169104-86-3

Relevant academic research and scientific papers

Synergizing combination having an antagonist effect on NKI and NK2 receptors

Synergising associations characterized in that they are comprised of at least one product having an antagonist activity on NK1 receptors and at least one product having an antagonist activity on NK2 receptors. Said associations are useful in the treatment

Perhydroisoindole derivatives as antagonists of substance P

This invention relates to novel perhydroisoindole derivatives of general formula (I), STR1 wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R 1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R 2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R 3 is optionally 2-substituted phenyl; R 4 is OH or fluorine when R 5 is H, or R 4 and R 5 are OH or R 4 and R 5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.

Perhydroisoindole derivatives and pharmaceutical compositions containing them

This invention relates to derivatives of perhydroisoindol of formula: STR1 in which the radicals R are hydrogen atoms or together form a bond, the symbols R' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen atom or an NH radical, R1 is optionally substituted phenyl, or cyclohexadienyl, naphthyl, or heterocyclyl, R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is halogen or OH and R4 is H or halogen if R3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.

Perhydroisoindole derivatives and preparation

This ivention relates to novel perhydroisoindole derivatives having formula (I), STR1 wherein the symbols R, which are the same or different, are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical, R'' is a phenyl radical optionally 2-substituted by a C 1-2 alkylk or alkyloxy radical, R"" is a fluorine atom or a hydroxy radical, and R''"" is a hydrogen atom, or else R'' and R''"" are hydroxy radicals, or R"" and R''"" together form a bond, and R o is a hydrogen atom or a protective radical; salts thereof whereever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.

Isoindolone derivatives, their preparation and the pharmaceutical compositions containing them

This invention relates to isoindolone derivatives of general formula (I) in which the radicals R are hydrogen atoms or together form a bond, the symbols R'' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen or sulphur atom or a radical N--R 3, R 3 being H, optionally substituted alkyl or dialkylamino, R 1 is optionally substituted phenyl or cyclohexadienyl, naphthyl or a heterocycle and R 2 is H, halogen, OH, alkyl, amionoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, carboxyl, optionally substituted alkoxycarbonyl, benzyloxycarbonyl, amino or acylamino, in their (3aR,7aR) forms or in the (3aRS,7aRS) form or their mixtures, and if appropriate their salts where such exist, and their preparation.The new derivatives according to the invention are particularly valuable as antagonists of substance P. STR1

Isoindolone derivatives

New isoindolone derivatives of general formula (I) are STR1 disclosed in which the radicals R represent hydrogen atoms or, together, form a bond, the symbol R' represents a hydrogen atom or a readily removable radical and the symbols R" are identical and