Patents Assigned to Etablissements Nativelle, S.A.
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Patent number: 4716171Abstract: Quinidine derivatives of general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, or an acyl group, and R.sub.2 represents a hydrogen atom, a hydroxy group, an alkoxy group, an acyloxy group or an aroyloxy group, as well as the acid addition salts thereof, useful in therapy, particularly, for the treatment of cardiac arrhythmia.Type: GrantFiled: April 9, 1984Date of Patent: December 29, 1987Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
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Patent number: 4584289Abstract: The present invention relates to new 14-aminosteroids and their application in therapy and also to a process for their preparation.Type: GrantFiled: August 12, 1983Date of Patent: April 22, 1986Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
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Patent number: 4578382Abstract: The invention relates to 4-acylamino-1-azaadamantanes represented by general formula (I): ##STR1## wherein R represents an alkyl group, a substituted alkyl group, an aryl group or a substituted aryl group, useful in particular, for the treatment of cardiovascular diseases.Type: GrantFiled: September 29, 1982Date of Patent: March 25, 1986Assignee: Etablissements Nativelle S.A.Inventors: Francois X. Jarreau, Jean-Jacques Koenig
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Patent number: 4552868Abstract: The invention relates to 14-amino steroid derivatives of formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group with 1 to 4 carbon atoms, R.sub.1 represents a substituted or unsubstituted sugar residue, and R.sub.2 represents a hydrogen atom, a hydroxyl group or an --OR.sub.3 group, wherein R.sub.3 is a substituted or unsubstituted sugar residue; and acid salts thereof useful in the treatment of cardiac incapacity.Type: GrantFiled: August 18, 1983Date of Patent: November 12, 1985Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
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Patent number: 4526895Abstract: The invention relates to new 3-pyridyl-5-alkoxy-pyrazole derivatives of the following formula: ##STR1## wherein R.sub.1 represents a 4-pyridyl, 3-pyridyl or 2-pyridyl group which is unsubstituted or which may be substituted with one or two lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl group; and R.sub.3 represents a lower alkyl group, a phenyl group or an aralkyl group; and the acid addition salts thereof. The derivatives may be prepared by alkylation of a 3-pyridyl-5-pyrazolone. The derivatives are medicinally useful, particularly for the treatment of cardiac deficiency.Type: GrantFiled: July 12, 1983Date of Patent: July 2, 1985Assignee: Etablissements NATIVELLE S.A.Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
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Patent number: 4377689Abstract: The invention relates to new derivatives of spiro compounds represented by the general formula (I) ##STR1## wherein R is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group; R.sub.1 and R.sub.2 represent a hydrogen atom or an alkyl group or together form a nitrogen-containing heterocyclic ring; A is a>CH.sub.2 group or a>CO group; n is 4 or 5. These compounds can be prepared from .beta.-hydroxyacids by intramolecular rearrangement by the action of a strong acid, in order to form a .gamma.-spirolactone which is converted into an .alpha.-carboxy .gamma.-spirolactone to form the compounds of formula (I) using a Mannich reaction. As necessary, a reduction is then carried out. These compounds are useful medically, in particular, as an antidepressant, a stimulant, and a neuroleptic.Type: GrantFiled: October 23, 1981Date of Patent: March 22, 1983Assignee: Etablissements Nativelle S.A.Inventors: Georges Tsatsas, Evan E. Costakis, Georges V. Foscolos
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Patent number: 4371538Abstract: The invention relates to new derivatives of spiro compounds represented by the general formula (I) ##STR1## wherein R is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group; R.sub.1 and R.sub.2 represent a hydrogen atom or an alkyl group or together form a nitrogen-containing heterocyclic ring; A is a >CH.sub.2 group or a >CO group; n is 4 or 5. These compounds can be prepared from .beta.-hydroxyacids by intramolecular rearrangement by the action of a strong acid, in order to form a .gamma.-spirolactone which is converted into an .alpha.-carboxy .gamma.-spirolactone to form the compounds of formula (I) using a Mannich reaction. As necessary, a reduction is then carried out. These compounds are useful medically, in particular, as an antidepressant, a stimulant, and a neuroleptic.Type: GrantFiled: October 9, 1980Date of Patent: February 1, 1983Assignee: Etablissements Nativelle S.A.Inventors: Georges Tsatsas, Evan E. Costakis, Georges V. Foscolos
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Patent number: 4330544Abstract: An aminoalkoxypyrazole of the general formula (I) ##STR1## wherein Ar is a phenyl, benzyl or naphthyl group, or a phenyl group substituted by one or more halogen atoms, or by one or more alkyl, cyano, nitro, hydroxy or alkoxy groups; R.sub.1 is a hydrogen atom or an alkyl group; R.sub.2 and R.sub.3, which may be the same or different, are a hydrogen atom or an alkyl group, or form, with the nitrogen atom to which they are attached, a 5- to 7-membered heterocyclic ring; n is an integer of from 1 to 4; as well as the mineral or organic acid salts thereof. A further embodiment of the invention is the application of the derivatives of the general formula (I) as medications, in particular, for the treatment of depression, polyfunctional disorders, migraines and cardiovascular diseases.Type: GrantFiled: April 1, 1981Date of Patent: May 18, 1982Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xavier Jarreau, Jean J. Koenig
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Patent number: 4325879Abstract: The invention relates to medicinally useful steroid derivatives, particularly amino-14 steroids substituted at the 17-position by a functional group represented by the general formula: ##STR1## wherein R.sub.1 is a hydroxy, hydroxyalkyl, alkoxy, acyloxy, carboxy or carbalkoxy group, or a hydrogen atom, and R.sub.2 is a hydroxy, alkoxy, or acyloxy group. These amino-14 steroids are prepared from the corresponding hydroxy-14 steroids, by the action of hydrazoic acid in the presence of boron trifluoride etherate to form the azido-14 derivative which is reduced.Type: GrantFiled: August 29, 1980Date of Patent: April 20, 1982Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xaver Jarreau, Jean J. Koenig
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Patent number: 4219549Abstract: Aminocardenolides of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.4, R.sub.5, and R.sub.6, which may be the same or different, each represents a hydrogen atom or a hydroxy, alkoxy or acyloxy group; R.sub.3 represents a lower alkyl, hydroxyalkyl, acyloxyalkyl, haloalkyl or ethylenedioxyalkyl group; R.sub.7 represents a hydrogen atom, or an alkyl or acyl group, and R.sub.8 represents a hydrogen atom, an alkyl group or an amino acid residue; a process for preparation of the compounds with the above formula by reaction of an oxo-3 genin with an ammonium salt in the presence of a borocyanohydride in an organic solvent. The aminocardenolides of formula (I) are useful especially for the treatment of cardiac ailments.Type: GrantFiled: January 26, 1979Date of Patent: August 26, 1980Assignee: Etablissements Nativelle S.A.Inventors: Francois X. Jarreau, Jean J. Koenig
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Patent number: 4217280Abstract: Amino-3-cardenolide derivatives represented by the general formula (I) ##STR1## wherein n and m, which may be the same or different, each represents an integer from 0 to 4; R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or a hydroxy, alkoxy or acyloxy group; R.sub.3 represents a lower alkyl, aldehyde, haloalkyl, hydroxyalkyl, acyloxyalkyl, or ethylenedioxyalkyl group; R.sub.7 represents a hydrogen atom or an alkyl group; R.sub.8 represents a hydrogen atom or an alkyl, acyl, alkyloxycarbonyl or aralkoxycarbonyl group; R.sub.9 represents a hydrogen atom or an alkyl group; R.sub.8 and R.sub.9 can combine and form with the nitrogen atom a heterocyclic ring; R.sub.10 represents a hydroxy, alkoxy or aralkoxy group, an amino residue of amino acid or of an oligo-peptide, useful especially for the treatment of cardiac ailments.Type: GrantFiled: January 26, 1979Date of Patent: August 12, 1980Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
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Patent number: 4093619Abstract: Method of oxidizing cinchona alkaloids by reacting specific ketone with cinchona alkaloid in the presence of a strong base and aprotic solvent; following oxidation the oxo compound is reduced to the corresponding stereoisomer.Type: GrantFiled: November 19, 1976Date of Patent: June 6, 1978Assignee: Etablissements Nativelle S.A.Inventors: Francois Xavier Jarreau, Jean-Jacques Koenig
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Patent number: 4060607Abstract: Cardiotonic cardenolide derivatives of the formula ##STR1## wherein n, m, R.sub.1 to R.sub.9 are as hereinafter defined, the mineral or organic salts thereof and a process for their preparation.Type: GrantFiled: May 10, 1976Date of Patent: November 29, 1977Assignee: Etablissements Nativelle S.A.Inventors: Francois-Xavier Jarreau, Roger Gerard Sarfati
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Patent number: 3944563Abstract: 1-AMINO-5-ALKOXY-PYRAZOLE COMPOUNDS OF THE FORMULA: ##EQU1## wherein R.sub.1 represents a lower alkyl group having 1 to 4 carbon atoms, R.sub.2 and R.sub.3, which may be identical or different, represent a hydrogen atom, a lower alkyl group, a phenyl group, a phenyl group substituted by one or more groups selected from lower alkyl, halogen, nitro and lower alkoxy; R.sub.4 represents an amino group, a mono-lower alkyl amino group or a di-lower alkyl amino group; as well as their salts with a mineral or organic acid.A method for the preparation thereof, consisting essentially in internally transforming, in the presence of hydrazine, a 5-hydrazino-isoxazole (or 5-halogenoisoxazole) derivative and alkylating the 5-hydroxy-derivative obtained with a suitable diazoalkane.Type: GrantFiled: March 7, 1975Date of Patent: March 16, 1976Assignee: Etablissements Nativelle, S.A.Inventors: Giorgio Adembri, Piero Tedeschi, Fabio Ponticelli, Maresco Marini