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).

  • Publication number: 20040067941
    Abstract: The present invention relates to new compounds of general formula (I), as well as to their physiologically acceptable salts, the procedures for their preparation, the intermediate compounds for obtaining them, the application of the compounds of general formula (I) as medicaments in the prevention and treatment of disorders of the Central nervous System and to the pharmaceutical compositions containing them.
    Type: Application
    Filed: April 8, 2003
    Publication date: April 8, 2004
    Inventors: Antonio Torrens-Jover, Jose Aurelio Castrillo-Perez, Jordi Frigola-Constansa
  • Publication number: 20040058920
    Abstract: The present invention relates to Benzoxazinone-derived compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.
    Type: Application
    Filed: April 4, 2003
    Publication date: March 25, 2004
    Inventors: Antoni Torrens Jover, Jose Aurelio Castrillo Perez, Jordi Frigola Constansa, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
  • Publication number: 20040048872
    Abstract: New derivatives of cyanoaryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines (I), where R1 represents an OR3 radical, where R3 represents a radical derived from a saturated hydrocarbon, with a linear or branched chain of 1 to 4 carbon atoms, and R2 represents a phenyl radical substituted at least by one cyan radical (—C≡N), or a radical of a heteroaromatic ring of 5 or 6 members substituted at least by one cyan radical (—C≡N); and their physiologically acceptable salts, are useful for application in human and/or veterinary therapeutics as sedatives, anticonvulsants, hypnotics and general anaesthetics.
    Type: Application
    Filed: December 17, 2002
    Publication date: March 11, 2004
    Inventors: Jordi Corbera- Arjona, David Vano-Domenech, Jordi Frigola-Constansa
  • Publication number: 20040034082
    Abstract: Derivatives of pyrazoline (I), wherein R1 is hydrogen, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, carboxylic acid, alkyl carboxylate with 1 to 4 carbon atoms, carboxamide or cyano, R1 is hydrogen or methyl, R3, R4, R7 and R8, independently are hydrogen, chlorine, fluorine, methyl, trifluoromethyl or methoxy, R5 and R6, independently, are hydrogen, chlorine, fluorine, methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl, aminosulphonyl or acetylaminosulphonyl, with the condition that one of the substituents R5 or R6 is a methylsulphonyl, aminosulphonyl or acetylaminosulphonyl group, and with the condition that when R1 is methyl, then R2 is hydrogen or methyl, R3 and R8, independently are hydrogen, chlorine, fluorine, methyl, or trifluoromethyl, R4 is hydrogen, fluorine, methyl, trifluoromethyl or methoxy, R5 is fluorine, trifluoromethyl, trifluoromethoxy, methylsulphonyl, aminosulphonyl or acetylaminosulphonyl, R6 is hydrogen, chlorine, fluorine, methyl, trifluoromethyl, methoxy, tri
    Type: Application
    Filed: December 17, 2002
    Publication date: February 19, 2004
    Inventors: Maria Rosa Cuberes-Altisen, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-Llobet, Jordi Frigola-Constansa
  • Publication number: 20040019222
    Abstract: Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomerically pure compounds (−)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and,
    Type: Application
    Filed: December 17, 2002
    Publication date: January 29, 2004
    Inventors: Montserrat Alcon- Marrugat, Miguel Angel Pericas-Brondo, Maria Rosa Cuberes-Altisen, Jordi Frigola-Constansa
  • Publication number: 20030191124
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them 1
    Type: Application
    Filed: November 13, 2002
    Publication date: October 9, 2003
    Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 6518295
    Abstract: The present invention relates to the use of derivatives of aryl (or heteroaryl) azolylcarbinols of general formula (1) of the specification, as well as their physiologically acceptable salts, in the manufacture of medicaments, useful in human and/or veterinary therapy, for the treatment of disorders that are mediated by an excess of substance P, and especially disorders of the central nervous system such as anxiety, depression, schizophrenia, manic depressive psychosis, sexual dysfunction, drug addiction, cognitive disorders, and locomotive disorders.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: February 11, 2003
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Jordi Frigola-Constansa
  • Publication number: 20030022925
    Abstract: Derivatives of aryl(or heteroaryl)azolylcarbinoles of general formula (I), in which Ar represents a phenyl radical or a thienyl radical, optionally substituted, R1 represents a hydrogen atom or a lower alkyl group, R2 represents a dialkylaminoalkyl or azaheterocylclylalkyl and Het represents an azole unsubstituted or optionally substituted by one or two substituents, and their physiologically acceptable salts; are useful as drugs in human and/or veterinary therapeutics to treat urinary incontinence in mammals, including man.
    Type: Application
    Filed: July 3, 2002
    Publication date: January 30, 2003
    Applicant: Laboratorios del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Publication number: 20020188017
    Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.
    Type: Application
    Filed: May 6, 2002
    Publication date: December 12, 2002
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 6410582
    Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: June 25, 2002
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 6384055
    Abstract: Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R1, R2 and R3, which are similar or different, represent each of them hydrogen, halogen, alkyl C1-C4, trifluoromethyl, hydroxyl, alkoxyl, or two adjacent radicals can form a ring; A is a C atom and the dotted line represents an additional bond, or A is a C atom joined to a hydroxyl group and the dotted line represents absence of additional bond; Z1 is N or CR4; Z2 is N or CR5; Z4 is N or CR7; and R4, R5, R6 and R7, which different, represent hydrogen, halogen, alkyl C1-C4, aryl or substituted aryl, or two adjacent radicals can form part of another ring. These derivatives are useful for the treatment of acute pain, neuropathic pain or nociceptive pain in mammals, including human beings.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: May 7, 2002
    Assignee: Laboratorios Del Dr. Esteves, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa
  • Patent number: 6372746
    Abstract: The derivatives of acyl-piperazinyl-pyrimidines of general formula (I), where X is O or S; R1 is alkoxy or trifluoromethyl; R2 is alkyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, show activity in the central nervous system. Compounds of general formula (I) in which X is O can be obtained by reacting a derivative of pyrimidine with a derivative of piperazine or by reacting a derivative of piperazinyl-pyrimidine with a carboxylic acid or a salt or derivative thereof. Compounds of general formula (I) in which X is S can be obtained by reacting (I) in which X is O with Lawesson's reagent or with phosphorous pentasulphide.
    Type: Grant
    Filed: February 24, 2000
    Date of Patent: April 16, 2002
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Jordi Corbera-Arjona, David Vaño-Domenech, Jordi Frigola-Constansa
  • Patent number: 6355659
    Abstract: Antipsychotic compound 4-(4-chlorophenyl)-1,2,3,6-tetrahydro-1-[4-(1H-1,2,4-triazol-1-yl) butyl]pyridine, or one of its physiologically acceptable salts, pharmaceutical compositions containing those compounds and a method of treating a disease selected from psychosis and dementias in which a deficit of cognition predominates comprising administering to a patient in need of such treatment a therapeutically effective amount of the antipsychotic compound.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: March 12, 2002
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Blas Andaluz-Mataró, Josep Mas-Prió
  • Patent number: 6353117
    Abstract: The present invention relates to new pyazoline derivatives of formula and to physiologically acceptable salts thereof, to the method for their preparation and to their application as medicaments.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: March 5, 2002
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: María Rosa Cuberes-Altisent, Juana María Berrocal-Romero, María Montserrat Contijoch-Llobet, Jordi Frigola-Constansa
  • Patent number: 6346620
    Abstract: Methods for preparing 2-(4-(4-(4,5-dichloro-2-methylimidazol-1yl)butyl)-1-piperazinyl)-5-fluoropyrimidine and its physiologically acceptable salts are disclosed.
    Type: Grant
    Filed: March 27, 2001
    Date of Patent: February 12, 2002
    Assignee: Laboratories del Dr. Esteve S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa
  • Patent number: 6303608
    Abstract: 2-{4-[4-(4,5-dichloro-2-methylimidazol-1-yl)butyl]-1-piperazinyl}-5-fluoropyrimidine, and its physiologically acceptable salts; pharmaceutical compositions containing these compounds, and a method of treating vertigo, travel sickness, nausea, depression, anxiety, gastric acid secretion, obsessive/compulsive disorders, panic attacks or sleep apnea using these compounds are disclosed.
    Type: Grant
    Filed: February 29, 2000
    Date of Patent: October 16, 2001
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa
  • Patent number: 6232329
    Abstract: The present invention relates to the compounds of general formula 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: February 26, 1998
    Date of Patent: May 15, 2001
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa
  • Patent number: 6187930
    Abstract: The procedure comprises reacting the mixture that comprises 2-[phenyl(1-methyl-1 H-pyrazole-5-yl)methoxy]-N,N-dimethylethanamine (I) with an enantiomer of an optically active acid to form a diastereoisomeric salt, separating said salt and liberating the enantiomer of said compound (I). The dextrorotatory enantiomer of (I) can be obtained by reacting a racemic mixture or non-racemic mixture of (I) with (+)-ditoluyl-L-tartaric acid, optionally mixed with p-toluensulphonic acid. Compound (I) has analgesic properties and its most active enantiomer is dextrorotatory.
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: February 13, 2001
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens-Jover, Jordi Frigola-Constansa
  • Patent number: 6118009
    Abstract: The procedure comprises (a) the enantioselective reduction of a pro-chiral ketone (III) by using a reducing and agent and chiral catalyst, both boron derivatives, in an anhydrous solvent or mixture of anhydrous solvents to form an enantiomer of an alcohol (II), and (b), the alkylation of (II), in phase transfer conditions, with optionally prior isolation and purification thereof, with 2-chloro-N,N-dimethylethylamine, to form an enantiomer of (I). Cyzolirtine exhibits analgesic properties.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: September 12, 2000
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens-Jover, Jordi Frigola-Constansa
  • Patent number: 5872125
    Abstract: It comprises the new polymorphs I and II of Lesopitron dihydrochloride, characterized by their infrared spectra and their X-ray diffraction patterns. They are obtained by crystallization of Lesopitron dihydrochloride. It also comprises the forms I-hydrate and II-hydrate, which are obtained from the corresponding polymorphs, which have a water content from 3 to 6% and from 1.5 to 2.5%, respectively. These products are used in human medicine mainly due to their pharmacological activity over the central nervous system.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: February 16, 1999
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Pilar Lupon-Roses, Jaime Tomas-Navarro, Salvador Puig-Torres, Jordi Frigola-Constansa