- DNA threading bis(9-aminoacridine-4-carboxamides): Effects of piperidine sidechains on DNA binding, cytotoxicity and cell cycle arrest
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We describe the synthesis of a series of DNA-threading bis(9-aminoacridine-4-carboxamides) comprising ethylpiperidino and N-methylpiperidin-4-yl sidechains, joined via neutral flexible alkyl chains, charged flexible polyamine chains and a semi-rigid charged piperazine linker. Their cytotoxicity towards human leukaemic cells gives IC50 values ranging from 99 to 1100 nM, with the ethylpiperidino series generally being more cytotoxic than the N-methylpiperidin-4-yl series. Measurements with supercoiled DNA indicate that they bisintercalate.
- He, Zhicong,Bu, Xianyong,Eleftheriou, Alexandra,Zihlif, Malik,Qing, Zhang,Stewart, Bernard W.,Wakelin, Laurence P.G.
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Read Online
- Synthesis process of 1-methyl-4-aminopiperidine
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The invention discloses a synthesis process of 1-methyl-4-aminopiperidine. The synthesis proces comprises the following steps: using 1-methyl-4-piperidone as a main raw material and dichloromethane asa solvent, forming Schiff base by ammonia water, and reducing by sodium borohydride to obtain the target compound 1-methyl-4-aminopiperidine. The synthesis proces has the advantages of simple and accessible raw materials, simple technological operation and mild reaction conditions, and is suitable for industrial amplification.
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Paragraph 0015-0016
(2021/02/10)
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- AZACYCLIC COMPOUNDS
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Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.
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Paragraph 0598
(2015/11/09)
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- 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
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Page/Page column 137
(2012/05/20)
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- NAPHTHALENYLOXYPROPENYL DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST HISTONE DEACETYLASE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation
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Page/Page column 36; 167
(2008/12/05)
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- USE OF 4-AMINO-PIPERIDINES FOR TREATING SLEEP DISORDERS
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Inverse agonists and antagonists of serotonin receptors are disclosed for use in treating sleep disorders such as insomnia, and specifically sleep maintenance insomnia. The compound increase slow wave sleep, decrease the number of awakenings after sleep onset, and decrease the time awake after sleep onset.
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Page/Page column 126-127
(2010/11/28)
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- ALKYLCARBAMOYL NAPHTHALENYLOXY- OCTENOYLHYDROXYAMIDE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST HISTONE DEACETYLASE AND PREPARATION THEREOF
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This invention discloses a novel alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide derivative of formula (1) useful for inhibiting the enzyme activity of histone deacetylase, which leads to effective suppression of the cancer cell proliferation, a method for preparing same and a pharmaceutical composition comprising same.
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Page/Page column 22
(2010/11/27)
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- Benzoxazole carboxamides for treating CINV and IBS-D
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Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds that exhibit central activity are useful in treating CINV; those that inhibit peripheral receptors are useful to treat IBS-D.
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Page/Page column 7
(2008/06/13)
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- PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): ; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
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- Isonitrile intermediates for the preparation of tri-substituted imidazole compounds with multiple therapeutic properties
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The invention relates to a novel group of isonitrile compounds and a process for their preparation, useful in the preparation of tri-substituted imadazoles having multiple therapeutic properties.
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- Imine intermediates for the preparation of trisubstituted imidazole compounds with multiple therapeutic properties
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The invention relates to a novel group of iminc compounds and a process for their preparation, useful in the preparation of tri-substituted imadazoles having multiple therapeutic properties.
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- Formamide intermediates for the preparation of tri-substituted imidazole compounds with multiple therapeutic properties
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The invention relates to a novel group of formamide compounds and a process for their preparation, useful in the preparation of tri-substituted imadazoles having multiple therapeutic properties.
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- One-pot, new stereoselective synthesis of endo-tropanamine
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A palladium-catalysed reduction of ketones to primary amines by reaction with ammonium formate in aqueous methanol is described. The proposed method provides a one-pot synthesis of 3-endo-tropanamine in high yields and stereoselectivity.
- Allegretti, Marcello,Berdini, Valerio,Cesta,Curti, Roberto,Nicolini, Luca,Topai, Alessandra
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p. 4257 - 4259
(2007/10/03)
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- Indazole derivatives having monocyclic amine
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An indazole compound having the formula (I): wherein: R1 is hydrogen, C1 -C6 alkyl, C3 -C6 alkenyl or C3 -C6 cycloalkyl; Q is carbonyl, thiocarbonyl or methylene; and R2 is a group of the formula (II) or (IV); STR1 wherein R1 is C1 -C6 alkyl, C3 -C6 alkenyl or benzyl, of which a phenyl group thereof is optionally mono- or di-substituted by the same or different halogen or methoxy; m is 0 to 2; n and o is 1 or 2. The compound exhibits 5-HT4 receptor agonist activity.
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- Synthesis of 1-methyl-4-(N-aroyl)-piperidinamides with anti- inflammatory and analgesic activities
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Two series of 1-methyl-4-(N-aroyl)-piperidinamides were synthesized and evaluated for their anti-inflammatory and analgesic properties, as well as for their gastrointestinal irritation liability. A non-aromatic derivative, 1-methyl-4-(N-cyclohexanoyl)-piperidinamide, was synthesized and evaluated in order to obtain a more exhaustive knowledge of the structure-activity relationship.
- Pau, Amedeo,Boatto, Gianpiero,Cerri, Riccardo,Palagiano, Francesco,Filippelli, Walter,Falcone, Giuseppe,Lampa, Enrico
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p. 233 - 240
(2007/10/03)
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- Imidazole compounds, use and process of making
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Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
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- Compounds
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Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
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- Pyridyl imidazole compounds and compositions
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Novel 1, 4, 5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
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- Synergistine derivatives, their preparation and pharmaceutical compositions containing them
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The invention provides novel synergistine derivatives of the formula: STR1 in which Y=H or N(CH3)2 : and R1 =H and R2 =OH or alkyl optionally substituted by COOH, alkoxycarbonyl or OH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R2 =cycloalkyl (of 3 to 7 carbons) or a heterocycle chosen from azetidine, pyrrolidine, piperidine or azepine (optionally substituted on the nitrogen by alkyl), or R1 =formyl or alkylcarbonyl and R2 =alkyl substituted by COOH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R2 is a heterocycle as defined above, or R1 and R2, which are identical or different, represent alkyl optionally substituted by COOH, alkoxycarbonyl, OH, alkylamino, or dialkylamino of which the alkyl radicals can form a heterocycle, or R1 and R2 form an azetidine, pyrrolidine, piperidine, morpholine or piperazine ring (optionally substituted by alkyl), all the alkyls having 1 to 5 carbon atoms. These compounds are useful as antibacterial agents.
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- SUBSTITUTED THIENOBENZODIAZEPINONES AND SALTS THEREOF
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Compounds of the formula STR1 wherein R is 1-methyl-4-piperididinyl, 4-methyl-1-piperazinyl, or 3-or 3-tropanyl, each of which may optionally have another methyl substituent attached to the heterocyclic ring;R 1 is hydrogen or alkyl of 1 to 4 carbon atoms;R 2 is hydrogen, halogen or alkyl of 1 to 4 carbon atoms; andX is oxygen,--NH--or--N(CH. sub.3)--;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
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