
- Frachey, Giuseppe,Crestini, Claudia,Bernini, Roberta,Saladino, Raffaele,Mincione, Enrico
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p. 2621 - 2630
(2007/10/02)
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- Imidazoline derivative
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Imidazoline derivative of the formula: STR1 wherein R is a halogenophenyl group or a pyridyl group and X1 and X2 are a hydrogen atom or a lower alkoxy group, or a pharmaceutically acceptable salt thereof, which is useful as an immunomodulator and as an agent for the treatment and/or prophylaxis of rheumathoid arthritis, multiple sclerosis, systemic lupus erythemathodes, rheumatic fever and the like, a process for the preparation thereof, and a pharmaceutical composition containing said compound as an active ingredient.
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- Production of 1-aminoethyl-imidazoles via the hydrolysis of 1-acylaminoethylimidazoles
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An imidazole compound represented by the general formula STR1 wherein R is an alkyl group having up to 17 carbon atoms or a phenyl group. This imidazole compound is useful as a curing agent or curing accelerator for epoxy resins.
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- Process for the production of low-viscosity amphoteric surfactants
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Low viscosity amphoteric surfactants are prepared by quaternization of low diamine content imidazolines by a process in which certain addition and temperature parameters are strictly observed. Imidazolines suitable as a starting material may be obtained by heating fatty acids and aminoethanolamine in an inert solvent until water is eliminated, removing the water formed from the reaction mixture by azeotropic distillation and, finally, distilling off the solvent and the residual amine.
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- Method of inhibiting sickling of sickle erythrocytes
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Method for inhibiting the sickling of sickle erythrocytes in blood by contacting the sickle erythrocytes with a compound of the formula: STR1 or a pharmaceutically-acceptable salt thereof wherein X represents sulfur, oxygen or imino; and Rm and Rp each independently represent hydrogen, cyano, nitro, alkylthio, alkylsulfinyl, alkylsulfonyl, alkyl or trifluoromethyl.
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- Compounds containing sulfur and amino groups
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This invention relates to the following: (1) An amino-containing composition characterized by polymercapto groups, (2) A polyamino-containing composition characterized by mercapto or polymercapto groups, (3) A composition characterized by the presence of A. a mercapto or polymercapto groups, and B. a nitrogen-containing group characterized by at least one of the following: 1. an amido or a polyamido group, 2. a cyclic amidine or a polycyclic amidine group, 3. an epihalohydrin-derived amino-containing group. This invention also relates to the use of the above compositions as corrosion inhibitors.
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- Processes for the preparation of tetramisole
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Processes for reacting aryl vinyl compounds, nitriles, and halogens to provide imidoyl halides; processes for preparing amidine hydrohalides from the imidoyl compounds; processes for producing novel imidazolines from the amidine hydrohalides; processes for preparing novel amidoamines from the imidazolines; processes for preparing novel diamines from the amidoamines, together with novel nitrogen-containing products so produced, such products being useful for the production of various imidazothiazoles including tetramisole.
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- CARBONYLATION OF AMINES AND DIAMINES CATALYZED BY NICKEL CARBONYL
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The carbonylation of amines and diamines was carried out using nickel carbonyl as the catalyst. reaction of butylamine, diethylamine, and diphenylamine with carbon monoxide all lead exclusively to the corresponding formamide derivative.Benzylamine reacts with carbon monoxide to yield urea and 1,2-diphenylethane.Diamines such as ethylenediamine, 1,2-diaminopropane, and 1,3-propylenediamine react to yield a cyclic condensation product, a cyclic uren, and a carbamic acid.
- Martin, Wilbur E.,Farona, Michael F.
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p. 393 - 397
(2007/10/02)
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- Parabanic acid aminals
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Parabanic acid aminals of the formula STR1 wherein R1 is STR2 wherein Z is selected from the group consisting of an aliphatic radical having 1-20 carbon atoms, an aromatic radical having 6-14 carbon atoms and an aliphatic-aromatic radical having 7-20 carbon atoms; R2 and R3 may be the same or different and each is selected from the group consisting of hydrogen, an aliphatic radical having 1-20 carbon atoms, an aromatic radical having 6-14 carbon atoms and an aliphatic-aromatic having 7-20 carbon atoms; R4 is hydrogen or STR3 with Z being as defined above; and R5 is the same as Z.
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