- NOVEL COMPOUNDS FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES
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The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neu
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- A novel polythiophene derivative as a sensitive colorimetric and fluorescent sensor for anionic surfactants in water
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A novel cationic polythiophene derivative, poly[N,N,N-trimethyl-4- (thiophen-3-ylmethylene)cyclohexanaminium chloride] (PTCA-Cl), has been prepared successfully and applied as a colorimetric and fluorometric probe for the detection of anionic surfactants. In particular, a new method for the polymerization of cationic polythiophene derivatives is found, which has not been reported previously. The colorimetric and fluorescent response of PTCA-Cl to anionic surfactants have been investigated by absorption and emission spectroscopy. The sensing interaction can be apparently observed by the naked eye, which presents a great advantage for its practical applications. Moreover, the sensor (PTCA-Cl) shows high selectivity towards anionic surfactants in the presence of other negatively charged analytes, as well as high sensitivity with a detection limit at 10-9 M by using fluorimetry, which is the lowest ever achieved among all synthetic anionic surfactants sensors available. Therefore, the water soluble polythiophene derivative can be applied as a colorimetric and fluorescent probe for the detection of anionic surfactants with high selectivity and sensitivity.
- Wang, Lin,Feng, Qilong,Wang, Xiangyong,Pei, Meishan,Zhang, Guangyou
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scheme or table
p. 1897 - 1901
(2012/10/08)
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- Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors
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A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were determined. In particular, a nitrile substituent at the C5 position of the indole ring gave poten
- Deskus, Jeffrey A.,Epperson, James R.,Sloan, Charles P.,Cipollina, Joseph A.,Dextraze, Pierre,Qian-Cutrone, Jingfang,Gao, Qi,Ma, Baoqing,Beno, Brett R.,Mattson, Gail K.,Molski, Thaddeus F.,Krause, Rudolph G.,Taber, Matthew T.,Lodge, Nicholas J.,Mattson, Ronald J.
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p. 3099 - 3104
(2008/02/13)
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- SUBSTITUTED 1,2,3,4-TETRAHYDRO-2-DIBENZOFURANAMINES AND 2-AMINOCYCLOHEPTA(b)BENZOFURANS
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The invention provides substituted-2-amino-1,2,3,4-tetrahydrodibenzofurans and 2-aminocyclohepta[b]benzo-furans useful as 5-HT1F agonists.
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- Preparation of 8-amido-2-dimethylamino-1,2,3,4-tetrahydro-2-dibenzofurans and several fluorinated derivatives via [3,3]-sigmatropic rearrangement of O-aryloximes
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Methodology to prepare 8-amido-2-amino-1,2,3,4-tetrahydro-2-dibenzofurans, analogues with a fluorine substituent incorporated in the 6-, 7-, and 9-positions, and a difluorinated analogue with fluorines in the 6- and 9-positions is described. The tetrahydrodibenzofuran ring systems are prepared by acid-catalyzed [3,3]-sigmatropic rearrangement of O-aryloximes. Regioselective reactions to prepare the requisite O-aryloxime intermediates from commercially available fluorobenzene derivatives are discussed.
- Guzzo, Peter R.,Buckle, Ronald N.,Chou, Ming,Dinn, Sean R.,Flaugh, Michael E.,Kiefer Jr., Anton D.,Ryter, Kendal T.,Sampognaro, Anthony J.,Tregay, Steven W.,Xu, Yao-Chang
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p. 770 - 778
(2007/10/03)
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- Anilide derivative, production and use thereof
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This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.
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- Quaternary ammonium salts and their use
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This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: wherein R1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is -CH2-, -S- or -O-; and R2, R3 and R4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.
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- METHODS OF TREATING OR AMELIORATING THE SYMPTOMS OF COMMON COLD OR ALLERGIC RHINITIS WITH SEROTONIN 5-HT1F
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This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT 1F agonist.
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- CARBODIIMIDE COUPLING REAGENT
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The present invention relates to compounds used for increasing activation of the 5-HT1F receptor.
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- Use of a serotonin 5-HTlf agonist in the manufacture of a medicament for treating or ameliorating the symptoms of common cold or allergic rhinitis
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This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT1F agonist.
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- Use of serotonin 5-HT1F agonists for the prevention of migraine
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This invention provides methods for the prevention of migraine which comprises administering to a mammal in need thereof a serotonin 5-HT1F agonist.
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- 6-SUBSTITUTED-1,2,3,4-TETRAHYDRO-9H-CARBAZOLES AND 7-SUBSTITUTED-10H-CYCLOHEPTA [7,6-B]INDOLES: NEW 5-HT1F AGONISTS
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This invention provides novel 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta[7,6-b]indoles. These compounds are 5-HT 1F agonists which are useful for the treatment of migraine and associated disorders.
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- Pyrimido[5,4]-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof
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Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[1-methyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine, and 4-[(3-Chloro-4-fluorophenyl)amino]-6-[trans-4-dimethyl-aminocycohexylamino]pyrimido[5,4-d]pyrimidine.
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- 5-SUBSTITUTED-3-(1,2,3,6-TETRAHYDROPYRIDIN-4-YL)-AND 3-(PIPERIDIN-4-YL)-1H-INDOLES: NEW 5-HT1F AGONISTS
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This invention provides novel 5-HT 1F agonists of Formula I STR1 where A--B, R, R 1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
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- Method for preparing aromatic secondary amino compound
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Disclosed are (1) a method for preparing an aromatic secondary amino compound which comprises reacting an N-cyclohexylideneamino compound in the presence of a hydrogen moving catalyst and a hydrogen acceptor by the use of a sulfur-free polar solvent and/or a cocatalyst, and (2) a method for preparing an aromatic secondary amino compound which comprises reacting cyclohexanone or a nucleus-substituted cyclohexanone, an amine and a nitro compound corresponding to the amine in a sulfur-free polar solvent in the presence of a hydrogen moving catalyst, a cocatalyst being added or not added. In a further aspect, a method is provided for the preparation of aminodiphenylamine by reacting phenylenediamine and cyclohexanone in the presence of a hydrogen transfer catalyst in a sulfur-free polar solvent while using nitroaniline as a hydrogen acceptor.
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- 5-HT1F agonists for the treatment of migraine
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This invention provides novel 5-HT1F agonists which are useful for the treatment of migraine and associated disorders.
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- 3--4--and 3--4-piperidinyl-1h-indoles: new 5-HT1F agonists
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This invention provides novel 5-HT1F agonists which are useful for the treatment of migraine and associated disorders having the following formula: STR1 wherein A, B, X, Y, Ar and n are defined in the specification.
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- Method for preparing aromatic secondary amino compound
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Disclosed are (1) a method for preparing an aromatic secondary amino compound which comprises reacting an N-cyclohexylideneamino compound in the presence of a hydrogen moving catalyst and a hydrogen acceptor by the use of a sulfur-free polar solvent and/or a cocatalyst, and (2) a method for preparing an aromatic secondary amino compound which comprises reacting cyclohexanone or a nucleus-substituted cyclohexanone, an amine and a nitro compound corresponding to the amine in a sulfur-free polar solvent in the presence of a hydrogen moving catalyst, a cocatalyst being added or not added.
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- Catalytic Epoxidation of Alkenes with Oxone
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A practical, general and efficient protocol for the catalytic epoxidation of alkenes has been developed.The in situ generation of reactive dioxiranes capable of epoxidizing a variety of alkenes under biphasic conditions has been accomplished using phase transfer catalysts bearing a carbonyl group.Optimal epoxidation conditions employ 10 mol percent of 1-dodecyl-1-methyl-4-oxopiperidinium triflate (8d(+)OTf(-)) in a CH2Cl2/pH 7.5-8.0 biphase using potassium monoperoxosulfate (Oxone) as the oxidant.Optimization of the conditions identified (1) slow addition rate, (2) pH 7.5-8.0, (3) N-dodecyl chain, and (4) the triflate salt as key experimental and structural variables.A selection of nine olefins was successfully oxidized to the corresponding epoxides in 83-96percent yield.
- Denmark, Scott E.,Forbes, David C.,Hays, David S.,DePue, Jeffrey S.,Wilde, Richard G.
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p. 1391 - 1407
(2007/10/02)
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- Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals
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This invention relates to new tetrahydrobenzthiazoles of general formula STR1 wherein R1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms, R2 represents a hydrogen atom or an alkyl group, R3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms, R4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, or R3 and R4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof. The compounds of general formula I above in which one of the groups R1 or R3 or both groups R1 and R3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
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