4424-20-8Relevant academic research and scientific papers
1,2,4-Triazol-3-yl-thiopropyl-tetrahydrobenzazepines: A series of potent and selective dopamine D3 receptor antagonists
Micheli, Fabrizio,Bonanomi, Giorgio,Blaney, Frank E.,Braggio, Simone,Capelli, Anna Maria,Checchia, Anna,Curcuruto, Ornella,Damiani, Federica,Di Fabio, Romano,Donati, Daniele,Gentile, Gabriella,Gribble, Andy,Hamprecht, Dieter,Tedesco, Giovanna,Terreni, Silvia,Tarsi, Luca,Lightfoot, Andrew,Stemp, Geoff,MacDonald, Gregor,Smith, Alex,Pecoraro, Michela,Petrone, Marcella,Perini, Ornella,Piner, Jacqui,Rossi, Tino,Worby, Angela,Pilla, Maria,Valerio, Enzo,Griffante, Cristiana,Mugnaini, Manolo,Wood, Martyn,Scott, Claire,Andreoli, Michela,Lacroix, Laurent,Schwarz, Adam,Gozzi, Alessandro,Bifone, Angelo,Ashby Jr., Charles R.,Hagan, Jim J.,Heidbreder, Christian
, p. 5076 - 5089 (2007)
The discovery of new highly potent and selective dopamine D3 receptor antagonists has recently permitted characterization of the role of the dopamine D3 receptor in a wide range of preclinical animal models. A novel series of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines demonstrating a high level of D3 affinity and selectivity with an excellent pharmacokinetic profile is reported here. In particular, the pyrazolyl derivative 35 showed good oral bioavailability and brain penetration associated with high potency and selectivity in vitro. In vivo characterization of 35 confirmed that this compound blocks the expression of nicotine- and cocaine-conditioned place preference in the rat, prevents nicotine-triggered reinstatement of nicotine-seeking behavior in the rat, reduces oral operant alcohol self-administration in the mouse, increases extracellular levels of acetylcholine in the rat medial prefrontal cortex, and potentiates the amplitude of the relative cerebral blood volume response to d-amphetamine in a regionally specific manner in the rat brain.
Compound as potassium channel modulator
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Paragraph 0606; 0608; 0613; 0614, (2018/07/30)
The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
HETEROCYCLIC COMPOUNDS AS AXL INHIBITORS
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Paragraph 052; 061, (2016/01/15)
Compounds of Formula I and their uses of effective AXL inhibitors and for the treatment of physical condition mediated by AXL.
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: Hit-to-lead optimization
Fish, Paul V.,Brown, Alan D.,Evrard, Edel,Roberts, Lee R.
scheme or table, p. 1871 - 1875 (2009/12/03)
New 7-sulfonamido-3-benzazepines 3 are disclosed as 5-HT2C receptor agonists. Appropriate substitution of the amino group (R1R2N-) gave compounds that were potent 5-HT2C agonists with minimal activation of the 5-HT2A and 5-HT2B receptors. Furthermore, representative examples had excellent in vitro ADME properties and good selectivity over ion channel activity.
FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND C-MET INHIBITORS
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Page/Page column 259; 315, (2008/12/05)
The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
USE OF ION CHANNEL MODULATORS IN THE PROPHYLAXIS AND TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISEASES
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Page/Page column 39-41, (2010/11/30)
Use of compounds of general formula (1) and pharmacologically acceptable salts and prodrugs thereof:Formula (1) wherein A and B are CH2 or CH2CH2, R1 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl or heteroaralkyl, R2, R3 and R4 are selected from hydrogen, alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl or cyano; X is R5CO, R5SO2, R5R7NCO, R5R7NSO2, R5SO2NR7CO or CO2R8, Y is R6CO, R6SO2, R6R7NCO, R6R7NSO2, R6SO2NR7CO or CO2R8, R5 and R6 are hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl, R7 is hydrogen, alkyl, aryl or aralkyl, and R8 is alkyl, aryl, aralkyl, alkoxyalkyl, heteroaryl or heteroarylalkyl, provided that when X is R5CO or R5SO2, then Y is not R6CO, R6SO2 or R6R7NCO, in the manufacture of a medicament for the prophylaxis or treatment of inflammatory or immunological disease.
Tetrahydrobenzazepines and their use
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Page/Page column 12, (2008/06/13)
The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meaninigs indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical compositon that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond benefically to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.
M3 MUSCARINIC ACETYLCHOLINE RECEPTOR ANTAGONISTS
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Page/Page column 21, (2010/02/14)
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
Tetrahydrobenzazepine derivatives useful as modulators of dopamine d3 receptors (antipsychotic agents)
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, (2008/06/13)
The invention provides compounds of formula (I): wherein: R2 and R3 independently represent various substituents; R1 and R4 independently represent H, F, Cl, Br, Cl1-2alkyl, C1alkoxy, OH, CN, or NO2; B represents a sulfur atom or a —CH2-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof. Preferably, A is selected from one of the groups (i), (ii) or (iii): wherein X1 and X2 are independently N or CR8, and X3 is NR8, O or S; Y1 and Y3 are independently N or CR9, and Y2 is NR9, O or S; Z1 is NR10, O or S, and Z2 and Z3 are independently N or CR10; R8, R9, and R10 are as herein defined, and R7 is H, a halogen atom, OH, cyano, nitro, C1-4alkyl, C1-4alkoxy, C1-4alkylenedioxy, C1-4alkanoyl, or C1-4alkylsulfonyl, an optionally substituted 3-, 4-, 5- or 6-membered cycloalkyl ring, or a group of the formula (a), (b), (c) or (d) as defined by the formulas (a), (b), (c) or (d). The compounds are modulators of dopamine D3 receptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.
Piperadinyl-substituted pyridylalkane, alkene and alkine carboxamides
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, (2008/06/13)
The invention relates to new piperidinyl-substituted pyridyl carboxamides of the general formula (I), wherein the structure element E has meanings (E1) or (E2) and whereby the heterocyclic ring can optionally have a double bond. These substances have especially high cytostatic activities and pronounced immunosuppressive properties which make them suitable for therapeutic treatment in broad tumor spectrum.
