17910-72-4Relevant academic research and scientific papers
Tricyclic antidepressant derivatives and immunoassay
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, (2008/06/13)
The present invention is directed to novel tricyclic antidepressant drug derivatives synthesized for covalent attachment to proteins or polypeptide antigens for use in the preparation of antibodies or receptors to tricyclic antidepressant drugs and tricyclic antidepressant metabolites. The new derivatives are characterized by a saturated double bond on the amitriptyline portion of the molecule and are represented by the structure where R1is a saturated or unsaturated, substituted or unsubstituted, straight or branched chain of 0-10 carbon or heteroatoms, X is a linker group consisting of 0-2 substituted or unsubstituted aromatic rings, and Y is an activated ester or NH—Z, where Z is a poly(amino acid). The novel tricyclic antidepressant activated hapten derivatives are useful for preparing tracers and conjugates for tricyclic antidepressant immunoassays, including an enzyme immunoassay and a microparticle capture inhibition assay using an antibody produced from the novel immunogen with a conjugate derivatized either at the N-1 position of imipramine or at the C-2 position of dihydroamitriptyline.
Synthesis of 5--10,11-dihydrodibenzocyclohepten-2-yl>oxy>valeric Acid (CHA) and 5-dibenzocyclohepten-2-yl>oxy>valeric Acid (CHE) Handles for the Solid-Phase Synthesis of C-Terminal ...
Noda, Masaki,Yamaguchi, Minoru,Ando, Eiji,Takeda, Kenji,Nokihara, Kiyoshi
, p. 7968 - 7975 (2007/10/02)
Two novel handles for peptide amide preparation under mild conditions were developed for use in highly efficient solid-phase peptide sythesis.These handles, 5--10,11-dihydrodibenzocyclohepten-2-yl>oxy>valeric acid (CHA) and 5-dibenzocyclohepten-2-yl>oxy>valeric acid (CHE), were attached to the solid support and were used for syntheses of peptides having a C-terminal amide by the fluorenylmethoxycarbonyl strategy.The cleavability of CHA and CHE was determined and compared with the that commercially available amide handles.CHA and CHE handles can be rapidly cleaved from the polymer support without significant side reactions using lower acid concentrations than those required for conventional handles.As CHA can be easily synthesized in large amounts, it is suitable for peptide amide preparation for pharmaceuticals.As CHE can be cleaved at very low concentrations of acid, it is especially suitable for preparing side chain-protected peptide amides.Several brain-gut peptides having a C-terminal amide were synthesized in high yield and high purity with these novel handles.
Design of a versatile linker for solid phase peptide synthesis: Synthesis of C-terminal primary/seconary amides and hydrazides
Ramage,Irving,McInnes
, p. 6599 - 6602 (2007/10/02)
An efficient, versatile linker for solid phase peptide synthesis, based upon the dibenzocyclohepta-1,4-diene system, has been developed for the synthesis of C-terminal primary/secondary amides and hydrazides.
New Triazine Derivatives as Potent Modulators of Multidrug Resistance
Dhainaut, Alain,Regnier, Gilbert,Atassi, Ghanem,Pierre, Alain,Leonce, Stephane,et al.
, p. 2481 - 2496 (2007/10/02)
A series of 70 triazine derivatives have been synthesized and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity.Among the 12 selected compounds, 16 (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5μM in DC-3F/AD and KB-A1 cells, respectively) and induced a strong accumulation of adriamycin.The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the P-glycoprotein (Pgp) catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators.In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), 16 (100 mg/kg) increased the T/C by 39percent in mice bearing the resistant tumor cell line P388/VCR.According to these interesting properties, 16 was selected for a clinical development because it is more bioavailable than 34, even though it was less active.
Process for preparing 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-one compounds
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, (2008/06/13)
The present invention relates to a method of preparing 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-one or substitution products thereof from dibenzyl-o-carboxylic acid or its corresponding substitution products, by cyclocondensation. The cyclocondensation is performed in either of two ways, namely (a) with catalytic amounts of a concentrated acid as catalyst, or (b) with the aid of di- and/or trichloromethyl aromatic compounds in the presence of catalysts, preferably catalysts from the group of the Lewis acids.
5-Alkyl or hydroxyalkyl substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines and anticonvulsant use thereof
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, (2008/06/13)
5-Substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anticonvulsants.
