Patents by Inventor Aldemio Temperilli
Aldemio Temperilli 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).
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Patent number: 5079364Abstract: t-alkyl eroline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinynoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.Type: GrantFiled: March 24, 1989Date of Patent: January 7, 1992Assignee: Farmitalia Carlo ErbaInventors: Aldemio Temperilli, Enzo Brambilla, Mauro Gobbini, Maria A. Cervini
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Patent number: 4920099Type: GrantFiled: October 29, 1987Date of Patent: April 24, 1990Assignee: Farmitalie Carlo Erba S.p.A.Inventors: Laura Chiodini, Mauro Gobbini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Gabriella Traquandi, Patrizia Ferrari
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Patent number: 4895836Type: GrantFiled: October 29, 1987Date of Patent: January 23, 1990Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Laura Chiodini, Mauro Gobbini, Sergio Mantegani, Daniel Ruggieri, Aldemio Temperilli, Gabriella Traquandi, Patrizia Ferrari
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Patent number: 4882315Type: GrantFiled: October 29, 1987Date of Patent: November 21, 1989Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Laura Chiodini, Mauro Gobbini, Sergio Mantegani, Daniel Ruggieri, Aldemio Temperilli, Gabriella Traquandi, Patrizia Ferrari
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Patent number: 4861793Abstract: Pharmaceutical compounds of the formula ##STR1## wherein R is H or CH.sub.3, R.sub.1 is H or OCH.sub.3, R.sub.2 is a C.sub.1 -C.sub.4 hydrocarbon group and X is an organic group. Also disclosed is a process for the preparation of these compounds. The compounds have dopamine agonist or antagonist activity.Type: GrantFiled: March 31, 1987Date of Patent: August 29, 1989Assignee: Farmitalia Carlo Erba, S.p.AInventors: Luigi Bernardi, Laura Chiodini, Aldemio Temperilli
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Patent number: 4859678Abstract: An ergoline derivative of the formula I: ##STR1## wherein R.sub.1 represents hydrogen or a methyl group; R.sub.2 represents hydrogen or a halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to about 4 carbon atoms; R.sub.3 represents a hydrocarbon group having from 1 to about 4 carbon atoms; R.sub.4 represents hydrogen, a phenyl group or a hydrocarbon group having from 1 to about 4 carbon atoms; wherein either (a) R.sub.6 and R.sub.7 represent a valence bond or hydrogen atoms and R.sub.8 represents a hydrogen atom or a methoxy group, or (b) R.sub.6 represents a hydrogen atom and R.sub.7 and R.sub.8 taken together represent a valence bond; W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.5, CH.dbd.CR.sub.5 or CH.sub.2 CHR.sub.5 wherein R.sub.Type: GrantFiled: June 21, 1988Date of Patent: August 22, 1989Assignee: Farmitalia Carlo ErbaInventors: Sergio Mantegani, Enzo Brambilla, Aldemio Temperilli, Daniela Ruggieri, Patricia Salvati
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Patent number: 4843073Abstract: t-Alkyl ergoline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 =H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.Type: GrantFiled: June 23, 1987Date of Patent: June 27, 1989Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Aldemio Temperilli, Enzo Brambilla, Mauro Gobbini, Maria A. Cervini
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Patent number: 4839363Abstract: Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;R.sub.3 represents a hydrocarbon group having from 1 to 4 carbon atoms;X represents a nitrogen atom and Y represents an oxygen atom, a ##STR2## group wherein R.sub.4 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl or a phenyl group, R.sub.5 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a phenyl, an amino or di(C.sub.1 -C.sub.4 alkyl)amino group and the nitrogen atom of the group ##STR3## is not joined to the nitrogen atom represented by X, or Y represents a nitrogen atom and X represents an oxygen atom or a ##STR4## group wherein R.sub.4 is as above defined; and the pharmaceutically acceptable salt thereof; are useful for treatment of Parkinsonism and dyskinetic symptoms.Type: GrantFiled: January 27, 1988Date of Patent: June 13, 1989Assignee: Farmitalia Carlo ErbaInventors: Enzo Brambilla, Sergio Mantegani, Lorenzo Pegrassi, Alessandro Rossi, Aldemio Temperilli
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Patent number: 4801588Abstract: Compounds of the formula I: ##STR1## wherein R.sub.1 =H, CH.sub.3 ; m=0,1; R.sub.2 =R.sub.3 =H or R.sub.2, R.sub.3 =bond, R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon, n=1 or 2 and their pharmaceutically acceptable salts are antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: July 15, 1987Date of Patent: January 31, 1989Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Aldemio Temperilli, Rosanna Eccel, Enzo Brambilla, Patricia Salvati
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Patent number: 4785001Abstract: Ergoline Esters having the formula (I) ##STR1## in which R.sub.1 =H or CH.sub.3 ; R.sub.2 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.3 =H or OCH.sub.3 ; R.sub.4 =H or halogen; R.sub.5 =C.sub.1 -C.sub.4 alkyl and their pharmaceutically acceptable salts are active at the central nervous system level. A process for their preparation is described.Type: GrantFiled: May 21, 1987Date of Patent: November 15, 1988Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Aldemio Temperilli, Roberto Maj, Sergio Mantegani, Enzo Brambilla
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Patent number: 4746666Abstract: Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 =H,CH.sub.3 ; R.sub.2 =H, halogen, CH.sub.3, CN, C.sub.1 -C.sub.4 alkylthio or phenylthio; R.sub.3 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.4 =H, OCH.sub.3 ; R.sub.5 =H and R.sub.6 =--CH.dbd.CH--CONHR.sub.7 or R.sub.5 and R.sub.6 =.dbd.CH--CONHR.sub.7 ; R.sub.7 =2-thiazolyl, 3-pyridazinyl, 1,3,4-thiadiazol-2-yl or 4-pyrimidinyl group optionally substituted, and pharmaceutically acceptable salts thereof, display activity on the Central Nervous System and are useful as antiprolactinic agents. Their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: June 16, 1986Date of Patent: May 24, 1988Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Luigi Bernardi, Sergio Mantegani, Aldemio Temperilli, Gabriella Traquandi, Alessandro Rossi
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Patent number: 4728649Abstract: The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: January 8, 1986Date of Patent: March 1, 1988Assignee: Farmitalia Carlo ErbaInventors: Sergio Mantegani, Aldemio Temperilli, Gabriella Traquandi, Alessandro Rossi, Lorenzo Pegrassi
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Patent number: 4690929Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.Type: GrantFiled: April 26, 1984Date of Patent: September 1, 1987Assignee: Farmitalia Carlo ErbaInventors: Luigi Bernardi, Laura Chiodini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Patricia Salvati
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Patent number: 4675404Abstract: Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.Type: GrantFiled: July 14, 1986Date of Patent: June 23, 1987Assignee: Farmitala Carlo Erba S.p.A.Inventors: Luigi Bernardi, Aldemio Temperilli, Germano Bosisio, Gabriella Traquandi, Rosanna Eccel, Alessandro Rossi, Patricia Salvati
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Patent number: 4657914Abstract: There are provided ergoline compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl group; R.sub.2 is a hydrogen or halogen atom, a methyl or thiomethyl group; R.sub.3 is a hydrogen atom or a methoxy group; R.sub.4 is a hydrocarbon group having from 1 to 4 carbon atoms; n is 1 or 2; each of R.sub.5 and R.sub.6 independently is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, or a phenyl or hydroxy or alkoxy group having from 1 to 4 carbon atoms, and X is an oxygen atom or a group of the formula NR.sub.7 wherein R.sub.7 is selected from the group consisting of a hydrogen atom, an alkyl having from 1 to 4 carbon atoms and a phenyl group, or a group of the formula N.dbd.C--R.sub.8 wherein the carbon atom is positioned between the nitrogen atoms in the ring and R.sub.8 is an amino, substituted amino, methyl, phenyl, thiomethyl or mercapto group. The compounds have antihypertensive and antiprolactin activity.Type: GrantFiled: April 25, 1983Date of Patent: April 14, 1987Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Luigi Bernardi, Aldemio Temperilli, Sergio Mantegani, Gabriella Traquandi, Patricia Salvati
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Patent number: 4632990Abstract: There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.Type: GrantFiled: April 13, 1983Date of Patent: December 30, 1986Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Luigi Bernardi, Enzo Brambilla, Laura Chiodini, Enrico di Salle, Daniela Ruggieri, Osvaldo Sapini, Aldemio Temperilli
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Patent number: 4526892Abstract: Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.Type: GrantFiled: December 9, 1982Date of Patent: July 2, 1985Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Patricia Salvati, Anna M. Caravaggi, Aldemio Temperilli, Germano Bosisio, Osvaldo Sapini, Enrico di Salle
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Patent number: 4500712Abstract: There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.Type: GrantFiled: November 1, 1982Date of Patent: February 19, 1985Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Luigi Bernardi, Aldemio Temperilli, Daniela Ruggieri, Giuliana Arcari, Patricia Salvati
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Patent number: 4382940Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;X represents an oxygen or sulphur atom or an NH or NCH.sub.3 group;R.sub.3 represents a hydrogen atom, a trifluoromethyl or phenyl group or a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.4 represents a hydrogen atom, a methyl or acetyl group or a hydrocarbon having from 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 together represent a 3- or 4-membered carbon atom chain;Y represents an electron-withdrawing group such as a cyano, nitro, alkylsulphonyl or alkylsulprinyl group or a group of the formula COR.sub.5 wherein R.sub.5 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl, alkoxy, amino or N-substituted amino group or R.sub.5 and R.sub.3 together represent a 2- or 3-membered carbon atom chain;R.sub.6 represents a hydrocarbon group having from 1 to 4 carbon atoms or a benzyl or phenethyl group; andR.sub.Type: GrantFiled: December 1, 1980Date of Patent: May 10, 1983Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Luigi Bernardi, Germano Bosisio, Sergio Mantegani, Alessandro Rossi, Aldemio Temperilli
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Patent number: 4317912Abstract: A compound is disclosed of the formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, or a carboxy, alkoxycarbonyl, piperidinocarbonyl, 1-pyrrolidinylcarbonyl, morpholinocarbonyl, carbamoyl or benzylcarbamoyl group, or an alkylcarbamoyl or dialkylcarbamoyl group in which the, or each, alkyl group has from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen or fluorine atom, or a cyano, acetyl or carbamoyl group; andR.sub.3 represents a hydrogen atom or a methyl group; andrepresents a single or a double bond, with the proviso that R.sub.1 and R.sub.2 do not simultaneously represent hydrogen atoms;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 11, 1980Date of Patent: March 2, 1982Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Aldemio Temperilli, Sergio Mantegani, Giuliana Arcari, Anna M. Caravaggi