Patents Assigned to Istituto de Angeli S.p.A.
  • Patent number: 5164386
    Abstract: Pharmacologically active R(-) 3-quinuclidinol derivatives are described which are muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula (I) ##STR1## wherein R represents a linear or branched lower alkyl group, a cycloalkyl-C.sub.1-2 alkyl or an aralkyl group, or it is absent;X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;R.sub.1 represents H, a linear or branched lower alkyl group or an acyl group of the type R.sub.2 --CO, in which R.sub.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: November 17, 1992
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Enzo Cereda, Giuseppe Bietti, Giovanni B. Schiavi, Arturo Donetti, Antonio Schiavone, Henri N. Doods
  • Patent number: 5106851
    Abstract: Compounds of the formula (I) ##STR1## wherein R represents H or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 represent H, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkythio, C.sub.1-6 alkoxycarbonyl, carboxyl, hydroxy, nitro, cyano, optionally C.sub.1-4 alkyl mono- or disubstituted carbamoyl, optionally C.sub.1-4 alkyl mono- or disubstituted amino, C.sub.1-6 acylamino, C.sub.1-4 alkoxy carbonylamino, C.sub.1-6 alkylsulphynyl, C.sub.1-6 alkylsulphonyl or C.sub.1-6 acyl;R.sub.3 represents H, C.sub.1-6 alkyl, aryl or aralkyl, or it may be absent;A represents CO or C.dbd.S;E represents nitrogen;D represents CO or CR.sub.4 R.sub.5 when the E--D bond is single, or D is C--R when the D--E bond is double, in which R.sub.4 represents H, C.sub.1-6 alkyl, aryl, aralkyl, hydroxy or C.sub.1-4 alkoxy and R.sub.5 represents H;X represents oxygen or N--R, or it is absent;Y represents a basic group selected from: ##STR2## in which n is 2 or 3; p is 0 or 1 at the same time or not; q is 0,2 or 3; R.sub.6 and R.sub.
    Type: Grant
    Filed: February 2, 1990
    Date of Patent: April 21, 1992
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Marco Turconi, Rosamarie Micheletti, Giovanni B. Schiavi, Arturo Donetti, Angelo Sagrada, Henri N. Doods
  • Patent number: 5047410
    Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: September 10, 1991
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
  • Patent number: 4699915
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or methyl;R.sub.1 is straight or branched alkyl of 1 to 6 carbon atoms, hydroxy(alkyl of 1 to 6 carbon atoms), mono- or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 cabon atoms)thio(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R.sub.2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andX is pyrazol-3-yl, 1,2,4-triazol-3-yl, pyridin-2-yl, pyridin-3-yl, thiazol-4-yl, 2-methyl-thiazol-4-yl or 2-methylamino-thiazol-4-yl;tautomers thereof, and non-toxic, pharmacologiically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics and gastric acid secretion inhibitors.
    Type: Grant
    Filed: July 2, 1985
    Date of Patent: October 13, 1987
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Enzo Cereda, Giuseppe Bietti, Arturo Donetti, Piero del Soldato, Antonio Giachetti, Ferdinando Pagani
  • Patent number: 4666932
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or methyl;R.sub.1 is straight or branched alkyl of 1 to 6 carbon atoms, dimethyldioxolylmethyl, hydroxymethyldioxolylmethyl, hydroxy(alkyl of 1 to 6 carbon atoms), mono- or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 carbon atoms)thio- (alkyl of 1 to 6 carbon atoms), (alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms)thio-(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), di-lower alkyl-amino(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R.sub.2 and R.sub.3 are each independently hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andZ is imidazol-2-yl or imidazol-4-yl;provided however that, when R.sub.1 is straight or branched alkyl, alkenyl, alkynyl, cycloalkyl or cyano and R, R.sub.2 and R.sub.3 are hydrogen, Z is other than imidazol-4-yl; tautomers thereof and non-toxic, pharmacologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: July 2, 1985
    Date of Patent: May 19, 1987
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Enzo Cereda, Giuseppe Bietti, Arturo Donetti, Piero del Soldato, Antonio Giachetti, Ferdinando Pagani
  • Patent number: 4649150
    Abstract: Compounds of the formula ##STR1## wherein R represents substituents of various types;R.sub.1 and R.sub.2 are each independently hydrogen or lower alkyl;R.sub.3 represents substituents of various types; andR.sub.4 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halogen, cyano or carbamoyl;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics.
    Type: Grant
    Filed: May 16, 1984
    Date of Patent: March 10, 1987
    Assignee: Istituto de Angeli, S.p.A.
    Inventors: Giuseppe Bietti, Enzo Cereda, Arturo Donetti, Antonio Giachetti, Ferdinando Pagani
  • Patent number: 4645841
    Abstract: Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: February 24, 1987
    Assignee: Istituto de Angeli, S.p.A.
    Inventors: Giuseppe Bietti, Enzo Cereda, Arturo Donetti, Piero Del Soldato, Antonio Giachetti, Rosamaria Micheletti
  • Patent number: 4643993
    Abstract: Compounds of the formula ##STR1## wherein Het is a heterocycle containing 2 to 3 nitrogen atoms;R is hydrogen, lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen;Y is --SO.sub.3 H or ##STR2## R" is alkyl of 1 to 3 carbon atoms; and R' is straight or branched alkyl which may contain a heteroatom such as sulfur, oxygen or nitrogen; straight or branched alkenyl; cycloalkyl; alkyl-cycloalkyl; aryl; or aralkyl optionally substituted by lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics and gastric acid secretion inhibitors.
    Type: Grant
    Filed: May 18, 1983
    Date of Patent: February 17, 1987
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Enzo Cereda, Arturo Donetti, Antonio Giachetti, Piero del Soldato
  • Patent number: 4548944
    Abstract: Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms;tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
    Type: Grant
    Filed: February 10, 1983
    Date of Patent: October 22, 1985
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Giuseppe Bietti, Enzo Cereda, Arturo Donetti, Piero del Soldato, Antonio Giachetti, Rosamaria Micheletti
  • Patent number: 4386099
    Abstract: This invention relates to imidazolylphenyl amidines, the preparation thereof, and pharmaceutical compositions containing them. More particularly, this invention relates to compounds of the general formula ##STR1## in which R, R.sub.1, R.sub.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group, and R.sub.2 represents a linear or branched alkyl, alkenyl, or alkynyl group, a cyano group, a hydroxyl group, a substituted or unsubstituted cycloalkyl or cycloaliphatic alkyl group, a bicyclic group, an aralkyl or aryl group optionally substituted by halogen, methyl, methoxy, or methylenedioxy groups, or a substituted or unsubstituted heterocyclylalkyl or heterocyclic group which may also contain a further hetero atom, or a non-toxic, pharmacologically acceptable acid addition salt thereof. These compounds are useful in treating disorders of the gastrointestinal tract.
    Type: Grant
    Filed: November 19, 1981
    Date of Patent: May 31, 1983
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Enzo Cereda, Arturo Donetti, Piero del Soldato, Mario Bergamaschi
  • Patent number: 4301177
    Abstract: The compound of the formula ##STR1## and non-toxic, pharmacologically acceptable salts thereof, which are useful as analgesics, antipyretics and anti-rheumatics.
    Type: Grant
    Filed: March 31, 1980
    Date of Patent: November 17, 1981
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Gianfranco Pala, Enzo Cereda
  • Patent number: 4259253
    Abstract: A novel process for the preparation of pure trans, trans-farnesylacetic acid of the formula ##STR1## by recrystallization of a mixture of alkali metal salts of trans, trans- and cis, trans-farnesylacetic acid from an organic solvent, and conversion of the isolated alkali metal trans, trans-farnesylacetate into the free acid.
    Type: Grant
    Filed: January 28, 1980
    Date of Patent: March 31, 1981
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Arturo Donetti, Enzo Cereda, Elio Bellora
  • Patent number: 3952108
    Abstract: The specification describes quaternary bromides of scopolamine in which the substituent on the nitrogen atom has the formula --(CH.sub.2).sub.n -R in which R represents a cycloalkyl group containing up to six carbon atoms, an alkyl-substituted cycloalkyl group containing up to six carbon atoms or an epoxyethyl group and n is 1 or 2. Such compounds have valuable spasmolytic and anti-ulcer properties and pharmaceutical preparations containing them are also described.
    Type: Grant
    Filed: July 22, 1974
    Date of Patent: April 20, 1976
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Silvano Casadio, Arturo Donetti