Patents by Inventor Jordi Frigola-Constansa

Jordi Frigola-Constansa has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5849931
    Abstract: A method for predominantly preparing the enantiomer (R)-(+)-5-(phenyl)hydroxymethyl-1-methyl-1H-pyrazole, (R)-(+)-1, by separating the racemate (+)-5-(phenyl)hydroxymethyl-1-methyl-1H-pyrazole of formula (1), comprising the series of steps of using a lipase or material derived therefrom having enzymatic activity in a transesterification reaction, as well as hydrolysing the resulting ester, (S)-(-)-5-(phenyl)alkylcarbonyloxymethyl-1-methyl-1H-pyrazole, of formula (S)-(-)-4, wherein R.sub.1 is a methyl or ethyl radical.
    Type: Grant
    Filed: August 5, 1997
    Date of Patent: December 15, 1998
    Assignee: Laboratorios Del Dr. Esteve S.A.
    Inventors: Jordi Frigola-Constansa, Juana Maria Berrocal Romero, Maria Rosa Cuberes Altisent, Vicente Gotor Santamaria
  • Patent number: 5731331
    Abstract: The present invention relates to the compounds of general formula ##STR1## used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 24, 1998
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa
  • Patent number: 5641781
    Abstract: The present invention relates to a topical ophthalmic composition comprising at least one compound of general formula I ##STR1## in which n may have the values 0 or 1,m may have the values 2 or 3,and Het represents a heteroaromatic radical of formula ##STR2## in which X, Y, Z and W, which may be the same or different, represent a nitrogen atom or a carbon atom linked to a hydrogen atom, a halogen atom, a methyl radical, an ethyl carboxylate radical, a carboxylic radical or a sulphonic radical, and the pharmaceutically acceptable salts thereof, combined with an ophthalmically acceptable vehicle, in particular for the treatment of allergic conjunctivitis.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: June 24, 1997
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Maria Rosa Cuberes-Altisent, Jordi Frigola-Constansa
  • Patent number: 5536836
    Abstract: The present invention relates to a process for the preparation of 2-{4-[4-(4-chloro-1-pyrazolyl)buty1]-1-piperazinyl}pyrimidine (Lesopitron) of formula I: ##STR1## characterized in that the reaction between 2-(1-piperazinyl)pyrimidine, 4-chloropyrazole and the carbon chain of formula (III) ##STR2## in which X and Y, which may be identical or different, represent a suitable leaving group, is carried out in a single step in a suitable solvent.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: July 16, 1996
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa
  • Patent number: 5532234
    Abstract: The present invention relates to the use of 1-{4-[4-aryl(or heteroaryl)-1-piperazinyl]butyl}-1H-azole derivatives and of their physiologically acceptable salts for the manufacture of medicaments intended for the treatment of disorders associated with gastric secretion.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: July 2, 1996
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Jordi Frigola-Constansa, Ramon Merce-Vidal
  • Patent number: 5444059
    Abstract: 2-[4-(4-azolylbutyl)-1-piperazinyl]-pyrimidine derivatives characterized in that they correspond to the general formula I ##STR1## in which X.sub.2 represents a nitrogen atom or a C-R.sub.2 group, X.sub.4 represents a nitrogen atom or a C-R.sub.4 group, X.sub.5 represents a nitrogen atom or a C-R.sub.5 group, the process for preparing them, their application as medicinal product, and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: August 22, 1995
    Assignee: Laboratorios Del. Dr. Esteve, S.A.
    Inventors: Jordi Frigola-Constansa, Ramon Merce-Vidal
  • Patent number: 5382586
    Abstract: The present invention relates to heterocyclic compounds, characterized in that they have the general formula I ##STR1## wherein Ar, n, and Z.sub.1 and Z.sub.6 are defined in the specification, are disclosed to have pharmaceutical activity on the central nervous system.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: January 17, 1995
    Assignee: Laboratorios del Dr. Esteve S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5292739
    Abstract: The present invention relates to heterocyclic compounds, characterized in that they have the general formula I ##STR1## Wherein Ar, n and Z.sub.1 -Z.sub.6 are defined in the specification, are disclosed to have pharmaceutical activity on the central nervous system.
    Type: Grant
    Filed: January 27, 1992
    Date of Patent: March 8, 1994
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5227486
    Abstract: The present invention relates to a process for the preparation of aryl (or heteroaryl) piperazinyl-butylazole derivatives corresponding to the general formula I ##STR1## in which Ar denotes a nitrogenous or other aromatic radical chosen from differently substituted aryls, differently substituted 2-pyrimidine, 2-N-methyl-imidazole and 3-(1,2-benzisothiazole)Z.sub.1 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.1Z.sub.2 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.2Z.sub.4 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.4 and R.sub.1, R.sub.2, R.sub.3 and R.sub.
    Type: Grant
    Filed: March 6, 1992
    Date of Patent: July 13, 1993
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5214040
    Abstract: The present invention relates to novel benzimidazole derivatives characterized in that they are of the general formula I, and their therapeutically acceptable salts, ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent a hydrogen or a halogen atom, a lower alkyl radical, a hydroxyl radical, an alkoxy radical, an alkyl carboxylate radical, or an aryl or substituted aryl radical,n may take the values 0 or 1,m may take the values 2 to 4,X, Y, Z and W, which are identical or different, and which may even form part of another aromatic or nonaromatic ring, represent a nitrogen atom or a carbon atom linked to a hydrogen or to a halogen atom, or to another alkyl, aryl, carboxyalkyl, carboxylic, hydroxyl, alkyl hydroxyl, sulphonic or alkylsulphonic radical.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: May 25, 1993
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5182280
    Abstract: The present invention relates to novel compounds derived from benzimidazole, characterized in that they correspond to the formula I, or their therapeutically acceptable salts, ##STR1## in which: R.sub.1 and R.sub.2, equal or different, represent a hydrogen atom, a halogen, a lower alkyl radical, a hydroxy radical, an alkoxy radical, an alkyl carboxylate radical, an aryl or substituted aryl radical,n may have the values 0 or 1,m may have the values 2 to 4,X, Y, Z and W, equal or different, represents a nitrogen atom or a carbon atom bonded to a hydrogen atom, a halogen or another alkyl, aryl, alkoxycarbonyl, carboxy, hydroxyl, sulfonic and alkylsulfonic radical. The present invention relates also to the treatment of various allergic disorders caused by histamine.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: January 26, 1993
    Assignee: Laboratorios Del Dr. Esteve, S. A.
    Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5182281
    Abstract: The present invention relates to the use of the derivatives of general formula I ##STR1## in which: n can have values 1 to 6, andR represents a hydrogen atom, a halogen, a C.sub.1 to C.sub.4 lower alkyl radical, a heteroaryl radical, a sulpho radical, an N-substituted or N,N-disubstituted sulphamoyl radical, a nitro radical, a hydroxyl radical, an oxo radical, a C.sub.1 to C.sub.4 lower alkoxy radical, a cyano radical, a C.sub.1 to C.sub.4 lower alkylcarboxylate radical, an aryl or substituted aryl radical, or an amino or substituted amino radical of formula ##STR2## in which R.sub.1 and R.sub.
    Type: Grant
    Filed: January 24, 1992
    Date of Patent: January 26, 1993
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5166205
    Abstract: The present invention relates to novel derivatives of 1-diphenylmethyl piperazinyl, characterized in that they correspond to the general formula I, and their therapeutically acceptable salts, ##STR1## in which: R.sub.1 and R.sub.2, equal or different, represent a hydrogen atom, a halogen, a lower alkyl radical, a hydroxy radical, an alkoxy radical, an alkyl carboxylate radical, an aryl or substituted aryl radical,n may have the values 2 to 4,X, Y, Z and W, equal or different, represent a nitrogen atom or a carbon atom linked to a hydrogen atom, a halogen or to another alkyl, aryl, carboxyalkyl, carbonyl, hydroxyl, sulfonyl and alkylsulfonyl radical.The present invention also relates to the process of preparing these compounds and their use for the manufacture of medicaments intended for prophylaxis and for the treatment of various allergic disorders caused by histamine.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: November 24, 1992
    Assignee: Laboratorios Del Dr. Esteve, S. A.
    Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5162323
    Abstract: The present invention relates to the use of the derivatives of general formula I ##STR1## in which: n can have the values 1 to 6, andR represents a hydrogen atom, a halogen, a C.sub.1 to C.sub.4 lower alkyl radical, a nitro radical, a hydroxyl radical, an oxo radical, a C.sub.1 to C.sub.4 lower alkoxy radical, a cyano radical, a C.sub.1 to C.sub.4 lower alkyl carboxylate radical, an aryl or substituted aryl radical, or an amino or substituted amino radical of formula ##STR2## in which R.sub.1 and R.sub.2, which may be identical or different, represent a hydrogen atom, an alkyl radical, an aryl radical, an alkylcarboxy radical, an arylcarboxy radical, an alkylsulphonyl radical or an arylsulphonyl radical, the alkyl fragments of these radicals containing from 1 to 4 carbon atomsfor the manufacture of medicinal products intended for the treatment of disorders associated with the withdrawal syndrome induced by the discontinuation of benzodiazepines such as diazepam, cocaine, alcohol and/or nicotine.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: November 10, 1992
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 4797483
    Abstract: A process for obtaining 4-hydroxy-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, which may be used as a non-steroidal analgesic and anti-inflammatory drug. The process comprises reacting saccharin sodium with isopropyl chloroacetate in dimethylformamide, reacting the resultant isopropyl 3-oxo-1,2-benzoisothiazoline-2-acetate 1,1-dioxide with sodium isopropylate in isopropanol to produce an intermediate which, when methylated in an aqueous-alcoholic basic medium with dimethyl sulfate, gives an intermediate compound which when condensed with 2-aminopyridine in xylene, yields 4-hydroxy-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazone-3-carboxamide 1,1-dioxide.
    Type: Grant
    Filed: June 24, 1987
    Date of Patent: January 10, 1989
    Assignee: Induspol, S.A.
    Inventors: Jordi Frigola Constansa, Jose M. Ribalta Baro, Julio Campon Pardo