摘要:
This invention relates to a compound of the formula: ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position.a 1-piperazinyl radical substituted in the 4-position.a piperidino radical substituted in the 4-positioneither:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical, and their salts, are useful in therapy for their ability to block serotonin receptors.
摘要:
This invention relates to compounds of formula: ##STR1## in which R.sub.1 denotesa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by an optionally substituted phenyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical,a 1-piperazinyl radical substituted in the 4-position by an optionally substituted phenyl, 1,2-benzisothiazol-3-yl, 1,2-benzisoxazol-3-yl or 2-pyridyl radical,a piperidino radical substituted in the 4-position by an optionally substituted phenyl, bis(4-fluorophenyl)methylene, 4-fluorobenzoyl, optionally substituted 2-oxo-1-benzimidazolinyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, by two phenyl radicals or a hydroxyl radical and an optionally substituted phenyl radicalR.sub.2 denotes a radical SO.sub.2 R.sub.4 in which R.sub.4 denotes an alkyl or phenyl radical,R.sub.3 denotes a phenyl or naphthyl radical,or else R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached form a ring,n is equal to 2, 3 or 4, processes for their preparation and medications containing them.The invention relates to treating a disease ameliorated by serotonin.
摘要:
This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.
摘要:
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.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R.sub.3 is optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.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.
摘要:
This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists. ##STR1##
摘要:
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.sub.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.sup.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.
摘要:
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.sub.2 are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, R.sub.3 is a halogen atom or a hydroxy radical, R.sub.4 is H or halogen if R.sub.3 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.
摘要:
This invention relates to novel derivatives of thiopyranopyrrole of general formula (I): ##STR1## in which R is hydrogen, allyl, or a radical having the structure: --CR.sub.a R.sub.b R.sub.c where R.sub.a and R.sub.b are hydrogen atoms or phenyl radicals optionally substituted (by halogen, alkyl, alkyloxy or nitro), and R.sub.c is defined as R.sub.a and R.sub.b or stands for an alkyl or alkyloxyalkyl radical, at least one of R.sub.a, R.sub.b and R.sub.c being a substituted or unsubstituted phenyl radical, and n is 0 to 2, in their stereoisomer forms, and mixtures thereof, and possibly the salts if they exist, and preparation thereof. The novel derivatives of the invention are particularly interesting as synthesis intermediates.
摘要:
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, R.sub.1 is optionally substituted phenyl, or cyclohexadienyl, naphthyl, or heterocyclyl, R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R.sub.3 is halogen or OH and R.sub.4 is H or halogen if R.sub.3 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.
摘要:
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 represent phenyl radicals which can be substituted with a halogen atom or a methyl radical at the ortho or meta position, in the (3aR, 7aR) form or in the form of a mixture of the (3aRS, 7aRS) forms, as well as their salts.These derivatives are useful as intermediates for the preparation of therapeutically active products.